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NO913923L - 17beta-substituerte-4-aza-5alfa-androstan-3-on-derivater ogfremgangsmaate ved fremstilling av disse - Google Patents

17beta-substituerte-4-aza-5alfa-androstan-3-on-derivater ogfremgangsmaate ved fremstilling av disse

Info

Publication number
NO913923L
NO913923L NO91913923A NO913923A NO913923L NO 913923 L NO913923 L NO 913923L NO 91913923 A NO91913923 A NO 91913923A NO 913923 A NO913923 A NO 913923A NO 913923 L NO913923 L NO 913923L
Authority
NO
Norway
Prior art keywords
alkyl
cycloalkyl
group
hydrogen
substituted
Prior art date
Application number
NO91913923A
Other languages
English (en)
Other versions
NO913923D0 (no
Inventor
Achille Panzeri
Enrico Di Salle
Marcella Nesi
Original Assignee
Erba Carlo 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 Erba Carlo Spa filed Critical Erba Carlo Spa
Publication of NO913923D0 publication Critical patent/NO913923D0/no
Publication of NO913923L publication Critical patent/NO913923L/no

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)

Abstract

Foreliggende oppfinnelse vedrorer steroide 5a-reduk- tasehemmere med følgende formel (I) (l) hvor R! er hydrogen, en C^-Cg-alkylgruppe, en C6-alkylgruppe, eller en aroylgruppe; Y er oksygen eller svovel; W er en gruppe R2 3 hvor hver av og uavhengig er valgt fra gruppen som består av hydrogen, Cl-C6-alkyl, C5-C6-cykloalkyl, C6-C9-cykloalkylalkyl og aryl, hvor hver av gruppene alkyl, cykloalkyl, cyklo- alkylalkyl og aryl kan være usubstituert eller substituert med en sub- stituent -OR4 , hvor R4 er hydrogen eller C1-C4-alkyl; A er hydrogen, C-L-Cg-alkyl, C5-C6-cykloalkyl eller C6- Cg-cykloalkylalkyl hvor hver av gruppene alkyl, cykloalkyl og cykloalkylalkyl kan være usubstituert eller substituert med en substituent valat fra: a) -OR4 hvor R4 er som definert ovenfor, og b) ~N R6 hvor enten hver av R4 og R6 uavhengig er valgt fra gruppen som består av hydrogen, Cl-c6-al*yl< C5-C6-cykloalkyl og aryl, eller R5 og R6 , sammen med nitrogenatomet som det er bundet til, danner en pentatoroisk eller heksatomisk mettet heteromono- cyklisk ring, som eventuelt inneholder minst ett ytterligere heteroatom valgt blandt oksygen og nitrogen; og symbolet ( ---- 1 betyr en enkelt- eller en dobbeltbin- ding, samt farmasøytisk akseptable salter derav. Med henblikk på deres 5o-reduktasehemmende aktivitet kan forbindelsene ifolge oppfinnelsen være nyttige ved behandling av androgenavhengige tilstander.
NO91913923A 1990-02-09 1991-10-07 17beta-substituerte-4-aza-5alfa-androstan-3-on-derivater ogfremgangsmaate ved fremstilling av disse NO913923L (no)

Applications Claiming Priority (2)

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
PCT/EP1991/000228 WO1991012261A1 (en) 1990-02-09 1991-02-06 17β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONE DERIVATIVES AND PROCESS FOR THEIR PREPARATION

Publications (2)

Publication Number Publication Date
NO913923D0 NO913923D0 (no) 1991-10-07
NO913923L true NO913923L (no) 1991-12-06

Family

ID=10670693

Family Applications (1)

Application Number Title Priority Date Filing Date
NO91913923A NO913923L (no) 1990-02-09 1991-10-07 17beta-substituerte-4-aza-5alfa-androstan-3-on-derivater ogfremgangsmaate ved fremstilling av disse

Country Status (26)

