Entries |
Document | Title | Date |
20080214610 | Thiazolylimidazole Derivatives and Their Use as Inhibitors of Microsmal Triglyceride Transfer Protein - The present invention relates to thiazolylimidazole derivatives of the general formula (I) in which: G represents a bond or a divalent radical chosen from the groups g1, g2 and g3; and R | 09-04-2008 |
20080214611 | Pharmaceutical Compositions - 659 - The invention relates to a process for the preparation of a stable dispersion of amorphous particles of a CB1 modulator of sub-micron size in an aqueous medium. | 09-04-2008 |
20080227813 | Pharmaceutical compositions and methods for treating diseases associated with neurodegeneration - The present invention relates to methods for treating diseases, conditions or disorders using hydroxyamine compounds, and in particular, N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboximidoyl chloride (Compound I) alone or in combination with one or more other therapeutic agents for the treatment of conditions, disorders or diseases associated with neurodegeneration in the central nervous system. Additional therapeutic agents are provided. The present invention also relates to pharmaceutical compositions comprising hydroxyamine compounds, an additional therapeutic agent and a pharmaceutically acceptable carrier and methods for treating diseases using them. | 09-18-2008 |
20080262038 | Diarylmethylidene Piperidine Derivatives, Preparations Thereof and Uses Thereof - Compounds of Formula: wherein R | 10-23-2008 |
20080262039 | Vanilloid Receptor Ligands, Pharmaceutical Compositions Containing Them, Process For Making Them, and Use Thereof For Treating Pain and Other Conditions - Vanilloid receptor ligand compounds corresponding to formula I: | 10-23-2008 |
20080269287 | Substituted Pyridone Derivative - Compounds of a formula (I) | 10-30-2008 |
20080269288 | CHEMICAL COMPOUNDS - Compounds of formula (I): | 10-30-2008 |
20080269289 | Vanilloid receptor ligand compounds, pharmaceutical compositions containing them, a method of producing them and the use thereof to treat pain and various other conditions - Compounds corresponding to formula I: | 10-30-2008 |
20080275085 | Piperidine derivative and use thereof - The present invention provides a novel piperidine derivative and a tachykinin receptor antagonist containing same, as well as a compound represented by the formula: | 11-06-2008 |
20080293767 | 1-Isopropyl-2-Oxo-1,2-Dihydropyridine-3-Carboxamide Derivatives Having 5-Ht4 Receptor Agonistic Activity - This invention provides a compound of formula (I): wherein R | 11-27-2008 |
20080293768 | Novel Compounds Derived From 5-Thioxylose And Their Use In Therapeutics - The invention relates to novel 5-thioxylose compounds, preferably derivatives of the 5-thioxylopyranose type, to the process for their preparation and to their use as active principles of drugs intended especially for the treatment or prevention of thrombosis or cardiac insufficiency. | 11-27-2008 |
20080293769 | Polymorphs of a C-Met/Hgfr Inhibitor - This invention relates to polymorphs of (R)-3-[1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to compositions including such salts and polymorphs, and to methods of using such compositions in the treatment of abnormal cell growth in mammals, especially humans. | 11-27-2008 |
20080300273 | Method of Treating Abnormal Cell Growth - The present invention relates to the use of (R)-3-[1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine, a novel c-Met/HGFR inhibitor, for treating abnormal cell growth in mammals. In particular, the invention provides methods of treating mammals suffering from cancer. | 12-04-2008 |
20080312281 | G-Protein Coupled Receptor (Gpr116) Agonists and Use Thereof for Treating Obesity and Diabetes - Compounds of formula (I), or pharmaceutically acceptable salts thereof, are agonists of GPR116 and are useful for the treatment of obesity, and for the treatment of diabetes. | 12-18-2008 |
20080319018 | ORGANIC COMPOUNDS - The present invention relates to a compound of the formula I | 12-25-2008 |
20090005415 | 1,2-Diarylimidazoles for Use as Cb1 Modulators - Salts of 1,2-diarylimidazole-4-carboxamides 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. | 01-01-2009 |
20090005416 | BENZIMIDAZOLE DERIVATIVES - The present invention relates to a compound of the Formula I | 01-01-2009 |
20090012122 | N-AROYL CYCLIC AMINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS - Disclosed are N-aroyl cyclic amine derivatives having the formula: | 01-08-2009 |
20090018166 | New Pyridine Analogues X 161 - The present invention relates to certain new pyridin analogues of Formula (I) | 01-15-2009 |
20090030040 | Substituted Heterocyclic Ethers and Their Use in CNS Disorders - The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders. | 01-29-2009 |
20090042938 | Chemical Compounds - The use of a compound of formula (I), Y is a single bond, C═O, C═S or S(O) | 02-12-2009 |
20090048299 | Biphenyl compounds useful as muscarinic receptor antagonists - This invention provides compounds of formula I: | 02-19-2009 |
20090054487 | Pharmaceutical composition for increasing the mitochondrial genesis - The invention refers to the use of O-(3-piperidino-2-hydroxypropyl)nicotinic amidoxime or a pharmaceutically suitable acid addition salt thereof for the preparation of a pharmaceutical composition increasing the mitochondrial genesis. | 02-26-2009 |
20090062341 | Nuclear receptor binding agents - The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity. | 03-05-2009 |
20090062342 | AMINES - The invention relates to novel amine derivatives and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin. | 03-05-2009 |
20090069376 | VLA-4 Antagonists - Substituted N—[N-(sulphonylphenyl)sulfonyl-prolyl]-phenylalanine derivatives of the present invention are antagonists of the VLA-4 integrin and are useful in the treatment, prevention and suppression of diseases mediated by VLA-4-binding and cell adhesion and activation. Moreover, the compounds of the present invention demonstrate significant receptor occupancy of VLA-4 bearing cells after oral administration and are suitable for once-, twice-, or thrice-a-day oral administration. This invention also relates to compositions containing such compounds and methods of treatment using such compounds. | 03-12-2009 |
20090069377 | DEUTERIUM-ENRICHED ENZASTAURIN - The present application describes deuterium-enriched enzastaurin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-12-2009 |
