ES2118222T3 - Inhibidores de 5-alfa-testosterona reductasa. - Google Patents

Inhibidores de 5-alfa-testosterona reductasa.

Info

Publication number
ES2118222T3
ES2118222T3 ES93902691T ES93902691T ES2118222T3 ES 2118222 T3 ES2118222 T3 ES 2118222T3 ES 93902691 T ES93902691 T ES 93902691T ES 93902691 T ES93902691 T ES 93902691T ES 2118222 T3 ES2118222 T3 ES 2118222T3
Authority
ES
Spain
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 - Lifetime
Application number
ES93902691T
Other languages
English (en)
Inventor
Stephen Vernon Frye
Cynthia Markert Cribbs
Curt Dale Haffner
Patrick Reed Maloney
Robert Carl 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
Application granted granted Critical
Publication of ES2118222T3 publication Critical patent/ES2118222T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime 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

Abstract

LA PRESENTE INVENCION SE REFIERE A CIERTO SUSTITUYENTE 17BETA CARBONILO SUSTITUIDO-6-AZAANDROS-4-EN-3ONAS DE FORMULA (I), ESPECIALMENTE LOS DE FORMULA (IG) DONDE R1 Y R2 SON (I) INDEPENDIENTEMENTE HIDROGENO O ALQUILO INFERIOR Y EL ENLACE ENTRE LOS ATOMOS DE CARBONO QUE LLEVAN R1 Y R2 ES UN ENLACE SENCILLO O DOBLE, O II) TOMADOS JUNTOS SON UN GRUPO -CH2 ANILLO CICLOPROPANO, Y EL ENLACE ENTRE LOS ATOMOS DE CARBONO QUE LLEVAN R1 Y R2 ES UN ENLACE SENCILLO; R3 ES HIDROGENO; R4 ES HIDROGENO, ALQUILO INFERIOR, CICLOALQUILO INFERIOR, ALQUENILO INFERIOR, ALCANOILO DE 2-6 ATOMOS DE CARBONO, -(CH2)MCO2R16, -(CH2)MPARA, (CH2)N''CONT17R18, -(CH2)N''NR17R18 O -CH2)N''OR16, DONDE R16 ES HIDROGENO, ALQUILO INFERIOR O ALQUENILO INFERIOR, R17 Y R18 SON INDEPENDIENTEMENTE HIDROGENO, ALQUILO INFERIOR CICLOALQUILO O ALQUENILO INFERIOR; PARA ES UN GRUPO AROMATICO DE 6 A 12 ATOMOS DE CARBONO; N ES 0 O UN NUMERO ENTERO DE 1 A 5; M ES UN NUMERO ENTERO DE 1 A 5, R19 Y R20 SON INDEPENDIENTEMENTE HIDROGENO ALQUILO INFERIOR, O TOMADOS JUNTOS R19 Y R20 FORMAN UN GRUPO CARBONILO (=O); R5 ES ALQUILO INFERIOR, ALQUENILO INFERIOR, CICLOALQUILO INFERIOR, ALCOXI INFERIOR, O NR21R22, DONDE R21 Y R22 SON INDEPENDIENTEMENTE HIDROGENO, ALQUILO INFERIOR O ALQUENILO INFERIOR; Y SALES FARMACEUTICAMENTE ACEPTABLES DE ESTOS, SU PREPPARACION Y SU USO MEDICO Y FORMULACIONES FARMACEUTICAS.
ES93902691T 1991-12-20 1992-12-18 Inhibidores de 5-alfa-testosterona reductasa. Expired - Lifetime ES2118222T3 (es)

Applications Claiming Priority (4)

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

Publications (1)

Publication Number Publication Date
ES2118222T3 true ES2118222T3 (es) 1998-09-16

Family

ID=27487892

Family Applications (1)

Application Number Title Priority Date Filing Date
ES93902691T Expired - Lifetime ES2118222T3 (es) 1991-12-20 1992-12-18 Inhibidores de 5-alfa-testosterona reductasa.

