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7598243 |
Heterocyclic cyclopentyl tetrahydroisoquinoline and tetrahydropyridopyridine modulators of chemokine receptor activity
The present invention is directed to compounds of the formula I:
Wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , X, n and the broken lines are as defined herein which are useful...
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7576209 |
Inhibitors of Akt activity
The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The...
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7563788 |
Substituted Imidazo[1,2-a]pyridines as Antibacterial Agents
Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable...
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7557101 |
4,5,6,7-tetrahydro-thieno[3,2-c] pyridine derivatives
The present invention relates to compounds of formula I
wherein R 1 and R 2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are...
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7547779 |
Preparation of 1,6-disubstituted azabenzimidazoles as kinase inhibitors
Novel inhibitors of Rho-kinases are disclosed.
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7544677 |
Inhibitors of Akt activity
The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further...
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7476671 |
2-amino-imidazo[4,5-d]pyridazin-4-ones, their preparation and their use as pharmaceutical compositions
The present invention relates to 2-amino-imidazo[4,5-d]pyridazin-4-ones and 2-amino-imidazo[4,5-c]pyridin-4-ones of general formula
wherein R 1 to R 4 and X are defined as in claims 1 to 6...
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7465726 |
Substituted pyrrolo[2.3-B]pyridines
Compounds represented by Formula (I):
or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least two of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3,...
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7459451 |
Pyrazolopyridine derivatives
The invention relates to compound of the formula (I) or its salt, in which R 1 , R 2 , R 3 and R 4 are as defined in the description, their use of as medicament, the process for their preparation...
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7429584 |
Furo[2.3-b]pyridine derivatives for the treatment of hyper-proliferative disorders
This invention relates to a compound of Formula (I) wherein Y is CH or N; Ar 1 is phenyl or pyridyl each optionally substituted with 1 or 2 substituents each selected independently from (C 1 -C 3...
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7358249 |
Heterocyclic compounds having inhibitory activity against HIV integrase
A heterocyclic compound of the formula (I):
wherein B 1 is —C(R 2 )═ or —N═; R 1 ′ is H, etc.; one of R 1 and R 2 is -Z 1 -Z 2 -Z 3 -R 5 wherein Z 1 and Z 3 are independently...
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7358244 |
Azabicycloalkane compounds
This invention provides compounds of formula I:
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or...
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7348339 |
Imidazopyridine derivatives as kinase inhibitors
A compound of the formula
and physiologically acceptable salts and or N-oxides thereof wherein,
X 1 is N or CR 3 ; X 2 is N or CR 4 ; X 3 is N or CR 5 ; X 4 is N or CR 6 . with the proviso...
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7326784 |
Intermediates for the preparation of tricyclic dihydropyrano-imidazo-pyridines derivatives
The invention relates to compounds of the formula 1,
in which R1, R2, R3, Arom and PG have the meanings as indicated in the description. These compounds are valuable intermediates for the...
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7323460 |
N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides useful as HIV integrase inhibitors
N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and inhibitors of HIV replication. The naphthyridine carboxamides are of Formula (I):
wherein R...
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7273865 |
Thiazolopyridine
The present invention relates to compounds of formula I
wherein R 1 and R 2 are described hereinbelow. These compounds have high affinity to A 2A receptors and good selectivity to A 1 and A...
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7268232 |
Androgen receptor modulators and method of treating disease using the same
Disclosed herein are bicycloaryl compounds of Formula (I) that selectively modulate nuclear receptors, preferably the androgen receptor, or a pharmaceutically acceptable salt, ester, amide, or...
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7256293 |
Imidazopyridine intermediates
The invention relates to compounds of the formula 1,
in which the substituents and symbols have the meanings indicated in the description. The compounds are valuable intermediates for the...
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7230009 |
Pyridoxal analogues and methods of treatment
Pyridoxal analogues can be useful for treating B 6 deficiency and related diseases; cardiovascular and related diseases; melanoma and related diseases; and symptoms thereof. One such analogue is a...
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7227020 |
Azaindoles
Chemical compositions containing physiologically active compounds of general formula (I):
wherein R 1 is aryl or heteroaryl; R 2 represents hydrogen, acyl, cyano, halo, lower alkenyl or lower...
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7220758 |
Ether substituted imidazopyridines
Imidazopyridine compounds that contain an ether or thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the...
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7199119 |
Antiinflammation agents
Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic, infectious and cell proliferative diseases or conditions are provided herein. In...
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7189727 |
Guanidino compounds
Compounds having the general structure III are provided:
where D is N or C; W is selected from
Z 1 , Z 2 , and Z 3 are independently selected from CR 8 and N; and the other variables have...
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7186716 |
3-Pyrrol-pyridopyrazoles and 3-pyrrolyl-indazoles as novel kinase inhibitors
Compounds of Formula I are useful as mediators of protein kinases and have activity as cell proliferation inhibitors:
where X, R 1 –R 7 and R 9 are as defined herein.
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7169787 |
7-azaindoles, use thereof as phosphodiesterase 4 inhibitors and method for producing the same
The invention relates to new 7-azaindoles, their use as inhibitors of phosphodiesterase 4 and to methods for their synthesis.
