ES2042725T3 - Procedimiento para preparar inhibidores de 5-alfa-estersa de esteroide. - Google Patents

Procedimiento para preparar inhibidores de 5-alfa-estersa de esteroide.

Info

Publication number
ES2042725T3
ES2042725T3 ES88300697T ES88300697T ES2042725T3 ES 2042725 T3 ES2042725 T3 ES 2042725T3 ES 88300697 T ES88300697 T ES 88300697T ES 88300697 T ES88300697 T ES 88300697T ES 2042725 T3 ES2042725 T3 ES 2042725T3
Authority
ES
Spain
Prior art keywords
alpha
estersa
preparing
procedure
steroid inhibitors
Prior art date
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.)
Expired - Lifetime
Application number
ES88300697T
Other languages
English (en)
Spanish (es)
Inventor
Dennis Alan Holt
Brian Walter Metcalf
Mark Alan Levy
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.)
Filing date
Publication date
Application filed by SmithKline Beecham Corp filed Critical SmithKline Beecham Corp
Application granted granted Critical
Publication of ES2042725T3 publication Critical patent/ES2042725T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/003—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring the S atom directly linked to a ring carbon atom of 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
    • 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
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/16—Benz[e]indenes; Hydrogenated benz[e]indenes

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
ES88300697T 1987-01-28 1988-01-27 Procedimiento para preparar inhibidores de 5-alfa-estersa de esteroide. Expired - Lifetime ES2042725T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US07/007,539 US4888336A (en) 1987-01-28 1987-01-28 Steroid 5-alpha-reductase inhibitors

Publications (1)

Publication Number Publication Date
ES2042725T3 true ES2042725T3 (es) 1993-12-16

Family

ID=21726780

Family Applications (1)

Application Number Title Priority Date Filing Date
ES88300697T Expired - Lifetime ES2042725T3 (es) 1987-01-28 1988-01-27 Procedimiento para preparar inhibidores de 5-alfa-estersa de esteroide.

Country Status (13)

Country Link
US (1) US4888336A (2)
EP (1) EP0277002B1 (2)
JP (1) JPS63192800A (2)
AT (1) ATE77388T1 (2)
AU (1) AU608560B2 (2)
CA (1) CA1325006C (2)
DE (1) DE3871965T2 (2)
DK (4) DK168525B1 (2)
ES (1) ES2042725T3 (2)
GR (1) GR3005284T3 (2)
IE (1) IE61594B1 (2)
PT (1) PT86652B (2)
ZA (1) ZA88549B (2)

