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7618958 |
Stereospecific anxiolytic and anticonvulsant agents with reduced muscle-relaxant, sedative-hypnotic and ataxic effects
The present invention provides compositions and methods of using stereospecific benzodiazepine derivatives, their salts and prodrugs for the treatment of anxiolytic or convulsant disorders having...
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7612062 |
Pyrrolobenzodiazepines
Compounds of the formula: (I) or solvate thereof, wherein: R 2 is an optionally substituted C 5-20 aryl group; R 6 and R 9 are independently selected from H, R, OH, OR, SH, SR, NH 2 , NHR,...
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7608615 |
Pyrrolo[2,1-C][1,4]benzodiazepine hybrids and a process for the preparation thereof
The present invention provides quinazolinone linked pyrrolo[2,1-c][1,4]benzodiazepine hybrid of general formula 5,
wherein, R is alkyl or halo group selected from H, Cl, F or CH 3 and n=1 to 3...
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7569561 |
2,4-diaminopyrimidines useful for treating cell proliferation diseases
The present invention encompasses compounds of general formula (1)
wherein
R 1 to R 6 , X and Y are defined as in claim 1 , which are suitable for the treatment of diseases...
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7566707 |
Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula
wherein Y and R 1 to R 4 are defined as in claim 1 , the tautomers, enantiomers,...
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7560454 |
Condensed azepines as vasopressin agonists
This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V 1 and V 2 are both H, OMe or F, or one of V 1 and V 2 is Br,...
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7557099 |
Pyrrolobenzodiazepines as key intermediates in the synthesis of dimeric cytotoxic pyrrolobenzodiazepines
Compounds and a method of synthesis of compounds of formula (Ia) or (Ib): and salts, solvates, and chemically protected forms thereof, wherein the dotted lines indicate the optional presence of a...
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7547705 |
Substituted 8′-pyri(MI)dinyl-dihydrospiro-[cycloalkylamine]-pyrimido[1,2-a]pyrimidin-6-one derivatives
The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof:
wherein: X, Y, R1, R2, R3, R4, o, m, n, p and q are as defined...
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7531530 |
Therapeutic compounds
The invention relates to trycyclic lactam indole derivatives and triacyclic lactam benzimodole derivatives and their use in inhibiting the activity of PARP enzyme. The invention also relates to the...
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7528128 |
Pyrrolo[2,1-C][1,4]benzodiazepine hybrids and a process for the preparation thereof
The present invention provides a compound of general formula 5, useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the...
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7528126 |
Pyrrolobenzodiazepines
A compound of formula (I) and salts and solvates thereof, wherein: R 10 is a nitrogen protecting group and R 11 is either OH or O—R 12 , wherein R 12 is an oxygen protecting group, or R 10 ...
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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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7511037 |
N-[[4-fluoro-2-(5-methy-1H-1,2,4-triazol-1-yl)phenyl]methyl]-4-,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide as an HIV integrase inhibitor
The invention encompasses a series of bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful...
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7511032 |
Pyrrolobenzodiazepine derivatives, compositions comprising the same and methods related thereto
Disclosed are compounds of Formula (I) wherein X, Y, Ri-R 7 , T 1 , T 2 , Z, and p are as described herein; a pharmaceutical composition comprising a compound of Formula (I) and a carrier; a method...
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7507397 |
Delivery of muscle relaxants through an inhalation route
The present invention relates to the delivery of muscle relaxants through an inhalation route. Specifically, it relates to aerosols containing muscle relaxants that are used in inhalation therapy....
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7498334 |
Pyrrolopyrimidines as phosphodiesterase VII inhibitors
Pyrrolopyrimidine derivatives of the formula I
in which R 3 , R 4 , R 5 , R 6 and X are as defined in claim 1 , act as phosphodiesterase VII inhibitors and can be employed for the treatment...
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7494984 |
Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors
The invention encompasses a series of bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the...
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7491716 |
Purine derivatives as kinase inhibitors
The present invention provides kinase inhibitors of Formula I.
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7476664 |
Bis-2-difluoro-pyrrolo[2,1-C][1,4]benzodiazepine dimers
The present invention provides a novel bis 2-difluoro pyrrolo[2,1-c][1,4]benzodiazepine of formula VII
wherein, n is 3 to 10. novel bis 2-difluoro pyrrolo[2,1-c][1,4]benzodiazepine of formula...
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7465724 |
Bis-pyrrolo[2,1-c][1,4]benzodiazepine-anthraquinone conjugates and a process for the preparation thereof
The present invention provides novel bis-pyrrolo[2,1-c][1,4]benzodiazepine-anthraquinone conjugates of general formula V, useful as potential antitumour agents against human cancer cell lines. The...
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7465722 |
Biphenyl vasopressin agonists
A compound of the formulae (I) or (II):
wherein:
Y is a moiety selected from NR or —(CH 2 ) n ;
wherein R is hydrogen or (C 1 -C 6 ) lower alkyl,
and n is 1;
represents:
...
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7459449 |
Stable salts of olanzapine
Several salts of olanzapine, including olanzapine malonate, olanzapine glycolate, olanzapine maleate, and olanzapine benzoate, have been found to have favorable solid state characteristics.
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7456170 |
Triazolobenzodiazepines and their use as vasopressin antagonists
Compounds of formula (I),
or pharmaceutically acceptable derivatives thereof, wherein
R represents H, C 1-6 alkyl, SO 2 R 1 , SO 2 NR 1 R 2 , or COR 1 ; R 1 and R 2 independently...
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7456169 |
Heterocyclic kinase inhibitors
Compounds having the formula
are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using...
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7429580 |
Compositions of an anticonvulsant and an antipsychotic drug and methods of using the same for affecting weight loss
Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is a psychotherapeutic agent and the second compound is a...
