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7629346 |
Pyrazinecarboxamide derivatives as CB1 antagonists
The present invention relates to compounds of the formula I:
wherein R 1 to R 8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are...
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7625905 |
Octahydro-pyrrolo[3,4-c]pyrrole CCR5 receptor antagonists
Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) wherein R 1 -R 3 and Ar are as defined herein are antagonists of chemokine CCR5...
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7625908 |
Quinazoline derivatives
A quinazoline derivative of the Formula (I): wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part...
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7618973 |
Isoxazolo-pyrazine derivatives
The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, and...
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7618972 |
Substituted triazole derivatives as oxytocin antagonists
The present invention relates to a class of substituted triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions...
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7608618 |
Urea or thiourea substituted 1,4-pyrazine compounds useful as anti-cancer agents and for inhibiting Chk1
Compounds of the formula
wherein: Y′ is O or S, W′ is
optionally substituted,
Z′ is selected from the group consisting of
wherein Q′ is OR 7 and R 7 is C 1-3 alkyleneC 3-8...
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7605164 |
Compositions and methods for treating heart failure
Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including...
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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,...
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7601714 |
Pyrimidine derivatives useful as inhibitors of PKC-theta
Disclosed are novel compounds of formula (I):
wherein X, Y, R 1 , R 2 and R 3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of...
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7601723 |
Pyridyl substituted xanthines
The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xanthines of formula I
which are selective antagonists of A 2B adenosine receptors...
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7598251 |
Aminopyrazine derivatives and compositions
The present invention relates to aminopyrazine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and...
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7598247 |
Immunomodulating heterocyclic compounds
Compounds of formula (I) are inhibitors of CD80 and useful in immunomodulation therapy:
wherein R 1 and R 3 independently represent H; F; Cl; Br; —NO 2 ; —CN; C 1 -C 6 alkyl optionally...
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7595322 |
Heterocyclic sulfonamides as modulators of cardiac sarcomeres
Certain substituted sulfonamide derivatives of Formula I selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart...
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7595321 |
Compounds having selective inhibiting effect at GSK3
The present invention relates to new compounds of formula (I) wherein Z is N; Y is CONR 5 , NR 5 CO, SO 2 NR 5 , NR 5 SO 2 , CH 2 NR 5 , NR 5 , NR 5 CONR 5 , CH 2 CO, CO, O or CH 2 O; X is CH or N;...
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7595323 |
N-phenyl-2-pyrimidine-amine derivatives and process for the preparation thereof
The present invention relates to an N-phenyl-2-pyrimidine-amine derivative showing a superior effect on lung cancer, gastric cancer, colon cancer, pancreatic cancer, hepatoma, prostatic cancer,...
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7592337 |
Di-aryl substituted tetrazole modulators of metabotropic glutamate receptor-5
Tetrazole compounds substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring,...
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7585853 |
Compounds having selective inhibiting effect at GSK3
The present invention relates to new compounds of formula (I) wherein: Z is N and X is CH or N; Y is CONR 5 ; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms...
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7579349 |
4-(pyrazol-3-ylamino) pyrimidine derivatives for use in the treatment of cancer
A compound of Formula (I); wherein the substituents are as defined in the text for use in modulating insulin-like growth factor 1 receptor activity in a warm blooded animal such as man.
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7576086 |
Aralkyl-alcohol peiperazine derivatives and their uses as antidepressant
Aryl alkanol piperazine derivatives of the formula
and pharmaceutical compositions comprising the same. Also disclosed are methods for treating depression using the pharmaceutical composition....
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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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7569590 |
Use of thianecarboxamides as dgat inhibitors
The present application describes methods of treating obesity using DGAT-1 inhibitors according to Formula I:
including all prodrugs, solvates, pharmaceutically acceptable salts and...
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7560462 |
Compounds useful for inhibiting CHK1
Substituted urea compounds useful in the treatment of diseases and C 1-3 alkyleneOR 3 conditions related to DNA damage or lesions in DNA replication are disclosed formula (I), wherein X 1 is...
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7560463 |
Diaryl ethers as opioid receptor antagonists
Compound 5-(2-Methoxy-4-{[2-(tetrahydro-pyran-4-yl)-ethylamino]-methy
l}-phenoxy)-pyrazine-2-carboxamide or a pharmaceutically acceptable salt thereof, useful for the treatment of irritable bowel...
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7534797 |
6,6-Bicyclic ring substituted heterobicyclic protein kinase inhibitors
Compounds of the formula
and pharmaceutically acceptable salts thereof, wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , R 1 , and Q 1 are defined herein, inhibit the IGF-1R enzyme and...
