Entries |
Document | Title | Date |
20080262042 | Pyrrole compounds - The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity, which is represented by the formula (I) | 10-23-2008 |
20090012126 | Certain chemical entities, compositions, and methods - Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, and chemical entities, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described. | 01-08-2009 |
20090048301 | HETEROCYCLIC COMPOUNDS AND THEIR USE AS ANTICANCER AGENTS - The present invention relates to heterocyclic compounds that have anticancer activity, and pharmaceutical compositions that contain such compounds, methods of treating diseases and conditions in mammals using such compounds and composition and methods for their manufacture. | 02-19-2009 |
20090054490 | METHODS FOR THE TREATMENT OF GERD WITH MGLUR5 ANTAGONISTS - The present invention relates to methods for the treatment, prevention and/or delay of progression of gastro-esophageal reflux disease (GERD) by administering compounds that act as antagonists of metabotropic glutamate type-5 receptors (mGluR5 receptor antagonists), for example compounds of formula (I) | 02-26-2009 |
20090076086 | SUBSTITUTED NICOTINAMIDE COMPOUNDS AND USES THEREOF - Substituted nicotinamide compounds corresponding to formula I | 03-19-2009 |
20090082403 | PYRIDINE DERIVATIVES SUBSTITUTED BY HETEROCYCLIC RING AND PHOSPHONOAMINO GROUP, AND ANTI-FUNGAL AGENT CONTAINING SAME - Anti-fungal agent having excellent anti-fungal action physicochemical properties including safety and water solubility. Compound represented by formula (I), or salt thereof: | 03-26-2009 |
20090182013 | Derivatives of 5-Thioxylopyranose and Use of Same for Treatment - The invention relates to new compounds of 5-thioxilose, preferably derivatives of the 5-thioxilopyranose type, and to a method for preparing the same and their use as the active ingredient of drugs mainly intended for treating or inhibiting thrombosis or heart failure or thromboembolic diseases. | 07-16-2009 |
20090192196 | Fungicide hydroximoyl-tetrazole derivatives - The present invention relates to hydroximoyl-tetrazole derivatives of formula (I) wherein T represent a tetrazolyl substituent, A represents a carbo- or heterocycle, L | 07-30-2009 |
20090215826 | SOLID FORMS OF A PYRROLIDINE-3,4-DICARBOXAMIDE DERIVATIVE - The invention is concerned with crystalline forms or amorphous forms of a pyrrolidine-3,4-dicarboxamide derivative, which is useful as an active ingredient of medicaments for the diseases which can be treated by the coagulation factor Xa inhibitors. | 08-27-2009 |
20090270456 | Novel chemical compounds - This invention relates to newly identified compounds for inhibiting hYAK3 and/or CK2 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 and/or CK2 proteins. | 10-29-2009 |
20090291981 | 5-Lipoxygenase-Activating Protein Inhibitor - Described herein is the FLAP inhibitor 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxy-pyridin-3-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the FLAP inhibitor, or a pharmaceutically acceptable salt thereof, including solvates, and polymorphs thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the FLAP inhibitor, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases. | 11-26-2009 |
20090318503 | BIS-QUATERNARY AMMONIUM SALTS AND METHODS FOR MODULATING NEURONAL NICOTINIC ACETYLCHOLINE RECEPTORS - Provided are bis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders. | 12-24-2009 |
20100056577 | PYRROLE COMPOUNDS - The present invention relates to a compound represented by the formula: | 03-04-2010 |
20100063097 | Azabicyclo [3.1.0] Hexane Derivatives as Modulators of Dopamine D3 Receptors - The present invention relates to certain azabicyclic compounds of formula (I)′: | 03-11-2010 |
