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Details for Patent: 4,519,946

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Details for Patent: 4,519,946

Title: Steroids
Abstract:Novel 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR1## wherein R.sub.1 is an organic radical of 1 to 18 carbons atoms containing at least one atom selected from the group consisting of nitrogen, phosphorous and silicon with the atom immediately adjacent to the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is selected from the group consisting of a pentagonal ring and a hexagonal ring optionally substituted and optionally containing a double bond, B and C together form a double bond or an epoxy group, the C=A group at position 3 is selected from the group consisting of C-O, ketal, which may be open or closed ##STR2## --C.dbd.NOH,--C--NOAlK.sub.3 and C--CH.sub.2,AlK.sub.1, AlK.sub.2 and AlK.sub.3 are selected from the group consisting of alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 15 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anti-glucocoritcoid activity and a process for their preparation.
Inventor(s): Teutsch; Jean G. (Pantin, FR), Costerousse; Germain (Saint-Maurice, FR), Philibert; Daniel (La Varenne Saint Hilaire, FR), Deraedt; Roger (Pavillons sous Bois, FR)
Assignee: Roussel Uclaf (Paris, FR)
Filing Date:May 25, 1984
Application Number:06/614,440
Claims:1. A compound selected from the group consisting of 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR101## wherein R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is selected from the group consisting of pentagonal ring and a hexagonal ring optionally substituted and optionally containing a double bond, and K is a ketone blocked in the form of a ketal, thioketal, oxime or methyloxime.

2. A compound of claim 1 wherein X is pentagonal ring.

3. A compound of claim 1 which is 3,3-(1,2-ethanediyl-bisoxy)-5.alpha.,10.alpha.-epoxy-17.alpha.-(prop-1-yny l)-.DELTA..sup.9(11) -estrene-17.beta.-ol.

4. A compound of claim 1 which is 3,3-dimethoxy-5.alpha.,10.alpha.-epoxy-17.beta.-ethynyl-.DELTA..sup.9(11) -estrene-17.beta.-ol.

5. A compound of claim 1 wherein X and the carbons to which it is attached form the ring of the formula ##STR102## wherein R.sub.2 has the above definition, the dotted line in the 16,17-position is an optional double bond, Y is ##STR103## n is 1 or 2, R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, aryl of 6 to 14 carbon atoms and aralkyl of 7 to 15 carbon atoms, R.sub.6 may be the same as R.sub.5 and may be selected from the same group of members as R.sub.5 -- or --OH, R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen, --OH, --OAlK.sub.4, --OCOAlK.sub.5, alkenyl and alkynyl of 2 to 8 carbon atoms, ##STR104## and --CN wherein AlK.sub.4, AlK.sub.5 and AlK.sub.8 are selected from the group consisting of alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 15 carbon atoms, AlK.sub.6 is selected from the group consisting of optionally substituted alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 15 carbon atoms and AlK.sub.7 is alkyl of 1 to 8 carbon atoms and R.sub.3 and R.sub.4 form the group ##STR105## and Z.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and acyl of an organic carboxylic acid of 1 to 8 carbon atoms and Z.sub.2 is alkyl of 1 to 8 carbon atoms.

6. A compound of claim 5 wherein the D ring is saturated, R.sub.5 and R.sub.6 are hydrogen and n is 1.

7. A compound of claim 6 wherein R.sub.3 is an OH group and R.sub.4 is an alkynyl of 2 to 8 carbon atoms.
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