The Nitrogen Is Bonded Directly At The 3-position Patents (Class 552/520)
  • .DELTA..sup.4 -19-sulfur substituted-androstene derivatives having aromatase-inhibiting activity
    Patent number: 5030627
    Abstract: The invention relates to .DELTA..sup.4 -androstene derivatives with aromatase-inhibiting activity having the formula: ##STR1## wherein R.sub.1 =O, (.alpha.R.sub.5,.beta.H) or N--O--R.sub.6 ;R.sub.2 =H, (1-12C)hydrocarbon radical, --SH, --S--(1-12C)-hydrocarbon radical or (1-12C)acyl;R.sub.3 =O or (.alpha.R.sub.7,.beta.R.sub.8);R.sub.4 =H or (1-12C)hydrocarbon radical;R.sub.5 =OH, O--(1-12C)hydrocarbon radical or O--(1-12C)acyl;R.sub.6 =H or (1-12C)hydrocarbon radical;R.sub.7 =H or (1-12C)hydrocarbon radical; andR.sub.8 =OH, O--(1-12C)acyl or O--(1-12C)hydrocarbon radical with the proviso that R.sub.1 is not O if R.sub.4 is H.
    Type: Grant
    Filed: March 22, 1989
    Date of Patent: July 9, 1991
    Assignee: Akzo N.V.
    Inventors: Helenius J. Kloosterboer, Hubert J. J. Loozen
  • 11 .beta.-substituted progesterone analogs
    Patent number: 4954490
    Abstract: A 11.beta.-aryl-19-norprogesterone steroid of the formula: ##STR1## wherein (i) R.sup.1 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, OH, OC(O)CH.sub.3, or OC(O)R.sup.5, wherein R.sup.5 is C.sub.2-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl or aryl, R.sub.2 is H, R.sup.3 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl, R.sup.4 is H, CH.sub.3, F or Cl, R.sup.6 is H, (CH.sub.3).sub.2 N, CH.sub.3 O, CH.sub.3 CO, CH.sub.3 S, CH.sub.3 SO, CH.sub.3 SO.sub.2, and X is O or NOCH.sub.3 ; or(ii) R.sup.1 and R.sup.2 taken together are a carbon-carbon bond and R.sup.3, R.sup.4, R.sup.6 and X are as defined above; or(iii) R.sup.1 and R.sup.3 taken together are --CH.sub.2 -- or --N.dbd.N--CH.sub.2 --, R.sup.2 is H and R.sup.4, R.sup.6 and X are as defined above; or(iv) R.sup.2 and R.sup.3 taken together are .dbd.CH.sub.2 and R.sup.1, R.sup.4, R.sup.6 and X are as defined above.
    Type: Grant
    Filed: June 23, 1988
    Date of Patent: September 4, 1990
    Assignee: Research Triangle Institute
    Inventors: C. Edgar Cook, Mansukh C. Wani, Y.-W Lee, Jerry R. Reel, Douglas Rector