CoNCERT Pharmaceuticals Inc. Patent applications |
Patent application number | Title | Published |
20160068519 | INHIBITORS OF THE ENZYME UDP-GLUCOSE: N-ACYL-SPHINGOSINE GLUCOSYLTRANSFERASE - This invention relates to novel inhibitors of UDP-glucose: N-acyl-sphingosine glucosyltransferase and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of UDP-glucose: N-acyl-sphingosine glucosyltransferase. | 03-10-2016 |
20160031801 | DEUTERATED 2-AMINO-3-HYDROXYPROPANOIC ACID DERIVATIVES - This invention relates to novel 2-amino-3-hydroxypropanoic acid derivatives and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an NMDA glycine-site antagonist. | 02-04-2016 |
20150366853 | Derivatives of Pyrazole-Substituted Amino-Heteroaryl Compounds - This invention relates to novel pyrazole-substituted amino-heteroaryl compounds of Formula I: | 12-24-2015 |
20150291594 | Deuterated Ponatinib - The present invention provides novel derivatives of ponatinib (AP-24534), a BCR-ABL kinase inhibitor with activity against the T3151 Gatekeeper mutant. | 10-15-2015 |
20150210699 | Deuterated Ibrutinib - The present invention in one embodiment provides a compound of Formula (I); or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula (I) are as defined in the specification. | 07-30-2015 |
20150141431 | PYRAZINOISOQUINOLINE COMPOUNDS - This invention in one embodiment is directed to a compound of Formula Ia; | 05-21-2015 |
20150105438 | SUBSTITUTED ISOINDOLINE-1,3-DIONE DERIVATIVES - This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast. | 04-16-2015 |
20150073009 | MORPHINAN COMPOUNDS - This invention relates to novel morphinan compounds and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ | 03-12-2015 |
20150011595 | Inhibitors of Cholesterol Ester Transfer Protein - The invention relates to novel oxazolidinones their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering cholesterol ester transfer protein inhibitors. | 01-08-2015 |
20140343119 | 4-HYDROXYBUTYRIC ACID ANALOGS - This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate. | 11-20-2014 |
20140336387 | SYNTHESIS OF DEUTERATED CATECHOLS AND BENZO[D][1,3]DIOXOLES AND DERIVATIVES THEREOF - The present invention provides a convenient and efficient process for the synthesis of d | 11-13-2014 |
20140315940 | MORPHINAN COMPOUNDS - This invention relates to novel morphinan compounds and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ | 10-23-2014 |
20140296263 | SUBSTITUTED XANTHINE DERIVATIVES - The present invention in one embodiment relates to a compound of Formula (I); or a pharmaceutically acceptable salt thereof, wherein: each of R | 10-02-2014 |
20140213553 | CARBAMOYLPYRIDONE DERIVATIVES - This invention relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an HIV integrase inhibitor. | 07-31-2014 |
20140155444 | TETRAHYDRONAPHTHALENE DERIVATIVES - This invention relates to novel tetrahydronaphthalene derivatives, and pharmaceutically acceptable salts thereof according to the following formulae, in one embodiment: | 06-05-2014 |
20140128469 | DEUTERATED N-BUTYL BUMETANIDE - The present invention provides a compound of Formula I: | 05-08-2014 |
20140121226 | SUBSTITUTED XANTHINE DERIVATIVES - This invention relates to novel deuterated compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. In particular, this invention relates to novel substituted xanthine derivatives that are deuterated derivatives of a pentoxifylline metabolite. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed deuterated compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial. The compounds of the invention are represented by the following structural formula: | 05-01-2014 |
20140113925 | Morphinan Compounds - This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ | 04-24-2014 |
20140046060 | METHOD OF UTILIZING RECYCLED DEUTERIUM OXIDE IN THE SYNTHESIS OF DEUTERATED COMPOUNDS - The present invention provides a method for utilizing recycled deuterium oxide synthesis of deuterated compounds. | 02-13-2014 |
20140024652 | SUBSTITUTED TRIAZOLOPHTHALAZINE DERIVATIVES - This invention relates to novel substituted triazolophthalazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering selective α5 receptor partial or full inverse agonists. | 01-23-2014 |
