DE69113155T2 - 17-beta-substituierte-4-aza-5-alpha-androstan-3-one-derivate und verfahren zu ihrer herstellung. - Google Patents

17-beta-substituierte-4-aza-5-alpha-androstan-3-one-derivate und verfahren zu ihrer herstellung.

Info

Publication number
DE69113155T2
DE69113155T2 DE69113155T DE69113155T DE69113155T2 DE 69113155 T2 DE69113155 T2 DE 69113155T2 DE 69113155 T DE69113155 T DE 69113155T DE 69113155 T DE69113155 T DE 69113155T DE 69113155 T2 DE69113155 T2 DE 69113155T2
Authority
DE
Germany
Prior art keywords
alpha
androstan
aza
beta
derivatives
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.)
Expired - Fee Related
Application number
DE69113155T
Other languages
English (en)
Other versions
DE69113155D1 (de
Inventor
Achille Panzeri
Salle Enrico Di
Marcella Nesi
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.)
Pfizer Italia SRL
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 DE69113155D1 publication Critical patent/DE69113155D1/de
Application granted granted Critical
Publication of DE69113155T2 publication Critical patent/DE69113155T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related 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
    • 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)
DE69113155T 1990-02-09 1991-02-06 17-beta-substituierte-4-aza-5-alpha-androstan-3-one-derivate und verfahren zu ihrer herstellung. Expired - Fee Related DE69113155T2 (de)

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
DE69113155D1 DE69113155D1 (de) 1995-10-26
DE69113155T2 true DE69113155T2 (de) 1996-02-29

Family

ID=10670693

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69113155T Expired - Fee Related DE69113155T2 (de) 1990-02-09 1991-02-06 17-beta-substituierte-4-aza-5-alpha-androstan-3-one-derivate und verfahren zu ihrer herstellung.

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)

* Cited by examiner, † Cited by third party
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
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
DE69329856D1 (de) * 1992-05-20 2001-02-15 Merck & Co Inc Ester derivate von 4-aza-steroiden
EP0641204B1 (de) * 1992-05-20 2000-08-16 Merck & Co. Inc. 17-ether und thioether von 4-aza-steroiden
JPH07508035A (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５α−レダクターゼ阻害剤
RU94046044A (ru) * 1992-05-20 1996-10-10 Мерк Энд Ко. Новые 7 бета -замещенные 4-аза- 5 альфа -холестан-оны в качестве ингибиторов 5 альфа -редуктазы, фармацевтическая композиция на их основе, способ ее получения
JPH07508034A (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 １７−アミノ置換４−アザステロイド５α−レダクターゼ阻害剤
SK140494A3 (en) * 1992-05-21 1995-07-11 Endorecherche Inc Inhibitors of testosterone 5-alpha-reductase activity
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
AU7078296A (en) * 1995-09-27 1997-04-17 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
WO2005027901A1 (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
WO2023070071A2 (en) * 2021-10-21 2023-04-27 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
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
IL74365A (en) * 1984-02-27 1990-07-26 Merck & Co Inc 17beta-(n-t.-butylcarbamoyl)-4-aza-5alpha-androst-1-en-3-one and pharmaceutical compositions containing it
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
DE69113155D1 (de) 1995-10-26
IL97025A (en) 1995-05-26
ATE128143T1 (de) 1995-10-15
DK0468012T3 (da) 1995-11-06
IE910408A1 (en) 1991-08-14
WO1991012261A1 (en) 1991-08-22
MY105402A (en) 1994-09-30
US5155107A (en) 1992-10-13
AU642215B2 (en) 1993-10-14
IL97025A0 (en) 1992-03-29
ES2080297T3 (es) 1996-02-01
CA2049318A1 (en) 1991-08-10
HU913193D0 (en) 1992-01-28
GR3017996T3 (en) 1996-02-29
NO913923L (no) 1991-12-06
GB9002922D0 (en) 1990-04-04
RU2088589C1 (en) 1997-08-27
NZ237023A (en) 1993-01-27
CN1054771A (zh) 1991-09-25
NO913923D0 (no) 1991-10-07
CS9100274A2 (en) 1991-12-17
HUT59158A (en) 1992-04-28
ZA91918B (en) 1991-11-27
HRP921221A2 (en) 1995-12-31
PT96699A (pt) 1991-10-31
FI914723A0 (fi) 1991-10-07
AU7230791A (en) 1991-09-03
EP0468012A1 (de) 1992-01-29
EP0468012B1 (de) 1995-09-20
JPH04505462A (ja) 1992-09-24
KR920701234A (ko) 1992-08-11
CZ279484B6 (cs) 1995-05-17

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Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee