CN1230163C - 与雌激素联合的2－苯基－1－[4－(2－氨基乙氧基)－苄基]－吲哚 - Google Patents

与雌激素联合的2－苯基－1－[4－(2－氨基乙氧基)－苄基]－吲哚 Download PDF

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Publication number
CN1230163C
CN1230163C CNB99808655XA CN99808655A CN1230163C CN 1230163 C CN1230163 C CN 1230163C CN B99808655X A CNB99808655X A CN B99808655XA CN 99808655 A CN99808655 A CN 99808655A CN 1230163 C CN1230163 C CN 1230163C
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CN
China
Prior art keywords
methyl
benzyl
phenyl
benzyloxy
indole
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 - Lifetime
Application number
CNB99808655XA
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English (en)
Chinese (zh)
Other versions
CN1326347A (zh
Inventor
J·H·皮卡
B·S·科姆
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.)
Wyeth LLC
Original Assignee
Wyeth LLC
American Home Products Corp
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
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22151320&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN1230163(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Wyeth LLC, American Home Products Corp filed Critical Wyeth LLC
Publication of CN1326347A publication Critical patent/CN1326347A/zh
Application granted granted Critical
Publication of CN1230163C publication Critical patent/CN1230163C/zh
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • 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
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • 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
    • 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
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CNB99808655XA 1998-05-15 1999-05-11 与雌激素联合的2－苯基－1－[4－(2－氨基乙氧基)－苄基]－吲哚 Expired - Lifetime CN1230163C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US7956198A 1998-05-15 1998-05-15
US09/079561 1998-05-15

Publications (2)

Publication Number Publication Date
CN1326347A CN1326347A (zh) 2001-12-12
CN1230163C true CN1230163C (zh) 2005-12-07

Family

ID=22151320

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB99808655XA Expired - Lifetime CN1230163C (zh) 1998-05-15 1999-05-11 与雌激素联合的2－苯基－1－[4－(2－氨基乙氧基)－苄基]－吲哚

Country Status (41)

