IL97025A - 17 beta-substituted-4-aza-5alfa-androstan-3-one derivatives their preparation and pharmaceutical compositions containing them - Google Patents

17 beta-substituted-4-aza-5alfa-androstan-3-one derivatives their preparation and pharmaceutical compositions containing them

Info

Publication number
IL97025A
IL97025A IL9702591A IL9702591A IL97025A IL 97025 A IL97025 A IL 97025A IL 9702591 A IL9702591 A IL 9702591A IL 9702591 A IL9702591 A IL 9702591A IL 97025 A IL97025 A IL 97025A
Authority
IL
Israel
Prior art keywords
aza
carbamoyl
methyl
androst
androstan
Prior art date
Application number
IL9702591A
Other languages
English (en)
Other versions
IL97025A0 (en
Inventor
Achille Panzeri
Salle Enrico Di
Marcella Nesi
Original Assignee
Pharmacia Spa
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 Pharmacia Spa filed Critical Pharmacia Spa
Publication of IL97025A0 publication Critical patent/IL97025A0/xx
Publication of IL97025A publication Critical patent/IL97025A/en

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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
IL9702591A 1990-02-09 1991-01-24 17 beta-substituted-4-aza-5alfa-androstan-3-one derivatives their preparation and pharmaceutical compositions containing them IL97025A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB909002922A GB9002922D0 (en) 1990-02-09 1990-02-09 17 beta-substituted-4-aza-5 alpha-androstan-3-one derivatives and process for their preparation

Publications (2)

Publication Number Publication Date
IL97025A0 IL97025A0 (en) 1992-03-29
IL97025A true IL97025A (en) 1995-05-26

Family

ID=10670693

Family Applications (1)

Application Number Title Priority Date Filing Date
IL9702591A IL97025A (en) 1990-02-09 1991-01-24 17 beta-substituted-4-aza-5alfa-androstan-3-one derivatives their preparation and pharmaceutical compositions containing them

Country Status (26)

Country Link
US (1) US5155107A (de)
EP (1) EP0468012B1 (de)
JP (1) JPH04505462A (de)
KR (1) KR920701234A (de)
CN (1) CN1054771A (de)
AT (1) ATE128143T1 (de)
AU (1) AU642215B2 (de)
CA (1) CA2049318A1 (de)
CZ (1) CZ279484B6 (de)
DE (1) DE69113155T2 (de)
DK (1) DK0468012T3 (de)
ES (1) ES2080297T3 (de)
FI (1) FI914723A0 (de)
GB (1) GB9002922D0 (de)
GR (1) GR3017996T3 (de)
HR (1) HRP921221A2 (de)
HU (1) HUT59158A (de)
IE (1) IE910408A1 (de)
IL (1) IL97025A (de)
MY (1) MY105402A (de)
NO (1) NO913923L (de)
NZ (1) NZ237023A (de)
PT (1) PT96699A (de)
RU (1) RU2088589C1 (de)
WO (1) WO1991012261A1 (de)
ZA (1) ZA91918B (de)

Families Citing this family (34)

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Publication number Priority date Publication date Assignee Title
GB9115676D0 (en) * 1991-07-19 1991-09-04 Erba Carlo Spa Process for the preparation of 17 beta substituted-4-aza-5 alpha-androstan-3-one derivatives
CA2084799C (en) 1991-12-17 2003-01-28 Glenn J. Gormley Method of prevention of prostatic carcinoma with 17 beta-n-monosubstituted-carbamoyl-4-aza-5 alpha-androst-1 -en-3-ones
WO1993013124A1 (en) * 1991-12-20 1993-07-08 Glaxo Inc. Inhibitors of 5-alpha-testosterone reductase
JPH07508039A (ja) * 1992-05-20 1995-09-07 メルク　エンド　カンパニー　インコーポレーテッド ４−アザステロイドのエステル誘導体
SK137994A3 (en) * 1992-05-20 1995-04-12 Merck & Co Inc 7-beta-substituted-4-aza-5-alpha-cholestan-ons their using for production of pharmaceutical agent and pharmaceutical agent containing them
WO1993023038A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. 17-AMINO SUBSTITUTED 4-AZASTEROID 5α-REDUCTASE INHIBITORS
US5536727A (en) * 1992-05-20 1996-07-16 Merck & Co., Inc. 17-Ethers and thioethers of 4-aza-steroids
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
ATE195129T1 (de) * 1992-05-20 2000-08-15 Merck & Co Inc 4-azasteroide als 5-alpha-reduktase
UA35589C2 (uk) * 1992-05-21 2001-04-16 Андорешерш Інк. ІНГІБІТОРИ ТЕСТОСТЕРОН 5-<font face="Symbol">a</font>-РЕДУКТАЗИ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ ТА СПОСІБ ІНГІБУВАННЯ АКТИВНОСТІ ТЕСТОСТЕРОН 5-<font face="Symbol">a</font>-РЕДУКТАЗИ
GB9216284D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa Fluorinated 17beta-substituted 4-aza-5alpha-androstane-3-one derivatives
GB9216280D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa Steroids with a fluorinated acylureidic type side chain
GB9216329D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa 17beta-substituted 4-aza-5alpha-androstan-3-one derivatives
US5302589A (en) * 1992-08-07 1994-04-12 Glaxo, Inc. Heterocyclic inhibitors of 5-α-testosterone reductase
HU212459B (en) * 1992-10-02 1996-06-28 Richter Gedeon Vegyeszet Process for producing new 17-beta-substituted 4-aza-androstane-derivatives and pharmaceutical compositions containing them
US5278159A (en) * 1992-10-06 1994-01-11 Merck & Co., Inc. Aryl ester derivatives of 3-oxo-4-aza-androstane 17-β-carboxylates as 5-α-reductase inhibitors
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
WO1994021614A1 (en) * 1993-03-24 1994-09-29 Merck & Co., Inc. SUBSTITUTED 3-PHENANTHRIDINONE DERIVATIVES AS 5α-REDUCTASE INHIBITORS
JP3325026B2 (ja) * 1993-06-28 2002-09-17 メルク エンド カンパニー インコーポレーテッド ４−アザ−プレグナン５α−レダクターゼアイソザイム１阻害剤
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
GB9415178D0 (en) * 1994-07-28 1994-09-21 Erba Carlo Spa 4-azasteroids with side-chain fluoroketones
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
CN1072679C (zh) * 1995-07-30 2001-10-10 重庆医科大学 一种氮杂甾体化合物、制备及其用途
GB9518858D0 (en) * 1995-09-14 1995-11-15 Pharmacia Spa Phenylsubstituted 4-azasteroid fluoroderivatives
WO1997011702A1 (en) * 1995-09-27 1997-04-03 Merck & Co., Inc. Method of preventing androgenetic alopecia with 5-alpha reductase inhibitors
GB9727522D0 (en) * 1997-12-31 1998-02-25 Pharmacia & Upjohn Spa Process for preparing carboxamido-4-azasteroids
US6645974B2 (en) * 2001-07-31 2003-11-11 Merck & Co., Inc. Androgen receptor modulators and methods for use thereof
WO2003059293A2 (en) * 2002-01-15 2003-07-24 Merck & Co., Inc. 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators
KR100503193B1 (ko) * 2002-08-19 2005-07-25 한미약품 주식회사 3-옥소-4-아자-5α-안드로스탄 화합물의 선택적인 제조방법
EP1663199B1 (de) * 2003-09-25 2013-04-03 Tel Aviv University Future Technology Development L.P. Zusammensetzungen und diese verwendende verfahren zur behandlung von amyloid-bedingten erkrankungen
WO2005092341A1 (en) * 2004-03-22 2005-10-06 Ranbaxy Laboratories Limited Combination therapy for lower urinary tract symptoms
CN100355772C (zh) * 2005-12-28 2007-12-19 天津大学 具有5α－还原酶抑制活性的甾体化合物及其制备方法
US20240400606A1 (en) * 2021-10-21 2024-12-05 The Board Of Trustees Of The University Of Illinois Small molecule activators of the immune system

