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WO2000007576A3 - INHIBITION DE LA 3$G(a)-HYDROXYSTEROID-DESHYDROGENASE DE TYPE 3 - Google Patents

INHIBITION DE LA 3$G(a)-HYDROXYSTEROID-DESHYDROGENASE DE TYPE 3 Download PDF

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Publication number
WO2000007576A3
WO2000007576A3 PCT/CA1999/000724 CA9900724W WO0007576A3 WO 2000007576 A3 WO2000007576 A3 WO 2000007576A3 CA 9900724 W CA9900724 W CA 9900724W WO 0007576 A3 WO0007576 A3 WO 0007576A3
Authority
WO
WIPO (PCT)
Prior art keywords
inhibitors
type
hydroxysteroid dehydrogenase
dehydrogenase
novel
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/CA1999/000724
Other languages
English (en)
Other versions
WO2000007576A2 (fr
Inventor
Fernand Labrie
Yves Merand
Sylvain Gauthier
Louis Provencher
Van Luu-The
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Endorecherche Inc
Original Assignee
Endorecherche Inc
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 Endorecherche Inc filed Critical Endorecherche Inc
Priority to AU51449/99A priority Critical patent/AU5144999A/en
Priority to JP2000563261A priority patent/JP2002522380A/ja
Priority to EP99936218A priority patent/EP1102582A2/fr
Priority to CA002339368A priority patent/CA2339368A1/fr
Publication of WO2000007576A2 publication Critical patent/WO2000007576A2/fr
Publication of WO2000007576A3 publication Critical patent/WO2000007576A3/fr
Priority to NO20010651A priority patent/NO20010651L/no
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • 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
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/566Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol having an oxo group in position 17, e.g. estrone
    • 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
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A61K31/5685Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
    • 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
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A61K31/585Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
    • 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
    • A61P17/00Drugs for dermatological disorders
    • 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
    • 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
    • A61P5/26Androgens

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)

Abstract

L'invention porte sur de nouveaux procédés de traitement et/ou inhibition du développement du cancer de la prostate, de l'hyperplasie prostatique bénigne, des prostatites, de l'acné, de la séborrhée, de l'hirsutisme ou de l'alopécie masculine à l'aide de 3α-hydroxystéroid-déshydrogénase de type 3 seule ou combinée à d'autres produits pharmaceutiques actifs tels que les inhibiteurs 17β-hydroxystéroid-déshydrogénase de type 5. L'invention porte également sur de nouveaux inhibiteurs et produits pharmaceutiques.
PCT/CA1999/000724 1998-08-07 1999-08-06 INHIBITION DE LA 3$G(a)-HYDROXYSTEROID-DESHYDROGENASE DE TYPE 3 Ceased WO2000007576A2 (fr)

Priority Applications (5)

Application Number Priority Date Filing Date Title
AU51449/99A AU5144999A (en) 1998-08-07 1999-08-06 Inhibition of type 3 3alpha-hydroxysteroid dehydrogenase
JP2000563261A JP2002522380A (ja) 1998-08-07 1999-08-06 タイプ33α−ヒドロキシステロイドデヒドロゲナーゼの阻害
EP99936218A EP1102582A2 (fr) 1998-08-07 1999-08-06 INHIBITION DE LA 3$G(a)-HYDROXYSTEROID-DESHYDROGENASE DE TYPE 3
CA002339368A CA2339368A1 (fr) 1998-08-07 1999-08-06 Inhibition de la 3$g(a)-hydroxysteroid-deshydrogenase de type 3
NO20010651A NO20010651L (no) 1998-08-07 2001-02-07 Inhibering av type 3 3<alfa>-hydroxysteroiddehydrogenase

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9562398P 1998-08-07 1998-08-07
US60/095,623 1998-08-07

Publications (2)

Publication Number Publication Date
WO2000007576A2 WO2000007576A2 (fr) 2000-02-17
WO2000007576A3 true WO2000007576A3 (fr) 2000-03-30

