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IL132952A - Derivatives of benzothiophene - Google Patents

Derivatives of benzothiophene

Info

Publication number
IL132952A
IL132952A IL13295296A IL13295296A IL132952A IL 132952 A IL132952 A IL 132952A IL 13295296 A IL13295296 A IL 13295296A IL 13295296 A IL13295296 A IL 13295296A IL 132952 A IL132952 A IL 132952A
Authority
IL
Israel
Prior art keywords
benzo
thiophene
ethoxy
phenoxy
formula
Prior art date
Application number
IL13295296A
Other languages
English (en)
Hebrew (he)
Original Assignee
Lilly Co Eli
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 US08/552,679 external-priority patent/US5856339A/en
Priority claimed from US08/552,890 external-priority patent/US5919800A/en
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of IL132952A publication Critical patent/IL132952A/en

Links

Classifications

    • 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
    • C07D333/62Benzo[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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • A61P3/06Antihyperlipidemics
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • 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
    • C07D333/62Benzo[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
    • C07D333/64Oxygen 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)
IL13295296A 1995-02-28 1996-02-27 Derivatives of benzothiophene IL132952A (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
US08/552,679 US5856339A (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
IL11727696A IL117276A (en) 1995-02-28 1996-02-27 Benziophene compounds, their preparation and their related compositions

Publications (1)

Publication Number Publication Date
IL132952A true IL132952A (en) 2002-02-10

Family

ID=27559919

Family Applications (7)

Application Number Title Priority Date Filing Date
IL13295296A IL132952A (en) 1995-02-28 1996-02-27 Derivatives of benzothiophene
IL13295496A IL132954A (en) 1995-02-28 1996-02-27 Derivatives of benzothiophene
IL11727696A IL117276A (en) 1995-02-28 1996-02-27 Benziophene compounds, their preparation and their related compositions
IL13295396A IL132953A (en) 1995-02-28 1996-02-27 Derivatives of benzothiophene
IL13295499A IL132954A0 (en) 1995-02-28 1999-11-15 Benzothiophene derivatives
IL13295299A IL132952A0 (en) 1995-02-28 1999-11-15 Benzothiophene derivatives
IL13295399A IL132953A0 (en) 1995-02-28 1999-11-15 Benzothiophene derivatives

Family Applications After (6)

Application Number Title Priority Date Filing Date
IL13295496A IL132954A (en) 1995-02-28 1996-02-27 Derivatives of benzothiophene
IL11727696A IL117276A (en) 1995-02-28 1996-02-27 Benziophene compounds, their preparation and their related compositions
IL13295396A IL132953A (en) 1995-02-28 1996-02-27 Derivatives of benzothiophene
IL13295499A IL132954A0 (en) 1995-02-28 1999-11-15 Benzothiophene derivatives
IL13295299A IL132952A0 (en) 1995-02-28 1999-11-15 Benzothiophene derivatives
IL13295399A IL132953A0 (en) 1995-02-28 1999-11-15 Benzothiophene derivatives

Country Status (16)

Country Link
EP (2) EP0729956B1 (pl)
JP (2) JP3989569B2 (pl)
AR (1) AR003930A1 (pl)
AT (1) ATE207913T1 (pl)
DE (1) DE69616396T2 (pl)
DK (1) DK0729956T3 (pl)
ES (1) ES2163587T3 (pl)
FI (1) FI20095804A (pl)
HK (1) HK1013991A1 (pl)
IL (7) IL132952A (pl)
PE (1) PE44597A1 (pl)
PL (1) PL182493B1 (pl)
PT (1) PT729956E (pl)
SG (2) SG64896A1 (pl)
SI (1) SI0729956T1 (pl)
UA (1) UA44710C2 (pl)

