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7625892 Pharmaceutical compositions for the treatment of diseases related to neurotrophines  
The present invention refers to pharmaceutical preparations including as active compounds 3-aza-bicyclo[3.2.1]octane derivatives of general formula (I) and/or their dimers of general formula (II)...
7585863 Therapeutic amides  
The invention provides compounds of the formula: wherein A, X, Y, and Z are as defined in the specification. The compounds are effective anti-tumor agents. The invention also provides...
7541355 Conversion process for 2,3-benzodiazepine enantiomers  
Methods for the racemization of an enantiomer of a 2,3-benzodiazepine molecule into the corresponding racemic mixture under either basic or acidic conditions are described. Furthermore, the...
7498433 Process and intermediates for the preparation of olanzapine  
The invention provides an improved process for preparing Olanzapine as well as intermediates therefor.
7459414 Herbicides  
Compounds of formula wherein the substituents have the meanings given in claim 1 , and agronomically tolerable salts, isomers and enantiomers of those compounds, are suitable for use as...
7427613 7-aryl-3,9-diazabicyclo(3.3.1)non-6-ene derivatives and their use as renin inhibitors in the treatment of hypertension, cardiovascular or renal diseases  
The invention relates to novel 3,9-diazabicyclo[3.3.1]nonene derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions....
7407950 N-(heteroaryl)-1H-indole-2-carboxamide derivatives and their use as vanilloid TRPV1 receptor ligands  
The invention concerns compounds of general formula (I), wherein n, X 1 , X 2 , X 3 , X 4 , Z 1 , Z 2 , Z 3 , Z 4 , Z 5 and W are as defined herein. Said compounds are ligands of the TRPV 1 ...
7265106 Method for isolating (R)-tofisopam  
(R)-tofisopam, substantially free of the (S)-enantiomer of tofisopam, is obtained by separating the enantiomers of tofisopam by chromatography employing a chiral separation medium comprising (i)...
7189711 2, 3-benzodiazepine derivatives and pharmaceutical compositions containing the same as the active ingredient  
The invention refers to novel 2,3-benzodiazepine derivatives of formula (I) and pharmaceutical compositions containing the same as the active ingredient. The novel compounds antipasmodic, muscle...
7183274 Piperidine-2,6-diones heterocyclically substituted in the 3-position  
Piperidine-2,6-diones heterocyclically substituted in the 3-position corresponding to formula I Also the production and use of such compounds in pharmaceutical formulations and related methods...
7176195 Fused azepine derivatives and their use as antidiuretic agents  
Compounds according to general formulae (1 and 2), wherein G 1 is an azepine derivative and G 2 is a group according to general formulae (9–11) are new. Compounds according to the invention are...
7153958 Farnesyl transferase inhibiting benzoheterocyclic derivatives  
This invention comprises the novel compounds of formula (I) wherein r, s, t, X, Z, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 have defined meanings, having farnesyl transferase inhibiting...
7141562 Substituted benzoxazinones and uses thereof  
Compound of the Formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein: X is CH or N, Y is C or S, Z is —SO 2 — or —(CR a R b ) r —, n is 1 or 2, R 2 is aryl or...
7129235 Amides useful for treating pain  
The present invention relates to compounds of formula (I-VII) or a pharmaceutically acceptable salt or prodrug thereof, in which A, L, R 6 , R 7 and R 8 are defined herein. The present...
7101869 2,4-diaminopyrimidine compounds useful as immunosuppressants  
Novel compounds according to the formula and pharmaceutically acceptable salts, solvates, or hydrates thereof; wherein each occurrence of A is independently selected from CH or N; X is...
7015214 Cyanamide, alkoxyamino, and urea derivatives of 1,3-benzodiazepine as HIV reverse transcriptase inhibitors  
The present invention relates to 1,3-benzodiazepin-2-ones and 1,3-benzoxazepin-2-ones of formula I: or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms...
6995154 Heterocyclic topoisomerase poisons  
The invention provides compounds of formula I: wherein R 1 to R 5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds,...
6930104 Heterocyclic derivatives  
The object of the present invention is to provide soluble β-amyloid precursor protein secretory stimulators, which are effective in treating neurodegenerative diseases as well as cerebrovascular...
