CN1744930A - 治疗雄激素依赖性疾病的3型17β－羟基类固醇脱氢酶抑制剂 - Google Patents

治疗雄激素依赖性疾病的3型17β－羟基类固醇脱氢酶抑制剂 Download PDF

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Publication number
CN1744930A
CN1744930A CNA2003801094364A CN200380109436A CN1744930A CN 1744930 A CN1744930 A CN 1744930A CN A2003801094364 A CNA2003801094364 A CN A2003801094364A CN 200380109436 A CN200380109436 A CN 200380109436A CN 1744930 A CN1744930 A CN 1744930A
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chemical compound
alkyl
treatment
compound
compounds
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Chinese (zh)
Inventor
T·J·古兹
Y·-T·刘
R·J·多尔
A·萨克塞纳
V·M·吉里亚瓦拉布汉
J·A·帕奇特
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Merck Sharp and Dohme LLC
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Schering Corp
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero 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
    • A61K31/435—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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/08—Antiseborrheics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/16—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
    • C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Pregnancy & Childbirth (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CNA2003801094364A 2002-12-17 2003-12-15 治疗雄激素依赖性疾病的3型17β－羟基类固醇脱氢酶抑制剂 Pending CN1744930A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US43410102P 2002-12-17 2002-12-17
US60/434,101 2002-12-17

Publications (1)

Publication Number Publication Date
CN1744930A true CN1744930A (zh) 2006-03-08

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ID=32713010

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CNA2003801094364A Pending CN1744930A (zh) 2002-12-17 2003-12-15 治疗雄激素依赖性疾病的3型17β－羟基类固醇脱氢酶抑制剂

Country Status (11)

Country Link
US (3) US7053091B2 (https=)
EP (1) EP1572299B1 (https=)
JP (1) JP4585320B2 (https=)
CN (1) CN1744930A (https=)
AT (1) ATE409065T1 (https=)
AU (1) AU2003293555A1 (https=)
CA (1) CA2509758A1 (https=)
DE (1) DE60323765D1 (https=)
ES (1) ES2312845T3 (https=)
MX (1) MXPA05006485A (https=)
WO (1) WO2004060488A1 (https=)

Cited By (3)

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Publication number Priority date Publication date Assignee Title
CN105461705A (zh) * 2015-11-30 2016-04-06 中国医科大学 二苯并氮杂卓二酮类抗肿瘤化合物及其制备方法
CN112321515A (zh) * 2020-10-21 2021-02-05 上海馨远医药科技有限公司 一种手性1-叔丁基-3-甲基-6-甲基哌嗪-1,3-二甲酸酯的制备方法
CN112321538A (zh) * 2020-10-28 2021-02-05 都创(上海)医药开发有限公司 一种合成单胺保护的哌嗪-（r/s）2-甲酸酯的方法