20100087486 | METHODS FOR USING TGF-B RECEPTOR INHIBITORS OR ACTIVIN-LIKE KINASE (ALK) 5 INHIBITORS A-83-01 AND SB-431542 TO TREAT EYE DISEASE AND WOUND HEALING CONDITIONS - A pharmaceutical composition useful in the prevention of subconjunctival scarring that may occur after glaucoma filtration surgery comprising an effective amount of an activin receptor-like kinase 5 inhibitor. Also disclosed is a method of treating corneal haze and subconjunctival scarring that may develop after ocular surgery comprising applying an amount of a pharmaceutical composition including an activin receptor-like kinase 5 inhibitor. | 04-08-2010 |
20100093803 | SUBSTITUTED DIPYRIDYL-DIHYDROPYRAZOLONES AND USE THEREOF - The present application relates to novel substituted dipyridyldihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing. | 04-15-2010 |
20100099713 | 2-AMINOPYRIDINE DERIVATIVES AS GLUCOKINASE ACTIVATORS - Provided are compounds having the Formula I | 04-22-2010 |
20100105737 | PYRIDINE DERIVATIVES SUBSTITUTED WITH HETEROCYCLIC RING AND gamma-GLUTAMYLAMINO GROUP, AND ANTIFUNGAL AGENTS CONTAINING SAME - The present invention provides an antifungal agent which has excellent antifungal action, and which is also excellent in terms of its properties, and in particular its solubility in water and safety. The present invention discloses a compound represented by the following formula (I) or a salt thereof. | 04-29-2010 |
20100130552 | Therapeutic Agents Useful for Treating Pain - A compound of Formula: (I) or a pharmaceutically acceptable derivative thereof, where Ar | 05-27-2010 |
20100144793 | NOVEL COMPOUNDS FOR THE TREATMENT OF DISEASES ASSOCIATED WITH AMYLOID OR AMYLOID-LIKE PROTEINS - The present invention relates to compounds of the general formula (I) wherein (formula 2) independently represents a single bond or a double bond, represents a linking group A and A′ are each independently a 5- to 7-membered heterocyclic ring, wherein the heterocyclic rings A und A′ are optionally substituted by one or more substituents, selected from C | 06-10-2010 |
20100160379 | HETEROCYCLES SUBSTITUTED PYRIDINE DERIVATIVES AND ANTIFUNGAL AGENT CONTAINING THEREOF - An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: | 06-24-2010 |
20100168173 | HETEROCYCLES SUBSTITUTED PYRIDINE DERIVATIVES AND ANTIFUNGAL AGENT CONTAINING THEREOF - An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: | 07-01-2010 |
20100204278 | Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment - The present invention encompasses compounds of Formula (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included. | 08-12-2010 |
20100216843 | NOVEL SALT 628 - 6-Methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-{[5-(methylsulfonyl)pyridin-2-yl]methyl}-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide 4-methylbenzenesulfonate and a novel crystalline form thereof are disclosed together with processes for preparing such salt and form, pharmaceutical compositions comprising such a salt and form, and the methods of treatment using such a salt and form. | 08-26-2010 |
20100331368 | 2,5-DIARYL SELENOPHENE COMPOUNDS, AZA 2,5-DIARYL THIOPHENE COMPOUNDS, AND THEIR PRODRUGS AS ANTIPROTOZOAL AGENTS - Novel dicationic 2,5-diaryl selenophene compounds are described. Also described are novel aza analogues of dicationic 2,5-diaryl thiophenes. The presently disclosed dicationic compounds exhibit in vitro activity versus | 12-30-2010 |
20100331369 | Therapeutic Agents Useful for Treating Pain - A compound of formula: | 12-30-2010 |
20110003858 | MULTIMERIC HETEROCYCLIC COMPOUNDS USEFUL AS NEUTROPHIL ELASTASE INHIBITORS - The invention provides compounds of formula (I) and formula (IV) (M)-(L)-(M) (I) [(M)-(L | 01-06-2011 |
20110009453 | S1P3 RECEPTOR INHIBITORS FOR TREATING INFLAMMATION - Disclosed herein are compositions and methods for treating inflammation using S1 P3 receptor inhibitors. | 01-13-2011 |
20110015231 | ISOXAZOLE AND ISOTHIAZOLE COMPOUNDS USEFUL IN THE TREATMENT OF INFLAMMATION - Compounds of Formula (I), pharmaceutical compositions comprising compounds of Formulae (I a) or (VII) and a method of treating a subject with an inflammatory cytokine-mediated disorder comprising administering to the subject a compound of Formulae (I a) or (VIIa). | 01-20-2011 |