Family

ID=22252842

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CA1999/000724 Ceased WO2000007576A2 (fr) 1998-08-07 1999-08-06 INHIBITION DE LA 3$G(a)-HYDROXYSTEROID-DESHYDROGENASE DE TYPE 3

Country Status (9)

Country Link
EP (1) EP1102582A2 (fr)
JP (1) JP2002522380A (fr)
CN (1) CN1322130A (fr)
AR (1) AR021757A1 (fr)
AU (1) AU5144999A (fr)
CA (1) CA2339368A1 (fr)
ID (1) ID28791A (fr)
NO (1) NO20010651L (fr)
WO (1) WO2000007576A2 (fr)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5504074A (en) 1993-08-06 1996-04-02 Children's Medical Center Corporation Estrogenic compounds as anti-angiogenic agents
US6908910B2 (en) 1993-08-06 2005-06-21 The Children's Medical Center Corporation Estrogenic compounds as anti-mitotic agents
EP1321146A3 (fr) * 1998-03-11 2004-06-02 Endorecherche Inc. Inhibiteurs de la 17beta-hydroxysteroide deshydrogénase du type 5 et du type 3 ainsi que leurs méthodes d'utilisation
US7087592B1 (en) 1999-08-23 2006-08-08 Entre Med, Inc. Compositions comprising purified 2-methoxyestradiol and methods of producing same
US6891953B1 (en) 2000-06-27 2005-05-10 Microsoft Corporation Method and system for binding enhanced software features to a persona
US7135581B2 (en) 2000-08-18 2006-11-14 Entremed, Inc. Antiangiogenic agents
US6995278B2 (en) * 2000-08-18 2006-02-07 Entre Med, Inc. Antiangiogenic agents
WO2002042319A2 (fr) * 2000-11-27 2002-05-30 Entremed, Inc. Antiangiogènes
US6710037B2 (en) * 2001-05-01 2004-03-23 Schering Corporation Method of treating androgen-dependent disorders
JP2003137814A (ja) * 2001-08-10 2003-05-14 Takeda Chem Ind Ltd GnRHアゴニストの併用剤
US7524866B2 (en) 2001-11-29 2009-04-28 Gtx, Inc. Prevention and treatment of androgen—deprivation induced osteoporosis
SI1460969T1 (sl) * 2001-11-29 2008-10-31 Gtx Inc Preprečevanje in zdravljenje s pomanjkanjem androgena inducirane osteoporoze
CA2527074A1 (fr) 2003-05-28 2005-04-07 Entremed, Inc. Agents anti-angiogenese
EP1756139A4 (fr) 2004-03-12 2009-07-29 Entremed Inc Agents anti-angiogeniques
DE102004032674A1 (de) * 2004-07-02 2006-01-26 Schering Ag Neue 2-substituierte Estra-1,3,5(10)-trien-17-one als Inhibitoren der 17β-Hydroxysteroiddehydrogenase Typ 1
US7419972B2 (en) 2004-07-02 2008-09-02 Schering Ag 2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17β-hydroxy steroid dehydrogenase type 1
US8399440B2 (en) 2006-03-20 2013-03-19 Entremed, Inc. Disease modifying anti-arthritic activity of 2-methoxyestradiol
US9284345B2 (en) * 2007-04-12 2016-03-15 Endorecherche, Inc. 17alpha-substituted steroids as systemic antiandrogens and selective androgen receptor modulators
WO2009028618A1 (fr) * 2007-08-31 2009-03-05 Astellas Pharma Inc. Dérivé de pipéridine
CN101698834B (zh) * 2009-09-08 2012-05-23 北京利德曼生化股份有限公司 3α-羟基类固醇脱氢酶及其核苷酸序列、重组载体、重组宿主细胞和试剂盒
JP6196302B2 (ja) 2012-07-10 2017-09-13 バイエル・ファルマ・アクティエンゲゼルシャフト 3−置換エストラ−1,3,5(10),16−テトラエン誘導体、その調製法、これらを含む医薬製剤および医薬を調製するためのその使用
AP3826A (en) * 2013-02-21 2016-09-30 Bayer Pharma Aktiengellschaft Estra-1,3,5(10),16-tetraene-3-carboxamides for inhibition of 17.beta.-hydroxysteroid dehydrogenase (akr1 c3)
CN104873520A (zh) * 2014-02-27 2015-09-02 天津药物研究院 一种11β-羟基类固醇脱氢酶抑制剂、药用组合物及其用途
CN104873525A (zh) * 2014-02-27 2015-09-02 天津药物研究院 一种11β-羟基类固醇脱氢酶抑制剂及其药用组合物和用途

