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WO2000007576A3 - INHIBITORS OF TYPE 3 3α-HYDROSTEROID DEHYDROGENASE - Google Patents

INHIBITORS OF TYPE 3 3α-HYDROSTEROID DEHYDROGENASE 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
French (fr)
Other versions
WO2000007576A2 (en
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 EP99936218A priority patent/EP1102582A2/en
Priority to CA002339368A priority patent/CA2339368A1/en
Priority to JP2000563261A priority patent/JP2002522380A/en
Publication of WO2000007576A2 publication Critical patent/WO2000007576A2/en
Publication of WO2000007576A3 publication Critical patent/WO2000007576A3/en
Priority to NO20010651A priority patent/NO20010651L/en
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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Novel methods of treating and/or inhibiting development of prostatic cancer, benign prostatic hyperplasia, prostatitis, acne, seborrhea, hirsutism or androgenic alopecia utilize inhibitors of type 3 3α-hydroxysteroid dehydrogenase alone or in combination with other active pharmaceuticals such as inhibitors of type 5 17β-hydroxysteroid dehydrogenase. Novel inhibitors and pharmaceutical products are also disclosed.
PCT/CA1999/000724 1998-08-07 1999-08-06 INHIBITORS OF TYPE 3 3α-HYDROSTEROID DEHYDROGENASE Ceased WO2000007576A2 (en)

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
EP99936218A EP1102582A2 (en) 1998-08-07 1999-08-06 Inhibitors of type 3 3alpha-hydroxysteroid dehydrogenase
CA002339368A CA2339368A1 (en) 1998-08-07 1999-08-06 Inhibitors of type 3 3.alpha.-hydroxysteroid dehydrogenase
JP2000563261A JP2002522380A (en) 1998-08-07 1999-08-06 Inhibition of type 33 α-hydroxysteroid dehydrogenase
NO20010651A NO20010651L (en) 1998-08-07 2001-02-07 Inhibition of type 3 <alpha> -hydroxysteroid dehydrogenase

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 (en) 2000-02-17
WO2000007576A3 true WO2000007576A3 (en) 2000-03-30

Family

ID=22252842

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CA1999/000724 Ceased WO2000007576A2 (en) 1998-08-07 1999-08-06 INHIBITORS OF TYPE 3 3α-HYDROSTEROID DEHYDROGENASE

Country Status (9)

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

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 (en) * 1998-03-11 2004-06-02 Endorecherche Inc. Inhibitors of type 5 and 3 17beta-hydroxysteroid dehydrogenase and methods for their use
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
AU8838601A (en) * 2000-11-27 2002-06-03 Entremed Inc Antiangiogenic agents
US6710037B2 (en) * 2001-05-01 2004-03-23 Schering Corporation Method of treating androgen-dependent disorders
ATE498408T1 (en) * 2001-08-10 2011-03-15 Takeda Pharmaceutical GNRH AGONISTIC COMBINATION AGENTS
US7524866B2 (en) 2001-11-29 2009-04-28 Gtx, Inc. Prevention and treatment of androgen—deprivation induced osteoporosis
DE60230687D1 (en) * 2001-11-29 2009-02-12 Gtx Inc Prevention and treatment of androgen deficiency-induced osteoporosis
WO2005030120A2 (en) 2003-05-28 2005-04-07 Entremed, Inc. Antiangiogenic agents
US7498322B2 (en) 2004-03-12 2009-03-03 Entremed, Inc. Antiangiogenic agents
DE102004032674A1 (en) * 2004-07-02 2006-01-26 Schering Ag New 2-substituted Estra-1,3,5 (10) -triene-17-ones as inhibitors of 17β-hydroxysteroid dehydrogenase type 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
EP2001482B1 (en) 2006-03-20 2016-08-24 CASI Pharmaceuticals, 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
AU2008292420A1 (en) * 2007-08-31 2009-03-05 Astellas Pharma Inc. Piperidine derivative
CN101698834B (en) * 2009-09-08 2012-05-23 北京利德曼生化股份有限公司 3 alpha-hydroxysteroid dehydrogenase and nucleotide sequence, recombinant vector, recombinant host cell and kit thereof
ES2603258T3 (en) 2012-07-10 2017-02-24 Bayer Pharma Aktiengesellschaft Derivatives of estra-1,3,5 (10), 3-substituted 16-tetraene, procedure for their preparation, pharmaceutical preparations containing them as well as their use for the preparation of medicines
CN105008382B (en) * 2013-02-21 2018-01-30 拜耳医药股份公司 Estra‑1,3,5(10),16‑tetraene‑3‑carboxamide for the inhibition of 17β‑hydroxysteroid dehydrogenase (AKR1 C3)
CN104873525A (en) * 2014-02-27 2015-09-02 天津药物研究院 11 beta-hydroxysteroid dehydrogenase inhibitor and its pharmaceutical composition and use
CN104873520A (en) * 2014-02-27 2015-09-02 天津药物研究院 11 beta-hydroxysteroid dehydrogenase inhibitor and its pharmaceutical composition and use

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 (en) * 1983-02-22 1984-08-29 Joachim Georg Liehr Improvements in or relating to the treatment of estrogen deficiency conditions
US4568673A (en) * 1984-03-20 1986-02-04 Wayne State University Compositions inhibiting murine MXT ductal carcinoma
WO1995004535A1 (en) * 1993-08-06 1995-02-16 The Children's Medical Center Corporation Estrogenic compounds as anti-mitotic agents
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

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 (en) * 1983-02-22 1984-08-29 Joachim Georg Liehr Improvements in or relating to the treatment of estrogen deficiency conditions
US4568673A (en) * 1984-03-20 1986-02-04 Wayne State University Compositions inhibiting murine MXT ductal carcinoma
WO1995004535A1 (en) * 1993-08-06 1995-02-16 The Children's Medical Center Corporation Estrogenic compounds as anti-mitotic agents
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 (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
WO2000007576A2 (en) 2000-02-17
ID28791A (en) 2001-07-05
AR021757A1 (en) 2002-08-07
CN1322130A (en) 2001-11-14
JP2002522380A (en) 2002-07-23
NO20010651L (en) 2001-04-05
AU5144999A (en) 2000-02-28
NO20010651D0 (en) 2001-02-07
EP1102582A2 (en) 2001-05-30
CA2339368A1 (en) 2000-02-17

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