AU6551190A

AU6551190A – 11-keto or hydroxy 3,5-diene steroids as inhibitors of steroid 5-alpha-reductase
– Google Patents

AU6551190A – 11-keto or hydroxy 3,5-diene steroids as inhibitors of steroid 5-alpha-reductase
– Google Patents
11-keto or hydroxy 3,5-diene steroids as inhibitors of steroid 5-alpha-reductase

Info

Publication number
AU6551190A

AU6551190A
AU65511/90A
AU6551190A
AU6551190A
AU 6551190 A
AU6551190 A
AU 6551190A
AU 65511/90 A
AU65511/90 A
AU 65511/90A
AU 6551190 A
AU6551190 A
AU 6551190A
AU 6551190 A
AU6551190 A
AU 6551190A
Authority
AU
Australia
Prior art keywords
alpha
keto
reductase
inhibitors
steroid
Prior art date
1989-11-01
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.)

Granted

Application number
AU65511/90A
Other versions

AU641701B2
(en

Inventor
Dennis Alan Holt
Mark Alan Levy
Brian Walter Metcalf
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.)
1989-11-01
Filing date
1990-10-26
Publication date
1991-07-18

1990-10-26
Application filed by SmithKline Beecham Corp
filed
Critical
SmithKline Beecham Corp

1991-07-18
Publication of AU6551190A
publication
Critical
patent/AU6551190A/en

1993-09-30
Application granted
granted
Critical

1993-09-30
Publication of AU641701B2
publication
Critical
patent/AU641701B2/en

2010-10-26
Anticipated expiration
legal-status
Critical

Status
Ceased
legal-status
Critical
Current

Links

Espacenet

Global Dossier

Discuss

Classifications

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

C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane

A—HUMAN NECESSITIES

A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE

A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

A61P13/00—Drugs for disorders of the urinary system

A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers

A—HUMAN NECESSITIES

A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE

A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

A61P15/00—Drugs for genital or sexual disorders; Contraceptives

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

C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa

C07J1/0022—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa the substituent being an OH group free esterified or etherified

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

C07J1/0051—Estrane derivatives

C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa

C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified

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

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

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

C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 – C07J43/00

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07J—STEROIDS

C07J61/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by contraction of only one ring by one or two atoms

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07J—STEROIDS

C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms

C07J63/002—Expansion of ring A by one atom, e.g. A homo steroids

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07J—STEROIDS

C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms

C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21

C07J7/0095—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21 carbon in position 21 is part of carboxylic group

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07J—STEROIDS

C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring

C07J71/0005—Oxygen-containing hetero ring

C07J71/001—Oxiranes

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

Abstract

Compounds of structure: in which X is keto or H and OH; R<1> is H or C1-8alkyl; R<2> is (1) alpha -H, alpha =OH or alpha -acetoxy and/or beta -WCOR<3> where W is a bond or C1-12alkyl and R<3> is C1-8alkyl, C1-8alkoxy of N(R<4>)2 where R<4> is, inter alia, H or C1-8alkyl; (2) =CHWCOR<3> or =CHWOR<5> where W and R<3> are as above and R<5> is, inter alia, phenylalkylcarbonyl, benzoyl, alkoxycarbonyl, aminocarbonyl, alkyl or alkylcarbonyl; (3) alpha -H and beta -NHCOR<6> where R<6> is alkyl or beta -N(R<4>)2 or (4) keto, processes for their preparation, pharmaceutical compositions containing them and their use in therapy as inhibitors of 5- alpha -reductase.

