ATE114665T1 - Aromatische steroide als 5-alpha-reduktase- inhibitoren. - Google Patents

Aromatische steroide als 5-alpha-reduktase- inhibitoren.

Info

Publication number: ATE114665T1
Authority: AT; Austria
Prior art keywords: alpha; beta; reductase inhibitors; alpha reductase; aromatic steroids
Prior art date: 1988-05-25

Application number

AT89305246T

Other languages

English (en)

Inventor

Dennis Alan Holt

Mark Alan Levy

Brian Walter Metcalf

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.)

1988-05-25

Filing date

1989-05-24

Publication date

1994-12-15

1989-05-24 Application filed by Smithkline Beecham Corp filed Critical Smithkline Beecham Corp

1994-12-15 Application granted granted Critical

1994-12-15 Publication of ATE114665T1 publication Critical patent/ATE114665T1/de

Links

239000002677 5-alpha reductase inhibitor Substances 0.000 title 1
150000003431 steroids Chemical class 0.000 title 1
125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 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
229930194542 Keto Natural products 0.000 abstract 1
150000001875 compounds Chemical class 0.000 abstract 1
125000002541 furyl group Chemical group 0.000 abstract 1
229910052736 halogen Inorganic materials 0.000 abstract 1
150000002367 halogens Chemical class 0.000 abstract 1
229910052739 hydrogen Inorganic materials 0.000 abstract 1
150000002431 hydrogen Chemical class 0.000 abstract 1
239000001257 hydrogen Substances 0.000 abstract 1
239000003112 inhibitor Substances 0.000 abstract 1
239000000543 intermediate Substances 0.000 abstract 1
125000000468 ketone group Chemical group 0.000 abstract 1
238000000034 method Methods 0.000 abstract 1
229910052760 oxygen Inorganic materials 0.000 abstract 1
239000008194 pharmaceutical composition Substances 0.000 abstract 1
229910052717 sulfur Inorganic materials 0.000 abstract 1
238000002560 therapeutic procedure Methods 0.000 abstract 1
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
- C07J13/005—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 16 (17)
- 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
- C07J1/0051—Estrane derivatives
- C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
- C07J13/007—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
- 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
- C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
- 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
- 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
- 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

Landscapes

Organic Chemistry (AREA)
Chemical & Material Sciences (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)
Steroid Compounds (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

AT89305246T 1988-05-25 1989-05-24 Aromatische steroide als 5-alpha-reduktase- inhibitoren. ATE114665T1 (de)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US19853488A	1988-05-25	1988-05-25

Publications (1)

Publication Number	Publication Date
ATE114665T1 true ATE114665T1 (de)	1994-12-15

Family

ID=22733779

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
AT89305246T ATE114665T1 (de)	1988-05-25	1989-05-24	Aromatische steroide als 5-alpha-reduktase- inhibitoren.

Country Status (15)

Country	Link
EP (1)	EP0343954B1 (de)
JP (1)	JP2675418B2 (de)
AT (1)	ATE114665T1 (de)
AU (1)	AU627466B2 (de)
CA (1)	CA1331457C (de)
DE (1)	DE68919537T2 (de)
DK (2)	DK168295B1 (de)
ES (1)	ES2065378T3 (de)
GR (1)	GR3015135T3 (de)
IE (1)	IE68858B1 (de)
IL (1)	IL91968A (de)
NO (1)	NO174964C (de)
PT (1)	PT90656B (de)
WO (1)	WO1989011282A1 (de)
ZA (1)	ZA893971B (de)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US5138063A (en) *	1984-02-27	1992-08-11	Merck & Co., Inc.	17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
US5571817A (en) *	1984-02-27	1996-11-05	Merck & Co., Inc.	Methods of treating androgenic alopecia with finasteride [17β-N-mono-substituted-carbamoyl-4-aza-5-α-androst-1-en-ones]
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
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
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
AU4291993A (en) *	1992-04-30	1993-11-29	Smithkline Beecham Corporation	17alpha and 17beta -substituted estra-1,3,5(10)-triene-3-carboxylic acid
US5237064A (en) *	1992-05-20	1993-08-17	Merck & Co., Inc.	Process for producing 7β-substituted-aza-5αandrostan-3-ones
SK137994A3 (en) *	1992-05-20	1995-04-12	Merck & Co Inc	7-beta-substituted-4-aza-5-alpha-cholestan-ons their using for production of pharmaceutical agent and pharmaceutical agent containing them
ATE198601T1 (de) *	1992-05-20	2001-01-15	Merck & Co Inc	Ester derivate von 4-aza-steroiden
CA2135057A1 (en) *	1992-05-20	1993-11-25	Bruce E. Witzel	17-amino substituted 4-azasteroid 5a-reductase inhibitors
WO1993023040A1 (en) *	1992-05-20	1993-11-25	Merck & Co., Inc.	17-ethers and thioethers of 4-aza-steroids
WO1993023048A1 (en) *	1992-05-20	1993-11-25	Merck & Co., Inc.	4-azasteroid 5-alpha-reductase inhibitors
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
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
US5683995A (en) *	1992-11-18	1997-11-04	Smithkline Beecham Corporation	17 substituted acyl-3-carboxy 3,5-diene steroidals as α-reductase inhibitors
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
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
CA2165077A1 (en) *	1993-06-28	1995-01-05	Philippe L. Durette	4-aza-pregnane 5.alpha.-reductase isozyme 1 inhibitors
TW369521B (en) *	1993-09-17	1999-09-11	Smithkline Beecham Corp	Androstenone derivative
US5430157A (en) *	1993-12-13	1995-07-04	Eli Lilly And Company	Reduced phenanthrenes
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
GB201102913D0 (en)	2011-02-18	2011-04-06	Univ Birmingham	Novel therapeutic