20090082399 | Carbamate derivatives as positive allosteric modulators of metabotropic glutamate receptors - The present invention relates to new compounds which are Carbamate derivatives of formula I wherein X, B, P, Q5W, R | 03-26-2009 |
20090111854 | 1,2,4-TRIAZOLE ARYL N-OXIDES DERIVATIVES AS MODULATORS OF MGLUR5 - The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds. | 04-30-2009 |
20090143430 | ERYTHROPOIETIN PRODUCTION ACCELERATOR - The present invention relates to a preventive or therapeutic agent for pathological conditions caused by reduced production of erythropoietin, or for anemia, or for chronic anemia, renal anemia, aplastic anemia, or pure red cell aplasia, the agent comprising, as an active ingredient, a cyclic amine compound represented by the following formula (1): | 06-04-2009 |
20090149498 | Pharmaceutical composition having prokinetic effect - The invention refers to the use of O-(3-piperidino-2-hydroxypropyl)nicotinic amidoxime or a pharmaceutically suitable acid addition salt thereof for the preparation of a pharmaceutical composition that restores and/or enhances the activity of the neuronal nitric oxide synthase enzyme. | 06-11-2009 |
20090192193 | DIAGNOSTIC AGENT AND METHOD FOR DETECTION OF CANCER AND A MEANS FOR TREATMENT OF SAME - A method is disclosed for detecting colorectal carcinoma having at least one HERG potassium ion channel, where at least one HERG potassium channel is detected in a tissue biopsy of the human color or rectum. In addition, a method is disclosed for treating colorectal carcinoma having at least one HERG potassium channel in a patient in need of said treatment, which comprises the step of administering to said patient, a therapeutically effective amount of 4-[1-{2-(6-methyl-2-pyridinyl)ethyl-4-piperidinyl}carbonyl]methane-sulfoanilide 2HCl sufficient to treat the colorectal carcinoma having at least one HERG potassium channel by selectively blockading the HERG potassium channel. | 07-30-2009 |
20090203737 | Pyrrole Derivatives as Positive Allosteric Modulators of Metabotropic Receptors - The present invention relates to new compounds which are Pyrrole derivatives of formula (I) wherein A, B, P, Q | 08-13-2009 |
20090215821 | N-Substituted Azacycles - N-substituted azacycle derivative compounds represented by formula (I): | 08-27-2009 |
20090215822 | Substituted Oxadiazole Derivatives as Positive Allosteric Modulators of Metabotropic Glutamate Receptors - The present invention relates to new compounds which are Oxadiazole derivatives of formula (I) wherein B, P, Q, W, R | 08-27-2009 |
20090215823 | COMPOSITIONS AND METHODS FOR EFFECTING NAD+ LEVELS USING A NICOTINAMIDE PHOSPHORIBOSYL TRANSFERASE INHIBITOR - The present invention relates to methods for decreasing cellular DNA repair in a patient diagnosed with or suspected to have chronic lymphocytic leukemia (CLL); decreasing cellular NAD | 08-27-2009 |
20090221639 | Heterocyclic GPCR Agonists - Compounds of formula (I) or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful as regulators of satiety, e.g. for the treatment of obesity, and for the treatment of diabetes. | 09-03-2009 |
20090221640 | Novel Crystal Modifications - Novel crystal modifications of (5S)-5-[4-(5-chloro-pyridin-2-yloxy)-piperidine-1-sulfonylmethyl]-5-methyl-imidazolidine-2,4-dione are disclosed together with processes for preparing such modifications, pharmaceutical compositions comprising such a modification, and the use of such a modification in therapy. | 09-03-2009 |
20090253744 | Acylated piperidine derivatives as melanocortin-4 receptor modulators - Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction. | 10-08-2009 |
20090253745 | MODULATORS OF OCULAR OXIDATIVE STRESS - Described herein are compounds, compositions and methods directed to the treatment of ophthalmic conditions characterized by oxidative stress or damage in a subject by reducing the reactive oxygen species in the subject. Also described herein are methods for reducing ophthalmic photooxidative damage in a subject. | 10-08-2009 |
20090258900 | AMIDE DERIVATIVE - Amide derivatives represented by the formula (I): | 10-15-2009 |
20090264466 | Certain Chemical Entities, Compositions and Methods - Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described. | 10-22-2009 |
20090270452 | USE OF SOLUBLE EPOXIDE HYDROLASE INHIBITORS IN THE TREATMENT OF SMOOTH MUSCLE DISORDERS - Disclosed herein are compounds, compositions, and methods for enhancing smooth muscle function in a subject by administration of soluble epoxide hydrolase inhibitors and for treating subjects with smooth muscle disorders including erectile dysfunction, overactive bladder, uterine contractions and irritable bowel syndrome. | 10-29-2009 |
20090281143 | Dose Reduction of a Cannabinoid CB1 Receptor Antagonist in the Treatment of Overweight or Obesity - O-(3-Piperidino-2-hydroxy-1-propyl)-nicotinic amidoxime or a pharmaceutically acceptable acid addition salt thereof is administered to patients suffering from overweight or obesity and treated with a cannabinoid CB | 11-12-2009 |
20090298878 | OXIME COMPOUNDS AND THE USE THEREOF - The invention relates to oxime compounds of Formula (I) and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X is hydrogen, optionally substituted aryl, optionally substituted heteroaryl or the like; Y is CO, SO | 12-03-2009 |
20090306136 | Benzenesulfonamide Compounds and the Use Thereof - The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R | 12-10-2009 |
20090312368 | Pyridine Analogues IV - The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y | 12-17-2009 |
20100004284 | Novel Heterocyclic Compounds as Positive Allosteric Modulators of Metabotropic Glutamate Receptors - The present invention relates to new compounds which are Heterocyclic derivatives of formula (I) wherein A, B, P, X, Y, Q, W, R | 01-07-2010 |
20100010042 | ARYLVINYLAZACYCLOALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF - Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain. | 01-14-2010 |
20100016358 | GAMMA-GLOBIN INDUCER - The present invention is directed to a γ-globin inducer, to a prophylactic and/or therapeutic agent for sickle cell disease, and to a prophylactic and/or therapeutic agent for β-thalassemia, each containing, as an active ingredient, 4-[N-(4-methoxyphenyl)-N-[[5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]methyl]amino]-1-[[2-(3,4,5-trimethoxyphenyl)pyridin-4-yl]methyl]piperidine, a salt thereof, or a solvate of either of these. | 01-21-2010 |
