AU704933B2 - 16-substituted-6-aza-steroid 5-alpha-reductase inhibitors - Google Patents

16-substituted-6-aza-steroid 5-alpha-reductase inhibitors Download PDF

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Publication number
AU704933B2
AU704933B2 AU74416/96A AU7441696A AU704933B2 AU 704933 B2 AU704933 B2 AU 704933B2 AU 74416/96 A AU74416/96 A AU 74416/96A AU 7441696 A AU7441696 A AU 7441696A AU 704933 B2 AU704933 B2 AU 704933B2
Authority
AU
Australia
Prior art keywords
compound
aza
methyl
androst
composition
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
AU74416/96A
Other languages
English (en)
Other versions
AU7441696A (en
Inventor
Susan D Aster
Donald W. Graham
Derek J. Von Langen
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
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of AU7441696A publication Critical patent/AU7441696A/en
Application granted granted Critical
Publication of AU704933B2 publication Critical patent/AU704933B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • 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
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/18—Ring systems of four or more rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
AU74416/96A 1995-10-19 1996-10-15 16-substituted-6-aza-steroid 5-alpha-reductase inhibitors Ceased AU704933B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US563695P 1995-10-19 1995-10-19
US60/005636 1995-10-19
PCT/US1996/016347 WO1997014418A1 (en) 1995-10-19 1996-10-15 16-substituted-6-aza-steroid 5-alpha-reductase inhibitors

Publications (2)

Publication Number Publication Date
AU7441696A AU7441696A (en) 1997-05-07
AU704933B2 true AU704933B2 (en) 1999-05-06

Family

ID=21716906

Family Applications (1)

Application Number Title Priority Date Filing Date
AU74416/96A Ceased AU704933B2 (en) 1995-10-19 1996-10-15 16-substituted-6-aza-steroid 5-alpha-reductase inhibitors

Country Status (6)

Country Link
US (1) US5741795A (enExample)
EP (1) EP0862436A1 (enExample)
JP (1) JPH11513684A (enExample)
AU (1) AU704933B2 (enExample)
CA (1) CA2233084A1 (enExample)
WO (1) WO1997014418A1 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5547957A (en) * 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
US5994334A (en) * 1997-02-05 1999-11-30 University Of Maryland Androgen synthesis inhibitors
US5994335A (en) 1997-10-17 1999-11-30 The University Of Maryland, Baltimore 17-azolyl steroids useful as androgen synthesis inhibitors
US20100048914A1 (en) 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal Cyp17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
BRPI1008745A2 (pt) 2009-02-05 2019-09-17 Tokai Pharmaceuticals Inc pró-fármacos de inibidores esteroidais de cyp17/antiandrogênios
GB201102913D0 (en) 2011-02-18 2011-04-06 Univ Birmingham Novel therapeutic
CN105682662A (zh) 2013-03-14 2016-06-15 马里兰大学巴尔的摩校区 雄激素受体减量调节剂及其用途
BR112016002970A2 (pt) 2013-08-12 2017-09-12 Tokai Pharmaceuticals Inc biomarcadores para o tratamento de distúrbios neoplásicos que usa terapias direcionadas ao androgênio
CN105348277B (zh) * 2015-12-08 2018-03-13 苏州科技学院 一种含苯并噁唑及咔唑结构单元的化合物及其应用
CN108003210A (zh) * 2018-01-24 2018-05-08 四川理工学院 一种雌甾-4,9-二烯-3,17-二酮的制备方法
EP4334298A1 (en) 2021-06-14 2024-03-13 Scorpion Therapeutics, Inc. Urea derivatives which can be used to treat cancer

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5438061A (en) * 1993-07-16 1995-08-01 Merck & Co., Inc. 7-substituted-δ4-6-azasteroid derivatives as 5α-reductase inhibitors

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3193554A (en) * 1962-01-03 1965-07-06 Syntex Corp Cyclopentanophenanthrene compounds and process
US5571817A (en) * 1984-02-27 1996-11-05 Merck & Co., Inc. Methods of treating androgenic alopecia with finasteride [17β-N-mono-substituted-carbamoyl-4-aza-5-α-androst-1-en-ones]
AU646069B2 (en) * 1990-08-10 1994-02-03 Pharmacia & Upjohn Company Llc Stimulation of hair growth with potassium channel openers and 5alpha-reductase inhibitors
ES2118222T3 (es) * 1991-12-20 1998-09-16 Glaxo Wellcome Inc Inhibidores de 5-alfa-testosterona reductasa.
ATE192646T1 (de) * 1992-01-21 2000-05-15 Howard Alliger Verwendung eines stoffgemisches enthaltend alpha hydroxy organische säure zur herstellung eines arzneimittels zur behandlung von kleinen mundgeschwüren
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
US5302589A (en) * 1992-08-07 1994-04-12 Glaxo, Inc. Heterocyclic inhibitors of 5-α-testosterone reductase
AP459A (en) * 1992-12-18 1996-02-14 Glaxo Wellcome Inc Substituted 6-azaandrostenones.
WO1994021614A1 (en) * 1993-03-24 1994-09-29 Merck & Co., Inc. SUBSTITUTED 3-PHENANTHRIDINONE DERIVATIVES AS 5α-REDUCTASE INHIBITORS
US5547957A (en) * 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
EP0724592B1 (en) * 1993-10-21 1999-01-07 Merck & Co. Inc. 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors
US5516779A (en) * 1994-06-08 1996-05-14 Merck & Co., Inc. 17β-substituted-6-azasteroid derivatives useful as 5α-reductase inhibitors
US5541322A (en) * 1994-10-14 1996-07-30 Glaxo Wellcome Inc. Synthesis of 6-azaandrostenones
US5543417A (en) * 1994-10-21 1996-08-06 Merck & Co., Inc. Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents
GB9506678D0 (en) * 1995-03-31 1995-05-24 Glaxo Inc Substituted 6-azacholesten-3-ones

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5438061A (en) * 1993-07-16 1995-08-01 Merck & Co., Inc. 7-substituted-δ4-6-azasteroid derivatives as 5α-reductase inhibitors

Also Published As

Publication number Publication date
CA2233084A1 (en) 1997-04-24
EP0862436A4 (enExample) 1998-09-30
WO1997014418A1 (en) 1997-04-24
US5741795A (en) 1998-04-21
AU7441696A (en) 1997-05-07
JPH11513684A (ja) 1999-11-24
EP0862436A1 (en) 1998-09-09

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Legal Events

Date Code Title Description
MK14 Patent ceased section 143(a) (annual fees not paid) or expired