Entries |
Document | Title | Date |
20080200469 | PHTHALAZINONE DERIVATIVES - Compounds of the formula (I): | 08-21-2008 |
20080221110 | Compounds - Tricyclic nitrogen containing compounds and their use as antibacterials | 09-11-2008 |
20080234278 | Beta-agonists, methods for the preparation thereof and their use as pharmaceutical compositions - The present invention relates to new beta-agonists of general formula (I) | 09-25-2008 |
20080249098 | 3-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide Derivatives, Their Preparation and Therapeutic Use - A subject-matter of the invention is the compounds of general formula (I) | 10-09-2008 |
20080255128 | PHTHALAZINONE DERIVATIVES - A compound of the formula (I): | 10-16-2008 |
20080255129 | 3-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-b]indole-1-acetamide derivatives, their preparation and their application in therapeutics - The invention discloses and claims therapeutic uses of compounds of general formula (I) | 10-16-2008 |
20080261988 | IMIDAZO[1,2-beta]PYRIDAZINE AND PYRAZOLO[1,5-alpha]PYRIMIDINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS - The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II): | 10-23-2008 |
20080280909 | NEW PHENYLALANINE DERIVATIVES - Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning α4 integrin in which α4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection. | 11-13-2008 |
20080280910 | PHTHALAZINONE DERIVATIVES - A compound of the formula (I): | 11-13-2008 |
20080280911 | Cinnoline Compounds as Inhibitors of Phosphodiesterase Type IV (Pde4) - There are provided according to the invention novel compounds of formula (I) | 11-13-2008 |
20080293724 | Methods Using Hydralazine Compounds and Isosorbide Dinitrate or Isosorbide Mononitrate - The invention provides methods for (a) treating decompensated heart failure; (b) treating compensated heart failure; (c) treating renovascular diseases and (d) treating end-stage renal diseases in a patient in need thereof comprising administering an effective amount of (i) at least one hydralazine compound or a pharmaceutically acceptable salt thereof, (ii) isosorbide dinitrate and/or isosorbide mononitrate, and (iii) optionally at least one compound selected from the group consisting of an angiotensin converting enzyme inhibitor, a β-adrenergic antagonist, an angiotensin II antagonist, an aldosterone antagonist, a cardiac glycoside (digitalis) and a diuretic compound or a combination of two or more thereof. The hydralazine compound may be hydralazine hydrochloride. | 11-27-2008 |
20080300250 | ACETYLENYL-PYRAZOLO-PYRIMIDINE DERIVATIVES - The present invention relates to compounds of formula (I): | 12-04-2008 |
20080318960 | PAR2-modulating compounds and their use - The present invention relates to compounds, and uses thereof, having the chemical formula: | 12-25-2008 |
20080318961 | Drugs comprising chymase inhibitors and ACE inhibitors as effective ingredients - It is an object of the present invention to provide drugs which are effective for treatment of hypertension, cardiac disease (cardiac hypertrophy, cardiac failure, myocardial infarction, etc.), cerebral apoplexy, nephritis and the like. The invention also provides circulatory disease treatment agents in forms that allow combined use of chymase inhibitors and ACE inhibitors, and circulatory disease treatment methods which produce simultaneous chymase inhibition and ACE inhibition. | 12-25-2008 |
20090018137 | MODULATION OF CELL FATES AND ACTIVITIES BY PHTHALAZINEDIONES - Phthalazinediones that function as intracellular redox modulators are useful in treating cells in various disease states where intracellular redox status is impaired. By buffering aberrant redox states, phthalazinediones enable cellular processes essential for survival and augment medical treatments. The phthalazinediones of the invention can modulate functions related to cell growth, differentiation, activity, or death, to correct aberrations and restore homeostasis, and can serve as adjunctive therapy in treating various disease conditions. | 01-15-2009 |
20090023737 | Imidazo-Pyridazines, Triazolo-Pyridazines and Related Benzodiazepine Receptor Ligands - Compounds of the Formula: | 01-22-2009 |
20090023738 | DIAMINOPYRIMIDINES AS MODULATORS OF THE EP2 RECEPTOR - The present invention relates to diaminopyrimidines of the general formula I, process for their preparation, and the use thereof for the manufacture of pharmaceutical compositions for the treatment of disorders and indications connected with the EP | 01-22-2009 |
20090023739 | CAPASE INHIBITORS AND USES THEREOF - This invention provides novel caspase inhibitors of formula I: | 01-22-2009 |
20090023740 | SODIUM CHANNEL INHIBITORS - Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel. | 01-22-2009 |
20090036453 | Pyrrolopyridazinone Compound - The present invention discloses a pyrrolopyridazinone compound represented by the formula (1): | 02-05-2009 |
20090036454 | Compounds and Uses Thereof - This invention relates to novel compounds having the structural formula I below: | 02-05-2009 |
20090042889 | Pharmaceutical Composition For The Sustained Release Of Hydralazine And Use Thereof As A Support For Cancer Treatment - The invention relates to a sustained release form of hydralazine for use in cancer therapy. Said sustained release form of hydralazine can be used to obtain a constant concentration of the active principle in the blood, thereby enabling the demethylating effect of the hydralazine without producing the hypotensive action thereof, such that the inventive composition can be used in cancer therapy. | 02-12-2009 |
20090048259 | Phthalazine compounds, compositions and methods of use - The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders such as cancer. | 02-19-2009 |
20090062289 | IMMUNOMODULATING OXOPYRRAZOLOCINNOLINES AS CD 80 INHIBITORS - N-(1-Aza-bicyclo[2.2.2]oct-3-yl)-4-(6,9-difluoro-3-oxo-1,3-dihydro-pyrazolo[4,3-c]cinnolin-2-yl)-benzamide is a CD80 antagonist, useful in the treatment of dieases which benefit from immuno-inhibition. | 03-05-2009 |
20090062290 | HETEROCYCLES AS POTASSIUM CHANNEL MODULATORS - Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions. | 03-05-2009 |
20090062291 | PHOSPHODIESTERASE 10 INHIBITORS - The present invention is directed to compounds, useful as PDE10 inhibitors, having the formula | 03-05-2009 |
20090088436 | P38 Kinase Inhibiting Agents - Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: | 04-02-2009 |
20090105262 | Bridged polycyclic compound based compositions for coating oral surfaces in humans - A pharmaceutically active agent, a pharmaceutically active agent carrier and method of use thereof are described. In some embodiments, a system may include a composition. The composition may include one or more bridged polycyclic compounds. At least one of the bridged polycyclic compounds may include at least two cyclic groups, and at least two pharmaceutically active agents may be associated with the bridged polycyclic compound. In some embodiments, one or more bridged polycyclic compounds may be applied to an oral surface of a human such that an oral malady may be inhibited and/or ameliorated. | 04-23-2009 |
20090111816 | POLYCYCLIC ARYL SUBSTITUTED TRIAZOLES AND POLYCYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed. | 04-30-2009 |
20090118292 | CYTOKINE INHIBITORS - A compound of Formula I: | 05-07-2009 |
20090118293 | METHODS FOR REDUCING HOSPITALIZATIONS RELATED TO HEART FAILURE - The invention provides methods for (a) prolonging time to hospitalization for heart failure; (b) prolonging time to first hospitalization for heart failure; (c) reducing the total number of days a patient with heart failure spends in the hospital for heart failure for a single hospital stay (i.e., reducing the duration of a single hospital stay for a patient with heart failure); (d) reducing the total number of days a patient spends in the hospital for heart failure for multiple hospital stays; (e) reducing the number of hospital admissions for heart failure; and (f) reducing mortality and reducing hospitalizations for heart failure (e.g., the total number of days in the hospital and/or the number of hospital visits) in a patient in need thereof comprising administering to the patient a therapeutically effective amount of (i) a hydralazine compound or pharmaceutically acceptable salt thereof, (ii) isosorbide dinitrate and/or isosorbide mononitrate, and (iii) optionally at least one compound selected from the group consisting of angiotensin converting enzyme inhibitors, β-adrenergic antagonists, angiotensin II antagonists, aldosterone antagonists, cardiac glucosides (digitalis), and diuretic compounds. | 05-07-2009 |
20090118294 | COMPOSITIONS AND METHODS RELATED TO HEART FAILURE - The invention provides methods for reducing the total number of days a patient with heart failure spends in the hospital for heart failure for a single hospital stay (i.e., reducing the duration of a single hospital stay for a patient with heart failure); reducing the total number of days a patient spends in the hospital for heart failure for multiple hospital stays (i.e., two or more hospital stays); reducing the number of hospital admissions for heart failure; and reducing mortality and reducing hospitalizations for heart failure (e.g., the total number of days in the hospital and/or the number of hospital visits); by administering to a patient a therapeutically effective amount of (i) a hydralazine compound or pharmaceutically acceptable salt thereof, (ii) isosorbide dinitrate and/or isosorbide mononitrate, and (iii) optionally at least one angiotensin converting enzyme inhibitors, β-adrenergic antagonists, angiotensin II antagonists, aldosterone antagonists, cardiac glucosides (digitalis), or diuretic compounds. | 05-07-2009 |
20090124624 | SUBSTITUTED 1-AMINOPHTHALAZINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF - The invention concerns 1-amino-phthalazine derivatives of general formula (I): | 05-14-2009 |
20090131444 | Aminopiperidine Quinolines and Their Azaisosteric Analogues with Antibacterial Activity - The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans. | 05-21-2009 |
20090137595 | FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof. | 05-28-2009 |
20090143389 | HETEROCYCLIC INHIBITORS OF MEK AND METHODS OF USE THEREOF - Disclosed are compounds of the Formulas III and IV | 06-04-2009 |
20090156605 | Quinolones and azaquinolones that inhbit prolyl hydroxylase - Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: | 06-18-2009 |
20090163506 | Urea-compounds active as vanilloid receptor antagonists for the treatment of pain - Certain compounds of formula (I), | 06-25-2009 |
20090170854 | New Use - The present invention relates to a new use of certain pharmaceutically active compounds in the treatment and/or prevention of medicament induced gastric ulcer. More particularly the invention is directed to the use of said compounds, and pharmaceutically acceptable salts thereof, for the treatment and/or prevention of NSAID (non-steroidal antiinflammatory drugs) induced gastric ulcer as well as a pharmaceutical composition in the unit dosage form for the prevention of NSAID induced gastric ulcer in a mammal comprising an NSAID together with a 6-carboxamido-imidazo[1,2-a]pyridine compounds. Other pharmaceutically active compounds used in the present invention comprises COX-2 inhibitors, NO-NSAIDs and bisphosphonates. | 07-02-2009 |
20090170855 | HIV INHIBITING 3,4-DIHYDRO-IMIDAZO[4,5-B]PYRIDIN-5-ONES - HIV inhibitory compounds of formula: | 07-02-2009 |
20090170856 | HETEROCYCLIC ANTIVIRAL COMPOUNDS - Compounds of formula I, wherein R | 07-02-2009 |
