Abstract: There is disclosed a pharmaceutical compound of the formula ##STR1## in which R.sup.1 is C.sub.7-20 alkyl, C.sub.7-20 alkenyl, or C.sub.7-20 alkynyl, the alkyl, alkenyl or alkynyl group being optionally substituted by phenyl or substituted phenyl, R.sup.2 is --CN, --COOR.sup.3 or ##STR2## wherein R.sup.3 is hydrogen or a protecting group, X is alkylene containing 1 to 6 carbon atoms and Y is a nitrogen-containing group selected from ##STR3## where each R.sup.4 independently is hydrogen or C.sub.1-4 alkyl; and salts thereof.
Type:
Grant
Filed:
April 18, 1988
Date of Patent:
November 6, 1990
Assignee:
Lilly Industries Limited
Inventors:
Stephen R. Baker, John Goldsworthy, William J. Ross
Abstract: Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 is hydrogen or C.sub.1-6 alkyl, R.sup.2 is hydrogen, C.sub.1-6 alkyl optionally substituted by C.sub.3-9 cycloalkyl or optionally substituted phenyl, C.sub.3-9 cycloalkyl, optionally substituted phenyl, or --SR.sup.4 where R.sup.4 is C.sub.1-6 alkyl optionally substituted by C.sub.3-9 cycloalkyl or optionally substituted phenyl, or C.sub.3-9 cycloalkyl, R.sup.3 is hydrogen, C.sub.1-6 alkyl optionally substituted by C.sub.3-9 cycloalkyl or optionally substituted phenyl, c.sub.3-9 cycloalkyl, or optionally phenyl, and either X and Y are both hydrogen or together are .dbd.O; and acid addition salts thereof. These compounds show useful effects on the central nervous system.
Type:
Grant
Filed:
December 7, 1989
Date of Patent:
October 16, 1990
Assignee:
Lilly Industries Limited
Inventors:
Terrence M. Hotten, Graham H. Timms, David E. Tupper
Abstract: There are described compounds of formula ##STR1## in which n is 0, 1 or 2, R.sup.1 is a hydrocarbyl group optionally substituted with an optionally substituted phenyl group and containing from 5 to 30 carbon atoms, R.sup.2 is optionally substituted phenyl or C.sub.1-10 alkyl optionally substituted by one or more substituents selected from optionally protected hydroxyl, optionally protected carboxyl, nitrile, optionally protected tetrazolyl, --COR.sup.6 where R.sup.6 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, an optionally protected amino acid residue or --NR.sub.2.sup.7 where each R.sup.7 is hydrogen or C.sub.1-4 alkyl, and --NHR.sup.8 where R.sup.8 is hydrogen, a protecting group, an optionally protected amino acid residue, C.sub.1-4 alkyl or --COR.sup.9 where R.sup.9 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy, and R.sup.3, R.sup.4 and R.sup.5 are each selected from hydrogen, carboxyl, C.sub.2-5 alkoxycarbonyl, C.sub.1-4 alkyl, C.sub.
Type:
Grant
Filed:
November 1, 1989
Date of Patent:
October 16, 1990
Assignee:
Lilly Industries Limited
Inventors:
Stephen R. Baker, William B. Jamieson, deceased, Alec Todd
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:
June 5, 1989
Date of Patent:
July 31, 1990
Assignee:
Eli Lilly and Company
Inventors:
Nancy G. Bollinger, Theodore Goodson, Jr., David K. Herron
Abstract: This invention provides certain 4-substituted benzamide derivatives, their pharmaceutical formulations, and their use as anticonvulsant agents.
Abstract: This invention provides (8.beta.)-N-cycloalkyl-1-alkyl-6-(substituted) ergoline-8-carboxamides useful for blocking 5HT.sub.2 receptors in mammals having an excess of serotonin centrally or peripherally. The invention also provides methods for treating hypertension, migraine, vasospasm, thrombosis, ischemia, depression, anxiety, sleep disorders and appetite disorders with a compound of the invention.
Type:
Grant
Filed:
August 14, 1989
Date of Patent:
June 5, 1990
Assignee:
Eli Lilly and Company
Inventors:
Mark M. Foreman, William L. Garbrecht, Gifford P. Marzoni, Kathleen R. Whitten
Abstract: This invention provides a method of treating or preventing cardiac arrhythmias employing certain 4-amino-N-2,6-(dimethylphenyl)benzamide derivatives.
Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.
Type:
Grant
Filed:
June 14, 1989
Date of Patent:
May 1, 1990
Assignee:
Eli Lilly and Company
Inventors:
Marlene L. Cohen, William B. Lacefield, David W. Robertson
Abstract: This invention provides for certain 2-phenylimidazo[4,5-c]pyridines, their pharmaceutical formulations, and their use as positive inotropic agents, bronchodilators, vasodilators, and anticoagulants.
Abstract: The present invention provides novel bicyclic derivatives useful as excitatory amino acid receptor antagonists and in treating a variety of associated nervous system disorders.
