ATE165368T1 - Inhibitoren von testosteron-5-alpha reductase. - Google Patents

Inhibitoren von testosteron-5-alpha reductase.

Info

Publication number: ATE165368T1
Authority: AT; Austria
Prior art keywords: lower alkyl; pct; hydrogen; independently hydrogen; carbons
Prior art date: 1991-12-20

Application number

AT93902691T

Other languages

English (en)

Inventor

Stephen Vernon Frye

Cynthia Markert Cribbs

Curt Dale Haffner

Patrick Reed Maloney

Robert Carl Andrews

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.)

1991-12-20

Filing date

1992-12-18

Publication date

1998-05-15

1992-12-18 Application filed by Glaxo Wellcome Inc filed Critical Glaxo Wellcome Inc

1998-05-15 Application granted granted Critical

1998-05-15 Publication of ATE165368T1 publication Critical patent/ATE165368T1/de

Links

102000001779 3-oxo-5-alpha-steroid 4-dehydrogenase Human genes 0.000 title 1
108010029908 3-oxo-5-alpha-steroid 4-dehydrogenase Proteins 0.000 title 1
239000003112 inhibitor Substances 0.000 title 1
125000000217 alkyl group Chemical group 0.000 abstract 7
229910052739 hydrogen Inorganic materials 0.000 abstract 7
239000001257 hydrogen Substances 0.000 abstract 7
125000003342 alkenyl group Chemical group 0.000 abstract 5
150000002431 hydrogen Chemical class 0.000 abstract 4
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
125000000753 cycloalkyl group Chemical group 0.000 abstract 3
NJFPVDFQZGPHID-ZDMKNRLGSA-N C(=O)=C1[C@@H]2[C@](CC1)(C)CC[C@H]1[C@H]2CNC2=CC(CC[C@]12C)=O Chemical class C(=O)=C1[C@@H]2[C@](CC1)(C)CC[C@H]1[C@H]2CNC2=CC(CC[C@]12C)=O NJFPVDFQZGPHID-ZDMKNRLGSA-N 0.000 abstract 1
125000002252 acyl group Chemical group 0.000 abstract 1
125000003545 alkoxy group Chemical group 0.000 abstract 1
125000003118 aryl group Chemical group 0.000 abstract 1
125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
239000008194 pharmaceutical composition Substances 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

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)
Cosmetics (AREA)

AT93902691T 1991-12-20 1992-12-18 Inhibitoren von testosteron-5-alpha reductase. ATE165368T1 (de)

Applications Claiming Priority (4)

Application Number	Priority Date	Filing Date
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
ATE165368T1 true ATE165368T1 (de)	1998-05-15

Family

ID=27487892

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
AT93902691T ATE165368T1 (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
ATE165368T1 (de) *	1991-12-20	1998-05-15	Glaxo Wellcome Inc	Inhibitoren von testosteron-5-alpha reductase.
US5710275A (en) *	1992-05-20	1998-01-20	Merck & Co., Inc.	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
EP1597233A1 (de) *	2003-02-11	2005-11-23	Warner-Lambert Company LLC	Benzylharnstoff- und benzylthioharnstoff-derivate als androgenantagonisten
CA2521883C (en)	2003-04-15	2013-09-17	Inflazyme Pharmaceuticals Ltd.	Indene derivatives as pharmaceutical agents
GB201102913D0 (en)	2011-02-18	2011-04-06	Univ Birmingham	Novel therapeutic
US10100056B2 (en)	2013-03-14	2018-10-16	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.
US9944590B2 (en)	2015-06-26	2018-04-17	Aquinox Pharmaceuticals (Canada) Inc.	Crystalline solid forms of the acetate salt of (1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexanol
US10053415B2 (en)	2016-01-20	2018-08-21	Aquinox Pharmaceuticals (Canada) Inc.	Synthesis of a substituted indene derivative
WO2017190034A1 (en) *	2016-04-29	2017-11-02	The Research Foundation For The State University Of New York	Azasteroids for treatment of tuberculosis