20090170857 | Method for healing a wound using a direct vasodilator - A method for healing a wound comprising the step of topically administering a wound healing composition to a wounded area, wherein the wound healing composition comprises a first medicament characterized as a direct vasodilator and pharmaceutically acceptable salts thereof. | 07-02-2009 |
20090176788 | Imidazo[1,2-B]Pyridazines, Processes, Uses, Intermediates and Compositions - The invention provides novel imidazo[1,2-b]pyridazines of formula (I) and pharmaceutically acceptable salts, polymorphs, hydrates, tautomers, solvates and stereoisomers thereof. | 07-09-2009 |
20090186896 | PDE Inhibitors and Combinations Thereof for the Treatment of Urological Disorders - The invention provides pharmacological compositions comprising PDE-5 and PDE-4 inhibitors, alone or in combination, for the treatment of urological disorders comprising Benign Prostate Hyperplasia (BPH), Lower Urinary Tract Symptoms (LUTS) and in particular irritative symptoms caused by BPH-induced bladder outlet obstruction (BOO). The invention also provides methods of screening for such PDE-5 and PDE-4 inhibitors for use, alone and in combination, in the preparation of medicaments for the treatment of said urological disorders. | 07-23-2009 |
20090186897 | PHTHALAZINONE DERIVATIVES - A compound of the formula (I): | 07-23-2009 |
20090186898 | Inhibitors of bruton's tyrosine kinase - This application discloses novel imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives according to Formulae I-VI: | 07-23-2009 |
20090197887 | PIPERAZINYLPIPERIDINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS - The present invention relates to compounds of Formula I: | 08-06-2009 |
20090203702 | INHIBITORS OF p38 - The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders. | 08-13-2009 |
20090221589 | Use of aminoalcohol derivatives for the treatment of overactive bladder - The present invention relates to the use of new beta-agonists of general formula (Ia) or (Ib) wherein the groups R | 09-03-2009 |
20090221590 | SALT OF CD 80 ANTAGONIST - The choline salt of the CD80 antagonist compound 4-(6-fluoro-3-oxo-1,3-dihydro-pyrazolo[4,3-c]cinnolin-2-yl)-N-(2,2-difluoro-ethyl)-benzamide (I) has good aqueous solubility and is therefore convenient for pharmaceutical use. | 09-03-2009 |
20090239870 | Spirohydantoin Aryl Cgrp Receptor Antagonists - Compounds of formula I: | 09-24-2009 |
20090239871 | SOLUBILIZED TOPOISOMERASE POISONS - The invention provides compounds of formula I: | 09-24-2009 |
20090239872 | TREATMENT OF MESOTHELIOMA - The present invention relates to a method of treating a warm-blooded animal, especially a human, having mesothelioma, especially malignant mesothelioma, comprising administering to said animal a therapeutically effective amount of a 4-pyridylmethyl-phthalazine derivative. | 09-24-2009 |
20090253705 | HYDROXYMETHYL PYRROLIDINES AS BETA 3 ADRENERGIC RECEPTOR AGONISTS - The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor. | 10-08-2009 |
20090264434 | PYRIDAZINONE GLUCOKINASE ACTIVATORS - Provided herein are compounds of the formula (I): | 10-22-2009 |
20090275585 | Novel Compounds and Therapeutic Use Thereof for Protein Kinase Inhibition - Novel compound having the following formula: | 11-05-2009 |
20090281107 | SUBSTITUTED 2,5-DIHYDRO-3H-PYRAZOLO[4,3-C]PYRIDAZIN-3-ONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE OF THE SAME - The invention relates to compounds having the formula (I): | 11-12-2009 |
20090286795 | USE OF VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR INHIBITORS FOR THE TREATMENT OF CANCER - The invention relates to a method for screening patients for tumor burden and the use of VEGF-R inhibitors alone or in combination with chemotherapy for the treatment of gastrointestinal, genitourinary, lymphoid and pulmonary (small cell and non-small cell) cancer patients and patients with cancers of neural crest origin having high serum or plasma LDH5 levels. | 11-19-2009 |
20090286796 | Compounds exhibiting type X sPLA2 inhibiting effect - A compound represented by the general formula: | 11-19-2009 |
20090291957 | HETEROCYCLIC DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS - Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise, for example, administering to a mammal in need thereof a compound of formula (II): | 11-26-2009 |
20090298836 | Thiadiazole modulators of PKB - The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. | 12-03-2009 |
20090298837 | COMPOUNDS, METHODS AND PHARMACEUTICAL COMPOSITIONS FOR INHIBITING PARP - The present invention provides compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein. | 12-03-2009 |
20090306082 | NOVEL HETEROCYCLIC COMPOUNDS USEFUL FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS: PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - The present invention relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the formula (1) and analogs, tautomers, enantiomers, a diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxides, pharmaceutically acceptable solvates thereof and the pharmaceutical compositions containing them which are useful in the treatment of allergic and inflammatory diseases including asthma, chronic bronchitis, atopic dermatitis, urticaria, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, eosinophilic granuloma, psoriasis, rheumatoid arthritis, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and reperfusion injury of the brain, chronic glomerulonephritis, endotoxic shock and adult respiratory distress syndrome. | 12-10-2009 |
20090306083 | Use of Trifluoromethyl Substituted Benzamides in teh Treatment of Neurological Disorders - The invention relates to methods of using the compounds of the invention, including trifluoromethyl substituted benzamide compounds and salts thereof, as well as pharmaceutical compositions comprising the same, in the treatment of Eph receptor-related (e.g., neurological) injuries and disorders. The invention also relates to modulating the activity of an Eph receptor in a cell, stimulating neural regeneration, and reversing neuronal degeneration, by administering a compound of the invention to a cell or subject in an effective amount. | 12-10-2009 |
20090306084 | HETEROARYL 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS - Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: | 12-10-2009 |
20090312333 | 2-Oxo-1-Pyrrolidine Derivatives, Processes for Preparing Them and Their Uses - The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals. | 12-17-2009 |
20090312334 | Immunomodulating Heterocyclic Compounds - Compounds of formula (I) are inhibitors of CD80 and useful in immunomodulation therapy: | 12-17-2009 |
20090325968 | Compositions Useful as Inhibitors of Protein Kinases - The present invention provides a compound of formula I: | 12-31-2009 |
20100016325 | TETRAHYDROCINNOLINE DERIVATIVES - Provided herein are compounds of formula (I): | 01-21-2010 |
20100029654 | CARDIOVASCULAR COMPOSITIONS AND USE OF THE SAME FOR THE TREATMENT OF ALZHEIMER'S DISEASE - Methods and compositions for the treatment of Alzheimer's Disease are described. More specifically, the invention demonstrates that administration of cardiovascular agents to a mammal suffering from the symptoms of Alzheimer's Disease causes an amelioration of those symptoms. The finding of the present invention can be used in treatment regimens designed to attenuate or prevent Alzheimer's Disease. | 02-04-2010 |
20100029655 | Processes For The Preparation Of Anti-Viral Compounds And Compositions Containing Them - Disclosed are processes for the preparation of compounds of formula I and compositions that comprise said compounds of formula I. | 02-04-2010 |
20100029656 | AZABICYCLIC HETEROCYCLES AS CANNABINOID RECEPTOR MODULATORS - The present application describes CB-1 inverse agonists according to Formula (I) and (Ia), pharmaceutical compositions comprising at least one compound according to Formula (I) or (Ia), and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula (I) or (Ia), both alone and in combination with one or more additional therapeutic agents. The preferred compounds have the general Formula (Ia), including all prodrugs, pharmaceutically acceptable salts and stereoisomer, thereof, wherein R | 02-04-2010 |
20100035883 | DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) - A compound having the structure set forth in Formula (I) and Formula (II): | 02-11-2010 |
20100041662 | Heterocyclic compounds as antiinflammatory agents - A compound of Formula Ia or Ib in free or salt or solvate form, where R | 02-18-2010 |
20100041663 | Organic Compounds as Smo Inhibitors - The present invention relates generally to novel compounds relating to the diagnosis and treatment of pathologies relating to the Hedgehog pathway, including but not limited to tumor formation, cancer, neoplasia, and non-malignant hyperproliferative disorders. The present invention includes novel compounds, novel compositions, methods of their use and methods of their manufacture, where such compounds are generally pharmacologically useful as agents in therapies whose mechanism of action involve methods of inhibiting tumorigenesis, tumor growth and tumor survival using agents that inhibit the Hedgehog and Smo signaling pathway. | 02-18-2010 |
20100041664 | BICYCLIC LACTAM FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS - The present invention provides novel bicyclic lactams derivatives, and analogues thereof, of Formula (I): | 02-18-2010 |
20100056529 | SUBSTITUTED TRIAZOLO-PYRIDAZINE DERIVATIVES - This invention relates to novel substituted triazolo-pyridazines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an α1-GABA-A receptor antagonist and/or a α2, α3 and α5 GABA-A receptor agonist. | 03-04-2010 |
20100063054 | cMET INHIBITORS - Compounds of the following formula are provided for use with cMET: | 03-11-2010 |
20100069392 | Combination of HMG-COA Reductase Inhibitors with Phosphodiesterase 4 Inhibitors for the Treatment of Inflammatory Pulmonary Disease - The invention relates to the combined use of a PDE4 inhibitor with a HMG-CoA reductase inhibitor for the preventive and curative treatment of an inflammatory pulmonary disease. | 03-18-2010 |
20100093739 | METHOD FOR DECREASING CAPILLARY PERMEABILITY IN THE RETINA - Disclosed herein are methods for decreasing or attenuating an increase in capillary permeability in the retina in a subject in need of such treatment, comprising administering a composition comprising an amount of a phthalazine derivative or a salt thereof to a subject suffering from excessive or pathological capillary permeability in the retina, the amount of phthalazine derivative or salt thereof being effective to decrease the permeability of capillaries in the retina of the subject. | 04-15-2010 |
20100105690 | LISOFYLLINE ANALOGS AND METHODS FOR USE - Analogs of a Lisofylline (LSF), and synthetic methods for the preparation of such analogs are provided. The analogs of LSF provided have the ability to protect cell viability, particularly the ability to protect pancreatic β-cells. | 04-29-2010 |
20100113458 | IMIDAZOPYRIDAZINECARBONITRILES USEFUL AS KINASE INHIBITORS - The invention provides compounds of Formula (I) | 05-06-2010 |
20100130499 | BICYCLOHETEROARYL COMPOUNDS AND THEIR USE AS TRPV1 LIGANDS - The invention relates to compounds of formula I | 05-27-2010 |
20100137320 | GAMMA SECRETASE MODULATORS - This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula | 06-03-2010 |
20100137321 | IMIDAZO[1,2-a]AZINES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to derivatives of imidazo[1,2-a]azines of formula I, | 06-03-2010 |