20140018390 | DEUTERATED BENZO[D][1,3]-DIOXOL DERIVATIVES - The present invention relates to an isotopologue of Compound 1 substituted with deuterium at the methylene carbon of the benzodioxol ring. The isotopologues of this invention selective serotonin reuptake inhibitors (SSRIs) and possess unique biopharmaceutical and metabolic properties compared to Compound 1. They may also be used to accurately determine the concentration of Compound 1 in biological fluids and to determine metabolic patterns of Compound 1 and its isotopologues. The invention further provides compositions comprising these deuterated isotopologues and methods of treating diseases and conditions that are responsive to increased neuronal serotonin transmission, alone and in combination with additional agents. | 01-16-2014 |
20140018379 | PYRIMIDINE DERIVATIVES - The present invention provides a compound of Formula I or Formula VI: | 01-16-2014 |
20140017739 | PROCESS FOR PREPARING AN ENANTIOMERICALLY ENRICHED, DEUTERATED SECONDARY ALCOHOL FROM A CORRESPONDING KETONE WITHOUT REDUCING DEUTERIUM INCORPORATION - The present invention provides a convenient and efficient process for the preparation of enantiomerically enriched, deuterated secondary alcohols without reducing deuterium incorporation. | 01-16-2014 |
20140005211 | DERIVATIVES OF PYRAZOLE-SUBSTITUTED AMINO-HETEROARYL COMPOUNDS | 01-02-2014 |
20130345282 | SUBSTITUTED ISOINDOLINE-1,3-DIONE DERIVATIVES - This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast. | 12-26-2013 |
20130324564 | POLYMORPHS OF (S)-1-(4,4,6,6,6-PENTADEUTERO-5-HYDROXYHEXYL)-3-7-DIMETHYL-1H-PURINE-2,6(- 3H,7H)-DIONE - The present invention provides individual crystalline polymorphs of (S)-1-(4,4,6, 6,6-pentadeutero-5-hydroxy-hexyl)-3,7-dimethyl-1H-purine-2,6(3H,7H)-dione designated Form 1, Form 2, Form 3 and Form 4. Each polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data (“XRPD”); (b) differential scanning calorimetry (“DSC”); and (e) thermo gravimetric analysis (TGA). | 12-05-2013 |
20130317033 | SUBSTITUTED TRIAZOLO-PYRIDAZINE DERIVATIVES - This invention relates to novel substituted triazolo-pyridazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an α1-GABA | 11-28-2013 |
20130310415 | MORPHINAN COMPOUNDS - This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ | 11-21-2013 |
20130280768 | PROCESS FOR PREPARING AN ENANTIOMERICALLY ENRICHED, DEUTERATED SECONDARY ALCOHOL FROM A CORRESPONDING KETONE WITHOUT REDUCING DEUTERIUM INCORPORATION - The present invention provides a process for the preparation of enantiomerically enriched, deuterated secondary alcohols of Formula 1-A by employing ketoreductases or carbonyl reductases without reducing deuterium incorporation. | 10-24-2013 |
20130225590 | SUBSTITUTED TRIAZOLO-PYRIDAZINE DERIVATIVES - This invention relates to novel substituted triazolo-pyridazines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an α1-GABA-A receptor antagonist and/or a α2, α3 and α5 GABA-A receptor agonist. | 08-29-2013 |
20130150408 | SUBSTITUTED DIOXOPIPERIDINYL PHTHALIMIDE DERIVATIVES - This invention relates to novel substituted dioxopiperidinyl phthalimide derivatives and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an immunomodulatory agent. | 06-13-2013 |
20130131021 | ANALOGUES OF CILOSTAZOL - This invention relates to novel compounds which are derivatives of the phosphodiesterase inhibitor, cilostazol and pharmaceutically acceptable salts thereof. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administration of a phosphodiesterase inhibitor, such as cilostazol. The invention also relates to the use of the disclosed compounds and compositions as reagents in analytical studies involving cilostazol. | 05-23-2013 |
20130121963 | N-PHENYL-2-PYRIMIDINEAMINE DERIVATIVES - This disclosure relates to novel N-phenyl-2-pyrimidineamines and pharmaceutically acceptable salts thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering protein-tyrosine kinase inhibitors. | 05-16-2013 |
20130109707 | FLUOROURACIL DERIVATIVES | 05-02-2013 |
20130109660 | NOVEL PYRIMIDINECARBOXAMIDE DERIVATIVES | 05-02-2013 |
20130095100 | HETEROCYCLIC KINASE INHIBITORS - This invention relates to novel 2-{6-[4-(2-hydroxy-ethyl)-piperazin-1-yl]-2-methyl-pyrimidin-4-ylamino}-thiazole-5-carboxylic acid (2-chloro-6-methyl-phenyl)-amide derivatives, and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by the inhibition of kinases including Src-kinase and Bcr-Abl kinase. | 04-18-2013 |
