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

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
Diabetes (AREA)
Endocrinology (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Engineering & Computer Science (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Pharmacology & Pharmacy (AREA)
Bioinformatics & Cheminformatics (AREA)
Animal Behavior & Ethology (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Toxicology (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
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
IL101243A (en) *	1991-03-20	1999-12-22	Merck & Co Inc	Pharmaceutical preparations for the treatment of benign prostatic hyperplasia containing steroid history
FI945105A7 (fi) *	1992-04-30	1994-10-31	Smithkline Beecham Corp	17alfa- ja 17beta-substituoitu estra-1,3,5(10)-trieeni-3-karboksyyliha ppo
ES2149208T3 (es) *	1992-05-20	2000-11-01	Merck & Co Inc	Inhibidores 4-azaesteroides de 5-alfa-reductasa.
US5610162A (en) *	1992-05-20	1997-03-11	Merck & Co., Inc.	Ester derivatives of 4-aza-steroids
US5237064A (en) *	1992-05-20	1993-08-17	Merck & Co., Inc.	Process for producing 7β-substituted-aza-5αandrostan-3-ones
CA2135057A1 (en) *	1992-05-20	1993-11-25	Bruce E. Witzel	17-amino substituted 4-azasteroid 5a-reductase inhibitors
ES2148229T3 (es) *	1992-05-20	2000-10-16	Merck & Co Inc	Eteres y tioeteres en la posicion 17 de 4-aza-esteroides.
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
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
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
US5683995A (en) *	1992-11-18	1997-11-04	Smithkline Beecham Corporation	17 substituted acyl-3-carboxy 3,5-diene steroidals as 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
WO1995000147A1 (en) *	1993-06-28	1995-01-05	Merck & Co., Inc.	4-AZA-PREGNANE 5α-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 WO PCT/US1989/002269 patent/WO1989011282A1/en not_active Ceased
- 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
- 1989-05-24 PT PT90656A patent/PT90656B/pt not_active IP Right Cessation
- 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 EP EP89305246A patent/EP0343954B1/de not_active Expired - Lifetime
- 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
DE68919537T2 (de)	1995-05-11
ZA893971B (en)	1990-05-30
GR3015135T3 (en)	1995-05-31
DK279790A (da)	1990-11-23
HK1006461A1 (en)	1999-02-26
EP0343954A3 (en)	1990-05-16
CA1331457C (en)	1994-08-16
DE68919537D1 (de)	1995-01-12
PT90656A (pt)	1989-11-30
PT90656B (pt)	1994-10-31
AU3748789A (en)	1989-12-12
NO894065L (no)	1991-04-12
EP0343954A2 (de)	1989-11-29
IL91968A (en)	1994-10-21
NO894065D0 (no)	1989-10-11
DK130393D0 (da)	1993-11-19
DK169787B1 (da)	1995-02-27
DK130393A (da)	1993-11-19
IE68858B1 (en)	1996-07-24
JPH03504498A (ja)	1991-10-03
IE891732L (en)	1989-11-25
NO174964C (no)	1994-08-10
AU627466B2 (en)	1992-08-27
ES2065378T3 (es)	1995-02-16
WO1989011282A1 (en)	1989-11-30
DK168295B1 (da)	1994-03-07
JP2675418B2 (ja)	1997-11-12
EP0343954B1 (de)	1994-11-30
NO174964B (no)	1994-05-02
DK279790D0 (da)	1990-11-23

Legal Events

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

Publication	Publication Date	Title
ATE114665T1 (de)	1994-12-15	Aromatische steroide als 5-alpha-reduktase- inhibitoren.
ATE118505T1 (de)	1995-03-15	Phosphinsäure-derivate von aromatischen steroiden als 5-alpha reduktase-inhibitoren.
DE68920128D1 (de)	1995-02-02	Sulfonsäure-substituierte aromatische Steroide als 5-Alpha-Reduktase-Inhibitoren.
DE68919660D1 (de)	1995-01-12	Phosphonsäure-Derivate von aromatischen Steroiden als 5-alpha-Reduktase-Inhibitoren.
MX9200109A (es)	1992-09-01	Derivados de acridina, procedimiento para su prepaderivados de acridina, procedimiento para su preparacion y composicion farmaceutica que los contieneracion y composicion farmaceutica que los contiene. .
ATE252576T1 (de)	2003-11-15	Heteroarylphenylpyrazolverbindungen zur verwendung als analgetisches/entzündungshemmendes mittel
Meira et al.	2018	Structural design, synthesis and substituent effect of hydrazone-N-acylhydrazones reveal potent immunomodulatory agents
DK0393493T3 (da)	1996-04-15	Fluorerede galdesyrederivater, fremgangsmåder til fremstilling heraf og farmaceutiske midler, som indeholder dem
DE68909107D1 (de)	1993-10-21	4-Amino-3-acylchinolin-Derivate und ihre Verwendung als Inhibitoren der Magensekretion.
DE68917885D1 (de)	1994-10-06	Phosphonsäure-Derivate von Steroiden als Hemmstoffe der 5-alpha-Reduktase.
US4213978A (en)	1980-07-22	Anti-acne and anti-seborrhea prodrug derivatives of progesterone
DK307587D0 (da)	1987-06-17	3-(4-benzyl-piperazin-1-yl)-rifamycin sv- og s-forbindelser samt deres fremstilling og anvendelse
DK0526313T3 (da)	1995-08-21	Nye ureaderivater, deres fremstilling og terapeutiske anvendelse
NO943567L (no)	1994-11-25	Bruede bis-arylcarbinolderivater, preparater og anvendelsesmetoder
NO168481C (no)	1992-04-01	14,17beta-ethano-14beta-oestratrienderivater, befruktningshindrende middel, og anvendelse derav for befruktningskontroll hos kvinner.
GB1514748A (en)	1978-06-21	Pharmaceutically active piperidine derivatives and preparation thereof
NO872115L (no)	1987-11-23	Analogifremgangsmaate for fremstilling av farmakologisk aktive steroider.
US3660385A (en)	1972-05-02	2-(5-nitro-2-furfurylidene)-1-tetralones
Omar et al.	1982	Steroidal oxazoline derivatives: Synthesis and in vitro effect on bovine pancreatic ribonuclease activity
DE68903188D1 (de)	1992-11-19	Acylsulfonamid-derivate von alpha-carbocyclyltoluylsaeuren und ihre verwendung als leukotrienantagonisten.