PT86652A - Steroid 5-alpha-reductase inhibitors - Google Patents

Steroid 5-alpha-reductase inhibitors

Info

Publication number: PT86652A
Authority: PT; Portugal
Prior art keywords: alpha; steroid; reductase inhibitors; double bond; reductase
Prior art date: 1987-01-28

Application number

PT86652A

Other languages

English (en)

Other versions

PT86652B (pt

Inventor

Dennis Alan Holt

Mark Alan Levy

Brian Walter Metcalf

Original Assignee

Smithkline Beckman Corp

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.)

1987-01-28

Filing date

1988-01-28

Publication date

1988-02-01

1988-01-28 Application filed by Smithkline Beckman Corp filed Critical Smithkline Beckman Corp

1988-02-01 Publication of PT86652A publication Critical patent/PT86652A/pt

1992-02-28 Publication of PT86652B publication Critical patent/PT86652B/pt

Links

239000002677 5-alpha reductase inhibitor Substances 0.000 title 1
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
239000003112 inhibitor Substances 0.000 abstract 1
238000000034 method Methods 0.000 abstract 1
239000008194 pharmaceutical composition Substances 0.000 abstract 1
-1 substituted-androsten-3-ones Chemical class 0.000 abstract 1
238000002560 therapeutic procedure Methods 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
- C07J31/003—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring the S atom directly linked to a ring carbon atom of the cyclopenta(a)hydrophenanthrene skeleton
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
- C07J3/005—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
- 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
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/02—Ortho- or ortho- and peri-condensed systems
- C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
- C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
- C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
- C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
- C07C2603/16—Benz[e]indenes; Hydrogenated benz[e]indenes

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)
Steroid Compounds (AREA)

PT86652A 1987-01-28 1988-01-28 Processo de preparacao de inibidores do esteroide 5-alfa-reductase e dos seus intermediarios PT86652B (pt)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US07/007,539 US4888336A (en)	1987-01-28	1987-01-28	Steroid 5-alpha-reductase inhibitors

Publications (2)

Publication Number	Publication Date
PT86652A true PT86652A (pt)	1988-02-01
PT86652B PT86652B (pt)	1992-02-28

Family

ID=21726780

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
PT86652A PT86652B (pt)	1987-01-28	1988-01-28	Processo de preparacao de inibidores do esteroide 5-alfa-reductase e dos seus intermediarios

Country Status (13)

Country	Link
US (1)	US4888336A (pt)
EP (1)	EP0277002B1 (pt)
JP (1)	JPS63192800A (pt)
AT (1)	ATE77388T1 (pt)
AU (1)	AU608560B2 (pt)
CA (1)	CA1325006C (pt)
DE (1)	DE3871965T2 (pt)
DK (4)	DK168525B1 (pt)
ES (1)	ES2042725T3 (pt)
GR (1)	GR3005284T3 (pt)
IE (1)	IE61594B1 (pt)
PT (1)	PT86652B (pt)
ZA (1)	ZA88549B (pt)

Families Citing this family (53)

