Abstract: This invention encompasses methods for the treatment or prevention of a physiological disorder associated with an excess of tachykinins, said disorder being an allergy which method comprises administering to a mammal in need of said treatment an effective amount of a compound of Formula I ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamthylenemino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
Abstract: A method of inhibiting cell-cell adhesion comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
Abstract: A method of lowering serum cholesterol levels comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R is hydrogen; hydroxy; C.sub.1 -C.sub.6 alkoxy; a group of the formula --O--C(O)--R.sup.a, wherein R.sup.a is hydrogen, optionally substituted C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl optionally substituted with aryl, C.sub.3 -C.sub.7 cycloalkyl, optionally substituted aryl or R.sup.a is optionally substituted --O--aryl,or R is a group of the formula --O--SO.sub.2 --R.sup.b wherein R.sup.b may be C.sub.1 -C.sub.6 alkyl or optionally substituted aryl;or R is carbamoyloxy wherein the nitrogen may be substituted once or twice with C.sub.1 -C.sub.6 alkyl;or R is a group of the formula --O--C(O)R.sup.c --O--(C.sub.1 -C.sub.6 alkyl) wherein R.sup.c is a bond or C.sub.1 -C.sub.6 alkanediyl;R.sup.1 is halo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.7 alkyl substituted with C.sub.1 -C.sub.6 alkyl, substituted or unsubstituted C.sub.3 -C.sub.
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 of inhibiting uterine fibrosis comprising administering to a human in need of treatment an effective amount of a benzothiophene compound.
Abstract: A method of inhibiting bone loss or resorption, or lowering serum cholesterol, comprising administering to a human in need thereof a compound having the formula ##STR1## or a pharmaceutically acceptable salt or solvate thereof, in a low dosage amount. Also encompased by the invention is a a pharmaceutical formulation in unit dosage form comprising, per unit dosage, a low dosage amount.
Abstract: A method of increasing thrombomodulin expression comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidino, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR3## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidino, hexamethyleneimino, and piperidino; and pharmaceutically acceptable salts and solvates thereof.Also encompassed by the invention is a method of inhibiting a thrombotic disorder or event which includes administering to a human in need thereof an effective amount of a compound of formula 1.
Abstract: A group of 2-amino-3-aroyl-benzo[.beta.]thiophenes are prepared by treating an aldehyde with an anion of dimethylamino thioformamide, cyclizing the .alpha.-hydroxy thioamide, and subsequently acylating the benzo[.beta.]thiophene to yield the 2-amino-3-aryl derivative. These compounds may be treated with suitable phenyl Grignard reagents, and after deprotection, yield 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[.beta .]thiophene.
Abstract: A method of lowering serum cholesterol levels comprising administering to a patient a serum cholesterol lowering amount of a compound having the formula ##STR1## wherein n is 0, 1 or 2;R is hydroxyl, methoxy, C.sub.1 -C.sub.7 alkanoyloxy, C.sub.3 -C.sub.7 cycloalkanoyloxy, (C.sub.1 -C.sub.6 alkoxy)-C.sub.1 -C.sub.7 alkanoyloxy, substituted or unsubstituted aroyloxy, or substituted or unsubstituted aryloxycarbonyloxy;R.sup.1 is hydrogen, hydroxyl, chloro, bromo, methoxy, C.sub.1 -C.sub.7 alkanoyloxy, C.sub.3 -C.sub.7 cycloalkanoyloxy, (C.sub.1 -C.sub.6 alkoxy)-C.sub.1 -C.sub.7 alkanoyloxy, substituted or unsubstituted aroyloxy, or substituted or unsubstituted aryloxycarbonyloxy;R.sup.2 is a heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, or hexamethyleneimino; or a pharmaceutically acceptable salt or solvate thereof.
Type:
Grant
Filed:
November 30, 1993
Date of Patent:
November 7, 1995
Assignee:
Eli Lilly and Company
Inventors:
Larry J. Black, Henry U. Bryant, George J. Cullinan, Raymond F. Kauffman
Abstract: Methods of inhibiting vascular smooth muscle cell proliferation and restinosis are disclosed comprising administering to a human or other mammal in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sub.1 and R.sub.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sub.2 is ##STR3## and R.sub.4 is hydrogen or --OR.sub.1, and pharmaceutically acceptable salts and solvates thereof.
Type:
Grant
Filed:
April 14, 1995
Date of Patent:
October 31, 1995
Assignee:
Eli Lilly and Company
Inventors:
George J. Cullinan, Jai P. Singh, Dan L. Wood
Abstract: A method of inhibiting fertility in women comprising administering to a female human an effective amount of a compound having the formula ##STR1## and pharmaceutically acceptable salts and solvates thereof.
Abstract: A method of inhibiting atrophy of the skin or vagina comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
Abstract: A method of inhibiting endometriosis comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## Wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl;R.sup.2 is selected from the group consisting of pyrrolidine and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
Type:
Grant
Filed:
October 15, 1993
Date of Patent:
October 24, 1995
Assignee:
Eli Lilly and Company
Inventors:
Larry J. Black, George J. Cullinan, Michael W. Draper, Charles D. Jones, David E. Seyler
Abstract: The current invention provides a method useful for inhibiting the loss of bone using 6-hydroxy-2-(4-hydroxyphenyl)-benzo(B)thien-3-yl-4[2-(piperidin-1-ethoxyph enol]methanone hydrochloride.
Abstract: Methods of inhibiting vascular smooth muscle cell proliferation and vascular restinosis comprising administering to a human or other mammal in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sub.1 and R.sub.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sub.2 is ##STR3## R.sub.4 is hydrogen or --OR.sub.1, and pharmaceutically acceptable salts and solvates thereof.
Type:
Grant
Filed:
October 15, 1993
Date of Patent:
October 10, 1995
Assignee:
Eli Lilly and Company
Inventors:
George J. Cullinan, Jai P. Singh, Dan L. Wood
Abstract: A method of inhibiting uterine fibrosis comprising administering to a human or other mammal in need of treatment an effective amount of a compound having the formula ##STR1## Wherein R.sup.1 and R.sup.3 are independently hydrogen, ##STR2## wherein Ar is optionally substituted phenyl; wherein R.sup.2 is selected from the group consisting of pyrrolidino and piperidino, a pharmaceutically acceptable salt or solvate thereof.
Type:
Grant
Filed:
October 15, 1993
Date of Patent:
October 10, 1995
Assignee:
Eli Lilly and Company
Inventors:
Larry J. Black, George J. Cullinan, Michael W. Draper, Charles D. Jones, David E. Seyler
Abstract: 7.beta.-Amino-3-hydroxy-1-carba(1-dethia)-3-cephem-4-carboxylic acid esters are provided via cyclization of cis-3-(substituted amino)-1-(2-substituted 2-oxoethyl)-4-substituted azetidinones. The 7.beta.-amino-3-hydroxy-1-carba(1-dethia)-3-cephem-4-carboxylic acid esters are useful chiral intermediates to .beta.-lactam antibiotics.
Type:
Grant
Filed:
August 9, 1993
Date of Patent:
September 26, 1995
Assignee:
Eli Lilly and Company
Inventors:
James Aikins, John P. Gardner, Billy G. Jackson, John R. Rizzo, Eddie V. Tao
Abstract: A method of inhibiting ovarian dysgenesis, delayed puberty, or sexual infantilism comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.