20130029997 | PYRAZINOISOQUINOLINE COMPOUNDS - This invention in one embodiment is directed to a compound of Formula Ia; | 01-31-2013 |
20130018193 | DEUTERATED PIRFENIDONE - This invention relates to novel substituted pyridinones, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a TNF (tumor necrosis factor)-alpha production inhibitor/TGF (transforming growth factor)-beta inhibitor. | 01-17-2013 |
20130012565 | 4-HYDROXYBUTYRIC ACID ANALOGS - This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate. | 01-10-2013 |
20120295925 | SUBSTITUTED DERIVATIVES OF BICYCLIC [4.3.0] HETEROARYL COMPOUNDS - This invention relates to novel compounds of the Formula A, B, or C, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier. | 11-22-2012 |
20120264721 | ANALOGUES OF CILOSTAZOL - This invention relates to novel compounds which are derivatives of the phosphodiesterase inhibitor, cilostazol and pharmaceutically acceptable salts thereof. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administration of an phosphodiesterase inhibitor, such as cilostazol. The invention also relates to the use of the disclosed compounds and compositions as reagents in analytical studies involving cilostazol. | 10-18-2012 |
20120237474 | FLUORINATED DIARYL UREA DERIVATIVES - This invention relates to novel diaryl urea compounds, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of multiple kinases. | 09-20-2012 |
20120149709 | PYRAZINOISOQUINOLINE COMPOUNDS - This invention relates to novel compounds that are pyrazinoisoquinoline derivatives, and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrazinoisoquinoline derivatives that are derivatives of praziquantel. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel. | 06-14-2012 |
20120122944 | TETRAHYDRONAPHTHALENE DERIVATIVES - This invention relates to novel tetrahydronaphthalene derivatives, and pharmaceutically acceptable salts thereof according to the following formulae, in one embodiment: | 05-17-2012 |
20120004236 | SUBSTITUTED TRIAZOLO-PYRIDAZINE DERIVATIVES - This invention relates to novel substituted triazolo-pyridazines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an α1-GABA-A receptor antagonist and/or a α2, α3 and α5 GABA-A receptor agonist. | 01-05-2012 |
20110313004 | DEUTERATED PYRIDINONES - This invention relates to novel substituted pyridinones, their deuterium-modified derivatives and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a TNF (tumor necrosis factor) alpha production inhibitor/TGF (transforming growth factor) beta inhibitor. | 12-22-2011 |
20110306627 | Morphinan Compounds - This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ | 12-15-2011 |
20110300132 | 4-AMINOQUINAZOLINE PRODRUGS - This invention relates to prodrugs of 4-aminoquinazoline compounds, and to pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the EGFR and HER2. | 12-08-2011 |
20110288126 | SUBSTITUTED DIOXOPIPERIDINYL PHTHALIMIDE DERIVATIVES - This invention relates to novel substituted dioxopiperidinyl phthalimide derivatives and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an immunomodulatory agent. | 11-24-2011 |
20110251131 | DEUTERATED 2-AMINO-3-HYDROXYPROPANOIC ACID DERIVATIVES - This invention relates to novel 2-amino-3-hydroxypropanoic acid derivatives and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an NMDA glycine-site antagonist. | 10-13-2011 |
20110237635 | TETRAHYDRONAPHTHALENE DERIVATIVES - This invention relates to novel tetrahydronaphthalene derivatives, and pharmaceutically acceptable salts thereof according to the following formulae, in one embodiment: | 09-29-2011 |
20110230514 | Morphinan Compounds - This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ | 09-22-2011 |
20110196012 | DEUTERATED MACROCYCLIC INHIBITORS OF VIRAL NS3 PROTEASE - This invention relates to novel macrocyclic protease inhibitors and their pharmaceutically acceptable salts thereof. This invention also provides compositions comprising at least one compound of this invention and the use of such compositions in methods of treating a flavivirus infection or liver fibrosis in a patient in need thereof. | 08-11-2011 |
20110172280 | Substituted Benzimidazoles - This invention relates to novel substituted benzimidazoles and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound that modulates the GABA | 07-14-2011 |
