Abstract: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, --CH.dbd.CH--, or --CH.dbd.N--;wherein R.sup.1 is --CO.sub.2 R.sup.2 or tetrazole;wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbons or a pharmaceutically acceptable cation;wherein R is an alkyl of from 1 to 20 carbons, --(CH.sub.2).sub.p CF.sub.3 or --(CH.sub.2).sub.q R.sup.3 wherein R.sup.3 is alkoxy, phenoxy or alkoxy substituted phenoxy wherein the alkoxy group has from 1 to 8 carbons;wherein p and q are integers from 0 to 20;wherein n is 0 or 1; andwherein m is 0, 1, 2, or 3.
Type:
Grant
Filed:
July 1, 1994
Date of Patent:
April 16, 1996
Assignee:
G. D. Searle & Co.
Inventors:
Stevan W. Djuric, Richard A. Haack, Julie M. Miyashiro
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: The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
Type:
Grant
Filed:
February 22, 1995
Date of Patent:
April 2, 1996
Assignee:
G. D. Searle & Co.
Inventors:
Joe T. Collins, Donald W. Hansen, Jr., Karen H. Peterson, Barnett S. Pitzele, David B. Reitz
Abstract: This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.
Type:
Grant
Filed:
March 30, 1995
Date of Patent:
February 6, 1996
Assignee:
G. D. Searle & Co.
Inventors:
Philippe R. Bovy, Joseph G. Rico, Thomas E. Rogers
Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and as prostaglandin-E.sub.2 antagonists for the treatment of prostaglandin-E.sub.2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal, and a method for treating prostaglandin-E.sub.2 mediated diseases in an animal, comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
Type:
Grant
Filed:
November 3, 1993
Date of Patent:
January 30, 1996
Assignee:
G. D. Searle & Co.
Inventors:
Robert A. Chrusciel, Timothy J. Hagen, E. Ann Hallinan, Jinglin Li, Sofya Tsymbalov, David B. Reitz
Abstract: The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
January 16, 1996
Assignee:
G. D. Searle & Co.
Inventors:
Norman A. Abood, Daniel L. Flynn, Scott A. Laneman, Roger Nosal, Lori A. Schretzman
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 derivatives of cyclic phenolic thioethers of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, which are inhibitors or stimulators of superoxide generation, and which may also inhibit cyclooxygenase and/or 5-lipoxygenase, to pharmaceutical compositions containing one or more of these compounds in combination with a pharmaceutically-acceptable carrier, and to medical methods of treatment employing these compounds.
Type:
Grant
Filed:
May 19, 1994
Date of Patent:
December 19, 1995
Assignee:
G. D. Searle & Co.
Inventors:
Richard A. Partis, Richard A. Mueller, Francis J. Koszyk, Richard M. Weier
Abstract: Novel urea compounds are provided which inhibit platelet aggregation as well as pharmaceutical compositions and methods of using said compounds.
Type:
Grant
Filed:
February 23, 1994
Date of Patent:
December 12, 1995
Assignee:
The Monsanto Company
Inventors:
Foe S. Tjoeng, Mihaly V. Toth, Dudley E. McMackins, Steven P. Adams
Abstract: The present invention provides dibenzoxazepine compounds, of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
Type:
Grant
Filed:
August 24, 1994
Date of Patent:
November 7, 1995
Assignee:
G. D. Searle & Co.
Inventors:
E. Ann Hallinan, Timothy J. Hagen, Robert K. Husa, Sofya Tsymbalov, Albert C. Lee, Jean-Pierre Van Hoeck
Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
Type:
Grant
Filed:
September 24, 1993
Date of Patent:
October 24, 1995
Assignee:
G. D. Searle & Co.
Inventors:
Robert K. Husa, Michael F. Rafferty, Timothy J. Hagen, E. Ann Hallinan
Abstract: The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and for prostaglandin-E.sub.2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal, and a method for treating prostaglandin-E.sub.2 mediated diseases in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
Type:
Grant
Filed:
May 18, 1994
Date of Patent:
October 24, 1995
Assignee:
G. D. Searle & Co.
Inventors:
Donald W. Hansen, Jr., Karen B. Peterson
Abstract: This invention relates to compounds having the following formula ##STR1## or pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.
Type:
Grant
Filed:
October 15, 1993
Date of Patent:
September 26, 1995
Assignee:
G. D. Searle & Co.
Inventors:
Philippe R. Bovy, Robert B. Garland, Masateru Miyano, Joseph G. Rico, Thomas E. Rogers, Jeffery A. Zablocki
Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
Type:
Grant
Filed:
January 10, 1994
Date of Patent:
September 12, 1995
Assignee:
G. D. Searle & Co.
Inventors:
Nizal S. Chandrakumar, Timothy J. Hagen, E. Ann Hallinan, Robert K. Husa
Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
Type:
Grant
Filed:
March 3, 1994
Date of Patent:
September 12, 1995
Assignee:
G. D. Searle & Co.
Inventors:
Timothy J. Hagen, Nizal S. Chandrakumar, E. Ann Hallinan, Shashidhar N. Rao, Barnett S. Pitzele
Abstract: The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
Type:
Grant
Filed:
June 9, 1994
Date of Patent:
September 12, 1995
Assignee:
G. D. Searle & Co.
Inventors:
Nizal S. Chandrakumar, Donald W. Hansen, Jr., Karen B. Peterson, Barnett S. Pitzele
Abstract: This invention relates to methods of treating conditions responsive to 5-HT.sub.4 agonists and/or antagonists and 5-HT.sub.3 antagonists by administering compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein Z is selected from the group consisting of ##STR2## R.sub.1 is alkoxy of one to six carbon atoms; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are selected from the group consisting of hydrogen, halogen, CF.sub.3, hydroxy, alkoxy of one to six carbon atoms, acyl of two to seven carbon atoms, amino, amino substituted by one or two alkyl groups of one to six carbon atoms, C.sub.2 -C.sub.7 acylamino, aminocarbonyl, aminosulfone optionally substituted by one or two alkyl groups of one to six carbon atoms, C.sub.1 -C.sub.6 alkylsulfone and nitro;n is 0, 1 or 2;m is 0 or 1;X is O or NR.sub.7 ; andR.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms.
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: The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
Type:
Grant
Filed:
June 9, 1994
Date of Patent:
August 15, 1995
Assignee:
G. D. Searle & Co.
Inventors:
Joe T. Collins, Donald W. Hansen, Jr., Karen B. Peterson, Barnett S. Pitzele, David B. Reitz
Abstract: An azatetracycle compound useful as 5HT.sub.3 antagonists of the general formula ##STR1## wherein D is a tetracycle of the structure ##STR2## wherein Ar is an aromatic moiety and B is either NH or O.
Type:
Grant
Filed:
August 18, 1994
Date of Patent:
April 23, 1996
Assignee:
G. D. Searle & Co.
Inventors:
Daniel P. Becker, Daniel L. Flynn, Roger Nosal, Dale P. Spangler, Daniel L. Zabrowski