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7625922 |
Imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof as therapeutic compounds
The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B-RAF) activity, inhibit...
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7622482 |
Chemical compounds
This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
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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.
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7598254 |
Substituted 1,3-thiazolo[5,4-d]pyrimidines as xanthine oxidase inhibitors
The invention relates to compounds of the following formula (I) or their salts:
in which R 1 is a group of phenyl, naphthyl, pyridyl or the like which may have a substituent such as an alkyl...
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7585867 |
Substituted thiazolo[4,5-d]pyrimidin-2(3H)-one
A compound of formula (I) and pharmaceutically acceptable salts or solvates thereof for use in therapy.
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7560552 |
Thiopyrimidine and isothiazolopyrimidine kinase inhibitors
Compounds having the formula
are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and...
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7557112 |
Aromatic-ring-fused pyrimidine derivative
There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a...
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7498333 |
Enantiomers of selected fused heterocyclics and uses thereof
This invention relates to novel compounds having the structural formula (I)
and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or...
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7476677 |
Substituted thieno- and thiazolo- [2,3-d]pyrimidines and [2,3-c]pyridines as inhibitors of Tie2
A compound of the formula(I); wherein the substituents are as defined in the text for use in the production of an anti-angiogenic effect in a warm blooded animal such as man. The compounds are...
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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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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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7427616 |
Condensed pyridines and pyrimidines with tie2 (TEK) activity
A compound of the Formula (I), wherein A together with the carbon atoms to which it is attached forms a fused 5-membered heteroaryl ring, wherein said heteroaryl ring contains 1 or 2 heteroatoms...
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7371766 |
Curcumin analogs with anti-tumor and anti-angiogenic properties
The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.
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7351826 |
Aryl acid pyrimidinyl methyl amides, pyridazinyl methyl amides and related compounds
The invention provides compounds of Formula (I) that bind to GABA A receptors. In the above formula, variables are defined herein. Such compounds may be used to modulate ligand binding to GABA A ...
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7321033 |
3-B-D-ribofuranosylthiazolo [4,5-d] pyrimidine nucleosides and uses thereof
The invention is directed to 3-β-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention...
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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...
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7262186 |
Substituted pyrazolo[3,4-d] pyrimidinones as a mitotic kinesin inhibitor
The present invention relates to azolopyriniidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for...
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7262187 |
Substituted oxazolo- and thizaolopyrimidinones as a mitotic kinesin inhibitor
The present invention relates to azolopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for...
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7253154 |
Substituted thiazolopyrimidines as xanthine oxidase inhibitors
The invention relates to compounds of the following formula (I) or their salts:
in which R 1 represents OR 4 or others, in which R 4 is an alkyl group having 1-8 carbon atoms which may have...
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7244727 |
Fused bicyclic nitrogen-containing heterocycles
Compounds, pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic and cell proliferative diseases or conditions are provided herein. In particular, the...
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7179915 |
Method for producing highly pure tris-ortho metalated organoiridium compounds
The present invention describes a process for preparing highly pure tris-ortho-metalled organoiridium compounds and pure organometallic compounds of this type, especially compounds of the d 8 ...
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7176215 |
Bicyclic oxopyridine and oxopyrimidine derivatives
Compounds of formulae (1a) and (1b) are described: in which the dashed line represents an optional bond; A is a —N═ atom or a —N(R b )—, —C(R b )═ or —C(R b )(R C )— group; R a , R...
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7141564 |
Nitrogen-containing bicyclic heterocycles for use as antibacterials
Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
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7115739 |
Triazole compounds useful as protein kinase inhibitors
This invention describes novel triazole compounds of formula IX:
wherein Z 1 is nitrogen or CR 9 and Z 2 is nitrogen or CH, provided that at least one of Z 1 and Z 2 is nitrogen; G is Ring...
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7105524 |
Pesticidal and parasiticidal di-and trifluorosubstituted alkene compounds
Di- and trifluorosubstituted alkene compounds of formula I
wherein
X is hydrogen or fluorine; Y is oxygen, NR 1 or S(O) m ;
R 1 is hydrogen or C 1 –C 6 -alkyl; m is 0, 1, or 2;
...
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7067657 |
Thiazolopyrimidine derivatives and use thereof as antagonists of the CX3 CR1 receptor
Provided herein is a compound having the formula (Ia):
wherein said compounds are useful for the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease and pain.
