Abstract: This invention relates to phenyl amidine alkanoic acids and lactones 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:
May 25, 1995
Date of Patent:
July 8, 1997
Assignee:
G. D. Searle & Co.
Inventors:
Norman Anthony Abood, Robert Everett Manning, Masateru Miyano
Abstract: The present invention relates to a novel process for the preparation of ethyl 3S-[[4-[[4-(aminoiminomethyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-pentyno ate and pharmaceutically acceptable acid addition salt thereof.
Type:
Grant
Filed:
May 14, 1996
Date of Patent:
May 20, 1997
Assignee:
G. D. Searle & Co.
Inventors:
Kevin A. Babiak, Srinivasan Babu, James R. Behling, Mark L. Boys, Kimberly J. Cain-Janicki, Wendel W. Doubleday, Payman Farid, Timothy J. Hagen, E. A. Hallinan, Donald W. Hansen, Jr., Donald E. Korte, Kathleen T. Mc Laughlin, John R. Medich, Sean T. Nugent, Vlasdislav Orlovski, Jung M. Park, Karen B. Peterson, Daniel R. Pilipauskas, Barnett S. Pitzele, Sofya Tsymbalov, Glenn L. Stahl
Abstract: This invention relates to phenyl amidine alkanoic acids and lactones 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:
May 26, 1995
Date of Patent:
March 18, 1997
Assignee:
G. D. Searle & Co.
Inventors:
Norman A. Abood, Robert E. Manning, Masateru Miyano
Abstract: This invention relates to compounds 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 amidines derivatives.
Type:
Grant
Filed:
March 24, 1995
Date of Patent:
September 3, 1996
Assignee:
G. D. Searle & Co.
Inventors:
Norman A. Abood, Robert B. Garland, Masateru Miyano
Abstract: This invention relates to a method of inhibiting platelet aggregation comprising administering compounds having the following formula ##STR1##
Type:
Grant
Filed:
October 28, 1994
Date of Patent:
August 6, 1996
Assignee:
G. D. Searle & Co.
Inventors:
Steven P. Adams, Richard J. Lindmark, Masateru Miyano, Joseph G. Rico
Abstract: The present invention relates to a novel process for the preparation of ethyl 3S-[[4-[[4-(aminoiminomethyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-pentyno ate and pharmaceutically acceptable acid addition salt thereof which comprises treating (trimethylsilyl)acetylene sequentially with n-butyllithium and 4-formylmorpholine followed by acid hydrolysis to give 3-(trimethylsilyl)-2-propynal; treating 3-(trimethylsilyl)-2-propynal with lithium bis(trimethylsilyl)amide to give in situ N,3-bis(trimethylsilyl)-2-propyn-1-imine; condensation of N,3-bis(trimethylsilyl)-2-propyn-1-imine with lithium t-butyl acetate to give (.+-.)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate; treating (.+-.)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate- with p-toluenesulfonic acid to give (.+-.)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate, mono p-toluenesulfonic acid salt, treatment of resulting salt with ethanol in the presence of p-toluenesulfonic acid to give (.+-.
Type:
Grant
Filed:
July 14, 1995
Date of Patent:
July 16, 1996
Assignee:
G. D. Searle & Co.
Inventors:
Kevin A. Babiak, Srinivasan Babu, James R. Behling, Mark L. Boys, Kimberly J. Cain-Janicki, Wendel W. Doubleday, Payman Farid, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Donald E. Korte, Kathleen T. McLaughlin, John R. Medich, Sean T. Nugent, Vlasdislav Orlovski, Jung M. Park, Karen B. Peterson, Daniel R. Pilipauskas, Barnett S. Pitzele, Sofya Tsymbalov, Glenn L. Stahl
Abstract: This invention relates to phenyl amidine alkanoic acids and lactones 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:
July 21, 1994
Date of Patent:
April 2, 1996
Assignee:
G. D. Searle & Co.
Inventors:
Norman A. Abood, Robert E. Manning, Masateru Miyano
Abstract: This invention relates to compounds having the following formula ##STR1## wherein Z is a lactone or a lactone which is fused to a benzene ring which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidines derivatives.
