DE69225244D1 - Inhibitoren von testosteron-5-alpha reductase. - Google Patents

Inhibitoren von testosteron-5-alpha reductase.

Info

Publication number
DE69225244D1
DE69225244D1 DE69225244T DE69225244T DE69225244D1 DE 69225244 D1 DE69225244 D1 DE 69225244D1 DE 69225244 T DE69225244 T DE 69225244T DE 69225244 T DE69225244 T DE 69225244T DE 69225244 D1 DE69225244 D1 DE 69225244D1
Authority
DE
Germany
Prior art keywords
lower alkyl
pct
hydrogen
independently hydrogen
carbons
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
DE69225244T
Other languages
English (en)
Other versions
DE69225244T2 (de
Inventor
Stephen Frye
Cynthia Cribbs
Curt Haffner
Patrick Maloney
Robert Andrews
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.)
SmithKline Beecham Corp
Original Assignee
Glaxo Wellcome 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 Glaxo Wellcome Inc filed Critical Glaxo Wellcome Inc
Publication of DE69225244D1 publication Critical patent/DE69225244D1/de
Application granted granted Critical
Publication of DE69225244T2 publication Critical patent/DE69225244T2/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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)
DE69225244T 1991-12-20 1992-12-18 Inhibitoren von testosteron-5-alpha reductase. Expired - Fee Related DE69225244T2 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US81225791A 1991-12-20 1991-12-20
US90526292A 1992-06-26 1992-06-26
US93010192A 1992-08-13 1992-08-13
US3138192A 1992-12-11 1992-12-11
PCT/US1992/011109 WO1993013124A1 (en) 1991-12-20 1992-12-18 Inhibitors of 5-alpha-testosterone reductase

Publications (2)

Publication Number Publication Date
DE69225244D1 true DE69225244D1 (de) 1998-05-28
DE69225244T2 DE69225244T2 (de) 1998-09-24

Family

ID=27487892

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69225244T Expired - Fee Related DE69225244T2 (de) 1991-12-20 1992-12-18 Inhibitoren von testosteron-5-alpha reductase.

Country Status (10)

Country Link
US (1) US5543406A (de)
EP (1) EP0641356B1 (de)
JP (1) JPH07502511A (de)
CN (1) CN1080639A (de)
AT (1) ATE165368T1 (de)
AU (1) AU3417493A (de)
CA (1) CA2126203A1 (de)
DE (1) DE69225244T2 (de)
ES (1) ES2118222T3 (de)
WO (1) WO1993013124A1 (de)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU3417493A (en) * 1991-12-20 1993-07-28 Glaxo Inc. Inhibitors of 5-alpha-testosterone reductase
WO1993023420A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS
AP459A (en) * 1992-12-18 1996-02-14 Glaxo Wellcome Inc Substituted 6-azaandrostenones.
US5438061A (en) * 1993-07-16 1995-08-01 Merck & Co., Inc. 7-substituted-δ4-6-azasteroid derivatives as 5α-reductase inhibitors
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US5708001A (en) * 1993-12-17 1998-01-13 Glaxo Wellcome Inc. Substituted 6-azaandrostenones
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
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
WO1997014418A1 (en) * 1995-10-19 1997-04-24 Merck & Co., Inc. 16-substituted-6-aza-steroid 5-alpha-reductase inhibitors
US5935968A (en) 1997-03-17 1999-08-10 Merck & Co., Inc. Methods for treating polycystic ovary syndrome
JP3774888B2 (ja) * 2001-11-28 2006-05-17 日本化薬株式会社 ステロイド類化合物のｌｃ−ｍｓによる高感度検出法
JP2006517579A (ja) * 2003-02-11 2006-07-27 ワーナー−ランバート カンパニー リミティド ライアビリティー カンパニー アンドロゲンアンタゴニストとして有用なベンジル尿素およびチオ尿素誘導体
DE602004031410D1 (de) 2003-04-15 2011-03-31 Aquinox Pharmaceuticals Inc Inden derivate als pharmazeutika
GB201102913D0 (en) 2011-02-18 2011-04-06 Univ Birmingham Novel therapeutic
JP6407951B2 (ja) 2013-03-14 2018-10-17 アクイノックス ファーマシューティカルズ （カナダ） インコーポレイテッド Ｓｈｉｐ１モジュレーターおよびそれに関連する組成物および方法
WO2014143561A1 (en) 2013-03-14 2014-09-18 Aquinox Pharmaceuticals Inc. Ship1 modulators and methods related thereto
JP2018518494A (ja) 2015-06-26 2018-07-12 アクイノックス ファーマシューティカルズ （カナダ） インコーポレイテッド （１Ｓ，３Ｓ，４Ｒ）−４−（（３ａＳ，４Ｒ，５Ｓ，７ａＳ）−４−（アミノメチル）−７ａ−メチル−１−メチレンオクタヒドロ−１Ｈ−インデン−５−イル）−３−（ヒドロキシメチル）−４−メチルシクロヘキサノールの酢酸塩の結晶固体形態
US10053415B2 (en) 2016-01-20 2018-08-21 Aquinox Pharmaceuticals (Canada) Inc. Synthesis of a substituted indene derivative
EP3448869A4 (de) * 2016-04-29 2020-01-08 The Research Foundation for The State University of New York Azasteroide zur behandlung von tuberkulose

Family Cites Families (36)

