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US 5,001,119 AGranted
16-substituted androstanes and 16-substituted androstenes
OwnerArthur G. Schwartz, Marvin L. Lewbartinventors
Life of this patent
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Abstract
Compounds of the formula: ##STR1## are useful as anti-cancer, anti-obesity, anti-diabetic, anti-coronary agents, anti-aging agents, anti-hypolipidemic agents and anti-autoimmune agents.
Claims100
A compound of the formula:
- ##STR67## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.7, R.sub.8, R.sub.11, R.sub.12, R.sub.13, R.sub.14, and R.sub.15 independently hydrogen, lower alkyl, halogen, hydroxy, or lower alkoxy;
- R.sub.5 and R.sub.6 are independently hydrogen, lower alkyl, halogen, or lower alkoxy;
- R.sub.9 is hydrogen, lower alkyl or halogen and
- R.sub.16 and R.sub.17 are independently hydrogen, amino, loweralkylamino, diloweralkylamino, aminoloweralkyl, loweralkylamino loweralkyl, diloweralkylaminolower alkyl, loweralkoxyloweralkyl, lower alkoxy, hydroxy lower alkyl, monohaloloweralkyl, dihaloloweralkyl, trihaloloweralkyl, loweralkanoyl, formyl, lower carbalkoxy, or lower alkonoyloxy or R.sub.16 and R.sub.17 taken together with the carbons to which they are attached form a lower cycloalkyl or a cyclic ether containing 1 ring oxygen atom and up to 5 ring carbon atoms. with the proviso that R.sub.16 and R.sub.17 are not hydrogen simultaneously.
1 more element
A compound of the formula:
- ##STR68## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.11, R.sub.12, R.sub.13, R.sub.14 and R.sub.15 are independently hydrogen, lower alkyl, halogen, hydroxy or lower alkoxy;
- R.sub.9 and R.sub.10 are independently lower alkyl, hydrogen or halogen;
- and
- R.sub.16 and R.sub.17 are independently hydrogen, amino, lower alkylamino, diloweralkyl amino, aminoloweralkyl, loweralkyl, aminoloweralkyl, diloweralkylamino loweralkyl, lower alkoxy, hydroxyloweralkyl, monohaloloweralkyl, dihaloloweralkyl, trihaloloweralkyl, loweralkoxy-loweralkyl, loweralkanoyl, formyl, or lower carbalkoxy;
- or
- R.sub.16 and R.sub.17 taken together with the carbon to which they are attached form a lower cycloalkyl or a cyclic ether containing 1 ring oxygen atom and up to 5 ring carbon atoms with the proviso that R.sub.16 and R.sub.17 are not hydrogen simultaneously and with the further proviso that when R.sub.1 -R.sub.15 and R.sub.17 are hydrogen, then R.sub.16 is not ethoxy.
3 more elements
A compound of the formula:
- ##STR69## wherein R.sub.5 and R.sub.6 are independently lower alkyl or hydrogen;
- and
- R.sub.16 and R.sub.17 are independently hydrogen, amino, lower alkylamino, diloweralkyl amino, aminoloweralkyl, loweralkyl aminoloweralkyl, diloweralkylamino loweralkyl, lower alkoxy, hydroxyloweralkyl, monohaloloweralkyl, dihaloloweralkyl, trihaloloweralkyl, loweralkoxy-loweralkyl, loweralkanoyl, formyl, lower carbalkoxy or lower alkanoyloxy;
- or
- R.sub.16 and R.sub.17 taken together with the carbon to which they are attached form a lower cycloalkyl or a cyclic ether containing 1 ring oxygen atom and up to a total of 5 ring carbon atoms with the proviso that R.sub.16 and R.sub.17 are not hydrogen simultaneously.
2 more elements
A compound of the formula:
- ##STR70## wherein R.sub.5 and R.sub.6 are independently lower alkyl or hydrogen;
- and
- R.sub.16 and R.sub.17 are independently hydrogen, amino, lower alkylamino, diloweralkyl amino, aminoloweralkyl, loweralkyl, aminoloweralkyl, diloweralkylamino loweralkyl, lower alkoxy, hydroxyloweralkyl, monohaloloweralkyl, dihaloloweralkyl, trihaloloweralkyl, loweralkoxy-loweralkyl, loweralkanoyl, formyl, lower carbalkoxy;
- or
- R.sub.16 and R.sub.17 taken together with the carbon to which they are attached form a lower cycloalkyl or a cyclic ether containing 1 ring oxygen atom and up to 5 ring carbon atoms with the proviso that R.sub.16 and R.sub.17 are not hydrogen simultaneously and with the further proviso that when R.sub.1 -R.sub.15 and R.sub.17 are hydrogen, then R.sub.16 is not ethoxy.
2 more elements
A compound of the formula:
- ##STR71## wherein R.sub.5 is loweralkyl or hydrogen;
- and
- R.sub.16 and R.sub.17 are independently hydrogen, amino, lower alkylamino, diloweralkyl amino, aminoloweralkyl, loweralkyl, aminoloweralkyl, diloweralkylamino loweralkyl, lower alkoxy, hydroxyloweralkyl, monohaloloweralkyl, dihaloloweralkyl, trihaloloweralkyl, loweralkoxy-loweralkyl, loweralkanoyl, formyl, lower carbalkoxy or lower alkanoyloxy;
- or
- R.sub.16 and R.sub.17 taken together with the carbon to which they are attached form a lower cycloalkyl or a cyclic ether containing 1 ring oxygen atom and up to 5 ring carbon atoms with the proviso that R.sub.16 and R.sub.17 are not hydrogen simultaneously.
2 more elements
A compound of the formula:
- ##STR72## wherein R.sub.5 is loweralkyl or hydrogen;
- and
- R.sub.16 and R.sub.17 are independently hydrogen, amino, lower alkylamino, diloweralkyl amino, aminoloweralkyl, loweralkyl, aminoloweralkyl, diloweralkylamino loweralkyl, lower alkoxy, hydroxyloweralkyl, monohaloloweralkyl, dihaloloweralkyl, trihaloloweralkyl, loweralkoxy-loweralkyl, loweralkanoyl, formyl, or lower carbalkoxy;
- or
- R.sub.16 and R.sub.17 taken together with the carbon to which they are attached form a lower cycloalkyl or a cyclic ether containing 1 ring oxygen atom and up to 5 ring carbon atoms with the proviso that R.sub.16 and R.sub.17 are not hydrogen simultaneously, and with the further proviso that when R.sub.5 and R.sub.17 are hydrogen, then R.sub.16 is not ethoxy.
2 more elements
Dependencies are inferred from the claim text.