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
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
US4191759A (en) *	1978-04-13	1980-03-04	Merck & Co., Inc.	N-substituted-17β-carbamoylandrost-4-en-3-one 5α reductase inhibitors
DK465481A (da) *	1980-11-21	1982-05-22	Hoffmann La Roche	Fremgangsmaade til fremstilling af d-homostemoider
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.
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
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
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
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.
US4888336A (en) *	1987-01-28	1989-12-19	Smithkline Beckman Corporation	Steroid 5-alpha-reductase inhibitors
US5110939A (en) *	1987-01-28	1992-05-05	Smithkline Beecham Corporation	Intermediates in the preparation of steriod 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
US4882319A (en) *	1988-12-23	1989-11-21	Smithkline Beckman Corporation	Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase
US4937237A (en) *	1988-12-23	1990-06-26	Smithkline Beckman Corporation	Phosphinic acid substituted aromatic steroids as inhibitors of steroid 5-60 -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
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
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
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
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
NZ239141A (en) *	1990-08-01	1994-04-27	Merrell Dow Pharma	4-amino-delta-4,6-steroids; preparatory processes and pharmaceutical compositions
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
CA2050824A1 (en) *	1990-09-24	1992-03-25	John M. Williams	Process for making 3-oxo-4-aza-androst-1-ene 17-.beta.-ketones
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
IE76452B1 (en) *	1990-10-29	1997-10-22	Sankyo Co	Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use
ATE165368T1 (de) *	1991-12-20	1998-05-15	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

1992
- 1992-12-18 AT AT93902691T patent/ATE165368T1/de not_active IP Right Cessation
- 1992-12-18 DE DE69225244T patent/DE69225244T2/de not_active Expired - Fee Related
- 1992-12-18 US US08/244,875 patent/US5543406A/en not_active Expired - Fee Related
- 1992-12-18 AU AU34174/93A patent/AU3417493A/en not_active Abandoned
- 1992-12-18 WO PCT/US1992/011109 patent/WO1993013124A1/en not_active Ceased
- 1992-12-18 JP JP5511251A patent/JPH07502511A/ja active Pending
- 1992-12-18 ES ES93902691T patent/ES2118222T3/es not_active Expired - Lifetime
- 1992-12-18 EP EP93902691A patent/EP0641356B1/de not_active Expired - Lifetime
- 1992-12-18 CA CA002126203A patent/CA2126203A1/en not_active Abandoned
1993
- 1993-01-12 CN CN93100373A patent/CN1080639A/zh active Pending

Also Published As

Publication number	Publication date
DE69225244T2 (de)	1998-09-24
US5543406A (en)	1996-08-06
WO1993013124A1 (en)	1993-07-08
AU3417493A (en)	1993-07-28
EP0641356B1 (de)	1998-04-22
CN1080639A (zh)	1994-01-12
DE69225244D1 (de)	1998-05-28
ES2118222T3 (es)	1998-09-16
EP0641356A1 (de)	1995-03-08
JPH07502511A (ja)	1995-03-16
CA2126203A1 (en)	1993-07-08

Legal Events

Date	Code	Title	Description
1998-10-15	RER	Ceased as to paragraph 5 lit. 3 law introducing patent treaties

Publication	Publication Date	Title
ATE165368T1 (de)	1998-05-15	Inhibitoren von testosteron-5-alpha reductase.
AU4264396A (en)	1996-06-19	Cosmetic or pharmaceutical compositions containing mangiferin or derivatives thereof
MY119150A (en)	2005-04-30	Azetidine derivatives, their preparation and medicaments containing them
FI963227A0 (fi)	1996-08-16	Mikrojauhettua nebivololia sisältäviä koostumuksia
BR1100412A (pt)	2000-06-06	Composto; método para propiciar tratamento imunomodulador; e composição farmacêutica para tratamento imunomodulador
PL316563A1 (en)	1997-01-20	Application of derivatives of carboxylic acids as therapeutic agents
ATE200289T1 (de)	2001-04-15	Derivate des carbapenem-3-carbonsäureesters
BG106235A (en)	2002-08-30	Streptogramin derivatives, preparation and compositions containing them
ATE289991T1 (de)	2005-03-15	Substituierte beta-alaninen
MX9805023A (es)	1998-11-30	Derivados de 1-metilcarbapenem.
ZA9429B (en)	1994-08-11	Pyrrolidine derivatives their preparation and medicaments containing them
GR3033333T3 (en)	2000-09-29	Carbamoyl carboxylic acid amides
NO950177D0 (no)	1995-01-17	Farmakologisk aktive erivater
AR027035A1 (es)	2003-03-12	Pirroles sustituidos
ZA9480B (en)	1994-08-11	Pyrrolidine derivatives their preparation and medicaments containing them
AU2621995A (en)	1995-12-21	Indole derivatives as prodrugs of 5-ht1-like receptor agonists
FR2695643B1 (fr)	1994-11-25	Dérivés d'uréido-acétamide, leur préparation et les médicaments les contenant.
BR9307388A (pt)	1999-08-31	Agentes terapêuticos