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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]
US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
US4814324A (en) * 1987-03-06 1989-03-21 Merck & Co., Inc. Sterol inhibitors of testosterone 5α-reductase
US5372996A (en) * 1989-03-10 1994-12-13 Endorecherche, Inc. Method of treatment of androgen-related diseases
US5595985A (en) 1989-03-10 1997-01-21 Endorecherche Inc. Combination therapy for prophylaxis and/or treatment of benign prostatic hyperplasia
US5405978A (en) * 1989-05-30 1995-04-11 The Upjohn Company Oxidative preparation of 3,5-secoandrost-5-one-3,17 β-dioic acid
HUT60139A (en) * 1989-07-07 1992-08-28 Endorecherche Inc Process for producing pharmaceutical composition suitable for treating prostate cancer connected with androgen
WO1991000732A1 (en) * 1989-07-07 1991-01-24 Endorecherche Inc. Androgen derivatives for use in the inhibition of sex steroid activity
ATE269066T1 (de) * 1989-07-07 2004-07-15 Endorech Inc Kombinationstherapie zur prophylaxe und/oder behandlung von gutartiger prostatischer hyperplasie
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
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
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
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
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
US5250539A (en) * 1991-08-21 1993-10-05 Eli Lilly And Company Hexahydrobenzo[f]quinolinones
US5304562A (en) * 1991-10-09 1994-04-19 Ciba-Geigy Corporation 17β-substituted Aza-androstane derivatives
CA2084799C (en) 1991-12-17 2003-01-28 Glenn J. Gormley Method of prevention of prostatic carcinoma with 17 beta-n-monosubstituted-carbamoyl-4-aza-5 alpha-androst-1 -en-3-ones
EP0547687A1 (en) * 1991-12-18 1993-06-23 Merck & Co. Inc. 17B-N-Substituted adamantyl/norbonanyl carbamoyl-4-aza-5a-and-rost-1-en-3-ones and androstan-3 ones
ATE165368T1 (de) * 1991-12-20 1998-05-15 Glaxo Wellcome Inc Inhibitoren von testosteron-5-alpha reductase.
ATE195129T1 (de) * 1992-05-20 2000-08-15 Merck & Co Inc 4-azasteroide als 5-alpha-reduktase
CZ283894A3 (en) * 1992-05-20 1995-09-13 Merck & Co Inc 7beta-substituted 4-aza-5alpha-cholestanones, their use for the preparation of pharmaceutical preparations and pharmaceutical compositions containing thereof
AU674145B2 (en) * 1992-05-20 1996-12-12 Merck & Co., Inc. New 17-ester, amide, and ketone derivatives of 3-oxo-4-azasteroids as 5a-reductase inhibitors
US5710275A (en) * 1992-05-20 1998-01-20 Merck & Co., Inc. 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
WO1993023039A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors
AU676478B2 (en) * 1992-05-20 1997-03-13 Merck & Co., Inc. New delta-17 and delta-20 olefinic and saturated 17beta- substituted-4-aza-5alpha-androstan-3-ones as 5alpha- reductase inhibitors
CA2135173A1 (en) * 1992-05-20 1993-11-25 Bruce E. Witzel Ester derivatives of 4-aza-steroids
DE69326008T2 (de) * 1992-05-20 2000-03-02 Merck & Co., Inc. 17-amino-substituierte 4-azasteroide als 5-alpha-reductase inhibitoren
EP0641204B1 (en) * 1992-05-20 2000-08-16 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
GB9210880D0 (en) * 1992-05-21 1992-07-08 Smithkline Beecham Corp Compounds
AU680818B2 (en) * 1992-05-21 1997-08-14 Endorecherche Inc. Improved antiandrogens
JPH07506575A (ja) * 1992-05-21 1995-07-20 アンドルシェルシュ・インコーポレイテッド テストステロン５α−レダクターゼ活性の阻害剤
GB9213901D0 (en) * 1992-06-30 1992-08-12 Smithkline Beecham Corp Compounds
US5302589A (en) * 1992-08-07 1994-04-12 Glaxo, Inc. Heterocyclic inhibitors of 5-α-testosterone reductase
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
HU212459B (en) * 1992-10-02 1996-06-28 Richter Gedeon Vegyeszet Process for producing new 17-beta-substituted 4-aza-androstane-derivatives and pharmaceutical compositions containing them
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
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
US5621104A (en) * 1993-03-24 1997-04-15 Merck & Co., Inc. Substituted 3-phenanthridinone derivatives as 5-alpha-reductase inhibitors
DE69405760T2 (de) * 1993-06-28 1998-04-09 Merck & Co Inc 4-aza-pregnan-5-alpha-reductase isozym 1 inhibitoren
TW408127B (en) * 1993-09-17 2000-10-11 Glaxo Inc Androstenones
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US5817818A (en) * 1994-09-16 1998-10-06 Glaxo Wellcome Inc. Androstenones
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
US6365597B1 (en) * 1996-02-14 2002-04-02 Aventis Pharmaceuticals Inc. 4-aza steroids
US5998427A (en) * 1998-05-14 1999-12-07 Glaxo Wellcome Inc. Androstenones
ES2347027T3 (es) 1998-05-22 2010-10-22 The Board Of Trustees Of The Leland Stanford Junior University Moleculas bifuncionales y terapias basadas en las mismas.
EP2671507A3 (en) 2005-04-28 2014-02-19 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
CA2752373C (en) 2009-02-20 2017-10-10 To-Bbb Holding B.V. Glutathione-based drug delivery system
IL255113B (en) 2009-05-06 2022-09-01 Laboratory Skin Care Inc Dermal delivery compositions comprising active agent-calcium phosphate particle complexes and methods of using the same

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2897202A (en) * 1956-03-19 1959-07-28 Monsanto Chemicals 3-keto-4-aza-delta5-steroids and method of preparing same
AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
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
KR830000085B1 (ko) * 1978-04-13 1983-02-08 제임스 에프. 너우톤 5α-환원효소 억제제로서 유용한 4-아자-17-치환-5α-안드로스탄-3-온류의 제조방법
US4220775A (en) * 1979-03-15 1980-09-02 Merck & Co., Inc. Preparation of 4-aza-17-substituted-5α-androstan-3-ones useful as 5α-reductase inhibitors
US4317817A (en) * 1979-08-27 1982-03-02 Richardson-Merrell Inc. Novel steroid 5α-reductase inhibitors
US4760071A (en) * 1984-02-27 1988-07-26 Merck & Co., Inc. 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors
IL74365A (en) * 1984-02-27 1990-07-26 Merck & Co Inc 17beta-(n-t.-butylcarbamoyl)-4-aza-5alpha-androst-1-en-3-one and pharmaceutical compositions containing it
GB8505862D0 (en) * 1985-03-07 1985-04-11 Erba Farmitalia Steroidic 5alpha-reductase inhibitors

Also Published As

Publication number Publication date
ATE77388T1 (de) 1992-07-15
IE880189L (en) 1988-07-28
AU608560B2 (en) 1991-04-11
PT86652A (pt) 1988-02-01
DK168525B1 (da) 1994-04-11
DK196691A (da) 1991-12-05
CA1325006C (en) 1993-12-07
IE61594B1 (en) 1994-11-16
EP0277002A3 (en) 1988-10-26
DE3871965T2 (de) 1993-01-14
DK169438B1 (da) 1994-10-31
GR3005284T3 (2) 1993-05-24
EP0277002B1 (en) 1992-06-17
US4888336A (en) 1989-12-19
DK37388D0 (da) 1988-01-26
DE3871965D1 (de) 1992-07-23
DK169840B1 (da) 1995-03-13
PT86652B (pt) 1992-02-28
DK37388A (da) 1988-07-29
DK196691D0 (da) 1991-12-05
JPS63192800A (ja) 1988-08-10
EP0277002A2 (en) 1988-08-03
AU1077888A (en) 1988-08-04
DK73594A (da) 1994-06-21
ZA88549B (en) 1988-07-27

Similar Documents

Publication Publication Date Title
ES2042725T3 (es) Procedimiento para preparar inhibidores de 5-alfa-estersa de esteroide.
GEP19981274B (en) Urinary follicle stimulating hormone, pharmaceutical composition, component of pharmaceutical composition
IL87885A (en) Pharmaceutical compositions having antiprogestational and anti-estrogenic activities for the treatment of hormone- dependent tumors
GR1001503B (el) Μέ?οδος δια την παρασκευή φαρμακευτικών ενώσεων αι οποίαι περιέχουν ως δραστική ουσία καρβονικά οξέα τα οποία περιέχουν ?είον κα?ώς και η χρησιμοποίησις αυτών δια την καταπολέμησιν των ρετροιών.
EP0293751A3 (en) Taurohyodeoxycholic acid for the therapy of calculosis of the biliary tract and of biliary dyspepsia
ZA886097B (en) Pharmaceutical composition for the treatment of psoriasis
ES8305684A1 (es) Procedimiento para la obtencion de derivados aminopropanolicos de 2-hidroxi b-fenil-propiofenonas.
AU623805B2 (en) New use of anti-progestomimetic compounds
SE8405588D0 (sv) New compounds
EP0266993A3 (en) Method and therapeutic compositions for the treatment of bleeding disorders
IL85189A (en) Beta-alkyl substituted melatonins,their preparation and pharmaceutical compositions containing them
DK99987D0 (da) Oestrogenpraeparater
AU1200488A (en) Protein c inhibitor (pci) as pharmaceutical and in vitro diagnostic aid, a process for the preparation of a pharmaceutical or diagnostic aid of this type, and an agent containing pci
BG90414A (bg) 2-азабицикло (2,2,1)-хепт-5- ен-2-оцетна киселина и нейни производни, метод за получаване и приложението им
DE3686706D1 (de) Glaukomhemmende zusammensetzungen und verfahren zu ihrer herstellung.
EP0348664A3 (en) Pharmaceutical compositions containing monoacetoacetins for treating tumours
EP0322352A3 (en) Use of anti-progestins for preparation of medicaments
EP0301449A3 (en) Enantiomers of propafenone-containing therapeutic agents
JO1493B1 (en) Pharmaceutical combination for treating high blood pressure
ES8800666A1 (es) Procedimiento para la obtencion de derivados de 1,4-dihidropiridina
AU577570B2 (en) Mefloquine quinates
ES532438A0 (es) Procedimiento para preparar 2-alquiltio-1-amino-alquil-2-pirrolin-3-carbonitrilos
GR3001809T3 (en) Benzylaminoaryldihydropyridine lactones, process for their preparation and their use in medicaments

Legal Events

Date Code Title Description
FG2A Definitive protection

Ref document number: 277002

Country of ref document: ES