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5932587 |
Heterocyclic-fused pyridines
The heterocyclic-fused pyridines are prepared by reaction of the corresponding heterocyclic-fused pyridine aldehydes with appropriately substituted Grignard or Wittig reagents. The...
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5929081 |
Method for treating diseases mediated by cellular proliferation in response to PDGF, EGF, FGF and VEGF
There is disclosed a method for: (1) inhibiting new blood vessel formation that is useful for treating or preventing progression of diabetic retinopathy, cavernous haemangiomas, Kaposi's...
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5929114 |
Arylthio compounds
Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O,...
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5908842 |
Substituted 2-acylamino-pyridines as inhibitors of nitric oxide synthase
Substituted 2-acylaminopyridine compounds and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders.
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5908835 |
Anti-tumor compositions containing taxane derivatives
Disclosed are antitumor compositions comprising taxol, taxotere or their derivatives in combination with an anthracycline antibiotic, the combination having a pharmacologic activity greater than...
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5905084 |
5-HT.sub.IF -agonists effective in treating migraine
This invention provides 5-HT 1F agonists of Formula: ##STR1## where A-B, X, and R are as defined in the specification. The invention also encompasses pharmaceutical formulations employing the...
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5900414 |
Methods for administering integrin receptor antagonists
The compositions and methods of the invention provide a convenient means for systemically administering an integrin receptor antagonist or a pharmaceutically effective amount thereof to a patient...
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5900413 |
Treatment of H. pylori infections
An infection with Helicobacter may successfully be treated with a compound of the formula ##STR1## wherein R 1 is hydrogen or methyl and R 2 is hydrogen or L-alanine-L-alanyl, and the...
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5891891 |
Use of imidazo 1, 2-A! pyridine-3-acetamide derivatives for the therapeutic treatment of neuropsychiatric syndromes associated with disfunction of the neural circuits of the basal ganglia
Treatment of Parkinson's disease, parkinsonian syndromes, extrapyramidal syndromes, obsessive-compulsive disorder and syndromes, and frontal and subcortical dementias, with imidazo...
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5889009 |
Method of inhibiting cell adhesion
A composition comprises a 1,7-disubstituted-4-oxo-3 -quinolinecarboxylic acid or 1,7-disubstituted-4-oxo-3 -naphthyridinecarboxylic acid derivative which is useful as a prophylactic and/or...
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5877182 |
Piperidines promote release of growth hormone
The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R 1 , R 1a , R...
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5874451 |
Propanolamine derivatives, processes for their preparation, pharmaceuticals comprising these compounds, and their use
The invention relates to substituted propanolamine derivatives and their acid addition salts. Propanolamine derivatives of formula I, ##STR1## in which R 1 to R 8 have the meanings indicated in...
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5874427 |
Substituted heteroaromatic 5-HT.sub.1F agonists
This invention provides novel 5-HT 1F agonists of the Formula ##STR1## in which X, Y, E, R, A, B, and n are as defined in the specification, which are useful for the treatment of migraine and...
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5869497 |
Method of treating or ameliorating the symptoms of common cold or allergic rhinitis
This invention provides methods for the treatment or amelioration of the symptoms of the common cold or allergic rhinitis which comprises administering to a mammal in need thereof a 5-HT 2 ...
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5866586 |
CNS-active pyridinylurea derivatives
The invention relates to heterocyclic compounds of formula (I) having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of...
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5854263 |
1- (1,4-benzodioxanyl)alkyl!-3-(heteroaryl) pyrrolidines and related compounds and their therapeutic utility
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a...
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5854257 |
Naphthyridinone derivatives
Compounds of formula I ##STR1## including pharmaceutically acceptable salts thereof in which R 1 represents a phenyl C 1 -6 alkyl group (in which the phenyl ring is optionally substituted by one...
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5854275 |
Cyclic imide derivatives
The invention relates to a compound of the formula I ##STR1## wherein R 1 is a cyclic imide group and X, Y, R 2 , and R 3 are as defined herein. The invention further relates to pharmaceutical...