20110021570 | PYRIDONE GLUCOKINASE ACTIVATORS - Provided herein are compounds of the formula (I): | 01-27-2011 |
20110034514 | 5-Lipoxygenase-Activating Protein (FLAP) Inhibitors - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases. | 02-10-2011 |
20110039893 | GSK-3BETA INHIBITOR - For the purpose of providing a GSK-3β inhibitor containing a 2-aminopyridine compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3β-related pathology or disease, the present invention provides a GSK-3β inhibitor containing a compound represented by the formula (IA): | 02-17-2011 |
20110071192 | Therapeutic Agents Useful for Treating Pain - A compound of formula: | 03-24-2011 |
20110105564 | THIENYLPYRIDYLCARBOXAMIDES - Novel thienylpyridylcarboxamides of the formula (I) | 05-05-2011 |
20110118315 | 5-LIPOXYGENASE-ACTIVATING PROTEIN (FLAP) INHIBITORS - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases. | 05-19-2011 |
20110124687 | PHARMACEUTICAL COMPOSITION - The present invention provides a pharmaceutical composition or a solid preparation containing a stabilized pharmaceutically active ingredient and a stabilizing method thereof. | 05-26-2011 |
20110130426 | Novel Sulphonamide Derivatives as Glucocorticoid Receptor Modulators for the Treatment of Inflammatory Diseases - A compound of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal). | 06-02-2011 |
20110144161 | 1-HETEROCYCLYLSULFONYL, 2-AMINOMETHYL, 5- (HETERO-) ARYL SUBSTITUTED 1-H-PYRROLE DERIVATIVES AS ACID SECRETION INHIBITORS - The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R | 06-16-2011 |
20110144162 | OXOTETRAHYDROFURAN-2-YL-BENZIMIDAZOLE DERIVATIVE - The present invention relates to compounds, which are useful for treatment and/or prevention of diabetes mellitus, diabetes mellitus complications or obesity, since the compounds have glucokinase-activating effects, and are presented in Formula (I): wherein R1 represents a carbamoyl group; R2 represents a lower alkyl group; both of X1 and X2 represent CH, or any one of X1 and X2 represents a nitrogen atom and the other represents CH; a group of represents a group selected from the group consisting of a pyridinyl, a pyrazinyl, a pyrazolyl, a thiadiazolyl, a triazolyl, an isoxazolyl and a thiazolyl group; and k is zero or 1, or relates to pharmaceutically acceptable salts thereof. | 06-16-2011 |
20110160249 | 5-LIPOXYGENASE-ACTIVATING PROTEIN INHIBITOR - A pharmaceutically acceptable salt comprising 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxy-pyridin-3-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionate as the anion and a cation selected from Na | 06-30-2011 |
20110172275 | PYRROLE COMPOUNDS - The present invention relates to a compound represented by the formula: | 07-14-2011 |
20110201648 | POLY-HETEROARYL DERIVATIVES FOR THE TREATMENT OF CANCER - The present invention relates to Penta-hexa-, hepta-, octa-, nona- and, deca-heteroaryl derivatives, comprising a combination of heterocycle 1 (Het-1) | 08-18-2011 |
20110212998 | PYRIDINE DERIVATIVES AS S1P1/EDG1 RECEPTOR MODULATORS - The invention relates to novel pyridine derivatives of formula (D, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I) wherein A represents and the other substituents are as defined in the claims. | 09-01-2011 |
20110212999 | TRIAZOLE DERIVATIVES AND THEIR USE AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS - This invention relates to novel triazole derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 09-01-2011 |
20110257230 | BENZIMIDAZOLE DERIVATIVES AND THEIR USE FOR MODULATING THE GABAA RECEPTOR COMPLEX - The present application discloses novel benzimidazole derivatives and their use as modulators of the GABA | 10-20-2011 |
20110263652 | Treatment and/or Prevention of Inner Ear Conditions by Modulation of a Metabotropic Glutamate Receptor - Described herein are compositions and methods of treating and/or preventing inner ear conditions by administering to a patient in need thereof a modulator of a metabotropic glutamate receptor. | 10-27-2011 |