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA970692A (en) * 1971-11-08 1975-07-08 Walter Voigt METHODS OF INHIBITING THE ACTIVITY OF TESTOSTERONE 5.alpha.-REDUCTASE
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
US4220778A (en) * 1978-10-30 1980-09-02 G. D. Searle & Co. 8-Aryl-1,2,3,4-tetrahydroisoquinoline and derivatives thereof
US4220775A (en) * 1979-03-15 1980-09-02 Merck & Co., Inc. Preparation of 4-aza-17-substituted-5α-androstan-3-ones useful as 5α-reductase inhibitors
US4317817A (en) * 1979-08-27 1982-03-02 Richardson-Merrell Inc. Novel steroid 5α-reductase inhibitors
US4396615A (en) * 1981-06-24 1983-08-02 Duke University Method of treating androgen-related disorders
NZ211145A (en) * 1984-02-27 1988-10-28 Merck & Co Inc 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions
GB8505862D0 (en) * 1985-03-07 1985-04-11 Erba Farmitalia Steroidic 5alpha-reductase inhibitors
US4845104A (en) * 1986-11-20 1989-07-04 Merck & Co., Inc. Oxidized analogs of 17β-N-monosubstituted-carbamoyl-4-aza-5-α-androstan-3-ones
NZ225100A (en) * 1987-06-29 1991-09-25 Merck & Co Inc Reaction of steroids (including 4-azasteroids) with a silylating agent in the presence of a quinone to introduce a delta' double bond and silylated intermediates

Also Published As

Publication number Publication date
ZA91918B (en) 1991-11-27
AU7230791A (en) 1991-09-03
CA2049318A1 (en) 1991-08-10
RU2088589C1 (en) 1997-08-27
FI914723A7 (fi) 1991-10-07
IL97025A0 (en) 1992-03-29
EP0468012A1 (de) 1992-01-29
ATE128143T1 (de) 1995-10-15
JPH04505462A (ja) 1992-09-24
US5155107A (en) 1992-10-13
HU913193D0 (en) 1992-01-28
PT96699A (pt) 1991-10-31
CZ279484B6 (cs) 1995-05-17
HUT59158A (en) 1992-04-28
IE910408A1 (en) 1991-08-14
CN1054771A (zh) 1991-09-25
DE69113155T2 (de) 1996-02-29
AU642215B2 (en) 1993-10-14
DE69113155D1 (de) 1995-10-26
NO913923L (no) 1991-12-06
DK0468012T3 (da) 1995-11-06
WO1991012261A1 (en) 1991-08-22
NZ237023A (en) 1993-01-27
GR3017996T3 (en) 1996-02-29
HRP921221A2 (en) 1995-12-31
MY105402A (en) 1994-09-30
GB9002922D0 (en) 1990-04-04
ES2080297T3 (es) 1996-02-01
NO913923D0 (no) 1991-10-07
CS9100274A2 (en) 1991-12-17
FI914723A0 (fi) 1991-10-07
EP0468012B1 (de) 1995-09-20
KR920701234A (ko) 1992-08-11

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