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5302593 |
Aminoalkylcarbamic esters of eseroline suitable for use as chlorinesterase activity inhibitors
Aminoalkylcarbamic esters of eseroline suitable for use as cholinesterase activity inhibitors, having general formula (I) ##STR1## where R stands for an amine selected out of the group consisting...
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5302611 |
Oxindole alkaloids having properties stimulating the immunologic system & preparation containing the same
Tetra- and pentacyclic oxindole alkaloids, in particular the alloisopteropodine, isomer A, a pentacyclic oxindole alkaloid, are suitable for the unspecific stimulation of the immunologic system,...
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5302599 |
Therapeutically useful heterocyclic indole compounds
A therapeutically useful compound of formula I ##STR1## or pharmaceutically acceptable salts thereof where A and B are oxygen, sulfur or CH 2 , X is an amine moiety as defined herein and R 1 and R...
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5296499 |
Indole derivatives, their production and use
An agent for inhibiting bone resorption comprising an indole derivative of the formula (I): ##STR1## wherein each ring of A and B is optionally substituted, R is a hydrogen atom, a lower alkyl...
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5296489 |
Immunosuppressive macrocyclic compounds
There are provided compounds of formula (I), wherein R 1 represents H, OH or alkoxy; R 2 represents H; in addition R 1 and R 2 may together represent a second bond between the carbon atoms to...
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5292765 |
Neuroprotection by indolactam V and derivatives thereof
A method for reducing adverse effects of neurotoxic injury, which comprises administering to a patient susceptible to neurotoxic injury an effective amount, sufficient to reduce the injury, of a...
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5284840 |
Alkylidene macrolides having immunosuppressive activity
Alkylidene macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by derivitization at C-9 or C-22. These macrolide immunosuppressants are useful in a...
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5284877 |
Alkyl and alkenyl macrolides having immunosuppressive activity
Alkyl and alkenyl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by oxidation and derivitization at C-17. These macrolide immunosuppressants...
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5276053 |
Polycyclic amines useful as cerebrovascular agents
A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of...
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5262409 |
Binary tumor therapy
Method for killing a cycling cell, by contacting the cell with a first agent that blocks progression of the cell cycle in the cell, and thereafter contacting the cell with a second agent that...
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5258383 |
DC-89 derivatives
DC-89 derivatives represented by the formula: ##STR1## wherein X represents hydrogen or CO 2 CH 3 ; and ##STR2## wherein Z represents Cl or Br; R represents hydrogen, CONR 1 R 2 (in which R 1 ...
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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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5250563 |
Inhibitors of HIV protease
Novel cytochalasins are the biotransformed products after incubation with a substrate in a culture of the microorganism Kibdelosporangium sp. (Merck Culture Collection MA 6559), ATCC No. 53771. The...
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5248692 |
DC-89 derivatives as anti-tumor agents
Novel DC-89 derivatives as shown below have an excellent anti-tumor activity, and thus are useful as anti-tumor agent ##STR1## wherein L represents chlorine or bromine; R represents ##STR2##...
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5248691 |
Furanoindolines
This invention provides novel furanoindoline compounds effective in inhibiting the growth of solid tumors.
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5244888 |
5-HT selective agents
Substituted 8-alkoxy-1,2,3,3a,8,8a-hexahydroindeno[1,2-c]pyrroles; 5-alkoxy-2,3,4,4a,9,9a-hexahydro-1-H-indeno[2,1-c]pyridines;
and 9-alkoxy-2,3,3a,4,5,9a-hexahydro-1H-benz[e]isoindoles are...
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5242918 |
Isatinoxime derivatives, their preparation and use
A compound having the formula ##STR1## wherein R 4 and R 5 independently are hydrogen, halogen, CF 3 , CN, NO 2 or SO 2 NR 1 R 2 wherein R 1 is hydrogen or straight, C 1 -6 -alkyl which...
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5240930 |
Pharmaceutical compositions for treatment of depression and low blood pressure
A pharmaceutical composition which comprises a mixture of an alpha-2 adrenoceptor antagonist, preferably idazoxan, or a pharmaceutically acceptable salt thereof, and either a catecholamine...
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5234941 |
Carbamate derivatives of 4-amino-3-isoxazolidinones, 3-amino-1-hydroxypyrrolidin-2-ones and 1-amino-1-cyclopropanecarboxylic acid analogs
There are disclosed various compounds of the formula below, ##STR1## where the parameters R 1 and R 2 are as defined in the specification, which compounds are useful for alleviating various...
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5229409 |
6-substituted-tetrahydrobenz[cd]indoles
The present invention involves certain 4-amino-6-substituted-tetrahydrobenz[cd]indoles and their use in treating disorders which can be benefited by modifying 5-HT A receptor function.
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5229411 |
Substituted benz[cd]indol-2-(1H)-ones and use as antihypertensive agents
Compounds of the formula: ##STR1## wherein R 1 , R 2 and m are defined in the specification are provided. These compounds are useful as antihypertensive agents.
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5225434 |
Pesticidal and herbicidal polycyclic 3-aryl-pyrrolidine-2,4-dione derivatives
Insecticidal, acaricidal and herbicidal polycyclic 3-aryl-pyrrolidine-2,4-dione derivatives of the formula ##STR1## in which A represents the radical of a bi-, tri- or polycyclic system which is...
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5225403 |
C-21 hydroxylated FK-506 antagonist
Described is a process for producing a new FK-506 antagonist agent, a C-21 hydroxylated analog of FR-900520 under novel fermentation conditions utilizing the novel microorganism, Streptomyces...
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5223517 |
Heterocyclically substituted cycloalkano[b]-indolesulphonamides
Heterocyclically substituted cycloalkano[b]-indolesulphonamides can be prepared by reaction of appropriate N-unsubstituted indoles with acrylonitrile, followed by hydrolysis, esterification or...
