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8168625 |
Pharmaceutical composition based on agonist of benzodiazepine
The present invention describes the use of pharmaceutical compounds in pharmaceutical compositions for sublingual administration, including as active ingredient thereof, an agonist of the central...
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8168626 |
Benzodiazepine compositions for treating epidermal hyperplasia and related disorders
The present invention provides, for example, pharmaceutical compositions comprising a benzodiazepine compound and an agent selected from the group consisting of a topical steroid, a keratolytic...
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8163737 |
CGRP receptor antagonists
The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.
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8163738 |
Aminodiazepines as toll-like receptor modulators
Provided are compositions and methods useful for modulation signaling through the Toll-like receptor TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation...
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8158619 |
1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl compounds and their medical use
This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be...
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8148366 |
Substituted pyrazolo[3,4-E][diazepin-6-5(H)ones and analogues thereof, their preparation and their use as antibacterial medicaments
The invention relates to nitrogenous heterocyclic compounds of formula (I): in which: R1 represents hydrogen, —(CH2)m—NH2, —(CH2)m—NH(C1-C6)alk, —(CH2)m—N(C1-C6)alk2, —(CH2)m—NH—...
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8128905 |
Stabilized uncoated particles of reversed liquid crystalline phase materials
Uncoated particles of reversed cubic phase or reversed hexagonal phase material containing an active disposed within are provided. The uncoated particles have an ionic charge that is sufficient to...
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8119630 |
Benzodiazepine derivatives and pharmaceutical compositions containing them
Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV Formula (I) Wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —...
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8119631 |
Inhibitors of interleukin-1β converting enzyme
The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural ...
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8106042 |
1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives useful as modulator of nicotinic acetylcholine receptors
This invention relates to novel N-oxides of a 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivative and their use in the manufacture of pharmaceutical compositions. The compounds of the invention...
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8101598 |
1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their medical use
This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be...
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8097612 |
Compositions and methods relating to novel compounds and targets thereof
The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and...
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8044043 |
CGRP receptor antagonists
The disclosure generally relates to the novel compounds of formula I, including their salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and...
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8039460 |
CGRP receptor antagonists
Compounds of Formula (I): and Formula (II): (where variables R2, R4, A, B, D, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention...
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8026234 |
Polo-like kinase inhibitors
Compounds of the following formula are provided for use with kinases: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture...
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8022061 |
N-aryl pyrazole compounds, compositions, and methods for their use
Compounds having formula I: where A1, A2, L, V, W, R1, R2, R3, R4 and R5 are as described herein, compositions thereof, and their use for the treatment or prevention of type 2 diabetes and type 2...
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8012960 |
Heterocyclic aspartyl protease inhibitors
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification;...
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7998953 |
Use of inhibitors of the renin-angiotensin system
It has been found that inhibitors of the rennin-angiotensin system are useful for the treatment or prevention of conditions associated with hypoxia or impaired metabolic function or efficiency. In...
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7994160 |
Pyridazine compounds as glycogen synthase kinase 3 inhibitors
Disclosed are pyridazine compounds of the formula I which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and...
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7994161 |
Derivatives of 2-alkoxy-3,4,5-trihydroxy-alkyl amides, preparation and use thereof, and compositions containing the same
The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such...
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7985747 |
Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the...
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7977330 |
Salts and crystal modifications thereof
The invention relates to salts of 1-(2-Fluoro-phenyl)-3-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e
][1,4]diazepin-3-yl)-urea and crystalline forms thereof, their production and usage, and...
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7968536 |
Heterocyclic compounds useful as RAF kinase inhibitors
The present invention provides compounds useful as inhibitors of protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
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7964591 |
Pyridazine derivatives and their use as therapeutic agents
Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human include administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3,...
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7960375 |
8-chloro-2,3-benzodiazepine derivatives
The invention relates to new 8-chloro-2,3-benzodiazepine derivatives of the general formula (I), wherein R stands for a lower alkyl group or a group of the general formula —NH—R′, wherein R′ st...