20100144737 | METHODS FOR INHIBITING T HELPER CELL DIFFERENTIATION - The present invention relates to methods and compounds useful for inhibiting T helper cell differentiation. Methods and compounds for decreasing IL-12 signaling in T helper cells are also provided. | 06-10-2010 |
20100144738 | INHIBITORS OF C-MET AND USES THEREOF - The present invention relates to compounds and methods use as inhibitors of c-Met. Certain compounds of the subject invention have the following structural formula (I). Other compounds of the subject invention have structural formulas as defined herein. Also disclosed herein are pharmaceutical compositions comprising the compounds of the subject invention. | 06-10-2010 |
20100144739 | HETEROCYCLIC INHIBITORS OF C-MET AND USES THEREOF - The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders. | 06-10-2010 |
20100144740 | SYNERGISTIC COMBINATIONS OF VR-1 ANTAGONISTS AND COX-2 INHIBITORS - A synergistic combination of a vanilloid receptor VR-1 antagonist and an NSAID or a pharmaceutically acceptable salt or solvate of either or both compounds thereof. | 06-10-2010 |
20100144741 | ETHANOLAMINE DERIVATIVES USEFUL AS BACE INHIBITORS - The invention relates to novel cyclic compounds of the formula (I), in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them. | 06-10-2010 |
20100144742 | MULTIPLY-SUBSTITUTED TETRAHYDRONAPHTHALENE DERIVATIVES, PROCESS FOR THEIR PRODUCTION AND THEIR USE AS ANTI-INFLAMMATORY AGENTS - The invention relates to multiply-substituted tetrahydronaphthalene derivatives of formula (I) | 06-10-2010 |
20100168116 | 3,6-SUBSTITUTED IMIDAZOL[1,2-B]PYRIDAZINE ANALOGS FOR TREATING ALLERGIC AND INFLAMMATORY DISEASES - Methods for treating an allergic or inflammatory disease or other Syk-mediated disease or Syk-mediated condition characterized by administering a composition which contains a therapeutically effective amount of a 3,6-substituted imidazol[1,2-b]pyridazine compound. | 07-01-2010 |
20100179153 | Bicyclic S1P Receptor Modulators - The invention relates to novel heterocyclic compounds of the formula | 07-15-2010 |
20100179154 | 6-CYCLOAMINO-3-(PYRID-4-YL)IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): | 07-15-2010 |
20100179155 | ACTIVATORS AND THERAPEUTIC APPLICATIONS THEREOF - The invention presents methods of identifying small molecule compounds that are activators of tumor suppressor protein p53 pathway, and its associated family members p63 and p73, function. The invention is further drawn to methods of killing tumor cells and treating cancers or other conditions requiring activation of the p53 family member pathways and DNA damage response pathways with the small molecules. | 07-15-2010 |
20100184770 | COMPOUNDS - The present invention relates to a compound of formula (I) | 07-22-2010 |
20100184771 | Bicyclic Heterocyclic Compound - A compound represented by the formula (I), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof: | 07-22-2010 |
20100190795 | BETULIN DERIVED COMPOUNDS USEFUL AS ANTIPROTOZOAL AGENTS - The invention relates to betulin derivatives, and to the use thereof as agents against protozoa of the genus | 07-29-2010 |
20100190796 | METHODS FOR IDENTIFYING INHIBITORS OF SOLUTE TRANSPORTERS - Provided herein are methods for identifying and characterizing agents that alter the volume of a cell. Methods are provided for rapid screening and identification of an agent that alters the capability of a small, neutrally charged solute transporter to transport the solute across a cell membrane. The methods described herein may be used to identify and characterize inhibitors of urea transporters, to identify and characterize inhibitors of aquaporins, and to identify and characterize inhibitors of other small, neutrally charged solutes such as glucose. | 07-29-2010 |
20100204235 | ORGANIC COMPOUNDS - Compounds of formula I | 08-12-2010 |
20100210657 | Bicyclic Benzamides of 3-or 4-Substituted 4-(Aminomethyl)-Piperidine Derivatives - The present invention of compounds of formula (I) | 08-19-2010 |
20100216798 | FUSED HETEROCYCLES AS LCK INHIBITORS - There is provided fused heterocycles of imidazopyridazine or pyrazolopyrimidine derivative represented by the formula (I), which have excellent Lck inhibitory activity and are useful for a medicament particularly an immunosuppressive agent. | 08-26-2010 |
20100216799 | PHTHALAZINE AND PYRIDO[3,4-D]PYRIDAZINE COMPOUNDS AS H1 RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula (I), | 08-26-2010 |
20100222353 | AMINOPHTHALAZINE DERIVATIVE COMPOUNDS - The invention pertains to new aminophthalazine compounds that serve as effective phosphodiesterase (PDE) inhibitors. The invention also relates to compounds that are selective inhibitors of PDE-10. The invention further relates to intermediates for preparation of such compounds; pharmaceutical compositions comprising such compounds; and the use of such compounds in methods for treating certain central nervous system (CNS) or other disorders. The invention relates also to methods for treating neurodegenerative and psychiatric disorders, for example psychosis and disorders comprising deficient cognition as a symptom. | 09-02-2010 |
20100234383 | TREATING, PREVENTING OR AMELIORATING A HYPERPROLIFERATIVE DISEASE/DISORDER - The invention provides a method for treating, preventing or ameliorating a hyperproliferative disease and/or disorder such as cancer (e.g. leukemia) in a mammal comprising administering a therapeutically effective amount of one or more compounds selected from the group consisting of compounds of Formula (I), quinolones and fluoroquinolones; or a pharmaceutically acceptable salt thereof to said mammal: | 09-16-2010 |
20100240663 | HETEROCYCLES AS POTASSIUM CHANNEL MODULATORS - Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions. | 09-23-2010 |
20100240664 | SOLUBILIZED TOPOISOMERASE POISON AGENTS - The invention provides compounds of formula I: | 09-23-2010 |
20100261724 | HETEROCYCLE PHENYL AMIDE T-TYPE CALCIUM CHANNEL ANTAGONISTS - The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved. | 10-14-2010 |
20100267730 | NOVEL COMPOUNDS - This invention relates to imidazopyridazine substituted piperidine derivatives and their use as pharmaceuticals. | 10-21-2010 |
20100273801 | BETULIN DERIVED COMPOUNDS USEFUL AS ANTIBACTERIAL AGENTS - The invention relates to compouns derived from betulin, and to the use thereof as antibacterial agents in pharmaceutical and cosmetic applications. | 10-28-2010 |
20100280035 | SOLID PHARMACEUTICAL COMPOSITION COMPRISING 1-(4-CHLOROANILINO)-4-(4-PYRIDYLMETHYL)PHTHALAZINE AND A PH MODIFIER - The present invention concerns pharmaceutical compositions comprising the pH dependent drug compound 1-(4-chloroanilino)-4-(4-pyridylmethyl)phthalazine and a pH modifier. | 11-04-2010 |
20100292238 | Phenoxymethyl Heterocyclic Compounds - Phenoxymethyl compounds that inhibit at least one phosphodiesterase 10 are described as are pharmaceutical compositions containing such compounds an methods for treating various CNS disorders by administering such compounds to a patient in need thereof. | 11-18-2010 |
20100298332 | Substituted Spirocyclic Piperidine Derivatives as Histamine-3 (H3) Receptor Ligands - The present invention provides compounds of Formula (I): | 11-25-2010 |
20100317665 | Anti-Inflammatory And Protein Kinase Inhibitor Compositions And Related Methods For Downregulation Of Detrimental Cellular Responses And Inhibition Of Cell Death - A novel class of pyridazine compositions and related methods of use. | 12-16-2010 |
20100324047 | RAF KINASE MODULATORS AND METHODS OF USE - The present invention comprises a new class of compounds capable of modulating the activity of Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula (I) wherein each of A | 12-23-2010 |
20100324048 | DISUBSTITUTED PHTHALAZINE HEDGEHOG PATHWAY ANTAGONISTS - The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer. | 12-23-2010 |
20100331333 | Imidazo [1,2-B] Pyridazine Compounds - This invention relates generally to imidazo[1,2-b]pyridazine-based modulators of Liver X receptors (LXRs) having formula (I) and related methods: | 12-30-2010 |
20100331334 | INHIBITORS OF MEK - This invention concerns to N-(2-aylamino)aryl sulfonamides, which are inhibitors of MEK, methods of using such compounds in the treatment of hyperproliferative diseases, and to pharmaceutical compositions containing such compounds. | 12-30-2010 |
20110009414 | HETEROCYCLIC DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS - Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise, for example, administering to a mammal in need thereof a compound of formula (II): | 01-13-2011 |
20110009415 | Thienopyridazine Compounds, Their Preparations, Pharmaceutical Compositions And Uses - The present invention relates to thienopyridazine compounds of formula (I), their pharmaceutically acceptable salts or hydrates, wherein R1 and R2 are independently H or C1-4 alkyl, R3 is a saturated or unsaturated 5- or 6-membered ring containing N, S or O, or its optical isomers, R4 is a halophenyl monosubstituted or disubstituted at any position. The present invention provides the preparation methods of these compounds, pharmaceutical compositions containing these compounds and the uses of these compounds, particularly in treating cancer. | 01-13-2011 |
20110015198 | DIARYLMETHYLAMIDE DERIVATIVE HAVING MELANIN-CONCENTRATING HORMONE RECEPTOR ANTAGONISM - [Problem] To provide a melanin-concentrating hormone receptor antagonist useful as a pharmaceutical agent for central diseases, circulatory diseases, and metabolic diseases. | 01-20-2011 |
20110028481 | HYDROXYMETHYL PYRROLIDINES AS BETA 3 ADRENERGIC RECEPTOR AGONISTS - The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor. | 02-03-2011 |
20110034467 | DIHYDRO-PYRROLOPYRIDINE-, DIHYDRO-PYRROLOPYRIDAZINE- AND DIHYDRO-PYRROLOPYRIMIDINE-DERIVATIVES AND USE THEREOF - The invention relates to novel dihydro-pyrrolopyridine, dihydro-pyrrolopyridazine and dihydro-pyrrolopyrimidine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders. | 02-10-2011 |
20110034468 | TRIAZOLO COMPOUNDS USEFUL AS DGAT1 INHIBITORS - Disclosed are triazolopyridine compounds of Formula (I), including pharmaceutically acceptable salts thereof. Also, disclosed are methods of using the compound in the treatment of obesity, dyslipidemia, diabetes and atherosclerosis, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof. | 02-10-2011 |
20110046143 | DISUBSTITUTED PHTHALAZINE HEDGEHOG PATHWAY ANTAGONISTS - The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer. | 02-24-2011 |
20110053943 | CARBAMATE AND UREA INHIBITORS OF 11 -HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the invention pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell. | 03-03-2011 |
20110059975 | NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A2 and R | 03-10-2011 |
20110065711 | SUBSTITUTED TRIAZOLO-PYRIDAZINE DERIVATIVES - This invention relates to novel substituted triazolo-pyridazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an α1-GABA | 03-17-2011 |
20110065712 | TRICYCLIC COMPOUNDS AND PHARMACEUTICAL USES THEREOF - The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These tricyclic compounds and compositions containing them are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, pathogenic infections, and certain immunological disorders. | 03-17-2011 |
20110082148 | TREATING, PREVENTING OR AMELIORATING A HYPERPROLIFERATIVE DISEASE/DISORDER - The invention provides a method for treating, preventing or ameliorating a hyperproliferative disease and/or disorder such as cancer (e.g. leukemia) in a mammal comprising administering a therapeutically effective amount of one or more compounds selected from the group consisting of compounds of Formula (I), quinolones and fluoroquinolones; or a pharmaceutically acceptable salt thereof to said mammal: | 04-07-2011 |
