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8163763 |
Pyrimidine compounds, compositions and methods of use
Disclosed are compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK...
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8133898 |
Renin inhibitors
The invention provides compounds, pharmaceutical compositions, kits, method of preparing, and method of using the compounds which exhibit renin and other S9 proteases activities and consist of the...
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8106081 |
Combination of organic compounds useful for treating diabetes
The present invention relates to a combination, especially a pharmaceutical composition, comprising as active ingredients (i) an AT1-receptor antagonist or a pharmaceutically acceptable salt...
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8097620 |
Diazaquinolones that inhibit prolyl hydroxylase activity
Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
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8071592 |
Derivatives and analogs of N-ethylquinolones and N-ethylazaquinolones
Bicyclic nitrogen containing compounds and their use as antibacterials.
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8058282 |
2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy
Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
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8039505 |
Compounds for modulating T-cells
Disclosed are compounds and compositions that modulate T-cells. Such compounds can be used to treat T-cell mediated disease like T-ALL, rheumatoid arthritis, multiple sclerosis, and graft-vs-host...
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8030317 |
MAPK/ERK kinase inhibitors
Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture...
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8022077 |
Pyrido[2,3-d]pyrimidines useful as HCV inhibitors, and methods for the preparation thereof
The present invention relates to the use of pyrido[2,3-d]pyrimidines of formula (I) wherein L, R1, R2 and R3 have specific meaning. The present invention also relates to the use of the compounds of...
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8003657 |
Heterocyclic substituted bisarylurea derivatives
The present invention relates to heterocyclic substituted bisarylurea derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds...
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8003656 |
2-phenoxy pyrimidinone analogues
2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo...
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7968557 |
Substituted pyrrolo[2,3-2]pyrimidines 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...
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7947690 |
Pyrimidine derivative condensed with a non-aromatic ring
The present invention provides a condensed pyrimidine compound represented by formula (I) or pharmaceutically acceptable salt thereof: where A represents a ring where at least one carbon atom...
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7939538 |
Compounds, compositions and methods for prevention and treatment of inflammatory and immunoregulatory disorders and diseases
Compounds are provided having the formula: wherein variables Ra, R1, R2, R3, R4, A1, A4, L, Q, X and subscript n as described herein. The subject compounds are useful for treatment of inflammatory...
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7928112 |
Substituted 5,6,7,8-tetrahydropyrido[4,3-D]pyrimidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment...
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7915264 |
Fused pyridine derivatives for use as vanilloid receptor antagonists for treating pain
The invention provides compounds of formula (I) wherein R1, R2, R3, R4, and R5 are as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as...
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7910595 |
Anti-viral compounds
Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-...
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7906520 |
Methods for treating pain
The present invention features methods and compositions for preventing, reducing, or treating a traumatic, metabolic or toxic peripheral nerve lesion or pain including, for example, neuropathic...
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7901708 |
Liposomal apparatus and manufacturing methods
The present invention provides apparatus and processes for producing liposomes. By providing a buffer solution in a first reservoir, and a lipid solution in a second reservoir, continuously...
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7884104 |
Aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
The present invention is directed to novel substituted aminopiperidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or pre...
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7879848 |
Dipeptidyl Peptidase-IV inhibiting compounds, method of preparing the same, and pharmaceutical compositions containing the same as an active agent
Novel compounds exhibiting good inhibitory activity versus Dipeptidyl Peptidase-IV(DPP-IV) include those of the following formula (1) or pharmaceutically acceptable salt thereof: wherein A is a...
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7875612 |
Folate mimetics and folate-receptor binding conjugates thereof
A cell population expressing folate receptors is selectively targeted with a non-peptide folic acid analogue. The non-peptide folic acid analogue is conjugated to a diagnostic or therapeutic agent...
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7868018 |
Compounds and compositions as protein kinase inhibitors
The invention provides compounds of Formula I: wherein R1-R6 are described in the Summary of the Invention; the pharmaceutical compositions comprising such compounds and methods of using such...
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7858631 |
Substituted pyrido [2,3-d] pyrimidinone compounds
A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have...
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7851468 |
Substituted pyrazolo[3,4-d]pyrimidines
The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that...
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7829572 |
Pyrido[4,3-d]pyrimidin-4(3H)-one derivatives as calcium receptor antagonists
The present invention is directed to novel pyrido[4,3-d]pyrimidin-4(3H)-one derivatives and pharmaceutically acceptable salts thereof of structural formula I wherein the variables R1, R2, R3, R4...
