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| Number | Title | Issue Date |
| 8183238 | Bicyclic and tricyclic compounds as KAT II inhibitors Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive defi... | 05/22/2012 |
| 8168634 | Thiazole derivatives as kinase inhibitors A series of thiazole derivatives which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardi... | 05/01/2012 |
| 8163744 | Tetrahydro-isoquinolin-1-ones for the treatment of cancer The present invention provides a compound selected from compounds of formula I as ligand binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy. Compounds of formula (I) can be used as therapeut... | 04/24/2012 |
| 8148372 | Metabotropic glutamate receptor isoxazole ligands and their use as potentiators—286 Compounds in accord with Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, pharmaceutically acceptable salts, methods of making, pharmaceutical composition... | 04/03/2012 |
| 8133889 | Dihydroindolone compounds, a process for their preparation and pharmaceutical compositions containing them Compounds of formula (I): wherein: m and n represent 1 or 2, A represents a pyrrolyl group, X represents a C(O), S(O) or SO2 group, ... | 03/13/2012 |
| 8129375 | Isoindoline compounds and methods of their use Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases. ... | 03/06/2012 |
| 8101608 | Compounds and compositions as protein kinase inhibitors The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or d... | 01/24/2012 |
| 8097623 | Indoles useful in the treatment of inflammation There is provided compounds of formula (I), wherein X1, Q, T, Y, R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts t... | 01/17/2012 |
| 8088768 | Protein kinase and phosphatase inhibitors The present invention provides a method for identifying inhibitors of protein kinases and/or protein phosphatases. Methods are also provided for inhibiting protein kinase and/or protein phosphatase activity. Specific non-peptide protein tyrosine kinase and/or protei... | 01/03/2012 |
| 8048880 | Treatment of cardiovascular disease and dyslipidemia using secretory phospholipase A(SPLA) inhibitors and SPLAinhibitor combination therapies Administration of sPLA2 inhibitors has been found to decrease cholesterol levels, atherosclerotic plaque formation and aortic aneurysm in mice, and to decrease cholesterol and triglyceride levels in humans. Interestingly, administration of sPLA2 | 11/01/2011 |
| 8039470 | Kinase inhibitor compounds The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes... | 10/18/2011 |
| 8017606 | Quinoline derivatives as antibacterial agents Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of Formula (Ia) or (Ib) | 09/13/2011 |
| 8012968 | Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, and compositions, and uses thereof This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a ... | 09/06/2011 |
| 8012967 | Minor groove binders There is provided compounds of formula (I), wherein R1, R11, R12, Qa, X, Qb, Qc, A and D have meanings given in the description, or a pharmaceutically acceptable salt or solvate thereof, which compoun... | 09/06/2011 |
| 8008294 | Citrate salt of an indole derivative and its pharmaceutical use The salt, the 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile citrate, a process for its preparation, pharmaceutical formulations containing it and the use of it in therapy, and particularly in the therapy of GSK3 related conditions and di... | 08/30/2011 |
| 8008295 | Tyrosine kinase inhibitors The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a... | 08/30/2011 |
| 7994165 | Aryl aniline derivatives as βadrenergic receptor agonists The invention provides novel β2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β2 adrenergic receptor... | 08/09/2011 |
| 7981888 | 1-oxyalkyl-2-carboxyl-7-nonsubstituted indole derivatives Compounds of Formula I wherein A1, B1, C1, D1, E1, F1 and L1 are as defined herein, which inhibit the activity of anti-apoptotic Mcl-1 protein, co... | 07/19/2011 |
| 7910584 | 3-spiroindolin-2-one derivatives, preparation and therapeutic use thereof The subject of the present invention is a compound of formula (I): in the base, hydrate or solvate state, in the form of cis/trans isomers or of mixtures thereof, preparation and therapeutic use thereof. ... | 03/22/2011 |
| 7906509 | Inhibitors of bruton's tyrosine kinase This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: wherein, variables R, X, Y1, Y2, Y3, Y4, n an... | 03/15/2011 |
