Entries |
Document | Title | Date |
20080214545 | Substituted Pyrazolyl Urea Derivatives Useful in the Treatment of Cancer - The present invention relates to compounds of formula (I), pharmaceutical compositions which contain them and methods for treating cancer using compounds of formula (I). | 09-04-2008 |
20080249095 | 1-Acyldihydropyrazole Derivatives - Compounds of the formula (I), in which R | 10-09-2008 |
20080293719 | Pyridiazinone Derivatives for the Treatment of Tumours - Compounds of the formula (I), in which R | 11-27-2008 |
20080306068 | Kinase Inhibitors - The present invention provides kinase inhibitors of Formula I: | 12-11-2008 |
20080306069 | Pyrazole Derivatives for the Inhibition of CDK'S and GSK'S - The invention provides compounds of the formula (I), or salts, tautomers, N-oxides or solvates thereof wherein: R1 is selected from: (a) 2,6-dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents for the phenyl group are selected from fluorine, chlorine, methyl and methoxy; (d) a group RO; (e) a group R a; (f) a group RIb; (g) a group RIc; (h) a group RId; and 0) 2,6-difluorophenylamino; wherein R) 0υ, r R>llaa, T Rj HbD, T R) HcC, r R>Iidα, r R>>2zaa, r R>22bD and RJ are as defined in the claims. The compounds have activity as inhibitors of cdk kinase (such as cdk1 or cdk2) and glycogen synthase kinase-3 activity. | 12-11-2008 |
20090012088 | Compounds for the Treatment of Neurodegeneration and Stroke - Compounds and related methods for synthesis, and the use of compounds for the treatment of neurodegenerative diseases are disclosed. Compounds are disclosed in connection with PARG and/or PARP inhibition. Therapeutic applications are relevant for preventing or inhibiting neurological cell death for a variety of neurodegenerative conditions including Parkinson's disease, ischemia, and stroke. Also disclosed is a high-throughput screen for identifying compounds capable of inhibiting PARG and/or PARP. | 01-08-2009 |
20090029996 | Pyridazin-3(2H)-One Derivatives And Their Use As Pde4 Inhibitors - The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives, to processes for their preparation and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatment, prevention and suppression of related pathological conditions, diseases and disorders, in particular asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, topic dermatitis, psoriasis or irritable bowel disease. | 01-29-2009 |
20090029997 | Thiazole Derivatives and Use Thereof - The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries. | 01-29-2009 |
20090036449 | Indazolesquaric Acid Derivatives as Chk1, Chk2 and Sgk Inhibitors - Novel squaric acid compounds of the formula (I), in which R, R1, R2, R2′, R2″, R3, B, B′ and X have the meanings indicated in Claim | 02-05-2009 |
20090036450 | PYRAZOLE COMPOUNDS AND USE THEREOF - The pyrazole compound of the present invention is represented by the following general formula (I). The pyrazole compound of the present invention or a salt thereof or a solvate thereof potently inhibits liver glycogen phosphorylase, and, therefore, is useful as a therapeutic or prophylactic agent for diabetes. | 02-05-2009 |
20090042884 | Pharmaceutical Compounds - Pyrimidines of formula (I): | 02-12-2009 |
20090048256 | Pyrazole Compounds Having Cannabinoid Receptor (CB1) Antagonizing Activity - The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: | 02-19-2009 |
20090069329 | CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING OBESITY - The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders. | 03-12-2009 |
20090088431 | Heteroaromatic Compounds as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase - Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; lipid disorders; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; fatty liver disease and cancer. | 04-02-2009 |
20090105254 | VHR PROTEIN TYROSINE PHOSPHATASE INHIBITORS, COMPOSITIONS AND METHODS OF USE - Disclosed herein are | 04-23-2009 |
20090118287 | ORGANIC COMPOUNDS - The present invention provides a compound of formula (I): | 05-07-2009 |
20090124621 | PYRAZOLE DERIVATIVES AS KINASE INHIBITORS - The present invention provides compounds having the general structure I, or a pharmaceutically acceptable salt thereof: | 05-14-2009 |
20090137591 | COMPOUNDS AND COMPOSITIONS AS PPAR MODULATORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPARδ. | 05-28-2009 |
20090143385 | ISOXAZOLO-PYRIDAZINE DERIVATIVES - The invention relates to isoxazolo-pyridazine compounds, in particular those of formula I as described above and to a pharmaceutically acceptable salts thereof, having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the treatment of cognitive disorders like Alzheimer's disease. | 06-04-2009 |
20090149463 | Therapeutic agents - The present invention relates to compounds of formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them. | 06-11-2009 |
20090163503 | SUBSTITUTED PYRROLO-PYRAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer. | 06-25-2009 |
20090170852 | NOVEL PYRAZOLE-BASED HMG CoA REDUCTASE INHIBITORS - Novel compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents are described. More specifically, potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (“HMG CoA reductase”) are described. Methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, Alzheimer's Disease, benign prostatic hypertrophy (BPH), diabetes and osteoporosis are also described. | 07-02-2009 |