Country Link
EP (1) EP1076558B1 (2)
JP (3) JP2002515431A (2)
KR (1) KR100620772B1 (2)
CN (1) CN1230163C (2)
AP (1) AP1424A (2)
AR (1) AR020074A1 (2)
AT (1) ATE245026T1 (2)
AU (1) AU760378B2 (2)
BE (1) BE2015C026I2 (2)
BG (1) BG64783B1 (2)
BR (1) BR9911040A (2)
CA (1) CA2329530A1 (2)
CU (1) CU23241B7 (2)
CY (1) CY2015020I1 (2)
CZ (1) CZ299334B6 (2)
DE (1) DE69909616T2 (2)
DK (1) DK1076558T3 (2)
EA (1) EA005932B1 (2)
EE (1) EE04262B1 (2)
ES (1) ES2203131T3 (2)
FR (1) FR15C0035I2 (2)
GE (1) GEP20033079B (2)
HR (1) HRP20000778B1 (2)
HU (2) HU226587B1 (2)
ID (1) ID26890A (2)
IL (1) IL139130A (2)
IN (1) IN192220B (2)
LT (1) LTC1076558I2 (2)
LU (1) LU92699I2 (2)
NO (2) NO328129B1 (2)
NZ (1) NZ508200A (2)
OA (1) OA11552A (2)
PL (1) PL194750B1 (2)
PT (1) PT1076558E (2)
SI (1) SI1076558T1 (2)
SK (1) SK284666B6 (2)
TR (1) TR200003377T2 (2)
TW (1) TW565554B (2)
UA (1) UA66861C2 (2)
WO (1) WO1999059581A1 (2)
ZA (1) ZA200006959B (2)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AP1424A (en) * 1998-05-15 2005-06-06 Wyeth Corp 2-Phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole in combination with estrogens.
US7005428B1 (en) 1998-06-11 2006-02-28 Endorecherche, Inc. Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
US6465445B1 (en) 1998-06-11 2002-10-15 Endorecherche, Inc. Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
JP4790178B2 (ja) 1999-07-06 2011-10-12 アンドルシェルシュ・インコーポレイテッド 体重増加の処置方法および／または抑制方法
US20020013327A1 (en) * 2000-04-18 2002-01-31 Lee Andrew G. Compositions and methods for treating female sexual dysfunction
AU2001273125A1 (en) * 2000-07-06 2002-01-21 American Home Products Corporation Combinations of bisphosphonates, estrogenic agents and optionally estrogens
AU2001271784A1 (en) * 2000-07-06 2002-01-21 Wyeth Therapy for prosthesis-related bone degeneration
US6376486B1 (en) 2000-07-06 2002-04-23 American Home Products Corporation Methods of inhibiting sphincter incontinence
US6455568B2 (en) 2000-07-06 2002-09-24 Wyeth Combination therapy for inhibiting sphincter incontinence
WO2002003989A2 (en) * 2000-07-06 2002-01-17 Wyeth Use of substituted indole compounds for treating sphincter incontinence
EP1359940A2 (en) * 2000-07-06 2003-11-12 Wyeth Combinations of statins, estrogenic agents and optionally estrogens
DE10117441A1 (de) * 2001-04-03 2002-10-10 Schering Ag 1-Indolylderivate, deren Verwendung zur Herstellung von Arzneimitteln, ein Verfahren zur Herstellung der 1-Indolylderivate sowie 1-Indolylderivate enthaltende pharmzeutische Präparate
CN1599606A (zh) 2001-07-31 2005-03-23 辉瑞产品公司 包含雌激素激动剂/拮抗剂、雌激素与孕激素组合的药物组合物、试剂盒和方法
KR100470274B1 (ko) 2002-11-08 2005-02-05 진 장 덮개층을 이용한 비정질 물질의 상 변화 방법
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
FR2880625B1 (fr) * 2005-01-07 2007-03-09 Sanofi Aventis Sa Derives de n-(heteroaryl)-1h-indole-2-carboxamides, leur preparation et leur application en therapeutique
RS54165B1 (sr) 2008-04-16 2015-12-31 Karo Bio Ab Novi ligandi za estrogenski receptor
AR072297A1 (es) * 2008-06-27 2010-08-18 Novartis Ag Derivados de indol-2-il-piridin-3-ilo, composicion farmaceutica que los comprende y su uso en medicamentos para el tratamiento de enfermedades mediadas por la sintasa aldosterona.
GB201113538D0 (en) 2011-08-04 2011-09-21 Karobio Ab Novel estrogen receptor ligands
CN102690225B (zh) * 2012-04-11 2014-12-24 南京友杰医药科技有限公司 巴多昔芬的合成方法
CN103709090A (zh) * 2014-01-16 2014-04-09 江苏万特制药有限公司 醋酸巴多昔芬的制备方法及其关键中间体
CN103739540B (zh) * 2014-01-20 2016-05-04 华润赛科药业有限责任公司 一种醋酸巴多昔芬中间体的制备方法
CN105669518B (zh) * 2014-12-04 2019-06-04 上海医药集团股份有限公司 醋酸巴多昔芬及其a晶型的制备方法
US12030878B2 (en) * 2017-12-15 2024-07-09 Bristol-Myers Squibb Company Substituted indole ether compounds
IT201800006562A1 (it) * 2018-06-21 2019-12-21 Procedimento e intermedi utili per la preparazione di indoli
CN115380026B (zh) * 2020-03-17 2023-11-07 南京明德新药研发有限公司 蛋白降解调节剂与其使用方法

