CN100374421C - 用于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

用于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
CN100374421C
CN100374421C CNB2003801086673A CN200380108667A CN100374421C CN 100374421 C CN100374421 C CN 100374421C CN B2003801086673 A CNB2003801086673 A CN B2003801086673A CN 200380108667 A CN200380108667 A CN 200380108667A CN 100374421 C CN100374421 C CN 100374421C
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compound
alkyl
salt
cancer
treatment
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Expired - Fee Related
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Chinese (zh)
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CN1738800A (zh
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K·帕鲁奇
T·J·古兹
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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
    • 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
    • C07D211/36—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • 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
    • 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
    • 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
    • A61P17/12—Keratolytics, e.g. wart or anti-corn preparations
    • 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
    • A61P5/26—Androgens
    • 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
    • C07D211/36—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Oncology (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)
  • Hydrogenated Pyridines (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CNB2003801086673A 2002-11-18 2003-11-14 用于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 Expired - Fee Related CN100374421C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US42726302P 2002-11-18 2002-11-18
US60/427,263 2002-11-18

Publications (2)

Publication Number Publication Date
CN1738800A CN1738800A (zh) 2006-02-22
CN100374421C true CN100374421C (zh) 2008-03-12

Family

ID=32326512

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB2003801086673A Expired - Fee Related CN100374421C (zh) 2002-11-18 2003-11-14 用于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 (16)

Country Link
US (2) US7074795B2 (https=)
EP (1) EP1562901B1 (https=)
JP (2) JP4614770B2 (https=)
CN (1) CN100374421C (https=)
AR (1) AR042046A1 (https=)
AT (1) ATE469886T1 (https=)
AU (1) AU2003290799A1 (https=)
CA (1) CA2506290C (https=)
CL (1) CL2003002356A1 (https=)
DE (1) DE60332862D1 (https=)
ES (1) ES2345146T3 (https=)
MX (1) MXPA05005360A (https=)
MY (1) MY130792A (https=)
PE (1) PE20040750A1 (https=)
TW (1) TW200412964A (https=)
WO (1) WO2004046111A1 (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
GB0513702D0 (en) 2005-07-04 2005-08-10 Sterix Ltd Compound
US7851474B2 (en) * 2005-08-02 2010-12-14 Neurogen Corporation Dipiperazinyl ketones and related analogues
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
US8501940B2 (en) * 2008-07-15 2013-08-06 Hoffmann-La Roche Inc. Tetrahydrocinnoline derivatives
CN106890100A (zh) * 2011-04-25 2017-06-27 朴俊炯 用于预防脱发和促进毛发生长的局部施用的组合物
TW201512215A (zh) 2013-06-25 2015-04-01 Forendo Pharma Ltd 治療活性雌三烯噻唑衍生物
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
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
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
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
JP6532599B2 (ja) 2015-09-02 2019-06-19 グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ （Ｎｏ．２） Ｌｉｍｉｔｅｄ ブロモドメイン阻害薬としての使用のためのピリジノンジカルボキサミド
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
AU2018386327B2 (en) * 2017-12-15 2023-04-13 Inthera Bioscience AG 1 -(piperidinocarbonylmethyl)-2-oxopiperazine derivatives for treating cancer
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
EP4168014A1 (en) 2020-06-19 2023-04-26 Inthera Bioscience AG Oxopiperazine derivatives for the treatment of cancer

Citations (1)

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Publication number Priority date Publication date Assignee Title
WO1999046279A2 (en) * 1998-03-11 1999-09-16 Endorecherche, Inc. INHIBITORS OF TYPE 5 AND TYPE 3 17β-HYDROXYSTEROID DEHYDROGENASE AND METHODS FOR THEIR USE

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IE58836B1 (en) 1984-08-02 1993-11-17 Labrie Fernand Pharmaceutical composition for combination therapy of hormone dependent cancers
ZA901847B (en) 1989-03-10 1991-10-30 Endorecherche Inc Combination therapy for the treatment of estrogen sensitive diseases
ATE230994T1 (de) 1989-07-07 2003-02-15 Endorech Inc Methode zur behandlung androgenbedingter krankheiten
DE69034148T2 (de) 1989-07-07 2005-06-30 Endorecherche Inc., Ste-Foy Kombinationstherapie zur Prophylaxe und/oder Behandlung von gutartiger prostatischer Hyperplasie
US6060503A (en) 1991-12-02 2000-05-09 Endorecherche, Inc. Benzopyran-containing compounds and method for their use
ATE197458T1 (de) 1993-05-17 2000-11-11 Endorech Inc Verbesserte antiandrogene
US6124115A (en) 1995-09-22 2000-09-26 Endorecherche Inc. Production and use of isolated type 5 17β-hydroxysteroid dehydrogenase
AU4801197A (en) * 1996-09-13 1998-04-02 Schering Corporation Tricyclic antitumor compounds being farnesyl protein transferase inhibit ors
PE20030703A1 (es) 2001-09-06 2003-08-21 Schering Corp Inhibidores de la 17b-hidroxiesteroide deshidrogenasa tipo 3
EP1436281B1 (en) * 2001-10-17 2010-06-16 Schering Corporation Piperidine- and piperazineacetamides as 17beta hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
WO1999046279A2 (en) * 1998-03-11 1999-09-16 Endorecherche, Inc. INHIBITORS OF TYPE 5 AND TYPE 3 17β-HYDROXYSTEROID DEHYDROGENASE AND METHODS FOR THEIR USE

Non-Patent Citations (1)

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journal of enzyme inhibition and medicinal chemistry 2002 united kingdom. LE LAIN R ET AL,93～100,some coumarins and triphenylethene derivativesasinhebitorsof humam testes microsomal 17'beta！-hydroxysteroiddehydrogenase (17'beta!-HSD type 3):furtherstudies withtamoxifen on the rat testes microsomalenzyme. 2002 *

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Publication number Publication date
CA2506290C (en) 2012-04-24
CA2506290A1 (en) 2004-06-03
CN1738800A (zh) 2006-02-22
AR042046A1 (es) 2005-06-08
JP2010138204A (ja) 2010-06-24
US7476681B2 (en) 2009-01-13
MY130792A (en) 2007-07-31
AU2003290799A1 (en) 2004-06-15
US20040127503A1 (en) 2004-07-01
WO2004046111A1 (en) 2004-06-03
US7074795B2 (en) 2006-07-11
ATE469886T1 (de) 2010-06-15
CL2003002356A1 (es) 2005-02-11
TW200412964A (en) 2004-08-01
EP1562901B1 (en) 2010-06-02
DE60332862D1 (de) 2010-07-15
US20060148816A1 (en) 2006-07-06
PE20040750A1 (es) 2004-11-06
JP2006513169A (ja) 2006-04-20
JP4614770B2 (ja) 2011-01-19
HK1073313A1 (en) 2005-09-30
EP1562901A1 (en) 2005-08-17
ES2345146T3 (es) 2010-09-16
MXPA05005360A (es) 2005-08-03

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Granted publication date: 20080312

Termination date: 20111114