DE69033538D1 - Verfahren zur Herstellung der 1,2-Doppelbindung von 4-aza-Steroiden und kristallinen Proscor(R) und pharmazeutische Präparate davon - Google Patents

Verfahren zur Herstellung der 1,2-Doppelbindung von 4-aza-Steroiden und kristallinen Proscor(R) und pharmazeutische Präparate davon

Info

Publication number
DE69033538D1
DE69033538D1 DE69033538T DE69033538T DE69033538D1 DE 69033538 D1 DE69033538 D1 DE 69033538D1 DE 69033538 T DE69033538 T DE 69033538T DE 69033538 T DE69033538 T DE 69033538T DE 69033538 D1 DE69033538 D1 DE 69033538D1
Authority
DE
Germany
Prior art keywords
proscor
crystalline
preparation
double bond
pharmaceutical preparations
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
DE69033538T
Other languages
English (en)
Other versions
DE69033538T2 (de
Inventor
Anthony O King
Leonard M Weinstock
R Kevin Anderson
Richard F Shuman
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.)
Merck Sharp and Dohme LLC
Original Assignee
Merck and Co Inc
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 Merck and Co Inc filed Critical Merck and Co Inc
Publication of DE69033538D1 publication Critical patent/DE69033538D1/de
Application granted granted Critical
Publication of DE69033538T2 publication Critical patent/DE69033538T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)
DE69033538T 1989-11-13 1990-11-13 Verfahren zur Herstellung der 1,2-Doppelbindung von 4-aza-Steroiden und kristallinen Proscor(R) und pharmazeutische Präparate davon Expired - Lifetime DE69033538T2 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US07/434,663 US5021575A (en) 1989-11-13 1989-11-13 Method for introducing a 1,2 double bond into azasteroids

Publications (2)

Publication Number Publication Date
DE69033538D1 true DE69033538D1 (de) 2000-06-08
DE69033538T2 DE69033538T2 (de) 2001-01-04

Family

ID=23725148

Family Applications (2)

Application Number Title Priority Date Filing Date
DE69033538T Expired - Lifetime DE69033538T2 (de) 1989-11-13 1990-11-13 Verfahren zur Herstellung der 1,2-Doppelbindung von 4-aza-Steroiden und kristallinen Proscor(R) und pharmazeutische Präparate davon
DE69022540T Expired - Fee Related DE69022540T2 (de) 1989-11-13 1990-11-13 Verfahren zur 1,2 Dehydrogenierung der Azasteroiden.

Family Applications After (1)

Application Number Title Priority Date Filing Date
DE69022540T Expired - Fee Related DE69022540T2 (de) 1989-11-13 1990-11-13 Verfahren zur 1,2 Dehydrogenierung der Azasteroiden.

Country Status (8)

Country Link
US (1) US5021575A (de)
EP (2) EP0428366B1 (de)
JP (1) JPH0651718B2 (de)
CA (1) CA2029859C (de)
CY (2) CY2079B1 (de)
DE (2) DE69033538T2 (de)
HK (1) HK1002708A1 (de)
LV (1) LV12572B (de)

Families Citing this family (32)

