IL132952A0 - Benzothiophene derivatives - Google Patents

Benzothiophene derivatives

Info

Publication number
IL132952A0
IL132952A0 IL13295299A IL13295299A IL132952A0 IL 132952 A0 IL132952 A0 IL 132952A0 IL 13295299 A IL13295299 A IL 13295299A IL 13295299 A IL13295299 A IL 13295299A IL 132952 A0 IL132952 A0 IL 132952A0
Authority
IL
Israel
Prior art keywords
benzothiophene derivatives
benzothiophene
derivatives
Prior art date
Application number
IL13295299A
Other languages
English (en)
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 US08/552,565 external-priority patent/US5977093A/en
Priority claimed from US08/552,564 external-priority patent/US5998441A/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 IL132952A0 publication Critical patent/IL132952A0/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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (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)
IL13295299A 1995-02-28 1999-11-15 Benzothiophene derivatives IL132952A0 (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
US08/552,565 US5977093A (en) 1995-02-28 1995-11-03 Benzothiophene compounds, intermediates, compositions, and methods
US08/552,564 US5998441A (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
IL11727699 1999-11-15

Publications (1)

Publication Number Publication Date
IL132952A0 true IL132952A0 (en) 2001-03-19

Family

ID=27559919

Family Applications (7)

Application Number Title Priority Date Filing Date
IL13295496A IL132954A (en) 1995-02-28 1996-02-27 Derivatives of benzothiophene
IL13295296A IL132952A (en) 1995-02-28 1996-02-27 Derivatives of benzothiophene
IL13295396A IL132953A (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
IL13295399A IL132953A0 (en) 1995-02-28 1999-11-15 Benzothiophene derivatives
IL13295299A IL132952A0 (en) 1995-02-28 1999-11-15 Benzothiophene derivatives
IL13295499A IL132954A0 (en) 1995-02-28 1999-11-15 Benzothiophene derivatives

Family Applications Before (5)

Application Number Title Priority Date Filing Date
IL13295496A IL132954A (en) 1995-02-28 1996-02-27 Derivatives of benzothiophene
IL13295296A IL132952A (en) 1995-02-28 1996-02-27 Derivatives of benzothiophene
IL13295396A IL132953A (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
IL13295399A IL132953A0 (en) 1995-02-28 1999-11-15 Benzothiophene derivatives

Family Applications After (1)

Application Number Title Priority Date Filing Date
IL13295499A IL132954A0 (en) 1995-02-28 1999-11-15 Benzothiophene derivatives

Country Status (16)

Country Link
EP (2) EP0729956B1 (xx)
JP (2) JP3989569B2 (xx)
AR (1) AR003930A1 (xx)
AT (1) ATE207913T1 (xx)
DE (1) DE69616396T2 (xx)
DK (1) DK0729956T3 (xx)
ES (1) ES2163587T3 (xx)
FI (1) FI20095804A (xx)
HK (1) HK1013991A1 (xx)
IL (7) IL132954A (xx)
PE (1) PE44597A1 (xx)
PL (1) PL182493B1 (xx)
PT (1) PT729956E (xx)
SG (2) SG90193A1 (xx)
SI (1) SI0729956T1 (xx)
UA (1) UA44710C2 (xx)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG90193A1 (en) * 1995-02-28 2002-07-23 Lilly Co Eli Benzothiophene compounds, intermediates, compositions, and methods
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
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.
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.
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
US6288108B1 (en) 1998-06-16 2001-09-11 Eli Lilly And Company Methods for increasing levels of acetylcholine
KR20010052891A (ko) 1998-06-16 2001-06-25 피터 지. 스트링거 아세틸콜린 수치를 상승시키는 방법
IL138914A0 (en) * 1998-06-16 2001-11-25 Lilly Co Eli 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
ATE240310T1 (de) * 1998-12-14 2003-05-15 Vertex Pharma San Diego Llc Optische molekularsensoren für cytochrome p-450 aktivität
AU3964400A (en) * 1999-04-06 2000-10-23 Akzo Nobel N.V. Selective estrogenic compounds
DE60005693T2 (de) * 1999-07-29 2004-07-29 Eli Lilly And Co., Indianapolis Eine kristalline form von 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophen-hydrochlorid
WO2001009116A2 (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
WO2001068654A2 (en) * 2000-03-10 2001-09-20 Baylor University Tubulin binding ligands and corresponding prodrug constructs
HUP0302190A3 (en) * 2000-05-08 2009-03-30 Lilly Co Eli Stabilized formulations of 6-hydroxy-3-(4-[2-(piperidin-1-yl) ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene and salts thereof
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
AR029538A1 (es) * 2000-07-06 2003-07-02 Wyeth Corp Composiciones farmaceuticas de agentes estrogenicos
CZ20031098A3 (cs) * 2000-10-20 2003-08-13 Eli Lilly And Company Nová krystalická forma 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]fenoxy)-2-(4-methoxyfenyl)benzo[b]thiofen hydrochloridu
CA2490580C (en) 2002-07-22 2012-12-11 Eli Lilly And Company Selective estrogen receptor modulators containing a naphthalene group
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
US20070111988A1 (en) * 2004-01-22 2007-05-17 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
KR20090112758A (ko) 2007-03-16 2009-10-28 일라이 릴리 앤드 캄파니 아르족시펜의 제조를 위한 방법 및 중간체
AU2014219283C1 (en) * 2013-02-19 2016-10-27 Novartis Ag Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders
ES2898965T3 (es) * 2014-08-29 2022-03-09 Chdi Foundation Inc Sondas de formación de imágenes de la proteína 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
US5484798A (en) * 1994-09-20 1996-01-16 Eli Lilly And Company Benzothiopene compounds, compositions, and method of inhibiting restenosis
SG90193A1 (en) * 1995-02-28 2002-07-23 Lilly Co Eli Benzothiophene compounds, intermediates, compositions, and methods

Also Published As

Publication number Publication date
JPH09183776A (ja) 1997-07-15
EP1113013A1 (en) 2001-07-04
IL132954A (en) 2002-02-10
SG90193A1 (en) 2002-07-23
IL132952A (en) 2002-02-10
DE69616396D1 (de) 2001-12-06
FI20095804A (fi) 2009-07-23
IL117276A (en) 2001-10-31
ES2163587T3 (es) 2002-02-01
IL117276A0 (en) 1996-06-18
DE69616396T2 (de) 2002-07-11
IL132954A0 (en) 2001-03-19
JP3989569B2 (ja) 2007-10-10
PL312955A1 (en) 1996-09-02
PL182493B1 (pl) 2002-01-31
SI0729956T1 (en) 2002-04-30
EP0729956A1 (en) 1996-09-04
PT729956E (pt) 2002-03-28
ATE207913T1 (de) 2001-11-15
UA44710C2 (uk) 2002-03-15
PE44597A1 (es) 1997-10-13
EP0729956B1 (en) 2001-10-31
DK0729956T3 (da) 2001-11-26
AR003930A1 (es) 1998-09-30
HK1013991A1 (en) 1999-09-17
IL132953A0 (en) 2001-03-19
IL132953A (en) 2002-02-10
JP2007238626A (ja) 2007-09-20
SG64896A1 (en) 1999-05-25

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