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7429578 |
Tricyclic inhibitors of poly(ADP-ribose) polymerases
Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma,...
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7407949 |
Benzamide derivatives as oxytocin agonists and vasopressin antagonists
Novel compounds according to general formula 1, wherein G 1 is NR 5 R 6 or a fused polycyclic group that are specific OT receptor agonists and/or V 1a receptor antagonists. Pharmaceutical...
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7384935 |
Phosphate prodrugs of a farnesyl dibenzodiazepinone, processes for their production and their use as pharmaceuticals
This invention relates to phosphate prodrugs of a farnesylated dibenzodiazepinone, to processes of their manufacture, to pharmaceutical compositions comprising the prodrugs, and to their use in the...
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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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7358242 |
Tetraazabenzo[e]azulene derivatives and analogs thereof
This invention relates to CCK-A agonists of Formula (I)
wherein R 1 -R 4 , A, B, X, D, E and G are as defined in the specification, as well as, among other things, pharmaceutical compositions...
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7358241 |
Compositions and methods comprising farnesyl dibenzodiazepinones for treating neoplastic cells and conditions
This invention relates to methods of inhibiting growth and/or proliferation of a neoplastic cell, and methods of treating neoplasms using the farnesylated dibenzodiazepinone compound of Formula I....
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7348321 |
Flumazenil for the treatment of alcohol dependency
The invention relates to the use of flumazenil in developing a drug used for the sequential administration of small quantities of flumazenil at short intervals, until a therapeutically effective...
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7329653 |
Cyclohexylphenyl vasopressin agonists
The present invention provides compounds of the general formulas:
wherein Y is NR or —(CH 2 ) n ; R is H or alkyl; “Z” represents optionally substituted phenyl or a 6-membered aromatic...
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7326701 |
Lactam compounds and pharmaceutical use thereof
An agent for increasing the sugar-transporting capacity and an agent for preventing and/or treating diabetes, diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic...
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7326700 |
Cyclohexenyl phenyl carboxamides tocolytic oxytocin receptor antagonists
The present invention provides tricyclic carboxamide compounds and methods and pharmaceutical compositions for their use in treatment, prevention, or suppression of disorders which may be remedied...
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7323459 |
Crystal forms, methods for their preparation and method for preparation of olanzapine
The invention is directed to a series of novel crystalline olanzapine forms, in particular hydrated and solvated crystalline forms of olanzapine, methods of use in pharmaceutical compositions, and...
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7323458 |
Dihydrobenzodiazepins and their use for treating dyslipidemia
The invention concerns a benzodiazepin derivative of formula (I) and their use for treating dyslipidemia, atherosclerosis, diabetes and its complications.
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RE40033 |
Process for preparing 2-methyl-thieno-benzodiazepine
2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-[2,3-b][1,5]b
enzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the...
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7317005 |
Tricyclic benzodiazepines as vasopressin receptor antagonists
The invention is directed to tricyclic benzodiazepines useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac insufficiency....
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7312210 |
Pyrrolo[2,1-c][1,4]benzodiazepine compounds and processes for the preparation thereof
The present invention provides novel pyrrolo [2,1-c][1,4]benzodiazepine compounds. This invention also provides a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine compounds....
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7309700 |
Crystalline forms of 5,11-dihydro-11-ethyl-5-methyl-8-{2-{(1-oxido-4-quinolinyl)oxy}ethyl}-6H-dipyrido[3,2-b:2′,3′-e] [1,4]diazepin-6-one
Dihydrate and anhydrous crystalline forms of 5,11-dihydro-11-ethyl-5-methyl-8-{2-{(1-oxido-4-quinolinyl)o
xy}ethyl}-6H-dipyrido[3,2-b:2′,3′-e] [1,4]diazepin-6-one.
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7304054 |
Dibenzodiazepinone analogues, processes for their production and their use as pharmaceuticals
The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, to pharmaceutical compositions comprising them and to methods of...
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7303764 |
2-methyl-thieno-benzodiazepine formulation
The invention provides a pharmaceutically acceptable oleaginous or cholesterol microsphere formulation of olanzapine or olanzapine pamoate or solvates thereof. The invention further provides novel...
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7276571 |
Process for making phenylene dioxydiacetic acid and use thereof
A process for making phenylene dioxydiacetic acid comprises (a) contacting a dihydroxybenzene under reaction conditions with a salt of haloacetic acid in a solution without adding a haloacetic acid...
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7265105 |
Pyrrolobenzodiazepines
A compound of the formula II:
wherein:
R′ 2 is CHR″ 2 , where R″ 2 is H. R 6 and R 9 are H and R 7 is OMe and the compound is a dimer with each monomer being the same and...
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RE39743 |
2-halogenated derivatives of 5-0 desosaminyl-erythronolide a, their preparation process and their antibiotic use
Novel compounds of the formula
wherein the substituents are defined as in the application having antibiotic properties.
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7244724 |
Pyrrolobenzodiazepines
A compound of formula I:
or solvate thereof, wherein n is 1 to 10, and M and M′ are independently selected from monovalent pharmaceutically acceptable cations, or together represent a...
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7238702 |
Dihydroquinazolinones as 5HT modulators
The present invention relates to modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating obesity using such compounds and compositions.
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7238685 |
Benzo-fused heterocycles as endothelin antagonists
The invention relates to novel benzo-fused heterocycles and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including...
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7229984 |
Dibenzoxazepinone derivatives and uses thereof
Compounds of the Formula I:
wherein m, n, k, A, X, Y, Z, Ar, R 1 , R 2 , R 3 , and R 4 are as defined herein. The compounds are useful as 5-HT6 receptor antagonists. Also provided are...
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