WO2000059897A3 - Esters and carbonates of 2-(4-hydroxyphenyl)-6(or 5)-hydroxy-benzothiophene derivatives as selective estrogenic compounds - Google Patents

Esters and carbonates of 2-(4-hydroxyphenyl)-6(or 5)-hydroxy-benzothiophene derivatives as selective estrogenic compounds Download PDF

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Publication number
WO2000059897A3
WO2000059897A3 PCT/EP2000/002850 EP0002850W WO0059897A3 WO 2000059897 A3 WO2000059897 A3 WO 2000059897A3 EP 0002850 W EP0002850 W EP 0002850W WO 0059897 A3 WO0059897 A3 WO 0059897A3
Authority
WO
WIPO (PCT)
Prior art keywords
ester
hydroxyphenyl
carbonates
hydroxy
esters
Prior art date
Application number
PCT/EP2000/002850
Other languages
French (fr)
Other versions
WO2000059897A2 (en
Inventor
Gerrit Herman Veeneman
Original Assignee
Akzo Nobel Nv
Gerrit Herman Veeneman
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Akzo Nobel Nv, Gerrit Herman Veeneman filed Critical Akzo Nobel Nv
Priority to AU39644/00A priority Critical patent/AU3964400A/en
Publication of WO2000059897A2 publication Critical patent/WO2000059897A2/en
Publication of WO2000059897A3 publication Critical patent/WO2000059897A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/56—Radicals substituted by oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32—Antioestrogens

Abstract

Disclosed are compounds satisfying structural formula (I) wherein one of R5 or R6 is OR7 and the other is H; R4 and R7 each independently is an ester or a carbonate of lower alkyl, alkenyl or alkynyl, or a benzoyl ester, each optionally substituted with halogen, lower alkyl, methoxy, NO2, CN, CF3; an alkylsulphonyl ester, or an arylsulphonyl ester; or one of R4 and R7 is H; R2, R2', R3, R3' each independently are H, halogen, lower alkyl, lower alkenyl, alkynyl, aryl, methylthio, methoxy, dimethyl amino, NO2, CN, alkyl carbonyl, or CF3; or wherein R2 and R3 form a ring system. The resulting compounds have a desirable selective agonistic profile for estrogen receptor β.
PCT/EP2000/002850 1999-04-06 2000-03-31 Esters and carbonates of 2-(4-hydroxyphenyl)-6(or 5)-hydroxy-benzothiophene derivatives as selective estrogenic compounds WO2000059897A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU39644/00A AU3964400A (en) 1999-04-06 2000-03-31 Selective estrogenic compounds

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP99201071 1999-04-06
NL99201071.0 1999-04-06

Publications (2)

Publication Number Publication Date
WO2000059897A2 WO2000059897A2 (en) 2000-10-12
WO2000059897A3 true WO2000059897A3 (en) 2001-04-05

Family

ID=8240067

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2000/002850 WO2000059897A2 (en) 1999-04-06 2000-03-31 Esters and carbonates of 2-(4-hydroxyphenyl)-6(or 5)-hydroxy-benzothiophene derivatives as selective estrogenic compounds

Country Status (2)

Country Link
AU (1) AU3964400A (en)
WO (1) WO2000059897A2 (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1165184E (en) * 1999-04-09 2004-04-30 Karobio Ab ANTAGONISM OF ESTROGEN'S RECEPTOR-BETA AND BONES DISEASES
UA83620C2 (en) 2001-12-05 2008-08-11 Уайт Substituted benzoxazoles and analogues as estrogenic agents
US6884814B2 (en) 2001-12-13 2005-04-26 Wyeth Phenyl benzisoxazoles as estrogenic agents
US6835745B2 (en) 2002-01-15 2004-12-28 Wyeth Phenyl substituted thiophenes as estrogenic agents
AU2005282554A1 (en) 2004-09-07 2006-03-16 Wyeth 6H-[1]benzopyrano[4,3-b]quinolines and their use as estrogenic agents

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0729956A1 (en) * 1995-02-28 1996-09-04 Eli Lilly And Company Benzothiophene compounds, intermediates, compositions, and methods
EP0832888A1 (en) * 1996-09-27 1998-04-01 Eli Lilly And Company Benzothiophene compounds, compositions, and methods
US5760030A (en) * 1997-06-30 1998-06-02 Eli Lilly And Company Benzothiophene compounds and methods of use
US5843940A (en) * 1996-10-24 1998-12-01 Eli Lilly And Company Benzothiophene compounds, compositions, and method
WO1998056812A2 (en) * 1997-06-10 1998-12-17 Karo Bio Ab Estrogen receptor crystals and ligands
EP0963981A1 (en) * 1998-06-12 1999-12-15 Galderma Research & Development, S.N.C. Biaryl heterocyclic aromatic compounds, pharmaceutical and cosmetic compositions containing them and uses thereof

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0729956A1 (en) * 1995-02-28 1996-09-04 Eli Lilly And Company Benzothiophene compounds, intermediates, compositions, and methods
EP0832888A1 (en) * 1996-09-27 1998-04-01 Eli Lilly And Company Benzothiophene compounds, compositions, and methods
US5843940A (en) * 1996-10-24 1998-12-01 Eli Lilly And Company Benzothiophene compounds, compositions, and method
WO1998056812A2 (en) * 1997-06-10 1998-12-17 Karo Bio Ab Estrogen receptor crystals and ligands
US5760030A (en) * 1997-06-30 1998-06-02 Eli Lilly And Company Benzothiophene compounds and methods of use
EP0963981A1 (en) * 1998-06-12 1999-12-15 Galderma Research & Development, S.N.C. Biaryl heterocyclic aromatic compounds, pharmaceutical and cosmetic compositions containing them and uses thereof

Also Published As

Publication number Publication date
AU3964400A (en) 2000-10-23
WO2000059897A2 (en) 2000-10-12

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