20100016359 | METHODS FOR CONTROLLING SR PROTEIN PHOSPHORYLATION, AND ANTIVIRAL AGENTS WHOSE ACTIVE INGREDIENTS COMPRISE AGENTS THAT CONTROL SR PROTEIN ACTIVITY - The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses. | 01-21-2010 |
20100016360 | ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR INHIBITORS - The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate α7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system. | 01-21-2010 |
20100016361 | ARYL CARBOXYLIC ACID CYCLOHEXYL AMIDE DERIVATIVES - A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: (I) wherein the variants R and X are defined in the specification. | 01-21-2010 |
20100022589 | PYRIDINE-3-CARBOXAMIDE COMPOUNDS AND THEIR USE FOR INHIBITING 11-BETA-HYDROXYSTEROID DEHYDROGENASE - Compounds of formula (I): | 01-28-2010 |
20100029718 | ORGANIC COMPOUNDS - The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed. | 02-04-2010 |
20100041702 | BENZIMIDAZOLE CANNABINOID AGONISTS - The present invention is related to novel benzimidazole compounds of Formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans. | 02-18-2010 |
20100048625 | PIPERIDINE GPCR AGONISTS - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes. | 02-25-2010 |
20100048626 | Aryl Substituted Pyridines and the Use Thereof - This invention relates aryl substituted pyridines of Formula I: | 02-25-2010 |
20100048627 | SYNERGISTIC PHARMACEUTICAL COMBINATION FOR THE PREVENTION OR TREATMENT OF DIABETES - The invention refers to a synergistic pharmaceutical combination which comprises (a) a first pharmaceutical composition containing an antidiabetic or anti-hyperlipidemic active agent and one or more conventional carrier(s), and (b) a second pharmaceutical composition containing a hydroximic acid derivative of the formula I and one or more conventional carrier(s). The pharmaceutical combination is suitable for the prevention or treatment of, among others, diabetes mellitus. | 02-25-2010 |
20100063091 | RENIN INHIBITORS - The present invention relates to disubstituted piperidinyl renin inhibitor compounds having the structure (Formula I) and their use in treating cardiovascular events and renal insufficiency. | 03-11-2010 |
20100063092 | 3-CYANO-4-(4-PHENYL-PIPERIDIN-1-YL)-PYRIDIN-2-ONE DERIVATIVES - The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved. | 03-11-2010 |
20100069436 | IMIDAZOLE COMPOUNDS HAVING AN ANTIINFLAMMATORY EFFECT - The invention relates to imidazole derivatives of the Formula (I) in which the radicals R | 03-18-2010 |
20100076021 | Organic Compounds - The present invention provides a compound of formula (I): | 03-25-2010 |
20100081690 | OXAZOLE DERIVATIVES AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention provides new compounds of formula I, wherein P, A, W, B, Q, R1 and R2 are defined as in formula I; invention compounds are positive allosteric modulators of metabotropic receptors—subtype 5 (“mGluR5”) which are useful for the treatment or prevention of central nervous system disorders such as for example: cognitive decline, both positive and negative symptoms in schizophrenia as well as other disorders in which the mGluR5 subtype of glutamate metabotropic receptor is involved. | 04-01-2010 |
20100081691 | MULTICYCLIC COMPOUNDS AND METHODS OF THEIR USE - This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders. | 04-01-2010 |
20100099709 | PYRIDIN-2-YL-METHYLAMINE DERIVATIVES FOR TREATING OPIATE DEPENDENCE - The invention concerns the use pf compounds of general formula (I) | 04-22-2010 |
20100099710 | SRC FAMILY KINASE INHIBITORS - The invention relates to compounds of general formula (I) wherein X, A, R | 04-22-2010 |
20100105731 | NOVEL BENZAMIDINE COMPOUND -
Compounds represented by formula (1) and pharmaceutically acceptable salt thereofs:
| 04-29-2010 |
20100105732 | PIPERIDINE GPCR AGONISTS - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes. | 04-29-2010 |
20100120858 | Piperidine Derivatives - The invention relates to compounds of Formula (I) | 05-13-2010 |
20100120859 | NOVEL CASE OF RENIN INHIBITORS - The present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups, and their use in treating cardiovascular events and renal insufficiency. | 05-13-2010 |
20100137367 | NOVEL CRYSTALLINE BEPOTASTINE METAL SALT HYDRATE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME - The present invention discloses a non-hygroscopic crystalline bepotastine metal salt hydrate, a method for preparing same, and a pharmaceutical composition comprising same for treating or preventing a histamine-mediated disease or an allergic disease. | 06-03-2010 |
20100137368 | PYRIDINE DERIVATIVES AS FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS - The present invention relates to (1-benzyl-piperidin-4-yl)-(pyridin-2-yl)-amines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects. | 06-03-2010 |
20100144789 | 1-Isopropyl-2-Oxo-1,2-dihydropyridine-3-carboxamide Derivatives having 5-HT4 Receptor Agonistic Activity - This invention provides a compound of formula (I): wherein R | 06-10-2010 |
20100152239 | Method to Improve Survival in Sepsis - This invention relates to the use of an α7nAChR-agonist such as GTS to control systemic inflammation during resuscitation following severe trauma such blood loss because of severe hemorrhage. | 06-17-2010 |
20100160377 | DERIVATIVES OF PYRAZOLE 3,5-CARBOXYLATES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS - The invention relates to derivatives of pyrazole 3,5-carboxylates, of general formula (I): | 06-24-2010 |
20100168167 | Piperidinones Useful in the Treatment of Inflammation - There is provided compounds of formula (I): wherein R | 07-01-2010 |
20100190824 | Novel Substituted Piperidones as HSP Inducers - The present invention relates to novel compounds of formula (I) or (II), their pharmaceutically acceptable salts and their hydrates, solvates, stereoisomers, conformers, tautomers, polymorphs and prodrugs and also pharmaceutically acceptable compositions containing them Wherein R | 07-29-2010 |
20100204274 | PIPERIDINYL DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY - The present application describes modulators of MIP-1α of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R | 08-12-2010 |
20100204275 | N-PIPERIDIN-4-YLMETHYL-AMIDE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to novel N-piperidin-4-ylmethyl amide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. | 08-12-2010 |
