EP0859761A4 - 4-azasteroids for treatment of hyperandrogenic conditions - Google Patents

4-azasteroids for treatment of hyperandrogenic conditions

Info

Publication number
EP0859761A4
EP0859761A4 EP96930822A EP96930822A EP0859761A4 EP 0859761 A4 EP0859761 A4 EP 0859761A4 EP 96930822 A EP96930822 A EP 96930822A EP 96930822 A EP96930822 A EP 96930822A EP 0859761 A4 EP0859761 A4 EP 0859761A4
Authority
EP
European Patent Office
Prior art keywords
azasteroids
treatment
hyperandrogenic conditions
hyperandrogenic
conditions
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
EP96930822A
Other languages
German (de)
French (fr)
Other versions
EP0859761A1 (en
Inventor
Raman K Bakshi
Soumya P Sahoo
Richard L Tolman
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.)
Merck and Co Inc
Original Assignee
Merck and Co 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
Priority claimed from GBGB9603487.1A external-priority patent/GB9603487D0/en
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of EP0859761A1 publication Critical patent/EP0859761A1/en
Publication of EP0859761A4 publication Critical patent/EP0859761A4/en
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
EP96930822A 1995-09-15 1996-09-11 4-azasteroids for treatment of hyperandrogenic conditions Ceased EP0859761A4 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US382695P 1995-09-15 1995-09-15
US3826 1995-09-15
GBGB9603487.1A GB9603487D0 (en) 1996-02-20 1996-02-20 4-azasteroids for the treatment of hyperandrogenic conditions
GB9603487 1996-02-20
PCT/US1996/014564 WO1997010217A1 (en) 1995-09-15 1996-09-11 4-azasteroids for treatment of hyperandrogenic conditions

Publications (2)

Publication Number Publication Date
EP0859761A1 EP0859761A1 (en) 1998-08-26
EP0859761A4 true EP0859761A4 (en) 2000-01-26

Family

ID=26308763

Family Applications (1)

Application Number Title Priority Date Filing Date
EP96930822A Ceased EP0859761A4 (en) 1995-09-15 1996-09-11 4-azasteroids for treatment of hyperandrogenic conditions

Country Status (5)

Country Link
EP (1) EP0859761A4 (en)
JP (1) JPH11512434A (en)
AU (1) AU707324B2 (en)
CA (1) CA2231041A1 (en)
WO (1) WO1997010217A1 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU6137399A (en) * 1998-09-09 2000-03-27 Merck & Co., Inc. Method of determining and reducing the risk of bph-related urologic events
US6645974B2 (en) 2001-07-31 2003-11-11 Merck & Co., Inc. Androgen receptor modulators and methods for use thereof
US7402577B2 (en) * 2001-10-03 2008-07-22 Merck & Co., Inc. Androstane 17-beta-carboxamides as androgen receptor modulators
PL372920A1 (en) * 2002-03-13 2005-08-08 Merck & Co,Inc. Fluorinated 4-azasteroid derivatives as androgen receptor modulators
EP1636183A1 (en) 2003-05-16 2006-03-22 Ambit Biosciences Corporation Pyrrole compounds and uses thereof
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
EP2371367A1 (en) 2005-03-25 2011-10-05 Merck Sharp & Dohme (I.A.) Corp. Method of treating men with testosterone supplement and 5alpha reductase inhibitor

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994007861A1 (en) * 1992-10-06 1994-04-14 Merck & Co., Inc. 17β-CARBOXANILIDES OF 4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
US5151429A (en) * 1984-02-27 1992-09-29 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α reductase inhibitors
US4760071A (en) * 1984-02-27 1988-07-26 Merck & Co., Inc. 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors
IE76452B1 (en) * 1990-10-29 1997-10-22 Sankyo Co Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use
US5304562A (en) * 1991-10-09 1994-04-19 Ciba-Geigy Corporation 17β-substituted Aza-androstane derivatives
US5468860A (en) * 1992-11-19 1995-11-21 Merck & Co., Inc. New finasteride processes

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994007861A1 (en) * 1992-10-06 1994-04-14 Merck & Co., Inc. 17β-CARBOXANILIDES OF 4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS

Non-Patent Citations (8)

* Cited by examiner, † Cited by third party
Title
BAKSHI ET AL: "Erratum to J. Med. Chem. Vol 38, Nr 17, pages 3189-3192, 18 August 1995", JOURNAL OF MEDICINAL CHEMISTRY., vol. 39, no. 5, 1 March 1996 (1996-03-01), WASHINGTON US, pages 1192, XP002089558 *
BAKSHI R K ET AL: "4-Aza-3-oxo-5.alpha.-androst-1-ene-17.beta.-N-arylcarboxamides as Dual Inhibitors of Human Type 1 and Type 2 Steroid 5.alpha.-Reductases. Dramatic Effect of N-Aryl Substituents on Type 1 and Type 2 5.alpha.-Reductase Inhibitory Potency", JOURNAL OF MEDICINAL CHEMISTRY., vol. 38, no. 17, 18 August 1995 (1995-08-18), WASHINGTON US, XP002087243 *
CHEMICAL ABSTRACTS, vol. 122, no. 25, 19 June 1995, Columbus, Ohio, US; abstract no. 314919, ZHENG, JINHONG ET AL: "Synthesis of N-substituted-4-methyl-3-oxo-4-aza-5.alpha.-androstane- 17.beta.-carboxamide compounds" XP002121894 *
KURATA H ET AL: "SYNTHESIS AND TESTOSTERONE 5ALPHA-REDUCTASE-INHIBITORY ACTIVITY OF 4-AZA-5ALPHA-ANDROSTANE-17-CARBOXAMIDE COMPOUND WITH AN AROMATIC MOIETY IN THE C-17 CARBAMOYL GROUP", CHEMICAL AND PHARMACEUTICAL BULLETIN,JP,PHARMACEUTICAL SOCIETY OF JAPAN. TOKYO, vol. 44, no. 1, pages 115-121, XP000569266, ISSN: 0009-2363 *
MELLIN T N ET AL: "AZASTEROIDS AS INHIBITORS OF TESTOSTERONE 5ALPHA-REDUCTASE IN MAMMALIAN SKIN", JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, vol. 44, no. 2, February 1993 (1993-02-01), pages 121 - 131, XP002028037 *
RASMUSSON G H ET AL: "AZASTEROIDS AS INHIBITORS OF RAT PROSTATIC 5ALPHA-REDUCTASE", JOURNAL OF MEDICINAL CHEMISTRY, vol. 27, no. 12, December 1984 (1984-12-01), pages 1690 - 1701, XP002043194 *
See also references of WO9710217A1 *
ZHONGGUO YAOKE DAXUE XUEBAO (1995), 26(1), 1-4 *

Also Published As

Publication number Publication date
AU707324B2 (en) 1999-07-08
CA2231041A1 (en) 1997-03-20
JPH11512434A (en) 1999-10-26
EP0859761A1 (en) 1998-08-26
AU6973796A (en) 1997-04-01
WO1997010217A1 (en) 1997-03-20

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Legal Events

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