EP0617030A1
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Sulfonate and carbamate derivatives of 3-aroylbenzo (beta) thiophenes
Assignee: Eli Lilly and Co
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Filing: 1994-03-16
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Granted: —
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Expires: 2014-03-16
Abstract
Abstract The present invention relates to sulfonate and carbamate 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.
Inventors
- 👤 Larry John Black
- 👤 Henry Uhlman Bryant
- 👤 George Joseph Cullinan
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-03 18:17
CPC Classifications
C; C07; C07D; C07D333/00; C07D333/50; C07D333/52; C07D333/54; C07D333/56; A; A61; A61P; A61P19/00; A61P19/08; A61P19/10; A61P3/00; A61P3/06; A61P35/00; A61P37/00; A61P37/08; A61P43/00; A61P9/00; A61P9/10
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
92 words
A compound of the formula where X is a bond or -CH₂-; R² is a heterocyclic ring selected from pyrrolidino, piperidino or hexamethyleneimino; R is OH -OSO₂-(CH₂) n -CH₃ or R¹ is hydrogen, OH, fluoro, chloro, -OSO₂-(CH₂) n -CH₃ or each R³ is independently C₁-C₆ alkyl, C₃-C₆ cycloalkyl, unsubstituted or substituted phenyl where the substituent is fluoro, chloro, C₁-C₃ alkyl or C₁-C₃ alkoxy; each n is independently 3, 4 or 5; and pharmaceutically acceptable salts and solvates thereof; provided that at least one of R and R¹ is -OSO₂-(CH₂) n -CH₃ or
Claim 2
Dependent Claim
13 words
A compound of Claim 1 where R² is a pyrrolidino or piperidino ring.
Claim 3
Dependent Claim
18 words
A compound of Claim 1 where R is -OSO₂-(CH₂) n -CH₃ and n is 3, 4 or 5.
Claim 4
Dependent Claim
23 words
A compound of Claim 3 where R¹ is hydrogen, OH, chloro, fluoro or -OSO₂-(CH₂) n -CH₃ and n is 3, 4 or 5.
Claim 5
Dependent Claim
26 words
A compound of Claim 1 where R² is a piperidino ring; R and R¹ are -OSO₂-(CH₂) n -CH₃; and each n is independently 3 or 4.
Claim 6
Dependent Claim
17 words
A compound of Claim 5 which is [6-(n-butylsulfonoyl)-2-[4-(n-butylsulfonoyl)phenyl]benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]-phenyl] methanone or a pharmaceutically acceptable salt or solvate thereof.
Claim 7
Dependent Claim
17 words
A compound of Claim 5 which is [6-(n-pentylsulfonoyl)-2-[4-(n-pentylsulfonoyl)phenyl]benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]-phenyl] methanone or a pharmaceutically acceptable salt or solvate thereof.
Claim 8
Dependent Claim
29 words
A pharmaceutical formulation comprising as an active ingredient a compound as claimed is any one of claims 1 to 7, associated with one or more pharmaceutically acceptable carriers therefor.
Claim 9
Dependent Claim
17 words
A compound as claimed in any of claims 1 to 7 for use in inhibiting bone loss.
Claim 10
Dependent Claim
16 words
A compound of any of claims 1 to 7 for use in lowering serum cholesterol levels.
Claim 11
Dependent Claim
17 words
A compound of any of claims 1 to 7 for treating hormone dependent breast or uterine carcinoma.
References Cited (Backward Citations)
US4133814A
Cited
US4418068A
Cited
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