SI0729956T1 - Benzothiophene compounds, intermediates, compositions, and methods - Google Patents

Benzothiophene compounds, intermediates, compositions, and methods

Info

Publication number
SI0729956T1
SI0729956T1 SI9630423T SI9630423T SI0729956T1 SI 0729956 T1 SI0729956 T1 SI 0729956T1 SI 9630423 T SI9630423 T SI 9630423T SI 9630423 T SI9630423 T SI 9630423T SI 0729956 T1 SI0729956 T1 SI 0729956T1
Authority
SI
Slovenia
Prior art keywords
intermediates
compositions
methods
benzothiophene compounds
benzothiophene
Prior art date
Application number
SI9630423T
Other languages
English (en)
Slovenian (sl)
Inventor
Alan David Palkowitz
Kenneth Jeff Thrasher
Original Assignee
Eli Lilly And Company
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
Priority claimed from US08/396,401 external-priority patent/US5510357A/en
Priority claimed from US08/552,564 external-priority patent/US5998441A/en
Priority claimed from US08/552,565 external-priority patent/US5977093A/en
Priority claimed from US08/552,890 external-priority patent/US5919800A/en
Priority claimed from US08/552,679 external-priority patent/US5856339A/en
Application filed by Eli Lilly And Company filed Critical Eli Lilly And Company
Publication of SI0729956T1 publication Critical patent/SI0729956T1/xx

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
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic 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
    • A61K31/4025—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • 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
    • A61P5/30—Oestrogens
    • 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
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/64—Oxygen atoms

Landscapes

  • 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)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
SI9630423T 1995-02-28 1996-02-27 Benzothiophene compounds, intermediates, compositions, and methods SI0729956T1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US08/396,401 US5510357A (en) 1995-02-28 1995-02-28 Benzothiophene compounds as anti-estrogenic agents
US55276095A 1995-11-03 1995-11-03
US08/552,564 US5998441A (en) 1995-02-28 1995-11-03 Benzothiophene compounds, intermediates, compositions, and methods
US08/552,565 US5977093A (en) 1995-02-28 1995-11-03 Benzothiophene compounds, intermediates, compositions, and methods
US08/552,890 US5919800A (en) 1995-02-28 1995-11-03 Benzothiophene compounds, intermediates, compositions, and methods
US08/552,679 US5856339A (en) 1995-02-28 1995-11-03 Benzothiophene compounds, intermediates, compositions, and methods
EP96301304A EP0729956B1 (fr) 1995-02-28 1996-02-27 Composés du benzothiophène, intermédiaires, compositions et méthodes

Publications (1)

Publication Number Publication Date
SI0729956T1 true SI0729956T1 (en) 2002-04-30

Family

ID=27559919

Family Applications (1)

Application Number Title Priority Date Filing Date
SI9630423T SI0729956T1 (en) 1995-02-28 1996-02-27 Benzothiophene compounds, intermediates, compositions, and methods

Country Status (16)