20110098304 | Small molecule inhibitors of PARP activity - Componds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such componds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer. | 04-28-2011 |
20110098305 | ARYLSULFONAMIDE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member. | 04-28-2011 |
20110105509 | INDOLE BASED RECEPTOR CRTH2 ANTAGONISTS - Disclosed are compounds of Formula (I): | 05-05-2011 |
20110105510 | PROPHYLACTIC/AMELIORATING OR THERAPEUTIC AGENT FOR NON-ALCOHOLIC STEATOHEPATITIS - Disclosed are: a safe and highly effective prophylactic/ameliorating or therapeutic agent for NASH; and a method for using the agent. The prophylactic/ameliorating or therapeutic agent for NASH comprises a combination of at least one component selected from the group consisting of ω3PUFAs, a pharmaceutically acceptable salt thereof and an ester thereof and a PDE4 inhibitor as active ingredients. | 05-05-2011 |
20110105511 | POLYCYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. | 05-05-2011 |
20110105512 | BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase AxI. Methods of using the compounds in treating diseases or conditions associated with AxI activity are also disclosed. | 05-05-2011 |
20110136812 | SOLUBILIZED TOPOISOMERASE POISONS - The invention provides compounds of formula I: | 06-09-2011 |
20110136813 | WNT PROTEIN SIGNALLING INHIBITORS - The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis. | 06-09-2011 |
20110136814 | Diazepine and Diazocane Compounds As MC4 Agonists - The present invention relates to compounds of formula (I) wherein R | 06-09-2011 |
20110144115 | SUBSTITUTED 1-BENZYL-CINNOLIN-4(1H)-ONE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF - The present invention is related to novel substituted 1-benzylcinnolin-4(1H)-one derivatives having affinity for cannabinoid CB | 06-16-2011 |
20110160213 | PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS - The present invention relates to the pharmaceutical compositions, more particularly to the pharmaceutical compositions comprising novel phosphodiesterase type 4 (PDE4) inhibitors, and their use in treating allergic and inflammatory disorders. | 06-30-2011 |
20110166145 | Stabilization of hypoxia inducible factor (HIF) alpha - The present invention relates to methods of stabilizing the alpha subunit of hypoxia inducible factor (HIF). The invention further relates to methods of preventing, pretreating, or treating conditions associated with HIF, including ischemic and hypoxic conditions. Compounds for use in these methods are also provided. | 07-07-2011 |
20110166146 | IMIDAZO[1,2-a]PYRIDINE COMPOUNDS - Imidazo[1,2-a]pyridines are disclosed. Compounds of the invention are useful therapeutic agents and their inclusion in pharmaceutical formulations and use in methods of treatment are disclosed. | 07-07-2011 |
20110172235 | SUBSTITUTED TRIAZOLOPHTHALAZINE DERIVATIVES - This invention relates to novel substituted triazolophthalazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering selective α5 receptor partial or full inverse agonists. | 07-14-2011 |
20110183984 | SMALL MOLECULE INHIBITORS OF LCK SH2 DOMAIN BINDING - The present invention provides materials and methods for modulating an immune response. The materials and methods may be used to treat diseases associated with an aberrant immune response. In some embodiments, materials and methods of the invention may be used to treat autoimmune diseases, for example, rheumatoid arthritis. | 07-28-2011 |
20110183985 | SUBSTITUTED FUSED ARYL AND HETEROARYL DERIVATIVES AS PI3K INHIBITORS - The present invention provides fused aryl and heteroaryl derivatives of Formula I: | 07-28-2011 |
20110183986 | POLYCYCLIC ARYL SUBSTITUTED TRIAZOLES AND POLYCYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed. | 07-28-2011 |
20110190303 | NOVEL HETEROCYCLIC COMPOUNDS USEFUL FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS: PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - The present invention relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the formula (1) and analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxides, pharmaceutically acceptable solvates thereof and the pharmaceutical compositions containing them which are useful in the treatment of allergic and inflammatory diseases including asthma, chronic bronchitis, atopic dermatitis, urticaria, allergic rhinitis, allergic conjunctivitis, vernal conjuctivitis, eosinophilic granuloma, psoriasis, rheumatoid arthritis, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and reperfusion injury of the brain, chronic glomerulonephritis, endotoxic shock and adult respiratory distress syndrome. | 08-04-2011 |
20110190304 | DISUBSTITUTED PHTHALAZINE HEDGEHOG PATHWAY ANTAGONISTS - The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer. | 08-04-2011 |
20110212968 | PHENETHYLAMIDE DERIVATIVES AND THEIR HETEROCYCLIC ANALOGUES - The invention relates to novel phenethylamide derivatives and their wherein A, B, R | 09-01-2011 |
20110218202 | SOLUBLE GUANYLATE CYCLASE ACTIVATORS - Compounds of Formula I are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the Formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the Formula I. | 09-08-2011 |
20110224214 | PROCESS FOR PREPARING POLYMORPH - Disclosed is a novel process for preparing crystalline Form II of 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide. | 09-15-2011 |
20110230490 | HETEROARYL-SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE - Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis). | 09-22-2011 |
20110237596 | HETEROARYL-SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE - Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis). | 09-29-2011 |
20110245254 | HETEROCYCLIC COMPOUNDS AS INHIBITORS OF BETA-LACTAMASES - This invention discloses and claims methods for inhibiting bacterial β-lactamases and treating bacterial infections by inhibiting bacterial β-lactamases in man or an animal comprising administering a therapeutically effective amount to said man or said animal of a compound, or pharmaceutically acceptable salt thereof, of formula (I) either alone or in combination with a β-lactamine antibiotic wherein said combination can be administered separately, together or spaced out over time. Pharmaceutical compositions comprising a compound of formula (I), or a combination of a compound of formula (I) and a therapeutically effective amount of a β-lactamine antibiotic, and a pharmaceutically acceptable carrier are also disclosed and claimed. | 10-06-2011 |
20110251199 | NITROGEN-CONTAINING BICYCLIC HETEROARYL COMPOUNDS AND METHODS OF USE - The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I | 10-13-2011 |
20110257186 | COMPOSITIONS AND METHODS FOR TREATING VISUAL DISORDERS - Disclosed are methods of treating disorders of the eye by administering to a patient in need of such treatment a compound represented by the formula | 10-20-2011 |
20110257187 | PHTHALAZIN-(2H)-ONE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 10-20-2011 |
20110275642 | NEW METHOD FOR OBTAINING 5-AMINO 2,3-DIHYDROPHTHALAZINE-1,4-DIONE ALKALI METAL SALTS AND THEIR USE IN MEDICINE - The invention is related to a method for preparing 5-amino-2,3-dihydrophthalazine-1,4-dione salt with alkali metals of the formula II wherein 5-nitro-2,3-dihydrophthalazine-1,4-dione is solved in water solution of MOH1 where M has the below mentioned meaning, with formation of solution of 5-nitro-2,3-dihydrophthalazine-1,4-dione alkali metal salt, which is catalytically transformed into 5-amino-2,3-dihydrophthalazine-1,4-dione salt at the temperature 40-900C by means of hydrogen under the pressure 1-4 MPa in at the presence of a transition metal catalyst (Pt, Pd) on activated carbon, and separation of crystalline 5-amino-2,3-dihydrophthalazine-1,4-dione salt is performed by water solution diluting with lower alcohol or cyclic lower ether with cooling to the temperature −5° C. to −15° C., providing that there is used 5-nitro-2,3-dihydrophthalazine-1,4-dione formed in the reaction of anhydride of 3-nitrophthalic acid with hydrazine hydrate in anhydrous acetic acid at the temperature 100-110° C. with distilling the mixture of acetic acid and water off. There was also presented a pharmaceutical composition containing such obtained 5-amino-2,3-dihydrophthalazine-1,4-dione salt with alkali metals and its application in medicine. There was also presented new use of 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt for production of a drug for treatment of heart diseases, pancreas diseases and diabetes as well as application of sodium salt optionally in combination with lithium salt for treatment of the nervous system diseases. Besides, the methods of treatment of these diseases were also presented. Formula II where M represents Li, Na, K | 11-10-2011 |
20110281877 | Dithiinopyridazinone Derivatives - The present invention relates to new dithiinopyridazinedione derivatives, to processes for preparing them, to their use for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to crop protection compositions comprising these dithiinopyridazinedione derivatives. | 11-17-2011 |
20110281878 | INHIBITORS OF p38 - The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders. | 11-17-2011 |
20110301167 | PYRAZOLO [4,3-c] CINNOLIN-3-ONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to pyrazolo[4,3-c]cinnolin-3-one compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 12-08-2011 |
20110306616 | Novel Compounds as Cannabinoid Receptor Ligands - Disclosed herein are cannabinoid receptor ligands of formula (I) | 12-15-2011 |
20110312966 | Dithiinopyridazinone Derivates - The present invention relates to new dithiinopyridazinone derivatives, to processes for preparing them, to their use for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to crop protection compositions comprising these dithiinopyridazinone derivatives. | 12-22-2011 |
20120004234 | PHTHALAZINE-CONTAINING ANTIDIABETIC COMPOUNDS - This invention provides for certain phthalazine-containing compounds of the formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof, wherein G is an optionally substituted N—N containing heteroaryl group and the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders. | 01-05-2012 |
20120004235 | METHODS TO TREAT CANCER - The invention provides methods and pharmaceutical compositions for treating certain cancers with compounds of formula (I) wherein A, B, W, Y, Z, and R | 01-05-2012 |
20120004236 | SUBSTITUTED TRIAZOLO-PYRIDAZINE DERIVATIVES - This invention relates to novel substituted triazolo-pyridazines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an α1-GABA-A receptor antagonist and/or a α2, α3 and α5 GABA-A receptor agonist. | 01-05-2012 |
20120004237 | SALT OF CD 80 ANTAGONIST - Choline salt of the CD80 antagonist compound 4-(6-fluoro-3-oxo-1,3-dihydro-pyrazolo[4,3-c]cinnolin-2-yl)-N-(2,2-difluoro-ethyl)-benzamide. | 01-05-2012 |
20120010208 | 6-CYCLOAMINO-3-(1H-PYRROLO[2,3-b]PYRIDIN-4-YL)IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to 6-cycloamino-3-(1H-pyrrolo[2,3-b]pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives corresponding to the general formula (I) in which R | 01-12-2012 |
20120010209 | IMIDAZO[1,2-A]PYRIDINES AND IMIDAZO[1,2-b]PYRIDAZINES AS MARK INHIBITORS - The invention encompasses imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included. | 01-12-2012 |