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3562260A (en) * 1965-08-23 1971-02-09 Ormonoterapia Richter Spa 2-carbonyl-estratrienes and method of their preparation
US4340602A (en) * 1978-10-18 1982-07-20 Wayne State University Compositions inhibiting estrogen sulfotransferase activity
EP0117117A1 (fr) * 1983-02-22 1984-08-29 Joachim Georg Liehr Traitement des états estrogéno-déficients
US4568673A (en) * 1984-03-20 1986-02-04 Wayne State University Compositions inhibiting murine MXT ductal carcinoma
WO1995004535A1 (fr) * 1993-08-06 1995-02-16 The Children's Medical Center Corporation Composes ×strogenes utilises comme agents antimitotiques
WO1999046279A2 (fr) * 1998-03-11 1999-09-16 Endorecherche, Inc. INHIBITEURS DE LA 17β-HYDROXYSTEROIDE DESHYDROGENASE DU TYPE 5 ET DU TYPE 3 ET METHODES D'UTILISATION ASSOCIEES

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3562260A (en) * 1965-08-23 1971-02-09 Ormonoterapia Richter Spa 2-carbonyl-estratrienes and method of their preparation
US4340602A (en) * 1978-10-18 1982-07-20 Wayne State University Compositions inhibiting estrogen sulfotransferase activity
EP0117117A1 (fr) * 1983-02-22 1984-08-29 Joachim Georg Liehr Traitement des états estrogéno-déficients
US4568673A (en) * 1984-03-20 1986-02-04 Wayne State University Compositions inhibiting murine MXT ductal carcinoma
WO1995004535A1 (fr) * 1993-08-06 1995-02-16 The Children's Medical Center Corporation Composes ×strogenes utilises comme agents antimitotiques
WO1999046279A2 (fr) * 1998-03-11 1999-09-16 Endorecherche, Inc. INHIBITEURS DE LA 17β-HYDROXYSTEROIDE DESHYDROGENASE DU TYPE 5 ET DU TYPE 3 ET METHODES D'UTILISATION ASSOCIEES

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
DUFORT, ISABELLE ET AL: "Molecular cloning of human type 3 3.alpha.-hydroxysteroid dehydrogenase that differs from 20.alpha.-hydroxysteroid dehydrogenase by seven amino acids", BIOCHEM. BIOPHYS. RES. COMMUN. (1996), 228(2), 474-479, XP000867346 *
LUU-THE V ET AL: "CHARACTERISTICS OF HUMAN TYPES 1, 2 AND 3 17BETA-HYDROXYSTEROID DEHYDROGENASE ACTIVITIES: OXIDATION/REDUCTION AND INHIBITION", JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY,GB,ELSEVIER SCIENCE LTD., OXFORD, vol. 55, no. 5/06, pages 581-587, XP000196678, ISSN: 0960-0760 *
PAGE, PHILIP C. BULMAN ET AL: "Efficient regioselective A-ring functionalization of estrogens", TETRAHEDRON (1990), 46(6), 2059-68, XP000867284 *

Also Published As

Publication number Publication date
AU5144999A (en) 2000-02-28
CN1322130A (zh) 2001-11-14
ID28791A (id) 2001-07-05
AR021757A1 (es) 2002-08-07
NO20010651D0 (no) 2001-02-07
WO2000007576A2 (fr) 2000-02-17
EP1102582A2 (fr) 2001-05-30
NO20010651L (no) 2001-04-05
CA2339368A1 (fr) 2000-02-17
JP2002522380A (ja) 2002-07-23

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