* 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
US4191759A (en) * 1978-04-13 1980-03-04 Merck & Co., Inc. N-substituted-17β-carbamoylandrost-4-en-3-one 5α reductase inhibitors
AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
DK465481A (da) * 1980-11-21 1982-05-22 Hoffmann La Roche Fremgangsmaade til fremstilling af d-homostemoider
EP0314199B1 (de) * 1984-02-27 1991-09-18 Merck & Co. Inc. 17-Beta-substituierte-4-aza-5-alpha-Androstenone und ihre Anwendung als 5-Alpha-Reduktase-Inhibitoren
US5049562A (en) * 1984-02-27 1991-09-17 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α-reductase inhibitors
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
EP0271219B1 (de) * 1986-11-20 1992-07-29 Merck & Co. Inc. Topisches Arzneimittel enthaltend 17-beta-Methoxy-carbonyl-4-methyl-4-aza-5-alpha-androst-1-en-3-one
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
US5110939A (en) * 1987-01-28 1992-05-05 Smithkline Beecham Corporation Intermediates in the preparation of steriod 5-alpha-reductase inhibitors
US4888336A (en) * 1987-01-28 1989-12-19 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
DE3888378T2 (de) * 1987-04-03 1994-09-29 Merck & Co Inc Behandlung von Prostatacarcinoma mit 17-beta-n-monosubstituierten-Carbamoyl-4-aza-5-alpha-Androst-1-en-3-onen.
ZA883034B (en) * 1987-04-29 1989-03-29 Smithkline Beckman Corp Steroid 5-alpha-reductase inhibitors
US4937237A (en) * 1988-12-23 1990-06-26 Smithkline Beckman Corporation Phosphinic acid substituted aromatic steroids as inhibitors of steroid 5-60 -reductase
US4882319A (en) * 1988-12-23 1989-11-21 Smithkline Beckman Corporation Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase
CA2023157A1 (en) * 1989-08-21 1991-02-22 Gary H. Rasmusson 17 beta-acyl-4-aza-5 alpha-androst-1-ene-3-ones as 5 alpha-reductase inhibitors
US5021575A (en) * 1989-11-13 1991-06-04 Merck & Co., Inc. Method for introducing a 1,2 double bond into azasteroids
US5100917A (en) * 1989-12-29 1992-03-31 Merrell Dow Pharmaceuticals Inc. Novel a-nor-steroid-3-carboxylic acid derivatives
GB9002922D0 (en) * 1990-02-09 1990-04-04 Erba Carlo Spa 17 beta-substituted-4-aza-5 alpha-androstan-3-one derivatives and process for their preparation
US5061802A (en) * 1990-06-20 1991-10-29 Merck & Co. Inc. 17β-aminobenzoyl-4-aza-5α-androst-1-en-3-ones as benign prostatic hypertrophy agents
EP0462665A3 (en) * 1990-06-20 1993-06-30 Merck & Co. Inc. Selected 17beta-polyaroyl-4-aza-5alpha-androst-1-en-3-ones as steroidal reductase inhibitors
EP0462662A3 (en) * 1990-06-20 1992-08-19 Merck & Co. Inc. 17beta-n-monosubstituted adamantyl/norbornanyl carbamoyl-4-aza-5alpha-androst-1-en-3-ones and androstan-3-ones
EP0462664A3 (en) * 1990-06-20 1992-11-25 Merck & Co. Inc. Specific 17beta-thiobenzoyl-4-aza-5alpha-androst-1-en-3-ones as antiandrogenic agents
US5098908A (en) * 1990-06-20 1992-03-24 Merck & Co., Inc. 17β-hydroxybenzoyl-4-aza-5α-androst-1-en-3-ones as testosterone reductase inhibitors
AU642757B2 (en) * 1990-08-01 1993-10-28 Merrell Dow Pharmaceuticals Inc. 4-amino-delta4, 6-steroids and their use as 5alpha-reductase inhibitors
NZ239142A (en) * 1990-08-01 1994-05-26 Merrell Dow Pharma 4-amino-delta-4-steroids; preparatory processes and pharmaceutical compositions
US5091534A (en) * 1990-08-27 1992-02-25 Merck & Co., Inc. Trialkylsilyl trifluoromethanesulfonate mediated α-methylenic carbon functionalization of 4-AZA-5α-androstan-3-one steroids
US5120847A (en) * 1990-08-27 1992-06-09 Merck & Co., Inc. Process for iodinating or brominating the α-methylenic carbon of a secondary amide
US5061803A (en) * 1990-09-24 1991-10-29 Merck & Co., Inc. Process for making 17-beta alkanoyl 3-oxo-4-aza-5-α-androst-1-enes
US5061801A (en) * 1990-09-24 1991-10-29 Merck & Co., Inc. Intermediate for making 3-oxo-4-aza-androst-1-ene 17β-ketones
CA2050824A1 (en) * 1990-09-24 1992-03-25 John M. Williams Process for making 3-oxo-4-aza-androst-1-ene 17-.beta.-ketones
IE76452B1 (en) * 1990-10-29 1997-10-22 Sankyo Co Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use
AU3417493A (en) * 1991-12-20 1993-07-28 Glaxo Inc. Inhibitors of 5-alpha-testosterone reductase
US5302589A (en) * 1992-08-07 1994-04-12 Glaxo, Inc. Heterocyclic inhibitors of 5-α-testosterone reductase
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
EP0641356A1 (de) 1995-03-08
ES2118222T3 (es) 1998-09-16
US5543406A (en) 1996-08-06
AU3417493A (en) 1993-07-28
CN1080639A (zh) 1994-01-12
ATE165368T1 (de) 1998-05-15
WO1993013124A1 (en) 1993-07-08
JPH07502511A (ja) 1995-03-16
CA2126203A1 (en) 1993-07-08
EP0641356B1 (de) 1998-04-22
DE69225244T2 (de) 1998-09-24

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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