ATE171188T1 - In 15-stellung substituierte 4-azasteroide - Google Patents

In 15-stellung substituierte 4-azasteroide

Info

Publication number: ATE171188T1
Authority: AT; Austria
Prior art keywords: group; alkyl; hydrogen; azasteroids; substituted
Prior art date: 1993-03-12

Application number

AT94911577T

Other languages

English (en)

Inventor

Philippe L Durette

Craig K Esser

William Hagmann

Ihor E Kopka

Original Assignee

Merck & Co 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.)

1993-03-12

Filing date

1994-03-11

Publication date

1998-10-15

1994-03-11 Application filed by Merck & Co Inc filed Critical Merck & Co Inc

1998-10-15 Application granted granted Critical

1998-10-15 Publication of ATE171188T1 publication Critical patent/ATE171188T1/de

Links

150000000520 4-azasteroids Chemical group 0.000 title 1
125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 4
229910052739 hydrogen Inorganic materials 0.000 abstract 3
239000001257 hydrogen Substances 0.000 abstract 3
125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
125000003545 alkoxy group Chemical group 0.000 abstract 2
150000001875 compounds Chemical class 0.000 abstract 2
108010029908 3-oxo-5-alpha-steroid 4-dehydrogenase Proteins 0.000 abstract 1
102000001779 3-oxo-5-alpha-steroid 4-dehydrogenase Human genes 0.000 abstract 1
125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
239000005557 antagonist Substances 0.000 abstract 1
125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
125000004093 cyano group Chemical group *C#N 0.000 abstract 1
150000002148 esters Chemical class 0.000 abstract 1
125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
150000003839 salts Chemical class 0.000 abstract 1

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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/28—Antiandrogens
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0003—Androstane derivatives
- C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J21/001—Lactones
- C07J21/003—Lactones at position 17
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00

Landscapes

Organic Chemistry (AREA)
Chemical & Material Sciences (AREA)
Health & Medical Sciences (AREA)
General Health & Medical Sciences (AREA)
Engineering & Computer Science (AREA)
Pharmacology & Pharmacy (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Medicinal Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
Endocrinology (AREA)
Diabetes (AREA)
Animal Behavior & Ethology (AREA)
Bioinformatics & Cheminformatics (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Steroid Compounds (AREA)
Saccharide Compounds (AREA)

AT94911577T 1993-03-12 1994-03-11 In 15-stellung substituierte 4-azasteroide ATE171188T1 (de)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US08/030,508 US5359071A (en)	1993-03-12	1993-03-12	15-substituted 4-azasteroids

Publications (1)

Publication Number	Publication Date
ATE171188T1 true ATE171188T1 (de)	1998-10-15

Family

ID=21854519

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
AT94911577T ATE171188T1 (de)	1993-03-12	1994-03-11	In 15-stellung substituierte 4-azasteroide

Country Status (9)

Country	Link
US (1)	US5359071A (de)
EP (1)	EP0700291B1 (de)
JP (1)	JP3337689B2 (de)
AT (1)	ATE171188T1 (de)
AU (1)	AU674222B2 (de)
CA (1)	CA2157363A1 (de)
DE (1)	DE69413393T2 (de)
ES (1)	ES2122258T3 (de)
WO (1)	WO1994020104A1 (de)

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AU4251993A (en) *	1992-05-20	1993-12-13	Merck & Co., Inc.	Substituted 4-aza-5A-androstan-ones as 5A-reductase inhibitors
HUT71484A (en) *	1992-05-20	1995-11-28	Merck & Co Inc	Process for producing of 7beta-substituted-4-aza-5alpha-cholestan-ones as 5-alpha-reductase inhibitors and pharmaceuticals compositions containing them
JP3300359B2 (ja) *	1993-06-24	2002-07-08	リチュテル・ゲデオン・ヴェジェーセティ・ジャール・エルテー	１７−ハロゲノ−４−アザアンドロステン誘導体およびその製造方法
NZ275293A (en)	1993-10-21	1998-02-26	Merck & Co Inc	16-substituted-4-aza-androstanes for use as 5-alpha-reductase isozyme 1 inhibitors
US5525608A (en) *	1994-04-20	1996-06-11	Merck & Co., Inc.	17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors
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
JPH10508586A (ja) *	1994-10-21	1998-08-25	メルクエンドカンパニーインコーポレーテッド	組み合わせ式アクネ治療方法
US5595996A (en) *	1994-10-25	1997-01-21	Merck & Co., Inc.	7-substituted 4-aza cholanic acid derivatives and their use
US5656613A (en) *	1995-01-04	1997-08-12	Merck & Co., Inc.	Treatment of hyperandrogenic conditions
US5811510A (en) *	1995-04-14	1998-09-22	General Hospital Corporation	Biodegradable polyacetal polymers and methods for their formation and use
CA2231434A1 (en) *	1995-09-27	1997-04-03	Glenn J. Gormley	Method of preventing androgenetic alopecia with 5-.alpha. reductase inhibitors
US5763361A (en) *	1995-10-23	1998-06-09	Merck & Co., Inc.	17-alkyl-7-substituted-4-aza steroid derivatives as 5-α-reductase inhibitors
US6365597B1 (en)	1996-02-14	2002-04-02	Aventis Pharmaceuticals Inc.	4-aza steroids
US5872126A (en) *	1996-09-06	1999-02-16	Merck & Co., Inc.	Methods and compositions for treating preterm labor
WO1998041509A1 (en) *	1997-03-17	1998-09-24	Merck & Co., Inc.	Methods and compositions for treating polycystic ovary syndrome
US5935968A (en) *	1997-03-17	1999-08-10	Merck & Co., Inc.	Methods for treating polycystic ovary syndrome
EP1321146A3 (de) *	1998-03-11	2004-06-02	Endorecherche Inc.	Typ 5 und Typ 3 17 Beta-Hydroxisteroid-Dehydrogenasehemmer und Verfahren zu ihrer Anwendung
KR100872722B1 (ko) *	2002-06-28	2008-12-05	주식회사 중외제약	피나스테라이드의 제조방법
US7519874B2 (en) *	2002-09-30	2009-04-14	Lecroy Corporation	Method and apparatus for bit error rate analysis
JP4832303B2 (ja) *	2003-05-07	2011-12-07	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およびこれらの使用
PL2300489T3 (pl)	2008-06-06	2016-11-30		Sposoby wytwarzania 17-alkinylo-7-hydroksysteroidów i związków pokrewnych

