HK1013991A1 - Benzothiophene compounds, intermediates, compositions, and methods - Google Patents

Benzothiophene compounds, intermediates, compositions, and methods

Info

Publication number
HK1013991A1
HK1013991A1 HK98115195A HK98115195A HK1013991A1 HK 1013991 A1 HK1013991 A1 HK 1013991A1 HK 98115195 A HK98115195 A HK 98115195A HK 98115195 A HK98115195 A HK 98115195A HK 1013991 A1 HK1013991 A1 HK 1013991A1
Authority
HK
Hong Kong
Prior art keywords
intermediates
compositions
methods
benzothiophene compounds
benzothiophene
Prior art date
Application number
HK98115195A
Other languages
English (en)
Inventor
Alan David Palkowitz
Kenneth Jeff Thrasher
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 US08/552,679 external-priority patent/US5856339A/en
Priority claimed from US08/552,890 external-priority patent/US5919800A/en
Priority claimed from US08/552,565 external-priority patent/US5977093A/en
Priority claimed from US08/552,564 external-priority patent/US5998441A/en
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of HK1013991A1 publication Critical patent/HK1013991A1/xx

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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • Hematology (AREA)
  • Obesity (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)
HK98115195A 1995-02-28 1998-12-23 Benzothiophene compounds, intermediates, compositions, and methods HK1013991A1 (en)

Applications Claiming Priority (6)

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
US08/552,679 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
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

Publications (1)

Publication Number Publication Date
HK1013991A1 true HK1013991A1 (en) 1999-09-17

Family

ID=27559919

Family Applications (1)

Application Number Title Priority Date Filing Date
HK98115195A HK1013991A1 (en) 1995-02-28 1998-12-23 Benzothiophene compounds, intermediates, compositions, and methods

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) SG64896A1 (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
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.
ZA982818B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Prevention of breast cancer using selective estrogen receptor modulators.
ZA982877B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Treatment of central nervous system disorders with selective estrogen receptor modulators.
AU7550398A (en) * 1997-06-05 1998-12-21 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
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
US6288108B1 (en) 1998-06-16 2001-09-11 Eli Lilly And Company Methods for increasing levels of acetylcholine
CA2335295A1 (en) 1998-06-16 1999-12-23 Eli Lilly And Company Methods for increasing levels of acetylcholine
JP2002518299A (ja) * 1998-06-16 2002-06-25 イーライ・リリー・アンド・カンパニー アセチルコリンレベルを増加させる方法
US6087378A (en) * 1998-10-13 2000-07-11 Eli Lilly And Company Pharmaceutical formulations and applications thereof for the treatment of estrogen deprivation syndrome
ES2199605T3 (es) * 1998-12-14 2004-02-16 Vertex Pharmaceuticals (San Diego) Llc Indicadores moleculares opticos de actividad del citocromo p450.
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
EP1204656A2 (en) * 1999-07-29 2002-05-15 Eli Lilly And Company A crystalline form of 6-hydroxy-3-(4-[2-(piperidin-1-yl) ethoxy] phenoxy)-2-(4-methoxyphenyl) benzo[b]thiophene hydrochloride
ES2208384T3 (es) * 1999-07-29 2004-06-16 Eli Lilly And Company Forma cristalina de clorhidrato de 6 hidroxi-3-(4-(2-(piperidin-1-il)-etoxi)-fenoxi)2--(4-metoxifenil)-benzo(b)tiofeno.
EP1263763B1 (en) * 2000-03-10 2007-07-25 Baylor University Tubulin binding ligands
CZ20023651A3 (cs) * 2000-05-08 2003-02-12 Eli Lilly And Company Stabilizované přípravky 6-hydroxy-3-(4-[2-(piperidin-1-yl)-ethoxy]fenoxy)-2-(4-methoxyfenyl)benzo[b]thiofen a jejich sole
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
PL360946A1 (en) * 2000-10-20 2004-09-20 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
AU2003253129B2 (en) 2002-07-22 2008-12-11 Eli Lilly And Company Selective estrogen receptor modulators containing a phenylsulfonyl 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
WO2005073205A1 (en) * 2004-01-22 2005-08-11 Eli Lilly And Company Selective estrogen receptor modulators
EP1853263A1 (en) * 2005-02-11 2007-11-14 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
AU2008229183A1 (en) 2007-03-16 2008-09-25 Eli Lilly And Company Process and intermediates for preparing arzoxifene
SI2958907T1 (en) 2013-02-19 2018-05-31 Novartis Ag Benzothiophene derivatives and their compositions as selective estrogen receptor antagonists
SG11201701600QA (en) * 2014-08-29 2017-03-30 Chdi Foundation Inc Probes for imaging huntingtin protein