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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...
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5849752 |
Crystal modification of CDCH a process for its preparation and pharmaceutical formulations comprising this modification
The invention relates to the new monohydrate of 1-cyclopropyl-7-( S,S!-2,8-diazabicyclo- 4.3.0!non-8-yl)6-fluoro-1,4-dihyd ro-8-methoxy-4-oxo-3-quinolinecarboxylic acid hydrochloride (CDCH), a...
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5840732 |
Imidazopyridine or imidazopyrimidine compounds, their production and use
This invention provides a new condensed imidazole compound possessing inhibitory activity of adhesion molecule expression. This invention also provides a therapeutic and prophylactic agent for...
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5837710 |
HIV protease inhibitors
HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These...
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5830901 |
Tetrahydropyridinylmethyl derivatives of pyrrolo 2,3-B!pyridine
Disclosed is a class of pyrrolo 2,3-b!pyridine derivatives of formula (I) wherein Q represents a moiety of formula Qa or Qb, which are ligands for dopamine receptor subtypes within the body, in...
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5824687 |
Pyridinium salts and their use for the control of helicobacter bacteria
8-phenalkoxyimidazo 1,2-a!pyridinium salts are useful for controlling Helicobacter bacteria. Medicament compositions based on such compounds are prepared and used for the noted purpose.
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5821241 |
Fibrinogen receptor antagonists
Compounds of the invention have the formula ##STR1## The compounds have fibrinogen receptor antagonist activity.
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5817671 |
5-HT.sub.1F agonists
This invention provides 5-HT 1F agonists of Formula I: ##STR1## where A--B, X, and R are as defined in the specification. The invention also encompasses pharmaceutical formulations employing...
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5817669 |
Compounds, processes for the preparation thereof and anti-tumor agents
This invention relates to pyridone-carboxylic acid derivatives of the following formula or salts thereof: ##STR1## wherein R 1 is a hydrogen atom, a halogen atom, etc., R 2 is a carboxyl group...
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5817670 |
Naphthyridine derivatives and pharmaceutical compositions thereof
1,8-Naphthyridine derivatives represented by the following general formula (I), salts thereof, hydrates thereof and solvates thereof. ##STR1## They have an activity to inhibit type IV...
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5811433 |
1,6-naphthyridonecarboxylic acid derivatives
The invention relates to novel 1,6-naphthyridonecarboxylic acid derivatives, to processes for their preparation, to antibacterial compositions and feed additives in which they are present, and to...
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5811432 |
Azaoxindole derivatives
This invention relates to novel 4-, 5-, 6-, and 7-azaoxindole derivatives. The compounds are anti-inflammatory and analgesic agents and inhibitors of one or more of prostaglandin H 2 synthase,...
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5811427 |
Heterocyclic N-acetonylbenzamides
Certain N-acetonylbenzamides and their use as fungicides are disclosed. The N-acetonylbenzamides disclosed contain a heterocyclic ring fused to an aromatic ring. These compounds are particularly...
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5801183 |
Aza and aza (N-oxy) analogs of glycine/NMDA receptor antagonists
Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease,...
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5786363 |
Aqueous compositions containing ciprofloxacine, and related use
Aqueous compositions containing ciprofloxacine and corresponding use and process, said composition comprising from 0.12-0.6 g/ml of chlorohydrate monohydrate of ciprofloxacine (equivalent to...
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5783585 |
Solid bulk compositions containing quinolone carboxylic acids or naphthyridine carboxylic acids in free base form
The present invention provides a method of making quinolone carboxylic acids or naphthyridine carboxylic acids in free base form, the method comprising dissolving a quinolone carboxylic acid salt...
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5780482 |
Condensed 4-aminopyridines with antirheumatic activity
Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which one of A or B represents N and the other represents N or C--R 3 ; R 1 represents hydrogen, halo, alkyl,...