6887867 5H-2,3-benzodiazepine antagonists of excitatory amino acid receptors  
Substituted benzodiazepine compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compounds are generally 7- or 8-mono substituted...
6858605 Substituted 2,3-benzodiazepine derivatives  
The invention relates to new 2,3-benzodiazepine derivatives of formula (I), isomers and acid addition salts thereof and to pharmaceutical compositions containing the same, as well as to...
6667302 Heterocyclic topoisomerase poisons  
The invention provides compounds of formula I: wherein R 1 to R 5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds,...
6566357 Spirocyclic-6,7-dihydro-5H-pyrazolo&lsqb 1,2-a&rsqb pyrazol-1-ones which control inflammatory cytokines  
The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms...
6407095 1,4-diazabicylo&lsqb 3,2,2&rsqb nonane derivatives, their preparation and their therapeutic application  
The invention relates to 1,4-diazabicyclo[3.2.2]nonane derivatives, to pharmaceutical compositions containing them, and to methods for the treatment or prevention of disorders associated with a...
6369221 Thiazolobenzoheterocycles, preparation and medicines containing same  
Disclosed are thiazolobenzoheterocycles of the general formula Including their isomers, racemates, enantioners and salts thereof, as well as processes for preparing these compounds and...
6274577 Benzodiazepines  
Benzodiazapine derivatives of formula (1) are described: ##STR1## wherein Ar 1 is an aromatic or heteroaromatic group; L 1 is a linker atom or group; Ar 2 is an optionally substituted...
6200970 2,3-benzodiazepine derivatives and their use as AMPA-receptor inhibitors  
A compound of formula I ##STR1## in which X means hydrogen or halogen, Y means --NR 3 -- or --N, R 1 and R 2 are the same or different and mean hydrogen, C 1 -C 6 alkyl, nitro,...
6177565 Process for synthesizing piperazic acid  
The invention relates to a process for synthesizing piperazic acid and similar, ring-containing acids. The invention also relates to a process for simultaneously N(2)-acylating piperazic acid or an...
6121258 1,5-heterocyclic metalloprotease inhibitors  
The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable...
6075018 1-[2-(substituted vinyl)]-3,4-dihydro-4-dihydro-5H-2,3-benzodiazepine derivatives  
The invention relates to new 1-[2-(substituted vinyl)]-3,4-dihydro-5H-2,3-benzodiazepine derivatives, a process for the preparation thereof and pharmaceutical compositions comprising them. The new...
5985869 Benzoheterocyclic compounds  
Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R 1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R 2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally...
5942506 1- 2-(substituted vinyl)!-5H-2,3-benzodiazepine derivatives  
This invention relates to new 1- 2-(substituted vinyl)!-5H-2,3-benzodiazepine derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the...
5854239 Diazabicyclic neuokinin antagonists  
The present invention relates to diazabicyclic compounds and, specifically, to compounds of the formula ##STR1## wherein A, G, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 are as defined in the...
5834463 Condensed heterocyclic compounds, their production and use  
Compounds represented by the formula: ##STR1## wherein ring A is benzene; Ar is aromatic group; R 1 , R 2 and R 3 each stands for H, acyl, hydrocarbon or heterocyclic, or R 2 and R 3 , taken...
5807851 2,3-Benzodiazepine Derivatives as non-competitive AMPA  
Derivatives of 2,3-benzodiazepine are substituted by one or two halogen atom(s) and have the general formula ##STR1## These derivatives are non-competitive AMPA antagonists and are used in...
5750690 Asymmetric hydrogenation process using ruthenium-diphosphine complexe  
A process for the asymmetric hydrogenation of a compound of the formula ##STR1## wherein each R, independently, is alkyl, arylmethyl, aryl, alkoxy, arylmethoxy or aryloxy or both R's, taken...
5698691 Condensed cyclic compounds and their use  
Disclosed is a squalene synthetase inhibitor which comprises the compound represented by the formula ##STR1## wherein R 1 is hydrogen or an optionally substituted hydrocarbon group; R 2 is...
