JP4585320B2 - 男性ホルモン依存性疾患の処置のための17β−ヒドロキシステロイドデヒドロゲナーゼ3型インヒビター - Google Patents

男性ホルモン依存性疾患の処置のための17β−ヒドロキシステロイドデヒドロゲナーゼ3型インヒビター Download PDF

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JP4585320B2
JP4585320B2 JP2004565490A JP2004565490A JP4585320B2 JP 4585320 B2 JP4585320 B2 JP 4585320B2 JP 2004565490 A JP2004565490 A JP 2004565490A JP 2004565490 A JP2004565490 A JP 2004565490A JP 4585320 B2 JP4585320 B2 JP 4585320B2
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JP2006514054A (ja
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ティモシー ジェイ. グジ,
イー−ツン リュー,
ロナルド ジェイ. ドール,
アニル サクセナ,
ビヨール エム. ギリジャバラブハン,
ジョナサン エー. パクター,
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Merck Sharp and Dohme LLC
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Schering Corp
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • 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
    • 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
    • A61K31/495Heterocyclic 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/08Antiseborrheics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28Antiandrogens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/10Heterocyclic 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
    • C07D211/16Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06Heterocyclic 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
    • C07D241/08Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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)
  • 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (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)
JP2004565490A 2002-12-17 2003-12-15 男性ホルモン依存性疾患の処置のための17β−ヒドロキシステロイドデヒドロゲナーゼ3型インヒビター Expired - Fee Related JP4585320B2 (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US43410102P 2002-12-17 2002-12-17
PCT/US2003/039863 WO2004060488A1 (en) 2002-12-17 2003-12-15 17 beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases

Publications (3)

Publication Number Publication Date
JP2006514054A JP2006514054A (ja) 2006-04-27
JP2006514054A5 JP2006514054A5 (https=) 2006-12-28
JP4585320B2 true JP4585320B2 (ja) 2010-11-24

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JP2004565490A Expired - Fee Related JP4585320B2 (ja) 2002-12-17 2003-12-15 男性ホルモン依存性疾患の処置のための17β−ヒドロキシステロイドデヒドロゲナーゼ3型インヒビター

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=)

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DE60323765D1 (de) * 2002-12-17 2008-11-06 Schering Corp Inhibitoren der 17 beta-hydroxysteroiddehydrogenase des typs 3 zur behandlung androgenabhängiger krankheiten
EA015517B1 (ru) * 2004-04-13 2011-08-30 Инсайт Корпорейшн Производные пиперазинилпиперидина в качестве антагонистов хемокинового рецептора
US7598259B2 (en) * 2004-06-15 2009-10-06 Schering Corporation mGluR1 antagonists as therapeutic agents
US8036244B2 (en) * 2004-08-06 2011-10-11 Sharp Kabushiki Kaisha Transmitter, receiver, communication system, communication method, non-transitory computer readable medium
CA2964111A1 (en) 2005-03-29 2006-10-05 The Trustees Of The University Of Pennsylvania Methods for generating new hair folicles, treating baldness, and hair removal
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
CN102369186B (zh) 2009-04-02 2014-07-09 默克专利有限公司 作为自分泌运动因子抑制剂的哌啶和哌嗪衍生物
AU2011338530B2 (en) 2010-12-06 2017-06-15 Follica, Inc. Methods for treating baldness and promoting hair growth
JP6456373B2 (ja) 2013-06-25 2019-01-23 フォレンド ファーマ リミテッド 17β−ヒドロキシステロイドデヒドロゲナーゼ タイプ1の阻害剤として治療活性のあるエストラトリエンチアゾール誘導体
JP6556125B2 (ja) 2013-06-25 2019-08-07 フォレンド ファーマ リミテッド 17β−ヒドロキシステロイドデヒドロゲナーゼの阻害剤としての治療的に活性な17−窒素置換エストラトリエンチアゾール誘導体
TW201512215A (zh) 2013-06-25 2015-04-01 Forendo Pharma Ltd 治療活性雌三烯噻唑衍生物
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
JP6545266B2 (ja) 2014-12-23 2019-07-17 フォレンド ファーマ リミテッド 17β‐HSD1抑制剤のプロドラッグ
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
UA124972C2 (uk) 2016-07-29 2021-12-22 Янссен Фармацевтика Нв Способи лікування раку передміхурової залози
HRP20240679T1 (hr) 2017-06-08 2024-08-16 Organon R&D Finland Ltd 17-oksimi 15.beta.-[3-propanamido]-supstituiranih etera-1,3,5(10)-trien-17-ona za uporabu u inhibiciji 17.beta.-hidroksisteroid dehidrogenaza
JP7417608B2 (ja) 2018-12-05 2024-01-18 フォレンド ファーマ リミテッド 17-hsd1阻害剤としての16(17)位でピラゾール環と縮合しているエストラ-1,3,5(10)-トリエン化合物
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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WO2004046111A1 (en) 2002-11-18 2004-06-03 Schering Corporation 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
DE60323765D1 (de) * 2002-12-17 2008-11-06 Schering Corp Inhibitoren der 17 beta-hydroxysteroiddehydrogenase des typs 3 zur behandlung androgenabhängiger krankheiten

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Publication number Publication date
ATE409065T1 (de) 2008-10-15
US20080004248A1 (en) 2008-01-03
MXPA05006485A (es) 2005-08-26
EP1572299B1 (en) 2008-09-24
HK1074592A1 (en) 2005-11-18
US20060142338A1 (en) 2006-06-29
US20040138226A1 (en) 2004-07-15
US7485645B2 (en) 2009-02-03
US7053091B2 (en) 2006-05-30
ES2312845T3 (es) 2009-03-01
US7271175B2 (en) 2007-09-18
JP2006514054A (ja) 2006-04-27
AU2003293555A1 (en) 2004-07-29
EP1572299A1 (en) 2005-09-14
CA2509758A1 (en) 2004-07-22
CN1744930A (zh) 2006-03-08
DE60323765D1 (de) 2008-11-06
WO2004060488A1 (en) 2004-07-22

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