20090186895 | ETHERS, SECONDARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together. | 07-23-2009 |
20090197885 | COMPOSITIONS AND TREATMENTS USING PYRIDAZINE COMPOUNDS AND CHOLINESTERASE INHIBITORS - The invention relates to compositions, conjugates and methods comprising pyridazine compounds and cholinesterase inhibitors for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications. | 08-06-2009 |
20090197886 | HEXAHYDRO-CYCLOHEPTAPYRAZOLE CANNABINOID MODULATORS - This invention is directed to a hexahydro-cycloheptapyrazole cannabinoid modulator compound of formula (I): | 08-06-2009 |
20090247525 | SIGMA RECEPTOR INHIBITORS - The invention relates to compounds of formula I | 10-01-2009 |
20090281102 | THERAPEUTIC N-ARYL OR N-HETEROARYL PYRAZOLIDINE AND PYRAZOLIDINONE DERIVATIVES - Compounds comprising | 11-12-2009 |
20090286791 | Amide Compounds - The present invention provides compounds represented by the formula (Ia): | 11-19-2009 |
20090312327 | PYRROLIDINE DERIVATIVES AS NK2 RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula I | 12-17-2009 |
20090325958 | METHOD FOR TREATING PULMONARY DISEASES USING RHO KINASE INHIBITOR COMPOUNDS - This invention is directed to methods of preventing or treating diseases or conditions of the lungs associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema. Particularly, this invention is directed to methods of treating pulmonary diseases such as asthma; chronic obstructive pulmonary disease; respiratory tract illness caused by respiratory syncytial virus; pulmonary arterial hypertension; acute respiratory distress syndrome and ventilator induced lung injury; cystic fibrosis; bronchiectasis; alpha-1-antitrypsin deficiency; rhinitis; rhinosinusitis; primary ciliary dyskinesia; pneumonia; bronchiolitis caused by agents other than respiratory syncytial virus; and interstitial lung disease including lymphangioleiomyomatosis; idiopathic pulmonary fibrosis; obliterative bronchiolitis or bronchiolitis obliterans organizing pneumonia due to lung transplantation or HSCT; nonspecific interstitial pneumonia; cryptogenic organizing pneumonia; acute interstitial pneumonia; respiratory bronchiolitis-associated interstitial lung disease; or pulmonary sarcoidosis. The method comprises administering to a subject an effective amount of a rho kinase inhibitor compound to treat the disease. | 12-31-2009 |
20090325959 | METHOD FOR TREATING OPHTHALMIC DISEASES USING RHO KINASE INHIBITOR COMPOUNDS - This invention is directed to methods of preventing or treating ocular diseases with inflammation, excessive cell proliferation, remodeling, neurite retraction, corneal neurodegeneration, excessive vaso-permeability and edema. Particularly, this invention relates to methods treating ocular diseases such as allergic conjunctivitis, corneal hyposensitivity, neurotrophic keratopathy, dry eye disease, proliferative vitreal retinopathy, macular edema, macular degeneration, and blepharitis, using novel Rho kinase inhibitor compounds. The method comprises identifying a subject in need of the treatment, and administering to the subject an effective amount of a novel Rho kinase inhibitor compound to treat the disease. | 12-31-2009 |
20090325960 | METHOD FOR TREATING INFLAMMATORY DISEASES USING RHO KINASE INHIBITOR COMPOUNDS - This invention is directed to methods of preventing or treating diseases or conditions associated with excessive cell proliferation, remodeling, edema and inflammation. Particularly, this invention is directed to methods of treating inflammatory diseases or conditions such as rheumatoid arthritis and inflammatory bowel disease. The method comprises identifying a subject in need of the treatment, and administering to the subject an effective amount of a compound of a novel rho kinase inhibitor compound to treat the disease. | 12-31-2009 |
20100004243 | PHARMACEUTICAL COMPOUNDS - The invention provides a cyclin dependent kinase (e.g. cdk-4 kinase) inhibitor of the formula (I) or a salt, tautomer, solvate or N-oxide thereof; wherein R | 01-07-2010 |
20100016319 | ARYLMETHYLENE UREA DERIVATIVE AND USE THEREOF - This invention relates to a pharmaceutical comprising as an effective ingredient an arylmethylene urea exemplified by the following formula: | 01-21-2010 |
20100016320 | ARYL-SUBSTITUTED PYRAZOLE-AMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS - The present invention relates to compounds having the formula, | 01-21-2010 |
20100029651 | ARYL-SUBSTITUTED HETEROCYCLES, AND USE THEREOF - The invention relates to aryl-substituted heterocycles, 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. | 02-04-2010 |
20100041656 | Novel amide derivatives and medicinal use thereof - The present invention relates to an amide derivative of the formula (1), having a C5a receptor antagonistic action | 02-18-2010 |
20100056527 | BENZOFURAN COMPOUNDS USEFUL IN THE TREATMENT OF CONDITIONS MEDIATED BY THE ACTION OF PGE2 AT THE EP1 RECEPTOR - A compound of formula (I): | 03-04-2010 |
20100063050 | NOVEL HETEROPYRROLE ANALOGS ACTING ON CANNABINOID RECEPTORS - Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect. | 03-11-2010 |
20100063051 | MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF - Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g. a hydrate), or a pharmaceutically-acceptable salt, thereof, wherein: M is selected from alkyl, substituted alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl, provided that if M is alkyl then R | 03-11-2010 |
