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| Number | Title | Issue Date |
| 8163753 | 2,3-dihydro-6-nitroimidazo (2,1-b) oxazole compounds for the treatment of tuberculosis The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1) in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and —(CH2)nR2 m... | 04/24/2012 |
| 8163755 | Hexahydrooxazinopterine compounds The present invention provides mTOR inhibitors of the formula wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods o... | 04/24/2012 |
| 8163754 | Purine derivatives for use as adenosine A-2A receptor agonists Compounds of formula I in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adeno... | 04/24/2012 |
| 8114878 | 6,7-dihydrothieno[3,2-d]pyrimidine for the treatment of inflammatory diseases The invention relates to new dihydrothienopyrimidine of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein X is SO or SO2, but p... | 02/14/2012 |
| 8114877 | Organic compounds Compounds of formula I in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adeno... | 02/14/2012 |
| 8093249 | Pyrazolo[1,5-A]pyrimidine-carbonyl-piperazine derivatives The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calc... | 01/10/2012 |
| 8063051 | 9-substituted-8-oxo-adenine compounds as toll-like receptor (TLR7) modulators The present invention provides compounds of formula where n, R1, R2, A, X1, Y1, Z1, X2 and Y2 are as defined in the specification, processes for t... | 11/22/2011 |
| 8063050 | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compou... | 11/22/2011 |
| 8044056 | Adenine compound A novel adenine compound represented by the formula (1): [wherein R1 is substituted or unsubstituted alkyl, etc., X is oxygen, etc., A1 is 4- to 8-membered substituted or unsubstituted saturated nitrog... | 10/25/2011 |
| 8017614 | Arylindenopyrimidines compound and use as an adenosine A2a receptor antagonists This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. ... | 09/13/2011 |
| 8003651 | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of us... | 08/23/2011 |
| 7994172 | [1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases The invention provides compounds of formula (I) and methods for inhibition of kinases, more specifically p70S6 kinases, and more preferably p70S6, Akt-1 and Akt-2 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulati... | 08/09/2011 |
| 7863279 | Triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives, preparation thereof and therapeutic use thereof The invention relates to the triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives of general formula (I): Wherein X, A, R1 and R2 are as defined herein. The invention... | 01/04/2011 |
| 7863278 | Isethionate salt of a selective CDK4 inhibitor Disclosed are polymorphs of the isethionate salt of 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one, which is a selective cyclin-dependent kinase 4 (CDK4) inhibitor useful for treating inflammation and cell prol... | 01/04/2011 |
| 7834019 | Substituted pyrazolo[3,4-d]pyrimidinone derivatives The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alk... | 11/16/2010 |
| 7825122 | Diaza heterocyclic sulfonamide derivatives and their uses Diaza heterocyclic sulfonamide derivatives according to formula I have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R7, R8, R... | 11/02/2010 |
| 7737147 | Methods and compositions to enhance the efficacy of phosphodiesterase inhibitors Methods for treatment of sexual dysfunction in men and women using combinations of phosphodiesterase (PDE) type 5 inhibitors and l-deprenyl or propargylamine compounds are described. Methods of reducing the dosage and preventing the side effects of PDE type 5 inhibi... | 06/15/2010 |
| 7723340 | Haloaryl substituted aminopurines, compositions thereof, and methods of treatment therewith Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and and R3 are as defined herein, compositions comprising an effective amoun... | 05/25/2010 |
| 7723341 | Compounds for the treatment of inflammatory diseases Dihydrothienopyrimidines of formula 1 and the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of respiratory or gastrointestinal complaints or ... | 05/25/2010 |
| 7691860 | Sulfonamide derivatives The present invention relates to compounds of the general formula (I): wherein A, B, C and D each independently are a methine group or a nitrogen atom, said methine group optionally having a substit... | 04/06/2010 |
| 7666872 | Use for PDE5 inhibitors The present invention is concerned with the use of PDE5 inhibitors in medicine. ... | 02/23/2010 |
| 7662822 | Substituted azaquinazolines having an antiviral action This invention relates to substituted azaquinazolines, to a process for their preparation, to pharmaceutical compositions containing them, and to their use for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular agains... | 02/16/2010 |
