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7618983 |
Bicyclic triazole α4 integrin inhibitors
The compounds of the present invention are novel bicyclic triazole amino acid-derivatives useful as α4 integrin receptor antagonists. The invention is further directed to methods for treating...
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7618964 |
Benzamide derivatives, their manufacture and use as pharmaceutical agents
Objects of the present invention are the compounds of formula I
their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the...
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7618650 |
Combination of a hypnotic agent and substituted bis aryl and heteroaryl compound and therapeutic application thereof
The invention concerns the combination of a short-acting hypnotic agent and a compound of formula (I):
Wherein X, Y, Z, A, B, D, Ar, R 1 and R 2 are as defined herein. The combination of this...
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7615555 |
Piperidine derivatives as modulators of chemokine receptor CCR5
Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
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7612094 |
Tri-substituted heteroaryls and methods of making and using the same
Compounds of formula (I) possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic...
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7608717 |
Sulfonyldihydroimidazopyridinone compounds as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
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7601737 |
Isotopically substituted proton pump inhibitors
The invention relates to compounds of formula 1
and formula 10
and to compositions comprising these compounds and methods of treating gastrointestinal disorders by administering these...
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7601726 |
Substituted pyrazolo[3,4-d]pyrimidines as p38 MAP kinase inhibitors
Compounds of formula Ia or Ib:
wherein A, W, X, Y, R 1 , R 2 , R 3 and R 4 are as defined herein. Also disclosed are methods of making the compounds and methods of using the compounds for...
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7598266 |
Fused heterocyclic derivatives as PPAR modulators
The present invention is directed to compounds represented by the following structural formula, Formula I:
wherein:
(a) X is selected from the group consisting of a single bond, O, S,...
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7592354 |
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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7582652 |
Kinase inhibitors
The present invention provides kinase inhibitors of Formula I.
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7579470 |
Fused heterocyclic compounds
Certain fused pyrrole- and pyrazole-containing heterocyclic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.
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7579360 |
Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing...
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7579359 |
1-alkoxy 1H-imidazo ring systems and methods
Imidazo-containing compounds (e.g., imidazonaphthyridines, imidazopyridines, imidazoquinolines, and imidazote-trahydroquinolines) with an alkoxy substituent at the 1-position, pharmaceutical...
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7579355 |
Inhibitors of Akt activity
The present invention is directed to compounds which contain a substituted pyridine moeity which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to...
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7576072 |
Heterocyclic inhibitors of MEK and methods of use thereof
Disclosed are compounds of the Formula I
and pharmaceutically acceptable salts and prodrugs thereof, wherein R 1 , R 2 , R 7 , R 8 and R 9 , W, X, Y and Z are as defined in the specification....
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7572808 |
Triazolopyridine cannabinoid receptor 1 antagonists
The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional...
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7572807 |
Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing...
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7569688 |
Propane-1, 3-dione derivative
Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione...
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7563799 |
Substituted pyrazolo[3,4-D]pyrimidines as p38 map kinase inhibitors
Compounds of the formula Ia or Ib:
wherein X and Y are N or one of X and Y is N and the other is CR g , and A, D, E, G, W, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. Also disclosed...
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7560446 |
Use of angiotensin II receptor antagonists for treating acute myocardial infarction
The invention relates to the use of an angiotensin II receptor antagonist or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of acute MI and for the...
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7541367 |
3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders
The present invention is directed to novel 3-benzoimidazolyl-pyrazolopyridine compounds of formula (I):
and pharmaceutically acceptable forms thereof and their synthesis and use as inhibitors...
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7541354 |
Bicyclo-pyrazoles
Bicyclo-pyrazole compounds of formula (I), as herein defined, are useful for treating diseases linked to disregulated protein kinases.
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7531531 |
Method of treating diseases associated with altered kinase activity with bicyclo-pyrazoles
Bicyclo-pyrazole compounds of formula (I), as herein defined, are useful for treating diseases linked to disregulated protein kinases.
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7528149 |
Respiratory syncytial virus replication inhibitors
This invention concerns compounds of formula (I)
prodrugs, addition salts, or stereochemically isomeric forms thereof for use as, inter alia, respiratory syncytial virus replication inhibitors;...
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7528148 |
Pyrazolo[3,4-B]pyridine compounds, and their use as phosphodiesterase inhibitors
The invention relates to a compound of formula (I)
or a salt thereof: wherein: R 1 is C 1-4 alkyl, C 1-3 fluoroalkyl or —(CH 2 ) 2 OH; R 2 is a hydrogen atom (H), methyl or C 1 fluoroalkyl;...