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE1107664B (de) *	1959-11-05	1961-05-31	Schering Ag	Verfahren zur Herstellung neuer in 3-Stellung substituierter OEstratriene
US3622670A (en) *	1969-08-22	1971-11-23	American Home Prod	Method of inducing ovulation
US4185101A (en) *	1977-08-11	1980-01-22	Schering Corporation	1,3,5(10),6,8-19-Nor-pregnapentaenes, their use as anti-psoriatic agents, and pharmaceutical formulations useful therefor
US4191759A (en) *	1978-04-13	1980-03-04	Merck & Co., Inc.	N-substituted-17β-carbamoylandrost-4-en-3-one 5α reductase inhibitors
US4340602A (en) *	1978-10-18	1982-07-20	Wayne State University	Compositions inhibiting estrogen sulfotransferase activity
US4910226A (en) *	1987-04-29	1990-03-20	Smithkline Beckman Corporation	Steroid 5-alpha-reductase inhibitors

1989
- 1989-05-23 CA CA000600335A patent/CA1331457C/en not_active Expired - Fee Related
- 1989-05-23 JP JP1506391A patent/JP2675418B2/ja not_active Expired - Lifetime
- 1989-05-23 AU AU37487/89A patent/AU627466B2/en not_active Ceased
- 1989-05-23 WO PCT/US1989/002269 patent/WO1989011282A1/en not_active Ceased
- 1989-05-24 PT PT90656A patent/PT90656B/pt not_active IP Right Cessation
- 1989-05-24 EP EP89305246A patent/EP0343954B1/de not_active Expired - Lifetime
- 1989-05-24 DE DE68919537T patent/DE68919537T2/de not_active Expired - Fee Related
- 1989-05-24 AT AT89305246T patent/ATE114665T1/de not_active IP Right Cessation
- 1989-05-24 ES ES89305246T patent/ES2065378T3/es not_active Expired - Lifetime
- 1989-05-25 ZA ZA893971A patent/ZA893971B/xx unknown
- 1989-06-12 IE IE173289A patent/IE68858B1/en not_active IP Right Cessation
- 1989-10-11 NO NO894065A patent/NO174964C/no unknown
- 1989-10-12 IL IL9196889A patent/IL91968A/en not_active IP Right Cessation
1990
- 1990-11-23 DK DK279790A patent/DK168295B1/da not_active IP Right Cessation
1993
- 1993-11-19 DK DK130393A patent/DK169787B1/da active
1995
- 1995-02-22 GR GR950400355T patent/GR3015135T3/el unknown