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4729999A (en) * 1984-10-12 1988-03-08 Bcm Technologies Antiestrogen therapy for symptoms of estrogen deficiency
WO1993023374A1 (fr) * 1992-05-08 1993-11-25 Otsuka Pharmaceutical Factory, Inc. Derive d'indole
TW366342B (en) * 1992-07-28 1999-08-11 Lilly Co Eli The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss
GB9326332D0 (en) * 1993-12-23 1994-02-23 Karo Bio Indole derivatives
DE4426625A1 (de) * 1994-07-27 1996-03-14 Schering Ag 2-Phenylindole, Verfahren zu deren Herstellung, diese enthaltende pharmazeutische Präparate sowie deren Verwendung zur Herstellung von Arzneimitteln
TW397821B (en) * 1996-04-19 2000-07-11 American Home Produits Corp 3-[4-(2-phenyl-indole-1-ylmethyl)-phenyl]-acrylamides and 2-phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol as well as pharmaceutical compositions of estrogenic agents thereof
SK281737B6 (sk) * 1996-04-19 2001-07-10 American Home Products Corporation 2-fenylindolové zlúčeniny, farmaceutický prostriedok s ich obsahom a ich použitie
BR9710230A (pt) * 1996-07-09 1999-08-10 Smithkline Beecham Spa Derivados de indol para o tratamento de osteoporose
US5672609A (en) * 1996-07-18 1997-09-30 Eli Lilly And Company Pyridine compounds, intermediates compositions and methods of use
PT1025077E (pt) * 1997-10-15 2007-05-31 Wyeth Corp Novas ariloxi-alquil-dialquilaminas
AU1197299A (en) * 1997-10-28 1999-05-17 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
UA68365C2 (en) * 1997-11-06 2004-08-16 Wyeth Corp Peroral contraception by combination of anti-estrogen and progestin
AP1424A (en) * 1998-05-15 2005-06-06 Wyeth Corp 2-Phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole in combination with estrogens.

Also Published As

Publication number Publication date
SI1076558T1 (en) 2003-10-31
CZ299334B6 (cs) 2008-06-25
HRP20000778A2 (en) 2001-06-30
NO2015015I1 (no) 2015-06-02
AP1424A (en) 2005-06-06
KR20010043641A (ko) 2001-05-25
DE69909616T2 (de) 2004-06-17
JP2002515431A (ja) 2002-05-28
BR9911040A (pt) 2001-02-13
HK1031691A1 (en) 2001-06-22
HUP0103096A2 (hu) 2002-05-29
FR15C0035I1 (2) 2015-06-26
NO20005770D0 (no) 2000-11-14
EA005932B1 (ru) 2005-08-25
HUS1500023I1 (hu) 2017-03-28
IL139130A (en) 2005-11-20
SK284666B6 (sk) 2005-08-04
CN1326347A (zh) 2001-12-12
EE200000652A (et) 2002-04-15
TR200003377T2 (tr) 2001-03-21
EE04262B1 (et) 2004-04-15
HU226587B1 (en) 2009-04-28
IN192220B (2) 2004-03-20
JP2014159472A (ja) 2014-09-04
JP2009019042A (ja) 2009-01-29
PL194750B1 (pl) 2007-06-29
EA200001193A1 (ru) 2001-12-24
PL345268A1 (en) 2001-12-03
AU3894499A (en) 1999-12-06
AU760378B2 (en) 2003-05-15
LU92699I2 (fr) 2015-06-24
CZ20004254A3 (cs) 2001-12-12
PT1076558E (pt) 2003-11-28
ID26890A (id) 2001-02-15
NO328129B1 (no) 2009-12-14
OA11552A (en) 2004-06-07
JP5607871B2 (ja) 2014-10-15
ATE245026T1 (de) 2003-08-15
LTC1076558I2 (lt) 2016-11-10
IL139130A0 (en) 2001-11-25
DK1076558T3 (da) 2003-11-03
BG104930A (en) 2001-07-31
AR020074A1 (es) 2002-04-10
FR15C0035I2 (fr) 2015-08-28
CY2015020I1 (el) 2020-05-29
GEP20033079B (en) 2003-10-27
HRP20000778B1 (en) 2004-10-31
KR100620772B1 (ko) 2006-09-13
ZA200006959B (en) 2001-11-27
BE2015C026I2 (en) 2018-08-24
CU23241B7 (es) 2007-10-17
DE69909616D1 (de) 2003-08-21
UA66861C2 (uk) 2004-06-15
HUP0103096A3 (en) 2002-11-28
SK17202000A3 (sk) 2001-07-10
NO20005770L (no) 2001-01-12
EP1076558A1 (en) 2001-02-21
EP1076558B1 (en) 2003-07-16
JP5872624B2 (ja) 2016-03-01
NZ508200A (en) 2003-09-26
WO1999059581A1 (en) 1999-11-25
BG64783B1 (bg) 2006-04-28
ES2203131T3 (es) 2004-04-01
TW565554B (en) 2003-12-11
NO2015015I2 (no) 2015-06-02
CA2329530A1 (en) 1999-11-25
AP2000001970A0 (en) 2000-12-31

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