EP0669932A4 - 17-alpha and 17-beta substituted acyl-3-carboxy-3,5-dienes and use in inhibiting 5-alpha-reductase. - Google Patents

17-alpha and 17-beta substituted acyl-3-carboxy-3,5-dienes and use in inhibiting 5-alpha-reductase.

Info

Publication number: EP0669932A4
Authority: EP; European Patent Office
Prior art keywords: alpha; dienes; reductase; carboxy; inhibiting
Prior art date: 1992-11-18
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 Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Withdrawn

Application number

EP94902307A

Other languages

German (de)

French (fr)

Other versions

EP0669932A1 (en

Inventor

Dennis Alan Holt

Mark Alan Levy

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

SmithKline Beecham 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.)

1992-11-18

Filing date

1993-11-18

Publication date

1995-10-25

1992-11-18 Priority claimed from GB929224213A external-priority patent/GB9224213D0/en

1993-08-14 Priority claimed from GB939316954A external-priority patent/GB9316954D0/en

1993-11-18 Application filed by SmithKline Beecham Corp filed Critical SmithKline Beecham Corp

1995-09-06 Publication of EP0669932A1 publication Critical patent/EP0669932A1/en

1995-10-25 Publication of EP0669932A4 publication Critical patent/EP0669932A4/en

Status Withdrawn legal-status Critical Current

Links

108010066551 Cholestenone 5 alpha-Reductase Proteins 0.000 title 1
230000002401 inhibitory effect Effects 0.000 title 1

Classifications

- 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
- 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
- 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
- C07J1/0014—Androstane derivatives substituted in position 17 alfa, not substituted in position 17 beta
- 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
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
- C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0066—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by a carbon atom forming part of an amide group
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
- C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton

Landscapes

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

EP94902307A 1992-11-18 1993-11-18 17-alpha and 17-beta substituted acyl-3-carboxy-3,5-dienes and use in inhibiting 5-alpha-reductase. Withdrawn EP0669932A4 (en)

Applications Claiming Priority (5)

Application Number	Priority Date	Filing Date	Title
GB929224213A GB9224213D0 (en)	1992-11-18	1992-11-18	Compounds
GB9224213		1992-11-18
GB939316954A GB9316954D0 (en)	1993-08-14	1993-08-14	Compounds
GB9316954		1993-08-14
PCT/US1993/011241 WO1994011386A1 (en)	1992-11-18	1993-11-18	17-alpha and 17-beta substituted acyl-3-carboxy-3,5-dienes and use in inhibiting 5-alpha-reductase

Publications (2)

Publication Number	Publication Date
EP0669932A1 EP0669932A1 (en)	1995-09-06
EP0669932A4 true EP0669932A4 (en)	1995-10-25

Family

ID=26302003

Family Applications (2)

Application Number	Title	Priority Date	Filing Date
EP94901600A Withdrawn EP0673251A1 (en)	1992-11-18	1993-11-18	17 substituted acyl-3-carboxy 3,5-diene steroidals as 5-alpha-reductase inhibitors
EP94902307A Withdrawn EP0669932A4 (en)	1992-11-18	1993-11-18	17-alpha and 17-beta substituted acyl-3-carboxy-3,5-dienes and use in inhibiting 5-alpha-reductase.

Family Applications Before (1)

Application Number	Title	Priority Date	Filing Date
EP94901600A Withdrawn EP0673251A1 (en)	1992-11-18	1993-11-18	17 substituted acyl-3-carboxy 3,5-diene steroidals as 5-alpha-reductase inhibitors

Country Status (12)

Country	Link
EP (2)	EP0673251A1 (en)
JP (1)	JPH08503471A (en)
CN (2)	CN1101914A (en)
AP (1)	AP9300589A0 (en)
AU (2)	AU5613394A (en)
CA (1)	CA2149427A1 (en)
IL (1)	IL107611A0 (en)
MA (1)	MA23036A1 (en)
MX (1)	MX9307203A (en)
NZ (1)	NZ258723A (en)
SI (1)	SI9300601A (en)
WO (2)	WO1994011004A1 (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
TW369521B (en) *	1993-09-17	1999-09-11	Smithkline Beecham Corp	Androstenone derivative
GB9415178D0 (en) *	1994-07-28	1994-09-21	Erba Carlo Spa	4-azasteroids with side-chain fluoroketones
GB9415183D0 (en) *	1994-07-28	1994-09-21	Erba Carlo Spa	3-carboxysteroids with a fluorinated side-chain
EP0784627A4 (en) *	1994-10-05	1998-05-06	Smithkline Beecham Corp	METHOD FOR PRODUCING 17-BETA-SUBSTITUTED ANDROSTA-3,5-DIEN-3-CARBONIC ACID
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
DE69824632T2 (en)	1997-11-12	2005-06-09	Mitsubishi Chemical Corp.	PURINE DERIVATIVES AND MEDICAMENTS CONTAINING THE SAME AS AN ACTIVE INGREDIENT
KR100747106B1 (en)	1999-05-11	2007-08-08	미쯔비시 가가꾸 가부시끼가이샤	Purine derivative dihydrates, pharmaceuticals containing the same as active ingredients and intermediates thereof
FR2817257B1 (en)	2000-11-30	2009-03-20	Sanofi Synthelabo	CYCLOHEXYL (ALKYL) -PROPANOLAMINES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
GB201102913D0 (en)	2011-02-18	2011-04-06	Univ Birmingham	Novel therapeutic