AU65511/90A
1989-11-01
1990-10-26
11-keto or hydroxy 3,5-diene steroids as inhibitors of steroid 5-alpha-reductase

Ceased

AU641701B2
(en)

Applications Claiming Priority (2)

Application Number
Priority Date
Filing Date
Title

US430152

1989-11-01

US07/430,152

US5041433A
(en)

1987-04-29
1989-11-01
11-keto or hydroxy 3,5-diene steroids as inhibitors of steriod 5-α-reductase

Publications (2)

Publication Number
Publication Date

AU6551190A
true

AU6551190A
(en)

1991-07-18

AU641701B2

AU641701B2
(en)

1993-09-30

Family
ID=23706275
Family Applications (1)

Application Number
Title
Priority Date
Filing Date

AU65511/90A
Ceased

AU641701B2
(en)

1989-11-01
1990-10-26
11-keto or hydroxy 3,5-diene steroids as inhibitors of steroid 5-alpha-reductase

Country Status (15)

Country
Link

US
(1)

US5041433A
(en)

EP
(1)

EP0427434B1
(en)

JP
(1)

JPH03169890A
(en)

KR
(1)

KR100187945B1
(en)

AT
(1)

ATE115587T1
(en)

AU
(1)

AU641701B2
(en)

CA
(1)

CA2028622A1
(en)

DE
(1)

DE69015129T2
(en)

DK
(1)

DK0427434T3
(en)

ES
(1)

ES2064661T3
(en)

GR
(1)

GR3015372T3
(en)

IE
(1)

IE65562B1
(en)

NZ
(1)

NZ235871A
(en)

PT
(1)

PT95750A
(en)

ZA
(1)

ZA908730B
(en)

Families Citing this family (21)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

US5516768A
(en)

*

1990-03-16
1996-05-14
Smithkline Beecham Corporation
Uncompetitive inhibition of steroid and 5α-reductose

US5300294A
(en)

*

1990-06-27
1994-04-05
Smithkline Beecham Corporation
Method of treating prostatic adenocarcinoma

IT1259419B
(en)

*

1991-05-24
1996-03-18
Erba Carlo Spa

3-CARBOSE STEROIDS 17B – UNSATURATED SUBSTITUTES USEFUL AS INHIBITORS OF TESTOSTERONE 5 IN REDUCTASE

EP0548793A3
(en)

*

1991-12-20
1995-11-02
Hoechst Ag
Ethylenic-unsaturated bile acid derivatives, process for their production and preliminary processes therefor

US5215894A
(en)

*

1992-02-25
1993-06-01
Merck & Co., Inc.
Biological process for producing 17β-N-monosubstituted carbamoyl-11-oxo-4-aza-5-α-androst-3-one testosterone-5-α reductase inhibitors

EP0641211A1
(en)

*

1992-05-21
1995-03-08
Endorecherche Inc.
INHIBITORS OF TESTOSTERONE 5$g(a)-REDUCTASE ACTIVITY

US5683995A
(en)

*

1992-11-18
1997-11-04
Smithkline Beecham Corporation
17 substituted acyl-3-carboxy 3,5-diene steroidals as α-reductase inhibitors

IL107611A0
(en)

*

1992-11-18
1994-02-27
Smithkline Beecham Corp
Steroid compounds and pharmaceutical compositions containing them

US5641765A
(en)

*

1992-11-18
1997-06-24
Smithkline Beecham Corporation
17-αand 17-βsubstituted acyl-3-carboxy-3,5-dienes and use in inhibiting 5-α-reductase

TW369521B
(en)

*

1993-09-17
1999-09-11
Smithkline Beecham Corp
Androstenone derivative

US5637310A
(en)

*

1993-12-20
1997-06-10
Smithkline Beecham Corporation
Method of treating prostatic adenocarcinoma

WO1995028413A1
(en)

*

1994-04-15
1995-10-26
Smithkline Beecham Corporation
17β-SUBSTITUTED 3-CARBOXY STEROIDS THAT INHIBIT 5-α-REDUCTASE

US5541322A
(en)

*

1994-10-14
1996-07-30
Glaxo Wellcome Inc.
Synthesis of 6-azaandrostenones

EP1079859B1
(en)

1998-05-22
2010-07-14
The Board Of Trustees Of The Leland Stanford Junior University
Bifunctional molecules and therapies based thereon

US20060148725A1
(en)

*

2001-12-21
2006-07-06
The Miriam Hospital
Selective 11beta HSD inhibitors and methods of use thereof