20120028984 | Compound Useful As A c-MET Inhibitor - The present invention relates to a c-Met inhibitor (disclosed herein) or a pharmaceutically acceptable salt thereof useful in treating cancer mediated by activity of c-Met receptors. | 02-02-2012 |
20120035179 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, | 02-09-2012 |
20120040987 | DERIVATIVES OF 6-(6-NH-SUBSTITUTED-TRIAZOLOPYRIDAZINE-SULFANYL) BENZOTHIAZOLES AND BENZIMIDAZOLES, PREPARATION THEREOF, USE THEREOF AS DRUGS, AND USE THEREOF AS MET INHIBITORS - The invention relates to novel products of the formula (I) where: (II) is a single or double bond; Rb is a hydrogen or fluorine atom; Ra is a NH-Rc radical in which Rc is an optionally substituted heterocycloalkyl, aryl, heteroaryl or -alkylcycloalkyl radical; X is S, SO, or SO2; A is NH or S; W is H, alkyl, or COR with R being cycloalkyl; alkyl; alkoxy; O-phenyl; —O— (CH2)n-phenyl with n=1 to 4; or NR1R2 with R1 being H or alk and R2 is H, cycloalkyl or alkyl; or R1, R2 form a cycle together with N optionally containing O, S, N and/or NH; all of said radicals being optionally substituted; wherein said products can be in any isomer or salt form, and can be used as drugs, in particular as MET inhibitors. | 02-16-2012 |
20120046294 | Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 02-23-2012 |
20120065208 | CANCER TREATMENT - A method for treating, preventing or ameliorating a hyperliferative disease and/or disorder in a mammal, comprises administering a therapeutically effective amount of one or more compounds selected from the group consisting of a compound of Formula (III), a compound of Formula (IV), and a pharmaceutically acceptable salt of Formula (III) or Formula (IV): | 03-15-2012 |
20120077816 | SUBSTITUTED HETEROCYCLES AND THEIR USE AS ALLOSTERIC MODULATORS OF NICOTINIC AND GABAA RECEPTORS - The present invention is related to heterocycles represented by a compound of Formula I that are novel allosteric modulators of α7 nAChRs and/or GABA | 03-29-2012 |
20120095006 | TREATMENT OF PULMONARY HYPERTENSION - This invention relates to the use of certain cyclic guanosine 3′,5′-monophosphate phosphodiesterase type five (cGMP PDE5) inhibitors, including in particular the compound sildenafil, for the treatment of pulmonary hypertension. | 04-19-2012 |
20120108595 | PLATELET-ACTIVATING FACTOR RECEPTOR ANTAGONISTS - Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders. | 05-03-2012 |
20120115873 | DIAZABENZO[DE] ANTHRACEN-3-ONE COMPOUNDS AND METHODS FOR INHIBITING PARP - The present invention relates to diazabenzo[de]anthracen- | 05-10-2012 |
20120129863 | CHYMASE INHIBITORS - Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase. | 05-24-2012 |
20120129864 | SUBSTITUTED 1-ALKYLCINNOLIN-4(1H)-ONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION OF SAME - The subject of the present invention is compounds corresponding to the formula (I) in which: X represents a divalent (C | 05-24-2012 |
20120129865 | CRYSTALLINE (8S,9R)-5-FLUORO-8-(4-FLUOROPHENYL)-9-(1-METHYL-1H-1,2,4-TRIAZOL-5-YL)-8,- 9-DIHYDRO-2H-PYRIDO[4,3,2-DE]PHTHALAZIN-3(7H)-ONE TOSYLATE SALT - Provided herein are (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt forms, including crystalline forms, and methods of their preparation. Pharmaceutical compositions comprising a (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt are also provided, as are methods of using (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt to treat a disease or condition, such as a cancer. | 05-24-2012 |
20120135996 | CYTOPROTECTIVE AGENT - Disclosed is a cytoprotective agent for use with respect to ischemic damage, including as an active ingredient a triprenyl phenol compound represented by the following general formula (I), wherein X is —CHY—C(CH | 05-31-2012 |
20120172365 | USE OF PHOSPHORDIESTERASE INHIBITORS IN THE TREATMENT OF PROSTATIC DISEASES - The present invention pertains to the use of inhibitors of phosphodiesterase I, IV and V for the prophylaxis and treatment of prostatic diseases, in particular the use of
| 07-05-2012 |
20120196868 | THERAPEUTIC COMPOSITIONS AND METHODS - The present invention relates in general to therapeutic compositions and methods of use. In preferred embodiments, the invention relates to the field of eye health. In some embodiments, the invention relates to the prevention and treatment of macular degeneration by administering compounds disclosed herein. In some embodiments, the invention relates to compositions and methods of improving vision. | 08-02-2012 |
20120202819 | COMBINATION THERAPY USING A BETA 3 ADRENERGIC RECEPTOR AGONISTS AND AN ANTIMUSCARINIC AGENT - Described herein is an improved method of treating overactive bladder, wherein the method comprises administering to a patient in need thereof a beta 3 adrenergic receptor agonist, an antimuscarinic agent, and an optional selective M | 08-09-2012 |
20120208820 | DIAZABICYCLIC CENTRAL NERVOUS SYSTEM ACTIVE AGENTS - Compounds of formula I | 08-16-2012 |
20120214815 | 2-Oxo-1-Pyrrolidine Derivatives, Processes for Preparing Them and Their Uses - The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals. | 08-23-2012 |
20120232081 | CYCLIC (AZA)INDOLIZINECARBOXAMIDES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS - The present invention relates to cyclic indolizinecarboxamides and azaindolizinecarboxamides of the formulae Ia and Ib, | 09-13-2012 |
20120232082 | NOVEL COMPOUNDS AND THERAPEUTIC USE THEREOF FOR PROTEIN KINASE INHIBITION - Novel compound having the following formula: (I) wherein Y is N, O, or S. Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same. The novel compounds of the present invention are found to inhibit protein kinases, especially Checkpoint kinase Chk1/Chk2. | 09-13-2012 |
20120289510 | Benzyl Amines, A Process For Their Production And Their Use As Anti-Inflammtory Agents - The present invention relates to the compounds of formula I, | 11-15-2012 |
20120289511 | COMPOSITIONS AND METHODS FOR TREATING ALZHEIMER'S DISEASE - The present invention provides compositions for reducing amyloid plaque burden associated with Alzheimer's disease and methods of using the same. | 11-15-2012 |
20120295912 | PIPERAZINYLPIPERIDINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS - The present invention relates to compounds of Formula I: | 11-22-2012 |
20120316174 | DISUBSTITUTED PHTHALAZINE HEDGEHOG PATHWAY ANTAGONISTS - The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer. | 12-13-2012 |
20120329801 | CRYSTALLINE FORMS FOR 5-AMINO-2, 3-DIHYDROPHTHALAZINE-1, 4-DIONE SODIUM SALT, PHARMACEUTICAL PREPARATIONS CONTAINING THE SAME AND METHOD FOR THE PRODUCTION OF SAID FORMS - The invention relates to the provision of two novel crystalline forms I and II for 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt. Surprisingly, it was discovered that form I and form II have differing immunological effects. This advantageous property is useful for immunospecific applications. In addition, both forms have advantageous physicochemical properties, which are useful in the production, further processing and/or use of a pharmaceutical preparation of form I or form II or a mixture of both. | 12-27-2012 |
20130012516 | 6-CYCLOAMINO-3-(PYRID-4-YL)IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): | 01-10-2013 |
20130018051 | BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. | 01-17-2013 |
20130040955 | 6-CYCLOALKYL-PYRAZOLOPYRIMIDINONES FOR THE TREATMENT OF CNS DISORDERS - The invention relates to novel pyrazolopyrimidinones according to formula (I). | 02-14-2013 |
20130045980 | IMIDAZOPYRIDAZINYL COMPOUNDS - Disclosed are imidazopyridazinyl compounds of Formula (I): (I), or pharmaceutically salts and prodrugs thereof, wherein R | 02-21-2013 |
20130072492 | SOLUBLE GUANYLATE CYCLASE ACTIVATORS - A compound of Formula (I): or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula (I) or a pharmaceutically acceptable salt thereof. | 03-21-2013 |
20130109695 | POLYCYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS | 05-02-2013 |
20130116258 | ANDROGEN RECEPTOR MODULATORS AND USES THEREOF - Described herein are compounds that are androgen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such androgen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon androgen receptors. | 05-09-2013 |
20130123265 | COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity. | 05-16-2013 |
20130123266 | TREATMENT OF A PATHOLOGY LINKED TO AN EXCESSIVE EFFECT OF TNF WITH A BENZENE SULPHONAMIDE COMPOUND - A benzene sulphonamide compound of formula I | 05-16-2013 |
20130131068 | PHTHALAZINONE KETONE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL USE THEREOF - A phthalazinone ketone derivative as represented by formula (I), a preparation method thereof, a pharmaceutical composition containing the derivative, a use thereof as a poly (ADP-ribose) polymerase (PARP) inhibitor, and a cancer treatment method thereof are described. | 05-23-2013 |
20130137693 | LISOFYLLINE ANALOGS AND METHODS FOR USE - Analogs of a Lisofylline (LSF), and synthetic methods for the preparation of such analogs are provided. The analogs of LSF provided have the ability to protect cell viability, particularly the ability to protect pancreatic β-cells. | 05-30-2013 |
20130137694 | NOVEL MODULATORS OF NRF2 AND USES THEREOF - There is provided modulators of Nrf2 protein which comprises a compound which binds at least one of the BTB domain, IVR domain and Kelch domain of Keap1 protein, activating or inhibiting Nrf2. There is also provided pharmaceutical compositions containing the modulators, as well as uses and method of use of the modulators for the treatment of conditions. | 05-30-2013 |
20130137695 | SUBSTITUTED 4-(4-FLUORO-3-(PIPERAZINE-1-CARBONYL)BENZYL)PHTHALAZIN-1(2H)-ONE DERIVATIVES AS POLY (ADP-RIBOSE) POLYMERASE-1 INHIBITORS - Disclosed are compounds of general formula (I), their stereoisomers, regioisomers, tautomeric forms and novel intermediates involved in their synthesis, their pharmaceutically acceptable salts. These compounds are suitable as Poly (ADP-ribose) polymerase-1 inhibitors (PARP-1 inhibitors). | 05-30-2013 |
20130143887 | NOVEL COMPOUNDS AND THERAPEUTIC USE THEREOF FOR PROTEIN KINASE INHIBITION - Novel compound having the following formula: | 06-06-2013 |
20130143888 | PHENOXYMETHYL HETEROCYCLIC COMPOUNDS - Phenoxymethyl compounds that inhibit at least one phosphodiesterase 10 are described as are pharmaceutical compositions containing such compounds an methods for treating various CNS disorders by administering such compounds to a patient in need thereof. | 06-06-2013 |
20130143889 | Heterocycles As Potassium Channel Modulators - Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-10 related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions. | 06-06-2013 |
20130165446 | BENZO-OR PYRIDO-IMIDAZOLE DERIVATIVE - The present invention addresses the problem of finding a compound having both PPAR activation activity and angiotensin receptor antagonistic activity. The present invention is a benzo- or pyrido-imidazole derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, or a ester or amide thereof (where A is biphenyl methyl-imidazolyl, biphenyl methyl-benzimidazolyl, or the like, B is divalent benzimidazolyl or the like, C is carboxyl or the like, E is divalent phenyl, naphthyl, or the like, G is a dangling bond, oxygen, or the like, Q is oxygen or sulfur, n is an integer from 1 to 6, p is an integer from 1 to 6, V is a dangling bond, oxygen, or the like, and R is hydrogen, alkyl, or the like). | 06-27-2013 |
