EA200200358A1 - Глюкопиранозидные конъюгаты 2-(4-гидроксифенил)-1-[4-(2-амин-1-илэтокси)бензил]-1h-индол-5-олов - Google Patents

Глюкопиранозидные конъюгаты 2-(4-гидроксифенил)-1-[4-(2-амин-1-илэтокси)бензил]-1h-индол-5-олов

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Publication number
EA200200358A1
EA200200358A1 EA200200358A EA200200358A EA200200358A1 EA 200200358 A1 EA200200358 A1 EA 200200358A1 EA 200200358 A EA200200358 A EA 200200358A EA 200200358 A EA200200358 A EA 200200358A EA 200200358 A1 EA200200358 A1 EA 200200358A1
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EA
Eurasian Patent Office
Prior art keywords
carbon atoms
iletoxi
hydroxifenil
glucopiranoside
benzil
Prior art date
Application number
EA200200358A
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English (en)
Other versions
EA005371B1 (ru
Inventor
Кристофер Пол Миллер
Майкл Дэвид Коллини
Бэч Динх Трэн
Анита Вай-Йин Чан
Аркадий Зиновий Рубежов
Original Assignee
Американ Хоум Продактс Корпорейшн
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
Application filed by Американ Хоум Продактс Корпорейшн filed Critical Американ Хоум Продактс Корпорейшн
Publication of EA200200358A1 publication Critical patent/EA200200358A1/ru
Publication of EA005371B1 publication Critical patent/EA005371B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32—Antioestrogens
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

Данное изобретение относится к гистоселективным эстрогенам формулы (I), имеющим структуру (I), в которой Rи Rнезависимо представляют собой водород, алкильную цепь из 1-6 атомов углерода, бензил, ацил из 2-7 атомов углерода, бензоил, (1) или (2); Х представляет собой водород, алкил из 1-6 атомов углерода, CN, галоген, трифторметил или тиоалкил из 1-6 атомов углерода; n=1-3; при условии, что, по меньшей мере, один из Rи Rпредставляет собой (1) или (2); или к их фармацевтически приемлемым солям.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200200358A 1999-09-13 2000-09-11 Глюкопиранозидные конъюгаты 2-(4-гидроксифенил)-1-[4-(2-амин-1-илэтокси)бензил]-1h-индол-5-олов EA005371B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US39424099A 1999-09-13 1999-09-13
PCT/US2000/024738 WO2001019839A1 (en) 1999-09-13 2000-09-11 Glucopyranosides conjugates of 2-(4-hydroxy-phenyl)-1-[4-(2-amin-1-yl-ethoxy)-benzyl]-1h-indol-5-ols

Publications (2)

Publication Number Publication Date
EA200200358A1 true EA200200358A1 (ru) 2002-08-29
EA005371B1 EA005371B1 (ru) 2005-02-24

Family

ID=23558135

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200200358A EA005371B1 (ru) 1999-09-13 2000-09-11 Глюкопиранозидные конъюгаты 2-(4-гидроксифенил)-1-[4-(2-амин-1-илэтокси)бензил]-1h-индол-5-олов

Country Status (25)

Country Link
EP (1) EP1212335B1 (ru)
JP (1) JP2003509435A (ru)
KR (1) KR100653570B1 (ru)
CN (1) CN1196708C (ru)
AR (1) AR025638A1 (ru)
AT (1) ATE316093T1 (ru)
AU (1) AU764436B2 (ru)
BR (1) BR0013943A (ru)
CA (1) CA2382683A1 (ru)
CY (1) CY1104970T1 (ru)
CZ (1) CZ298862B6 (ru)
DE (1) DE60025630T2 (ru)
DK (1) DK1212335T3 (ru)
EA (1) EA005371B1 (ru)
ES (1) ES2254215T3 (ru)
HK (1) HK1044777B (ru)
HU (1) HUP0202679A3 (ru)
IL (2) IL148273A0 (ru)
MX (1) MXPA02002654A (ru)
NO (1) NO322250B1 (ru)
NZ (1) NZ517645A (ru)
PL (1) PL354179A1 (ru)
TW (1) TWI287018B (ru)
WO (1) WO2001019839A1 (ru)
ZA (1) ZA200201876B (ru)

