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5726195 |
Aminoacyl adenylate mimics as novel antimicrobial and antiparasitic agents
Certain novel aminoacyl adenylate mimics are described. An exemplary compound of this invention is S-(R*,R*)!-3,6-anhydro-1,2-dideoxy-1- 5- 4- (5-nitro-2-thienyl)ethynyl!ph...
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5714498 |
Benzimidazole derivatives
The invention is directed to substituted benzimidazole compounds which are ligands for dopamine receptor subtypes used in the treatment of the dopamine system.
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5681836 |
Methanesulfonate salts of antipsychotic benzofuran derivatives
The methanesulfonate salt of a class of antipsychotic compounds comprising a benzo b!furan moiety and a substituted heterocyclic moiety, linked via the 3-position of the benzo b!furan moiety by a...
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5670511 |
Indolepiperidine derivatives
Indolepiperidine derivatives of the formula I ##STR1## and their physiologically acceptable salts exhibit action on the central nervous system, in particular dopamine-agonistic or...
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5668145 |
Amino-substituted pyrazoles having CRF antagonistic activity
The invention relates to compounds of the formula I ##STR1## and to pharmaceutically acceptable salts thereof, wherein Z, A, Y, X 1 , R 1 , R 2 , and R 3 are as defined herein. The invention...
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5668131 |
Substituted aminoalkylaminopyridines
Compounds of formula I ##STR1## wherein R1, R2, R3, R4, R5, R6, X, n and A have the meanings as given in the description, can be used for combatting Helicobacter bacteria.
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5665722 |
Benzofuran derivatives as D.sub.4 receptor antagonists
A class of chemical compounds comprising a benzo [b] furan moiety and a substituted heterocyclic moiety, linked via the 3-position of the benzo [b] furan moiety by a methylene group, are...
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5663449 |
Intermediate compounds in the synthesis of heteroarylpiperidines, pyrrolidines and piperazines
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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5654319 |
N-[(4-heteroaryl-1-piperidinyl)alkyl]-2,3-naphthalimides 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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5652368 |
1,2,3,4-tetrahydroquinoline 2,3,4-trione-3 or 4-oximes
Disclosed herein are substituted or unsubstituted 1,2,3,4-tetrahydroquinoline-2,3,4-trione-3 or 4-oximes or pharmaceutically acceptable salts thereof that have high binding to the glycine receptor...
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5646161 |
Heteroarylpyrrolidines and their use as antipsychotics and analgesics
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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5641787 |
Indole derivatives as dopamine D.sub.4 antagonists
The present invention accordingly provides the use of a compound of formula I, or a pharmaceutically acceptable salt thereof or a prodrug thereof: ##STR1## wherein R 1 represents hydrogen or C 1...
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5639764 |
2-[(4-heteroaryl)-1-piperidinyl)alkyl]-1,3-indandiones and related compound 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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5637708 |
Structure based design of capsid stabilizing or antiviral agents
Agents having the structure, U--CH 2 --V--CH 2 --W, and agents having the structure, U--CH 2 --V--CH 2 --W--X--Y--Z, where U, W, and Z are double fused aromatic rings, V is a single...
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5635516 |
(Thia) cycloalkyl[B]indole compounds as anti-inflammatory agents
A compound selected from those of formula (I): ##STR1## in which R 1 , R 2 , R 3 and A are as defined in the description.
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5629430 |
Trifluoromethylpyrroloindolecarboxylic acid ester and process for production thereof
Trifluoromethylpyrroloindolecarboxylic acid ester derivatives, and optical isomers and pharmaceutically acceptable salts thereof are provided which are represented by the general formula (1):...
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5620988 |
Substituted tetrahydropyridines and hydroxypiperidines as central nervous system agents
Substituted tetrahydropyridines and hydroxypiperidines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as...
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5614543 |
1-(aryloxyalkyl)-3- (heteroaryl) pyrrolidines and related compounds useful as antipsychotics and analgesics
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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5612342 |
***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***
[(4-heteroaryl-1-piperindyl)alkoxy]-3,4-dihydro-1(2H)-naphthalenones 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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5612343 |
N-[(4-heteroaryl-1-piperazinyl)alkyl]-2,3-naphthalimides 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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5607624 |
Process for the preparation of 3-arylbenzofuranones
A process for the preparation of compounds of formula I ##STR1## wherein the general symbols are as defined in claim 1, which comprises reacting a compound of formula III ##STR2## wherein the...
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5605913 |
***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***
1-(arylthioalkyl, arylaminoalkyl or arylmethylenealkyl)-4-(heteroaryl) piperidines and related compounds useful as antipsychotics and analgesics
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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5597842 |
3-heteroaryl-1-pyrrolidinealkanols and derivatives thereof 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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5591745 |
(4-heteroaryl)-1-[(2,3-dihydro-1H-isoindol-2-yl)alkyl] piperidines 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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5589494 |
2-[(3-heteroaryl-1-pyrrolidinyl)alkyl]-1,3-dioxanes 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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5580891 |
N-[heteroaryl-1-pyrrolidinyl)alkyl]-2-benoxazolinones 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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5580875 |
1-[(2-pyrimidinyloxy)alkyl]-3-(heteroaryl)pyrrolidines and related compounds and 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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5578605 |
N-[(4-heteroaryl)-1-piperidinyl)alkyl]-1,2,3,4-tetrahydroquinolines 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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5578624 |
Heteroarylpyrrolidines and their use as antipsychotics and analgesics
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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5576313 |
Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to...
