ATE195530T1 - 17-ether und thioether von 4-aza-steroiden - Google Patents

17-ether und thioether von 4-aza-steroiden

Info

Publication number
ATE195530T1
ATE195530T1 AT93911358T AT93911358T ATE195530T1 AT E195530 T1 ATE195530 T1 AT E195530T1 AT 93911358 T AT93911358 T AT 93911358T AT 93911358 T AT93911358 T AT 93911358T AT E195530 T1 ATE195530 T1 AT E195530T1
Authority
AT
Austria
Prior art keywords
pct
thioether
ether
date nov
sec
Prior art date
Application number
AT93911358T
Other languages
English (en)
Inventor
Bruce E Witzel
Richard L Tolman
Gary H Rasmusson
Raman K Bakshi
Shu Shu Yang
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
Application granted granted Critical
Publication of ATE195530T1 publication Critical patent/ATE195530T1/de

Links

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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Cosmetics (AREA)
AT93911358T 1992-05-20 1993-05-19 17-ether und thioether von 4-aza-steroiden ATE195530T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US88603192A 1992-05-20 1992-05-20
PCT/US1993/004746 WO1993023040A1 (en) 1992-05-20 1993-05-19 17-ethers and thioethers of 4-aza-steroids

Publications (1)

Publication Number Publication Date
ATE195530T1 true ATE195530T1 (de) 2000-09-15

Family

ID=25388234

Family Applications (1)

Application Number Title Priority Date Filing Date
AT93911358T ATE195530T1 (de) 1992-05-20 1993-05-19 17-ether und thioether von 4-aza-steroiden

Country Status (9)

Country Link
US (1) US5536727A (de)
EP (1) EP0641204B1 (de)
JP (1) JPH07508038A (de)
AT (1) ATE195530T1 (de)
AU (1) AU668180B2 (de)
CA (1) CA2135174A1 (de)
DE (1) DE69329240D1 (de)
ES (1) ES2148229T3 (de)
WO (1) WO1993023040A1 (de)

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JP5461405B2 (ja) 2007-09-14 2014-04-02 バーテックス ファーマシューティカルズ インコーポレイテッド 嚢胞性線維症膜コンダクタンス制御因子の調節因子
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Also Published As

Publication number Publication date
EP0641204B1 (de) 2000-08-16
ES2148229T3 (es) 2000-10-16
CA2135174A1 (en) 1993-11-25
AU668180B2 (en) 1996-04-26
EP0641204A1 (de) 1995-03-08
EP0641204A4 (de) 1995-08-23
WO1993023040A1 (en) 1993-11-25
US5536727A (en) 1996-07-16
DE69329240D1 (de) 2000-09-21
AU4252193A (en) 1993-12-13
JPH07508038A (ja) 1995-09-07

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