Abstract: This invention provides (8.beta.)-N-heteroalkyl-1-alkyl-6-(substituted)ergoline-8-carboxamides useful for blocking 5HT.sub.2 receptors in mammals having an excess of serotonin centrally or peripherally. The invention also provides methods for treating sexual dysfunction, hypertension, migraine, vasospasm, thrombosis, ischemia, depression, anxiety, sleep disorders and appetite disorders with a compound of the invention.
Abstract: The present invention provides novel piperazine derivatives useful as excitatory amino acid receptor antagonists and in treating a variety of associated nervous system disorders.
Abstract: Compounds of the following formula have pharmaceutical properties: ##STR1## in which X is R.sup.1 (HO)C.dbd.C(CN)--, R.sup.1 (CO)--CH(CN)-- or ##STR2## R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-6 alkyl, R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, hydroxy, halogen, nitro, cyano, carboxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halo-substituted C.sub.1-4 alkyl, halo-substituted C.sub.1-4 alkoxy, halo-substituted C.sub.1-4 alkylthio, C.sub.2-5 alkoxycarbonyl, optionally substituted phenyl, optionally substituted phenoxy, R'R"N- where R' and R" are each hydrogen or C.sub.1-4 alkyl R'"CONH-- where R'" is C.sub.1-4 alkyl, R.sup.6, R.sup.7 and R.sup.8 are each C.sub.1-6 alkyl, halo-substituted C.sub.1-6 alkyl or optionally substituted phenyl, or R.sup.6 and R.sup.7, together with the carbon atom to which they are attached, form a cycloalkyl group containing 3 to 7 carbon atoms, or R.sup.6, R.sup.7 and R.sup.
Type:
Grant
Filed:
August 7, 1987
Date of Patent:
January 9, 1990
Assignee:
Lilly Industries Limited
Inventors:
Peter T. Gallagher, Terence A. Hicks, Graham W. Mullier
Abstract: A pharmaceutical compound of the formula: ##STR1## in which R.sup.1 is C.sub.7-20 alkyl, C.sub.7-20 alkenyl or C.sub.7-20 alkynyl, the alkyl, alkenyl or alkynyl group being optionally substituted by phenyl or substituted phenyl and the alkenyl and alkynyl groups containing 1 to 3 unsaturated bonds, R.sup.2 is (i) optionally substituted phenyl, (ii) C.sub.1-10 alkyl optionally substituted by one or more substituents selected from optionally protected hydroxyl, optionally protected carboxyl, nitrile, optionally protected tetrazolyl, --COR.sup.4 where R.sup.4 is C.sub.1-14 alkyl, C.sub.1-4 alkoxy, an optionally protected amino acid residue or --NR.sub.2.sup.5 where each R.sup.5 is hydrogen or C.sub.1-4 alkyl, and --NHR.sup.6 where R.sup.6 is hydrogen, a protecting group, an optionally protected amino acid residue, C.sub.1-4 alkyl or --COR.sup.7 where R.sup.7 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy, or (iii) C.sub.1-10 alkyl substituted with a group selected from ##STR2## where each R.sup.8 is hydrogen or C.sub.
Abstract: This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
Type:
Grant
Filed:
April 10, 1987
Date of Patent:
October 17, 1989
Assignee:
Eli Lilly and Company
Inventors:
F. Patrick Carr, Robert D. Dillard, Doris E. McCullough
Abstract: A method of inhibiting superoxide release and reducing tissue damage following an inflammatory or ischemic event employing benzothiophenes, benzofurans, and naphthalenes is disclosed.
Abstract: This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
Type:
Grant
Filed:
April 13, 1987
Date of Patent:
August 1, 1989
Assignee:
Eli Lilly and Company
Inventors:
F. P. Carr, Robert D. Dillard, Doris E. McCullough
Abstract: There are described compounds of formula ##STR1## in which n is 0, 1 or 2, R.sup.1 is a hydrocarbyl group optionally substituted with an optionally substituted phenyl group and containing from 5 to 30 carbon atoms, R.sup.2 is optionally substituted phenyl or C.sub.1-10 alkyl optionally substituted by one or more substituents selected from optionally protected hydroxyl, optionally protected carboxyl, nitrile, optionally protected tetrazolyl, --COR.sup.6 where R.sup.6 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, an optionally protected amino acid residue or --NR.sub.2.sup.7 where each R.sup.7 is hydrogen or C.sub.1-4 alkyl, and --NHR.sup.8 where R.sup.8 is hydrogen, a protecting group, an optionally protected amino acid residue, C.sub.1-4 alkyl or --COR.sup.9 where R.sup.9 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy, and R.sup.3, R.sup.4 and R.sup.5 are each selected from hydrogen, carboxyl, C.sub.2-5 alkoxycarbonyl, C.sub.1-4 alkyl, C.sub.
Type:
Grant
Filed:
November 1, 1989
Date of Patent:
August 14, 1990
Assignee:
Eli Lilly and Company
Inventors:
Stephen R. Baker, William B. Jamieson, Alec Todd