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US2227876A (en) *	1937-10-16	1941-01-07	Firm Of N V Organon	Steroid derivatives with nuclear substituted nitrogen
US3285918A (en) *	1962-04-18	1966-11-15	Norman J Doorenbos	1', 4', 5', 6'-tetrahydropyrimidino[a-4, 3]-4-aza-5-cholestene
US3239417A (en) *	1962-12-07	1966-03-08	Smith Kline French Lab	Methods and compositions for inhibiting sterol biosynthesis
US3264301A (en) *	1963-08-22	1966-08-02	Norman J Doorenbos	Substituted-4-azasteroids
FR1465544A (fr) *	1965-11-29	1967-01-13	Roussel Uclaf	Dérivés stéroïdes aromatiques substitués par un atome d'azote endocyclique et procédé de préparation
CA970692A (en) *	1971-11-08	1975-07-08	Walter Voigt	METHODS OF INHIBITING THE ACTIVITY OF TESTOSTERONE 5.alpha.-REDUCTASE
US4596812A (en) *	1976-05-24	1986-06-24	The Upjohn Company	Methods and solutions for treating male pattern alopecia
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
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
US5151429A (en) *	1984-02-27	1992-09-29	Merck & Co., Inc.	17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α reductase inhibitors
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
US5138063A (en) *	1984-02-27	1992-08-11	Merck & Co., Inc.	17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
US4760071A (en) *	1984-02-27	1988-07-26	Merck & Co., Inc.	17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors
ATE67503T1 (de) *	1984-02-27	1991-10-15	Merck & Co Inc	17-beta-substituierte-4-aza-5-alpha-androstenon und ihre anwendung als 5-alpha-reduktaseinhibitoren.
NZ211145A (en) *	1984-02-27	1988-10-28	Merck & Co Inc	4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions
US4859681A (en) *	1984-02-27	1989-08-22	Merck & Co., Inc.	17 α-Acyl-4-aza-5a-androst-1-en-3-ones as 5 alpha-reductase inhibitors
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
US4888336A (en) *	1987-01-28	1989-12-19	Smithkline Beckman Corporation	Steroid 5-alpha-reductase inhibitors
DE3888994T2 (de) *	1987-04-03	1994-11-03	Merck & Co Inc	Behandlung von androgener Alopecia mit 17-beta-n-mono-substituierten-carbamoyl-4-aza-5-alpha-androst-1-en-3-onen.
US4910226A (en) *	1987-04-29	1990-03-20	Smithkline Beckman Corporation	Steroid 5-alpha-reductase inhibitors
WO1989011282A1 (en) *	1988-05-25	1989-11-30	Smithkline Beckman Corporation	AROMATIC STEROID 5-alpha-REDUCTASE INHIBITORS
US5026882A (en) *	1988-12-23	1991-06-25	Smithkline Beecham Corporation	Phosphinic acid substituted steroids as inhibitors of steroid 5α-reductase
US4937237A (en) *	1988-12-23	1990-06-26	Smithkline Beckman Corporation	Phosphinic acid substituted aromatic steroids as inhibitors of steroid 5-60 -reductase
US4970205A (en) *	1988-12-23	1990-11-13	Smithkline Beecham Corporation	Sulfonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase
US4882319A (en) *	1988-12-23	1989-11-21	Smithkline Beckman Corporation	Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase
US5021575A (en) *	1989-11-13	1991-06-04	Merck & Co., Inc.	Method for introducing a 1,2 double bond into azasteroids
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
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

1993
- 1993-03-12 US US08/030,508 patent/US5359071A/en not_active Expired - Lifetime
1994
- 1994-03-11 ES ES94911577T patent/ES2122258T3/es not_active Expired - Lifetime
- 1994-03-11 JP JP52035094A patent/JP3337689B2/ja not_active Expired - Fee Related
- 1994-03-11 AU AU64065/94A patent/AU674222B2/en not_active Ceased
- 1994-03-11 DE DE69413393T patent/DE69413393T2/de not_active Expired - Fee Related
- 1994-03-11 EP EP94911577A patent/EP0700291B1/de not_active Expired - Lifetime
- 1994-03-11 CA CA002157363A patent/CA2157363A1/en not_active Abandoned
- 1994-03-11 AT AT94911577T patent/ATE171188T1/de active
- 1994-03-11 WO PCT/US1994/002697 patent/WO1994020104A1/en not_active Ceased

Also Published As

Publication number	Publication date
JPH08507535A (ja)	1996-08-13
AU674222B2 (en)	1996-12-12
US5359071A (en)	1994-10-25
CA2157363A1 (en)	1994-09-15
WO1994020104A1 (en)	1994-09-15
EP0700291A1 (de)	1996-03-13
AU6406594A (en)	1994-09-26
JP3337689B2 (ja)	2002-10-21
ES2122258T3 (es)	1998-12-16
DE69413393T2 (de)	1999-05-12
DE69413393D1 (de)	1998-10-22
EP0700291B1 (de)	1998-09-16
EP0700291A4 (de)	1996-07-03

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