Also Published As

Publication number	Publication date
DK279790A (da)	1990-11-23
WO1989011282A1 (en)	1989-11-30
EP0343954B1 (de)	1994-11-30
NO174964C (no)	1994-08-10
DK279790D0 (da)	1990-11-23
NO174964B (no)	1994-05-02
JP2675418B2 (ja)	1997-11-12
DK130393D0 (da)	1993-11-19
IL91968A (en)	1994-10-21
PT90656B (pt)	1994-10-31
DK169787B1 (da)	1995-02-27
HK1006461A1 (en)	1999-02-26
DE68919537T2 (de)	1995-05-11
DK130393A (da)	1993-11-19
ZA893971B (en)	1990-05-30
DK168295B1 (da)	1994-03-07
AU3748789A (en)	1989-12-12
DE68919537D1 (de)	1995-01-12
NO894065L (no)	1991-04-12
IE68858B1 (en)	1996-07-24
JPH03504498A (ja)	1991-10-03
EP0343954A2 (de)	1989-11-29
AU627466B2 (en)	1992-08-27
ES2065378T3 (es)	1995-02-16
PT90656A (pt)	1989-11-30
GR3015135T3 (en)	1995-05-31
EP0343954A3 (en)	1990-05-16
CA1331457C (en)	1994-08-16
IE891732L (en)	1989-11-25
NO894065D0 (no)	1989-10-11

Legal Events

Date	Code	Title	Description
1999-02-15	REN	Ceased due to non-payment of the annual fee

Publication	Publication Date	Title
DE68919537D1 (de)	1995-01-12	Aromatische Steroide als 5-alpha-Reduktase-Inhibitoren.
ATE118505T1 (de)	1995-03-15	Phosphinsäure-derivate von aromatischen steroiden als 5-alpha reduktase-inhibitoren.
ZA899669B (en)	1990-11-28	Sulfonic acid substituted aromatic steroids as inhibitors of steroid 5-alpha-reductase
GR3015039T3 (en)	1995-05-31	Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5alpha-reductase.
DE68917884D1 (de)	1994-10-06	Phosphinsäure-Derivate von Steroiden als 5-alpha-Reduktase-Inhibitoren.
AU4257889A (en)	1990-04-12	Sulphonamido-phenylalkanoic acid derivatives having thromboxane A2 antagonist activity
ATE252576T1 (de)	2003-11-15	Heteroarylphenylpyrazolverbindungen zur verwendung als analgetisches/entzündungshemmendes mittel
AU2013277423B2 (en)	2018-08-09	Compounds with (1E, 6E)-1,7-bis-(3,4-dimethoxyphenyl)-4,4-disstituted-hepa-1,6-diene-3,5-dione structural scaffold, their biological activity, and uses thereof
DE69215694D1 (de)	1997-01-16	Benzamid-derivate
DK0390114T3 (da)	1994-10-17	Undertrykkelse af syntese og udskillelse af parathyroidhormoner med vitamin D3 derivater
ATE138663T1 (de)	1996-06-15	Oxothiolane und derivate, diese enthaltende pharmazeutische zubereitungen und ihre verwendung als arzneimittel
DE68909107D1 (de)	1993-10-21	4-Amino-3-acylchinolin-Derivate und ihre Verwendung als Inhibitoren der Magensekretion.
DK307587A (da)	1987-06-17	3-(4-benzyl-piperazin-1-yl)-rifamycin sv- og s-forbindelser samt deres fremstilling og anvendelse
GB2041219A (en)	1980-09-10	Topical pharmaceutical compositions containing thiazolidine-substituted corticosteroids
NO943567L (no)	1994-11-25	Bruede bis-arylcarbinolderivater, preparater og anvendelsesmetoder
O'BRIEN et al.	1960	Amino derivatives of Kojic acid
DK259387A (da)	1987-11-22	Steroide forbindelser, der er virksomme mod kraeft og obesitet
DE69414396D1 (de)	1998-12-10	Acylphenylglycin-derivat und dieses als aktivbestandteil enthaltendes vorbeugungs -und heilmittel gegen durch erhöhte collagenaseaktivität verursachte krankheiten
GB1514748A (en)	1978-06-21	Pharmaceutically active piperidine derivatives and preparation thereof
ES2001893A6 (es)	1988-07-01	Procedimiento para la obtencion de derivados de metilendioxifenantreno
DE69305684D1 (de)	1996-12-05	Octahydronaphthalenoxim Derivate für die Inhibierung der Cholesterin Biosynthese, ihre Herstellung und Verwendung
DE69110219D1 (de)	1995-07-13	3-(1H-Indazol-3-yl)-4-pyridiname, Verfahren und Zwischenprodukte zu ihrer Herstellung und ihre Verwendung als Arzneimittel.
US3660385A (en)	1972-05-02	2-(5-nitro-2-furfurylidene)-1-tetralones
GB1471546A (en)	1977-04-27	1-acyl-4-substituted alkyl-piperazine or homopiperazine derivatives nad process for preparation thereof
NO924947L (no)	1993-02-19	Tetrazolderivater og legemidler