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7618963 Bicyclic heteroaromatic compounds  
A bicyclic heteroaromatic compound according to general formula I, or a pharmaceutically acceptable salt thereof, wherein R1 is (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl or...
7605154 Substituted Thiazolo [4,5-d]pyrimidines as protein kinase inhibitors  
The present invention is directed to novel thiazolopyrimidine compounds of Formula (I) or a form or composition thereof and the use thereof as inhibitors of ATP-protein kinase interactions.
7605155 Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors  
In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), methods of preparing such compounds,...
7601713 Kinase inhibitors and their uses  
The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein...
7598244 [1,2,4]triazolo[1,5,a]pyrimidin-2-ylurea derivative and use thereof  
Novel [1,2,4]triazolo[1,5-a]pyrimidine derivative of the general formula (1): (1) its prodrug or a pharmaceutically acceptable salt thereof, which exhibits an antigen presentation inhibiting...
7582627 3-aminoquinazolin-2,4-dione antibacterial agents  
Antibacterial 3-aminoquinazolin-2,4-diones have formula (I) wherein: R 1 and R 3 include alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclic, and heteroaryl; R 5 , R 6 , and R 8 include H,...
7579348 Derivatives of 8-substituted xanthines  
The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xantbines of formula I which are selective antagonists of A 2B adenosine receptors...
7575757 Stabilized formulations of alpha adrenergic receptor antagonists and the uses thereof  
The present invention provides compositions and stable liquid formulations comprising alpha adrenergic receptor antagonists and use thereof for increasing blood flow. In one embodiment, the stable...
7569574 Purine derivatives, the preparation thereof and their use as pharmaceutical compositions  
The invention relates to new purine derivatives of general formula wherein R 1 to R 4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and...
7560483 Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof  
The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require...
7560458 Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors  
This invention concerns compounds of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines and stereochemically isomeric forms thereof, their use, pharmaceutical...
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...
7544682 Pyrido-pyrimidine derivatives, preparation thereof, and therapeutic use thereof  
The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I) and acid addition salts, hydrates and solvates thereof,...
7528140 Substituted pyrrolo[3,2-d]pyrimidines as glycogen synthase kinase (GSK) inhibitors  
The invention provides pyrrolo[3,2-d]pyrimidine derivatives represented by formula (I), and their medically acceptable salts. The compounds of the invention exhibit GSK-3 inhibiting activity and...
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...
7514442 Trisubstituted 4-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors  
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds,...
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...
7504398 Substituted-4-(pyrrolo pyrimidin-6-yl)benzenesulphonamide derivatives  
This invention is directed to selective antagonists of A 2A and/or A 2B adenosine receptors having the general formula (I); to processes for their preparation; to pharmaceutical compositions...
7494993 Amide derivatives of 7-amino-3-phenyl-dihydropyrimido[4,5-d]pyrimidinones, their manufacture and use as pharmaceutical agents  
The present invention relates to novel amide derivatives of 7-amino-3-phenyl dihydropyrimido[4,5-d]pyrimidinones, to a process for their manufacture, medicaments containing them and their...
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]Py rimidine or a salt thereof for the manufacture of a medicament for the treatment of functional bowel disorder.
7470695 N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors  
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds,...
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...
7456168 2-(pyridin-2-ylamino)-pyrido[2,3, d]pyrimidin-7-ones  
The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent...
7452880 Substituted pyrazolo [3,4-d] pyrimidines and methods of using the same  
Compounds of the formula I: where A, B, X, Y, Z, k, R 1 , R 2 and R 3 are those defined herein, and compositions comprising the same. The present invention also provides methods for preparing...
7452886 Pyrrolo pyrimidines as agents for the inhibition of cystein proteases  
The invention provides compounds of Formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use...
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...
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...
7414058 Adenosine A2a receptor 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...
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,...
7378417 Pyrazolo-pyrimidine derivatives  
The invention relates to compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 and p are as defined in the description and to pharmaceutically acceptable salts thereof, to...
