28-05-2015 дата публикации
Номер: US20150148321A1
Принадлежит:
The disclosure relates to novel C4 and C6 substituted androst-4-ene diones as well as andros-1,4-diene diones and derivatives thereof, their process of preparation, pharmaceutical compounds containing them, and the use of said compounds for the treatment of hormone-related disorders in mammals. This includes hormone-dependent cancers, particularly those caused by elevated levels of estrogen and its intermediates. These compounds can also be used in the treatment of other hormone-related disorders, including benign prostatic hyperplasia, cardiovascular disease, and neurodegenerative disorders. 2. The method of claim 1 , wherein the substituent is selected from OH claim 1 , phenyl claim 1 , benzyl claim 1 , naphthyl claim 1 , substituted aryl claim 1 , or Cto Calkyl group.3. The method of claim 1 , wherein the substituent is selected from aryl claim 1 , substituted aryl claim 1 , heterocyclo claim 1 , substituted heterocyclo claim 1 , carbocyclo claim 1 , substituted carbocyclo claim 1 , or halo.4. The method of claim 1 , wherein the substituent is selected from alkoxy claim 1 , aryloxy claim 1 , alkylester claim 1 , arylester claim 1 , alkanoyl or aryoyl claim 1 , any of which may be optionally substituted.5. The method of claim 1 , wherein the compound is selected from the list:(6R,8R,9S,10R,13 S,14S)-10,13-dimethyl-6-((E)-pent-2-en-1-yloxy)-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione;(6R,8R,9S,10R,13 S,14S)-10,13-dimethyl-6-((Z)-pent-2-en-1-yloxy)-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione;(6R,8R,9S,10R,13 S,14S)-6-(cinnamyloxy)-10,13-dimethyl-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione;(6R,8R,9S,10R,13 S,14S)-10,13-dimethyl-6-(3-phenylpropoxy)-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione;(6R,8R,9S,10R,13 S,14S)-10,13-dimethyl-6-((5-phenylpentyl)oxy)-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17 ...
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