[go: up one dir, main page]

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

Info

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
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/EP2000/002850
Other languages
French (fr)
Other versions
WO2000059897A2 (en
Inventor
Gerrit Herman Veeneman
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Akzo Nobel NV
Original Assignee
Akzo Nobel NV
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 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
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Rheumatology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

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 Ceased 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 Ceased 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
WO2000061230A2 (en) * 1999-04-09 2000-10-19 Karo Bio Ab Estrogen receptors-beta antagonism and bone 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
US7354927B2 (en) 2004-09-07 2008-04-08 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
WO2000059897A2 (en) 2000-10-12
AU3964400A (en) 2000-10-23

Similar Documents

Publication Publication Date Title
EE200100246A (en) Novel ester derivatives of substituted phenylcyclohexyl compounds
DE69705829D1 (en) META-SUBSTITUTED PHENYLSULPHONAMIDE DERIVATIVES
HUP0204034A3 (en) Stable salts of novel derivatives of 3,3-diphenylpropylamines
DK1176195T3 (en) Method for controlling the activity of immunologically functional molecule
PL349036A1 (en) Quinoline derivatives and quinazoline derivatives
NO985293D0 (en) New 2,3-disubstituted-4 (3H) -quinazolinones
NO20100667L (en) Process for the preparation of intermediates of benzoxazine derivatives
EP1020452A4 (en) Benzimidazole derivatives
HK1044940A1 (en) Isoxazolecarboxamide derivatives
HUP0103144A3 (en) 2-(2-methylphenyl)-3,4-dihydro-2h-pyrrol derivatives
AU4787797A (en) Thienylcyclohexanone derivatives as ligands of the gabaa alpha5 receptor subtype
WO2000059897A3 (en) Esters and carbonates of 2-(4-hydroxyphenyl)-6(or 5)-hydroxy-benzothiophene derivatives as selective estrogenic compounds
WO2000005214A3 (en) Isoquinolines as urokinase inhibitors
FI922308A0 (en) SUBSTITUERADE OXOFTALAZINYLAETTIKS- SYROR OCH DERAS ANALOGER.
WO2002092602A3 (en) PROCESSES FOR THE SYNTHESIS OF DERIVATIVES OF 2,3-DIHYDRO-1,4-DIOXINO-[2,3-f] QUINOLINE
EP1031556A4 (en) 2-PHENOXYANILINE DERIVATIVES
FR2794169B1 (en) METHOD FOR CONTROLLING THE OPERATING CAPABILITY OF A CATALYTIC POT
DZ2607A1 (en) Process for the synthesis of pharmaceutically active quinoline derivatives.
EP1231215A4 (en) Process for the production of aspartyldipeptide ester derivatives, novel intermediates therefor and process for the production of the intermediates
HUP0103241A3 (en) New process for the synthesis of (1h)-benzo[c]quinolizin-3-ones derivatives
AU1394397A (en) Pyridine derivatives as fungicides
DE60009319D1 (en) SUBSTITUTED N-PHENYL-2-HYDROXY-2-METHYL-3,3,3-TRIFLUORPROPANAMIDE DERIVATIVE FOR INCREASING PYRUVATE DEHYDROGENASE ACTIVITY
AU9623698A (en) New 2-(3h)-oxazolone derivatives
EP1364945A4 (en) BENZIMIDAZOLIDINONE DERIVATIVES
IL124226A (en) Preparation of methyl 2-(2-methylphenyl)-3-methoxyacrylate by methoxymethylenation of methyl 2-methylphenylacetate

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AL AU BA BB BG BR CA CN CU CZ EE GE HR HU ID IL IN IS JP KP KR LC LK LR LT LV MG MK MN MX NO NZ PL RO RU SG SI SK SL TR TT UA US UZ VN YU ZA

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
AK Designated states

Kind code of ref document: A3

Designated state(s): AL AU BA BB BG BR CA CN CU CZ EE GE HR HU ID IL IN IS JP KP KR LC LK LR LT LV MG MK MN MX NO NZ PL RO RU SG SI SK SL TR TT UA US UZ VN YU ZA

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): GH GM KE LS MW SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: JP

DPE2 Request for preliminary examination filed before expiration of 19th month from priority date (pct application filed from 20040101)