* 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]
US5120847A (en) * 1990-08-27 1992-06-09 Merck & Co., Inc. Process for iodinating or brominating the α-methylenic carbon of a secondary amide
IE76452B1 (en) * 1990-10-29 1997-10-22 Sankyo Co Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use
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 (de) * 1991-12-18 1993-06-23 Merck & Co. Inc. 17-Beta-substituierte Adamantyl/Norbornanyl Carbamoyl-4-Aza-5-Alpha-Androsta-1-En-3-Onen und Androstan-3-Onen
WO1993013124A1 (en) * 1991-12-20 1993-07-08 Glaxo Inc. Inhibitors of 5-alpha-testosterone reductase
US5302589A (en) * 1992-08-07 1994-04-12 Glaxo, Inc. Heterocyclic inhibitors of 5-α-testosterone reductase
US5468860A (en) * 1992-11-19 1995-11-21 Merck & Co., Inc. New finasteride processes
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
TW408127B (en) * 1993-09-17 2000-10-11 Glaxo Inc Androstenones
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
US6001844A (en) 1995-09-15 1999-12-14 Merck & Co., Inc. 4-Azasteroids for treatment of hyperandrogenic conditions
US6365597B1 (en) 1996-02-14 2002-04-02 Aventis Pharmaceuticals Inc. 4-aza steroids
AUPO533497A0 (en) 1997-02-21 1997-03-20 Frontier Tower Pty Ltd Self-adhesive decorative devices
US6187925B1 (en) 1997-12-23 2001-02-13 Merck & Co., Inc. Intermediates and process for the synthesis of azasteroids
US5998427A (en) * 1998-05-14 1999-12-07 Glaxo Wellcome Inc. Androstenones
MXPA03002031A (es) 2000-09-07 2004-12-13 Reddys Lab Ltd Dr Forma polimorfica novedosa de 17-beta-(n-tercbutil carbamoil)-4-aza-5-alfa-androst-1-en-3-ona y proceso para preparar la misma.
HUP0300937A3 (en) * 2000-09-07 2007-10-29 Reddys Lab Ltd Dr Novel polymorphic form of 17-betha-(n-ter. butyl carbamoyl)-4-aza-5alpha-androst-1-en-3-one and process for preparing it
EP1790653A3 (de) * 2000-09-07 2010-06-02 Dr. Reddy's Laboratories Ltd. Neue polymorphe Form von 17-beta-(n-ter.butyl carbomyol)-4-aza-5- alpha-androst-1-en-3-one und ein Verfahren zu ihrer Herstellung
US6645974B2 (en) 2001-07-31 2003-11-11 Merck & Co., Inc. Androgen receptor modulators and methods for use thereof
ES2185503B1 (es) * 2001-09-29 2004-08-01 Ragactives, S.L. Procedimiento para la obtencion de 17beta-(sustituido)-3-oxoalfa1,2-4-azaesteroides e intermedios.
HU227117B1 (en) 2002-05-10 2010-07-28 Richter Gedeon Nyrt Process for dehydrogenation of aza-androstane compounds
KR100872722B1 (ko) * 2002-06-28 2008-12-05 주식회사 중외제약 피나스테라이드의 제조방법
BR0312672A (pt) 2002-07-16 2005-04-26 Siegfried Ltd Processo para a preparação de compostos
ES2206065B1 (es) 2002-10-31 2005-08-16 Ragactives, S.L. Procedimiento para la obtencion de la forma polimorfica i de finasterida.
KR100508019B1 (ko) * 2003-07-19 2005-08-17 한미약품 주식회사 고순도 1-안드로스텐 유도체의 제조 방법
AU2004256860A1 (en) * 2003-07-21 2005-01-27 Siegfried Generics International Ag Method for production of $g(a),$g(b)-unsaturated amide compounds
WO2005066196A1 (en) * 2003-12-30 2005-07-21 Ranbaxy Laboratories Limited Amorphous form of finasteride and processes for its preparation
US7531658B2 (en) * 2006-01-20 2009-05-12 Apotex Pharmachem Inc. Process for the preparation of 17-N-substituted-carbamoyl-4-aza-androst-1-en-3-ones
HU230730B1 (hu) 2011-06-30 2017-12-28 Richter Gedeon Nyrt Eljárás (5alfa,17béta)-N-[2,5-bisz-(trifluormetil)-fenil]-3-oxo-4-aza-5-androszt-1-én-17-karbonsavamid előállítására

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
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
NZ211145A (en) * 1984-02-27 1988-10-28 Merck & Co Inc 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions
NZ225100A (en) * 1987-06-29 1991-09-25 Merck & Co Inc Reaction of steroids (including 4-azasteroids) with a silylating agent in the presence of a quinone to introduce a delta' double bond and silylated intermediates

