Patent number: 6444688
Abstract: The instant invention provides compounds of formula I
wherein
R1 is OH, O—C(O)—(C1-C6 alkyl), O—C(O)—O(C1-C6 alkyl), O—C(O)—Ar, or O—C(O)—O—Ar;
R2 is H, OH, O(C1-C6 alkyl), O—C(O)—(C1-C6 alkyl), O—C(O)—O(C1-C6 alkyl), O—C(O)—Ar, O—C(O)—O—Ar, O—SO2—(C4-C6 alkyl), chloro, fluoro, or bromo;
V is S, O, or CH2CH2;
W is CHOH, C(O), or CH2;
X is (CH2)n;
R3 and R4 each, independently, are H, C1-C6 alkyl, C(O)—(C1-C6 alkyl), C(O)—NH—(C1-C6 alkyl), C(O)—Ar, or together with the nitrogen to which they are attached form a 5- or 6-membered imide or cyclic amide;
n is 1, 2, or 3; and
Ar is optionally substituted phenyl;
povided that at least one of R3 and R4 contains a carbonyl functional group, and their use in the treatment of estrogen deficiency pathologies.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
September 3, 2002
Assignee:
Eli Lilly and Company
Inventors:
Jeffrey A. Dodge, Charles D. Jones, Kristin Marron, James P. Sluka, Mark G. Stocksdale
Patent number: 6432982
Abstract: The invention provides novel benzothiophenes of the formula:
wherein R1 is —H, —OH, —O(C1-C4 alkyl), —O—CO(C1-C6 alkyl), —OSO2(C4-C6 alkyl, or —OCOAr where Ar is optionally substituted phenyl; R2 is —H, —OH, —Cl, —Br, —O(C1-C4 alkyl), —OCO(C1-C6 alkyl), —OSO2(C4-C6 alkyl, or —OCOAr where Ar is optionally substituted phenyl; R3 is —H, —F, —Cl, —(C1-C4 alkyl), —CN, or —O(C1-C3 alkyl); R4 is —H, —F, —Cl, —(C1-C4 alkyl), —CN or —O(C1-C3 alkyl); R5 is —H, —F, —Cl, —(C1-C4 alkyl), or —O(C1-C3 alkyl); and R6 is —H, —F, —Cl, —(C1-C4 alkyl), or —O(C1-C3 alkyl); with the provisos that R3, R4, R5 and R6 can not all be hydrogen, and that when one of R3, R4, R5 or R6 is C1-C4 alkyl, no more than two of R3, R4, R5 and R6 can be hydrogen; Y is —CO—, —CHOH—, or &mda
Type:
Grant
Filed:
January 14, 1997
Date of Patent:
August 13, 2002
Assignee:
Eli Lilly and Company
Inventors:
George Joseph Cullinan, Kennan Joseph Fahey
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