20100063052 | USE OF SERUM AMYLOID A GENE IN DIAGNOSIS AND TREATMENT OF GLAUCOMA AND IDENTIFICATION OF ANTI-GLAUCOMA AGENTS - The present invention provides compositions and methods for treating glaucoma, methods for diagnosing glaucoma, and methods for identifying agents which may be useful in the treatment of glaucoma. More specifically, the present invention describes the use of agents that modulate the expression of serum amyloid A. | 03-11-2010 |
20100081659 | SIGMA RECEPTOR INHIBITORS - The invention relates to compounds of formula IV | 04-01-2010 |
20100105684 | HETEROCYCLYL-SUBSTITUTED-TETRAHYDRO-NAPHTHALEN-AMINE DERIVATIVES, THEIR PREPARATION AND USE AS MEDICAMENTS - The present invention relates to heterocyclyl-substituted-tetrahydro-naphthalen-amine compounds of general formula (I) and compositions thereof, methods for their preparation, and the use of said compounds for the treatment or prophylaxis of various disorders of humans or animals. | 04-29-2010 |
20100137313 | HETEROCYCLIC DERIVATIVES AND METHODS OF USE THEREOF - Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. | 06-03-2010 |
20100137314 | HARMFUL ORGANISM CONTROL COMPOSITION - This invention provides a harmful organism control composition comprising as an effective ingredient the following 4-(2-chlorobenzyl)-6-(2-butynyloxy)pyrimidine (X): | 06-03-2010 |
20100160325 | 4-(3-AMINOPYRAZOLE) PYRIMIDINE DERIVATIVES FOR USE AS TYROSINE KINASE INHIBITORS IN THE TREATMENT OF CANCER - This invention relates to novel compounds having the formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer. | 06-24-2010 |
20100168110 | Novel Compounds - The present invention discloses a novel thyroid like compounds of formula (I), wherein R | 07-01-2010 |
20100179148 | PYRIDAZINONE DERIVATIVES - Compounds of the formula (I), in which R | 07-15-2010 |
20100179149 | ARYL ETHER PYRIDAZINONE DERIVATIVES - Compounds of the formula I, in which R | 07-15-2010 |
20100190790 | SIGMA RECEPTOR INHIBITORS - The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved. | 07-29-2010 |
20100197690 | Pyrimidinyl Pyridazinone Derivatives - Compounds selected from the group according to Claim | 08-05-2010 |
20100210649 | PYRIDAZINONES AND FURAN-CONTAINING COMPOUNDS - The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries. | 08-19-2010 |
20100216793 | HETEROARYL SUBSTITUTED PYRIDAZINONE DERIVATIVES - The present invention is concerned with novel pyridazinone derivatives of formula (I) | 08-26-2010 |
20100234379 | Dual modulation of endocannabinoid transport and fatty-acid amide hydrolase for treatment of excitotoxicity - The endocannabinoid transporter and FAAH are sites of modulation that allow pharmacological enhancement of protective endocannabinergic signals. Selective inhibitors of the transporter and inhibitors of FAAH caused additive augmentation of endogenous signaling events mediated by the cannabinoid CB1 receptor. Disruption of such signals has been shown to prevent neuronal maintenance processes and increase vulnerability to brain damage. Here, blocking endocannabinoid inactivation enhanced cannabinergic activity and ameliorated cellular disturbances associated with excitotoxicity. Modulating the endocannabinoid system in this way also prevented excitotoxic behavioral abnormalities including memory impairment. Collectively, these results indicate that increasing endocannabinoid responses by inhibiting the endocannabinoid transported and/or the inhibiting FAAH leads to molecular, cellular, and functional protection against excitotoxic insults like stroke and traumatic brain injury. | 09-16-2010 |
20100234380 | CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF PHENYL-PYRAZOLES USEFUL AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR - The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HT | 09-16-2010 |
20100240659 | NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVE HAVING 11SS-HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORY ACTIVITY - Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor. | 09-23-2010 |
20100273796 | 2-BENZYLPYRIDAZINONE DERIVATIVES AS MET KINASE INHIBITORS - Compounds of the formula I | 10-28-2010 |
20100273797 | ALPHA-KETOAMIDES AND DERIVATIVES THEREOF - The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory agents. There are further provided methods for the preparation of such agents and their use in preventing or treating conditions medicated by cytokines such as arthritis. | 10-28-2010 |
20100280033 | Pyrazole Derivatives - The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrazole compounds and derivatives are described which inhibit protein kinases. The organic compounds are useful in treating proliferative disease. | 11-04-2010 |
20100292236 | 5-Membered Heterocyclic Amides And Related Compounds - 5-Membered heterocyclic amides and related compounds are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies. | 11-18-2010 |
20100311752 | Substituted pyridazine derivatives - The present invention is directed to compounds having histamine H | 12-09-2010 |
20110003817 | Whitening Agent And Skin External Preparation - The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a compound represented by formula (1) or a pharmacologically acceptable salt thereof: | 01-06-2011 |
