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    Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids
    4.
    发明授权
    Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids 失效

    公开(公告)号：US5064822A

    公开(公告)日：1991-11-12

    申请号：US438359

    申请日：1989-11-16

    申请人： Daniel Philibert ,  Jean G. Teutsch ,  Germain Costerousse ,  Roger Deraedt

    发明人： Daniel Philibert ,  Jean G. Teutsch ,  Germain Costerousse ,  Roger Deraedt

    IPC分类号： C07J1/00 ,  C07J7/00 ,  C07J17/00 ,  C07J21/00 ,  C07J31/00 ,  C07J33/00 ,  C07J41/00 ,  C07J51/00 ,  C07J71/00

    CPC分类号： C07J7/003 ,  C07J1/0096 ,  C07J17/00 ,  C07J21/006 ,  C07J31/006 ,  C07J33/002 ,  C07J41/0016 ,  C07J41/0077 ,  C07J41/0083 ,  C07J41/0094 ,  C07J51/00 ,  C07J7/0045 ,  C07J7/0075 ,  C07J71/001

    摘要： Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of naphthyl, phenylphenyl, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms optionally containing additional unsaturations, phenoxy, furyl, cycloalkyl of 3 to 6 carbon atoms, thienyl optionally substituted with at least one member of the group consisting of halogen and alkyl and haloalkyl of 1 to 6 carbon atoms and phenyl optionally substituted with at least one member of the group consisting of --OH, halogen, --CF.sub.3, alkyl and alkoxy of 1 to 6 carbon atoms, alkenyloxy of 2 to 6 carbon atoms, phenoxy and alkylthio of 1 to 6 carbon atoms optionally oxidized to the sulfoxide or sulfone, R.sub.2 is selected from the group consisting of methyl and ethyl, R.sub.3 is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 6 carbon atoms, --OH, acetyl, hydroxyacetyl, carboxyalkoxy of 2 to 4 carbon atoms optionally esterified or salified and hydroxyalkyl of 1 to 6 carbon atoms optionally esterified, R.sub.4 is selected from the group consisting of hydrogen, alkylthio and alkoxy of 1 to 12 carbon atoms, trialkylsilyl of 1 to 6 carbon atoms, --CN, --OH and alkyl, alkenyl and alkynyl of up to 12 carbon atoms optionally substituted with at least one member of the group consisting of halogen and alkylamino and dialkylamino of 1 to 6 alkyl carbon atoms, R.sub.5 is selected from the group consisting of hydrogen and methyl in the .alpha.- or .beta.-position, X is .dbd.0 or hydroxyimino or alkoxyimino of 1 to 4 carbon atoms in the syn or anti form and A and B are an epoxy or a second bond in the 9(10) position and their non-toxic, pharmaceutically acceptable acid addition salts where R.sub.4 is an amino group, with the proviso that A and B are not a second bond in the 9(10)-position when X is .dbd.0 and R.sub.5 is hydrogen and a) R.sub.2 is methyl and .alpha.) R.sub.3 is --OH and i) R.sub.1 is ethyl or phenyl and R.sub.4 is hydrogen or ii) R.sub.1 is ethyl, propyl, isopropyl, vinyl, allyl, isopropenyl, phenyl, 4-fluorophenyl, methoxyphenyl or thienyl and R.sub.4 is ethynyl or iii) R.sub.1 is propyl, isopropyl, vinyl, allyl, isopropenyl, 4-methoxyphenyl or thienyl and R.sub.4 is methyl and .beta.) R.sub.3 is acetyl and i) R.sub.1 is ethyl, vinyl or phenyl and R.sub.4 is --OH or ii) R.sub.1 is vinyl and R.sub.4 is methyl and b) R.sub.2 is ethyl and R.sub.1 is vinyl, R.sub.3 is --OH and R.sub.4 is hydrogen possessing a remarkable antiglucocorticoidal activity.

    15alpha,16alpha-methylene steroids and processes for their production and use
    7.
    发明授权
    15alpha,16alpha-methylene steroids and processes for their production and use 失效

    公开(公告)号：US3749742A

    公开(公告)日：1973-07-31

    申请号：US3749742D

    申请日：1972-02-24

    申请人： SCHERING AG

    发明人： WIECHERT R ,  STEINBECK H

    IPC分类号： C07J7/00 ,  C07J53/00 ,  D06F75/14 ,  C07C169/22

    CPC分类号： C07J7/0075 ,  C07J53/008

    摘要： WHEREIN R1 IS A HYDROGEN ATOMS OR SATURATED OR UNSATURATED ALKYL OF 1-4 CARBON ATOMS, AND PHYSIOLOGICALLY ACCEPTABLE 17-ESTERS THEREOF POSSESS HIGH ANDROGENIC ACTIVITY WITH RELATIVELY LOW ANABOLIC ACTIVITY. THEY CAN BE PRODUCED BY OXIDATION OF THE CORRESPONDING $4 AND $5-3-HYDROXYSTEROIDS AND BY ALKYLATION OF THE CORRESPONDING $5-3-ACYLOXY-17-KETO STEROIDS FOLLOWED BY HYDROLYSIS OF THE 3-ACYLOXY GROUP AND OXIDATION OF THE THUS-PRODUCED 3-HYDROXY GROUP.

    3-(O=),15,16-(-CH2-),17-R1,17-HO-ANDROST-4-ENE

    15A,16A-METHYLENE STEROIDS OF THE FORMULA