Type:
Grant
Filed:
May 25, 1994
Date of Patent:
August 15, 1995
Assignee:
G. D. Searle & Co.
Inventors:
Philippe R. Bovy, Thomas E. Rogers, Masateru Miyano, Joseph G. Rico
Abstract: This invention relates to compounds 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 amidines derivatives.
Type:
Grant
Filed:
December 19, 1991
Date of Patent:
June 13, 1995
Assignee:
G. D. Searle & Co.
Inventors:
Norman A. Abood, Robert B. Garland, Masateru Miyano
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:
October 29, 1992
Date of Patent:
May 24, 1994
Assignee:
G. D. Searle & Co.
Inventors:
Daniel P. Becker, Daniel L. Flynn, Clara I. Villamil
Abstract: The present invention relates to a class of compounds represented by the formula ##STR1## or a pharmaceutically acceptable salt thereof useful in the treatment of diseases or disorders mediated by platelet activating factor (PAF).
Type:
Grant
Filed:
November 6, 1992
Date of Patent:
April 12, 1994
Assignee:
G. D. Searle & Co.
Inventors:
Ish K. Khannal, Roger Nosal, Richard M. Weier, Kirk T. Lentz
Abstract: A process for the resolution of (.+-.)-.alpha.-[2-[acetyl(1-methylethyl)amino]ethyl-.alpha.-(2-chloropheny l)-1-piperidinebutanamide having the following structure ##STR1## into its (+) and (-) enantiomers using camphorsulfonic acid.
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 sulfones derivatives.
Type:
Grant
Filed:
February 14, 1992
Date of Patent:
November 23, 1993
Assignee:
G. D. Searle & Co.
Inventors:
Steven P. Adams, Joseph G. Rico, Masateru Miyano
Abstract: The present invention relates to pentanedioic acid derivatives. The present invention further relates to pharmaceutical compositions containing such compounds and the use of such compounds and compositions as hypolipidemic drugs.
Abstract: The present invention relates to a class of compounds represented by the formula ##STR1## or a pharmaceutically acceptable salt thereof useful in the treatment of diseases or disorders mediated by platelet activating factor (PAF).
Type:
Grant
Filed:
March 15, 1991
Date of Patent:
July 13, 1993
Assignee:
G. D. Searle & Co.
Inventors:
Ish K. Khanna, Roger Nosal, Richard M. Weier
Abstract: This invention relates to 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 amidines derivatives.
Type:
Grant
Filed:
November 12, 1991
Date of Patent:
June 15, 1993
Assignee:
G. D. Searle & Co.
Inventors:
Philippe R. Bovy, Dudley E. McMackins, Joseph G. Rico, Foe S. Tjoeng, Mihaly V. Toth, Robert B. Garland, Masateru Miyano, Jeffery A. Zablocki
Abstract: The invention relates to compound of the formula ##STR1## useful in regulating cardiac arrhythmias. This invention also relates to pharmaceutical compositions of the above-described compounds.
Abstract: The present invention relates to a class of 5-substituted-4-phenyl-5H-imidazo[4-phenyl-5H-imidazo[ 4,5-c]pyridines represented by the formula ##STR1## or a pharmaceutically acceptable salt thereof useful in the treatment of diseases or disorders mediated by platelet activating factor (PAF).
Abstract: A series of ethers and thioethers of 5-methanol thiohydantoins, unsubstituted at the number one position heterocyclic nitrogen atom of the thiohydantoin ring, useful in reversing the effects of collagen and ADP-induced platelet aggregation.
Type:
Grant
Filed:
May 30, 1989
Date of Patent:
August 11, 1992
Assignee:
G. D. Searle & Co.
Inventors:
John S. Baran, Tom Lindberg, Robert H. Mazur, Alan E. Moorman, Doug Steinman
Abstract: Cyanoguanidines which have activity as Class III antiarrhythmic agents, acting by prolonging cardiac action potential repolarization. The invention further provides for compositions incorporating the compounds and methods of their use, as well as providing for pharmaceutically acceptable salts of the compounds.