CYCLOPAMINE ANALOGUES AND METHODS OF THEIR APPLICATION Russian patent published in 2010 - IPC C07D491/48 A61K31/4355 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to novel compounds of formula 1: or its pharmaceutically acceptable salt; in which each R¹ and R⁸ independently represents H or hydroxyl; each R² and R⁹ independently represents H or hydroxyl; R⁵ represents H; each R³, R⁴, R⁶, R⁷, R¹³ and R¹⁴ independently represents H; or R¹ and R², taken together, form =O; or R⁴ and R⁵, taken together form double bond; or R⁵ and R⁶, taken together form double bond; R¹⁰ and R¹¹, taken together form double bond; R¹² represents H, alkyl, hydroxyl, aralkyl, halogenalkyl, alcoxyl,- -[(W)- N(R²¹)C(O)]_qR²¹, -[(W)-N(R²¹)SO₂]_qR²¹, -[(W)-O]_qR²¹ or -[(W)-N(R²¹)]_qR²¹; where each W independently represent bivalent alkyl or aralkyl radical, and q is equal 1, 2, 3 or 4; each R¹⁵, R¹⁶ and R¹⁷ independently represent H; each R¹⁸ and R¹⁹ independently represents H; and each R²¹ independently represents H, alkyl, aryl or aralkyl. Invention also relates to pharmaceutical composition. Claimed invention provides cycloamine analogues which can be applied to counteract phenotypic effects of undesirable activation of Hedgehog pathway, such as acquiring function from Hedgehog, Ptc loss of function or mitigated acquired from function mutations.

EFFECT: compounds by claimed invention are especially applicable in cancer treatment.

19 cl, 1 tbl, 28 ex