FI945441L - Uusi menetelmä 7beta-substituoitu-4-atsa-5alfa-androstan-3-onien valmistamiseksi - Google Patents

Uusi menetelmä 7beta-substituoitu-4-atsa-5alfa-androstan-3-onien valmistamiseksi Download PDF

Info

Publication number
FI945441L
FI945441L FI945441A FI945441A FI945441L FI 945441 L FI945441 L FI 945441L FI 945441 A FI945441 A FI 945441A FI 945441 A FI945441 A FI 945441A FI 945441 L FI945441 L FI 945441L
Authority
FI
Finland
Prior art keywords
7beta
5alpha
androstan
aza
ones
Prior art date
Application number
FI945441A
Other languages
English (en)
Finnish (fi)
Swedish (sv)
Other versions
FI945441A0 (fi
FI945441A7 (fi
Inventor
Raman K Bakshi
Gary H Rasmusson
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 FI945441L publication Critical patent/FI945441L/fi
Publication of FI945441A0 publication Critical patent/FI945441A0/fi
Publication of FI945441A7 publication Critical patent/FI945441A7/fi

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40Unsaturated compounds
    • C07C59/76Unsaturated compounds containing keto groups
    • C07C59/80Unsaturated compounds containing keto groups containing rings other than six-membered aromatic rings
    • C07C59/82Unsaturated compounds containing keto groups containing rings other than six-membered aromatic rings the keto group being part of a ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • C07F7/1872Preparation; Treatments not provided for in C07F7/20
    • C07F7/1892Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003Androstane derivatives
    • C07J1/0018Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • C07J1/0022Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Steroid Compounds (AREA)
FI945441A 1992-05-20 1993-05-11 Uusi menetelmä 7beta-substituoitu-4-atsa-5alfa-androstan-3-onien valmi stamiseksi FI945441A7 (fi)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/886,049 US5237064A (en) 1992-05-20 1992-05-20 Process for producing 7β-substituted-aza-5αandrostan-3-ones
PCT/US1993/004443 WO1993023376A1 (en) 1992-05-20 1993-05-11 NEW PROCESS FOR PRODUCING 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES

Publications (3)

Publication Number Publication Date
FI945441L true FI945441L (fi) 1994-11-18
FI945441A0 FI945441A0 (fi) 1994-11-18
FI945441A7 FI945441A7 (fi) 1994-11-18

Family

ID=25388268

Family Applications (1)

Application Number Title Priority Date Filing Date
FI945441A FI945441A7 (fi) 1992-05-20 1993-05-11 Uusi menetelmä 7beta-substituoitu-4-atsa-5alfa-androstan-3-onien valmi stamiseksi

Country Status (11)

