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)
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 (16)

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)
HK (1)	HK1006461A1 (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
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
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
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
HUT72467A (en) *	1992-04-30	1996-04-29	Smithkline Beecham Corp	17alpha and 17beta-substituted estra-1,3,5(10)-triene-3-carboxylic acids, pharmaceutical compositions containing them, intermediates and process for their production
WO1993023038A1 (en) *	1992-05-20	1993-11-25	Merck & Co., Inc.	17-AMINO SUBSTITUTED 4-AZASTEROID 5α-REDUCTASE INHIBITORS
JPH07508039A (ja) *	1992-05-20	1995-09-07	メルク　エンド　カンパニー　インコーポレーテッド	４−アザステロイドのエステル誘導体
ATE195129T1 (de) *	1992-05-20	2000-08-15	Merck & Co Inc	4-azasteroide als 5-alpha-reduktase
US5536727A (en) *	1992-05-20	1996-07-16	Merck & Co., Inc.	17-Ethers and thioethers of 4-aza-steroids
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
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
JP3325026B2 (ja) *	1993-06-28	2002-09-17	メルクエンドカンパニーインコーポレーテッド	４−アザ−プレグナン５α−レダクターゼアイソザイム１阻害剤
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 AU AU37487/89A patent/AU627466B2/en not_active Ceased
- 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
- 1989-05-24 EP EP89305246A patent/EP0343954B1/de not_active Expired - Lifetime
- 1989-05-24 PT PT90656A patent/PT90656B/pt not_active IP Right Cessation
- 1989-05-24 AT AT89305246T patent/ATE114665T1/de not_active IP Right Cessation
- 1989-05-24 DE DE68919537T patent/DE68919537T2/de not_active Expired - Fee Related
- 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
1998
- 1998-06-18 HK HK98105689A patent/HK1006461A1/en not_active IP Right Cessation

Also Published As

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

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.
DE68919660D1 (de)	1995-01-12	Phosphonsäure-Derivate von aromatischen Steroiden als 5-alpha-Reduktase-Inhibitoren.
ATE115960T1 (de)	1995-01-15	Sulfonsäure-substituierte aromatische steroide als 5-alpha-reduktase-inhibitoren.
DE69434063D1 (de)	2004-11-11	Substituierte Morpholinderivate und ihre Verwendung als therapeutische Mittel
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. .
DE60006057D1 (de)	2003-11-27	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
DE60001623D1 (de)	2003-04-17	Sulfamoylheteroarylpyrazolverbindungen zur Verwendung als analgetisches/entzündungshemmendes Mittel
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
US4213978A (en)	1980-07-22	Anti-acne and anti-seborrhea prodrug derivatives of progesterone
DK307587A (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
DE69410419D1 (de)	1998-06-25	Quinolin-Carboxylsäurester von 21-Hydroxypregnan Derivaten und antibakterielle und entzüdungshemmende Präparate davon
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.
NO941084L (no)	1994-03-24	Neuroleptiske 2-substituerte perhydro-1-H-pyrido[1,2-aÅpyraziner
GB1514748A (en)	1978-06-21	Pharmaceutically active piperidine derivatives and preparation thereof
NO872115D0 (no)	1987-05-20	Analogifremgangsmaate for fremstilling av farmakologisk aktive steroider.
ES2001893A6 (es)	1988-07-01	Procedimiento para la obtencion de derivados de metilendioxifenantreno
DE69110219D1 (de)	1995-07-13	3-(1H-Indazol-3-yl)-4-pyridiname, Verfahren und Zwischenprodukte zu ihrer Herstellung und ihre Verwendung als Arzneimittel.
NO931752D0 (no)	1993-05-14	Oktahydronaftalenoksimderivater til inhibering av kolesterolbiosyntese, samt fremgangsmaate til fremstilling og anvendelse derav
US3660385A (en)	1972-05-02	2-(5-nitro-2-furfurylidene)-1-tetralones
NO903583D0 (no)	1990-08-15	Nye forbindelser.