20110172235 | SUBSTITUTED TRIAZOLOPHTHALAZINE DERIVATIVES - This invention relates to novel substituted triazolophthalazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering selective α5 receptor partial or full inverse agonists. | 07-14-2011 |
20110160235 | TRIAZOLYL TROPANE DERIVATIVES - This invention relates to novel triazolyl tropane derivatives, their acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by blocking or reducing the binding ability of the CCR5 receptor. | 06-30-2011 |
20110160217 | DEUTERIUM ENRICHED ANALOGUES OF TADALAFIL AS PDE5 INHIBITORS - The present invention relates to derivatives of tadalafil, substituted with fluorine on the methylene carbon atom situated between the oxygens of the benzodioxol ring, and optionally further substituted with deuterium atoms in place of normally abundant hydrogen, and | 06-30-2011 |
20110152227 | DEUTERIUM LABELLED DERIVATIVES OF 3-(2-HYDROXY-5-METHYPHENYL)-N,N-DIISOPROPYL-3-PHENYLPROPYLAMINE AND METHODS OF USE THEREOF - This invention relates to novel derivatives of tolterodine, 5-hydroxymethyl tolterodine, fesoterodine and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by muscarinic receptor antagonists. | 06-23-2011 |
20110117084 | VANDETANIB DERIVATIVES - This invention relates to novel quinazoline derivatives and their acceptable acid addition salts. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by inhibitory activity against the VEGF receptor tyrosine kinase. | 05-19-2011 |
20110097320 | 4-AMINOQUINAZOLINE DERIVATIVES AND METHODS OF USE THEREOF - This invention relates to novel 4-aminoquinazolines, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the EGFR and HER-2. | 04-28-2011 |
20110092468 | Pharmaceutical Calcimimetics - This invention relates to novel calcimimetic compounds, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by binding to, and modulating the sensitivity of, calcium receptors on the parathyroid gland. | 04-21-2011 |
20110082147 | SUBSTITUTED IMIDAZOTRIAZINES - This invention relates to novel substituted imidazotriazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound showing partial-agonist activity at the GABA α2, α3 and α5 subtype receptors, and antagonist activity at the al subtype receptor. | 04-07-2011 |
20110065711 | SUBSTITUTED TRIAZOLO-PYRIDAZINE DERIVATIVES - This invention relates to novel substituted triazolo-pyridazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an α1-GABA | 03-17-2011 |
20110059046 | DERIVATIVES OF GEFITINIB - This invention relates to novel quinazoline derivatives, their derivatives, pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by inhibiting cell surface tyrosine receptor kinases. | 03-10-2011 |
20100305173 | HYDROXYETHYLAMINO SULFONAMIDE DERIVATIVES - This invention relates to novel hydroxyethylamino sulfonamides, their derivatives, pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound with the ability to act as an HIV (human immunodeficiency virus) protease inhibitor. | 12-02-2010 |
20100260674 | QUINAZOLINE DERIVATIVES AND METHODS OF TREATMENT - This invention relates to novel quinazoline derivatives, and their pharmaceutically acceptable salts. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by inhibiting cell surface tyrosine receptor kinases. | 10-14-2010 |
20100221221 | N-PHENYL-2-PYRIMIDINEAMINE DERIVATIVES - This disclosure relates to novel N-phenyl-2-pyrimidineamines and pharmaceutically acceptable salts thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering protein-tyrosine kinase inhibitors. | 09-02-2010 |
20100184862 | PROSTACYCLIN DERIVATIVES - This invention relates to novel prostacyclin derivatives, their acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by prostacyclin, and in particular those diseases and conditions beneficially treated by dilators of systemic and pulmonary arterial vascular beds or by platelet aggregation inhibitors. | 07-22-2010 |
20100160247 | Synthesis of deuterated morpholine derivatives - The present invention is directed to a process for preparing a 2,26,6-d | 06-24-2010 |
20100152214 | NOVEL PYRIMIDINECARBOXAMIDE DERIVATIVES - This disclosure relates to novel HIV integrase inhibitors their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating HIV infections. | 06-17-2010 |