EP1587574A4
(en)

*

2001-12-21
2009-03-18
Rhode Island Hospital
SELECTIVE 11b-HSD INHIBITORS AND METHODS FOR USE THEREOF

CA2524165A1
(en)

*

2003-04-29
2004-11-11
The Miriam Hospital
Selective testicular 11.beta.-hsd inhibitors and methods of use thereof

CA2789262C
(en)

2005-04-28
2016-10-04
Proteus Digital Health, Inc.
Pharma-informatics system

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

CA2969926C
(en)

2009-02-20
2018-05-15
2-Bbb Medicines B.V.
Glutathione-based drug delivery system

CN102458374A
(en)

2009-05-06
2012-05-16
实验室护肤股份有限公司
Dermal delivery compositions comprising active agent-calcium phosphate particle complexes and methods of using the same

Family Cites Families (6)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

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

US4317817A
(en)

*

1979-08-27
1982-03-02
Richardson-Merrell Inc.
Novel steroid 5α-reductase inhibitors

DK465481A
(en)

*

1980-11-21
1982-05-22
Hoffmann La Roche

PROCEDURE FOR THE MANUFACTURE OF D-HOMOSTOMOIDS

US4814324A
(en)

*

1987-03-06
1989-03-21
Merck & Co., Inc.
Sterol inhibitors of testosterone 5α-reductase

US4910226A
(en)

*

1987-04-29
1990-03-20
Smithkline Beckman Corporation
Steroid 5-alpha-reductase inhibitors

1989

1989-11-01
US
US07/430,152
patent/US5041433A/en
not_active
Expired – Lifetime

1990

1990-10-26
CA
CA002028622A
patent/CA2028622A1/en
not_active
Abandoned

1990-10-26
AU
AU65511/90A
patent/AU641701B2/en
not_active
Ceased

1990-10-29
AT
AT90311807T
patent/ATE115587T1/en
not_active
IP Right Cessation

1990-10-29
EP
EP90311807A
patent/EP0427434B1/en
not_active
Expired – Lifetime

1990-10-29
DE
DE69015129T
patent/DE69015129T2/en
not_active
Expired – Fee Related

1990-10-29
DK
DK90311807.3T
patent/DK0427434T3/en
active

1990-10-29
NZ
NZ235871A
patent/NZ235871A/en
unknown

1990-10-29
ES
ES90311807T
patent/ES2064661T3/en
not_active
Expired – Lifetime

1990-10-31
PT
PT95750A
patent/PT95750A/en
not_active
Application Discontinuation

1990-10-31
JP
JP2297020A
patent/JPH03169890A/en
active
Pending

1990-10-31
IE
IE392090A
patent/IE65562B1/en
unknown

1990-10-31
ZA
ZA908730A
patent/ZA908730B/en
unknown

1990-11-01
KR
KR1019900017704A
patent/KR100187945B1/en
not_active
IP Right Cessation

1995

1995-03-13
GR
GR940403878T
patent/GR3015372T3/en
unknown

Also Published As

Publication number
Publication date

JPH03169890A
(en)

1991-07-23

EP0427434A3
(en)

1992-03-04

IE903920A1
(en)

1991-05-08

ATE115587T1
(en)

1994-12-15

DE69015129D1
(en)

1995-01-26

IE65562B1
(en)

1995-11-01

DE69015129T2
(en)

1995-05-04

ZA908730B
(en)

1991-11-27

DK0427434T3
(en)

1995-05-08

CA2028622A1
(en)

1991-05-02

ES2064661T3
(en)

1995-02-01

AU641701B2
(en)

1993-09-30

NZ235871A
(en)

1991-12-23

EP0427434A2
(en)

1991-05-15

US5041433A
(en)

1991-08-20

KR100187945B1
(en)

1999-06-01

PT95750A
(en)

1991-09-13

KR910009725A
(en)

1991-06-28

EP0427434B1
(en)

1994-12-14

GR3015372T3
(en)

1995-06-30

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