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Publication number Priority date Publication date Assignee Title
EP1406898B1 (en) * 2001-07-19 2005-04-06 Cv Therapeutics, Inc. Substituted piperazine compounds and their use as fatty acid oxidation inhibitors
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
WO2006027987A1 (ja) * 2004-09-06 2006-03-16 Kissei Pharmaceutical Co., Ltd. 排尿障害の予防又は治療薬
EP2419406A1 (en) * 2009-04-13 2012-02-22 Sandoz AG Processes for the synthesis of bazedoxifene acetate and intermediates thereof
CN101857617A (zh) * 2010-04-28 2010-10-13 中国海洋大学 喹唑啉类糖衍生物及其制备方法和应用
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
CN104798294B (zh) * 2012-11-22 2018-09-25 艾默生电气公司 电机、定子和压缩机，以及制造它们的方法
CN104151265B (zh) * 2013-05-13 2016-10-05 上海医药工业研究院 醋酸巴多昔芬中间体的制备方法
CN104725334A (zh) * 2013-12-20 2015-06-24 北京蓝贝望生物医药科技股份有限公司 (4-(2-(氮杂环庚烷-1-基)乙氧基)苯基)甲醇的制备方法
CN105085365B (zh) * 2014-05-12 2018-06-19 四川科伦药业股份有限公司 醋酸巴多昔芬及其中间体的制备方法
CN107033062B (zh) * 2017-03-24 2019-10-29 梯尔希（南京）药物研发有限公司 一种巴多昔芬衍生物的制备方法
CN107400087B (zh) * 2017-09-15 2019-12-13 济南美高生物医药科技有限公司 一种1-(2-(4-(氯甲基)苯氧基)乙基)氮杂环庚烷盐酸盐的制备方法
CN111196831B (zh) * 2020-01-20 2023-05-09 山西医科大学 一种呋喃酚葡萄糖醛酸结合物的制备方法

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DE3821148A1 (de) * 1988-06-23 1989-12-28 Erwin Von Dr Angerer Aminoalkylindole, verfahren zu deren herstellung und diese enthaltende pharmazeutische praeparate
EP0639567A1 (en) * 1992-05-08 1995-02-22 Otsuka Pharmaceutical Factory, Inc. Indole derivative
GB9326332D0 (en) * 1993-12-23 1994-02-23 Karo Bio Indole derivatives
KR100362864B1 (ko) * 1994-02-22 2003-04-16 메렐 파마슈티칼스 인크. 에스트로겐관련신생물및질환의치료에유용한신규인돌유도체
US6723739B1 (en) * 1994-05-20 2004-04-20 Eli Lilly And Company Glucopyranoside benzothiophenes
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
DE122009000061I1 (de) * 1996-04-19 2009-12-31 Wyeth N D Ges D Staates Delawa Östrogene Verbindungen
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
SI1025077T1 (sl) * 1997-10-15 2007-06-30 Wyeth Corp Novi ariloksi-alkil-dialkilamini
ID24568A (id) * 1997-11-06 2000-07-27 American Home Prod Kontrasepsi oral yang mengandung anti-estrogen plus progestin

Also Published As

Publication number Publication date
MXPA02002654A (es) 2002-07-30
IL148273A0 (en) 2002-09-12
HK1044777B (zh) 2006-04-13
CZ2002881A3 (cs) 2003-01-15
EA005371B1 (ru) 2005-02-24
AR025638A1 (es) 2002-12-04
ZA200201876B (en) 2003-08-27
TWI287018B (en) 2007-09-21
DE60025630D1 (de) 2006-04-06
AU7128400A (en) 2001-04-17
EP1212335B1 (en) 2006-01-18
CY1104970T1 (el) 2010-03-03
CN1382151A (zh) 2002-11-27
HUP0202679A2 (hu) 2003-01-28
AU764436B2 (en) 2003-08-21
NO20021203L (no) 2002-03-12
CZ298862B6 (cs) 2008-02-27
HUP0202679A3 (en) 2003-04-28
KR100653570B1 (ko) 2006-12-05
WO2001019839A1 (en) 2001-03-22
BR0013943A (pt) 2002-05-14
DE60025630T2 (de) 2006-08-10
ATE316093T1 (de) 2006-02-15
NO322250B1 (no) 2006-09-04
NO20021203D0 (no) 2002-03-12
HK1044777A1 (en) 2002-11-01
CN1196708C (zh) 2005-04-13
ES2254215T3 (es) 2006-06-16
NZ517645A (en) 2003-09-26
JP2003509435A (ja) 2003-03-11
CA2382683A1 (en) 2001-03-22
DK1212335T3 (da) 2006-03-20
IL148273A (en) 2007-03-08
KR20020027643A (ko) 2002-04-13
PL354179A1 (en) 2003-12-29
EP1212335A1 (en) 2002-06-12

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Legal Events

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FA9A Withdrawal of a eurasian application
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU