CN1053886C - 萘基化合物、中间体、制法和应用 - Google Patents

萘基化合物、中间体、制法和应用 Download PDF

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Publication number
CN1053886C
CN1053886C CN96105727A CN96105727A CN1053886C CN 1053886 C CN1053886 C CN 1053886C CN 96105727 A CN96105727 A CN 96105727A CN 96105727 A CN96105727 A CN 96105727A CN 1053886 C CN1053886 C CN 1053886C
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compound
formula
compounds
alkyl
pharmaceutically acceptable
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Expired - Fee Related
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CN96105727A
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Chinese (zh)
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CN1137525A (zh
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A·D·帕尔考维茨
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Eli Lilly and Co
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Eli Lilly and Co
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • 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
    • 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
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00—Ethers; Compounds having groups, groups or groups
    • C07C43/02—Ethers
    • C07C43/257—Ethers having an ether-oxygen atom bound to carbon atoms both belonging to six-membered aromatic rings
    • C07C43/295—Ethers having an ether-oxygen atom bound to carbon atoms both belonging to six-membered aromatic rings containing hydroxy or O-metal groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/68—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
    • C07C45/70—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form
    • C07C45/71—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form being hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C47/00—Compounds having —CHO groups
    • C07C47/52—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings
    • C07C47/575—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings containing ether groups, groups, groups, or groups
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Steroid Compounds (AREA)
CN96105727A 1995-02-28 1996-02-26 萘基化合物、中间体、制法和应用 Expired - Fee Related CN1053886C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/395,950 US5998401A (en) 1995-02-28 1995-02-28 Naphthyl compounds, intermediates, compositions, and methods
US395,950 1995-02-28

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CNB99123572XA Division CN1152683C (zh) 1995-02-28 1999-11-05 含萘基化合物的药物组合物

Publications (2)

Publication Number Publication Date
CN1137525A CN1137525A (zh) 1996-12-11
CN1053886C true CN1053886C (zh) 2000-06-28

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Family Applications (2)

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CN96105727A Expired - Fee Related CN1053886C (zh) 1995-02-28 1996-02-26 萘基化合物、中间体、制法和应用
CNB99123572XA Expired - Fee Related CN1152683C (zh) 1995-02-28 1999-11-05 含萘基化合物的药物组合物

Family Applications After (1)

Application Number Title Priority Date Filing Date
CNB99123572XA Expired - Fee Related CN1152683C (zh) 1995-02-28 1999-11-05 含萘基化合物的药物组合物