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7524860 |
Antibacterial agents
The present invention is directed to a new class of triazolopyridine derivatives, to their use as antimicrobials, and to pharmaceuticals containing these compounds.
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7511058 |
Heterocyclic inhibitors of MEK and methods of use thereof
Disclosed are compounds of the Formula III
and pharmaceutically acceptable salts and prodrugs thereof, wherein R 1 , R 2 , R 7 , R 8 , R 9 R 10 , and W are as defined in the specification....
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7511057 |
Triazolopyridinylsulfanyl derivatives as p38 MAP kinase inhibitors
A compound of formula (I), or a pharmaceutically acceptable salt and/or solvate (including hydrate) thereof;
and the use of a compound of formula (I) in the treatment of a TNF-mediated disease,...
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7507746 |
Enantiomer of tenatoprazole and the use thereof in therapy
This invention relates to optically active substances of tenatoprazole, (+) and (−)-5-methoxy-2-{(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]
sulfinyl}-1H-imidazo[4,5-b]pyridine. The compound and...
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7504414 |
Substituted benzimidazoles and imidazo-[4,5]-pyridines
2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines are disclosed as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer.
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7495010 |
Muscarinic acetylcholine receptor antagonists
Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.
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7495009 |
Imidazopyridine derivatives as melancortin receptor agonists
Derivatives of imidazopyridine which have a good affinity for certain sub-types of melanocortin receptors, in particular MC4 receptors and are useful for treating pathological states and diseases...
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7491733 |
Bicyclic guanidine derivatives and therapeutic uses thereof
The invention relates to compounds of general formula (I), in which A, X, Y and R1 are defined in Claim 1 . These compounds may be used in the treatment of pathologies associated with insulin...
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7491692 |
Methods for making and delivering Rho-antagonist tissue adhesive formulations to the injured mammalian central and peripheral nervous systems and uses thereof
The present invention provides methods for making, delivering and using formulations that combine a therapeutically active agent(s) (such as for example a Rho antagonist(s)) and a flowable carrier...
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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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7470693 |
Oxalamide derivatives as kinase inhibitors
The invention is directed to compounds having the following Formula I:
and methods of using them for the treatment of proliferative diseases.
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7468377 |
Imidazopyridine-derivatives as inductible no-synthase inhibitors
The compounds of Formula (I)
in which R1, R2, R3, R4, R5 and A have the meanings as given in the description are novel effective iNOS inhibitors.
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7468376 |
Pyrazolopyridine derivates
New compounds of formula (I) and the salts, solvates and prodrugs thereof, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38...
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7465743 |
Pyrazolo[3,4-b]pyridine compounds, and their use as PDE4 inhibitors
The invention relates to a compound of formula (I) or a salt thereof:
wherein: R 1 is Et, n-Pr, i-Pr, C 2 fluoroalkyl, or —CH 2 CH 2 OH;
R 2 is H, Me, Et, n-Pr, i-Pr, C 1-2...
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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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7449585 |
Indazol-3-ones and analogues and derivatives thereof which modulate the function of the vanilloid-1 receptor (VR1)
Compounds of formula (I), which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1...
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7442709 |
N3-substituted imidazopyridine c-Kit inhibitors
Compounds represented by Formula (I):
or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
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7439246 |
Fused heterocyclic kinase inhibitors
In general, the instant invention comprises compounds of Formulas I and II
including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase...
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7435731 |
Substituted pyrazolo[3,4-d]pyrimadines and methods of using the same
Compounds of the formula Ia or Ib:
wherein A, B, X, Y, Z, W, k, R 1 , R 2 , R 3 , R 4 and R 5 are those defined herein, and compositions comprising the same. The present invention also...
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7417041 |
Imidazopyrimidines as transforming growth factor (TGF) inhibitors
Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described....
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7410966 |
Use of and some novel imidazopyridines
The use of compounds of formula (I) wherein R 1 , R 3 , R 10 , m and Ar are as defined in the Specification and pharmaceutically acceptable salts thereof in the manufacture of a medicament for the...
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7407968 |
Compounds
Compounds of formula (I) wherein R F1 , R F2 , Z, R 1 , R 2 , Ar, X and Y are as defined in the specification as well as salts and pharmaceutical compositions including the compounds were prepared....
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7402593 |
Monohydrated sodium salt of S-tenatoprazole and the use thereof in therapy
The present invention relates to S-tenatoprazole monohydrated sodium salt, represented by the following formula
and the use thereof in therapy for the treatment of digestive diseases.
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7381732 |
Pyrazolobenzamides and derivatives as factor Xa inhibitors
The present application describes pyrazolobenzamides and derivatives thereof of Formula I:
P 4 -P-M-M 4 I
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