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5574032 |
N-[(4-(he teroaryl)-1-piperazinyl)alkyl]-10,11-dihydro-5H-dibenz[BFS]azepines 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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5571814 |
N-[(4-heteroaryl-1-pyrrolidinyl)alkyl]phthalimides 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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5565470 |
Cycloaminoalkoxyphenyl derivatives, a process for their preparation as well as the compositions containing them
Cycloaminoalkoxyphenyl derivatives useful for the treatment of certain pathological syndromes of the cardiovascular system and ocular diseases of formula: ##STR1## in which: B represents a --S--,...
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5563144 |
Antiserotonins, their preparation and pharmaceutical compositions containing them
This invention relates to compounds having the formula R 1 -(CH 2 ) n -Het wherein R 1 is a residue having the formula (B), (C), (D); Het represents a radical phenyl-4 tetrahydro-1,2,3,6...
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5561128 |
N-[(4-(hete roaryl)-1-piperidinyl)alkyl]-10,11-dihydro-5H-dibenz[B,F]azepines 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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5559116 |
N-[(4-heteroaryl-1-piperazinyl) alkyl]-1H-benz[de]isoquinoline-1,3 (2H-)-diones 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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5554631 |
5-pyrrolyl-6-halogeno-2-pyridylmethylsulfinyl benzimidazole derivatives
The present invention relates to a novel compound 5-pyrrolyl-6-halogeno-2-pyridylmethylsulfinylbenzimidazole derivative having the following formula (I): ##STR1## or a pharmaceutically acceptable...
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5545651 |
Imidazole 5-position substituted angiotensin II antagonists
Novel substituted imidazoles of Formula (I), which are useful as angiotensin II antagonists, are disclosed: ##STR1##
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5532243 |
Antipsychotic nitrogen-containing bicyclic compounds
There are provided nitrogen-containing bicyclic compounds, pharmaceutical compositions containing these compounds and methods of using these compounds to treat physiological or drug-induced...
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5523299 |
5-(2-oxyphenyl)-pyrrole derivatives as dopamine D.sub.3 receptor antagonists
Compounds of formula (I), ##STR1## wherein R 1 represents C 1 -4 alkyl; and R 2 , R 3 , R 4 and R 5 each independently represent hydrogen, halogen, C 1 -4 alkyl, C 1 -4 alkoxy, C 1 -4 alkoxyC 1...
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5519034 |
Tetraisoquinoline compounds which have useful pharmaceutical utility
Tetrahydroisoquinoline compounds of formula I ##STR1## and pharmaceutically acceptable salts and lipophilic ester thereof have utility as analgesics and in the treatment of psychoses, Parinson's...
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5504082 |
Pyridine compound and pharmaceutical compostions
A pyridine compound of the formula ##STR1## wherein R 1 is a hydrogen, a halogen, an alkyl, an alkoxy or the like, R 2 and R 3 are each a hydrogen, a halogen or an alkyl, --PQ-- is...
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5498717 |
6,7-dialkoxy-3,4-diydroisoquinolin-8-yl compounds
This invention relates to novel 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols, a process for preparing the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols reioselectively and in a high yield utilizing the...
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5488057 |
2-oxindole compounds which have useful tyrosine kinase activity
The present invention provides novel aryl- and heteroarylethenylene derivatives which are useful as tyrosine kinase activity inhibitors.
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5484804 |
Perhydroisoindole derivatives as antagonists of substance P
This invention relates to novel perhydroisoindole derivatives of general formula (I), ##STR1## wherein radicals R are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl...
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5472962 |
Benzothiophene derivative
A benzothiophene derivative represented by the formula ##STR1## or a salt thereof has an excellent antiestrogenic activity, and is useful as a therapeutic agent of breast cancer, endometrial...
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5470855 |
Certain heterocyclic thiazole derivatives and their therapeutic use
The invention relates to compounds of formula: ##STR1## in which: A is selected from O or S; B is selected from C or N; Z 1 is selected from C 1 -C 4 alkylene or phenylene; Z 2 is C 1 -C...
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5466698 |
Substituted tetrahydrophyridines and hydroxypiperidines as central nervous system agents
Substituted tetrahydropyridines and hydroxypiperidines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as...
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5446164 |
Process for preparing 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ol
This invention relates to novel 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols, a process for preparing the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols reioselectively and in a high yield utilizing the...
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5444056 |
Aminoalkoxyphenyl derivatives, process for their preparation and compositions containing them
An aminoalkoxyphenyl derivative of general formula: Cy--B--Ph--O--A--Am (1) as well as a pharmaceutically acceptable salt thereof in which B represents a...
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