20120004267 | APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS - The present invention relates to compounds of Formula (I): | 01-05-2012 |
20120015980 | ANTHRANILIC DIAMIDE DERIVATIVES - The present invention relates to novel anthranilic acid derivatives of the general formula (I) | 01-19-2012 |
20120022110 | PHARMACEUTICAL DEPOT FOR 5-FLUORO-2-[[(1S)-1-(5-FLUORO-2-PYRIDYL)ETHYL]AMINO]-6-[(5-ISOPROPOXY-1H-- PYRAZOL-3-YL)AMINO]PYRIDINE-3-CARBONITRILE - A pharmaceutical depot comprising (i) 5-fluoro-2-[[(1S)-1-(5-fluoro-2-pyridyl)ethyl]amino]-6-[(5-isopropoxy-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrile, or a pharmaceutically-acceptable salt thereof, as a pharmaceutical agent (PA) and (ii) a polymer which degrades to create an acidic microclimate, wherein the PA is released from the polymer upon polymer degradation. | 01-26-2012 |
20120029023 | HETEROCYCLES SUBSTITUTED PYRIDINE DERIVATIVES AND ANTIFUNGAL AGENT CONTAINING THEREOF - An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: | 02-02-2012 |
20120035217 | Bis Aromatic Compounds for Use as LTC4 Synthase Inhibitors - There is provided compounds of formula I, | 02-09-2012 |
20120059037 | SUBSTITUTED PYRIDINE DERIVATIVES AND THEIR MEDICAL USE - The present application discloses novel substituted pyridinyl-methylamine derivatives and their use as modulators of the voltage gated K | 03-08-2012 |
20120071512 | 5-PYRIDIN-3-YL-1, 3-DIHYDRO-INDOL-2-ON DERIVATIVES AND THEIR USE AS MODULATORS OF ALDOSTERONE SYNTHASE AND/OR CYP11B1 - The present invention provides a compound of formula I; | 03-22-2012 |
20120108635 | Insecticidal Arylpyrrolines - The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide. | 05-03-2012 |
20120122930 | 1H-Benzimidazole-5-Carboxamides As Anti-Inflammatory Agents - There are provided compounds of formula (I), wherein R | 05-17-2012 |
20120122931 | INDOLE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - A compound represented by the general formula (I) of the present invention, which has an EP | 05-17-2012 |
20120129890 | INDOLE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - A compound (I) of the present invention, which has an EP | 05-24-2012 |
20120142736 | NOVEL PYRIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 06-07-2012 |
20120172397 | HEXAHYDROCYCLOPENTA[f]INDAZOLE 5-YL ETHANOLS AND DERIVATIVES THEREOF AS SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS - The present invention encompasses compounds of Formula (I) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included. | 07-05-2012 |
20120309792 | TETRAZOLE DERIVATIVES AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS - This invention relates to novel tetrazole derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 12-06-2012 |
20130005773 | FLUORO-SUBSTITUTED 2-ARYL-3,5-DICYANO-4-INDAZOLYL-6-METHYL-1,4-DIHYDROPYRIDINES AND USES THEREOF - The present invention relates to novel, fluoro-substituted 2-aryl-3,5-dicyano-4-(1H-indazol-5-yl)-6-methyl-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly Cancer and other proliferative disorders. | 01-03-2013 |
20130040992 | Substituted 2, 6-Diamino-3, 5-Dicyano-4-Aryl-Pyridines And Their Use As Adenosine-Receptor-Selective Ligands - The present invention relates to substituted 2,6-diamino-3,5-dicyano-4-arylpyridines of the formula (I) | 02-14-2013 |
20130090358 | PYRAZOLYLAMINOPYRIDINE DERIVATIVES USEFUL AS KINASE INHIBITORS - This invention relates to novel compounds having the formula (I): | 04-11-2013 |
20130096161 | Novel Dihydropyridin-2(1H)-One Compounds as S-Nitrosoglutathione Reductase Inhibitors and Neurokinin-3 Receptor Antagonists - The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same. | 04-18-2013 |
20130102636 | 5-Lipoxygenase-Activating Protein (FLAP) Inhibitors - A method for treating a human comprises administering a therapeutically effective amount of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid or a pharmaceutically acceptable salt or a pharmaceutically acceptable N-oxide thereof, to the human in need. | 04-25-2013 |
20130109720 | INDOLE INHIBITORS OF CRAC | 05-02-2013 |
20130131113 | PYRIDONE GLUCOKINASE ACTIVATORS - Provided herein are compounds of the formula (I): | 05-23-2013 |
20130143927 | COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity. | 06-06-2013 |
20130143928 | BIS-PYRINIDIUM COMPOUNDS - A method of treating, inhibiting, or preventing an infection in a subject is described. The method comprises administering to the subject an effective amount of at least one bis-pyridinium compound. The bis-pyridinium compound comprises two aromatic ring structures. Each of the ring structures comprises a pyridine ring, and the ring structures are linked by a linker group of at least 8 atoms in length, said linker group being attached to the nitrogen atoms of the pyridine rings. At least one substituent on at least one of the ring structures is an alkyl group having at least 2 carbon atoms, and no substituent on either of the ring structures is —OH, —SH or an amine group. | 06-06-2013 |
20130150411 | NOVEL PYRIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 06-13-2013 |
20130165483 | HETEROARYLS AND USES THEREOF - This invention provides compounds of formula IB: | 06-27-2013 |
20130190355 | DUAL INHIBITORS OF FARNESYLTRANSFERASE AND GERANYLGERANYLTRANSFERASE I - Many GTPases such as Ras, Ral and Rho require post-translational farnestylation or geranylgeranylation for mediating malignant transformation. Dual farnesyltransferase (FT) (FTI) and geranylgeranyltransferase-I (GGT-1) inhibitors (GGTI) were developed as anticancer agents from based on an ethylenediamine scaffold. On the basis of a 4-fold substituted ethylenediamine scaffold, the inhibitors are structurally simple and readily derivatized, facilitating extensive structure-activity relationship studies. The most potent inhibitor is compound exhibited an in vitro hFTase IC | 07-25-2013 |
20130261156 | PHARMACEUTICAL COMPOSITION - The present invention provides a pharmaceutical composition or a solid preparation containing a stabilized pharmaceutically active ingredient and a stabilizing method thereof. | 10-03-2013 |
20130289071 | TETRAZOLYL-TETRAHYDROPYRIDINE COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES - The invention relates to certain compounds according to formula (I): or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders. | 10-31-2013 |
20130289072 | NOVEL INDOLE OR INDAZOLE DERIVATIVE OR SALT THEREOF - The present invention relates to provision of a novel indazole compound which is capable of inhibiting HSP90 and shows a cytostatic effect on cancer cells. The present invention also relates to provision of a drug useful for preventing and/or treating, on the basis of an HSP90 inhibitory effect, a disease in which HSP90 participates, in particular, cancer. A compound represented by the general formula (I) or a salt thereof: | 10-31-2013 |
20130296370 | COMPOSITION COMPRISING A PHOTOACTIVATABLE LARVICIDE - A composition comprising a photoactivatable larvicide and a suitable vector, the latter allowing the larvicide to be ingested by the larvae and a method for controlling mosquito larvae by using said photoactivatable larvicide are disclosed. | 11-07-2013 |
20130296371 | MACROCYCLIC PICOLINAMIDES AS FUNGICIDES - The disclosure relates to macrocyclic picolinamides of Formula I and their use as fungicides. | 11-07-2013 |
20130303572 | NOVEL INHIBITORS OF MATRIX METALLOPROTEINASES - Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: | 11-14-2013 |
20130317065 | INDOLE DERIVATIVE AND PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF - The present invention provides a compound represented by the general formula (I) of the present invention, which has EP | 11-28-2013 |
20130338195 | NOVEL PYRIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 12-19-2013 |
