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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 R 1 , R 2 , R 3 , R 4 , and R 5 are described herein. The invention also provides syntheses for preparation of such compounds and...
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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
R 1 is hydrogen, halogen, lower alkyl, lower...
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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...
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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
R 1 , R 2 , R 3 , R 4 and n are as defined in the...
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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...
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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
R 1 is hydrogen, halogen, lower alkyl, lower...
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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 R 1 is H, halogen, (C 1-4 )alkyl, O(C 1-4 )alkyl, and haloalkyl; R 2 is H or methyl; R 3 is H or (C 1-4 )alkyl; R 4 is H or (C 1-4 )alkyl; R 5 ...
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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 R 1 and R 2 are each, independently, H, alkyl, cycloalkyl, —CH 2 -cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO...
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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:
R 1 is hydrogen, —C(O)CH 3 or alkyl of 1-6 carbon atoms; R 2 and R 3 are each, independently, hydrogen, alkyl of 1-6...
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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: R 1 and R 2 are H, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO 2 -alkyl, —SO 2...
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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 R 1 , R 5 , R 6a , R 6b , R 7 , R...
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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; R 1 , R 2 , R 4 and R 5 are H, —OH, alkyl,...
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7132451 |
Inhibition of TNF-α-initiated neutrophil response
The impact of lipoxin A 4 (LXA 4 ) and aspirin-triggered-lipoxins (ATL) was investigated in tumor necrosis factor (TNFα)-initiated neutrophil (PMN) responses in vitro and in vivo using...
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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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7129237 |
[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 R 1 through R 7 are defined herein. The compounds of Formula I are 5HT2c agonists or partial agonists,...
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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 R 2 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 R 1 through R 7 are defined herein. The compounds of Formula I are 5HT2 c agonists or partial...
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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,...
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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 R 1 , R 2 , R 3 , R 4 and R 5 each represent a hydrogen or halogen atom or a nitro, amino, trifluoromethyl, trifluoroalkoxy, cyano,...
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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 R 1 , R...
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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 R 1 , R 2 , R 3 , R 4 , R 5 and n are as defined herein, are administered for the treatment of inflammatory disorders mediated by LTB 4 .
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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 R 1 and R 2 are each, independently, H, alkyl, cycloalkyl, —CH 2 -cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN,...
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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; R 1 , R 2 are H, alkyl, alkoxy, halogen, fluorinated alkyl, —CN, alkyl sulfonamide, alkyl...
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6777407 |
Cyclopenta&lsqb b&rsqb &lsqb 1,4&rsqb diazepino&lsqb 6,7,1-hi&rsqb indoles and derivatives
This invention provides compounds of the formulae: wherein: R 1 is hydrogen, —C(O)CH 3 or alkyl of 1-6 carbon atoms; R 2 and R 3 are each, independently, hydrogen, alkyl of 1-6 carbon...
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6759405 |
Cycloocta&lsqb b&rsqb &lsqb 1,4&rsqb diazepino&lsqb 6,7,1-hi&rsqb indoles and derivatives
This invention provides compounds of formula I having the structure wherein: R 1 and R 2 are H, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO 2 -alkyl, —SO 2...
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6743789 |
Substituted imidazo&lsqb 1,5-a&rsqb &lsqb 1,2,4&rsqb triazolo&lsqb 4,3-d&rsqb &lsqb 1,4&rsqb benzodiazepine derivatives
The present invention is a compound of formula The compound and derivatives or pharmaceutically acceptable salts thereof of the invention have a good affinity and selectivity to the GABA A α5...
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6699849 |
Cyclodextrin complexes of benzodiazepines
Methods for enhancing the complexation efficiency of a drug with cyclodextrin and for enhancing the availability of a drug following administration of a cyclodextrin-drug complex.
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6699492 |
Quinolone carboxylic acid compositions and related methods of treatment
The present invention relates to the use of quinolone carboxylic acid formulations in the treatment of ocular and periocular infections. The present invention also relates to sustained release...
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6610271 |
System and method for intranasal administration of lorazepam
A therapeutic composition of lorazepam and its pharmaceutically acceptable derivatives are provided for intranasal administration of at least one predetermined volumetric unit dose in the form of a...
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6541468 |
Indolocarbazole derivatives useful for the treatment of neurodegenerative diseases and cancer
Novel indolocarbazole derivatives potentially useful for the treatment of dementias characterized by tau hyperphosphorylation [Alzheimer's disease (AD), frontal lobe degeneration (FLD),...
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6521266 |
Composition for growth hormone production and release, appetite suppression, and methods related thereto
A method for enhancing growth hormone production and release, for appetite suppression, or both, in a subject in need thereof. The method comprises administering to the subject an effective amount...
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6503900 |
&lsqb 1,4&rsqb diazepino &lsqb 6,7,1-jk &rsqb carbazoles and derivatives
This invention provides [1,4]diazepino[6,7,1-jk]carbazole compounds of the formula: wherein: R 1 and R 2 are H, alkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO 2 -alkyl, —SO 2...
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6486178 |
Indane derivatives
The present invention provides medicines for treating cardiac insufficiency which contain as an active ingredient indane derivatives of formula (I) wherein R 1 represents hydrogen atom, nitro...
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6469058 |
Chemotherapy of cancer with actyldinaline in combination with gemcitabine capecitabine or cisplatin
Acetyldinaline in combination with gemcitabine, a pharmaceutically acceptable salt thereof, capecitabine, or cisplatin is synergistic for treating cancer.
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6458784 |
Vitronectin receptor antagonists
Pharmaceutically active benzodiazapine compounds of formula (I) are disclosed. These compounds inhibit the vitronectin receptor and are useful for treatment of osteoporosis.
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6455521 |
Condensed thiophene compounds and pharmaceutical use thereof
A condensed thiophene compound of the formula (I) wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof and hydrates thereof. The compound of the...
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6413930 |
Use of cck-b receptor antagonists for the treatment of sleep disorders
The use of CCK-B antagonists for the treatment of sleep disorders.
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6288094 |
Polycyclic thiazol-2-ylidene amines, processes for their preparation and their use as medicaments
The invention relates to polycyclic thiazolidin-2-ylidene amines and their physiologically tolerated salts and physiologically functional derivatives. Polycyclic thiazolidin-2-ylidene amines of the...
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6277846 |
Use of platelet activating factor antagonists as anti-pruritic agents
The invention relates to a method for treating pruritus by administering a therapeutically effective amount of a PAF antagonist to a mammal afflicted with pruritus. The PAF antagonists may, for...
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6271225 |
Fused thiophene compounds and medicinal use thereof
A condensed thiophene compound of the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof and hydrates thereof. The compound of...
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