DE69724548T2 - Substituierte 2,3-Aryl-Benzothiophene und ihre östrogene Aktivität - Google Patents

Substituierte 2,3-Aryl-Benzothiophene und ihre östrogene Aktivität Download PDF

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Publication number
DE69724548T2
DE69724548T2 DE69724548T DE69724548T DE69724548T2 DE 69724548 T2 DE69724548 T2 DE 69724548T2 DE 69724548 T DE69724548 T DE 69724548T DE 69724548 T DE69724548 T DE 69724548T DE 69724548 T2 DE69724548 T2 DE 69724548T2
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DE
Germany
Prior art keywords
compound
formula
alkyl
medication
manufacture
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.)
Expired - Fee Related
Application number
DE69724548T
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German (de)
English (en)
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DE69724548D1 (de
Inventor
George Joseph Trafalgar Cullinan
Brian Stephen Indianapolis Muehl
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.)
Eli Lilly and Co
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Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of DE69724548D1 publication Critical patent/DE69724548D1/de
Application granted granted Critical
Publication of DE69724548T2 publication Critical patent/DE69724548T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/02Nutrients, e.g. vitamins, minerals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/56Radicals substituted by oxygen atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Nutrition Science (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)
DE69724548T 1996-10-24 1997-10-22 Substituierte 2,3-Aryl-Benzothiophene und ihre östrogene Aktivität Expired - Fee Related DE69724548T2 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US2905096P 1996-10-24 1996-10-24
US29050P 1996-10-24

Publications (2)

Publication Number Publication Date
DE69724548D1 DE69724548D1 (de) 2003-10-09
DE69724548T2 true DE69724548T2 (de) 2004-08-05

Family

ID=21846947

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69724548T Expired - Fee Related DE69724548T2 (de) 1996-10-24 1997-10-22 Substituierte 2,3-Aryl-Benzothiophene und ihre östrogene Aktivität

Country Status (7)

Country Link
US (2) US5843940A (enExample)
EP (1) EP0838461B1 (enExample)
JP (1) JPH10130260A (enExample)
AT (1) ATE248830T1 (enExample)
CA (1) CA2214872C (enExample)
DE (1) DE69724548T2 (enExample)
ES (1) ES2205133T3 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000059897A2 (en) * 1999-04-06 2000-10-12 Akzo Nobel N.V. Esters and carbonates of 2-(4-hydroxyphenyl)-6(or 5)-hydroxy-benzothiophene derivatives as selective estrogenic compounds
US7091199B1 (en) 1999-09-14 2006-08-15 Aventis Pharmaceuticals Inc. Thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives useful as d4 antagonists
US7253165B2 (en) * 1999-09-14 2007-08-07 Aventis Pharmaceuticals Inc. Benzisoxazolyl-, pyridoisoxazolyl-and benzthienyl-phenoxy derivatives useful as D4 antagonists
US7125903B1 (en) 1999-09-14 2006-10-24 Aventis Pharmaceuticals Inc. Thienoisoxazolyl-and thienylpyrrazolyl-phenoxy substituted propyl derivatives useful as D4 antagonists
AUPR283801A0 (en) * 2001-02-01 2001-03-01 Australian National University, The Chemical compounds and methods
GR1005694B (el) * 2005-06-08 2007-10-22 Αλεξης Μιχαηλ Ιστοειδικα αντιοιστρογονα ειδικα για τον αλφα υποδοχεα των οιστρογονων
US11058695B2 (en) * 2019-11-08 2021-07-13 Myongji University Industry And Academia Cooperation Foundation Inhibitor of carbapenem-hydrolyzing class D beta-lactamases

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3274213A (en) * 1961-09-05 1966-09-20 Upjohn Co Alkoxy-substituted 2-phenyl-1-(tertiary-aminoalkoxy)phenyl-3, 4-dihydronaphthalenes
DE1300575B (de) * 1965-05-21 1969-08-07 Bristol Myers Co Benzo[b]thiophene
US3394125A (en) * 1965-10-23 1968-07-23 Bristol Myers Co 2-phenyl-3-tertiary-aminoalkoxy phenyl-and corresponding tertiaryaminoalkyl thio benzfurans substituted in the benzo nucleus with an alkoxy or tertiaryamino alkoxy or alkylthio group
US4230862A (en) * 1975-10-28 1980-10-28 Eli Lilly And Company Antifertility compounds
US4133814A (en) * 1975-10-28 1979-01-09 Eli Lilly And Company 2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents
US4380635A (en) * 1981-04-03 1983-04-19 Eli Lilly And Company Synthesis of acylated benzothiophenes
US4418068A (en) * 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes
GB2097788B (en) * 1981-04-03 1985-04-24 Lilly Co Eli Benzothiophene compounds and process for preparing them
US4358593A (en) * 1981-04-03 1982-11-09 Eli Lilly And Company Process for preparing 3-(4-aminoethoxybenzoyl)benzo[b]thiophenes
JPH02501301A (ja) * 1987-09-25 1990-05-10 チバ‐ガイギー アクチェンゲゼルシャフト 4‐(トリアルキルベンジル)‐ピペラジニル化合物のジアシル誘導体
US5395842A (en) * 1988-10-31 1995-03-07 Endorecherche Inc. Anti-estrogenic compounds and compositions
DE4117512A1 (de) * 1991-05-25 1992-11-26 Schering Ag 2-phenylbenzo(b)furane und -thiophene, verfahren zu deren herstellung und diese enthaltende pharmazeutische praeparate
US5147880A (en) * 1991-07-22 1992-09-15 Eli Lilly And Company Benzo[a]fluorene compounds
JP3157882B2 (ja) * 1991-11-15 2001-04-16 帝国臓器製薬株式会社 新規なベンゾチオフエン誘導体
US5354861A (en) * 1992-11-04 1994-10-11 National University Of Singapore 2-(benzyl)-3-arylbenzofurans as antitumour and hypocholesterolemic agents
US6756388B1 (en) * 1993-10-12 2004-06-29 Pfizer Inc. Benzothiophenes and related compounds as estrogen agonists
US7501441B1 (en) * 1994-09-20 2009-03-10 Eli Lilly And Company Naphthyl compounds, intermediates, processes, compositions, and methods
US5492921A (en) * 1994-09-20 1996-02-20 Eli Lilly And Company Benzothiophene compounds, compositions, and methods for inhibiting aortal smooth muscle proliferation
US5552401A (en) * 1995-02-28 1996-09-03 Eli Lilly And Company 2-benzyl-3-arylbenzothiophenes

Also Published As

Publication number Publication date
EP0838461A2 (en) 1998-04-29
CA2214872C (en) 2002-01-22
EP0838461B1 (en) 2003-09-03
ES2205133T3 (es) 2004-05-01
US5843940A (en) 1998-12-01
DE69724548D1 (de) 2003-10-09
ATE248830T1 (de) 2003-09-15
US6121293A (en) 2000-09-19
EP0838461A3 (en) 1998-05-06
CA2214872A1 (en) 1998-04-24
JPH10130260A (ja) 1998-05-19

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8339 Ceased/non-payment of the annual fee