Abstract: This invention relates to L-Arginine aldehyde derivatives, pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents.
Type:
Grant
Filed:
October 5, 1994
Date of Patent:
February 11, 1997
Assignee:
Eli Lilly and Company
Inventors:
Aaron L. Schacht, Robert T. Shuman, Gerald F. Smith, James H. Wikel, Michael R. Wiley
Abstract: The present invention provides a method of inhibiting gastric acid secretion in mammals by administering a 5-HT1A agonist compound or a pharmaceutically acceptable salt thereof.
Abstract: The present invention provides a method of inhibiting gastric acid secretion in mammals by administering a 5-HT1A agonist compound or a pharmaceutically acceptable salt thereof.
Abstract: This invention relates to L-arginine aldehyde derivatives, having the formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
Type:
Grant
Filed:
March 2, 1995
Date of Patent:
November 26, 1996
Assignee:
Eli Lilly and Company
Inventors:
Robert T. Shuman, Robert B. Rothenberger, Kenneth D. Kurz, Daniel J. Sall, Gerald F. Smith, Michael R. Wiley
Abstract: The present invention provides a method of inhibiting gastric acid secretion in mammals by administering a 5-HT1A agonist compound or a pharmaceutically acceptable salt thereof.
Abstract: The present invention provides a method for treating hyperglycemia in mammals by administering an antiestrogen compound and pharmaceutically acceptable salts and solvates thereof.
Abstract: This invention relates to hexa- and octahydrobenzo[f]quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.
Type:
Grant
Filed:
May 22, 1995
Date of Patent:
July 30, 1996
Assignee:
Eli Lilly and Company
Inventors:
James E. Audia, Kenneth S. Hirsch, Charles D. Jones, David E. Lawhorn, Loretta A. McQuaid, Leland O. Weigel
Abstract: This invention relates to L-Arginine aldehyde derivatives, pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents.
Abstract: The present invention relates to sulfonate derivatives of 3-aroylbenzo[b]thiophenes, pharmaceutical formulations containing these compounds and methods of using such compounds for inhibiting the loss of bone, lowering serum cholesterol levels and therapeutically treating hormone dependent mammalian breast and uterine carcinoma.
Type:
Grant
Filed:
March 19, 1993
Date of Patent:
January 9, 1996
Assignee:
Eli Lilly and Company
Inventors:
Larry J. Black, Henry U. Bryant, George J. Cullinan
Abstract: A method for the recombinant production of forms of human protein C with higher activity is described. These forms differ from native protein C in their increased amidolytic and functional activities and novel carbohydrate structures. DNA compounds, vectors, and transformants useful in the method are also disclosed.
Abstract: The present invention provides a method of inhibiting gastric acid secretion in mammals by administering a 5-HT1A agonist compound or a pharmaceutically acceptable salt thereof.
Abstract: Human protein C derivatives with high activity and reduced dependence on thrombin activation are described. These derivatives differ from the native forms of human protein C in their increased activation rates, functional activities and carbohydrate structures. DNA compounds, transfer vectors, expression vectors and transformants useful in producing these derivatives are also described.
Abstract: This invention relates to bisulfite adducts of L-Arginine aldehyde derivatives, pharmaceutical formulations containing those adducts and methods of their use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents.
Type:
Grant
Filed:
March 4, 1994
Date of Patent:
July 25, 1995
Assignee:
Eli Lilly and Company
Inventors:
Kenneth J. Ruterbories, Robert T. Shuman
Abstract: Thrombin inhibitors represented by the formula ##STR1## as provided wherein A(C.dbd.O)-- is, inter alia, phenylglycyl, cyclohexylglycyl, cyclohexenylglycyl, thienylglycyl or naphthylglycyl, wherein the .alpha.-amino group is preferably substituted by alkyl e.g. methyl or an alkoxycarbonyl, cycloalkoxycarbonyl or arylkoxycarbonyl group e.g. t-butyloxycarbonyl. A(C.dbd.O)-- also represents an .alpha.-substituted acetyl group such as .alpha.-methoxyphenylacetyl; or a bicyclic group such as a tetrahydroisoquinolin-1- or 3-carbonyl group; a perhydroisoquinolin -1- or -3-carbonyl group; or a 1-amino or (substituted amino) cycloalkylcarbonyl group such as 1-aminocyclohexylcarbonyl. Also provided are a method for inhibiting the formation of blood clots in man and animals by administering a thrombin inhibitor of the above formula and pharmaceutical formulations useful in the method.
Abstract: The present invention relates to the use of certain ergoline analogues and BCD tricyclic ergoline part-structure analogues as defined herein as anti-inflammatory agents.
Type:
Grant
Filed:
December 8, 1992
Date of Patent:
May 16, 1995
Assignee:
Eli Lilly and Company
Inventors:
Alison M. Bendele, Henry U. Bryant, John M. Schaus
Abstract: This invention provides 1,2,4-trioxygenated benzene derivatives which are leukotriene B.sub.4 antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
Abstract: The present invention provides a method of inhibiting gastric acid secretion in mammals by administering a 5-HT1A agonist compound or a pharmaceutically acceptable salt thereof.
Abstract: This invention provides benzene derivatives, pharmaceutical formulations of those derivatives, and a method of using the derivatives for the treatment of inflammation in mammals.
Type:
Grant
Filed:
February 7, 1992
Date of Patent:
March 15, 1994
Assignee:
Eli Lilly and Company
Inventors:
Nancy G. Bollinger, Theodore Goodson, Jr., David K. Herron
Abstract: This invention relates to N-hydroxy-N-[3-[2-(4'-halophenylthio)phenyl]prop-2-enyl]ureas, formulations containing those compounds and methods of using such compounds as 5-lipoxygenase inhibiting agents.
Type:
Grant
Filed:
April 8, 1992
Date of Patent:
February 1, 1994
Assignee:
Eli Lilly and Company
Inventors:
Gary A. Hite, Edward D. Mihelich, David W. Snyder, Tulio Suarez
Abstract: A compound of the formula ##STR1## in which R.sup.1 is hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitrile, optionally protected carboxy, optionally protected tetrazolyl, trihalomethyl, hydroxy-C.sub.1-4 alkyl, aldehydo, --CH.sub.2 Z, --CH.dbd.CH--Z or --CH.sub.2 CH.sub.2 Z where Z is optionally protected carboxy or optionally protected tetrazolyl; R.sup.2 is halo, nitrile, an optionally protected acid group or --CONR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are each hydrogen or C.sub.1-4 alkyl; R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl, or C.sub.1-4 alkyl substituted by --CONR.sup.7 R.sup.8 or an optionally protected acid group; R.sup.5 is ##STR2## where W is --CH.dbd.CH--, --CH.dbd.N--, --N.dbd.CH--, --O-- or --S--, R.sup.9 is hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trihalomethyl, and R.sup.10 is hydrogen, C.sub.1-4 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.1-4 alkyl-C.sub.3-6 cycloalkyl; R.sup.6 is hydrogen or C.sub.