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Document Title |
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8168677 |
Method for treatment of inflammatory bowel disease
Method for therapeutic treatment of inflammatory bowel disease, including Crohn's disease, comprising administering to a patient in need thereof a therapeutically effective amount of a composition...
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8133885 |
Non steroidal glucocorticoid receptor modulators
The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to pharmaceutical compositions comprising...
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8101595 |
Antiviral indoles
Compounds of the formula (I) wherein A, B, D, M, Ar, W, X, Y, Z and R1 are as defined herein, are useful in the prevention and treatment of hepatitis C infections. The compounds, their preparation,...
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8063032 |
Histamine H3 inverse agonists and antagonists and methods of use thereof
Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of...
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8044042 |
Thienotriazolodiazepine compound and medicinal use thereof
A thienotriazolodiazepine compound of the following formula (I) a pharmaceutical agent containing the compound as an active ingredient, and a production intermediate and a production method of the...
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8034371 |
Intranasal compositions
The present invention provides compositions for the intranasal administration of zolpidem or a pharmaceutically acceptable salt thereof. Preferred compositions of the invention are in the form of...
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7989438 |
Therapeutic compounds
A class of macrocyclic compounds of formula (I), wherein R7, A, Ar, B, D, F, M, Q1, Q2, W, X, Y and Z are defined herein, that are useful as inhibitors of viral proteases, particularly the...
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7968540 |
Spirohydantoin tricyclic CGRP receptor antagonists
Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B1, B2, B3, B4, D1, D2, E1, E2, E3, E4, E5, G1, G2, R6, T, U, V, W, X, Y and Z are as described herein) which are antagonists...
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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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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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7888349 |
Piperazine, [1,4]Diazepane, [1,4]Diazocane, and [1,5]Diazocane fused imidazo ring compounds
Piperazine, [1,4]diazepane, [1,4]diazocane, and [1,5]diazocane fused imidazo ring compounds (i.e., imidazoquinolines, tetrahydroimidazoquinolines, imidazonaphthyridines,...
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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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7851464 |
Spirolactam aryl CGRP receptor antagonists
Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, E1, E2, E3, E4, E5, G1, G2, J and K are as described herein) which are antagonists of CGRP receptors and which are useful in...
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7781427 |
Process for preparing quinoline compounds and products obtained therefrom
Methods for synthesizing tetrahydroquinoline-containing compounds are provided, along with synthetic intermediates and products associated with such methods.
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7767660 |
Antiviral indoles
Compounds of the formula (I): wherein A, B, D, M, Ar, W, X, Y, Z and R1 are as defined herein, are useful in the prevention and treatment of hepatitis C infections. The compounds, their...
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7709470 |
11-phenyl-dibenzodiazepine derivatives as RXR-antagonists
The present invention relates to novel benzodiazepine compounds exhibiting RXR-antagonist efficacy, for delaying progression of, preventing or treating a condition or disease being associated with...
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7671048 |
Substituted imidazo [1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives
The present invention is concerned with a method of treating a disease selected from the group consisting of cognitive disorders, anxiety, Alzheimer's disease, and schizophrenia comprising...
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7659263 |
Thienopyrrole compound and use thereof as HCV polymerase inhibitor
The present invention relates to a thienopyrrole compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt...
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7611694 |
Aerosol formulation for inhalation comprising an anticholinergic
The present invention relates to a propellant-free, aqueous aerosol formulation for anticholinergics of formula 1 wherein X− denotes an anion.
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7524840 |
7,8-disubstituted pyrazolobenzodiazepines
The present invention provides compounds of formula I wherein R1, R2, R3, R4, and R5are described herein. The invention also provides syntheses for preparation of such compounds and pharmaceutical...
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7514426 |
Substituted imidazol[1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives
The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkynyl,...
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7507729 |
Substituted imidazo-[1,5-a][1,2,4]triazolo[1,5-d][1,4] benzodiazepine derivatives
The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the following formula wherein the definition of substituents is described...
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7507728 |
Halogen substituted imidazol[1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives
The invention relates to halogen substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of formula I wherein R1, R2, R3, R4 and n are as defined in the specification and to...
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7442694 |
Diazabicyclic compounds useful in the treatment of CNS and other disorders
The present invention relates to a compounds of formula I: wherein A, B, D, E and F are defined herein; that are useful in treating central nervous system (CNS) diseases, disorders and conditions,...
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7432256 |
Substitued imidazo [1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives
The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkyl...
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7384934 |
Piperazine substituted aryl benzodiazepines
Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk...
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7273861 |
Non-nucleoside reverse transcriptase inhibitors
Compounds represented by formula 1: wherein R1 is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, and haloalkyl; R2 is H or methyl; R3 is H or (C1-4)alkyl; R4 is H or (C1-4)alkyl; R5 is (C1-4)alkyl,...
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7271163 |
Cyclopenta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives
This invention provides compounds of the formulae: wherein: R1 is hydrogen, —C(O)CH3 or alkyl of 1-6 carbon atoms;R2 and R3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, c...
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7271162 |
Cycloocta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives
This invention provides compounds of formula I having the structure wherein: R1 and R2 are H, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl ami...
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7271164 |
Cyclohepta[b][1,4]diazepino[6,7,1,-hi]indoles and derivatives
This invention provides compounds of the formula: wherein R1 and R2 are each, independently, H, alkyl, cycloalkyl, —CH2-cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH...
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RE39680 |
Substituted heterocycle fused gamma-carbolines
The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k,...