5639745 Fused-bicyclic lactams as interleukin-1β converting enzyme inhibitors  
Disclosed are compounds, compositions and methods for inhibiting interleukin-1β protease activity. The compounds, bicyclic derivatives of aldehydes and α-substituted methyl ketones, have the...
5631372 Process for the manufacture of 1-substituted-4-fluoro-1,4-diazoniabicyclo[2.] octane salts  
A process for producing 1-substituted-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts having the formula ##STR1## wherein the Z substituent is OH, OR, OC(O)R, SO 3 , SO 2 R, NO 2 , NO, or PO(OR) 2...
5624922 Aryl-fused and hetaryl-fused-2,4-diazepine and 2,4-diazocine antiarrhythmic agents  
Aryl-fused- and hetaryl-fused-2,4-diazepines of formula XXXVI, benzodiazocines of formula XXX, benzodiazepines of formula II ##STR1## δ-aminoamides of formula III and aryldimethanamines of formula...
5534633 Aminoketone sensitizers for photopolymer compositions  
Aminoketone-substituted coumarin sensitizers having tethered tertiary amino groups are described which have extremely good photosensitivity. The sensitizers of the instant invention have the...
5510346 4-heteroaryl-1,3-benzodiazepines and 2-substituted-gamma-(heteroaryl)benzeneethanamines  
Novel 4,5-dihydro-4-heteroaryl-3H-1,3-benzodiazepines, intermediates, processes for the preparation thereof, and methods for treating depression, inhibiting convulsions and treating anxiety...
5489681 Method for the preparation of 4-phenyl-1,3-benzodiazepins  
A compound of the formula ##STR1## is prepared by reacting an N-acylated-o-toluidine of the formula ##STR2## with n-alkyllithium to form a dilithio intermediate of the formula ##STR3## which can...
5292760 4-heteroaryl-1,3-benzodiazepines and 2-substituted-α-(heteroaryl)benzeneethanamines  
Novel 4,5-dihydro-4-heteroaryl-3H-1,3-benzodiazepines, intermediates, processes for the preparation thereof, and methods for treating depression, inhibiting convulsions and treating anxiety...
5288863 Process for the preparation of high-purity 1-(3-chloro-phenyl)-4-methyl-7,8-dimethoxy-5H-2,3-benzodiazepine  
The invention relates to a process for the preparation of 1-(3-chlorophenyl)-4-methyl-7,8-dimethoxy-5 H-2,3-benzodiazepine of formula (I) ##STR1## in high purity and in a quality suitable for...
5212301 Substituted fluorobenzenes  
Introduction of a fluoro substituent into an aromatic ring adjacent an electron donating group is difficult producing mixed isomers and low yields of desired products. A process for the...
5204343 5H-benzodiazepin derivative  
The invention relates to the new 1-(3-chlorophenyl)-4-hydroxymethyl-7,8-dimethoxy-5H-2,3-benz odiazepine of formula (I) ##STR1## and pharmaceutically acceptable acid addition salts thereof,...
5036153 Preparation of 2,5-diazabicyclo[2.2.1]heptanes and intermediates  
(R,R)-2,5-Diazabicyclo[ 2.2.1]heptanes are prepared from a compound of the formula ##STR1## wherein X and R 2 are as defined herein, by heating with tosylchloride in pyridine, reacting the formed...
5008263 Diazepine antiallergy agents  
Platelet activating factor antagonists of formula (I), (II) or (III): ##STR1## where A is optionally substituted benzene, pyridine, naphthalene, quinoline, thiophene, benzothiophene, pyrazole or...
4977155 1,2,3-triazolo compounds  
Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R 2 is hydrogen, NO 2 , NH 2 , CN, halogen, or SO 2 NH 2 ; --X--Y--Z-- is selected from --NN--N 3 --,--NR 3 ...
4906630 Method of increasing cardiac contractility using pharmaceutical compositions comprising benzodiazinone- pyridazinone or hydroxy-pyrazolyl compounds  
A method for increasing cardiotonic contractility in humans or other animals using a class of benzodiazinone-pyridazinone and hydroxy-pyrazolyl compounds and pharmaceutical compositions including...
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