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7951791 |
Amino-substituted tricyclic derivatives and methods of use
Compounds of formula (I) wherein A and B are amine-substituted sidechains, Y1 and Y2 form various tricyclic cores, Xa and Xb are C, CH, or N, as defined herein, and Rx is an optional substituent....
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7935695 |
1,4-diaza-bicyclo[3.2.2]nonyl heteroaryl derivatives useful as nicotinic acetylcholine receptor ligands
This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl heteroaryl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be...
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7932248 |
1H-indazoles, benzothiazoles, 1,2-benzoisoxazoles, 1,2-benzoisothiazoles, and chromones and preparation and uses thereof
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with...
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7910578 |
8,10-diaza-bicyclo[4.3.1]decane derivatives and their medical use
This invention relates to novel 8,10-diaza-bicyclo[4.3.1]decane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile...
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7868000 |
Aspartyl protease inhibitors
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein j, k, U, W, R, R1, R2, R3, R4, R6, R7 and R7a are as described...
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7855196 |
Composition comprising a benzodiazepine agonist and a benzodiazepine antagonist
A composition comprising a benzodiazepine agonist, a benzodiazepine antagonist, and a pharmaceutical acceptable carrier in an effective ratio so as to preserve the therapeutic effects of the...
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7851465 |
Compositions and methods relating to novel compounds and targets thereof
The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine compounds, and...
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7842686 |
CGRP receptor antagonists
The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.
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7838517 |
Compounds useful as protein kinase inhibitors
The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of...
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7834006 |
Fused polycyclic compounds
The following fused polycyclic compound, analogues thereof or pharmaceutically acceptable salts thereof have an effect of increasing the sugar-transporting capacity and an effect of lowering the...
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7807683 |
N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds,...
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7807667 |
1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their medical use
This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be...
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7807666 |
CGRP antagonists
The invention relates to a method for treating irritable bowel syndrome through the use of effective amounts of a compound acting as CGRP antagonist.
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7795248 |
Substituted 7,8-dihydro-1H-pyrimido[4,5-B][1,4]diazepin-4-amines are novel kinase inhibitors
Compounds having the Formula (I) 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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7790713 |
Inhibitors of interleukin-1β converting enzyme
The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural ...
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7790709 |
Heterocyclic compounds, methods of making them and their use in therapy
In part, the present invention is directed to antibacterial compounds of formula (I) wherein A is a bicyclic heteroaryl ring or a tricyclic ring and R2 is an heterocyclic residue; L is a bond, or L...
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7763606 |
Heterocyclic aspartyl protease inhibitors
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification;...
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7763605 |
[1,4]benzodiazepines as vasopressin V2 receptor antagonists
The invention is directed to novel [1,4]benzodiazepine compounds useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac...
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7763616 |
Piperazine-piperidines with CXCR3 antagonist activity
The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of...
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7759346 |
[[2-(amino-3,4-dioxo-1-cyclobuten-1-yl)amino]alkyl]-acid derivatives for the treatment of pain
This invention provides a method of treating pain in a mammal that includes administering to a mammal in need of such treatment a pain treating effective amount of a compound of the formula (I):...
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7759354 |
Bicyclic guanidine derivatives as asparyl protease inhibitors, compositions, and uses thereof
The present application provides compounds of the Formula: and stereoisomers, tautomers, or pharmaceutically acceptable salts and solvates thereof, wherein U, W, R, R1, R2, R3 and R4 in each...
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7759338 |
Soluble 1,4 benzodiazepine compounds and stable salts thereof
The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and...
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7745426 |
Compositions and methods for reducing the risk of epileptic occurrence and/or for treatment of seizure disorders
The present invention relates to compounds and compositions useful for reducing the risk of epileptic occurrences and/or for alleviating epileptic phenomena in patients. In accordance with the...
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7745431 |
Pharmaceutical composition of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine and uses thereof
Pharmaceutical compositions comprising 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy
-5H-2,3-benzodiazepine; or a pharmaceutically acceptable salt thereof. The compositions are used...
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7718651 |
Inhibitors of FtsZ and uses thereof
The invention relates to inhibitors of FtsZ polymerization and uses thereof.
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