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

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
US5543406A (en) * 1991-12-20 1996-08-06 Glaxo Wellcome, Inc. Inhibitors of 5-α-testosterone reductase
CZ283894A3 (en) * 1992-05-20 1995-09-13 Merck & Co Inc 7beta-substituted 4-aza-5alpha-cholestanones, their use for the preparation of pharmaceutical preparations and pharmaceutical compositions containing thereof
AU668180B2 (en) * 1992-05-20 1996-04-26 Merck & Co., Inc. 17-ethers and thioethers of 4-aza-steroids
CA2135173A1 (en) * 1992-05-20 1993-11-25 Bruce E. Witzel Ester derivatives of 4-aza-steroids
ES2149208T3 (es) * 1992-05-20 2000-11-01 Merck & Co Inc Inhibidores 4-azaesteroides de 5-alfa-reductasa.
WO1993023038A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. 17-AMINO SUBSTITUTED 4-AZASTEROID 5α-REDUCTASE INHIBITORS
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
TW239145B (no) * 1992-05-21 1995-01-21 Endorech Inc
GB9216329D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa 17beta-substituted 4-aza-5alpha-androstan-3-one derivatives
GB9216280D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa Steroids with a fluorinated acylureidic type side chain
GB9216284D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa Fluorinated 17beta-substituted 4-aza-5alpha-androstane-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
US5621104A (en) * 1993-03-24 1997-04-15 Merck & Co., Inc. Substituted 3-phenanthridinone derivatives as 5-alpha-reductase inhibitors
DE69405760T2 (de) * 1993-06-28 1998-04-09 Merck & Co Inc 4-aza-pregnan-5-alpha-reductase isozym 1 inhibitoren
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
EP0859617A1 (en) * 1995-09-27 1998-08-26 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
JP4563032B2 (ja) * 2002-01-15 2010-10-13 メルク・シャープ・エンド・ドーム・コーポレイション アンドロゲン受容体モジュレータとしての１７−ヒドロキシ−４−アザ−アンドロスタン−３−オン
KR100503193B1 (ko) * 2002-08-19 2005-07-25 한미약품 주식회사 3-옥소-4-아자-5α-안드로스탄 화합물의 선택적인 제조방법
CA2540407A1 (en) * 2003-09-25 2005-03-31 Tel Aviv University Future Technology Development L.P. Compositions and methods using same for treating amyloid-associated diseases
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

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CA970692A (en) * 1971-11-08 1975-07-08 Walter Voigt METHODS OF INHIBITING THE ACTIVITY OF TESTOSTERONE 5.alpha.-REDUCTASE
AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
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
IL97025A0 (en) 1992-03-29
ATE128143T1 (de) 1995-10-15
KR920701234A (ko) 1992-08-11
AU7230791A (en) 1991-09-03
CZ279484B6 (cs) 1995-05-17
JPH04505462A (ja) 1992-09-24
EP0468012A1 (en) 1992-01-29
FI914723A7 (fi) 1991-10-07
ES2080297T3 (es) 1996-02-01
GR3017996T3 (en) 1996-02-29
EP0468012B1 (en) 1995-09-20
ZA91918B (en) 1991-11-27
DE69113155T2 (de) 1996-02-29
HRP921221A2 (en) 1995-12-31
MY105402A (en) 1994-09-30
FI914723A0 (fi) 1991-10-07
HU913193D0 (en) 1992-01-28
RU2088589C1 (en) 1997-08-27
CN1054771A (zh) 1991-09-25
NZ237023A (en) 1993-01-27
US5155107A (en) 1992-10-13
PT96699A (pt) 1991-10-31
HUT59158A (en) 1992-04-28
NO913923D0 (no) 1991-10-07
GB9002922D0 (en) 1990-04-04
DE69113155D1 (de) 1995-10-26
AU642215B2 (en) 1993-10-14
CA2049318A1 (en) 1991-08-10
IL97025A (en) 1995-05-26
IE910408A1 (en) 1991-08-14
WO1991012261A1 (en) 1991-08-22
DK0468012T3 (da) 1995-11-06
CS9100274A2 (en) 1991-12-17

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