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MXPA05006485A (es) * 2002-12-17 2005-08-26 Schering Corp Inhibidores de la 17 beta-hidroxiesteroide deshidrogenasa tipo 3 para el tratamiento de enfermedades dependientes de androgeno.
BRPI0509803A (pt) 2004-04-13 2007-09-18 Incyte Corp derivados de piperazinilpiperidina como antagonistas de receptor de quimiocina
US7598259B2 (en) * 2004-06-15 2009-10-06 Schering Corporation mGluR1 antagonists as therapeutic agents
EP1780984A4 (en) * 2004-08-06 2012-05-30 Sharp Kk Transmitter, receiver, communication system, communication method and communication program
ES2931949T3 (es) 2005-03-29 2023-01-05 Univ Pennsylvania Minoxidilo para generar nuevos folículos pilosos y tratar la calvicie
GB0513702D0 (en) * 2005-07-04 2005-08-10 Sterix Ltd Compound
WO2007130712A1 (en) * 2006-01-31 2007-11-15 Janssen Pharmaceutica, Nv Substituted dipiperidine as ccr2 antagonists for the treatment of inflammatory diseases
US20080051380A1 (en) 2006-08-25 2008-02-28 Auerbach Alan H Methods and compositions for treating cancer
US8080540B2 (en) 2006-09-19 2011-12-20 Abbott Products Gmbh Therapeutically active triazoles and their use
US8288367B2 (en) 2006-11-30 2012-10-16 Solvay Pharmaceuticals Gmbh Substituted estratriene derivatives as 17BETA HSD inhibitors
KR20120027177A (ko) 2009-04-02 2012-03-21 메르크 파텐트 게엠베하 오토탁신 저해제로서의 피페리딘 및 피라진 유도체
EP2648676A4 (en) 2010-12-06 2016-05-04 Follica Inc METHODS FOR TREATING CALVITIA AND PROMOTING HAIR GROWTH
WO2014207311A1 (en) 2013-06-25 2014-12-31 Forendo Pharma Ltd Therapeutically active estratrienthiazole derivatives as inhibitors of 17.beta.-hydroxy-steroid dehydrogenase, type 1
US10377791B2 (en) 2013-06-25 2019-08-13 Forendo Pharma Ltd. Therapeutically active estratrienthiazole derivatives as inhibitors of 17 B-hydroxysteroid dehydrogenase, type 1
KR20160042873A (ko) 2013-06-25 2016-04-20 포렌도 파마 리미티드 17.베타.-하이드록시스테로이드 탈수소효소의 억제제로서 치료적 활성 17-질소 치환된 에스트라트리엔티아졸 유도체
DE102014005129A1 (de) 2014-04-08 2014-11-06 Daimler Ag Verfahren und Fahrerassistenzvorrichtung zur Unterstützung eines Fahrers beim Führen eines Fahrzeugs
CN107207561B (zh) 2014-12-23 2020-03-31 佛恩多制药有限公司 17β-HSD1–抑制剂的前药
US10626140B2 (en) 2014-12-23 2020-04-21 Forendo Pharma Ltd Prodrugs of 17β-HSD1-inhibitors
BR112019001398A2 (pt) 2016-07-29 2019-05-07 Janssen Pharmaceutica Nv métodos para tratamento de câncer de próstata
FI3634975T3 (fi) 2017-06-08 2024-05-03 Organon R&D Finland Ltd 15-beeta-[3-propanamido]substituoitujen estra-1,3,5(10)-trien-17-onien 17-oksiimeja käytettäväksi 17-beeta-hydroksisteroididehydrogenaasien inhiboimisessa
BR112021010598A2 (pt) 2018-12-05 2021-08-24 Forendo Pharma Ltd Compostos, método para preparação de um composto e composição farmacêutica

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105461705A (zh) * 2015-11-30 2016-04-06 中国医科大学 二苯并氮杂卓二酮类抗肿瘤化合物及其制备方法
CN105461705B (zh) * 2015-11-30 2018-04-10 中国医科大学 二苯并氮杂卓二酮类抗肿瘤化合物及其制备方法
CN112321515A (zh) * 2020-10-21 2021-02-05 上海馨远医药科技有限公司 一种手性1-叔丁基-3-甲基-6-甲基哌嗪-1,3-二甲酸酯的制备方法
CN112321538A (zh) * 2020-10-28 2021-02-05 都创(上海)医药开发有限公司 一种合成单胺保护的哌嗪-（r/s）2-甲酸酯的方法

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US7485645B2 (en) 2009-02-03
US20080004248A1 (en) 2008-01-03
WO2004060488A1 (en) 2004-07-22
JP2006514054A (ja) 2006-04-27
CA2509758A1 (en) 2004-07-22
US7053091B2 (en) 2006-05-30
DE60323765D1 (de) 2008-11-06
US20040138226A1 (en) 2004-07-15
EP1572299A1 (en) 2005-09-14
EP1572299B1 (en) 2008-09-24
US20060142338A1 (en) 2006-06-29
MXPA05006485A (es) 2005-08-26
AU2003293555A1 (en) 2004-07-29
ATE409065T1 (de) 2008-10-15
US7271175B2 (en) 2007-09-18
HK1074592A1 (en) 2005-11-18
ES2312845T3 (es) 2009-03-01
JP4585320B2 (ja) 2010-11-24

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