PT90656A - Processo de preparacao de esteroides aromaticos, inibidores da 5-alfa-redutase, e de composicoes farmaceuticas que os contem - Google Patents

Processo de preparacao de esteroides aromaticos, inibidores da 5-alfa-redutase, e de composicoes farmaceuticas que os contem

Info

Publication number: PT90656A
Authority: PT; Portugal
Prior art keywords: alpha; beta; inhibitors; pharmaceutical compositions; redutase
Prior art date: 1988-05-25

Application number

PT90656A

Other languages

English (en)

Other versions

PT90656B (pt

Inventor

Dennis Alan Holt

Mark Alan Levy

Brian Walter Metcalf

Original Assignee

Smithkline Beckman 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

1989-11-30

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

1989-11-30 Publication of PT90656A publication Critical patent/PT90656A/pt

1994-10-31 Publication of PT90656B publication Critical patent/PT90656B/pt

Links

238000002360 preparation method Methods 0.000 title abstract 3
239000003112 inhibitor Substances 0.000 title abstract 2
239000008194 pharmaceutical composition Substances 0.000 title abstract 2
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
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
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)

PT90656A 1988-05-25 1989-05-24 Processo de preparacao de esteroides aromaticos, inibidores da 5-alfa-redutase, e de composicoes farmaceuticas que os contem PT90656B (pt)

Applications Claiming Priority (1)

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

Publications (2)

Publication Number	Publication Date
PT90656A true PT90656A (pt)	1989-11-30
PT90656B PT90656B (pt)	1994-10-31

Family

ID=22733779

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
PT90656A PT90656B (pt)	1988-05-25	1989-05-24	Processo de preparacao de esteroides aromaticos, inibidores da 5-alfa-redutase, e de composicoes farmaceuticas que os contem

Country Status (16)

Country	Link
EP (1)	EP0343954B1 (pt)
JP (1)	JP2675418B2 (pt)
AT (1)	ATE114665T1 (pt)
AU (1)	AU627466B2 (pt)
CA (1)	CA1331457C (pt)
DE (1)	DE68919537T2 (pt)
DK (2)	DK168295B1 (pt)
ES (1)	ES2065378T3 (pt)
GR (1)	GR3015135T3 (pt)
HK (1)	HK1006461A1 (pt)
IE (1)	IE68858B1 (pt)
IL (1)	IL91968A (pt)
NO (1)	NO174964C (pt)
PT (1)	PT90656B (pt)
WO (1)	WO1989011282A1 (pt)
ZA (1)	ZA893971B (pt)

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/en 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 (en)	1994-11-30
DK130393D0 (da)	1993-11-19
IL91968A (en)	1994-10-21
IE68858B1 (en)	1996-07-24
WO1989011282A1 (en)	1989-11-30
ES2065378T3 (es)	1995-02-16
DK168295B1 (da)	1994-03-07
DE68919537T2 (de)	1995-05-11
DE68919537D1 (de)	1995-01-12
ATE114665T1 (de)	1994-12-15
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 (en)	1989-11-29

Legal Events

Date

Code

Title

Description

1994-10-31

FG3A

Patent granted, date of granting

Effective date: 19940406

1999-02-26

MM3A

Annulment or lapse

Free format text: LAPSE DUE TO NON-PAYMENT OF FEES

Effective date: 19981031

Publication	Publication Date	Title
PT90656A (pt)	1989-11-30	Processo de preparacao de esteroides aromaticos, inibidores da 5-alfa-redutase, e de composicoes farmaceuticas que os contem
ATE118505T1 (de)	1995-03-15	Phosphinsäure-derivate von aromatischen steroiden als 5-alpha reduktase-inhibitoren.
ATE114666T1 (de)	1994-12-15	Phosphonsäure-derivate von aromatischen steroiden als 5-alpha-reduktase-inhibitoren.
GR3015476T3 (en)	1995-06-30	Sulphonic acid substituted aromatic steroids as inhibitors of steroid 5-alpha-reductase.
PT92437A (pt)	1990-05-31	Processo de preparacao de derivados da quinazolinona, dos seus intermediarios e de composicoes farmaceuticas que os contem
PT91931A (pt)	1990-04-30	Processo de preparacao de derivados de acido fenilalcanoico e de composicoes farmaceuticas que os contem
DK0787489T3 (da)	2003-08-18	Sammensætning, der indeholder propionyl-L-carnitin og hydroxycitronsyre eller pantothensyre
ATE104845T1 (de)	1994-05-15	Tocopherolsorbat und entzuendungshemmende wirkstoffe enthaltende lichtschutzmittel.
DK0393493T3 (da)	1996-04-15	Fluorerede galdesyrederivater, fremgangsmåder til fremstilling heraf og farmaceutiske midler, som indeholder dem
PT82987B (pt)	1988-07-01	Processo para a preparacao de novos de derivados de acidos carboxilicos bem como de composicoes farmaceuticas que os contem
PT82512B (pt)	1988-03-03	Processo para a preparacao de derivados de quinolilglicinamidas com actividade psicotropica e de composicoes farmaceuticas que os contem
PT81576B (pt)	1987-11-11	Processo para a preparacao de derivados de mercaptano e de composicoes faramceuticas que os contem
ATE35996T1 (de)	1988-08-15	1alpha, 2alpha-methylen-6-methylen- und 6alphamethyl-pregnene, verfahren zu deren herstellung und diese enthaltende pharmazeutische praeparate.
PT94078A (pt)	1991-01-08	Processo para a preparacao de derivados de acido butenoico e de composicoes farmaceuticas que os contem
ES8703423A1 (es)	1987-02-16	Un procedimiento para producir un derivado de acido indola- cetico
DK666989D0 (da)	1989-12-27	Carboximidamidderivater, deres anvendelse og fremgangsmaade til deres fremstilling
ES8200364A1 (es)	1981-11-01	Procedimiento para la obtencion de derivados de la fenotia- zina
ES8307803A1 (es)	1983-08-01	Procedimiento de preparar trimetoxibenzoatos de apovincaminol substituidos con efecto inhibidor de las fosfodiestebasas.
ES8506756A1 (es)	1985-08-01	Procedimiento para preparar derivados de afidicolina.
PT81066B (pt)	1987-10-20	Processo para a preparacao de derivados de arfamenina (acido 5-amino-8-guanidino-4-oxo-2-fenilmetil-octanoico) e de composicoes farmaceuticas que os contem
ZA892643B (en)	1989-12-27	Carbocyclic compounds