20100210686 | THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN - Piperidine Compounds; compositions comprising a Piperidine Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperidine Compound are disclosed. In one embodiment, the Piperidine Compound has the formula: | 08-19-2010 |
20100216839 | Pim kinase inhibitors and methods of their use - The present invention relates to new compounds of Formulas I and II, their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pim kinase activity and/or the prophylaxis or treatment of cancer. | 08-26-2010 |
20100240701 | TUBULYSINS AND PROCESSES FOR PREPARING - Processes are described for the preparation of tubulysins. The processes are useful for preparing predetermined mixtures of tubulysins, preparing single tubulysins from mixtures of tubulysins, and for converting one tubulysin into a different tubulysin. The tubulysins described herein are useful in treating diseases and disease states that include pathogenic cell populations. | 09-23-2010 |
20100249187 | NOVEL DICARBOXYLIC ACID DERIVATIVES AS S1P1 RECEPTOR AGONISTS - The present invention relates to new compounds of formula (I) possessing agonistic activity at sphingosine-1-phosphate (S1P) receptors, their process of preparation and their use as immunosuppressive agents. The invention is also directed to pharmaceutical compositions containing these compounds and use of these compounds for treatment/prevention of immune mediated diseases and conditions or inflammatory diseases and conditions. | 09-30-2010 |
20100273828 | 4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS - The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs). R | 10-28-2010 |
20100298377 | NOVEL SUBSTITUTED INDAZOLES, THE PREPARATION THEREOF AND USE OF SAME IN THERAPEUTICS - This disclosure relates to compounds of formula (I): | 11-25-2010 |
20100298378 | ARYL-SUBSTITUTED POLYCYCLIC AMINES, METHOD FOR THE PRODUCTION THEREOF, AND USE THEREOF AS A MEDICAMENT - The invention relates to aryl-substituted polycyclic amines of formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; | 11-25-2010 |
20100305157 | DERIVATIVES OF DICARBOXYLIC AMINO ACIDS AND THEIR APPLICATION IN THE TREATMENT OF NEURODEGENERATIVE DISEASES - Products of a general formula (I) and their use in the manufacture of medicines useful for the treatment of neurodegenerative diseases such as Alzheimer's disease or, in general, any disease or pathology produced by alterations of biological functions that can be treated or therapeutically modified by these products. | 12-02-2010 |
20110003852 | N-ADAMANTYL BENZAMIDES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE - Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome. | 01-06-2011 |
20110003853 | Metalloproteinase Inhibitors - Compounds of the formula (I) wherein z is SO | 01-06-2011 |
20110021565 | PIPERIDINE DERIVATIVES AS NK3 ANTAGONISTS - The invention relates to a compound of formula | 01-27-2011 |
20110028515 | NEW PIPERIDINE DERIVATIVES - Compounds of formula (I) | 02-03-2011 |
20110034511 | SUBSTITUTED 2-CARBONYLAMINO-6-PIPERIDINAMINOPYRIDINES AND SUBSTITUTED 1-CARBONYLAMINO-3-PIPERIDINAMINOBENZENES AS 5-HT1F AGONISTS - The present invention relates to compounds of formula I: | 02-10-2011 |
20110053979 | PYRIDINE DERIVATIVES USED TO TREAT OREXIN RELATED DISORDERS - This invention relates to pyridinamine methyl substituted piperidinyl derivatives I and their use as pharmaceuticals. | 03-03-2011 |
20110071191 | INSECTICIDAL COMPOUNDS - A compound of formula (I): wherein R | 03-24-2011 |
20110098320 | Lactam Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1 - This invention relates to novel compounds of the Formula (I), (I*), (Ia), (Ib), (Ic), (Id), (Ie), (If), (If*), (Ig), (Ih), (Ij), (Ik), (ll1-3), (Im1-3), (In1-3), (lo1-2), (Ip1-9), (Iq1-9), (Ir1-9) and (Is1-3) 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. | 04-28-2011 |
20110112143 | ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to new compounds of formula (I) wherein A, B, P, Q, W, R | 05-12-2011 |
20110118311 | AZOLE COMPOUND - A compound which is useful as an active ingredient of a pharmaceutical composition for treating neuropathic pain is provided. The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that an azole compound substituted with an N-(pyridine-3-yl)oxycarbonyl-piperidin-4-yl group and a phenyl group or a pharmaceutically acceptable salt thereof has an excellent FAAH inhibitory activity, thereby completing the present invention. The compound of the present invention is confirmed to have an excellent FAAH inhibitory activity and an antiallodynic effect in rat models with neuropathic pain, and thus is useful as an agent for preventing and/or an agent for treating neuropathic pain. | 05-19-2011 |
20110136866 | INSECTICIDAL PHENYL- OR PYRIDYL-PIPERDINE COMPOUNDS - A compound of formula (I): wherein A, p, R | 06-09-2011 |
20110144158 | ISOINDOLE-IMIDE COMPOUNDS AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME - This invention relates to isoindole-imide compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed. | 06-16-2011 |
20110184020 | Vanilloid Receptor Ligands, Pharmaceutical Compositions Containing Them, Process For Making Them, and Use Thereof For Treating Pain and Other Conditions - Vanilloid receptor ligand compounds corresponding to formula I: | 07-28-2011 |
20110190346 | Diphenyl Substituted Alkanes as Flap Inhibitors - The instant invention provides compounds of formula I which are 5-lipoxygenase activating protein inhibitors. | 08-04-2011 |
20110195993 | PPAR AGONIST COMPOUNDS, PREPARATION AND USES - The present invention relates to novel PPAR agonist compounds as well as pharmaceutical compositions containing them. | 08-11-2011 |
20110237622 | RENIN INHIBITORS - The present invention relates to 3,4-substituted piperidinyl—based renin inhibitor compounds bearing at 4-position oxopyridine or Isoquinolone and having the formula (I): wherein S is Formula (IIa) or Formula (IIb). The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency. | 09-29-2011 |
20110306636 | OXAZOLE PYRIDINE DERIVATIVES USEFUL AS S1P1 RECEPTOR AGONISTS - The present invention provides oxadiazole pyridine derivatives of Formula (I), their use as medicaments and their use for treating multiple sclerosis and other diseases. | 12-15-2011 |