20140018394 | 5-LIPOXGENASE-ACTIVATING PROTEIN (FLAP) INHIBITORS - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases. | 01-16-2014 |
20140024680 | Insecticidal Arylpyrrolines - The invention relates to novel arylpyrroline compounds of formula (I) | 01-23-2014 |
20140031393 | PYRROLE COMPOUNDS - The present invention relates to a compound represented by the formula: | 01-30-2014 |
20140045895 | PHARMACEUTICAL DEPOT FOR 5-FLUORO-2-[[(1S)-1-(5-FLUORO-2-PYRIDYL)ETHYL]AMINO]-6-[(5-ISOPROPOXY-1H-- PYRAZOL-3-YL)AMINO]PYRIDINE-3-CARBONITRILE - A pharmaceutical depot comprising (i) 5-fluoro-2-[[(1S)-1-(5-fluoro-2-pyridyl)ethyl]amino]-6-[(5-isopropoxy-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrile, or a pharmaceutically-acceptable salt thereof, as a pharmaceutical agent (PA) and (ii) a polymer which degrades to create an acidic microclimate, wherein the PA is released from the polymer upon polymer degradation. | 02-13-2014 |
20140045896 | 1,4-dihydropyridine-3,5-dicarboxylate Derivatives And Preparation And Use Thereof - The present invention relates to a 1,4-dihydropyridine-3,5-dicarboxylate compound of general compound (I), a process for preparing the same, a use thereof for the manufacture of a medicament for treating and/or preventing kidney injury, cardiovascular diseases and/or endocrine diseases, as well as a pharmaceutical composition and a pharmaceutical formulation containing said compounds, wherein the definitions of R | 02-13-2014 |
20140088148 | SMALL MOLECULE INHIBITORS OF XBP1 SPLICING - Small molecule inhibitors of XBP1 splicing by IRE1 are provided, as well as methods for their use in treating or preventing cancer (e.g., endocrine resistant breast cancer), diabetes, and obesity. | 03-27-2014 |
20140100250 | PYRIDYL AMINOPYRIDINES AS SYK INHIBITORS - The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer. | 04-10-2014 |
20140179742 | COMPOSITIONS FOR KILLING OR PREVENTING THE GROWTH OF MICROBES - Described herein are methods and compositions for killing or preventing the growth of microbes. It has been discovered that a class of porphyrins can kill or prevent the growth of microbes. The porphyrins can be used in a number of different applications where microbes grow. | 06-26-2014 |
20140194469 | HISTONE DEMETHYLASE INHIBITORS - Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like. | 07-10-2014 |
20140194470 | DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF - The invention relates to compounds corresponding to formula (I), in the form of the base or of an acid-addition salt: | 07-10-2014 |
20140249185 | Therapeutic Agents Useful for Treating Pain - A compound of formula: | 09-04-2014 |
20140329863 | NOVEL ANTIPRION COMPOUNDS - Described herein are novel compositions and methods of treatment addressing diseases such as neurodegenerative diseases, including prion diseases and Alzheimer's disease. | 11-06-2014 |
20140343103 | PYRIDONE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES - Compounds useful in the treatment of mammalian cancers and especially human cancers according to Formula I are disclosed. | 11-20-2014 |
20140357669 | 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. | 12-04-2014 |
20150025113 | RODENTICIDAL NORBORMIDE ANALOGUES - The present invention relates to norbormide analogues having rodenticidal activity; rodenticidal compositions comprising the analogues; uses of the analogues as rodenticides; uses of the analogues in the manufacture of rodenticidal compositions; and methods for controlling rodents using the compositions. | 01-22-2015 |
20150051251 | PREMATURE-TERMINATION-CODONS READTHROUGH COMPOUNDS - Premature termination codons readthrough compounds, composition thereof, and methods of making and using the same are provided. | 02-19-2015 |
20150126558 | 4-[5-(PYRIDIN-4-YL)-1H-1,2,4-TRIAZOL-3-YL]PYRIDINE-2-CARBONITRILE CRYSTALLINE POLYMORPH AND PRODUCTION METHOD THEREFOR - To provide crystal polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile, which is a useful pharmaceutical, and a production method therefor. Through purification of a corresponding salt, recrystallization, or storage under humidified conditions, three different crystal forms; i.e., crystalline polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile are produced. | 05-07-2015 |