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7022850 |
Bicyclicpyrimidones and their use to treat diseases
The present invention is directed to dihydropyrimidones having formula I or II and methods of using them to induce mitotic arrest, thereby making them useful as anti-cancer agents and other...
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6969713 |
Piperidine and piperazine acetamide derivatives
The invention provides piperidine and piperazine derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the...
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6958343 |
Thiazolopyrimidines and their use as modulators of chemokine receptor activity
Compounds of formula (I):
are described herein. The compounds can be used, for example, in the treatment of chemokine mediated diseases, including inflammatory diseases such as psoriasis and...
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6949643 |
Thiazolopytimidines and their use as modulators of chemokine receptor activity
The invention provides certain thiazolopyrimidine compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof: in which: A is a group of formula (a) or (b): processes and...
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6930101 |
Thiazolopyrimidines useful as TNFα inhibitors
The invention provides derivatives of thiazolo[4,5-dl]pyrimidine and their use as inhibitors of proinflammatory cytokines.
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6841549 |
Condensed imidazole compounds and a therapeutic agent for diabetes mellitus
The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action. That is,...
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6835726 |
Pyrimidine derivatives
Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.
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6828326 |
Pyrimidinone fused bicyclic metalloproteinase inhibitors
The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R 1 are as defined in the specification, and to pharmaceutical compositions...
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6790850 |
Thiazolo(4,5-d)pyrimidine compounds
The invention provides certain thiazolopyrimidine compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof; processes and intermediates used in their preparation,...
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6777416 |
Isoxazolo pyrimidinones and the use thereof
The invention relates to novel isoxazolo pyrimidinones of general formula (I), a method for producing the same and the pharmaceutical use thereof.
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6734180 |
NF-&kgr B inhibitor comprising an indan derivative as an active ingredient
An inhibitor of NF-κB comprising as an active ingredient an indan derivative represented by the general formula (I) or a salt thereof.
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6617330 |
Pyrimidin-4-enamine as fungicide
Novel pyrimidine derivatives of formula I as well as possible isomers and mixtures of isomers thereof. The novel compounds have plant-protective properties and are suitable for protecting plants...
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6589958 |
Isoxazolo &lsqb 4,5-d&rsqb pyrimidines as CRF antagonists
The present invention describes novel isoxazolo[1,5-a]pyrimidines of formula: wherein R is an aromatic or heteroaromatic ring, or pharmaceutically acceptable salt form thereof, which are useful...
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6525056 |
Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone (CRH) antagonists, useful for treating cns and stress-related disorders
Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress...
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6410628 |
Photoactivatable nitrogen-containing bases based on alpha-amino ketones
The invention relates to organic compounds having a molecular weight of less than 1000 comprising at least one structural unit of the formula (I) in which R 1 is an aromatic or heteroaromatic...
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6376667 |
Solid phase synthesis of heterocycles
Methods and compounds for the synthesis of heterocycles, including pyrimidine-2,4-diones, are disclosed. Also disclosed are solid supports useful for solid phase synthesis, and methods for making...
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6228867 |
Antagonists of gonadotropin releasing hormone
There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety...
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6200957 |
Antagonists of gonadotropin releasing hormone
There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety...
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6165942 |
Heterocycle-fused pyrimidinone derivative and herbicidal composition
A compound represented by the general formula (I) and a salt thereof: ##STR1## wherein: Rf represents a (C 1 -C 4 )haloalkyl group; X.about.Y represents NN or CHN or the like; A represents a...
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6159975 |
Antagonists of gonadotropin releasing hormone
There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety...
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6143748 |
Process for synthesis of nucleoside analogues
The present invention is concerned with a process for the preparation of antiviral 1,3-oxathiolane nucleosides comprising an intramolecular glycosylation reaction to produce exclusively the...
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6133270 |
Isothiazolones and pharmaceutical formulations
Isothiazolones having the general structure ##STR1## where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R 1 and R 2 are substituent groups...
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6124306 |
Thioalkyl alpha substituted pyrimidine compounds
The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula I ##STR1## and pyrimidine-thioalkyl and alkylethers of Formula I, where R 4 is selected from the group...
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6124298 |
Pyrazinedicarboxylic-acid derivatives as cell proliferation regulators
The present invention relates to novel pyrazine compounds and their use in the regulation of haematopoiesis, in particular in the stimulation of haematopoiesis, and in the treatment of bacterial,...
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