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5470878 |
Cell signaling inhibitors
Therapeutic compounds have the formula: (X)j-(non-cyclic core moiety), j being an integer from one to three, the core moiety is non-cyclic and X is a racemic mixture, R or S enantiomer, solvate,...
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5466443 |
Herbal-based oral composition and process for producing the same
An herbal-based oral composition for promoting darkening of human hair color upon periodic retention of the composition within the oral cavity includes an herbal mixture included at a level of from...
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5455262 |
Mercaptosulfide metalloproteinase inhibitors
Novel mercaptosulfide matrix metalloproteinase inhibitors of the Formula I, ##STR1## wherein: n is 0 or 1; R 1 is selected from the group consisting of hydrogen, lower alkyl, amino lower alkyl,...
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5424329 |
Indole-2-carboxamides as inhibitors of cell adhesion
3-Substituted-indole-2-carboxamides are described as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory...
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5422361 |
Stable cream and lotion bases for lipophilic drug compositions
A cosmetically elegant, physically and chemically stable base in the form of an oil-in-water emulsion for use in cream and lotion lipophilic drug containing- pharmaceutical compositions containing...
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5407961 |
α-substituted benzenemethanamine derivatives and pharmaceutical use
The present invention is concerned with antiretroviral (e.g. anti HIV-1) compounds having the formula ##STR1## Pharmaceutical compositions containing said compounds of formula (I-a) or (I-b), and...
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5382593 |
New 3-(hydroxybenzylidenyl)-indolin-2-ones
The invention relates to a compound selected from those of formula (I): ##STR1## wherein R 1 , R 2 , R 3 , R 4 , R 5 and X are as defined in the description, its Z and E isomers, its optical...
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5380722 |
Indole carboxamides
Novel indole-carboxamides of the formula ##STR1## and their non-toxic pharmaceutically acceptable acid addition salts having remarkable anti-arrhytmic properties.
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5374652 |
2-oxindole compounds which are useful as tyrosine kinase inhibitors
Aryl- and heteroarylethenylene derivatives of formula ##STR1## wherein Y is a mono- or bicyclic ring system chosen from (A), (B), (C), (D), (E), (F) and (G) ##STR2## R is a group of formula R 1 ...
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5373019 |
Pharmaceutical lactam compositions for inhibition of erythrocyte and thrombocyte aggregation
The present invention provides compounds and pharmaceutical compositions containing indolones of the general formula: ##STR1## These indolones where no and the pharmaceutical compositions...
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5350761 |
Indolyl substituted hydroxylamine derivatives
Disclosed are the compound of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl, biaryl, C 3 -C 7 -cycloalkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl-lower alkynyl,...
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5312820 |
Substituted carbamoyl and oxycarbonyl derivatives of biphenylmethylamines
Carbamoyl and oxycarbonyl derivatives of biphenylmethylamines of structure I are angiotensin-II antagonists with balanced AT 1 and AT 2 activity useful in the treatment of hypertension and...
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5308839 |
Composition comprising non-steroidal anti-inflammatory agent tenidap and effectively non-antibacterial tetracycline
A method for treating mammals suffering from rheumatoid arthritis, other tissue-destructive conditions, and chronic inflammatory or other conditions associated with excess metalloproteinase...
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5288749 |
Tertiary and secondary amines as alpha-2 antagonists and serotonin uptake inhibitors
The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and...
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5288743 |
Indole carboxylate derivatives which inhibit leukotriene biosynthesis
Compounds of the structure ##STR1## where A is straight or branched divalent alkylene or divalent cycloalkylene, R 1 is selected from hydrogen; alkylthio; optionally substituted phenylthio;...
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5284841 |
Benzo-fused lactams promote release of growth hormone
There are disclosed certain novel compounds identified as benzo-fused lactams ##STR1## which promote the release of growth hormone in humans and animals. This property can be utilized to promote...
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5273993 |
Compounds having one or more aminosulfonyloxy radicals useful as pharmaceuticals
Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula: (HO)p--A--[--OS(O) 2 NR 1 R 2 ] z wherein A...