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...
7368449 2-alkynyl- and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists  
Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R 1 , R 2 , R 3 , R 4 and R 5 are H, alkyl or alkoxyalkyl; R 6 is...
7361659 Pyrrazolo-pyrimidine derivatives  
The present invention relates to pyrrazolo-pyrimidine derivatives of formula (I): wherein R 1 to R 4 and A are as defined in the specification, a process for the manufacture thereof, their...
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...
7338955 Medicament for treatment of neuropathies  
Compounds of formula (I) in which R 1 =C 1-6 alkyl, optionally halosubstituted; R 2 =H, C 1-4 alkyl, optionally halosubstituted or replaced by halogen; R 3 =C 2-4 alkyl, optionally...
7326699 4-Amino-5-phenyl-7-cyclobutyl-pyrrolo(2,3-d)pyrimidine derivatives  
The invention relates to new 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the...
7323469 7H-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,...
7317006 Thieno[2,3-d]pyrimidines with combined LH and FSH agonistic activity  
The invention relates to thieno[2,3-d]pyrimidine derivatives according to general formula I, or a pharmaceutically acceptable salt thereof, wherein N(R1)R2 are joined in a...
7294633 Oxazolo-and furopyrimidines and their use in medicaments against tumors  
The invention relates to pharmaceutically acceptable compounds of formula I, wherein the radicals have the significances given in the description. Compounds of formula I are useful against tumor...
7262192 Substituted pyrazolo[4,3-d]pyrimidines and their use as PDE-5 inhibitors  
The present invention comprises a class of 5,7-diaminopyrazolo[4,3-d]pyrimidine compounds. These compounds are useful as phosphodiesterase type 5 inhibitors. The present invention further comprises...
7258850 Methods and compositions for treating erectile dysfunction  
Methods are provided for increasing libido and/or treating erectile dysfunction in a man. The methods include the administration of a formulation testosterone alone, another fast-acting drug to...
7238664 Composition comprising a pulmonary surfactant and a PDE5 inhibitor for the treatment of lung diseases  
The invention relates to the combined administration of a pulmonary surfactant and a PDE5 inhibitor for the treatment of a disease in which pulmonary surfactant malfunction and/or phosphodiesterase...
7235551 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases  
Novel substituted pyrimidol[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
7229990 Bicyclic heteroaromatic compounds  
A bicyclic heteroaromatic compound according to general formula I, or a pharmaceutically acceptable salt thereof, wherein R 1 is (3–8C)cycloalkyl, (2–7C)heterocycloalkyl, (6–14C)aryl or...
7220748 Use of 4-(2-Flurophenyl)-6-methyl-2-(1-piperazinyl)thieno(2,3-D)-pyrimidine for treating of urinary incontinence  
4-(2-Fluorophenyl)-6-Methyl-2-(1-Piperazinyl)-Thieno(2,3-D)p yrimidine or a salt thereof is useful for the treatment of urinary incontinence.
7217720 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators  
Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while...
7196090 Kinase inhibitors  
This invention provides phenyl-substituted pyrimidopyrimidines, dihydropyrimido-pyrimidines, pyridopyrimidines, naphthyridines, and pyridopyrazines of the general formula: that inhibit...
7189726 Benzofuran derivatives as inhibitors of p38-α kinase  
The invention is directed to methods to inhibit p38-α kinase using compounds which contain an aromatic residue coupled to an benzofuran moiety through a piperidine.
7163941 Pyrido[2,3-d]pyrimidin-7-carboxylic acid derivatives, their manufacture and use as pharmaceutical agents  
The invention describes compounds of the general formula I a process for their manufacture, medicaments containing them and their manufacture as well as the use of these compounds as...
7157452 Substituted 4,9-dihydrocyclopenta{imn}phenanthridine-5-ones derivatives thereof and their uses  
This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.
Matches 1 - 50 out of 257 1 2 3 4 5 6 >