Country Link
US (2) US5237064A (en:Method)
CN (1) CN1084519A (en:Method)
AU (1) AU4243993A (en:Method)
CZ (1) CZ283794A3 (en:Method)
FI (1) FI945441A7 (en:Method)
HU (1) HUT68232A (en:Method)
RO (1) RO112427B1 (en:Method)
RU (1) RU2114117C1 (en:Method)
SK (1) SK137894A3 (en:Method)
TW (1) TW234129B (en:Method)
WO (1) WO1993023376A1 (en:Method)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
AU4251993A (en) * 1992-05-20 1993-12-13 Merck & Co., Inc. Substituted 4-aza-5A-androstan-ones as 5A-reductase inhibitors
WO1995012398A1 (en) * 1993-11-04 1995-05-11 Merck & Co., Inc. 7-substituted-4-aza-steroid derivatives as 5-alpha- reductase inhibitors
RU94046044A (ru) * 1992-05-20 1996-10-10 Мерк Энд Ко. Новые 7 бета -замещенные 4-аза- 5 альфа -холестан-оны в качестве ингибиторов 5 альфа -редуктазы, фармацевтическая композиция на их основе, способ ее получения
US5710275A (en) * 1992-05-20 1998-01-20 Merck & Co., Inc. 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
FI945457L (fi) * 1992-05-21 1995-01-16 Endorecherche Inc Testosteronin 5alfa-reduktaasiaktiviteetin inhibiittorit
CA2165077A1 (en) * 1993-06-28 1995-01-05 Philippe L. Durette 4-aza-pregnane 5.alpha.-reductase isozyme 1 inhibitors
IL111467A0 (en) * 1993-11-12 1994-12-29 Merck & Co Inc Pharmaceutical compositions comprising 7 beta -substituted -4-aza 5 alpha -cholestan-3-ones and 5 alpha reductase 1 inhibitors
WO1995013815A1 (en) * 1993-11-18 1995-05-26 Merck & Co., Inc. Combination method for the treatment of patterned alopecia
US5470976A (en) * 1994-09-07 1995-11-28 Merck & Co., Inc. Process for the stereoselective reduction of steroid enelactams
US5656613A (en) * 1995-01-04 1997-08-12 Merck & Co., Inc. Treatment of hyperandrogenic conditions
US5585383A (en) * 1995-05-03 1996-12-17 Merck & Co., Inc. Process for crystallizing a 4-azasteroid 5alpha-reductase inhibitor
JPH11513684A (ja) * 1995-10-19 1999-11-24 メルク エンド カンパニー インコーポレーテッド 16−置換−6−アザ−ステロイド5α−レダクターゼ阻害剤
US5763361A (en) * 1995-10-23 1998-06-09 Merck & Co., Inc. 17-alkyl-7-substituted-4-aza steroid derivatives as 5-α-reductase inhibitors
DE69615046T2 (de) * 1995-10-23 2002-06-27 Merck & Co., Inc. 17-alkyl-7-substituierte-4-aza-steroidderivate
AU5791698A (en) * 1996-12-09 1998-07-03 Merck & Co., Inc. Methods and compositions for preventing and treating bone loss
US5994334A (en) * 1997-02-05 1999-11-30 University Of Maryland Androgen synthesis inhibitors
WO1998041211A1 (en) * 1997-03-17 1998-09-24 Merck & Co., Inc. Methods and compositions for treating polycystic ovary syndrome
US5994335A (en) * 1997-10-17 1999-11-30 The University Of Maryland, Baltimore 17-azolyl steroids useful as androgen synthesis inhibitors
US6187925B1 (en) 1997-12-23 2001-02-13 Merck & Co., Inc. Intermediates and process for the synthesis of azasteroids
PT1955700E (pt) 1999-09-30 2011-05-04 Harbor Biosciences Inc Tratamento terap?utico de doen?as associadas ao receptor de androg?nios
HK1049787B (en) 1999-10-01 2014-07-25 Immunogen, Inc. Compositions and methods for treating cancer using immunoconjugates and chemotherapeutic agents
KR100503193B1 (ko) * 2002-08-19 2005-07-25 한미약품 주식회사 3-옥소-4-아자-5α-안드로스탄 화합물의 선택적인 제조방법
AU2003213807A1 (en) * 2002-11-06 2004-06-03 Pharmacia & Upjohn Company Llc Processes for preparing 7-carboxy substituted steroids
ATE354583T1 (de) * 2002-11-07 2007-03-15 Pharmacia & Upjohn Co Llc Verfahren zur herstellung c-7 substituierter 5- androstene
WO2007004429A1 (en) * 2005-07-06 2007-01-11 Matsushita Electric Industrial Co., Ltd. Brushless dc motor and electric device using the same
CN100355772C (zh) * 2005-12-28 2007-12-19 天津大学 具有5α-还原酶抑制活性的甾体化合物及其制备方法
US7847457B2 (en) * 2007-05-09 2010-12-07 Federal-Mogul World Wide, Inc BLDC motor assembly
US20100048524A1 (en) 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
ES2552087T3 (es) 2009-02-05 2015-11-25 Tokai Pharmaceuticals, Inc. Nuevos profármacos de inhibidores de CYP17 esteroidales/antiandrógenos
US9884067B2 (en) 2013-03-14 2018-02-06 University Of Maryland, Baltimore Androgen receptor down-regulating agents and uses thereof
MX2016001901A (es) 2013-08-12 2016-10-13 Tokai Pharmaceuticals Inc Biomarcadores para tratamiento de trastornos neoplasicos usando terapias dirigidas con andrógeno.