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5272170 |
Tetralones with pharmacological activity
The present invention relates to new tetralones having the formula I: ##STR1## wherein: R 1 and R 2 represent hydrogen, halogen, cyano, C 1 -4 alkyl, C 1 -4 alkoxy, trifluoromethyl,...
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5268385 |
Method for treating schizophrenia
This invention provides a method for treating the symptoms of schizophrenia by interacting selectively with presynaptic dopaminergic D 2 receptors without appreciably activating postsynaptic...
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5254595 |
Aryloxypropanolaminotetralins, a process for their preparation and pharmaceutical compositions containing them
Aryloxypropanolaminotetralins with beta-antagonist activity of the formula ##STR1## wherein R is hydrogen, hydroxy or methoxy and Ar is an optionally substituted aromatic or heteroaromatic group,...
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5250565 |
Indole-,benzofuran-,and benzothiophene-containing lipoxygenase-inhibiting compounds
Pro-drugs of potent 5-lipoxygenase inhibiting compounds comprise compounds of the formula ##STR1## in which A is an alkylene or alkenylene group, X is oxygen, sulfur, sulfoxyl, or substituted...
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5227395 |
Anti-platelet aggregating agent
The use of 1-phenoxycarbonyl-2-pyrrolidinone derivatives as an anti-platelet aggregating agent. The derivatives are of the formula ##STR1## wherein R is a C 1 -C 6 alkyl group, a C 1 -C 6 ...
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5212320 |
Indole derivatives and their use for testosterone 5-alpha-reductase-mediated diseases
Indole derivatives of the formula ##STR1## and pharmaceutical compositions thereof. They are useful for treating or preventing testosterone 5-alpha-reductase-mediated diseases, such as alopecia,...
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5206261 |
Oxindole derivative
The present invention provides an oxindole derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and...
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5198012 |
Phosphate activators for cyclohexenone herbicides
A biocide composition comprises an effective amount of a biocide and an effective amount of a biocide activator selected from the group consisting of an alkyl phosphate, an alkenyl phosphate, a...
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5198461 |
Isatine derivatives, their preparation and use
A method of treatment with compounds having the formula ##STR1## R 1 is hydrogen, C 1 -6 -alkyl which may be branched, C 3 -7 -cycloalkyl, benzyl, phenyl which may be substituted, acyl, hydroxy, C...
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5192792 |
Isatine derivatives, and their method of use
A method of treatment of central nervous system disorders with compounds having the formula ##STR1## and isomers thereof wherein R 1 , R 2 , R 4 , R 5 , R 6 , and R 7 and as defined in the...
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5192791 |
Fused ring heterocycles and pharmaceutical compositions containing same
A novel class of pyrrolidin-2-one and piperidin-2-one compounds in which the nitrogen atom is bonded to an oxyphenyl radical having tertiary-alkyl and tri-methylsilyl substituents. The compounds...
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5179119 |
1,3-dihydro-1-(pyridinylamino)-2H-indol-1-ones and intermediates for the preparation thereof
This invention relates to 1,3-dihydro-1-(pyridinylamino)-2H-indol-2-ones of the formula ##STR1## where R 1 , R 2 and R 3 are independently hydrogen, loweralkyl, aryl, arylloweralkyl or...
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5177102 |
Polyisoprene compounds and salts thereof
There are given disclosures on a polyisoprene compound of the formula ##STR1## wherein Y is S, O, NH or ##STR2## l is an integer of 2-10, Z is a group of ##STR3## R 1 and R 2 are same or...
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5169860 |
Antitumor compositions and methods of treatment
This invention provides the use of certain benzofuransulfonamide, benzothiophenesulfonamide, and indolesulfonamide derivatives in the treatment of susceptible neoplasms in mammals. Also provided...
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5164404 |
Hydrazone derivatives and their use
A method of antagonizing the biological effects of an excitatory amino acid of a subject in need of such antagonization, comprising the step of administering to said subject an effective excitatory...
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5155110 |
Fenamic acid hydroxamate derivatives having cyclooxygenase and 5-lipoxygenase inhibition
The present invention is novel selected hydroxamic acid derivatives of fenamic acids having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating...
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5137909 |
Indole derivative and method of production thereof
An indole derivative represented by the general formula (I) ##STR1## wherein R is hydrogen, lower alkyl having 1 to 6 carbons, carboxymethyl, or substituted or unsubstituted aralkyl; R 1 , R 2 , R...
