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FI945441L - Nytt förfarande för framställning av 7beta-substituerad-4-aza-5alfa-androstan-3-oner - Google Patents

Nytt förfarande för framställning av 7beta-substituerad-4-aza-5alfa-androstan-3-oner 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)
Other versions
FI945441A7 (sv
FI945441A0 (sv
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 FI945441A7 publication Critical patent/FI945441A7/sv
Publication of FI945441A0 publication Critical patent/FI945441A0/sv
Publication of FI945441L publication Critical patent/FI945441L/sv

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/76—Unsaturated compounds containing keto groups
    • C07C59/80—Unsaturated compounds containing keto groups containing rings other than six-membered aromatic rings
    • C07C59/82—Unsaturated compounds containing keto groups containing rings other than six-membered aromatic rings the keto group being part of a ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C07F7/1872—Preparation; Treatments not provided for in C07F7/20
    • C07F7/1892—Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888
    • 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
    • C07J1/0003—Androstane derivatives
    • C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • C07J1/0022—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • 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
    • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Steroid Compounds (AREA)
FI945441A 1992-05-20 1993-05-11 Nytt förfarande för framställning av 7beta-substituerad-4-aza-5alfa-androstan-3-oner FI945441L (sv)

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
FI945441A7 FI945441A7 (sv) 1994-11-18
FI945441A0 FI945441A0 (sv) 1994-11-18
FI945441L true FI945441L (sv) 1994-11-18

Family

ID=25388268

Family Applications (1)

Application Number Title Priority Date Filing Date
FI945441A FI945441L (sv) 1992-05-20 1993-05-11 Nytt förfarande för framställning av 7beta-substituerad-4-aza-5alfa-androstan-3-oner

Country Status (11)

Country Link
US (2) US5237064A (sv)
CN (1) CN1084519A (sv)
AU (1) AU4243993A (sv)
CZ (1) CZ283794A3 (sv)
FI (1) FI945441L (sv)
HU (1) HUT68232A (sv)
RO (1) RO112427B1 (sv)
RU (1) RU2114117C1 (sv)
SK (1) SK137894A3 (sv)
TW (1) TW234129B (sv)
WO (1) WO1993023376A1 (sv)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
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WO1993023420A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 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
FI945442A7 (sv) * 1992-05-20 1994-11-18 Merck & Co Inc Nya 7beta-substituerade 4-aza-5alfa-kolestanoner som 5alfa-reduktasinh ibitorer
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
EP0641211A1 (en) * 1992-05-21 1995-03-08 Endorecherche Inc. INHIBITORS OF TESTOSTERONE 5$g(a)-REDUCTASE ACTIVITY
US5658922A (en) * 1993-06-28 1997-08-19 Merck & Co., Inc. 4-aza-pregnane 5α-reductase isozyme 1 inhibitors
JPH09504553A (ja) * 1993-11-04 1997-05-06 メルク エンド カンパニー インコーポレーテッド ５α−レダクターゼ阻害薬としての７−置換−４−アザ−ステロイド誘導体
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
AU1097995A (en) * 1993-11-18 1995-06-06 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
CA2233084A1 (en) * 1995-10-19 1997-04-24 Merck & Co., Inc. 16-substituted-6-aza-steroid 5-.alpha.-reductase inhibitors
DE69615046T2 (de) * 1995-10-23 2002-06-27 Merck & Co., Inc. 17-alkyl-7-substituierte-4-aza-steroidderivate
US5763361A (en) * 1995-10-23 1998-06-09 Merck & Co., Inc. 17-alkyl-7-substituted-4-aza steroid derivatives as 5-α-reductase inhibitors
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
AU6462598A (en) * 1997-03-17 1998-10-12 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
EP1832598A3 (en) * 1999-09-30 2008-01-02 Hollis-Eden Pharmaceuticals Inc. Therapeutic treatment of androgen receptor driven conditions
WO2001024763A2 (en) 1999-10-01 2001-04-12 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
PL376919A1 (pl) * 2002-11-06 2006-01-09 Pharmacia & Upjohn Company Llc Sposoby wytwarzania 7-karboksy-podstawionych steroidów
TWI280133B (en) * 2002-11-07 2007-05-01 Upjohn Co Process for preparing C-7 substituted steroids
JP4682985B2 (ja) * 2005-07-06 2011-05-11 パナソニック株式会社 ブラシレスｄｃモータおよびそれを搭載した電気機器
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
BRPI1008745A2 (pt) 2009-02-05 2019-09-17 Tokai Pharmaceuticals Inc pró-fármacos de inibidores esteroidais de cyp17/antiandrogênios
EP4066841A1 (en) 2013-03-14 2022-10-05 University of Maryland, Baltimore Androgen receptor down-regulating agents and uses thereof
WO2015023710A1 (en) 2013-08-12 2015-02-19 Tokai Pharmaceuticals, Inc. Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies

Family Cites Families (31)

* Cited by examiner, † Cited by third party
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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
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
US4596812A (en) * 1976-05-24 1986-06-24 The Upjohn Company Methods and solutions for treating male pattern alopecia
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
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
ATE67503T1 (de) * 1984-02-27 1991-10-15 Merck & Co Inc 17-beta-substituierte-4-aza-5-alpha-androstenon und ihre anwendung als 5-alpha-reduktaseinhibitoren.
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
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US5237065A (en) * 1987-01-28 1993-08-17 Smithkline Beecham Corporation Steroid 5-alpha-reductase inhibitors
US4910226A (en) * 1987-04-29 1990-03-20 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
JP2675418B2 (ja) * 1988-05-25 1997-11-12 スミスクライン・ベックマン・コーポレイション 芳香族ステロイド５‐α‐レダクターゼ抑制剤
US4937237A (en) * 1988-12-23 1990-06-26 Smithkline Beckman Corporation Phosphinic acid substituted aromatic steroids as inhibitors of steroid 5-60 -reductase
US4882319A (en) * 1988-12-23 1989-11-21 Smithkline Beckman Corporation Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase
US5026882A (en) * 1988-12-23 1991-06-25 Smithkline Beecham Corporation Phosphinic acid substituted steroids as inhibitors of steroid 5α-reductase
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US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
WO1993023420A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 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 (sv) 1994-11-11
AU4243993A (en) 1993-12-13
FI945441A7 (sv) 1994-11-18
FI945441A0 (sv) 1994-11-18
SK137894A3 (en) 1995-05-10
US5578726A (en) 1996-11-26
RO112427B1 (ro) 1997-09-30
HUT68232A (en) 1995-06-28
CZ283794A3 (en) 1995-10-18
CN1084519A (zh) 1994-03-30
WO1993023376A1 (en) 1993-11-25
RU94046041A (ru) 1996-10-10
US5237064A (en) 1993-08-17
RU2114117C1 (ru) 1998-06-27

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Legal Events

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