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7531535 |
Lactam-containing compounds and derivatives thereof as factor Xa inhibitors
The present application describes lactam-containing compounds and derivatives thereof of Formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7...
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7528139 |
Sulfonamides
Compounds of the formula (I), in which R 6 , R 7 , R 8 , R 9 and X have the meanings indicated in claim 1 , are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be...
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7524849 |
5-arylpyrimidines as anticancer agents
This invention relates to certain 5-arylpyrimidine compounds or a pharmaceutically acceptable salt thereof, and compositions containing said compounds or a pharmaceutically acceptable salt thereof,...
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7524850 |
Substituted pyrazine inhibitors of AKT
The compounds of Formula E are useful as anti-cancer agents:
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7521453 |
Pyrimidine derivatives as modulators of insulin-like growth factor-1 receptor (IGF-I)
The invention provides compounds of formula
in which R 1 , R 2 , R 3 and R 4 have the meanings defined in the specification; processes for the preparation; pharmaceutical compositions...
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7514428 |
Pesticidal 1-aryl-3-amidoxime-pyrazole derivatives
1-Arylpyrazole-3-substituted-amidoxime derivatives of formula (Ia) or (Ib):
or salts thereof, wherein the various symbols are as defined in the description, and pesticidal compositions thereof,...
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7514437 |
Substituted diketopiperazines as oxytocin antagonists
A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a mammal in need thereof of an effective amount of a compound of...
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7507737 |
Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine H4receptor
Benzoimidazol-2-yl pyrimidines and pyrazines, pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H 4 receptor activity, including...
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7504401 |
Anti-cancer agents and uses thereof
The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I:
and solvates,...
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7501423 |
Tubulin inhibitor and process for its preparation
The invention provides 6-chloro-5-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-2
-pyrazin-2-yl-N-[(1S)-2,2,2-trifluoro-1-methylethyl]pyrimidi
n-4-amine hemifumarate which is a tubulin inhibitor...
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7501415 |
Selective inhibitors of ERK protein kinase and uses thereof
Described herein are compounds that are useful as ERK2 inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a...
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7501424 |
N-phenyl-2-pyrimidine-amine derivatives and process for the preparation thereof
The present invention relates to a novel N-phenyl-2-pyrimidine-amine derivative represented by the above formula (1) and its salt showing a superior effect on cancer in warm-blooded animals, such...
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7485638 |
Pyrimidine compounds
Compounds of the formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described...
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7482349 |
Amino-5,5-diphenylimidazolone derivatives for the inhibition of β-secretase
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated β-amyloid...
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7465728 |
Derivatives of 4-(imidazol-5-yl)-2-(4-sulfoanilino)pyrimidine with CDK inhibitory activity
Compounds of the formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described...
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7459454 |
Aminopyrazine derivatives and compositions
The present invention relates to aminopyrazine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and...
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7459457 |
Polycyclic pyridines as potassium ion channel modulators
The present invention provides a genus of polycyclic pyridines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic...
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7452906 |
Pyridine derivatives as Raf kinase inhibitors
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac...
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7452884 |
Methods for inhibiting angiogenesis
Novel methods for inhibiting angiogenesis and treating diseases associated with angiogenesis are described. The methods may comprise administering to a patient an effective amount of a...
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7442702 |
Prostaglandin agonists
This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such...
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7442699 |
Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure:
wherein R 1 ...
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7442701 |
Amino-heterocycles as VR-1 antagonists for treating pain
The present invention provides a compound of formula (I): wherein V represents NR 5 , O, S, SO or S(O) 2 ; W and X each independently represent CH or N; Y represents N, CH or C—Ar 2 , with the...
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7442697 |
4-imidazolyl substituted pyrimidine derivatives with CDK inhibitory activity
Compounds of the formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described...
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7432271 |
Pyrazolyl inhibitors of 15-lipoxygenase
The present invention provides pyrazolyl inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such...
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7432270 |
N-aroyl cyclic amines
This invention relates to N-aroyl cyclic amine derivatives and their use as orexin antagonists
wherein:
Y represents a bond, oxygen, or a group (CH 2 ) n , wherein n represents 1, 2 or 3; m...
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7432254 |
Method for treating glaucoma IC
Provided is a method of treating or ameliorating or preventing glaucoma, decreasing intraocular pressure or improving or amemliorting ocular accommodation in an animal, including a human comprising...
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