20130190314 | DERIVATIVES OF 6-CYCLOAMINO-2-THIENYL-3-(PYRIDIN-4-YL)IMIDAZO[1,2-b]-PYRIDAZINE AND 6-CYCLOAMINO-2-FURANYL-3-(PYRIDIN-4-YL)IMIDAZO[1,2-b]-PYRIDAZINE, PREPARATION AND THERAPEUTIC USE THEREOF - The invention relates to derivatives of 6-cycloamino-2-thienyl-3-(pyridin-4-yl)imidazo[1,2-b]-pyridazine and 6-cycloamino-2-furanyl-3-(pyridin-4-yl)imidazo[1,2-b]-pyridazine with general formula (I). The invention also relates to a method for the preparation and therapeutic application thereof, in the treatment or prevention of illnesses involving casein kinase 1 epsilon and/or casein kinase 1 delta. | 07-25-2013 |
20130210825 | SUBSTITUTED IMIDAZO[1,2-B]PYRIDAZINES - The invention relates to imidazo[1,2-b]pyridazines of general formula (I) a process for their manufacuture and their use for the treatment of benign and malignant neoplasia. | 08-15-2013 |
20130217693 | COMPOUNDS AND METHOD FOR TREATMENT OF HIV - The invention relates to a compound of Formulae I and/or II: | 08-22-2013 |
20130225590 | SUBSTITUTED TRIAZOLO-PYRIDAZINE DERIVATIVES - This invention relates to novel substituted triazolo-pyridazines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an α1-GABA-A receptor antagonist and/or a α2, α3 and α5 GABA-A receptor agonist. | 08-29-2013 |
20130231343 | COMPOUNDS AND METHODS FOR TREATING MULTIPLE SCLEROSIS - The invention described herein pertains to the treatment of multiple sclerosis. In particular, the invention described herein pertains to the treatment of multiple sclerosis using compounds that modulate the action of acrolein. | 09-05-2013 |
20130245021 | IMIDAZO[1,2-b]PYRIDAZINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE - Imidazo[1,2-b]pyridazine-based compounds of the formula: | 09-19-2013 |
20130245022 | HETEROARYL-SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE - Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis). | 09-19-2013 |
20130245023 | 6-CYCLOAMINO-3-(PYRIDAZIN-4-YL)IMIDAZO[1,2-b]-PYRIDAZINE AND DERIVATIVES THEREOF PREPARATION AND THERAPEUTIC APPLICATION THEREOF - The invention relates to the 6-cycloamino-3-(pyridazin-4-yl)imidazo[1,2-b]pyridazine derivatives corresponding to general formula (I): | 09-19-2013 |
20130267521 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. | 10-10-2013 |
20130289037 | INHIBITORS OF E1 ACTIVTING ENZYMES - This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia. | 10-31-2013 |
20130296326 | SUSCEPTIBILITY OF TUMORS TO TYROSINE KINASE INHIBITORS AND TREATMENT THEREOF - This disclosure provides tyrosine kinase protein and nucleic acid variants, particularly FGFR2 variants, which are linked to drug resistance. The disclosure further provides methods of diagnosis and theranosis, using these molecules and fragments thereof, and kits for employing these methods and compositions. | 11-07-2013 |
20130310389 | SUBSTITUTED SPIROCYCLIC PIPERIDINE DERIVATIVES AS HISTAMINE-3 (H3) RECEPTOR LIGANDS - The present invention is directed to methods of treating disorders mediated by Histamine H | 11-21-2013 |
20130317033 | SUBSTITUTED TRIAZOLO-PYRIDAZINE DERIVATIVES - This invention relates to novel substituted triazolo-pyridazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an α1-GABA | 11-28-2013 |
20130324543 | REVERSAL OF HIGH BREAST CANCER RISK IN MAMMALS EXPOSED TO ESTROGENIC CHEMICALS IN UTERO BY ADULT EXPOSURE TO HDAC AND DNMT INHIBITORS - Methods of reducing breast cancer risk in an individual exposed in utero to an elevated estrogenic environment, where the individuals are identified by obtaining a measurement of at least one of: (a) DNMT1 expression; (b) methylation of normally unmethylated CpG islands of tumor suppressor genes; and (c) polycomb target genes, in cells obtained from the individual and comparing the measurement to a statistical level of a population not exposed in utero to an elevated estrogenic environment. Methods of reducing breast cancer risk in such an individual can be reduced by administering at least one DNA methyltransferase (DNMT) and/or histone deacetylase (HDAC) inhibitor. The administration of these inhibitors may be part of a treatment regime which may include the administration of at least one anti-cancer agent. | 12-05-2013 |
20130331393 | THERAPEUTIC FORMULATION AND METHODS OF TREATMENT - The present disclosure relates pharmaceutical formulations comprising hydralazine in the treatment of eye diseases and conditions with the formulations. The present disclosure also related to methods of preparing the pharmaceutical formulations. | 12-12-2013 |
20130338161 | AXL INHIBITORS FOR USE IN COMBINATION THERAPY FOR PREVENTING, TREATING OR MANAGING METASTATIC CANCER - This invention is directed to methods of preventing, treating or managing cancer, preferably metastatic cancer, in a patient. The methods comprise administering an effective amount of an Axl inhibitor in combination with the administration of an effective amount of one or more chemotherapeutic agents. | 12-19-2013 |
20130345225 | DIAZABENZO[DE] ANTHRACEN-3-ONE COMPOUNDS AND METHODS FOR INHIBITING PARP - The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein. | 12-26-2013 |
20140005198 | RAF KINASE MODULATORS AND METHODS OF USE | 01-02-2014 |
20140024652 | SUBSTITUTED TRIAZOLOPHTHALAZINE DERIVATIVES - This invention relates to novel substituted triazolophthalazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering selective α5 receptor partial or full inverse agonists. | 01-23-2014 |
20140031354 | Protein Kinase Inhibitors - The present invention relates to compounds of Formula I: | 01-30-2014 |
20140031355 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity. The present invention also enables methods for treating cancers that are mediated, dependent on or associated with pi 105 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 01-30-2014 |
20140031356 | THERAPY FOR LEUKEMIA - A pharmaceutically acceptable composition and method for leukemia therapy in a patient in need of such therapy. The composition contains, as the only active agents, the combination of (a) an inhibitor of c-Fos, (b) an inhibitor of Dusp-1, and (c) an inhibitor of BCR-ABL tyrosine kinase. The composition is administered to the patient in a dosing regimen for a period sufficient to provide therapy for leukemia. | 01-30-2014 |
20140031357 | ASYMMETRICALLY SUBSTITUTED ANTHRAPYRIDAZONE DERIVATIVES AS CYTOSTATICS - The invention relates to the new, asymmetrically substituted derivatives of 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-dione and their use as cytostatics exhibiting activity against tumor cells, especially against cells with multidrug resistance (MDR). In particular, the invention concerns derivatives of 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-dione represented by the general formula (I). | 01-30-2014 |
20140038969 | DIHYDROPYRIDONE P1 AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (VIII): | 02-06-2014 |
20140038970 | BRIDGED AND FUSED ANTIDIABETIC COMPOUNDS - This invention provides for certain bridged and fused compounds of the formula | 02-06-2014 |
20140045853 | MATERIALS, METHODS, AND SYSTEMS FOR TREATING CANCER - Aspects of the invention relate to methods of treatment, and to kits and systems for the same including materials for determining that an individual is susceptible to cancer and if warranted treating the patient of cancer or initiating a monitoring strategy and/or taking a preventive action. Therapeutic and preventive interventions include, treating the patient with a PARR inhibitors and/or laprascopic oophorectomy. The invention also relates to systems and methods of genotyping an individual, and to methods of identifying a patent with a higher than normal likelihood of developing cancer and/or genetically related individuals or groups at heighten risk for developing cancer, particularly ovarian cancer. | 02-13-2014 |
20140045854 | Methods and Compositions for the Treatment of Cancer and Related Hyperproliferative Disorders - The present invention relates to methods of treating a disease related to cell hyper-proliferation via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently. | 02-13-2014 |
20140066447 | IMMEDIATE RELEASE PHARMACEUTICAL FORMULATION OF 4-[3-(4-CYCLOPROPANECARBONYL-PIPERAZINE-1-CARBONYL)-4-FLUORO-BENZYL]-2H-P- HTHALAZIN-1-ONE - The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug. | 03-06-2014 |
20140066448 | SUBSTITUTED DIAMINO-PYRIMIDINE AND DIAMINO-PYRIDINE DERIVATIVES AS PI3K INHIBITORS - The present invention provides substituted diamino-pyrimidine and substituted diamino-pyridine derivatives of Formula I; wherein X, Y, R | 03-06-2014 |
20140080834 | INHIBITION OF ADAPTOR ASSOCIATED KINASE 1 FOR THE TREATMENT OF PAIN - This invention is directed to the treatment of pain by inhibiting adaptor associated kinase 1 (AAK1). Numerous AAK1 inhibitors are disclosed. | 03-20-2014 |
20140080835 | QUINAZOLINONE DERIVATIVES AS PARP INHIBITORS - The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) | 03-20-2014 |
20140088110 | FUSED BICYCLIC IMIDAZOLES - Compounds of formula (I) | 03-27-2014 |
20140094466 | SSH-2 (SLINGSHOT-2) INHIBITORS AND METHODS FOR MAKING AND USING THEM - In alternative embodiments, the invention provides compositions that inhibit the polypeptide SSH-2, or SlingSHot-2, a phosphatase enzyme that regulates actin filaments, and methods for making and using them, including methods comprising administering compositions of the invention to regulate or modify actin filament polymerization by inhibiting SSH-2, where in one embodiment compositions of the invention slow or inhibit F-actin depolymerization and severing. In alternative embodiments, compositions and methods of the invention are used to slow or inhibit cell motility and/or internal remodeling. In alternative embodiments, compositions and methods of the invention are used to slow or inhibit, or reverse, or ameliorate the progression of a cancer or a metastasis or other uncontrolled or unregulated cell growth, and/or Alzheimer's disease. | 04-03-2014 |
20140100231 | NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - Compounds of Formula I: | 04-10-2014 |
20140113901 | IMIDAZOPYRIDAZINES AS AKT KINASE INHIBITORS - Imidazopyridazines of formula (I) a process for their production and the use thereof. | 04-24-2014 |
20140113902 | METHOD FOR OBTAINING 5-AMINO-2,3-DIHYDROPHTHALAZINE-1,4-DIONE ALKALI METAL SALTS AND THEIR USE IN MEDICINE - A method for preparing 5-amino-2,3-dihydrophthalazine-1,4-dione salts with alkali metals of the formula II, pharmaceutical compositions including such salts, and their application in medicine. The sodium salt may be used for treatment of heart diseases, pancreas diseases and diabetes as well as optionally in combination with lithium salt for treatment of the nervous system diseases. | 04-24-2014 |
20140128400 | BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. | 05-08-2014 |
20140128401 | 8-FLUOROPHTHALAZIN-1(2H)-ONE COMPOUNDS - 8-Fluorophthalazin-1(2h)-one compounds of Formula I where one or two of X | 05-08-2014 |
20140135336 | TRIAZOLOPYRIDAZINE - Disclosed are compounds of general formula (I) | 05-15-2014 |
20140155404 | PIPERAZINYLPIPERIDINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS - The present invention relates to compounds of Formula I: | 06-05-2014 |
20140163034 | INHIBITORS OF ANANDAMIDE TRANSPORT AND THEIR THERAPEUTIC USES - Nucleic acid and polypeptide sequences corresponding to FLAT, a partly cytosolic variant of the intracellular anandamide-degrading enzyme, fatty acid amide hydrolase-1 (FAAH-1), are provided. FLAT lacks amidase activity but binds the endocannibinoid anandamide and facilitates its transport into cells. A chemical scaffold for the inhibition of anandamide transport is identified. Compositions of the invention prevent anandamide internalization in vitro, interrupt anandamide deactivation in vivo, and cause profound CB | 06-12-2014 |
