Abstract: Described is a process for preparing triazolone compounds of the formula ##STR1## comprising heating a mixture of a compound of the formula ##STR2## and a hydrazine derivative of the formula R.sup.5 --NH--NH--CHO, R.sup.5 --NH--NH--C(O)OC(CH.sub.3).sub.3 or R.sup.5 --NH--NH--C(O)OCH.sub.2 C.sub.6 H.sub.5, optionally in the presence of an added base.
Type:
Grant
Filed:
June 2, 1995
Date of Patent:
April 29, 1997
Assignee:
Schering Corporation
Inventors:
David R. Andrews, Dinesh Gala, Jacques Gosteli, Frank Guenter, William Leong, Ingrid Mergelsberg, Anantha Sudhakar
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Abstract: Thiazolemethine dyes of the formula ##STR1## where R.sup.1 and R.sup.2 are each hydrogen, C.sub.1 -C.sub.8 -alkyl with or without substitution, C.sub.3 -C.sub.4 -alkenyl, C.sub.5 -C.sub.7 -cycloalkyl, phenyl or tolyl, or are together with the nitrogen atom joining them together a heterocyclic radical,R.sup.3 is hydrogen, halogen, C.sub.1 -C.sub.8 -alkyl, substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, cyclohexyl, thienyl, hydroxyl or C.sub.1 -C.sub.8 -monoalkylamino, andQ is the radical of an acidic-CH compound,are useful in nonlinear optics.
Type:
Grant
Filed:
June 28, 1995
Date of Patent:
April 22, 1997
Assignee:
BASF Aktiengesellschaft
Inventors:
Stefan Beckmann, Karl-Heinz Etzbach, R udiger Sens
Abstract: Compounds of the formula ##STR1## wherein R.sub.3, R.sub.4, J, K, Z, and Het are as set forth herein are described.The compounds of formula I are useful as agents in the treatment of fungal infections.
Type:
Grant
Filed:
August 1, 1995
Date of Patent:
April 8, 1997
Assignee:
Schering Corporation
Inventors:
Alan B. Cooper, Anil K. Saksena, Raymond Lovey, Viyyoor Girijavallabhan, Ashit Ganguly
Abstract: Compounds of the formula ##STR1## and their salts with mineral or organic acids are useful as neurokinin receptor antagonists. Methods of preparing the compounds, especially pure STEREO ISOMERS thereof, are provided.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
April 8, 1997
Assignee:
Sanofi
Inventors:
Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
Abstract: A class of substituted piperazine derivatives of formula I ##STR1## are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated conditions, for which a selective agonist of these receptors is indicated.
Type:
Grant
Filed:
May 19, 1995
Date of Patent:
March 25, 1997
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
V. G. Matassa, L. J. Street, A. J. Reeve
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
March 25, 1997
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
March 18, 1997
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Joseph T. Strupczewski, Kenneth J. Bordeau
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Abstract: The invention is concerned with the compounds having the formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y is CH or N; R.sub.1, R.sup.2 and R.sup.3 each independently are hydrogen or C.sub.1-4 alkyl; R.sup.4 and R.sup.5 each independently are hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy; R.sup.6 is pyridinyl optionally substituted with up to two C.sub.1-4 alkyl groups; di(C.sub.1-4 alkyl) hydroxypyridinyl; di(C.sub.1-4 alkyl)C.sub.1-4 alkyloxypyridinyl; pyridazinyl optionally substituted with C.sub.1-4 alkyloxy; pyrimidinyl optionally substituted with hydroxy or C.sub.1-4 alkyloxy; thiazolyl optionally substituted with C.sub.1-4 alkyl; thiadiazolyl optionally substituted with C.sub.1-4 alkyl; benzoxazolyl or benzothiazolyl; or R.sup.6 is pyrazinyl or pyridazinyl substituted with C.sub.1-4 alkyl; Z is C.dbd.
Type:
Grant
Filed:
May 23, 1995
Date of Patent:
March 4, 1997
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Jan Heeres, Raymond A. Stokbroekx, Marc Willems, Robert J. M. Hendrickx
Abstract: Disclosed are substituted aryl piperazines of Formula I ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis. In particular compounds of Formula I are shown to be neurokinin antagonists.
Type:
Grant
Filed:
September 30, 1994
Date of Patent:
March 4, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Yuan-Ching P. Chiang, Paul E. Finke, Malcolm Maccoss, Laura C. Meurer, Daniel J. Miller, Sander G. Mills, Albert J. Robichaud, Shrenik K. Shah
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
March 4, 1997
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
February 25, 1997
Assignee:
Hoechst Roussel Pharmaceuticals, Inc.
Inventors:
Joseph T. Strupczewski, Yulin Chiang, Edward J. Glamkowski, Kenneth J. Bordeau, Grover C. Helsley
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
February 11, 1997
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
February 4, 1997
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
January 28, 1997
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
January 7, 1997
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
December 31, 1996
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
December 31, 1996
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Joseph T. Strupczewski, Edward J. Glamkowski
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
December 3, 1996
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
December 3, 1996
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
December 3, 1996
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Joseph T. Strupczewski, Edward J. Glamkowski
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
November 26, 1996
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Joseph T. Strupczewski, Kenneth J. Bordeau
Abstract: Pharmacologically active benzimidazolone derivatives as 5-HT.sub.1A and 5-HT.sub.2 receptors, useful in the treatment of CNS disorders, of formula: ##STR1## wherein the substituents are defined herein.