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5132319 |
1-(hydroxylaminoalkyl) indole derivatives as inhibitors of leukotriene biosynthesis
Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They...
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5132312 |
Substituted cyclohexene derivatives as HMG-CoA reductase inhibitors
Disclosed are novel 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy...
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5128352 |
Anti-inflammatory 1-heteroaryl-oxindole-3-carboxamides
Certain N-(substituted)-1-heteroaryl-oxindole-3-carboxamides wherein the N-substituent is thienyl, furyl, phenyl or substituted phenyl, are inhibitors of cycloxygenase and lipoxygenase enzymes and...
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5124347 |
3-5-ditertiarybutylphenyl-4-hydroxymethylidene derivatives of 1,3-dihydro-2H-indole-2-ones as antiinflammatory agents
The present invention is for selected novel compounds which are indoles substituted at the 3-position with [3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene as well as pharmaceutical...
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5124327 |
HIV reverse transcriptase
Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds or pharmaceutical...
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5122537 |
Arylvinylamide derivatives and pharmaceutical use
The invention relates to new arylvinylamide derivatives of formula ##STR1## wherein Y is a bicyclic ring system chosen from (A), (B), (C), (D), and (E); ##STR2## in which m is zero, 1 or 2; R is...
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5118703 |
Prodrugs of antiinflammatory 3-acyl-2-oxindole-1-carboxamides
Certain enol ethers and esters of the formula ##STR1## where X and Y are each hydrogen, fluoro or chloro; R 1 is 2-thienyl or benzyl and R is alkanoyl, cycloalkylcarbonyl, phenylalkanoyl,...
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5114952 |
Isoquinolinylsulfonamides as anti-arrhythmic agents
A series of novel alkanesulphonamidophenyl-N-alkyl-N-(heterocyclic-alkyl)alkyl
amine derivatives have been prepared, including their pharmaceutically acceptable salts. These compounds are useful in...
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5086070 |
4-benzyl-1H-indoles and anti-arrthymic use thereof
Novel 4-benzyl-1H-indoles of the formula ##STR1## in all diastereoisomeric forms and mixtures thereof having antiarhythmic activity.
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5081138 |
3-hetero-substituted-n-benzyl-indoles and prevention of leucotriene synthesis therewith
Compounds having the formula: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They...
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5075302 |
Mercaptoacyl aminolactam endopeptidase inhibitors
Mercaptoacyl aminolactam inhibitors of endopeptidases of the formula ##STR1## wherein Y is -(CHR 5 ) n (CR 3 R 4 )- or -(CR 3 R 4 ) p X(CR 3 R 4 ) q -, wherein two substituents selected...
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5041460 |
Heter-aliphatic carboxamides
This invention provides a series of novel heter-aliphatic carboxamides of formula I in which the group >Z--Y--X< is selected from >CCH--N<, >N--CHC<, >CN--N< and...
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5025005 |
Lipid derivatives, their production and use
Novel lipid derivatives of the formula ##STR1## [wherein R 1 is alkyl or alkylcarbamoyl; R 2 is hydrogen, hydroxy which may be substituted, amino which may be substituted or cyclic amino; R 3 is...
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5019587 |
Bicyclic carboxamides, compositions containing same and use thereof
The present invention provides compounds of the general formula (I) which inhibit the aggregation of erythrocytes or thrombocytes ##STR1## wherein A is hydrogen or C 1 -C 6 -alkyl, C 2 -C 6 ...
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5008283 |
Use of tenidap to inhibit activation of collagenase and to inhibit the activity of myeloperoxidase
This invention relates to the use of tenidap, 5-chloro-2,3-dihydro-2-oxo-3-(2-thienylcarbonyl)-indole-1-ca
rboxamide, and the pharmaceutically-acceptable base salts thereof to inhibit activation of...
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5006547 |
Tenidap as an inhibitor of the release of elastase by neutrophils
This invention relates to the use of tenidap, 5-chloro-2,3-dihydro-2-oxo-3-(2-thienylcarbonyl)-indole-1-ca
rboxamide, and the pharmaceutically-acceptable base salts thereof to inhibit the release...
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