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 (en) * 1996-08-29 2006-11-14 Eli Lilly And Company Benzo [b] thiophene compounds, intermediates, processes, compositions, and methods
CA2216592C (en) * 1996-10-24 2006-07-18 Brian Stephen Muehl Benzothiophene compounds, intermediates, compositions, and methods
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.
CA2291026A1 (en) 1997-06-05 1998-12-10 Takeda Chemical Industries, Ltd. Heterocyclic compounds, their production and use
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
US6096781A (en) * 1997-11-14 2000-08-01 Eli Lilly And Company 2-arylbenzo[B]thiophenes useful for the treatment of estrogen deprivation syndrome
ID24978A (id) * 1997-11-14 2000-08-31 Lilly Co Eli 2-ARYL-3-AROYLBENZO (b) THIOPHENES BERGUNA UNTUK PENGOBATAN SINDROM DEPRIVASI ESTROGEN
TR200003714T2 (tr) * 1998-06-16 2001-07-23 Eli Lilly And Company Asetilkolin seviyesinin yükseltilmesi
KR20010052891A (ko) 1998-06-16 2001-06-25 피터 지. 스트링거 아세틸콜린 수치를 상승시키는 방법
US6288108B1 (en) 1998-06-16 2001-09-11 Eli Lilly And Company Methods for increasing levels of acetylcholine
US6087378A (en) * 1998-10-13 2000-07-11 Eli Lilly And Company Pharmaceutical formulations and applications thereof for the treatment of estrogen deprivation syndrome
AU3119000A (en) * 1998-12-14 2000-07-03 Invitrogen Corporation Optical molecular sensors for cytochrome p450 activity
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
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
WO2001009115A2 (en) * 1999-07-29 2001-02-08 Eli Lilly And Company A NOVEL CRYSTALLINE FORM OF 6-HYDROXY-3- (4-[2-(PIPERIDIN-1- YL)ETHOXY] PHENOXY)-2- (4-METHOXYPHENYL) BENZO[b]THIOPHENE HYDROCHLORIDE
CA2407967C (en) * 2000-03-10 2010-10-05 Baylor University Tubulin binding ligands and corresponding prodrug constructs
EP1757291A3 (en) * 2000-05-08 2009-07-15 Eli Lilly & Company Stabilized formulations of 6-hydroxy-3-(4-[2-(piperidin-1-YL)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene and salts thereof
JP2003535827A (ja) * 2000-05-08 2003-12-02 イーライ・リリー・アンド・カンパニー 6−ヒドロキシ−3−(4−[2−(ピペリジン−1−イル)エトキシ]フェノキシ)−2−(4−メトキシフェニル)ベンゾ[b]チオフェンおよびその塩の安定化製剤
AR029538A1 (es) 2000-07-06 2003-07-02 Wyeth Corp Composiciones farmaceuticas de agentes estrogenicos
EA005116B1 (ru) * 2000-10-20 2004-10-28 Эли Лилли Энд Компани НОВАЯ КРИСТАЛЛИЧЕСКАЯ ФОРМА ГИДРОХЛОРИДА 6-ГИДРОКСИ-3-(4-[2-(ПИПЕРИДИН-1-ИЛ)ЭТОКСИ]ФЕНОКСИ)-2-(4-МЕТОКСИФЕНИЛ)БЕНЗО[b]ТИОФЕНА
CN1668303B (zh) 2002-07-22 2010-10-27 伊莱利利公司 含苯磺酰基的选择性雌激素受体调节剂
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 (en) * 2004-01-22 2005-08-11 Eli Lilly And Company Selective estrogen receptor modulators
WO2006088648A1 (en) * 2005-02-11 2006-08-24 Eli Lilly And Company 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
BRPI0808740A2 (pt) 2007-03-16 2014-08-12 Lilly Co Eli Processo e intermediários para preparação de arzoxifeno.
MA38325B1 (fr) 2013-02-19 2019-03-29 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
US4418068A (en) * 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes
IL65379A0 (en) * 1981-04-03 1982-05-31 Lilly Co Eli Process for preparing acylated 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 (en) * 1994-03-31 1995-10-01 Jeffrey A. Dodge Intermediates and processes for preparing benzothiophene compounds
US5492921A (en) * 1994-09-20 1996-02-20 Eli Lilly And Company Benzothiophene compounds, compositions, and methods for inhibiting aortal smooth muscle proliferation
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
JP3989569B2 (ja) 2007-10-10
IL117276A0 (en) 1996-06-18
SG64896A1 (en) 1999-05-25
PL312955A1 (en) 1996-09-02
JP2007238626A (ja) 2007-09-20
ATE207913T1 (de) 2001-11-15
IL132954A0 (en) 2001-03-19
AR003930A1 (es) 1998-09-30
PL182493B1 (pl) 2002-01-31
SI0729956T1 (en) 2002-04-30
JPH09183776A (ja) 1997-07-15
IL132952A0 (en) 2001-03-19
DE69616396D1 (de) 2001-12-06
DE69616396T2 (de) 2002-07-11
SG90193A1 (en) 2002-07-23
PE44597A1 (es) 1997-10-13
IL132953A0 (en) 2001-03-19
ES2163587T3 (es) 2002-02-01
IL117276A (en) 2001-10-31
PT729956E (pt) 2002-03-28
FI20095804A (fi) 2009-07-23
HK1013991A1 (en) 1999-09-17
IL132954A (en) 2002-02-10
EP1113013A1 (en) 2001-07-04
EP0729956B1 (en) 2001-10-31
UA44710C2 (uk) 2002-03-15
IL132953A (en) 2002-02-10
EP0729956A1 (en) 1996-09-04
DK0729956T3 (da) 2001-11-26

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