20110039848 | FIVE-MEMBERED RING COMPOUND - Provided are: a five-membered ring compound represented by formula (1) or a pharmaceutically acceptable salt thereof; and a medicine containing the compound or salt. The compound or salt inhibits the infiltration of leukocytes such as eosinophils and lymphocytes, is effective as a therapeutic agent for various kinds of inflammation, and is so safe that the compound or salt can be taken for long. | 02-17-2011 |
20110046137 | Pyrazole Derivatives as P2X7 Modulators - The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: | 02-24-2011 |
20110071152 | 5-MEMBERED HETEROCYCLE-BASED P38 KINASE INHIBITORS - Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38α and p38β kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders. | 03-24-2011 |
20110071153 | DIHYDROPYRAZOLE DERIVATIVES AS TYROSINE KINASE MODULATORS FOR THE TREATMENT OF TUMORS - Compounds of the formula I, in which R | 03-24-2011 |
20110112096 | PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS - The invention provides novel pyrimidine derivatives of formula (I) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-IR) or analplastic lymphoma kinase (ALK). | 05-12-2011 |
20110136809 | Substituted Pyrazolyl Urea Derivatives Useful In The Treatment Of Cancer - The present invention relates to compounds of formula (I), pharmaceutical compositions which contain them and methods for treating cancer using compounds of formula (I). | 06-09-2011 |
20110152265 | CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V - The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. | 06-23-2011 |
20110160209 | SUBSTITUTED PYRIDAZINE CARBOXAMIDE COMPOUNDS AS KINASE INHIBITOR COMPOUNDS - Pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer. | 06-30-2011 |
20110160210 | CONTROL OF INTRAOCULAR PRESSURE USING ALK5 MODULATION AGENTS - An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure comprising an effective amount of a selective modulator of ALK5 receptor activity is disclosed. Also disclosed is a method of treating glaucoma and controlling intraocular pressure comprising applying a therapeutically effective amount of a pharmaceutical composition comprising a selective modulator of ALK5 receptor activity to an affected eye of a patient. | 06-30-2011 |
20110166139 | PYRIDINE COMPOUNDS - The present invention relates to compounds that inhibit of focal adhesion kinase function, 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 in warm-blooded animals such as humans of diseases such as cancer. | 07-07-2011 |
20110183978 | Phenylpyri(mi)dinylazoles - Phenylpyri(mi)dinylazoles of the formula [I-a] and [I-b], | 07-28-2011 |
20110183979 | NITROGEN-CONTAINING HETEROARYL DERIVATIVES - The invention is concerned with novel nitrogen-containing heteroaryl derivatives of formula (I) | 07-28-2011 |
20110212962 | P38 MAP KINASE INHIBITORS - There are provided inter alia compounds of formula (I) wherein R | 09-01-2011 |
20110218201 | NOVEL PYRAZOLONE-DERIVATIVES AND THEIR USE AS PDE-4 INHIBITORS - The compounds of Formula (I), | 09-08-2011 |
20110237588 | Thienylpyri(mi)dinylazole - Thienylpyri(mi)dinylazole of the formula (I) | 09-29-2011 |
20110257178 | CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING METABOLIC DISORDERS, INCLUDING OBESITY AND DIABETES - The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers. | 10-20-2011 |
20110257179 | NOVEL THIAZOLES DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds of Formula (I), wherein M, P, A and (B) | 10-20-2011 |
20110257180 | Novel Polymorphic Forms of 6-(1-methyl-1H-pyrazol-4-yl)-2--2H-pyridazin-3-one Dihydrogenphosphate and Processes of Manufacturing thereof - The present invention relates to 6-(1-methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one dihydrogenphosphate, its solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer. | 10-20-2011 |
20110257181 | PYRIDAZINONE DERIVATIVES - Compounds of the formula (I), in which Y, R | 10-20-2011 |
20110263602 | TETRASUBSTITUTED PYRIDAZINE HEDGEHOG PATHWAY ANTAGONISTS - The present invention provides novel tetrasubstituted pyridine hedgehog pathway antagonists of the following formula I (I) or a pharmaceutically acceptable salt thereof, wherein: X is C—R | 10-27-2011 |
20110269761 | ARYLSULPHONYLGLYCINE DERIVATIVES, THE PREPARATION THEREOF AND THEIR USE AS MEDICAMENTS - The invention relates to substituted aryl-sulphonylglycine derivatives of general formula (I) wherein the groups R | 11-03-2011 |
20110288093 | Compounds, Compositions, and Methods Comprising Pyridazine Sulfonamide Derivatives - The present invention relates to methods for treating a disease in an animal, which disease is responsive to blocking of chloride channel by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-3 or encompassed by formula I-III) or compositions thereof | 11-24-2011 |
20110294812 | P38 MAP KINASE INHIBITORS - The invention relates to compounds of formula (I): | 12-01-2011 |
20110312963 | P38 MAP KINASE INHIBITORS - The present disclosure relates to compounds of formula (I): | 12-22-2011 |
20110312964 | CYSTEINE PROTEASE INHIBITORS - Compounds of the formula I | 12-22-2011 |
20120004231 | Substituted Pyridazine Derivatives - The present invention is directed to compounds having histamine H | 01-05-2012 |
20120015945 | USE OF CB1 ANTAGONISTS AND/OR INVERSE AGONISTS FOR THE PREPARATION OF DRUGS THAT INCREASE MOTOR NEURON EXCITABILITY - Use of a CB1 receptor antagonist and/or inverse agonist, preferably rimonabant, for the preparation of drugs useful for increasing motor neuron excitability in the cerebral cortex and/or in the brain stem and/or at the spinal level, as well as a method for increasing motor neuron excitability through the administration of a CB1 antagonist/inverse agonist receptors, and to the use of a pharmaceutical composition which comprises a CB1 receptor antagonist and/or inverse agonist, preferably rimonabant, for increasing motor neuron excitability in the cerebral cortex and/or in the brain stem and/or at the spinal level. | 01-19-2012 |