20100120786 | Piperazine Derivatives - This invention relates to novel compounds that are piperazine derivatives, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel piperazine compounds that are derivatives of the chemokine CCR5 receptor antagonist, vicriviroc. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering chemokine CCR5 receptor antagonists, such as vicriviroc. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving vicriviroc. | 05-13-2010 |
20100056529 | SUBSTITUTED TRIAZOLO-PYRIDAZINE DERIVATIVES - This invention relates to novel substituted triazolo-pyridazines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an α1-GABA-A receptor antagonist and/or a α2, α3 and α5 GABA-A receptor agonist. | 03-04-2010 |
20100029716 | NOVEL 1,2,3,4- TETRAHYDROQUINOLINE DERIVATIVES - The present invention relates to a novel derivative of Compound 1 selectively substituted with fluorine and/or deuterium and optionally further substituted with deuterium and | 02-04-2010 |
20100004340 | NAPHTHYL(ETHYL) ACETAMIDES - This disclosure relates to novel melatonin analogues or naphthyl(ethyl)acetamides, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a dual melatoninergic agonist and serotoninergic antagonist. | 01-07-2010 |
20090325976 | PROSTACYCLIN DERIVATIVES - This invention relates to novel prostacyclin derivatives, their acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by prostacyclin, and in particular those diseases and conditions beneficially treated by dilators of systemic and pulmonary arterial vascular beds or by platelet aggregation inhibitors. | 12-31-2009 |
20090291152 | DIBENZOTHIAZEPINE DERIVATIVES - This invention relates to novel 11-[4-[2-(2-Hydroxyethoxy)ethyl]piperazin-1-yl]dibenzo[b,f][1,4]thiazepine derivatives, their acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by antagonists of seratonergic 5HT1A and 5HT2 receptors, dopaminergic D1 and D2 receptor, histaminergic H1 receptors, and/or adrenergic α1 and α2 receptors. | 11-26-2009 |
20090270425 | 3-(DIHYDRO-1H-PYRAZOLO[4,3-D]PYRIMIDIN-5-YL)-4-PROPOXYBENZENESULFONAMIDE DERIVATIVES AND METHODS OF USE - This invention relates to novel 3-(dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide compounds, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of cyclic guanosine 3′,5′-monophosphate specific phosphodiesterase (cGMP-specific PDE), in particular PDE5. | 10-29-2009 |
20090270336 | Piperazine derivatives - This invention relates to novel compounds that are piperazine derivatives, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel piperazine compounds that are derivatives of the chemokine CCR5 receptor antagonist, vicriviroc. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering chemokine CCR5 receptor antagonists, such as vicriviroc. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving vicriviroc. | 10-29-2009 |
20090269354 | QUINAZOLINE DERIVATIVES AND METHODS OF TREATMENT - This invention relates to novel quinazoline derivatives, and their pharmaceutically acceptable salts. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by inhibiting cell surface tyrosine receptor kinases. | 10-29-2009 |
20090258902 | BIPHENYL-PYRAZOLECARBOXAMIDE COMPOUNDS - The present invention relates to biphenyl-pyrazole compounds and in particular biphenyl-pyrazolecarboxamides. The invention further provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by antagonism or inverse agonism of the CB | 10-15-2009 |
20090239886 | Substituted xanthine derivatives - This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial. | 09-24-2009 |
20090197899 | 3-(Dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide Derivatives and Methods of Use - This invention relates to novel 3-(dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide compounds, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of cyclic guanosine 3′,5′-monophosphate specific phosphodiesterase (cGMP-specific PDE), in particular PDE5. | 08-06-2009 |
20090185999 | DERIVATIVES OF GEFITINIB - This invention relates to novel quinazoline derivatives, their derivatives, pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by inhibiting cell surface tyrosine receptor kinases. | 07-23-2009 |
20090176744 | Deuterated fingolimod - This invention relates to novel compounds that are deuterated derivatives of fingolimod and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a lysophospholipid edg1 (S1P1) receptor agonist, such as fingolimod. | 07-09-2009 |