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7820682 |
LPA receptor antagonist
A compound of the general formula (I) or a non-toxic salt thereof. This compound engages in LPA receptor bonding and antagonism and is useful in the prevention and/or treatment of urinary system...
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7799775 |
Pyrimidine derivatives
This invention provides pyrimidine derivatives represented by a formula, in the formula, ring A stands for carbocyclic group or heterocyclic group,X1 stands for hydrogen, lower alkyl, amino,...
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7799795 |
Aryl nitrile compounds and compositions and their uses in treating inflammatory and related disorders
Provided herein are compounds of the formula where A1, A2, A3, A4, L, Q, R1, R2, R3, R4, Rx, Ry, Rz, X, Y1, Y2, Y4 and Z are as described herein, and compositions thereof that are useful in the...
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7790710 |
Imidazopyridine derivatives useful as iNOS inhibitors
The compounds of formula (I) in which R1, R11 and A have the meanings as given in the description are novel effective iNOS inhibitors.
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7767687 |
Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
The present invention provides compounds having the formula: wherein A-B together represent one of the following structures: n, R1, R2, R3, R4, L1, L2, Y and Z are as defined in classes and...
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7759353 |
Substituted spiro iminopyrimidinones as aspartyl protease inhibitors, compositions, and methods of treatment
Disclosed are certain substituted spiro iminopyrimidinones and other compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein U, W, A,...
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7759355 |
Adenosine A2A receptor antagonists for treating restless legs syndrome or nocturnal myoclonus
The present invention provides methods of treating restless legs syndrome or related disorders, comprising administering an effective amount of at least one adenosine A2A receptor antagonist to a...
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7678801 |
Compounds
Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use use in therapy as CSBP/RK/p38 kinase inhibitors.
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7662827 |
Pyrazole derivatives having tyrosine kinase inhibitory activity
Compounds of the formula (I), in which R, X, R1, R2, R3 and R4 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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7642255 |
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...
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7629350 |
Compounds
Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
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7608643 |
Compounds for inhibiting KSP kinesin activity
The present invention relates to compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: The present invention provides compositions comprising these compounds that are...
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7598255 |
Pyrimidine compounds as serotonin receptor modulators
Certain pyrimidine-containing compounds are serotonin receptor modulators useful in the treatment of serotonin-mediated diseases.
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7582627 |
3-aminoquinazolin-2,4-dione antibacterial agents
Antibacterial 3-aminoquinazolin-2,4-diones have formula (I) wherein: R1 and R3 include alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclic, and heteroaryl; R5, R6, and R8 include H, alkyl,...
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7572801 |
Pyridopyrimidinone derivatives which are HM74A agonists
The invention is concerned with novel pyridopyrimidinone derivatives of formula (I): wherein R1 to R8, X, Y, m and n are as defined in the description and in the claims. The compounds of the...
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7528139 |
Sulfonamides
Compounds of the formula (I), in which R6, R7, R8, R9 and X have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed,...
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7482336 |
Aminocyclohexanes as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or ...
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7442710 |
Substituted phenyl methanones
The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R″ andR1, R2,R3, R4,R5, and R6 are as defined in the specification and to pha...
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7429581 |
Pyrazole-derivatives as factor Xa inhibitors
The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active...
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7407963 |
Cyclopropane CGRP antagonists, medicaments containing these compounds, and method for the production thereof
A compound of general formula (I) wherein R and R1 are as defined herein, or a tautomer, diastereomer, enantiomer, or salt thereof, particularly the physiologically acceptable salts thereof, which...
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7378423 |
Pyrimidine compound and medical use thereof
The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] wherein each symbol is as defined in the specification...
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7332498 |
Modulation of KSP kinesin activity with heterocyclic-fused pyrimidinone derivatives
A method of modulating KSP kinesin activity in vitro comprising contacting KSP kinesin with at least one chemical entity chosen from compounds represented by Formula I: and pharmaceutically...
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7323472 |
2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds
The present invention is directed to the novel use of a CSBP/p38 inhibitor for the treatment, including prophylaxis of inflammation enhanced cough in a mammal in need thereof.
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7314873 |
(Halo-benzo carbonyl)heterobi cyclic p38 linase inhibiting agents
Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: (I) are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of...
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