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7141563 |
Process for the preparation of 1, 2, 3, 4, 8, 9, 10, 10a-octahydro-7bH-cyclopenta[b] [1, 4]diazepino[6, 7, 1-hi] indole derivatives
This invention provides processes for preparing compounds formula: wherein R is H, alkyl, acyl, aryl, aroyl or —C(O)R′; R′ is alkyl or aryl; R1, R2, R4 and R5 are H, —OH, alkyl, cycloalkyl, alkoxy,...
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7132418 |
Peptidyl heterocyclic ketones useful as tryptase inhibitors
The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment...
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7132451 |
Inhibition of TNF-α-initiated neutrophil response
The impact of lipoxin A4 (LXA4) and aspirin-triggered-lipoxins (ATL) was investigated in tumor necrosis factor (TNFα)-initiated neutrophil (PMN) responses in vitro and in vivo using metabolically ...
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7119087 |
4-(oxazolopyridin-2-yl)-1,4-diazabicyclo-[3.2.2]nonane derivatives, preparation and therapeutic use thereof
Compound corresponding to the general formula (I) in which R2 represents a chlorine atom, a methyl group or a 3-thienyl group. Therapeutic application.
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7105506 |
Tetracyclic compounds as PDE5-inhibitors
Compounds of structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.
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7071185 |
1,2,3,4,7,8-hexahydro-6H-[1,4]diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents
Compounds of Formula I or a pharmaceutically acceptable salt thereof are provided: where R1 through R7 are defined herein. The compounds of Formula I are 5HT2c agonists or partial agonists, and are...
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7026311 |
Dibenzodiazepine derivatives, their preparation and use
The invention relates to compounds of the formula I and their tautomeric forms, possible enantiomeric and diastereomeric forms and their prodrugs, and to their preparation and use, where A, B, R1...
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7022697 |
4-(Oxadiazol-3-yl)-1,4-diazabicyclo[3.2.2]-nonane derivatives, preparation and therapeutic use thereof
The invention relates to compounds of the Formula I, to pharmaceutical compositions comprising them, and to the method of use thereof in the treatment or prevention of disorders linked to a...
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7015213 |
Use of diazepines for preparing medicines for treating pathological conditions or diseases involving one of the growth hormone release inhibiting factor receptors
The invention concerns the use of pyrido-thieno-triazolo-diazepins for preparing a medicine for treating pathological conditions or diseases involving one of the growth hormone release inhibiting...
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7001902 |
4-(2 phenylthiazol-5-yl)-1, 4-diazabicyclo-[3.2.2]nonane derivatives, preparation and therapeutic use thereof
Compound corresponding to the general formula (I) in which R1, R2, R3, R4 and R5 each represent a hydrogen or halogen atom or a nitro, amino, trifluoromethyl, trifluoroalkoxy, cyano, hydroxyl,...
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6998399 |
4-(1,3,4-thiadiazol-2-yl)-1,4-diazabicyclo-[3.2.2]nonane derivatives, preparation and therapeutic use thereof
The invention relates to compounds of the Formula I, to pharmaceutical compositions comprising them, and to the method of use thereof in the treatment or prevention of disorders associated with a...
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6987106 |
1,4-diazabicyclo[3.2.2]nonane-4-carboxylates and carboxamide derivates, production and use thereof in therapeutics
Compounds of general formula in which X represents an oxygen atom or a group of formula NZ in which Z represents a hydrogen atom or an alkyl group, n represents a number 0, 1 or 2, and R1, R2, R3,...
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6979682 |
Platelet-activating factor antagonist inhibition of angiogenesis and tumor growth induced by basic fibroblast
A novel use of platelet-activating factor antagonists that bind to intracellular PAF binding sites such as BN-50730 (tetrahedra-4,7,8,10 methyl-1 (chloro-1 phenyl)-6 (methoxy-4 phenyl-carbamoyl)-9...
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6936604 |
Bridged bicyclic amino acid-derived [1,4]benzodiazepine vasopressin receptor antagonists
The invention is directed to bridged bicyclic amino acid-derived [1,4]benzodiazepine compounds, intermediates and pharmaceutical compositions thereof useful as vasopressin receptor antagonists and...
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6927238 |
Regulation of phospholipase D activity
Novel inhibitors of polyisoprenyl phosphate signaling regulates phopholipase D activity.
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6864251 |
Treatment of LTB4-mediated inflammatory disorders with optically-pure (R)-2,3-benzodiazepines
Compounds according to formula I: wherein R1, R2, R3, R4, R5 and n are as defined herein, are administered for the treatment of inflammatory disorders mediated by LTB4.
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6858604 |
Cyclohepta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives
This invention provides compounds of the formula: wherein R1 and R2 are each, independently, H, alkyl, cycloalkyl, —CH2-cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH...
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6784194 |
Therapeutic use of a thienylcyclohexylamine derivative
A method of inhibiting effects of exogenous neurotoxic or neurotoxinic products in warm-blooded animals comprising administering to warm-blooded animals before exposure to said products an...
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6784172 |
Processes for preparation of cyclopenta&lsqb b&rsqb &lsqb 1,4&rsqb diazepino&lsqb 6,7,1-hi&rsqb indoles and derivatives
This invention provides processes for synthesizing compounds of formula I: wherein R is H or alkyl; R1, R2 are H, alkyl, alkoxy, halogen, fluorinated alkyl, —CN, alkyl sulfonamide, alkyl amide, a...
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