20090149544 | Alpha-aminoamide derivatives - This invention relates to novel alpha-aminoamide derivatives, their pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of monoamine oxidase type B (MAO-B) and/or a sodium (Na | 06-11-2009 |
20090149399 | HETEROCYCLIC KINASE INHIBITORS - This invention relates to novel 2-{6-[4-(2-hydroxy-ethyl)-piperazin-1-yl]-2-methyl-pyrimidin-4-ylamino}-thiazole-5-carboxylic acid (2-chloro-6-methyl-phenyl)-amide derivatives, and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by the inhibition of kinases including Src-kinase and Bcr-Abl kinase. | 06-11-2009 |
20090143432 | Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof - The present invention provides a convenient and efficient process for the synthesis of d | 06-04-2009 |
20090143363 | Deuterated lorcaserin - This invention relates to novel compounds that are 3-benzazepine derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel 3-benzazepine derivatives that are derivatives of lorcaserin. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a 5-HT | 06-04-2009 |
20090137457 | Pyrimidinedione derivatives - This invention relates to novel compounds that are pyrimidinedione derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrimidinedione derivatives that are derivatives of alogliptin. This invention also provides compositions comprising one or more compounds of this invention and a carrier, and the use of the disclosed compound and compositions in methods of treating diseases and conditions that are beneficially treated by administering a dipeptidyl peptidase IV (DPP4) inhibitor. | 05-28-2009 |
20090131485 | Deuterated pirfenidone - This invention relates to novel substituted pyridinones, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a TNF (tumor necrosis factor)-alpha production inhibitor/TGF (transforming growth factor)-beta inhibitor. | 05-21-2009 |
20090105147 | Deuterated etravirine - This disclosure relates to novel di-aryl-pyrimidine (DAPY) compounds and pharmaceutically acceptable salts thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a non-nucleoside reverse transcriptase inhibitor (NNRTI). | 04-23-2009 |
20090042842 | Analogues of cilostazol - This invention relates to novel compounds which are derivatives of the phosphodiesterase inhibitor, cilostazol and pharmaceutically acceptable salts thereof. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administration of an phosphodiesterase inhibitor, such as cilostazol. The invention also relates to the use of the disclosed compounds and compositions as reagents in analytical studies involving cilostazol. | 02-12-2009 |
20090036357 | Azapeptide derivatives - This invention relates to novel compounds that are azapeptides, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel azapeptide compounds that are derivatives of the HIV protease inhibitor atazanavir sulfate. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering HIV protease inhibitors. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving atazanavir. | 02-05-2009 |
20090035324 | NOVEL PYRIMIDINECARBOXAMIDE DERIVATIVES - This disclosure relates to novel HIV integrase inhibitors their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating HIV infections. | 02-05-2009 |
20080280936 | Morphinan Compounds - This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ | 11-13-2008 |
20080280927 | 3-(DIHYDRO-1H-PYRAZOLO[4,3-D]PYRIMIDIN-5-YL)-4-PROPOXYBENZENESULFONAMIDE DERIVATIVES AND METHODS OF USE - This invention relates to novel 3-(dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide compounds, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of cyclic guanosine 3′,5′-monophosphate specific phosphodiesterase (cGMP-specific PDE), in particular PDE5. | 11-13-2008 |
20080280908 | NAPHTHYL(ETHYL) ACETAMIDES - This disclosure relates to novel melatonin analogues or naphthyl(ethyl)acetamides, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a dual melatoninergic agonist and serotoninergic antagonist. | 11-13-2008 |
20080261983 | Substituted morpholinyl compounds - This disclosure relates to novel substituted morpholinyl compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a 5HT4 serotonin receptor agonist. | 10-23-2008 |
20080255194 | 1,2-Benzisoxazol-3-yl Compounds - This invention relates to novel 1,2-benzisoxazol-3-yl compounds, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an antagonist of both dopamine and serotonin receptors. | 10-16-2008 |