Country Link
EP (2) EP1113013A1 (fr)
JP (2) JP3989569B2 (fr)
AR (1) AR003930A1 (fr)
AT (1) ATE207913T1 (fr)
DE (1) DE69616396T2 (fr)
DK (1) DK0729956T3 (fr)
ES (1) ES2163587T3 (fr)
FI (1) FI20095804A (fr)
HK (1) HK1013991A1 (fr)
IL (7) IL132952A (fr)
PE (1) PE44597A1 (fr)
PL (1) PL182493B1 (fr)
PT (1) PT729956E (fr)
SG (2) SG90193A1 (fr)
SI (1) SI0729956T1 (fr)
UA (1) UA44710C2 (fr)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3989569B2 (ja) * 1995-02-28 2007-10-10 イーライ リリー アンド カンパニー ベンゾチオフェン化合物、中間体、組成物および方法
CA2214072C (fr) * 1996-08-29 2006-11-14 Eli Lilly And Company Benzo [b] thiophenes, intermediaires, procedes, compositions et methodes
CA2216592C (fr) * 1996-10-24 2006-07-18 Brian Stephen Muehl Composes a base de benzothiophene, intermediaires, compositions et methodes
ZA982819B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Treatment or prophylaxis of prostatic cancer and benign prostatic hyperplasia with selective estrogn receptor modulators.
ZA982877B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Treatment of central nervous system disorders with selective estrogen receptor modulators.
ZA982818B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Prevention of breast cancer using selective estrogen receptor modulators.
EP0988289A2 (fr) * 1997-06-05 2000-03-29 Takeda Pharmaceutical Company Limited Composes heterocycliques, leur preparation et leur utilisation
US6653297B1 (en) * 1997-07-03 2003-11-25 Medical College Of Hampton Roads Control of selective estrogen receptor modulators
US6090843A (en) * 1997-08-11 2000-07-18 Eli Lilly And Company Benzothiophenes compounds which have useful pharmaceutical activity
ID24978A (id) * 1997-11-14 2000-08-31 Lilly Co Eli 2-ARYL-3-AROYLBENZO (b) THIOPHENES BERGUNA UNTUK PENGOBATAN SINDROM DEPRIVASI ESTROGEN
US6096781A (en) 1997-11-14 2000-08-01 Eli Lilly And Company 2-arylbenzo[B]thiophenes useful for the treatment of estrogen deprivation syndrome
AU751158B2 (en) 1998-06-16 2002-08-08 Eli Lilly And Company Methods for increasing levels of acetylcholine
US6288108B1 (en) 1998-06-16 2001-09-11 Eli Lilly And Company Methods for increasing levels of acetylcholine
AU748659B2 (en) * 1998-06-16 2002-06-06 Eli Lilly And Company Methods for increasing levels of acetylcholine
US6258826B1 (en) 1998-10-13 2001-07-10 Eli Lilly And Company Pharmaceutical formulations and applications thereof for the treatment of estrogen deprivation syndrome
DE69907962T2 (de) * 1998-12-14 2004-05-19 Vertex Pharmaceuticals (San Diego) Llc, San Diego Optische molekularsensoren für cytochrome p-450 aktivität
WO2000059897A2 (fr) * 1999-04-06 2000-10-12 Akzo Nobel N.V. Composes oestrogeniques selectifs
EP1204655B1 (fr) * 1999-07-29 2003-10-01 Eli Lilly And Company Forme cristalline de chlorhydrate de 6-hydroxy-3-(4- 2-(piperidin-e1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene
AU6335600A (en) * 1999-07-29 2001-02-19 Eli Lilly And Company A novel crystalline form of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-metho yphenyl)benzo[b]thiophene hydrochloride
JP2004505888A (ja) * 2000-03-10 2004-02-26 ベイラー・ユニバーシテイ チューブリン結合リガンドおよび対応するプロドラッグ構造
EP1757291A3 (fr) * 2000-05-08 2009-07-15 Eli Lilly & Company Formulations stabilisées de 6-hydroxy-3-(4- 2-(pipéridin-1-yl)éthoxyphénoxy)-2-(4-methoxyphényl) benzo(b)thiophène et sels de ces composés
DZ3376A1 (fr) * 2000-05-08 2001-11-15 Lilly Co Eli Formulations stabilisees de 6-hydroxy-3-(4-[2-(piperidin-1-yl) ethoxy]phenoxy)-2-(4-methoxyphenyl) benzo[b]thiophene et sels de ces composes
AR029538A1 (es) * 2000-07-06 2003-07-02 Wyeth Corp Composiciones farmaceuticas de agentes estrogenicos
US20040014672A1 (en) * 2000-10-20 2004-01-22 Luke Wayne Douglas Novel crystalline form of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene hydrochloride
MXPA05000898A (es) 2002-07-22 2005-05-16 Lilly Co Eli Moduladores de receptor de estrogeno selectivos que contiene, un grupo fenilsulfonilo.
CN1548434B (zh) * 2003-05-16 2010-07-28 中国科学院上海药物研究所 一类苯并噻吩类化合物、及制备和它的医药用途
WO2005073205A1 (fr) * 2004-01-22 2005-08-11 Eli Lilly And Company Modulateurs selectifs du recepteur des oestrogenes
US20090137632A1 (en) * 2005-02-11 2009-05-28 Erwin M Johnston Compositions And Methods For Treating Dyslipidemia
FR2913017A1 (fr) * 2007-02-23 2008-08-29 Cerep Sa Derives de piperidine et piperazine comme agents anti-neoplasiques ou inhibiteurs de proliferation cellulaire
EA200970863A1 (ru) * 2007-03-16 2010-02-26 Эли Лилли Энд Компани Способ и промежуточные соединения для получения арзоксифена
WO2014130310A1 (fr) 2013-02-19 2014-08-28 Novartis Ag Dérivés de benzothiophène et compositions correspondantes en tant qu'agents de dégradation sélectifs des récepteurs des œstrogènes
PT3186233T (pt) * 2014-08-29 2021-12-02 Chdi Foundation Inc Sondas para imagem de proteína de huntingtina

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1138163A (en) * 1965-05-21 1968-12-27 Bristol Myers Co Benzothiophene derivatives having anti-fertility properties
US4133814A (en) * 1975-10-28 1979-01-09 Eli Lilly And Company 2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents
FR2447914A1 (fr) * 1979-02-05 1980-08-29 Sanofi Sa Nouveaux benzothiophenes, leurs procedes de preparation et leur application notamment comme hypolipemiants et hypocholesterolemiants
IL65379A0 (en) * 1981-04-03 1982-05-31 Lilly Co Eli Process for preparing acylated benzothiophenes
US4418068A (en) * 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes
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
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
CA2145614A1 (fr) * 1994-03-31 1995-10-01 Jeffrey A. Dodge Intermediaires et procedes pour la preparation de benzothiofenes
US5484798A (en) * 1994-09-20 1996-01-16 Eli Lilly And Company Benzothiopene compounds, compositions, and method of inhibiting restenosis
JP3989569B2 (ja) * 1995-02-28 2007-10-10 イーライ リリー アンド カンパニー ベンゾチオフェン化合物、中間体、組成物および方法

Also Published As

Publication number Publication date
HK1013991A1 (en) 1999-09-17
DK0729956T3 (da) 2001-11-26
DE69616396T2 (de) 2002-07-11
PL312955A1 (en) 1996-09-02
JPH09183776A (ja) 1997-07-15
PE44597A1 (es) 1997-10-13
IL132953A (en) 2002-02-10
JP2007238626A (ja) 2007-09-20
IL117276A (en) 2001-10-31
ATE207913T1 (de) 2001-11-15
EP0729956A1 (fr) 1996-09-04
IL117276A0 (en) 1996-06-18
JP3989569B2 (ja) 2007-10-10
IL132954A0 (en) 2001-03-19
EP0729956B1 (fr) 2001-10-31
ES2163587T3 (es) 2002-02-01
SG64896A1 (en) 1999-05-25
AR003930A1 (es) 1998-09-30
IL132953A0 (en) 2001-03-19
IL132954A (en) 2002-02-10
UA44710C2 (uk) 2002-03-15
PL182493B1 (pl) 2002-01-31
DE69616396D1 (de) 2001-12-06
IL132952A (en) 2002-02-10
PT729956E (pt) 2002-03-28
FI20095804A (fi) 2009-07-23
IL132952A0 (en) 2001-03-19
SG90193A1 (en) 2002-07-23
EP1113013A1 (fr) 2001-07-04

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