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 EP99936218A priority Critical patent/EP1102582A2/fr
Priority to CA002339368A priority patent/CA2339368A1/fr
Priority to JP2000563261A priority patent/JP2002522380A/ja
Priority to AU51449/99A priority patent/AU5144999A/en
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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • 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
    • A61K31/565—Compounds 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
    • A61K31/566—Compounds 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
    • 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
    • A61K31/565—Compounds 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
    • A61K31/568—Compounds 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
    • A61K31/5685—Compounds 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
    • 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
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A61K31/585—Compounds 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
    • 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
    • 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
    • A61P17/08—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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (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
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
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
AU51449/99A AU5144999A (en) 1998-08-07 1999-08-06 Inhibition of type 3 3alpha-hydroxysteroid dehydrogenase
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
US6908910B2 (en) 1993-08-06 2005-06-21 The Children's Medical Center Corporation Estrogenic compounds as anti-mitotic agents
US5504074A (en) 1993-08-06 1996-04-02 Children's Medical Center Corporation Estrogenic compounds as anti-angiogenic 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
US6995278B2 (en) 2000-08-18 2006-02-07 Entre Med, Inc. Antiangiogenic agents
US7135581B2 (en) 2000-08-18 2006-11-14 Entremed, Inc. Antiangiogenic agents
EP1343803A2 (fr) * 2000-11-27 2003-09-17 EntreMed, Inc. Estrogenes substitues en position 2 comme agents antiangiogeniques
US6710037B2 (en) * 2001-05-01 2004-03-23 Schering Corporation Method of treating androgen-dependent disorders
ATE498408T1 (de) * 2001-08-10 2011-03-15 Takeda Pharmaceutical Gnrh-agonistische kombinationsmittel
CN1679956A (zh) * 2001-11-29 2005-10-12 Gtx公司 治疗因雄激素剥夺引起的症状
US7524866B2 (en) 2001-11-29 2009-04-28 Gtx, Inc. Prevention and treatment of androgen—deprivation induced osteoporosis
EP1633367A2 (fr) 2003-05-28 2006-03-15 EntreMed, Inc. Agents anti-angiogenese
CA2558014A1 (fr) 2004-03-12 2005-09-29 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
CA2646065C (fr) 2006-03-20 2014-01-14 Entremed, Inc. 2-methoxyestradiol presentant une activite anti-arthritique pouvant modifier l'evolution de la maladie
US9284345B2 (en) 2007-04-12 2016-03-15 Endorecherche, Inc. 17alpha-substituted steroids as systemic antiandrogens and selective androgen receptor modulators
KR20100050444A (ko) * 2007-08-31 2010-05-13 아스텔라스세이야쿠 가부시키가이샤 피페리딘 유도체
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
PE20150353A1 (es) * 2012-07-10 2015-03-28 Bayer Pharma AG Derivados de estra-1,3,5(10),16-tetraeno 3-sustituidos, metodos para su preparacion, preparaciones farmaceuticas que los contienen, asi como su uso para la preparacion de medicamentos
ES2678993T3 (es) * 2013-02-21 2018-08-21 Bayer Pharma Aktiengesellschaft Estra-1,3,5(10),16-tetraeno-3-carboxamidas para la inhibición de la 17beta-hidroxiesteroide deshidrogenada (AKR1C3)
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
NO20010651D0 (no) 2001-02-07
EP1102582A2 (fr) 2001-05-30
WO2000007576A2 (fr) 2000-02-17
AR021757A1 (es) 2002-08-07
CA2339368A1 (fr) 2000-02-17
CN1322130A (zh) 2001-11-14
ID28791A (id) 2001-07-05
AU5144999A (en) 2000-02-28
NO20010651L (no) 2001-04-05
JP2002522380A (ja) 2002-07-23

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