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5776944 |
7-(4-aminomethyl-3-methyloxyiminopyrroplidin-1-yl)-1-cyclopropyl-6-flu oro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid and the process for the preparation thereof
The present invention relates to a novel quinolone compound having an excellent antibacterial activity. More specifically, the present invention relates to...
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5776963 |
3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a...
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5770597 |
Quinolone derivatives and processes for preparing the same
The present invention relates to quinoline derivatives substituted in the 7-position by a trans-2,8-diazabicyclo 4.3.0!nonan-8-yl group having a broad antibacterial spectrum and to processes for...
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5767128 |
1,3-dihydro-2H-pyrrolo 2,3-b!pyridin-2-one compounds
The invention relates to a compound selected from those of formula (I): ##STR1## wherein R 1 , W and Y are as defined in the description, its geometric and/or optical isomers, and its...
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5763461 |
Therapeutic phenoxyalkylheterocycles
Compounds of the formula ##STR1## wherein Pyr is chosen from the group consisting of pyridyl, pyrazyl, pyrimidyl, quinolyl, indolyl and 7-azaindolyl or any of these substituted with one or two...
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5763454 |
Crystal form of anhydrous 7-( 1α,5α,6α!-6-amino-3-azabicyclo 3.1.0!hex-3-yl)-6-f luoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8 naphthyridine-3-carboxylic acid, methanessulfonic acid salt
The anhydrate of 7-( 1α,5α,6α!-6-amino-3-azabicyclo 3.1.0!hex-3-yl)-6-flu oro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridi
ne-3-carboxylic acid, methanesulfonic acid salt has...
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5760034 |
Heterocyclic substituted naphthyridinones and methods and compositions employing them
Nitrogen-containing heterocyclic substituted naphthyridinones and methods and compositions employing such compounds are disclosed.
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5753669 |
Quinolone--and naphthyridonecarboxylic acid derivatives
The invention relates to new quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by a tricyclic amine radical, their salts, processes for their...
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5753667 |
1-oxo-2- (phenylsulphonylamino) pentylpiperidine derivatives, their preparation and their therapeutic application
The present invention provides a compound of formula (I) ##STR1## in which R 1 represents a hydrogen atom or a (C 1 -C 4 )alkyl group, R 2 represents a hydrogen atom or a straight or branched (C...
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5750536 |
Tropyl 7-azaindol-3-ylcarboxyamides as antitussive agent
Tropyl 7-azaindol-3-ylcarboxamides of the formula ##STR1## or their N-oxides of the formula ##STR2## wherein R is hydrogen, alkyl, cyclo-alkyl, arylalkyl or acyl, are particularly effective as...
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5741796 |
Pyridyl and naphthyridyl compounds for inhibiting osteoclast-mediated bone resorption
Compounds of the following general structure X-Y-Z-Aryl-A-B, for example, ##STR1## which inhibit osteoclast mediated bone resorption. Specifically, the compounds are useful for treating mammals...
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5728712 |
3,4-disubstituted-phenylsulphonamides and their therapeutic use
3,4-Disubstituted-phenylsulphonamides have therapeutic utility via TNF or phosphodiesterase inhibition.
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5728684 |
Determination of prodrugs metabolizable by the liver and therapeutic use thereof
A method of ascertaining if a prodrug is useful for treating a disease is disclosed. The prodrug is acceptable if it is metabolized in liver cells by aldehyde oxidase to produce an active drug or...
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5721246 |
Heterobicyclic sulfonamide and sulfonic ester derivatives
Novel heterobicyclic sulfonamide and sulfonic ester derivatives represented by the following general formula(I), which exhibit an antitumor activity and are lowly toxic, and processes for the...
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5721223 |
Imidazo 1,2-a! Pyridinyldiacid compounds for cognitive enhancement and for treatment of cognitive disorders and neurotoxic injury
A class of imidazo 1,2-a!pyridinyldiacid compounds is described for cognitive enhancement and for treatment of cognitive disorders and which have activity as a cognitive enhancer. Such compounds...
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