20140163035 | HETEROCYCLIC AMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS - The invention relates to heterocyclic amide derivatives of formula (I), wherein R | 06-12-2014 |
20140171435 | Chemical Compounds - The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I): | 06-19-2014 |
20140194430 | SUBSTITUTED AMINOIMIDAZOPYRIDAZINES - The present invention relates to substituted aminoimidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients. | 07-10-2014 |
20140206693 | COMPOSITIONS AND METHODS FOR TREATING COLON CANCER - Certain embodiments are directed to methods of treating a pathophysiological state or symptoms thereof resulting from aldose reductase-mediated signaling in a cytotoxic pathway using an aldose reductase specific inhibitor. | 07-24-2014 |
20140213592 | Protein Kinase Inhibitors (Variants), Use Thereof in Treating Oncological Diseases and a Pharmaceutical Composition Based Thereon - The present invention relates to the treatment of oncological, chronic inflammatory and similar diseases with the aid of new families of chemical compounds having improved efficiency with regard to the inhibition of Abl kinase and mutant forms thereof, as well as other therapeutically significant kinases. It describes protein kinase inhibitors in the form of compounds of general formula (I) and compounds of general formula (II), or a tautomer, an individual isomer, a mixture of isomers, a pharmaceutically acceptable salt, a solvate or a hydrate thereof. | 07-31-2014 |
20140249150 | ACTIVATORS OF PYRUVATE KINASE M2 AND METHODS OF TREATING DISEASE - The invention described herein features methods, compositions, and kits that utilize activators of pyruvate kinase M2 (PKM2) for the treatment or amelioration of disorders related to PKM2 function and characterized by abnormally low levels of serine. | 09-04-2014 |
20140249151 | BICYCLIC HETEROCYCLIC COMPOUND - [Problem] To provide a compound useful as an active ingredient of a pharmaceutical composition for treating 11β-hydroxysteroid dehydrogenase type 1-related diseases such as dementia, schizophrenia, depression, pain (particularly, neuropathic pain or fibromyalgia), diabetes (particularly, type II diabetes mellitus), insulin resistance and the like. | 09-04-2014 |
20140256733 | MIXED LINEAGE KINASE INHIBITORS AND METHOD OF TREATMENTS - Provided herein are imidazopyridine compounds having an inhibitory effect on mixed lineage kinases (MLKs), methods of their synthesis, and methods of their therapeutic. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and pharmaceutical compositions. | 09-11-2014 |
20140296243 | BROMODOMAIN INHIBITORS AND USES THEREOF - The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders. | 10-02-2014 |
20140303168 | PHTHALAZINES AS POTASSIUM ION CHANNEL INHIBITORS - A compound of formula (I) | 10-09-2014 |
20140303169 | Crystalline forms for 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt, pharmaceutical preparations containing the same and method for the production of said forms - The invention relates to the provision of two novel crystalline forms I and II for 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt. Surprisingly, it was discovered that form I and form II have differing immunological effects. This advantageous property is useful for immunospecific applications. In addition, both forms have advantageous physicochemical properties, which are useful in the production, further processing and/or use of a pharmaceutical preparation of form I or form II or a mixture of both. | 10-09-2014 |
20140323489 | HYBRID NECROPTOSIS INHIBITORS - The present invention relates to heterocyclic compounds (e.g., compounds described by Formula (I)) and pharmaceutically acceptable salts thereof. The invention also features pharmaceutical compositions that include these compounds and their use in therapy for treating conditions in which necroptosis is likely to play a substantial role. The heterocyclic compounds described herein can also achieve improved activity and selectivity towards RIP1 and/or RIP3. | 10-30-2014 |
20140323490 | POLYCYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. | 10-30-2014 |
20140336195 | ARYLOXMETHYL CYCLOPROPANE DERIVATIVES AS PDE10 INHIBITORS - The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 11-13-2014 |
20140343065 | New Somatostatin receptor subtype 4 (SSTR4) agonists - 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4. | 11-20-2014 |
20140357638 | COMPOSITIONS AND METHODS FOR TREATING ALZHEIMER'S DISEASE - The present invention provides compositions for reducing amyloid plaque burden associated with Alzheimer's disease and methods of using the same. | 12-04-2014 |
20140364434 | Biomarkers for Prediction of Response to PARP Inhibition in Breast Cancer - Methods and systems for identifying a cancer patient suitable for treatment with a PARP inhibitor. A 6-gene, 7-gene and 8-gene predictor panels of genes that are predictive of patient resistance or sensitivity to PARP inhibitors such as Olaparib. | 12-11-2014 |
20140364435 | AMINO-SUBSTITUTED IMIDAZOPYRIDAZINES - The present invention relates to amino-substituted imidazopyndazine compounds of general formula (I): in which A, R1, R2, R3, R4 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients. | 12-11-2014 |
20140364436 | Protein Kinase Inhibitors - The present invention relates to compounds of Formula VIII with absolute configuration R or S: | 12-11-2014 |
20140371225 | PYRIDAZINONE COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS - The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I to a patient in need thereof: | 12-18-2014 |
20140378462 | TRICYCLIC SULFONAMIDE COMPOUNDS AND METHODS OF MAKING AND USING SAME - The invention provides tricyclic sulfonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2. | 12-25-2014 |
20150018356 | FUSED TETRA OR PENTA-CYCLIC PYRIDOPHTHALAZINONES AS PARP INHIBITORS - Provided are certain fused tetra or penta-cyclic compounds and salts thereof, compositions thereof, and methods of use thereof. | 01-15-2015 |
20150045368 | OXAZOLIDINONE COMPOUNDS AND DERIVATIVES THEREOF - Compounds of Formula (I) and Formula (II) are useful inhibitors of tankyrase. Compounds of Formula (I) and Formula (II) have the following structure: where the definitions of the variables are provided herein. | 02-12-2015 |
20150045369 | NOVEL MARKERS FOR DETECTING MICROSATELLITE INSTABILITY IN CANCER AND DETERMINING SYNTHETIC LETHALITY WITH INHIBITION OF THE DNA BASE EXCISION REPAIR PATHWAY - Described are mismatch repair (MMR-)deficient tumors. Markers are presented herein having a high sensitivity to detect whether a tumor is mismatch repair deficient or not. The markers are particularly mutations in microsatellite regions. Accordingly, methods and materials are provided for diagnosing microsatellite instability of a tumor. Such a method comprises determining the presence of these markers. Further, kits are provided to detect the presence of these markers (or subsets thereof) in a sample. | 02-12-2015 |
20150051211 | POLY (ADP-RIBOSE) POLYMERASE INHIBITOR - Disclosed are a phthalic hydrazide (phthalazine ketone) compound, and a pharmaceutical composition comprising the same. As a DNA repair enzyme poly (ADP-ribozyme) polymerase inhibitor, the compound and the pharmaceutical composition can effectively treat diseases involving PARP enzymatic activity, including cancer, neural degenerative diseases, inflammation and the like. | 02-19-2015 |
20150051212 | Compositions And Methods For Inhibiting Drusen - Described herein are methods for inhibiting drusen. | 02-19-2015 |
20150065509 | HIGHLY 6-SUBSTITUTED -2,4-DIAMINOPYRIMIDINES AS INHIBITORS OF ANTHRAX - 2,4-diaminopyrimidine compounds of generic Formula 1, where R and R′ may be the same or different and are independently selected from: C | 03-05-2015 |
20150065510 | Rilyazine Derivatives and Compositions for The Treatment of Cancer - The present application discloses Rilyazine analogs, methods for their preparation, and the treatment of cancer by the administration of an effective amount of the Rilyazine analogs to a patient in need thereof. | 03-05-2015 |
20150072987 | NOVEL COMPOUNDS AND THERAPEUTIC USE THEREOF FOR PROTEIN KINASE INHIBITION - Novel compound having the following formula: | 03-12-2015 |
20150072988 | USE OF N-(4-((3-(2-AMINO-4-PYRIMIDINYL)-2-PYRIDINYL)OXY)PHENYL)-4-(4-METHY- L-2-THIENYL)-1-PHTHALAZINAMINE IN COMBINATION WITH HISTONE DEACETYLASE INHIBITORS FOR TREATMENT OF CANCER - The present invention relates to methods of using AMG 900, a small molecule pan aurora kinase inhibitor, in combination with histone deacetylase (HDAC) inhibitor for the treatment of cancer, including solid tumors, hematologically derived tumors and the like. The invention further provides pharmaceutical compositions for administering the cancer therapeutic agents in combination. | 03-12-2015 |
20150099753 | FORM 5 POLYMORPH OF 7-(TERT-BUTYL-D9)-3-(2,5-DIFLUOROPHENYL)-6-((1-METHYL-1H-1,2,4-TRIAZOL-5-- YL)METHOXY)-[1,2,4]TRIAZOLO[4,3-B]PYRIDAZINE - The present invention provides individual crystalline polymorphs of 7-(tert-Butyl-d9)-3-(2,5-difluorophenyl)-6-((1-methyl-1H-1,2,4-triazol-5-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine designated Form 5. The Form 5 polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data (“XRPD”); (b) differential scanning calorimetry (“DSC”); (c) FT-Raman spectroscopy; (d) FT-IR spectroscopy; and (e) thermogravimetric analysis (TGA). | 04-09-2015 |
20150105394 | CYCLOLIC HYDRAZINE DERIVATIVES AS HIV ATTACHMENT INHIBITORS - Compounds of Formula I are provided, including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: wherein Z is selected from the group consisting of: which are useful as HIV attachment inhibitors. | 04-16-2015 |
20150105395 | ACTIVATORS OF HUMAN PYRUVATE KINASE - Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R | 04-16-2015 |
20150105396 | Chemical Compounds - The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I): | 04-16-2015 |
20150111894 | AROMATIC RING COMPOUND - The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula | 04-23-2015 |
20150111895 | SUBSTITUTED TRIAZOLO-PYRIDAZINE DERIVATIVES - This invention relates to novel substituted triazolo-pyridazines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an α1-GABA-A receptor antagonist and/or a α2, α3 and α5 GABA-A receptor agonist. | 04-23-2015 |
20150119398 | FORM 2 POLYMORPH OF 7-(TERT-BUTYL-D9)-3-(2,5-DIFLUOROPHENYL)-6-((1-METHYL-1H-1,2,4-TRIAZOL-5-- YL)METHOXY)-[1,2,4]TRIAZOLO[4,3-B]PYRIDAZINE - The present invention provides the Form 2 crystalline polymorph of 7-(ieri-Butyl-d9)-3-(2,5-difluorophenyl)-6((1-methyl-1H-1,2,4-triazol-5-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine. The polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data (“XRPD”); (b) differential scanning calorimetry (“DSC”); (c) FT-Raman spectrum; (d) FT-IT spectrum; and (e) thermogravimetric analysis (TGA). | 04-30-2015 |
20150126513 | 4-PIPERIDINYL COMPOUNDS FOR USE AS TANKYRASE INHIBITORS - The present invention provides for compounds of formula (I): | 05-07-2015 |
20150126514 | BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. | 05-07-2015 |
20150148349 | COMPLEMENT PATHWAY MODULATORS AND USES THEREOF - The present invention provides a compound of formula (I): a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 05-28-2015 |
20150291525 | INHIBITORS OF BRUTON'S TYROSINE KINASE - This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient. | 10-15-2015 |
20150291599 | AMINOIMIDAZOPYRIDAZINES - The present invention relates to amino-substituted imidazopyridazine compounds of general formula (I), in which A, R1, R2, R3, R4 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients. | 10-15-2015 |