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5223527 |
Isatineoxime derivatives and their use
A compound having the formula ##STR1## wherein R 1 is C 1 -6 -alkyl which may be branched or cyclic; R 2 is C 1 -6 -alkyl which may be branched or cyclic; or wherein R 1 and R 2 together...
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5221681 |
Substituted benzoxazepines and benzothiazepines
The present invention relates to new substituted benzoxazepines and benzothiazepines of the general formula I ##STR1## in which X, R 1 , R 2 and R 3 have the meaning given in the description,...
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5216017 |
Pyrrolo[2,3-b]indole-ketones and analogs
This invention relates to pyrrolo[2,3-b]indole ketones of the formula ##STR1## where R 1 is loweralkyl, aryl or arylloweralkyl; R 2 is hydrogen, halogen or loweralkyl; R 3 is hydrogen or...
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5208241 |
N-heteroaryl, N-alkylheteroaryl, N-alkenylheteroaryl and N-alkynylheteroarylmacrolides having immunosuppressive activity
N-Heteroaryl, N-alkylheteroaryl, N-alkenylheteroaryl and N-alkynylheteroaryl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by amination,...
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5206260 |
Hexahydropyrrolo[2,3-b]indole derivatives
Mammalian metabilites of the known acetylchloinesterase inhibitor trimethyl-1,3a,8-hexahydro-1,2,3,3a,8,8a-pyrrol[2,3-b]indole
-5(3aS,8aR) heptylcarbamate are themselves cholinesterase inhibitors...
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5204374 |
Cycloalkano(b)dihydroindoles and -indolesulphonamides substituted by heterocycles
New cycloalkano[b]dihydroindoles and -indolesulphonamides, substituted by heterocycles, of the formula (I) ##STR1## in which R 1 , R 2 , R 3 and R 4 are identical or different and represent...
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5202321 |
Thiopyrano[2,3,4-c,d]indoles 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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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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5196437 |
Method for treating hepatic diseases and regenerating liver tissue using FK 506 and related compounds
Macrolide compounds having the structure shown below ##STR1## wherein R 1 is hydroxy or protected hydroxy, R 2 is hydrogen, hydroxy or protected hydroxy, R 3 is methyl, ethyl, propyl or allyl, R...
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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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5190967 |
Medicaments for treating erectile disorders
The use of a compound of formula I ##STR1## wherein R is a hydrogen atom or a group selected from C 1 -6 alkyl (optionally substituted by C 3 -7 cycloalkyl), C 3 -6 alkenyl, C 3 -6 alkynyl, C 3 -7...
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5189042 |
Fluoromacrolides having immunosuppressive activity
Fluoromacrolides and derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by oxidation and fluorination at C-20. These macrolide immunosuppressants...
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5185028 |
N-acyl loline derivatives as insecticides and herbicides
N-substituted loline derivatives having the formula ##STR1## have utility as herbicides and insecticides.
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5183826 |
Antiviral agent
An antiviral agent produced by Hypoxylon fragiforme and having the structure: ##STR1## is described. The product has high activity as an HIV protease enzyme inhibitor and is useful in the treatment...
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5180733 |
Biogenic amine uptake inhibitors
Compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein M is 0, 1 or 2 and n is 0 or 1; R 1 is hydrogen or lower alkyl; R 2 is C 1 -C 6 -alkyl...
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5177101 |
Memory enhancing and analgesic aminocarbonylcarbamates related to physostigmine
There are disclosed various derivatives related to physostigmine of the formula below, ##STR1## where Z, R 1 and R 2 are as defined in the specification, which compounds are useful for enhancing...
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5173497 |
Alpha-oxopyrrolo[2,3-B]indole acetic acids, esters, amides and related analogs
This invention relates to compounds of the formula ##STR1## where X is --NH, oxygen, N-loweralkyl, or N-arylloweralkyl; R 1 is hydrogen, loweralkyl, cycloalkyl, aryl, arylloweralkyl,...
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5171750 |
Substituted phenserines as specific inhibitors of acetylcholinesterase
The present invention relates to substituted phenylcarbamate or naphthylcarbamate tricyclic compounds which provide highly potent and selective cholinergic agonist and blocking activity and their...
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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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5143918 |
Halomacrolides and derivatives having immunosuppressive activity
Novel C-3" and C-4" halogen-substituted macrolides of FK-506 type structural Formula I: ##STR1## are described. These macrolide immunosuppressants are useful in a mammalian host for the treatment...
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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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5128363 |
Trifluoromethoxy substituted 1,3,4,9-tetrahydropyrano-[3,4-b]indole-1-acetic acids
Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a trifluoromethoxy substituent in the 5-, 6-, 7-, or 8-position, and methods for...
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5128364 |
Pyrrolo[1,2-a]indole hydroxylamine 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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5120842 |
Silyl ethers of rapamycin
A compound of the structure ##STR1## wherein R 1 is --SiR 3 R 4 R 5 ; R 2 is hydrogen or --SiR 3 R 4 R 5 ; and R 3 , R 4 , and R 5 are each, independently, alkyl, alkenyl, aralkyl,...
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5109007 |
Attenuation of ethyl alcohol intoxication with alpha-2 adrenoceptor antagonists
A method is provided for attenuating the intoxicating effects of ethyl alcohol in a patient, by administering to a patient in need thereof, an alpha-2 adrenoceptor antagonist compound. Two...
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5096897 |
Antithrombotic substituted cycloalkano(b)dihydroindole- and -indole-sulphonamides
Substituted antithrombotic substituted cycloalkano[b]-dihydroindole- and -indole-sulphonamides for treatment of thromboses, thromboembolisms, ischaemias, asthma and allergies, of the formula...
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