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US5138063A (en) *	1984-02-27	1992-08-11	Merck & Co., Inc.	17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
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US4814324A (en) *	1987-03-06	1989-03-21	Merck & Co., Inc.	Sterol inhibitors of testosterone 5α-reductase
US5595985A (en) *	1989-03-10	1997-01-21	Endorecherche Inc.	Combination therapy for prophylaxis and/or treatment of benign prostatic hyperplasia
US5372996A (en) *	1989-03-10	1994-12-13	Endorecherche, Inc.	Method of treatment of androgen-related diseases
US5405978A (en) *	1989-05-30	1995-04-11	The Upjohn Company	Oxidative preparation of 3,5-secoandrost-5-one-3,17 β-dioic acid
EP0943328B1 (en) *	1989-07-07	2004-06-16	Endorecherche Inc.	Combination therapy for prophylaxis and/or treatment of benign prostatic hyperplasia
AU5856090A (en) *	1989-07-07	1991-02-06	Endorecherche Inc.	Androgen derivatives for use in the inhibition of sex steroid activity
ES2189784T3 (es) *	1989-07-07	2003-07-16	Endorech Inc	Procedimiento para el tratamiento de enfermedades relacionadas con adrogenos.
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
US5151430A (en) *	1990-06-20	1992-09-29	Merck & Co., Inc.	Specific 17β-thiobenzoyl-4-aza-5α-androst-1-en-3-ones as antiandrogen agents
US5162332A (en) *	1990-06-20	1992-11-10	Merck & Co., Inc.	Selected 17 β-polyaroyl-4-aza-5 α-androst-1-en-3-ones as steroidal reductase inhibitors
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
US5091380A (en) *	1990-06-28	1992-02-25	Merck & Co., Inc.	N-monosubstituted adamantyl/norbornanyl 17β-carbamides of 3-carboxy-androst-3,5-dienes as testosterone 5α-reductase inhibitors
NZ241979A (en) *	1991-03-20	1996-01-26	Merck & Co Inc	Treatment of benign prostatic hyperplasia using 5alpha-reductase inhibitor and an alpha1-adrenergic recepter blocker
US5250539A (en) *	1991-08-21	1993-10-05	Eli Lilly And Company	Hexahydrobenzo[f]quinolinones
US5304562A (en) *	1991-10-09	1994-04-19	Ciba-Geigy Corporation	17β-substituted Aza-androstane 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
EP0547687A1 (en) *	1991-12-18	1993-06-23	Merck & Co. Inc.	17B-N-Substituted adamantyl/norbonanyl carbamoyl-4-aza-5a-and-rost-1-en-3-ones and androstan-3 ones
EP0641356B1 (en) *	1991-12-20	1998-04-22	Glaxo Wellcome 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
WO1993023038A1 (en) *	1992-05-20	1993-11-25	Merck & Co., Inc.	17-AMINO SUBSTITUTED 4-AZASTEROID 5α-REDUCTASE INHIBITORS
EP0641209A4 (en) *	1992-05-20	1995-08-23	Merck & Co Inc	NEW 17-ESTER, AMID AND KETONE DERIVATIVES OF 3-OXO-4-AZASTEROIDS AS 5-ALPHA REDUCTINE INHIBITORS.
US5510351A (en) *	1992-05-20	1996-04-23	Merck & Co., Inc.	Delta-17 and delta-20 olefinic and saturated 17 beta-substituted 4-aza-5 alpha-androstan-ones as 5 alpha reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders
CA2135173A1 (en) *	1992-05-20	1993-11-25	Bruce E. Witzel	Ester derivatives of 4-aza-steroids
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
AU668180B2 (en) *	1992-05-20	1996-04-26	Merck & Co., Inc.	17-ethers and thioethers of 4-aza-steroids
AU4251993A (en) *	1992-05-20	1993-12-13	Merck & Co., Inc.	Substituted 4-aza-5A-androstan-ones as 5A-reductase inhibitors
US5710275A (en) *	1992-05-20	1998-01-20	Merck & Co., Inc.	7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
AU672978B2 (en) *	1992-05-20	1996-10-24	Merck & Co., Inc.	4-azasteroid 5-alpha-reductase inhibitors
AU680818B2 (en) *	1992-05-21	1997-08-14	Endorecherche Inc.	Improved antiandrogens
GB9210880D0 (en) *	1992-05-21	1992-07-08	Smithkline Beecham Corp	Compounds
JPH07506575A (ja) *	1992-05-21	1995-07-20	アンドルシェルシュ・インコーポレイテッド	テストステロン５α−レダクターゼ活性の阻害剤
GB9213901D0 (en) *	1992-06-30	1992-08-12	Smithkline Beecham Corp	Compounds
US5302589A (en) *	1992-08-07	1994-04-12	Glaxo, Inc.	Heterocyclic inhibitors of 5-α-testosterone reductase
US5324734A (en) *	1992-09-15	1994-06-28	Merck & Co., Inc.	Oxidization metabolites of 5-α-23-methyl-4-aza-21-nor-chol-1-ene-3, 20-dione
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
AU679769B2 (en) *	1993-06-28	1997-07-10	Merck & Co., Inc.	4-AZA-pregnane 5alpha-reductase isozyme 1 inhibitors
TW408127B (en) *	1993-09-17	2000-10-11	Glaxo Inc	Androstenones
TW369521B (en) *	1993-09-17	1999-09-11	Smithkline Beecham Corp	Androstenone derivative
US5817818A (en) *	1994-09-16	1998-10-06	Glaxo Wellcome Inc.	Androstenones
US5541322A (en) *	1994-10-14	1996-07-30	Glaxo Wellcome Inc.	Synthesis of 6-azaandrostenones
US5595996A (en) *	1994-10-25	1997-01-21	Merck & Co., Inc.	7-substituted 4-aza cholanic acid derivatives and their use
US6365597B1 (en) *	1996-02-14	2002-04-02	Aventis Pharmaceuticals Inc.	4-aza steroids
US5998427A (en) *	1998-05-14	1999-12-07	Glaxo Wellcome Inc.	Androstenones
ATE473759T1 (de)	1998-05-22	2010-07-15	Univ Leland Stanford Junior	Bifunktionelle moleküle sowie darauf basierende therapien.
CN102379684B (zh)	2005-04-28	2014-11-19	普罗透斯数字保健公司	药物信息系统
US9062126B2 (en)	2005-09-16	2015-06-23	Raptor Pharmaceuticals Inc.	Compositions comprising receptor-associated protein (RAP) variants specific for CR-containing proteins and uses thereof
EP2398500B1 (en)	2009-02-20	2019-03-13	2-BBB Medicines B.V.	Glutathione-based drug delivery system
ES2942923T3 (es)	2009-05-06	2023-06-07	Laboratory Skin Care Inc	Composiciones de administración dérmica que comprenden complejos de agente activo-partículas de fosfato de calcio y métodos de uso de las mismas