Type:
Grant
Filed:
March 23, 1994
Date of Patent:
November 19, 1996
Assignee:
Boehringer Ingelheim Italia S.p.A.
Inventors:
Giuseppe Bietti, Franco Borsini, Marco Turconi, Ettore Giraldo, Maura Bignotti
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
November 12, 1996
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
November 5, 1996
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
November 5, 1996
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: The invention is concerned with the compounds having the formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y is CH or N; R.sup.1, R.sup.2 and R.sup.3 each independently are hydrogen or C.sub.1-4 alkyl; R.sup.4 and R.sup.5 each independently are hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy; R.sup.6 is C.sub.1-4 alkyl; or phenyl optionally substituted with halo, C.sub.1-4 alkylcarbonylamino, C.sub.1-4 alkyloxy, C.sub.1-4 alkyl or nitro; Z is C.dbd.O or CHOH; and ##STR2## is a radical of formula ##STR3## Compositions comprising said compounds, processes for preparing the same and the use of these compounds as a method of treating Helicobacter infection.
Type:
Grant
Filed:
May 23, 1995
Date of Patent:
November 5, 1996
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Jan Heeres, Raymond A. Stokbroekx, Joseph H. Mostmans, Louis J. E. Van der Veken
Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
Type:
Grant
Filed:
July 29, 1994
Date of Patent:
October 29, 1996
Assignee:
Sterling Winthrop Inc.
Inventors:
John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
September 24, 1996
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Joseph T. Strupczewski, Edward J. Glamkowski
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
September 17, 1996
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: A class of substituted five-membered heteroaromatic compounds are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.
Type:
Grant
Filed:
May 18, 1995
Date of Patent:
September 3, 1996
Assignee:
Merck, Sharp & Dohme Ltd.
Inventors:
V. G. Matassa, L. J. Street, G. A. Showell
Abstract: 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 psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Abstract: The present invention provides an azole compound represented by the formula (I): ##STR1## wherein Ar is an optionally-substituted phenyl group; R.sup.1 and R.sup.2 are, the same or different, a hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 may combine together to form a lower alkylene group; R.sup.3 is a hydrogen atom or an acyl group; Y is a nitrogen atom or a methine group; and A is an optionally-substituted saturated cyclic amide group bonded through a first nitrogen atom, or a salt thereof, which is useful for prevention and therapy of fungal infections of mammals as antifungal agent.
Abstract: The present invention relates to novel benzocycloalkylazolethione compounds which are dopamine .beta.-hydroxylase inhibitors in which the benzocycloalkyl portion of the compound is selected from indanyl, 1,2,3,4-tetrahydronaphthalenyl and 6,7,8,9-tetrahydro-5H-benzocycloheptenyl (in which the benzo is optionally substituted with one to three substituents) and the azolethione portion of the compound is selected from 2-thioxo-2,3-dihydro-1H-imidazol-3-yl, 5-thioxo-4,5-dihydro-1H-[1,2,4]triazol-4-yl and 5-thioxo-4,5-dihydro-1H-[1,2,4]triazol-1-yl (each optionally substituted with one to three substituents); and the prodrugs, pharmaceutically acceptable salts, individual isomers and mixtures of isomers and the methods of using and preparing such benzocycloalkylazolethione compounds.
Type:
Grant
Filed:
March 17, 1995
Date of Patent:
July 23, 1996
Inventors:
Gregory R. Martinez, Owen W. Gooding, David B. Repke, Philip J. Teitelbaum, Keith A. M. Walker, Roger L. Whiting
Abstract: The present invention provides novel compounds of formula ##STR1## the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof, wherein A and B taken together form a bivalent radical of formula: --N.dbd.CH-- (a), --CH.dbd.N-- (b), --CH.sub.2 --CH.sub.2 -- (c), --CH.dbd.CH-- (d) --C(.dbd.O)--CH.sub.2 -- (e), --CH.sub.2 --C(.dbd.O)-- (f); R.sup.1 is hydrogen, C.sub.1-6 alkyl, or halo; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen; C.sub.1-8 alkyl; C.sub.3-6 cycloalkyl or C.sub.1-8 alkyl substituted with hydroxy, oxo, C.sub.3-6 cycloalkyl or aryl. Het is five- or six-membered optionally substituted heterocyclic ring. The use as a medicine, especially as a lipid lowering agent is disclosed as well as pharmaceutical compositions and processes for preparing compounds and compositions.
Type:
Grant
Filed:
May 31, 1995
Date of Patent:
May 28, 1996
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Jan Heeres, Leo J. J. Backx, Robert J. M. Hendrickx, Luc A. L. Van Der Eycken, Didier R. G. G. De Chaffoy De Courcelles
Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
Type:
Grant
Filed:
April 13, 1992
Date of Patent:
April 9, 1996
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
Abstract: Amide tetrazoles of the formula ##STR1## wherein aryl includes phenyl and naphthyl, unsubstituted or substituted, X is .dbd.O, .dbd.N--R.sub.5, or --NR.sub.3 R.sub.4, where R.sub.2, R.sub.4, and R.sub.5 include alkyl and alkoxy and R.sub.3 includes alkyl, are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia or atherosclerosis.
Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.