| 7902190 | Indol derivatives, the method for preparing thereof and composition for the prevention and treatment of metabolic disorder containing the same as an active ingredient Disclosed are indole derivatives, a preparation method thereof, and a composition for the prevention and treatment of metabolic diseases, containing the same as an active ingredient. The indole derivatives have inhibitory activity against DGAT (diacylglycerol acyltr... | 03/08/2011 |
| 7897601 | Cannabinoid receptor modulators A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, is useful in treating diseases, disorders, or conditions such as obesity, metabolic disorders, addict... | 03/01/2011 |
| 7897602 | Indolinone compounds as kinase inhibitors Indolinone compounds of formula (I) or (II): wherein A, R1, R2, R3, R4, R5, R6, R7, and n are defined herein. Also disclosed are methods for decre... | 03/01/2011 |
| 7888353 | Metabotropic glutamate receptor isoxazole ligands and their use as potentiators Compounds in accord with Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, pharmaceutically acceptable salts, methods of making, pharmaceutical composition... | 02/15/2011 |
| 7872004 | 6-(heterocyclyl-substituted benzyl)-4-oxoquinoline compound and use thereof as HIV integrase inhibitor The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmac... | 01/18/2011 |
| 7868003 | Substituted 4-phenyltetrahydroisoquinolines, pharmaceutical compositions comprising them and therapeutic methods for their use The invention relates to substituted 4-phenyltetrahydroisoquinolines of formula I wherein R1-R8, N, W, X and Z are defined herein. These compounds and pharmaceutical compositions comprising them are useful in the treatment ... | 01/11/2011 |
| 7863271 | 2-aminobenzoxazole carboxamides as 5HT3 modulators Compounds of formulae I, II and III: are disclosed as 5-HT3 inhibitors. The compounds are useful in treating CINV, IBS-D and other diseases and conditions. ... | 01/04/2011 |
| 7858619 | Substituted tetrahydroisochinolines as MMP inhibitors, related production method and use as medicine The present invention is directed to a compound of formula (I), wherein R1, R2, R3, R4, A, L and n are as defined herein, its pharmaceutical composition, preparation and uses as a... | 12/28/2010 |
| 7858620 | Cyanoisoquinoline This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present inven... | 12/28/2010 |
| 7846930 | Diaryl-substituted tetrahydroisoquinolines as histamine Hreceptor and serotonin transporter modulators Certain diaryl-substituted tetrahydroisoquinoline compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases. ... | 12/07/2010 |
| 7816352 | Apoptosis inhibitors The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastroi... | 10/19/2010 |
| 7786116 | 2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE) The present invention is directed to novel 2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD), mild cognitive impairment, senility and/or dementia. The compounds of the present invent... | 08/31/2010 |
| 7786115 | Amide derivatives The invention concerns a compound of the Formula I wherein m is 0-2 and each R1 is a group such as hydroxy, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is halogeno, trifluoromethyl o... | 08/31/2010 |
| 7781434 | Metabotropic glutamate receptor isoxazole ligands and their use as potentiators—286 Compounds in accord with Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, pharmaceutically acceptable salts, methods of making, pharmaceutical composition... | 08/24/2010 |
| 7772232 | Quinazolinyl compounds as inhibitors of potassium channel function A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein. Said compounds being useful as inhibitors of pot... | 08/10/2010 |
| 7763614 | Isoquinoline potassium channel inhibitors The present invention relates to compounds of structural formula I: I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like. ... | 07/27/2010 |
| 7745435 | Triheterocyclic compounds and compositions thereof The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, co... | 06/29/2010 |
| 7741322 | Isoquinolinone potassium channel inhibitors The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like. ... | 06/22/2010 |
| 7709477 | Methods for treating cancer The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, co... | 05/04/2010 |
| 7709476 | Isoquinolinone potassium channel inhibitors The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like. ... | 05/04/2010 |