20150291603 | SUBSTITUTED PHTHALAZIN-1 (2H)-ONE DERIVATIVES AS SELECTIVE INHIBITORS OF POLY (ADP-RIBOSE) POLYMERASE-1 - The present invention relates to novel compounds of general formula (I), their stereoisomers, regioisomers, tautomeric forms and novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them. The present invention also relates to a process of preparing novel compounds of general formula (I), their stereoisomers, regioisomers, their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis. | 10-15-2015 |
20150307495 | Use of Kinase Inhibitors to Increase the Susceptibility of Gram Positive Bacteria to Beta Lactam Antibiotics - Methods of using certain kinase inhibitors for treating Gram positive bacterial infections are disclosed. When co-administered with a β-lactam antibiotic, the disclosed compounds increase the susceptibility of infectious Gram positive bacteria to the β-lactam antibiotic. | 10-29-2015 |
20150307501 | Compositions and Methods for the Treatment of Metabolic and Related Disorders - The present invention relates to the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. Also provided are methods for the treatment and/or prevention of one or more metabolic disorders, for example, obesity or diabetes, utilizing fatostatin A and/or a derivative and/or analog thereof and/or the A-B-C tripartite compounds. | 10-29-2015 |
20150315188 | COMPOUNDS AND METHODS FOR TREATMENT OF HYPERTENSION - Hydrogenated pyrido[4,3-b]indoles and pyrido[3,4-b]indoles are described. The compounds may bind to and are adrenergic receptor α | 11-05-2015 |
20150315194 | CRYSTALLINE FORMS OF 3-(IMIDAZO[1,2-B] PYRIDAZIN-3-YLETHYNYL)-4-METHYL-N-BENZAMIDE AND ITS MONO HYDROCHLORIDE SALT - Novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyljbenzamide free base and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methyl piperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, pharmaceutical compositions thereof and methods of their preparation and use are disclosed herein. The instant application is directed to novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl}phenyl}benzamide and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, compositions comprising such crystalline forms, and to methods of their preparation and use. | 11-05-2015 |
20150368250 | IMIDAZOPYRIDAZINES AS AKT KINASE INHIBITORS - Imidazopyridazines of formula (I) | 12-24-2015 |
20150374696 | WNT PROTEIN SIGNALLING INHIBITORS - The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis. | 12-31-2015 |
20150376189 | AMIDOIMIDAZOPYRIDAZINES AS MKNK-1 KINASE INHIBITORS - The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I): in which A, R1, R2, R3, R4 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients. | 12-31-2015 |
20150376206 | MACROCYCLIC PYRIDAZINONE DERIVATIVES - The present invention relates to compounds of formula (I) Wherein R1, R2, R3, R4, L and Z have the meaning given in claim | 12-31-2015 |
20160002250 | POLYMORPHS AND SALTS OF A COMPOUND - Disclosed are novel crystalline polymorphic forms of 4-(4-(imidazo[1,2-b]pyridazin-2-ylmethoxy)phenyl)-2,2-dimethyl-5-(pyridin-4-yl)furan-3(2H)-one and salts thereof, methods of preparing the crystalline polymorphic forms and salts thereof, pharmaceutical compositions comprising the crystalline polymorphic forms and salts thereof, and methods of treating CNS disorders, eating disorders, obesity, compulsive gambling, sexual disorders, narcolepsy, sleep disorders, diabetes, metabolic syndrome, schizophrenia, schizo-affective conditions, Huntington's disease, bipolar disorders, dystonic conditions and tardive dyskinesia, or for use in smoking cessation treatment in a patient using the crystalline polymorphic forms and salts thereof. | 01-07-2016 |
20160008364 | METHODS FOR TREATING NEUROLOGIC DISORDERS | 01-14-2016 |
20160008473 | IMMEDIATE RELEASE PHARMACEUTICAL FORMULATION OF 4-[3-(4-CYCLOPROPANECARBONYL-PIPERAZINE-1-CARBONYL)-4-FLUORO-BENZYL]-2H-P- HTHALAZIN-1-ONE | 01-14-2016 |
20160016961 | PYRROLOPYRIDAZINES AS POTASSIUM ION CHANNEL INHIBITORS - A compound of formula (I) wherein A, R | 01-21-2016 |
20160021886 | CONDENSED HETEROCYCLIC COMPOUND OR SALT THEREOF, AGRICULTURAL AND HORTICULTURAL INSECTICIDE COMPRISING THE COMPOUND, AND METHOD FOR USING THE INSECTICIDE - An object of the present invention is to provide and develop novel agricultural and horticultural insecticides in view of the still immense damage caused by insect pests etc. and the emergence of insect pests resistant to existing insecticides in crop production in the fields of agriculture, horticulture and the like. | 01-28-2016 |
20160022674 | COMBINATION THERAPY WITH GLUTAMINASE INHIBITORS - The invention relates to methods of treating cancer, myeloproliferative diseases, or immunological or neurological diseases with a combination of a glutaminase inhibitor and an anticancer agent such as an enzyme inhibitor (such as a kinase inhibitor), a mitotic inhibitor, a DNA-modifying agent, or a cytidine analog. The invention further relates to methods of treating cancer, myeloproliferative diseases, or immunological or neurological diseases that are resistant to one or more anticancer agents. | 01-28-2016 |
20160024098 | HYBRID NECROPTOSIS INHIBITORS - The present invention relates to heterocyclic compounds (e.g., compounds described by Formula (I)) and pharmaceutically acceptable salts thereof. The invention also features pharmaceutical compositions that include these compounds and their use in therapy for treating conditions in which necroptosis is likely to play a substantial role. The heterocyclic compounds described herein can also achieve improved activity and selectivity towards RIP1 and/or RIP3. | 01-28-2016 |
20160024113 | MACROCYCLIC SALT-INDUCIBLE KINASE INHIBITORS - The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of SIK kinase, more in particular SIK1, SIK2 and/or SIK3 and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of SIK-kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent. | 01-28-2016 |
20160030431 | COMPOSITIONS AND METHODS FOR TREATING ALZHEIMER'S DISEASE - The present invention provides compositions for reducing amyloid plaque burden associated with Alzheimer's disease and methods of using the same. | 02-04-2016 |
20160031905 | Macrocyclic LRRK2 Kinase Inhibitors - The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of LRRK2 kinase, for use in the diagnosis, prevention and/or treatment of LRRK2-kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent. Finally, the present invention also relates to new macrocyclic compounds. | 02-04-2016 |
20160038489 | ANTI-INFLAMMATORY PHARMACEUTICAL COMPOSITION COMPRISING BENZOPYRANYL TETRACYCLES - Disclosed herein is an anti-inflammatory pharmaceutical composition comprising a benzopyranyl tetracycle compound represented by Chemical Formula 1 as an active ingredient. The compound exhibits excellent anti-inflammatory activity by perturbing the post-translational modification of the inflammation mediator HMGB, and thus finds applications in pharmaceutical compositions superior in the treatment or prevention of inflammation-related diseases. | 02-11-2016 |
20160038492 | Targeted Therapies for Cancer - Methods of selecting a chemotherapy regimen for treatment of cancer in a patient are disclosed. A patient genetic sample from a bilary cancer such as cholangiocarcinoma is analyzed for a mutation in ERRFI1 and a chemotherapeutic agent is selected as a result of the analysis. If a mutation in ERRFI1 is present, treatment with an inhibitor of Epidermal Growth Factor Receptor (EGFR) is shown to have inhibitory effects on tumor growth. In this manner, the chemotherapy regimen is targeted to a given mutation in a patient's cancer. | 02-11-2016 |
20160083376 | CERTAIN PROTEIN KINASE INHIBITORS - Disclosed herein are protein kinase inhibitors, more particularly pyridazine derivatives and pharmaceutical compositions thereof, and method of use thereof. | 03-24-2016 |
20160090632 | METHODS FOR DETECTING ONCOGENIC MUTATIONS - Provided herein are methods for the detection of genetic mutations associated with cancer, particularly in the KIT gene. | 03-31-2016 |
20160096839 | PYRIMIDINONES AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I): | 04-07-2016 |
20160102100 | FUSED HETEROCYCLIC COMPOUND - The fused heterocyclic compound represented by formula (1) has excellent effectiveness in pest control. | 04-14-2016 |
20160102107 | PYRAZOLO-PYRROLIDIN-4-ONE DERIVATIVES AS BET INHIBITORS AND THEIR USE IN THE TREATMENT OF DISEASE - The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 04-14-2016 |
20160106751 | SMALL MOLECULAR INHIBITORS OF RAD51 RECOMBINASE AND METHODS THEREOF - The invention includes compositions comprising a selective small-molecule inhibitor of RAD51 recombinase and a pharmaceutically acceptable carrier. The invention further includes methods of treating or preventing cancer in a subject, comprising the step of administering to the subject the compositions contemplated within the invention. | 04-21-2016 |
20160108049 | Novel Phthalazinone-Pyrrolopyrimidinecarboxamide Derivatives - The compounds of formula (1), in which R1, R7, R8, R9, R10, R17, R18, R19, R20 and m have the meanings as given in the description, are novel effective inhibitors of type 4 and 5 phosphodiesterase. | 04-21-2016 |
20160136164 | Methods and Compositions for the Treatment of Cancer and Related Hyperproliferative Disorders - The present invention relates to methods of treating a disease related to cell hyper-proliferation via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B—C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently. | 05-19-2016 |
20160137646 | Novel Compounds and Uses Thereof - The present invention provides novel compounds of any one of Formulae (I)-(IV), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of any one of Formulae (I)-(IV) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor signaling pathway (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof. | 05-19-2016 |
20160138114 | Biomarkers of Response to Inhibition of Poly-ADP Ribose Polymerase (PARP) in Cancer - Provided herein are methods of identifying a subject having a poly-ADP ribose polymerase (PARP) inhibitor-sensitive tumor by detecting a genomic gain in chromosome 1q21 and/or chromosome 20q13.3 in a tumor sample from the subject. Also provided are methods of identifying a subject having a PARP inhibitor-sensitive tumor by detecting gene amplification of a CHD1L gene or an RTEL1 gene in a tumor sample from the subject. Further provided are methods of treating a tumor with a genomic gain in chromosome 1q21 and/or chromosome 20q13.3 in a subject by administering an effective dose of a PARP inhibitor. | 05-19-2016 |
20160145255 | NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - Compounds of Formula I: | 05-26-2016 |
20160151368 | THERAPEUTIC FORMULATION AND METHODS OF TREATMENT | 06-02-2016 |
20160199372 | IMIDAZOPYRIDAZINE KINASE INHIBITORS USEFUL TO TREATING A DISEASE OR DISORDER MEDIATED BY AAK1, SUCH AS ALZHEIMER'S DISEASE, BIPOLAR DISORDER, PAIN, SCHIZOPHRENIA | 07-14-2016 |
20160199373 | COMPOSITIONS AND METHODS FOR TREATMENT OF FRAGILE X SYNDROME | 07-14-2016 |
20160200719 | CINNOLINE DERIVATIVES USEFUL AS CB-1 RECEPTOR INVERSE AGONISTS | 07-14-2016 |
20160251729 | ncRNA AND USES THEREOF | 09-01-2016 |
20190144445 | PESTICIDALLY ACTIVE POLYCYCLIC DERIVATIVES WITH SULFUR CONTAINING SUBSTITUENTS | 05-16-2019 |
20190144449 | (HETERO)ARYL-SUBSTITUTED-PIPERIDINYL DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM | 05-16-2019 |