LV12572B - Method for introducing a 1,2 double bond into 4-azasteroids, and crystalline phroscor(r) and pharmaceutical compositions thereof - Google Patents

Method for introducing a 1,2 double bond into 4-azasteroids, and crystalline phroscor(r) and pharmaceutical compositions thereof Download PDF

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Publication number
LV12572B
LV12572B LVP-00-117A LV000117A LV12572B LV 12572 B LV12572 B LV 12572B LV 000117 A LV000117 A LV 000117A LV 12572 B LV12572 B LV 12572B
Authority
LV
Latvia
Prior art keywords
crystalline
aza
androst
butylcarbamoyl
finasteride
Prior art date
Application number
LVP-00-117A
Other languages
English (en)
Latvian (lv)
Other versions
LV12572A (en
Inventor
Anthony O. King
Leonard M. WEINSTOCK
Kevin R. Anderson
Richard F. Shuman
Original Assignee
Merck & 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 & Co., Inc. filed Critical Merck & Co., Inc.
Publication of LV12572A publication Critical patent/LV12572A/xx
Publication of LV12572B publication Critical patent/LV12572B/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J73/00Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001Steroids 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
    • C07J73/005Steroids 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)
LVP-00-117A 1989-11-13 2000-09-07 Method for introducing a 1,2 double bond into 4-azasteroids, and crystalline phroscor(r) and pharmaceutical compositions thereof LV12572B (en)

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
LV12572A LV12572A (en) 2000-11-20
LV12572B true LV12572B (en) 2001-04-20

Family

ID=23725148

Family Applications (1)

Application Number Title Priority Date Filing Date
LVP-00-117A LV12572B (en) 1989-11-13 2000-09-07 Method for introducing a 1,2 double bond into 4-azasteroids, and crystalline phroscor(r) and pharmaceutical compositions thereof

Country Status (8)

Country Link
US (1) US5021575A (de)
EP (2) EP0655459B1 (de)
JP (1) JPH0651718B2 (de)
CA (1) CA2029859C (de)
CY (2) CY2079B1 (de)
DE (2) DE69022540T2 (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
ATE165368T1 (de) * 1991-12-20 1998-05-15 Glaxo Wellcome Inc Inhibitoren von testosteron-5-alpha 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
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
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
JP2004508380A (ja) * 2000-09-07 2004-03-18 ドクター・レディーズ・ラボラトリーズ・リミテッド 17−β−(N−ter−ブチルカルバモイル)−4−アザ−5−α−アンドロスト−1−エン−3−オンの新規の多形体及びその調製方法
KR20030029947A (ko) 2000-09-07 2003-04-16 닥터 레디스 레보러터리즈 리미티드 17-β-(엔-티-부틸카르바모일)-4-아자-5-α-안드로스트-1-엔-3-온의 신규의다형태 및 그 제조방법
SK2732003A3 (en) * 2000-09-07 2004-01-08 Reddys Lab Ltd Dr Novel polymorphic form of 17-beta-(N-ter.butyl carbamoyl)-4-aza- 5-alpha-androst-1-en-3-one and a process for preparing it
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
CN1319985C (zh) 2002-07-16 2007-06-06 西格弗里德杰耐克斯国际两合公司 3-氧代-4-氮杂甾族化合物引入1,2-双键的方法
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
DE502004007503D1 (de) * 2003-07-21 2008-08-14 Siegfried Generics Int Ag Verfahren zur herstellung von alpha, beta-ungesattigten ami dverbindungen
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
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
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
CY2079B1 (en) 1998-10-16
EP0655459A2 (de) 1995-05-31
EP0655459A3 (de) 1996-05-22
CY2199B1 (en) 2002-11-08
EP0428366A2 (de) 1991-05-22
LV12572A (en) 2000-11-20
EP0428366A3 (en) 1992-07-29
JPH0651718B2 (ja) 1994-07-06
JPH03206096A (ja) 1991-09-09
EP0655459B1 (de) 2000-05-03
DE69022540D1 (de) 1995-10-26
DE69022540T2 (de) 1996-05-02
US5021575A (en) 1991-06-04
CA2029859A1 (en) 1991-05-14
CA2029859C (en) 2002-05-14
DE69033538T2 (de) 2001-01-04
EP0428366B1 (de) 1995-09-20
HK1002708A1 (en) 1998-09-11
DE69033538D1 (de) 2000-06-08

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