20120046289 | Pyridazine Carboxamide Orexin Receptor Antagonists - The present invention is directed to pyridazine carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors 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 orexin receptors are involved. | 02-23-2012 |
20120059006 | SIGMA RECEPTOR INHIBITORS - The invention relates to compounds of formula I | 03-08-2012 |
20120071480 | 4-(3-AMINOPYRAZOLE) PYRIMIDINE DERIVATIVES FOR USE AS TYROSINE KINASE INHIBITORS IN THE TREATMENT OF CANCER - This invention relates to novel compounds having the formula (I): | 03-22-2012 |
20120115870 | CONTROL OF INTRAOCULAR PRESSURE USING ALK5 MODULATION AGENTS - An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure comprising an effective amount of a selective modulator of ALK5 receptor activity is disclosed. Also disclosed is a method of treating glaucoma and controlling intraocular pressure comprising applying a therapeutically effective amount of a pharmaceutical composition comprising a selective modulator of ALK5 receptor activity to an affected eye of a patient. | 05-10-2012 |
20120129858 | COMPOUNDS, COMPOSITIONS AND METHODS COMPRISING PYRIDAZINE SULFONAMIDE DERIVATIVES - The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-3 or encompassed by formula I-III) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease. | 05-24-2012 |
20120149705 | N-Thio-anthranilamid compounds and their use as pesticides - N-Thio-anthranilamid compounds of formula (I) | 06-14-2012 |
20120184553 | NOVEL COMPOUNDS - The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease. | 07-19-2012 |
20120196861 | IL17 AND IFN-GAMMA INHIBITION FOR THE TREATMENT OF AUTOIMMUNE INFLAMMATION - The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents. | 08-02-2012 |
20120196862 | IL17 AND IFN-GAMMA INHIBITION FOR THE TREATMENT OF AUTOIMMUNE INFLAMMATION - The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents. | 08-02-2012 |
20120202816 | NOVEL COMPOUNDS - The present invention discloses a novel thyroid like compounds of formula (I), wherein R | 08-09-2012 |
20120225880 | PYRAZOLE COMPOUNDS AND THIAZOLE COMPOUNDS AS PROTEIN KINASES INHIBITORS - A compound of formula (I): | 09-06-2012 |
20120252813 | CRYSTALLINE FORMS OF CERTAIN 3-PHENYL-PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - Provided are certain solvates of 3-methoxy-N-[3-(2-methyl-2H-pyrazol-3-yl)-4-(2-morpholin-4-yl-ethoxy)-phenyl]-benzamide or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions comprising such solvates and methods for their use. | 10-04-2012 |
20120264754 | CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING METABOLIC DISORDERS, INCLUDING OBESITY AND DIABETES - The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers. | 10-18-2012 |
20120283262 | PHARMACEUTICAL COMPOSITIONS COMPRISING SIGMA RECEPTOR LIGANDS - The present invention relates to a pharmaceutical composition that comprises a compound of formula (I) as active pharmaceutical ingredient: | 11-08-2012 |
20120289507 | 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. | 11-15-2012 |
20120295908 | PYRIMIDINYL PYRIDAZINONE DERIVATIVES - Compounds selected from the group according to claim | 11-22-2012 |
20120302568 | SIGMA LIGANDS FOR USE IN THE PREVENTION AND/OR TREATMENT OF POST-OPERATIVE PAIN - The invention refers to the use of a sigma ligand, particularly a sigma ligand of formulae (I), (II) or (III) to prevent and/or treat acute and chronic pain developed as a consequence of surgery, especially superficial and/or deep pain secondary to surgical tissue injury, and peripheral neuropathic pain, neuralgia, allodynia, causalgia, hyperalgesia, hyperesthesia, hyperpathia, neuritis or neuropathy secondary to surgical procedure. | 11-29-2012 |
20120316172 | PYRAZOLE DERIVATIVES - The invention relates to compounds of formula IA and IB | 12-13-2012 |
20130012512 | P38 MAP kinase inhibitors - There are provided inter alia compounds of formula (I) | 01-10-2013 |
20130023534 | PYRAZOLYL-PYRIMIDINES AS KINASE INHIBITORS - Disclosed are compounds having the formula (I): wherein Z, n, R | 01-24-2013 |
20130029990 | PYRAZOLE P38 MAP KINASE INHIBITORS - There are provided inter alia compounds of formula (I): wherein R | 01-31-2013 |
20130053386 | DIARYL ETHER DERIVATIVES AS NOTCH SPARING GAMMA SECRETASE INHIBITORS - The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative γ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included. | 02-28-2013 |
20130102606 | Compositions and Methods for Stimulating Collagen Synthesis in the Skin - Cosmetic compositions comprising substituted carbamoyl heterocyclic analogs and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The substituted carbamoyl heterocyclic analogs are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging. | 04-25-2013 |
20130102607 | UREIDO-PYRAZOLE DERIVATIVES FOR USE IN THE TREATMENT OF RHINOVIRUS INFECTIONS - Medicinal use The disclosure relates to compounds of formula (I) for use in the treatment or prophylaxis of respiratory syncitial virus (RSV) infection in particular viral exacerbation of a respiratory disorder such as bronchitis, asthma, COPD and/or cystic fibrosis, methods of treating or preventing RSV infection employing said compounds or pharmaceutical composition comprising the same. | 04-25-2013 |