Also Published As

Publication number Publication date
HK1002708A1 (en) 1998-09-11
JPH0651718B2 (ja) 1994-07-06
EP0655459A3 (de) 1996-05-22
EP0655459A2 (de) 1995-05-31
LV12572B (en) 2001-04-20
EP0428366B1 (de) 1995-09-20
US5021575A (en) 1991-06-04
CY2079B1 (en) 1998-10-16
JPH03206096A (ja) 1991-09-09
EP0428366A2 (de) 1991-05-22
EP0655459B1 (de) 2000-05-03
LV12572A (en) 2000-11-20
DE69022540D1 (de) 1995-10-26
CY2199B1 (en) 2002-11-08
CA2029859C (en) 2002-05-14
CA2029859A1 (en) 1991-05-14
DE69022540T2 (de) 1996-05-02
EP0428366A3 (en) 1992-07-29
DE69033538T2 (de) 2001-01-04

Similar Documents

Publication Publication Date Title
DE69033538T2 (de) Verfahren zur Herstellung der 1,2-Doppelbindung von 4-aza-Steroiden und kristallinen Proscor(R) und pharmazeutische Präparate davon
EP0263569A3 (en) 9-alpha-hydroxysteroids,process for their preparation,process for the preparation of the corresponding 9(11)-dehydro-derivatives and pharmaceutical preparations containing said steroids
PT86366A (en) Process for the preparation of phosphinic acid derivatives and of pharmaceutical compositions containing the same
PT84936A (en) Process for the preparation of tetrahydronaphthaline and indanederivatives and of pharmaceutical compositions containing the same
PT84964A (en) Process for the preparation of 1,5-diaryl-3-substituted-pyrazoles and of pharmaceutical compositions containing them
PT84857A (en) Process for the preparation of extracts of nerium species and of pharmaceutical compositions containing them
PT86018A (en) Process for the preparation of alpha-amino-alpha-(alkylphenyl)-alkyl-ethanoic acids and their by-products and pharmaceutical compositions therewith
PT86365A (en) Process for the preparation of pyridazodiazepine derivatives and of pharmaceutical compositions containing the same
NO872551D0 (no) Fremgangsmaate for fremstilling av farmasoeytiske preparater
PT84358A (en) Process for the preparation of naphthothiazepinones and of pharmaceutical compositions containing the same
PT84479A (en) Process for the preparation of acids 1,2,3,4-tetrahydro-6-substituted-4-aryl-(or heterocycycle)-3-](substituted amino)carbonyl"-2-thioxo-(or oxo)-5-pyrimidinecarboxylics and esters
ATE100095T1 (de) 2,2-dimethylchromenderivate, verfahren zur herstellung und diese enthaltende pharmazeutische zusammenstellungen.
PT87024A (pt) Process for the preparation of propiolophenone derivatives and of pharmaceutical compositions containing the same
NO874200L (no) Fremgangsmaate for fremstilling av farmasoeytiske preparater
PT84184A (pt) Process for the preparation of 8 alpha-acylaminoergolines and of pharmaceutical compositions containing them
ATE109137T1 (de) Pyridinderivate, verfahren zur herstellung und pharmazeutische zusammensetzungen.
DE69016592D1 (de) 4-Amidino-Chroman und 4-Amidino-Pyrano(3,2-c)pyridinderivate, Verfahren zur Herstellung und diese enthaltende pharmazeutische Zusammenstellungen.
PT83984A (en) Process for the preparation of novel 16,17-acetalsubstituted pregnane 21-oic derivatives and of pharmaceutical compositions containing the same
NO875359L (no) Fremgangsmaate for fremstilling av farmasoeytiske preparater
NO873423D0 (no) Fremgangsmaate for fremstilling av farmasoeytiske preparater
NO872233D0 (no) Fremgangsmaate for fremstilling av farmasoeytiske preparater
IL82294A0 (en) 1,3-dihydropyridine derivatives,process for the preparation thereof and pharmaceutical compositions containing the same
PT86489A (de) Verfahren zur herstellung von lipophilen aminosaeurederivaten sowie lipophile aminosaeurederivate
PT85667A (en) Process for the preparation of isoprene derivatives and of pharmaceutical compositions containing the same
DE69012430D1 (de) Verfahren zur Herstellung von Sulfoniumverbindungen und Methylthiophenylderivaten.

Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8327 Change in the person/name/address of the patent owner

Owner name: MERCK SHARP & DOHME CORP., NEW JERSEY, N.J., US