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2227876A (en) * 1937-10-16 1941-01-07 Firm Of N V Organon Steroid derivatives with nuclear substituted nitrogen
US3285918A (en) * 1962-04-18 1966-11-15 Norman J Doorenbos 1', 4', 5', 6'-tetrahydropyrimidino[a-4, 3]-4-aza-5-cholestene
US3239417A (en) * 1962-12-07 1966-03-08 Smith Kline French Lab Methods and compositions for inhibiting sterol biosynthesis
US3264301A (en) * 1963-08-22 1966-08-02 Norman J Doorenbos Substituted-4-azasteroids
FR1465544A (fr) * 1965-11-29 1967-01-13 Roussel Uclaf Dérivés stéroïdes aromatiques substitués par un atome d'azote endocyclique et procédé de préparation
CA970692A (en) * 1971-11-08 1975-07-08 Walter Voigt METHODS OF INHIBITING THE ACTIVITY OF TESTOSTERONE 5.alpha.-REDUCTASE
US4596812A (en) * 1976-05-24 1986-06-24 The Upjohn Company Methods and solutions for treating male pattern alopecia
US4139619A (en) * 1976-05-24 1979-02-13 The Upjohn Company 6-Amino-4-(substituted amino)-1,2-dihydro-1-hydroxy-2-iminopyrimidine, topical compositions and process for hair growth
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
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
EP0314199B1 (en) * 1984-02-27 1991-09-18 Merck & Co. Inc. 17 beta-substituted-4-aza-5 alpha-androstenones and their use as 5 alpha-reductase inhibitors
US4859681A (en) * 1984-02-27 1989-08-22 Merck & Co., Inc. 17 α-Acyl-4-aza-5a-androst-1-en-3-ones as 5 alpha-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
US5049562A (en) * 1984-02-27 1991-09-17 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α-reductase inhibitors
GB8505862D0 (en) * 1985-03-07 1985-04-11 Erba Farmitalia Steroidic 5alpha-reductase inhibitors
US4845104A (en) * 1986-11-20 1989-07-04 Merck & Co., Inc. Oxidized analogs of 17β-N-monosubstituted-carbamoyl-4-aza-5-α-androstan-3-ones
US5237065A (en) * 1987-01-28 1993-08-17 Smithkline Beecham Corporation Steroid 5-alpha-reductase inhibitors
US4888336A (en) * 1987-01-28 1989-12-19 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
US4910226A (en) * 1987-04-29 1990-03-20 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
AU627466B2 (en) * 1988-05-25 1992-08-27 Smithkline Beckman Corporation Aromatic steroid 5-alpha-reductase inhibitors
US4937237A (en) * 1988-12-23 1990-06-26 Smithkline Beckman Corporation Phosphinic acid substituted aromatic steroids as inhibitors of steroid 5-60 -reductase
US5026882A (en) * 1988-12-23 1991-06-25 Smithkline Beecham Corporation Phosphinic acid substituted steroids as inhibitors of steroid 5α-reductase
US4882319A (en) * 1988-12-23 1989-11-21 Smithkline Beckman Corporation Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase
US4970205A (en) * 1988-12-23 1990-11-13 Smithkline Beecham Corporation Sulfonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase
GB9002922D0 (en) * 1990-02-09 1990-04-04 Erba Carlo Spa 17 beta-substituted-4-aza-5 alpha-androstan-3-one derivatives and process for their preparation
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
US5710275A (en) * 1992-05-20 1998-01-20 Merck & Co., Inc. 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
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

Also Published As

Publication number Publication date
TW234129B (en:Method) 1994-11-11
CN1084519A (zh) 1994-03-30
RU2114117C1 (ru) 1998-06-27
AU4243993A (en) 1993-12-13
HUT68232A (en) 1995-06-28
SK137894A3 (en) 1995-05-10
FI945441A0 (fi) 1994-11-18
RU94046041A (ru) 1996-10-10
RO112427B1 (ro) 1997-09-30
FI945441A7 (fi) 1994-11-18
WO1993023376A1 (en) 1993-11-25
US5237064A (en) 1993-08-17
CZ283794A3 (en) 1995-10-18
US5578726A (en) 1996-11-26

Similar Documents

Publication Publication Date Title
FI945441L (fi) Uusi menetelmä 7beta-substituoitu-4-atsa-5alfa-androstan-3-onien valmistamiseksi
FI945451L (fi) Makeutusaineina käytettäviä yhdisteitä sekä menetelmä niiden valmistamiseksi
FI944619A7 (fi) Aldolisointi-dehydratointimenetelmä
FI951596L (fi) Menetelmä 10-desasetyylibakkatiini-III:n saamiseksi
DK317889A (da) Sproejtemetode
DE69326663D1 (de) Unterschneidungsverfahren
FI931736A0 (fi) Biodegraderbart tgf-b-leveranssystem foer benregeneration
FI103666B (fi) Menetelmä bifenyylijohdannaisen valmistamiseksi
EE03048B1 (et) Meetod lovastatiini valmistamiseks
FI925357L (fi) Rakennusmenetelmä
DK293686A (da) Begroning modvirkende maling
NO930574D0 (no) Fremgangsmaate for fremstilling av desfluran
FI970564L (fi) Uusi menetelmä di-isopinokamfeyyliklooriboraanin valmistamiseksi
DK96392D0 (da) Modifikationsmetode
FI933816L (fi) Understaell foer raelsfordon
NO923907L (no) Fremgangsmaate for fremstilling av et smoerepaalegg
FI904570A7 (fi) Menetelmä uusien alkanofenonien valmistamiseksi I
FI954749L (fi) Uusi menetelmä klonidiinijohdannaisten valmistamiseksi
NO931839D0 (no) Fremgangsmaate for fremstilling av pergolid
FI920675L (fi) Uusi menetelmä 9-amino-1,2,3,4-tetrahydroakridiinien valmistamiseksi
EP0474182A3 (en) Method for the purification of a bifidobacteria-proliferating substance
FI892144A7 (fi) Menetelmä 5-C-hydroksimetyylialdoheksoosipohjaisten yhdisteiden valmistamiseksi
FI972694A0 (fi) Uusi menetelmä sameridiinin valmistamiseksi
FI953617L (fi) Menetelmä substituoitujen 4-hydroksikumariinien valmistamiseksi
FI943660A7 (fi) Menetelmä 3-karbonyyliandrostadieeni-17-karboksamidien valmistamiseksi

Legal Events

Date Code Title Description
FD Application lapsed