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7166596 |
Heterocyclic aromatic compounds useful as growth hormone secretagogues
Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I
...
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7163948 |
Heterocyclic substituted 1,4-dihydri-4ox9-1,8-naphthyridine analogs
The present invention relates to 1,4-dihydro-4-oxo-1,8-napthpyridine analogs of the formula
and pharmaceutically acceptable salts, esters, and prodrugs thereof, wherein A, X, W and Y are...
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7153960 |
Synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones
A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described.
These compounds are useful...
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7138410 |
Aza-bicyclic N-biarylamides with affinity for the α7 nicotinic acetylcholine receptor
The invention relates to novel 1-aza-bicyclic N-biarylamides, methods for production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases and for...
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7125890 |
Ether substituted imidazopyridines
Imidazopyridine compounds that contain an ether or thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the...
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7122545 |
Imidazo-benzothiazoles
The invention relates to 2-imidazo-benzothiazoles of general formula
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R′, R″, X, R′″ and n are defined herein, or a pharmaceutically...
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7109196 |
1,8 Naphthyridine derivatives and their use to treat diabetes and related disorders
The invention relates generally to naphthyridine derivatives of the formula
wherein one of U, X, Y and Z is nitrogen and the others are C—R, where R is hydrogen or a substituent. More...
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7087601 |
Metabotropic glutamate receptor-5 modulators
Phenyl compounds substituted at the 1-position with a fused bicyclo moeity formed from a five-membered heterocycle fused to a six-membered carbocycle, to a six-membered aryl, or to a six-membered...
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7078522 |
Pyridopyrimidine or naphthyridine derivative
A pyridopyrimidine or a naphthyridine derivative of the formula (I):
wherein R 1 is an optionally substituted nitrogen-containing heterocyclic group, etc.; R 2 is H or a lower alkyl group; R...
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7067515 |
Quinuclidines-substituted-multi-cyclic-heteroaryls for the treatment of disease
The invention provides compounds of Formula I:
where in W is
These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The...
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7064123 |
Compounds and compositions as cathepsin inhibitors
The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
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7045528 |
Benzofused heterozryl amide derivatives of thienopyridines useful as therapeutic agents, pharmaceutical compositions including the same, and methods for their use
The invention relates to compounds represented by the formula I
and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and...
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7041675 |
Heterocyclic compounds and their use as PARP inhibitors
The invention relates to compounds of the formula I
and the tautomeric forms, possible enantiomeric and diasteromeric forms thereof, and prodrugs thereof, and use thereof as PARP inhibitors.
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7041667 |
CCR5 modulators
Compounds of Formula 1
[R egion α]—[R egion β]—[R egion γ]—[R egion δ] (1)
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7038053 |
Process for imidazo[4,5-c]pyridin-4-amines
A process and intermediates for preparing 1H-imidazo[4,5-c]pyridin-4-amines are disclosed. The process includes providing a 7H-imidazo[4,5-c]tetrazolo[1,5-a]pyridine and converting a...
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6995171 |
Bicyclic pyrimidine and pyrimidine derivatives useful as anticancer agents
The invention relates to compounds of the formulas 1 and 2
and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein X, R 1 and R 11 ...
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6984648 |
Cyclic β-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-α
The present application describes novel cyclic β-amino acid derivatives of formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system...
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6977262 |
Dihydropyrazolopyridine compounds and pharmaceutical use thereof
The present invention provides dihydropyrazolopyridine compounds represented by the formula (I):
wherein each symbol is as defined in the specification, optically active forms thereof, and...
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6964961 |
Thiophene derivatives useful as anticancer agents
The invention relates to compounds of the formula 1
or a pharmaceutically acceptable salt and to pharmaceutically acceptable salts and hydrates thereof, wherein X, Y, R 1 , R 2 and R 11 are...
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6962926 |
Antagonist of MCP-1 function, and compositions and methods of use thereof
Compounds of formula A and formula B:
and their pharmaceutically acceptable salts, compositions comprising them, methods for their use, and their use in the preparation of medicaments. The...
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6960597 |
Aza-bridged-bicyclic amino acid derivatives as α4 integrin antagonists
The invention is directed to aza-bridged-bicyclic compounds having Formula (I):
and pharmaceutically acceptable salts thereof. The compounds are useful (α4 integrin receptor antagonists and,...
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6951867 |
N-substituted piperidinyl-imidazopyridine compounds as 5-HT4 receptor modulators
This invention provides a compound of the formula (I):
or a pharmaceutically acceptable salt, amide or ester thereof, wherein R 1 represents a hydrogen atom or a halogen atom; R 2 represents...
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6924283 |
4-thioxo-4,7-dihydro-thieno[2,3-b]pyridine-5-carbothioamides as antiviral agents
The invention provides a compound of formula I:
wherein R 1 , R 2 , R 3 , and R 4 have any of the values defined in the specification, or a pharmaceutically acceptable salt thereof, as well...
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6921759 |
Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV...
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6919451 |
Synthesis of 4,5-dihydro-pyrazolo [3,4-c] pyrid-2-ones
A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described.
These compounds are useful...
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