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US2897202A (en) *	1956-03-19	1959-07-28	Monsanto Chemicals	3-keto-4-aza-delta5-steroids and method of preparing same
US4191759A (en) *	1978-04-13	1980-03-04	Merck & Co., Inc.	N-substituted-17β-carbamoylandrost-4-en-3-one 5α reductase inhibitors
KR830000085B1 (ko) *	1978-04-13	1983-02-08	제임스 에프. 너우톤	5α-환원효소 억제제로서 유용한 4-아자-17-치환-5α-안드로스탄-3-온류의 제조방법
US4377584A (en) *	1978-04-13	1983-03-22	Merck & Co., Inc.	4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
AU527030B2 (en) *	1978-04-13	1983-02-10	Merck & Co., Inc.	4-aza-17-substituted-5a-androstan-3-ones
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
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
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

1987
- 1987-01-28 US US07/007,539 patent/US4888336A/en not_active Expired - Fee Related
1988
- 1988-01-26 DK DK037388D patent/DK168525B1/da not_active IP Right Cessation
- 1988-01-26 DK DK037388A patent/DK37388A/da not_active IP Right Cessation
- 1988-01-26 IE IE18988A patent/IE61594B1/en not_active IP Right Cessation
- 1988-01-27 CA CA000557453A patent/CA1325006C/en not_active Expired - Fee Related
- 1988-01-27 AU AU10778/88A patent/AU608560B2/en not_active Ceased
- 1988-01-27 ZA ZA880549A patent/ZA88549B/xx unknown
- 1988-01-27 AT AT88300697T patent/ATE77388T1/de not_active IP Right Cessation
- 1988-01-27 EP EP88300697A patent/EP0277002B1/en not_active Expired - Lifetime
- 1988-01-27 DE DE8888300697T patent/DE3871965T2/de not_active Expired - Fee Related
- 1988-01-27 JP JP63016790A patent/JPS63192800A/ja active Pending
- 1988-01-27 ES ES88300697T patent/ES2042725T3/es not_active Expired - Lifetime
- 1988-01-28 PT PT86652A patent/PT86652B/pt not_active IP Right Cessation
1991
- 1991-12-05 DK DK196691A patent/DK169438B1/da not_active IP Right Cessation
1992
- 1992-07-29 GR GR920401614T patent/GR3005284T3/el unknown
1994
- 1994-06-21 DK DK073594A patent/DK169840B1/da not_active IP Right Cessation

Also Published As

Publication number	Publication date
EP0277002A3 (en)	1988-10-26
CA1325006C (en)	1993-12-07
DK73594A (da)	1994-06-21
EP0277002B1 (en)	1992-06-17
DK168525B1 (da)	1994-04-11
DK196691D0 (da)	1991-12-05
AU608560B2 (en)	1991-04-11
IE880189L (en)	1988-07-28
PT86652B (pt)	1992-02-28
US4888336A (en)	1989-12-19
AU1077888A (en)	1988-08-04
ATE77388T1 (de)	1992-07-15
ZA88549B (en)	1988-07-27
DK37388A (da)	1988-07-29
ES2042725T3 (es)	1993-12-16
DK37388D0 (da)	1988-01-26
DK169438B1 (da)	1994-10-31
JPS63192800A (ja)	1988-08-10
IE61594B1 (en)	1994-11-16
GR3005284T3 (pt)	1993-05-24
EP0277002A2 (en)	1988-08-03
DE3871965D1 (de)	1992-07-23
DK196691A (da)	1991-12-05
DE3871965T2 (de)	1993-01-14
DK169840B1 (da)	1995-03-13

Legal Events

Date

Code

Title

Description

1992-02-28

FG3A

Patent granted, date of granting

Effective date: 19910808

1997-06-30

MM3A

Annulment or lapse

Free format text: LAPSE DUE TO NON-PAYMENT OF FEES

Effective date: 19970228

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DK196691D0 (da)	1991-12-05	Steroid-5-alfa-reduktaseinhibitorer
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ZA899671B (en)	1990-11-28	Phosphinic acid substituted steroids as inhibitors of steroid 5-alpha-reductase
GR1001503B (el)	1994-02-28	Μέ?οδος δια την παρασκευή φαρμακευτικών ενώσεων αι οποίαι περιέχουν ως δραστική ουσία καρβονικά οξέα τα οποία περιέχουν ?είον κα?ώς και η χρησιμοποίησις αυτών δια την καταπολέμησιν των ρετροιών.
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