20110319448 | GUANIDINE-CONTAINING COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention provides compounds of formula I: | 12-29-2011 |
20120035214 | RENIN INHIBITORS - The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency. | 02-09-2012 |
20120088792 | Pyridin-2-YL Methylamine Derivatives for Treating Opiate Dependence - The invention concerns the use of compounds of general formula (I) | 04-12-2012 |
20120088793 | Bicyclic Compounds and Methods of Making and Using Same - Disclosed herein are compounds that may be modulators of 5-HT receptors, and methods of making and using same. | 04-12-2012 |
20120095047 | 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. | 04-19-2012 |
20120115908 | USE OF A HYDROXIMIC ACID HALIDE DERIVATIVE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES - The invention relates to the use of a chemical substance selected from the group consisting of N-′2-hydroxy-3-(1-piperidinyl)-propoxyl 1-pyridine-1-oxide-3-carboximidoyl chloride, the optically active enantiomers and the mixtures of enantiomers thereof and pharmaceutically acceptable salts of the racemic and optically active compounds in the preparation of a pharmaceutical composition for the treatment or prevention of neurodegenerative diseases. | 05-10-2012 |
20120115909 | TAZAROTENE DERIVATIVES - The presently described subject matter relates to new derivatives of tazarotene that also exhibit retinoid activity, pharmaceutical compositions comprising the derivatives, method of treating skin disorders with the pharmaceutical compositions, and process of making the derivatives. | 05-10-2012 |
20120122926 | BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention provides compounds of formula I: | 05-17-2012 |
20120142732 | HETEROARYLS AND USES THEREOF - This invention provides compounds of formula IA or IB: | 06-07-2012 |
20120142733 | 4-SUBSTITUTED-CYCLOHEXYLAMINO-4-PIPERIDINYL-ACETAMIDE ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula (I). | 06-07-2012 |
20120149732 | MULTIFUNCTIONAL LINKERS AND METHODS FOR THE USE THEREOF - In accordance with the present invention, novel multifunctional compounds have been developed which have orthogonal reactive groups thereon, thereby facilitating preparation of compounds having multiple functional properties (e.g., a targeting moiety and a biologically active moiety). Such constructs are useful for a variety of applications, e.g., for the delivery of biologically compatible materials, and release thereof in active form. Therefore, in accordance with the present invention, there are provided multifunctional linkers of defined structure, as well as various derivatives thereof bearing one or more biologically active components thereon. Also provided in accordance with the present invention are methods for the preparation of such constructs, as well as various uses thereof. | 06-14-2012 |
20120157494 | ISOINDOLYL COMPOUNDS - Compounds of the formula I: | 06-21-2012 |
20120202851 | PIM KINASE INHIBITORS AND METHODS OF THEIR USE - The present invention relates to new compounds of Formulas I and II, their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pim kinase activity and/or the prophylaxis or treatment of cancer. | 08-09-2012 |
20120225905 | BEPOTASTINE COMPOSITIONS - Novel compositions including bepotastine besilate are provided such as sorbitol-free compositions, compositions including at least about 0.008% w/v benzalkonium chloride, and compositions including hydroxypropylmethyl cellulose E15 LV. | 09-06-2012 |
20120264780 | SOLID COMPOSITIONS - The present invention features solid compositions comprising Compound I | 10-18-2012 |
20120264781 | METHOD FOR THE TREATMENT, ALLEVIATION OF SYMPTOMS OF, RELIEVING, IMPROVING AND PREVENTING A COGNITIVE DISEASE, DISORDER OR CONDITION - The present invention provides uses of a salt adduct comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted, for the preparation of a medicament for the treatment, alleviation of symptoms of relieving, improving and preventing a cognitive disease, disorder or condition in a subject. Additionally, the invention provides use of said salt adducts for the preparation of medicaments for the improvement of cognitive functions in a healthy subject. | 10-18-2012 |
20120270900 | NOVEL METHOD OF TREATMENT - The present application discloses a method for the treatment or for alleviating the symptoms of a cancer in a subject comprising the steps of a) determining the level of Nicotinic acid phosphoribosyltransferase (NAPRT) in said subject; and b) 1) in the event of a level of NAPRT which is lower than a predetermined threshold value, treating said subject sequentially/simultaneous with i) an effective amount of a nicotinamide phosphoribosyltransferase inhibitor (NAMPRTi), and ii) an effective amount of a nicotinic acid, a nicotinic acid precursor or a prodrug of nicotinic acid; or 2) in the event of a level of NAPRT which is higher than or equal to a predetermined threshold value, treating said subject with i) an effective amount of a NAMPRTi in the absence of sequential/simultaneous treatment with ii) an effective amount of a nicotinic acid, a nicotinic acid precursor or a prodrug of nicotinic acid. | 10-25-2012 |
20120302602 | Vanilloid Receptor Ligand Compounds, Pharmaceutical Compositions Containing Them, a Method of Producing Them and the Use Thereof to Treat Pain and Various Other Conditions - Compounds corresponding to formula I: | 11-29-2012 |
20120316201 | NOVEL BENZIMIDAZOLE AND IMIDAZOPYRIDINE DERIVATIVES AND USE THEREOF AS A MEDICAMENT - The invention relates to novel benzimidazole and imidazopyridine derivatives having the general Formula (I), which have a good affinity with certain subtypes of melanocortin receptors, particularly MC4 receptors. The derivatives are particularly suitable for the treatment of pathological states and diseases involving one or more melanocortin receptors. The invention also relates to pharmaceutical compositions containing said the compounds having the general Formula (I). | 12-13-2012 |
20120322825 | AQUEOUS LIQUID PREPARATIONS AND LIGHT-STABILIZED AQUEOUS LIQUID PREPARATIONS - An aqueous liquid preparation containing (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof, which is stabilized with a water-soluble metal chloride, is provided. | 12-20-2012 |
20130005770 | ORGANIC COMPOUNDS - The present invention relates to a compound of the formula I | 01-03-2013 |
20130012541 | Therapeutic Agents Useful for Treating Pain - A compound of formula: | 01-10-2013 |
