Abstract: This invention relates to phenyl amidine derivatives having the following formula ##STR1## or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidine derivatives.
Type:
Grant
Filed:
December 22, 1994
Date of Patent:
January 2, 1996
Assignee:
G. D. Searle & Co.
Inventors:
Robert B. Garland, Masateru Miyano, Jeffery A. Zablocki, Lori A. Schretzman
Abstract: The present invention relates to a novel process for the preparation of heterocyclic alkylamide derivatives having the following formula: ##STR1## and the pharmaceutically acceptable acid addition salt thereof wherein X represents halo, alkyl having 1 to 6 carbon atoms, hydrido, trifluoromethyl, phenyl, or lower alkoxy having 1 to 6 carbon atoms; Y represents the group --CN or --CONH.sub.2 ; R.sub.2 represents alkyl having 1 to 6 carbon atoms; R.sub.
Type:
Grant
Filed:
September 8, 1993
Date of Patent:
July 11, 1995
Assignee:
G. D. Searle & Co.
Inventors:
John H. Dygos, Thomas R. Kowar, Kathleen T. McLaughlin, Gatis Plume, Michael L. Prunier, Richard J. Salzmann, Mike G. Scaros, Joseph J. Wieczorek
Abstract: This invention relates to compounds having the following formula ##STR1## which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidine thio derivatives.
Type:
Grant
Filed:
February 12, 1993
Date of Patent:
April 25, 1995
Assignee:
G. D. Searle & Co.
Inventors:
Steven P. Adams, Richard J. Lindmark, Masateru Miyano, Joseph G. Rico
Abstract: This invention relates to novel N-substituted lactams having the following formula ##STR1## useful in the treatment and prevention of Cholecystokinin (CCK) related disorders of the gastrointestinal, central nervous and appetite regulatory systems of mammals.
Type:
Grant
Filed:
December 11, 1990
Date of Patent:
April 13, 1993
Assignee:
G. D. Searle & Co.
Inventors:
Daniel P. Becker, Daniel L. Flynn, Clara I. Villamil
Abstract: A novel S diastereomer of an N.sup.6 -[(2-hydroxypropyl)aryl] adenosine, which diastereomer exhibits fewer CNS side effects than the racemate, but with no decrease in cardiovascular activity. The invention further provides for compositions incorporating the diastereomer, and methods of its use, as well as pharmaceutically acceptable salts thereof.
Abstract: This invention relates to novel substituted imidazopyridine derivatives having the following formula ##STR1## or a pharmaceutically acceptable acid addition salt useful in the treatment of diseases or disorders mediated by platelet-activating factor. This invention relates to pharmaceutical compositions of such substituted imidazopyridines.
Type:
Grant
Filed:
March 6, 1989
Date of Patent:
May 28, 1991
Assignee:
G. D. Searle & Co.
Inventors:
Ish K. Khanna, Roger Nosal, Richard M. Weier
Abstract: The present disclosure relates to an external analgesic solid stick composition for the topical administration of active analgesic agents. The compositions are dimensionally stable solid compositions comprising an external analgesic agent incorporated into a non-reactive hydrophobic wax matrix.
Abstract: 25-Alkylcholest-5-ene-3.beta.,22-diols and esters thereof adapted to inhibit the activity of 3-hydroxy-3-methylglutaryl coenzyme A reductase are disclosed.
Abstract: 1-[2-Hydroxy-3-(4-alkyl-1-piperazinyl)-4-oxo-2-cyclobuten-1-ylidene]-4-alky lpiperazinium hydroxide inner salts and related compounds are described herein. These compounds are useful as anti-viral agents. They are prepared from 2-anilino-3-hydroxy-4-(phenylimino)-2-cyclobuten-1-one and the appropriate monosubstituted piperazine.
Abstract: The invention encompasses novel 5-substituted-2-phenylbenzo[b]thiophene-3-alkylamines and related compounds of the general formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sub.1 and R.sub.2 each independently represents H or an alkyl having from 1 to 8 carbon atoms or R.sub.1 and R.sub.2 together with N represents an azamonocyclic ring selected from the group comprising pyrrolidinyl, piperazinyl, substituted pyrrolidinyl wherein the substituent is an alkyl containing from 1 to 4 carbon atoms and substituted piperazinyl wherein the substituent is an alkyl containing from 1 to 4 carbon atoms or an alkanol wherein the alkyl moiety contains 1 to 4 carbon atoms; Y represents H, halogen or alkyl having 1 to 4 carbon atoms; X represents H, halogen, alkyl having 1 to 4 carbon atoms and alkoxy wherein the alkyl moiety contains 1 to 4 carbon atoms; and n is a positive integer from 1 to 4. These compounds possess utility as neuroleptics or anti-bacterial agents.
Abstract: This invention encompasses novel 2-(2,2-diphenyl-4-pentenyl-1-azabicyclo[2.2.2]octane and related compounds. These compounds are useful anti-diarrheal agents which possess little if any analgesic activity.
Abstract: This invention relates to a new class of compounds of the indole series. Particularly, it relates to novel thio esters of 1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid. These novel compounds are prepared by reacting 1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid with an appropriate thiol and diethyl phosphorocyanidate or diphenyl phosphorazidate in the presence of triethylamine in a dimethylformamide solution. These compounds are useful anti-inflammatory agents.
Abstract: A new process utilizing certain novel intermediates for the preparation of 1-diphenylmethyl-4-(6-methyl-2-pyridylmethyleneamino)piperazine is described herein. The process utilizes readily available starting material and has the distinct advantage of having no N-nitroso intermediate in its procedure.
Abstract: The preparation of 7-aza-6-alkoxy-1-tetralones which originates with dihydroresorcinol is disclosed herein. The subject compounds are useful intermediates in the synthesis of various compounds which possess valuable pharmacological properties.
Abstract: This invention encompasses novel 5-[1,1-diphenyl-3-(4-phenylpiperidino)propyl]-2-methyl-1,3,4-oxadiazoles and structurally related compounds. These compounds are useful anti-diarrheal agents which , in addition to their anti-diarrheal utility, possess a utility as potent analgesic agents.
Abstract: This invention encompasses novel 2-azabicyclo[2.2.2]-octan-2-yl-diphenyl-alkanones and related compounds. These compounds are useful as anti-diarrheal agents.
Abstract: This invention encompasses novel 5-[1,1-diphenyl-4-(cyclic amino)but-2-trans-en-1-yl]-2-alkyl-1,3,4-oxadiazoles and intermediates thereto. These compounds are useful anti-diarrheal agents.