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CN (2) CN1053886C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
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US5919800A (en) * 1995-02-28 1999-07-06 Eli Lilly And Company Benzothiophene compounds, intermediates, compositions, and methods
US5998401A (en) * 1995-02-28 1999-12-07 Eli Lilly And Company Naphthyl compounds, intermediates, compositions, and methods
US5856340A (en) 1995-02-28 1999-01-05 Eli Lilly And Company Method of treating estrogen dependent cancers
US5510357A (en) * 1995-02-28 1996-04-23 Eli Lilly And Company Benzothiophene compounds as anti-estrogenic agents
SI0826679T1 (en) * 1996-08-29 2002-04-30 Eli Lilly And Company Naphthyl compounds and compositions
ID19392A (id) * 1996-08-29 1998-07-09 Lilly Co Eli Senyawa naftil dan bahan pertengahan serta komposisi dan metode penggunaan
CA2213814A1 (en) * 1996-08-29 1998-02-28 Henry Uhlman Bryant Naphthalene compounds, intermediates, formulations, and methods
CA2214929A1 (en) * 1996-09-26 1998-03-26 Charles Willis Lugar, Iii Naphthofluorene compounds, intermediates, compositions and methods
CA2214931A1 (en) * 1996-09-26 1998-03-26 Henry Uhlman Bryant Tetrahydrobenzo-a-fluorene compounds and method of use
CA2214935A1 (en) * 1996-09-26 1998-03-26 Henry Uhlman Bryant Benzofluorene compounds, intermediates, compositions, and methods
CA2217810A1 (en) * 1996-10-10 1998-04-10 Eli Lilly And Company 2-aryl-3-aminoaryloxynaphthyl compounds, intermediates, compositions and methods
US5916916A (en) * 1996-10-10 1999-06-29 Eli Lilly And Company 1-aryloxy-2-arylnaphthyl compounds, intermediates, compositions, and methods
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ZA982877B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Treatment of central nervous system disorders with selective estrogen receptor modulators.
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US6107346A (en) * 1997-08-11 2000-08-22 Eli Lilly And Company Methods for treating hyperlipidemia
US5929090A (en) * 1997-09-12 1999-07-27 Eli Lilly And Company 2-aryl-3-aminoaryloxynaphthy1 compounds, intermediates, compositions and methods
EP1173164A2 (en) 1999-04-16 2002-01-23 AstraZeneca AB Estrogen receptor-beta ligands
US6312474B1 (en) * 1999-09-15 2001-11-06 Bio-Vascular, Inc. Resorbable implant materials
KR100370597B1 (ko) * 2000-06-22 2003-02-05 박정일 산형매립초로부터 분리한 신규한 나프탈렌계 화합물 및이를 유효성분으로 하는 약학적 조성물
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EP1395563B1 (en) 2001-05-22 2006-03-29 Eli Lilly And Company 2-substituted 1,2,3,4-tetrahydroquinolines and derivatives thereof, compositions and methods
WO2002094268A1 (en) * 2001-05-22 2002-11-28 Eli Lilly And Company Tetrahydroquinolin derivatives for the inhibition of diseases associated with estrogen deprivation or with an aberrant physiological response to endogenous estrogen
US6914074B2 (en) 2001-12-13 2005-07-05 Wyeth Substituted phenyl naphthalenes as estrogenic agents
DE60327931D1 (de) * 2002-07-22 2009-07-23 Lilly Co Eli Selektive östrogenrezeptor modulatoren, die eine phenylsulfonyl-gruppe enthalten
US9315539B2 (en) * 2002-10-01 2016-04-19 Yale University 11 beta-short chain substituted estradiol analogs and their use in the treatment of menopausal symptoms and estrogen sensitive cancer
JP2007537991A (ja) * 2003-02-25 2007-12-27 イーライ リリー アンド カンパニー 溶媒和していない結晶性１−（４−（２−ピペリジニルエトキシ）フェノキシ）−２−（４−メタンスルホニルフェニル）−６−ヒドロキシナフタレン塩酸塩
MXPA05009098A (es) 2003-02-25 2005-11-17 Lilly Co Eli Clorhidrato de 1- (4-(2 -piperidiniletoxifenoxi) -2-(4-metansulfonilfenil) -6-hidroxinaftaleno cristalino no solvatado.
US20040253319A1 (en) * 2003-06-11 2004-12-16 Shrirang Netke Pharmaceutical compositions and method for alleviating side-effects of estrogen replacement therapy
WO2005051898A2 (en) * 2003-11-20 2005-06-09 Eli Lilly And Company Vitamin d receptor modulators
JP4589337B2 (ja) * 2003-11-20 2010-12-01 イーライ リリー アンド カンパニー ビタミン受容体調節剤
CN1910167B (zh) * 2004-01-22 2011-08-10 伊莱利利公司 用于治疗血管舒缩症状的选择性雌激素受体调节剂
ES2347973T3 (es) * 2004-01-22 2010-11-26 Eli Lilly And Company Moduladores selectivos de receptor de estrogeno para el tratamiento de sintomas vasomotores.
ATE448215T1 (de) 2004-01-22 2009-11-15 Lilly Co Eli Selektive östrogen-rezeptor-modulatoren
RU2352555C2 (ru) * 2004-06-22 2009-04-20 Смитклайн Бичем Корпорейшн ХИМИЧЕСКИЕ СОЕДИНЕНИЯ, СОДЕРЖАЩАЯ ИХ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ИХ ПРИМЕНЕНИЕ (ВАРИАНТЫ) И СПОСОБ СВЯЗЫВАНИЯ ERα И ERβ-ЭСТРОГЕНОВЫХ РЕЦЕПТОРОВ
TWI396543B (zh) * 2005-05-12 2013-05-21 Sankyo Co 取代丙烯醯胺衍生物及含有它之醫藥組成物
BRPI0920825A2 (pt) * 2008-09-29 2015-12-22 Lilly Co Eli modulador seletivo do receptor de estrogênio
CN103037862A (zh) 2010-06-16 2013-04-10 恩多研究公司 治疗或预防雌激素相关疾病的方法
AU2016371466B2 (en) 2015-12-17 2020-04-09 Alonbio Ltd Small Molecules for Inhibiting Chemokine Activity and/or Cancer Cells Growth
IL288144B2 (en) * 2019-05-15 2024-03-01 Alonbio Ltd Compounds to treat cancer, to inhibit chemokines and/or to kill cells

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