20130059887 | SUBSTITUTED PYRIDOXINE-LACTAM CARBOXYLATE SALTS - The present invention provides salt adducts comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted, methods of their preparation, and pharmaceutical compositions and medicaments comprising them. Salt adducts of the invention and compositions comprising them may be used to in the treatment of diseases or disorders associated with or inflicted by alcohol consumption. | 03-07-2013 |
20130065923 | SUBSTITUTED N-HETEROARYL BIPYRROLIDINE CARBOXAMIDES, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I). | 03-14-2013 |
20130072524 | Compositions And Methods Of Synthesis Of Pyridinolypiperidine 5-HT1F Agonists - The present invention provides a novel polymorph of the hemisuccinate salt of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide (Form A) characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. This polymorph is useful in pharmaceutical compositions, for example, for the treatment and prevention of migraine. The invention also provides a process for the synthesis of pyridinoylpiperidine compounds of Formula I in high yield and high purity. In particular, the provides a process for the preparation of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide, its hemisuccinate salt and polymorph (Form A). | 03-21-2013 |
20130079369 | METHODS FOR CONTROLLING SR PROTEIN PHOSPHORYLATION, AND ANTIVIRAL AGENTS WHOSE ACTIVE INGREDIENTS COMPRISE AGENTS THAT CONTROL SR PROTEIN ACTIVITY - The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses. | 03-28-2013 |
20130085160 | NOVEL BENZAMIDE DERIVATIVES - The present invention provides a novel benzamide derivative or a pharmaceutically acceptable salt thereof, a method for preparing the same, and a 5-HT | 04-04-2013 |
20130085161 | PIPERIDINYL SUBSTITUTED 1,3-DIHYDRO-BENZOIMIDAZOL-2-YLIDENEAMINE DERIVATIVES - The invention relates to new derivatives of formula (I), | 04-04-2013 |
20130131111 | NMN MODULATORS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS - The invention relates to a nicotinamide mononucleotide (NMN) modulator useful as a neuroprotective medicament in the treatment of neurodegenerative disorders, in particular but not exclusively disorders involving axon degeneration of neuronal tissue such as Wallerian degeneration, to the use of NMN as a biomarker for axon degeneration, to a method of demonstrating axon degeneration using an NMN-based biomarker, to a diagnostic kit for detecting axon degeneration, to a method of screening for an NMN modulator, and to an NMN modulator identified using the aforementioned screening method. | 05-23-2013 |
20130137726 | CONFORMATIONALLY RESTRICTED UREA INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE - Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases. | 05-30-2013 |
20130150407 | PIPERIDINYL NAPHTHYLACETIC ACIDS - The invention is concerned with the compounds of formula (I): | 06-13-2013 |
20130203810 | Identification, Assessment, and Therapy of Cancers with Innate or Acquired Resistance to ALK Inhibitors - Described herein are compositions, kits, and methods for determining whether subjects having cancer(s) positive for ALK mutations are likely to respond to treatment with an ALK inhibitor and/or whether a patient having such cancer(s) is likely to have a relatively slower disease progression. Further described are methods for prognosing a time course of disease in a subject having such cancer. | 08-08-2013 |
20130231369 | 1-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives, preparation methods and uses thereof - Provided are N-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives represented by formula I, stereoisomers, pharmaceutically acceptable salts or solvates thereof. | 09-05-2013 |
20130261153 | USE OF CCR3-INHIBITORS - The present invention relates to CCR3 inhibitors of formula 1, | 10-03-2013 |
20130274288 | BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention provides compounds of formula I: | 10-17-2013 |
20130317062 | INSECTICIDAL PHENYL-OR PYRIDYL-PIPERDINE COMPOUNDS - A compound of formula (I) | 11-28-2013 |
20130317063 | ORAL CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS OF BEPOTASTINE - The present invention relates to oral controlled release pharmaceutical compositions comprising Bepotastine. The oral controlled release pharmaceutical composition comprises Bepotastine or pharmaceutically acceptable salts thereof and at least one release controlling agent. The present invention also provides the use of oral controlled release pharmaceutical compositions of Bepotastine for the treatment of allergic rhinitis and for the treatment of pruritus caused by urticaria. | 11-28-2013 |
20130324576 | THERAPEUTIC COMPOUNDS - The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof | 12-05-2013 |
20140039007 | COMPOSITIONS AND METHODS FOR MODULATING FARNESOID X RECEPTORS - The present invention relates to compounds of Formula I, a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR). | 02-06-2014 |
20140073671 | ORALLY DISINTEGRATING TABLET - Provided is an orally disintegrating tablet comprising a bitter-tasting pharmaceutically active ingredient in the form of bepotastine or a pharmacologically acceptable salt thereof that enables the bitter taste thereof to be masked, has both superior oral cavity disintegration and adequate hardness, and can be produced with ordinary tablet production equipment. The present invention relates to an orally disintegrating tablet containing bepotastine or a pharmacologically acceptable salt thereof, menthol or cyclodextrin, a water-insoluble polymer, and a disintegrating agent; and a method for producing an orally disintegrating tablet, comprising: 1) a step for obtaining granulated granules by mixing and granulating bepotastine or a pharmacologically acceptable salt thereof, a water-insoluble polymer, and optionally a vehicle, 2) a step for obtaining granules for tableting by mixing the granulated granules, menthol, a disintegrating agent, and optionally a lubricant and/or sweetener, and 3) a step for compressing the granules for tableting. | 03-13-2014 |
20140088146 | HETEROCYCLIC COMPOUNDS - The present invention provides a compound useful as an agent for the prophylaxis or treatment of neurodegenerative disease and the like, or a salt thereof. | 03-27-2014 |
20140088147 | METHOD OF INHIBITING MUTANT C-KIT - The present invention includes a method of reducing or inhibiting the kinase activity of C-KIT mutant tyrosine kinase activity in a cell or a subject, and the use of such compound for treating mutant C-KIT driven cell proliferative disorder(s) in a subject related to using a compound of the present invention: | 03-27-2014 |
20140094491 | DIMETHYL-BENZOIC ACID COMPOUNDS - The present invention provides a compound of the Formula II: | 04-03-2014 |
20140128432 | ANAPLASTIC THYROID CANCERS HARBOR NOVEL ONCOGENIC MUTATIONS OF THE ALK GENE - The present invention relates to diagnostic, therapeutic and prognostic methods for thyroid cancers. In one embodiment, the present invention provides a method for treating a an anaplastic thyroid cancer (ATC) patient comprising the step of administering to the patient an effective amount of an anaplastic lymphoma kinase (ALK) inhibitor. In another embodiment, a method for diagnosing ATC in patient comprises the step of performing an assay on a biological sample from the patient to identify the presence or absence of a C3592T and/or a G3602A mutation in exon 23 of the ALK gene according to SEQ ID NO:6, wherein the presence of either of both of the mutations correlates with a diagnosis of ATC in the patient. | 05-08-2014 |
20140135361 | ANTI-ALLERGY BENZOCYCLOHEPTATHIOPHENE DERIVATIVES - The present invention provides inhibitors of allergy, and allergic reactions specifically compounds of the present invention are described by the following chemical Formula I: | 05-15-2014 |
20140142139 | DIHYDROPYRAZOLE GPR40 MODULATORS - The present invention provides compounds of Formula (I): | 05-22-2014 |
20140288121 | Asthma - The invention provides methods of providing a prognosis of asthma severity in children and young adults. More specifically, the invention relates to novel single nucleotide polymorphisms (SNPs), and the cumulative genetic association of these and other SNPs in various genes, with the prognosis of asthma severity. The invention also extends to kits and other prognostic tools used to provide the prognosis of asthma severity. | 09-25-2014 |
20140343099 | AQUEOUS LIQUID PREPARATIONS AND LIGHT-STABILIZED AQUEOUS LIQUID PREPARATIONS - An aqueous liquid preparation containing (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof, which is stabilized with a water-soluble metal chloride, is provided. | 11-20-2014 |
20140350050 | PYRIDINE COMPOUNDS AS INHIBITORS OF KINASE - The present invention relates to novel pyridines, their derivatives, pharmaceutically acceptable salts, solvates, entiomers, prodrugs and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are expected to be useful for the treatment of protein kinases mediated diseases and conditions, including hyper-proliferative disorder, ALK kinases mediated disorder, and neoplasia. | 11-27-2014 |
20140371268 | BIPHENYLCARBOXAMIDES AS ROCK KINASE INHIBITORS - The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases, gastrointestinal diseases and respiratory diseases. | 12-18-2014 |
20140371269 | PHENYL METHANESULFONAMIDE DERIVATIVES USEFUL AS MGAT-2 INHIBITORS - The present invention provides compounds of Formula I or a pharmaceutical salt thereof, where the variables for R1, R2, and R3 are as described herein; methods of treating a condition such as hypertriglyceridemia; and processes for preparing the compounds. | 12-18-2014 |
20150025111 | SUBSTITUTED PYRIDOXINE-LACTAM CARBOXYLATE-SALTS - The present invention provides salt adducts comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted, methods of their preparation, and pharmaceutical compositions and medicaments comprising them. Salt adducts of the invention and compositions comprising them may be used to in the treatment of diseases or disorders associated with or inflicted by alcohol consumption, | 01-22-2015 |
20150031724 | AQUEOUS LIQUID PREPARATIONS AND LIGHT-STABILIZED AQUEOUS LIQUID PREPARATIONS - An aqueous liquid preparation containing (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof, which is stabilized with a water-soluble metal chloride, is provided. | 01-29-2015 |
20150087674 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF SEVERE PAIN - The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of severe pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of postoperative pain, cancer pain, kidney stones pain, fractures, local pain, chronic pain, chemotherapy induced pain, neuropathic pain, post herpetic neuralgia, neuralgia, motor neurone disease, diabetic neuropathy, postherpetic neuralgia, injury, post-operative pain, osteoarthritis, rheumatoid arthritis, multiple sclerosis, spinal cord injury, migraine, HIV related neuropathic pain, cancer pain and lower back pain. | 03-26-2015 |
20150099782 | ANTAGONISTS OF PROSTAGLANDIN EP3 RECEPTOR - Provided herein are antagonists of prostaglandin EP3 receptor, processes to make said antagonists, and methods comprising administering said antagonists to a mammal in need thereof. | 04-09-2015 |
20150099783 | USE OF CCR3-INHIBITORS - The present invention relates to CCR3 inhibitors of formula 1, | 04-09-2015 |
20150111922 | SULFONYL PIPERIDINE DERIVATIVES AND THEIR USE FOR TREATING PROKINETICIN MEDIATED DISEASES - The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: (I) in which m, n, W, X, Y, Z, R | 04-23-2015 |
20150126551 | USE OF A HYDROXIMIC ACID HALIDE DERIVATIVE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES - The invention relates to the use of a chemical substance selected from the group consisting of N-'2-hydroxy-3-(1piperidinyl)-propoxy]-1-pyridine-1-oxide-3-carboximidoyl chloride, the optically active enantiomers and the mixtures of enantiomers thereof and pharmaceutically acceptable salts of the racemic and optically active compounds in the preparation of a pharmaceutical composition for the treatment or prevention of neurodegenerative diseases. | 05-07-2015 |
20150133497 | GLYCINE REUPTAKE INHIBITOR AND USE THEREOF - Disclosed are a glycine reuptake inhibitor and the use thereof. The glycine reuptake inhibitor is a compound of formula I, or isomers, pharmaceutically acceptable salts or solvates thereof, wherein R1 is one or more groups selected from hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy; R2 is selected from hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, and C1-6 haloalkoxy; and each of R3 and R4 is independently selected from hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. | 05-14-2015 |
20150299170 | FLUORO-DERIVATIVES OF PYRAZOLE-SUBSTITUTED AMINO-HETEROARYL COMPOUNDS - This invention relates to novel fluoro-derivatives of pyrazole-substituted amino-heteroaryl compounds of Formula I: | 10-22-2015 |
20150322039 | 2-PYRIDYLAMINO-4-NITRILE-PIPERIDINYL OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 2-pyridylamino-4-nitrile-piperidinyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridylamino-4-nitrile-piperidinyl compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 11-12-2015 |
20150322041 | 2-PYRIDYLOXY-4-NITRILE-4-SUBSTITUTED OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 2-pyridyloxy-3-nitrile-4-substituted compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-3-nitrile-4-substituted compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 11-12-2015 |
20150346206 | Method of Identifying Treatment Responsive Non-Small Cell Lung Cancer Using Anaplastic Lymphoma Kinase (ALK) as a Marker - Disclosed herein are methods for identifying a subject as having NSCLC that is predicted or is likely to respond to treatment with an ALK inhibitor, for example crizotinib. The methods include identifying a sample including NSCLC tumor cells as ALK-positive or ALK-negative using immunohistochemistry (IBC) and scoring methods disclosed herein. A subject is identified as having NSCLC likely to respond to treatment with an ALK inhibitor if the sample is identified as ALK-positive and is identified as having NSCLC not likely to respond to treatment with an ALK inhibitor if the sample is identified as ALK-negative. According to certain embodiments of the methods, subjects predicted to respond to an ALK inhibitor may then be treated with an ALK inhibitor such as crizotinib. | 12-03-2015 |
20150353534 | THIAZOLE DERIVATIVES AS 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. | 12-10-2015 |
20150366852 | Prevention of Obesity in Antipsychotic, Antidepressant and Antiepileptic Medication - O-(3-piperidino-2-hydroxypropyl)-nicotinic amidoxime or a pharmaceutically suitable acid addition salt thereof (BGP-15) can be used for the prevention or reduction of weight gain or obesity in a patient treated with an antipsychotic drug or an antidepressant drug or an antiepileptic drug. | 12-24-2015 |
20150374662 | INHIBITORS OF BETA-CATENIN IN TREATMENT OF COLORECTAL CANCER - Compounds are disclosed which are effective for inhibiting β-catenin or disrupting a β-catenin/Tcf-4 complex, and for causing effective attenuation of colon carcinogenesis. The compounds may be effective treatment for colorectal cancer (CRC) when administered in an effective dose to a patient afflicted therewith. | 12-31-2015 |
20150376129 | SUBSTITUTED BENZAMIDES WITH ACTIVITY TOWARDS EP4 RECEPTORS - The present invention belongs to the field of EP4 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP4 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP4 receptor as well as to pharmaceutical compositions comprising them. | 12-31-2015 |
20160046598 | Glutarimide Derivatives, Use Thereof, Pharmaceutical Composition Based Thereon and Methods for Producing Glutarimide Derivatives - The present invention relates to novel biologically active glutarimide derivatives of general formula I or pharmaceutically acceptable salts thereof, their use as an agent for the treatment of upper respiratory tract diseases, pharmaceutical compositions comprising the glutarimide derivatives of general formula I, methods for preparing the glutarimide derivatives of general formula I by heating a dicarboxylic acid monoamide of general formula II with a dehydrating agent. | 02-18-2016 |
20160081998 | USE OF CCR3-INHIBITORS - The present invention relates to CCR3 inhibitors of formula 1, | 03-24-2016 |
20160122330 | PIPERIDINYL BENZOIMIDAZOLE DERIVATIVES AS MPGE-1 INHIBITORS - The compounds (R)-1-(5-chloro-6-methyl-1-(6-(trifluoromethyl)pyridin-2-yl)-1H-benzo[d]imidazol-2-yl)-N-(tetrahydrofuran-3-yl)piperidine-4-carboxamide and (R)-1-(6-chloro-1-methyl-1-(6-(trifluoromethyl)pyridin-2-yl)-1H-benzo[d]imidazol-2-yl)-N-(tetrahydrofuran-3-yl)piperidine-4-carboxamide, as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising any one of these compounds. The compounds are useful for the treatment and/or prevention of a disorder selected from an inflammatory disease; an autoimmune disease; pain; a breathing disorder; cancer; a cardiovascular disease; a neurodegenerative disease; a bone disease; a disorder due to familial adenomatous polyposis (FAP) condition; overactive bladder; fever; and inflammation-related anorexia. | 05-05-2016 |
20160122335 | AMIDE SUBSTITUTED THIAZOLES AS MODULATORS OF RORyt - The present invention comprises compounds of Formula I. | 05-05-2016 |
20160137628 | Aurora A Kinase Inhibitor - The present invention provides an aminopyridine compound, or a pharmaceutically acceptable salt thereof, that inhibits Aurora A and, therefore may be useful in treating cancer. | 05-19-2016 |
20160194308 | NOVEL PIPERIDINYL BENZOIMIDAZOLE DERIVATIVES AS MPGES-1 INHIBITORS | 07-07-2016 |
20160376256 | SULFONYL PIPERIDINE DERIVATIVES AND THEIR USE FOR TREATING PROKINETICIN MEDIATED DISEASES - The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof | 12-29-2016 |
20180022728 | Glutarimide Derivatives, Use Thereof, Pharmaceutical Composition Based Thereon and Methods for Producing Glutarimide Derivatives | 01-25-2018 |
20220133706 | TARGETING NAD BIOSYNTHESIS IN THE TREATMENT OF CANCER - There are provided, inter alia, methods for treatment of cancer. The methods include means of identifying the NAD biosynthetic pathway on which depend cancer cells in a tumor, in a subject suffering from cancer. The methods further include administering to a subject in need a therapeutically effective amount of an inhibitor of the NMRK1 enzyme pathway to a tumor where the cancer cells are dependent of the NAD salvage pathway, allowing to lower the of dose FK866 administered to the subject. The methods also include administering to a subject in need a therapeutically effective amount of a bacterial inhibitor of NADSYN1 to a tumor where the cancer cells depend on the Preiss Handler pathway. | 05-05-2022 |
20220133707 | ARIMOCLOMOL FOR TREATING GLUCOCEREBROSIDASE ASSOCIATED DISORDERS - The present invention relates to an active pharmaceutical ingredient selected from N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboximidoyl chloride, its stereoisomers and the acid addition salts thereof (arimoclomol), for use in a method of treating glucocerebrosidase associated disorders. | 05-05-2022 |