| 7550468 | Theophylline and 3-isobutyl-1 methylxanthine based N-7 substituted derivatives displaying inhibitory activities on PDE-5 phospodiesterase A variety of N-substituted derivatives are based upon the base chemicals of that provide for the induction of cavernosal relaxation in animals. R2 is a derivative based on a hetroaromatic group, an aromatic group or a cyclo... | 06/23/2009 |
| 7524847 | Fused 1,3-dihydro-imidazole ring compounds The objective of this invention is to provide novel compounds that show excellent DPPIV-inhibiting activity. The present invention provides compounds represented by the general formula (I), salts thereof, or hydrates thereof, | 04/28/2009 |
| 7511045 | Compounds for the treatment of inflammatory diseases Dihydrothienopyrimidines of formula 1 and the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of respiratory or gastrointestinal complaints or ... | 03/31/2009 |
| 7504398 | Substituted-4-(pyrrolo pyrimidin-6-yl)benzenesulphonamide derivatives This invention is directed to selective antagonists of A2A and/or A2B adenosine receptors having the general formula (I); to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy. | 03/17/2009 |
| 7470690 | 4-(2-Fluorophenyl)-6-methyl-2-(1-piperazinyl)thieno[2,3-D)pyrimidine in the treatment of functional bowel disorder Use of 4-(2-Fluorophenyl)-6-Methyl-2-(1-Piperazinyl)Thieno[2,3-D]Pyrimidine or a salt thereof for the manufacture of a medicament for the treatment of functional bowel disorder. ... | 12/30/2008 |
| 7462618 | Treatment of inflammatory autoimmune diseases with alpha-adrenergic antagonists and beta-adrenergic agonists The present invention discloses a novel compound and method for the treatment of inflammatory autoimmune diseases, for example, rheumatoid arthritis, using α-adrenergic antagonists and β-adrenergic agonists in combination. Treatment of animals, namely humans, with... | 12/09/2008 |
| 7429596 | 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof This invention generally relates to pyrazolo pyrimidine derivatives useful as inhibitors of short chain dehydrogenase/reductase (SDR) family of NAD(P)(H) dependent oxido-reductases. The invention further relates to pharmaceutical compositions and methods of preventi... | 09/30/2008 |
| 7419981 | Synergistic combinations of an alpha-2-delta ligand and a cGMP phosphodieterse 5 inhibitor The instant invention relates to a combination of an alpha-2-delta ligand and a PDEV inhibitor for use in therapy, particularly in the treatment of pain, particularly neuropathic pain. Particularly preferred alpha-2-delta ligands are gabapentin and pregabalin. A par... | 09/02/2008 |
| 7414058 | Adenosine Areceptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders There is disclosed a method for the treatment of Extra Pyramidal syndrome (EPS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents useful for treating EPS. ... | 08/19/2008 |
| 7390805 | 4-amino-6-phenyl-pyrrolo[2,3-d]pyrimidine derivatives The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions ... | 06/24/2008 |
| 7378417 | Pyrazolo-pyrimidine derivatives The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5 and p are as defined in the description and to pharmaceutically acceptable salts thereof, t... | 05/27/2008 |
| 7371750 | 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... | 05/13/2008 |
| 7368449 | 2-alkynyl- and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine Areceptor antagonists Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is | 05/06/2008 |
| 7361659 | Pyrrazolo-pyrimidine derivatives The present invention relates to pyrrazolo-pyrimidine derivatives of formula (I): wherein R1 to R4 and A are as defined in the specification, a process for the manufacture thereof, their use for treati... | 04/22/2008 |
| 7348331 | Hydroxyalkyl substituted pyrido-7-pyrimidin-7-ones Compounds of the Formula: where X1, Ar1, R1, and R2 are as defined herein, and compositions comprising the same. Also provided are methods for using compounds of Formula I in trea... | 03/25/2008 |
| 7345046 | Heteroaryl-fused pyrimidinyl compounds as anticancer agents Heteroaryl-fused pyrimidinyl compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the heteroaryl-fused pyrimidinyl compounds, either alone or in combination with at lea... | 03/18/2008 |
| 7338955 | Medicament for treatment of neuropathies Compounds of formula (I) in which R1=C1-6 alkyl, optionally halosubstituted; R2=H, C1-4 alkyl, optionally halosubstituted or replaced by halogen; R3=C2-4 alkyl, optionally halosubstituted; R4 | 03/04/2008 |
| 7329655 | Nitrogenous heterocyclic compounds The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to ... | 02/12/2008 |