Country Status (10)

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

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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
JPH11513684A (ja) * 1995-10-19 1999-11-24 メルク エンド カンパニー インコーポレーテッド １６−置換−６−アザ−ステロイド５α−レダクターゼ阻害剤
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
BRPI0409376A (pt) 2003-04-15 2006-04-25 Inflazyme Pharm Ltd derivados de indeno como agentes farmacêuticos
GB201102913D0 (en) 2011-02-18 2011-04-06 Univ Birmingham Novel therapeutic
CA2902764A1 (en) 2013-03-14 2014-09-18 Aquinox Pharmaceuticals (Canada) Inc. Ship1 modulators and methods related thereto
MX2015012111A (es) 2013-03-14 2016-05-05 Aquinox Pharmaceuticals Canada Inc Moduladores de ship1 y métodos relacionados con éstos.
CN107787315A (zh) 2015-06-26 2018-03-09 阿奎诺克斯药物（加拿大）公司 (1s,3s,4r)‑4‑((3as,4r,5s,7as)‑4‑(氨甲基)‑7a‑甲基‑1‑亚甲基八氢‑1h‑茚‑5‑基)‑3‑(羟甲基)‑4‑甲基环己醇的乙酸盐的结晶固体形式
AU2017209430A1 (en) 2016-01-20 2018-07-12 Aquinox Pharmaceuticals (Canada) Inc. Synthesis of a substituted indene derivative
BR112018072255B1 (pt) * 2016-04-29 2024-02-06 The Research Foundation For The State University Of New York Azasteroides para tratamento de tuberculose

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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
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DK465481A (da) * 1980-11-21 1982-05-22 Hoffmann La Roche Fremgangsmaade til fremstilling af d-homostemoider
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EP0314199B1 (en) * 1984-02-27 1991-09-18 Merck & Co. Inc. 17 beta-substituted-4-aza-5 alpha-androstenones and their use as 5 alpha-reductase inhibitors
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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
ATE78827T1 (de) * 1986-11-20 1992-08-15 Merck & Co Inc Topisches arzneimittel enthaltend 17-beta-methoxy-carbonyl-4-methyl-4-aza-5-alpha androst-1-en-3- one.
US5110939A (en) * 1987-01-28 1992-05-05 Smithkline Beecham Corporation Intermediates in the preparation of steriod 5-alpha-reductase inhibitors
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EP0285383B1 (en) * 1987-04-03 1994-03-16 Merck & Co. Inc. Treatment of prostatic carcinoma with 17beta-n-monosubstituted-carbamoyl-4-aza-5alpha-androst-1-en-3-ones
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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
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
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
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
AU637247B2 (en) * 1990-08-01 1993-05-20 Merrell Dow Pharmaceuticals Inc. 4-amino-delta4-steroids and their use as 5alpha-reductase inhibitors
NZ239141A (en) * 1990-08-01 1994-04-27 Merrell Dow Pharma 4-amino-delta-4,6-steroids; preparatory processes and pharmaceutical compositions
US5120847A (en) * 1990-08-27 1992-06-09 Merck & Co., Inc. Process for iodinating or brominating the α-methylenic carbon of a secondary amide
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
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CA2050824A1 (en) * 1990-09-24 1992-03-25 John M. Williams Process for making 3-oxo-4-aza-androst-1-ene 17-.beta.-ketones
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IE76452B1 (en) * 1990-10-29 1997-10-22 Sankyo Co Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use
DE69225244T2 (de) * 1991-12-20 1998-09-24 Glaxo Wellcome Inc Inhibitoren von testosteron-5-alpha 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
AU3417493A (en) 1993-07-28
CN1080639A (zh) 1994-01-12
ATE165368T1 (de) 1998-05-15
DE69225244D1 (de) 1998-05-28
WO1993013124A1 (en) 1993-07-08
US5543406A (en) 1996-08-06
CA2126203A1 (en) 1993-07-08
JPH07502511A (ja) 1995-03-16
EP0641356B1 (en) 1998-04-22
DE69225244T2 (de) 1998-09-24
EP0641356A1 (en) 1995-03-08

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