20130102608 | BIPYRIDYL DERIVATIVES - The present invention relates to novel bipyridyl derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors. | 04-25-2013 |
20130109691 | Cosmetic Use of N-Heteroarybisamide Analogs and Related Compounds | 05-02-2013 |
20130109692 | SIGMA LIGANDS FOR THE PREVENTION AND/OR TREATMENT OF EMESIS INDUCED BY CHEMOTHERAPY OR RADIOTHERAPY | 05-02-2013 |
20130123260 | Methods - The disclosure relates to compounds of formula (I) for use in the treatment or prophylaxis of rhinovirus infection, methods of treating or preventing rhinovirus infection employing said compounds or pharmaceutical composition comprising the same. The disclosure also relates to compounds of formula (I) for use in the treatment or prophylaxis of exacerbation of respiratory disorders (such as asthma, COPD, bronchitis and/or cystic fibrosis) by rhinovirus infection. | 05-16-2013 |
20130131062 | PYRIDAZINONES AND FURAN-CONTAINING COMPOUNDS - The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries. | 05-23-2013 |
20130143884 | 4-[2-[ [5-METHYL-1-(2-NAPHTALENYL)-1H-PYRAZOL-3-YL]OXY]ETHYL] MORPHOLINE SALTS - The present invention relates to 4-[-2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine salts, specifically to the hydrochloride, to pharmaceutical compositions comprising them, and to their use in therapy and/or prophylaxis of sigma receptor associated diseases. | 06-06-2013 |
20130172351 | Dihydropyrazoles - Novel dihydropyrazole derivatives of formula (I) | 07-04-2013 |
20130172352 | 5-MEMBERED HETEROCYCLE-BASED P38 KINASE INHIBITORS - Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38α, and p38β kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders. | 07-04-2013 |
20130190311 | Pyridazinone derivatives - Compounds of the formula I | 07-25-2013 |
20130225584 | 2-(BENZYLOXY) BENZAMIDES AS LRRK2 KINASE INHIBITORS - The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by LRRK2 kinase activity, for example Parkinson's disease or Alzheimer's disease. | 08-29-2013 |
20130225585 | PYRAZOLE AMIDE COMPOUNDS AND USES THEREOF - Disclosed is a pyrazole amide compound having fungicidal activity, with a structure shown by the general formula (I): | 08-29-2013 |
20130237540 | 3-PHENYL-PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT | 09-12-2013 |
20130237541 | DIARYL AND ARYLHETEROARYL UREA DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO - The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT | 09-12-2013 |
20130267519 | 1,2-PYRIDAZINES, 1,6-PYRIDAZINES AND PYRIMIDINES - This invention relates to novel 1,2-pyridazines, 1,6-pyridazines or pyrimidines of the formula | 10-10-2013 |
20130281455 | Phenylpyri(mi)dinylazoles - Phenylpyri(mi)dinylazoles of the formula [I-a] and [I-b], | 10-24-2013 |
20130296321 | CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF PHENYL-PYRAZOLES USEFUL AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR - The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HT | 11-07-2013 |
20130324535 | USE OF SIGMA LIGANDS IN BONE CANCER PAIN - The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat pain associated to bone cancer. | 12-05-2013 |
20130324536 | PYRAZOLYL GUANIDINE F1F0-ATPASE INHIBITORS AND THERAPEUTIC USES THEREOF - The invention provides pyrazolyl guanidine compounds that inhibit F | 12-05-2013 |
20140057915 | KINASE INHIBITORS - There are provided compounds of formula I, | 02-27-2014 |
20140107125 | HYDRAZONOPYRAZOLE DERIVATIVES AND THEIR USE AS THERAPEUTICS - Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines. | 04-17-2014 |
20140128396 | PYRIMIDINYL PYRIDAZINONE DERIVATIVES - Compounds selected from the group according to Claim | 05-08-2014 |
20140142106 | METHOD FOR TREATING PERITONEAL FIBROSIS - The present invention provides a method for treating, preventing or reducing peritoneal fibrosis comprising administering to a subject in need thereof a pharmacologically effective dose of a type I cannabinoid receptor (CB | 05-22-2014 |
20140163031 | SUBSTITUTED PYRAZOLES AS N-TYPE CALCIUM CHANNEL BLOCKERS - The present invention relates to compounds of Formula (I), | 06-12-2014 |
20140163032 | ETHERS, SECONDARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT 2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT | 06-12-2014 |
20140179702 | CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV - The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. | 06-26-2014 |
20140221376 | SUBSTITUTED PYRIDAZINE CARBOXAMIDE COMPOUNDS AS KINASE INHIBITOR COMPOUNDS - Pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer. | 08-07-2014 |
20140235641 | PYRAZOLE CARBOXAMIDES AS JANUS KINASE INHIBITORS - The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. | 08-21-2014 |
20140243338 | PHENYLPYRAZOLE DERIVATIVES AS POTENT ROCK1 AND ROCK2 INHIBITORS - The present invention provides compounds of Formula (I): | 08-28-2014 |
20140243339 | COMBINATIONS VEGF(R) INHIBITORS AND HEPATOCYTE GROWTH FACTOR (C-MET) INHIBITORS FOR THE TREATMENT OF CANCER - This invention is in the field of pharmaceutical agents and specifically relates to compounds, compositions, uses and methods for treating cancer, by combining VEGF(R) inhibitors and inhibitors of HGF/SF:c-Met. | 08-28-2014 |
20140256727 | METHODS AND COMPOSITIONS OF SMALL MOLECULE MODULATORS OF HEPATOCYTE GROWTH FACTOR (SCATTER FACTOR) ACTIVITY - The present invention provides compositions and formulations of compounds having formula (I) and pharmaceutically acceptable derivatives thereof, wherein p, R | 09-11-2014 |
20140288074 | FUNGICIDAL PYRAZOLES - Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, fungicides: | 09-25-2014 |
20140296238 | Dihydropyrazoles - Novel dihydropyrazole derivatives of formula (I) | 10-02-2014 |
20140309227 | QUINOLINE CARBOXAMIDE AND QUINOLINE CARBONITRILE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE - The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, R | 10-16-2014 |
20140315904 | ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described. | 10-23-2014 |
20140323485 | N-Substituted Heterocyclyl Carboxamides - A compound of Formula I | 10-30-2014 |
20140329817 | MYXOVIRUS THERAPEUTICS, COMPOUNDS, AND USES RELATED THERETO - This disclosure relates to antiviral compounds disclosed herein and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions. Typically, the pharmaceutical composition comprises a compound of formula I: Formula I, or salt, prodrug, or ester thereof wherein X, Y, and R | 11-06-2014 |
20140364432 | SUBSTITUTED PROLINES / PIPERIDINES AS OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX | 12-11-2014 |
20140364433 | SUBSTITUTED PROLINES / PIPERIDINES AS OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX | 12-11-2014 |
20140378458 | N-Thio-anthranilamid compounds and their use as pesticides - N-Thio-anthranilamid compounds of formula (I) | 12-25-2014 |
20150011552 | 4-ALKANOYLAMINO-3-PYRAZOLONE DERIVATIVE - The present invention provides a compound which enhances the production of erythropoietin. The present invention provides, for example, a compound represented by the formula (1) wherein R | 01-08-2015 |
20150018353 | 2-BENZYL, 3-(PYRIMIDIN-2-YL) SUBSTITUTED PYRAZOLES USEFUL AS SGC STIMULATORS - Compound of Table I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed. | 01-15-2015 |
20150080397 | PHARMACEUTICALLY ACCEPTABLE SALTS OF 3,5-DIAMINOPYRAZOLE KINASE INHIBITORS - Provided herein are pharmaceutically acceptable salts of 3,5-diaminopyrazoles, for example, pharmaceutically acceptable salts of compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition. | 03-19-2015 |
20150080398 | 3,5-DIAMINOPYRAZOLE KINASE INHIBITORS - Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition. | 03-19-2015 |
20150105388 | CARBOXAMIDE-SUBSTITUTED HETEROARYL-PYRAZOLES AND THE USE THEREOF - This invention relates to new carboxamide-substituted heteroaryl-pyrazoles, method for their production, their use for the treatment and/or prophylaxis of diseases, as well as their use for the production of pharmaceutical agents for the treatment and/or prophylaxis of diseases, in particular retroviral diseases, in humans and/or animals. | 04-16-2015 |
20150105389 | 3,5-DIAMINOPYRAZOLE KINASE INHIBITORS - Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition. | 04-16-2015 |
20150105390 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof. | 04-16-2015 |
20150133451 | HETEROCYCLIC COMPOUND - The present invention provides a heterocyclic compound having an IRAK-4 inhibitory action, which is useful for the prophylaxis or treatment of inflammatory disease, autoimmune disease, osteoarticular degenerative disease, neoplastic disease and the like, and a medicament containing thereof. The present invention relates to a compound represented by the formula (I): | 05-14-2015 |
20150133452 | PYRIMIDINYL PYRIDAZINONE DERIVATIVES - Compounds selected from the group according to claim | 05-14-2015 |
20150291563 | 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVE OR SALTS THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME - The present invention provides a 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt effectively increases the LXR transcriptional activity, and therefore can be usefully applied for preventing or treating a dysfunction in cholesterol metabolism, such as cholesterol gallstone, hyperlipidemia, or coronary atherosclerosis. | 10-15-2015 |
20150299171 | INHIBITORS OF BRUTON'S TYROSINE KINASE - The invention provides novel poly-substituted 5-membered heterocyclic compounds represented by Formula (IV), or a pharmaceutically acceptable salt, solvate, metabolites, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as selective irreversible bruton's tyrosine kinase (Btk) inhibitors and is further useful to treat inflammatory, auto immune diseases associated with aberrant B-cell proliferation such as RA (rheumatoid arthritis) and cancers. This invention also provided the preparation of a medicament using of Formula (IV), and methods of preventing or treating diseases associated with excessive Btk activity in mammals, especially humans. Formula (IV) | 10-22-2015 |
20150299183 | AMIDE-SUBSTITUTED HETEROCYCLIC COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFN ALPHA RESPONSES - Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R | 10-22-2015 |
20150322043 | TROPOMYOSIN-RELATED KINASE INHIBITORS - The present invention relates to compounds of Formula I | 11-12-2015 |
20150342954 | 2-BENZYL, 3-(PYRIMIDIN-2-YL) SUBSTITUTED PYRAZOLES USEFUL AS SGC STIMULATORS - Compound of Table I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed. | 12-03-2015 |
20150344437 | PYRAZOLONE DERIVATIVES AS NITROXYL DONORS - The disclosed subject matter provides pyrazolone derivative compounds, pharmaceutical compositions comprising such compounds, kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure. | 12-03-2015 |