Citations (2)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
EP0465123A2 (en) *	1990-06-28	1992-01-08	Merck & Co. Inc.	New intermediates in the synthesis of 17beta-acyl-3-carboxy-androsta-3,5-dienes
EP0465142A1 (en) *	1990-06-28	1992-01-08	Merck & Co. Inc.	17Beta-acyl-3-carboxy-androsta-3, 5-dienes as testosterone 5alpha-reductase inhibitors

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4910226A (en) *	1987-04-29	1990-03-20	Smithkline Beckman Corporation	Steroid 5-alpha-reductase inhibitors
US5041433A (en) *	1987-04-29	1991-08-20	Smithkline Beecham Corporation	11-keto or hydroxy 3,5-diene steroids as inhibitors of steriod 5-α-reductase
US4954446A (en) *	1988-05-25	1990-09-04	Smithkline Beecham Corporation	Aromatic steroid 5-α-reductase inhibitors
US5032586A (en) *	1989-08-24	1991-07-16	Smithkline Beecham Corporation	7-keto or hydroxy 3,5-diene steroids as inhibitors of steroid 5-alpha reductase
US5137882A (en) *	1990-06-11	1992-08-11	Holt Dennis A	Steroidal 3-acetic acid derivatives as 5-alpha-reductase inhibitors
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
US5196411A (en) *	1991-08-16	1993-03-23	Merck & Co., Inc.	17β-acyl-3-carboxy-androsta-3,5-dienes as testosterone 5α-reductase inhibitors

1993
- 1993-11-15 IL IL10761193A patent/IL107611A0/en unknown
- 1993-11-15 AP APAP/P/1993/000589A patent/AP9300589A0/en unknown
- 1993-11-17 MA MA23342A patent/MA23036A1/en unknown
- 1993-11-17 MX MX9307203A patent/MX9307203A/en unknown
- 1993-11-18 JP JP6512499A patent/JPH08503471A/en active Pending
- 1993-11-18 EP EP94901600A patent/EP0673251A1/en not_active Withdrawn
- 1993-11-18 AU AU56133/94A patent/AU5613394A/en not_active Abandoned
- 1993-11-18 AU AU56717/94A patent/AU5671794A/en not_active Abandoned
- 1993-11-18 SI SI9300601A patent/SI9300601A/en unknown
- 1993-11-18 CA CA002149427A patent/CA2149427A1/en not_active Abandoned
- 1993-11-18 WO PCT/US1993/011225 patent/WO1994011004A1/en not_active Ceased
- 1993-11-18 NZ NZ258723A patent/NZ258723A/en unknown
- 1993-11-18 EP EP94902307A patent/EP0669932A4/en not_active Withdrawn
- 1993-11-18 WO PCT/US1993/011241 patent/WO1994011386A1/en not_active Ceased
- 1993-11-18 CN CN93114775A patent/CN1101914A/en active Pending
- 1993-11-18 CN CN93121434A patent/CN1101916A/en active Pending

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
EP0465123A2 (en) *	1990-06-28	1992-01-08	Merck & Co. Inc.	New intermediates in the synthesis of 17beta-acyl-3-carboxy-androsta-3,5-dienes
EP0465142A1 (en) *	1990-06-28	1992-01-08	Merck & Co. Inc.	17Beta-acyl-3-carboxy-androsta-3, 5-dienes as testosterone 5alpha-reductase inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of WO9411386A1 *

Also Published As

Publication number	Publication date
MA23036A1 (en)	1994-07-01
AP9300589A0 (en)	1994-01-31
CA2149427A1 (en)	1994-05-26
WO1994011004A1 (en)	1994-05-26
AU5671794A (en)	1994-06-08
EP0669932A1 (en)	1995-09-06
EP0673251A4 (en)	1995-10-25
CN1101916A (en)	1995-04-26
JPH08503471A (en)	1996-04-16
NZ258723A (en)	1996-12-20
MX9307203A (en)	1994-07-29
IL107611A0 (en)	1994-02-27
EP0673251A1 (en)	1995-09-27
CN1101914A (en)	1995-04-26
SI9300601A (en)	1994-06-30
AU5613394A (en)	1994-06-08
WO1994011386A1 (en)	1994-05-26

Legal Events

Date	Code	Title	Description
1995-07-21	PUAI	Public reference made under article 153(3) epc to a published international application that has entered the european phase	Free format text: ORIGINAL CODE: 0009012
1995-09-06	17P	Request for examination filed	Effective date: 19950516
1995-09-06	AK	Designated contracting states	Kind code of ref document: A1 Designated state(s): AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE
1995-10-25	A4	Supplementary search report drawn up and despatched	Effective date: 19950908
1995-10-25	AK	Designated contracting states	Kind code of ref document: A4 Designated state(s): AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE
1995-10-25	RHK1	Main classification (correction)	Ipc: C07J 9/00
1999-10-08	STAA	Information on the status of an ep patent application or granted ep patent	Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN
1999-11-24	18D	Application deemed to be withdrawn	Effective date: 19990601

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