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1300575B (de) * 1965-05-21 1969-08-07 Bristol Myers Co Benzo[b]thiophene
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 (en) * 1994-03-31 1995-10-01 Jeffrey A. Dodge Intermediates and processes for preparing benzothiophene compounds
US6399634B1 (en) * 1994-09-20 2002-06-04 Eli Lilly And Company Benzothiophene compounds, compositions, and methods
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
JPH09183776A (ja) 1997-07-15
AR003930A1 (es) 1998-09-30
PL182493B1 (pl) 2002-01-31
SG90193A1 (en) 2002-07-23
EP1113013A1 (en) 2001-07-04
FI20095804A (fi) 2009-07-23
IL132954A0 (en) 2001-03-19
IL132954A (en) 2002-02-10
IL117276A (en) 2001-10-31
IL132952A (en) 2002-02-10
PT729956E (pt) 2002-03-28
PE44597A1 (es) 1997-10-13
EP0729956B1 (en) 2001-10-31
IL132953A0 (en) 2001-03-19
DK0729956T3 (da) 2001-11-26
IL132952A0 (en) 2001-03-19
DE69616396D1 (de) 2001-12-06
ES2163587T3 (es) 2002-02-01
SG64896A1 (en) 1999-05-25
IL117276A0 (en) 1996-06-18
JP3989569B2 (ja) 2007-10-10
IL132953A (en) 2002-02-10
ATE207913T1 (de) 2001-11-15
PL312955A1 (en) 1996-09-02
SI0729956T1 (en) 2002-04-30
UA44710C2 (uk) 2002-03-15
EP0729956A1 (en) 1996-09-04
JP2007238626A (ja) 2007-09-20
DE69616396T2 (de) 2002-07-11

Similar Documents

Publication Publication Date Title
SG90193A1 (en) Benzothiophene compounds, intermediates, compositions, and methods
ZA961563B (en) Benzothiophene compounds, intermediates, compositions, and methods.
AU3686495A (en) Benzothiophene compounds, compositions, and methods
GR3030407T3 (en) Naphthyl compounds, intermediates, compositions, and methods
ZA965857B (en) Cable-sheathing composition
GB9613043D0 (en) Improved compositions
AU6774096A (en) Benzothiophene compounds
SG52651A1 (en) Composition
PL322571A1 (en) Deodoising composition
GB9518033D0 (en) Composition
HUP9600352A3 (en) Bitumenous composition
SG84501A1 (en) Browning composition
ZA961514B (en) Novel compositions
GB9615378D0 (en) Benzene compounds, intermediates, processes, compositions, and methods
PL327087A1 (en) Solid composition
GB9508323D0 (en) Composition
GB9508785D0 (en) Novel compositions
AU699753C (en) Benzothiophene compounds, intermediates, compositions and methods
EP0757075A3 (en) Polyaminotriazine composition
AU4579796A (en) Benzothiophene compounds, intermediates, compositions and methods
AU5309096A (en) Novel benzothiophene compounds and methods
GB9511701D0 (en) Composition
GB9517113D0 (en) Novel compositions
SG45099A1 (en) Composition
GB9514450D0 (en) Composition

Legal Events

Date Code Title Description
PF Patent in force
PC Patent ceased (i.e. patent has lapsed due to the failure to pay the renewal fee)

Effective date: 20110227