20150361052 | PYRIMIDINONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE - The present invention provides compounds of Formula (I): (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. | 12-17-2015 |
20160016910 | PHENYLPYRAZOLE DERIVATIVES AS POTENT ROCK1 AND ROCK2 INHIBITORS - The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same. | 01-21-2016 |
20160016913 | COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF CANCER - Disclosed are compounds, such as pyridazinones, that can be, inter alia, used for treating cancer. | 01-21-2016 |
20160023991 | PPAR AGONISTS - Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases). | 01-28-2016 |
20160024016 | ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described. | 01-28-2016 |
20160031865 | COMPOUNDS AND USES THEREOF FOR THE MODULATION OF HEMOGLOBIN - Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation. | 02-04-2016 |
20160039766 | CANNABINOID RECEPTOR MEDIATING COMPOUNDS - A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CB | 02-11-2016 |
20160039769 | PYRAZOLYL GUANIDINE F1F0-ATPASE INHIBITORS AND THERAPEUTIC USES THEREOF - The invention provides pyrazolyl guanidine compounds that inhibit F | 02-11-2016 |
20160039784 | PYRAZOLE DERIVATIVE - Provided are a compound expressed by formula (I) or a pharmacologically permissible salt thereof, as well as a drug or drug composition that contains this compound as an active ingredient, having a xanthine oxidase inhibiting effect that is very useful for treating or preventing diseases that are contributed to by xanthine oxidase, such as gout, hyperuricemia, tumor lysis syndrome, urinary tract stones, hypertension, dyslipidemia, diabetes, cardiovascular disease such as heart failure and arterial sclerosis, renal disease such as diabetic near opacity and the like, respiratory disease such as chronic obstructive pulmonary disease and the like, autoimmune diseases such as inflammatory bowel disease, and the like. [In the formula, A, X, Y, Z, R, and R | 02-11-2016 |
20160039797 | KINASE INHIBITORS BASED UPON N-ALKYL PYRAZOLES - Compounds are of formula (I): | 02-11-2016 |
20160039801 | SUBSTITUTED ALDEHYDE COMPOUNDS AND METHODS FOR THEIR USE IN INCREASING TISSUE OXYGENATION - Provided are cycloalkyl- and cycloalkenyl-substituted benzaldehydes and heteroaldehydes of formula (I) that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions containing the modulators, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from increased tissue oxygenation. | 02-11-2016 |
20160046613 | COMPOUNDS AND USES THEREOF FOR THE MODULATION OF HEMOGLOBIN - Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation. | 02-18-2016 |
20160058771 | ALPHA-2 ADRENOCEPTOR AND SIGMA RECEPTOR LIGAND COMBINATIONS - The invention refers to a combination comprising a Sigma ligand of general formula (I) and alpha-2-adrenergic agonist compound, a medicament comprising said active substance combination, and the use of said active substance combination for the manufacture of a medicament, particularly for the prophylaxis and/or treatment of pain. | 03-03-2016 |
20160090362 | 5-AMINOPYRAZOLE-4-CARBOXAMIDE INHIBITORS OF CDPK1 FROM T. GONDII AND C. PARVUM - The present disclosure is generally directed to compositions and methods for treating apicomplexan protozoan related disease, such as toxoplasmosis and cryptosporidiosis. | 03-31-2016 |
20160106752 | Use of CB1 Antagonists and/or Inverse Agonists for the Preparation of Drugs that Increase Motor Neuron Excitability - Use of a CB1 receptor antagonist and/or inverse agonist, preferably rimonabant, for the preparation of drugs useful for increasing motor neuron excitability in the cerebral cortex and/or in the brain stem and/or at the spinal level, as well as a method for increasing motor neuron excitability through the administration of a CB1 antagonist/ inverse agonist receptors, and to the use of a pharmaceutical composition which comprises a CB1 receptor antagonist and/or inverse agonist, preferably rimonabant, for increasing motor neuron excitability in the cerebral cortex and/or in the brain stem and/or at the spinal level. | 04-21-2016 |
20160108018 | ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described. | 04-21-2016 |
20160130256 | NOVEL COMPOUNDS - There are provided inter alia compounds of formula (I) | 05-12-2016 |
20160151377 | USE OF SIGMA RECEPTOR LIGANDS FOR THE PREVENTION AND TREATMENT OF PAIN ASSOCIATED TO INTERSTITIAL CYSTITIS/BLADDER PAIN SYNDROME (IC/BPS) | 06-02-2016 |
20160158131 | Compositions and Methods for Stimulating Collagen Synthesis in the Skin - Cosmetic compositions comprising substituted carbamoyl heterocyclic analogs and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The substituted carbamoyl heterocyclic analogs are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging. | 06-09-2016 |
20160176825 | KINASE INHIBITORS FOR THE TREATMENT OF DISEASE | 06-23-2016 |
20160176900 | SUBSTITUTED PYRIDAZINE CARBOXAMIDE COMPOUNDS AS KINASE INHIBITOR COMPOUNDS | 06-23-2016 |
20160184267 | ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described. | 06-30-2016 |
20160185755 | 1,2-DISUBSTITUTED CYCLOBUTYL COMPOUNDS - The invention refers to compounds of general formula (I) | 06-30-2016 |
20160194316 | SUBSTITUTED BENZENE COMPOUNDS | 07-07-2016 |
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