20150141463 | SUBSTITUTED PYRAZOLONE COMPOUNDS AND METHODS OF USE - The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans. | 05-21-2015 |
20150299182 | CRYSTALLINE FORMS OF (1S)-1-[5-(AMINO)-1,2,4-THIADIAZOL-3-YL]ETHANE-1,2-DIOL - The present invention relates to crystalline polymorph forms of (1S)-1-[5-({3-[(2-methylpyridin-3-yl)oxy]-5-(pyridin-2-ylsulfanyl)pyridin-2-yl}amino)-1,2,4-thiadiazol-3-yl]ethane-1,2-diol, to pharmaceutical compositions comprising such crystalline polymorph forms, and to processes for preparing them. The invention further relates to methods of treatment of diabetes related disorders comprising administering such solid-state forms or compositions thereof to a subject, and to use of such crystalline polymorph forms in the manufacture of medicaments. | 10-22-2015 |
20150307464 | THERAPEUTIC THIAZOLIDINONE COMPOUNDS - Thiazolidinone compounds, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. | 10-29-2015 |
20150307472 | NOVEL PYRIDINE DERIVATIVES - The invention relates to a compound of formula (I) | 10-29-2015 |
20150322073 | Benzimidazole Derivatives - The present invention encompasses compounds of the general formula I | 11-12-2015 |
20150354011 | METHODS FOR DIAGNOSING CANCER BASED ON SMALL NUCLEOLAR RNA HBII-52 - Provided are compositions and methods for detecting in a sample the presence or absence, and/or the amount, of a small nucleolar RNA (snoRNA) HBII-52, also known as SNORD115. The compositions and methods are useful in diagnosis, prognosis, therapy recommendations, therapy, and monitoring of therapy for individuals who have a disorder that is positively correlated with elevated HBII-52, such as cancer, and particularly for prostate cancer. Kits containing primers for detecting and/or amplifying HBII-52 from a biological sample are provided. The disclosure includes a method for monitoring an individual undergoing therapy for a disorder associated with HBII-52 expression, a method for identifying an individual as a candidate for therapy with an antagonist of 5-HT | 12-10-2015 |
20160002201 | HISTONE DEMETHYLASE INHIBITORS - Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like. | 01-07-2016 |
20160007603 | ALKOXIMINO-SUBSTITUTED ANTHRANILIC ACID DIAMIDES AS PESTICIDES | 01-14-2016 |
20160068507 | HISTONE DEMETHYLASE INHIBITORS - Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like. | 03-10-2016 |
20160075682 | INHIBITORS OF NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE, COMPOSITIONS, PRODUCTS AND USES THEREOF - Compounds of formula (I): able to inhibit nicotinamide phosphoribosyltransferase. The disclosure also relates to the use of compounds of formula (I) for treatment of pathological conditions in which NAMPT inhibition might be beneficial, such as acute and chronic inflammation, cancer and metabolic disorders. | 03-17-2016 |
20160137627 | DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF - The invention relates to compounds corresponding to formula (I), in the form of the base or of an acid-addition salt: | 05-19-2016 |
20160143893 | SULFOXIMINE SUBSTITUTED 5-FLUORO-N-(PYRIDIN-2-YL)PYRIDIN-2-AMINE DERIVATIVES AND THEIR USE AS CDK9 KINASE INHIBITORS - The present invention relates to 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). | 05-26-2016 |
20160176860 | INHIBITORS OF LC3/ATG3 INTERACTION AND THEIR USE IN THE TREATMENT OF CANCER | 06-23-2016 |
20160184283 | ANTIBACTERIAL COMPOUNDS - Disclosed are compounds of formula (I): | 06-30-2016 |
20160185784 | BICYCLIC UREAS AND THIADIAZOLIDINE-1, 1-DIOXIDES AS CETP INHIBITORS - Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein X is —C(═O) or —S(O) | 06-30-2016 |
20190142813 | MULTISUBSTITUTED AROMATIC COMPOUNDS AS SERINE PROTEASE INHIBITORS | 05-16-2019 |