БЛАСКОВИЧ Марк Арнольд Томас (AU),КЭССИДИ Питер Джозеф (AU)
申请号：
RU2010137030/15
公开号：
RU2010137030A
申请日:
2009.02.27
申请国别(地区):
RU
年份:
2012
代理人:
摘要：
1. A method of down-regulating the activity of MC5R or its fragment, analog or functional equivalent, in which MC5R or its fragment or analog or functional equivalent is exposed to a compound of formula (I):! ! where Y represents a group of the formula - (CR9R10) n-； ! X is selected from the group consisting of —C (= O) -, —OC (= O) -, —NHC (= O) -, - (CR11R12) s, and —S (= O) 2-； ! R represents an amino acid side chain group； ! R1 is selected from the group consisting of H, optionally substituted C1-C12 alkyl, optionally substituted C2-C12 alkenyl, optionally substituted C2-C12 alkynyl, optionally substituted C1-C12 heteroalkyl, optionally substituted C3-C12 cycloalkyl, optionally substituted C2-C12 heterocyclo-cyclo-cyclo optionally substituted C1-C18 heteroaryl； ! R2 and R3 are each independently selected from the group consisting of H, optionally substituted C1-C12 alkyl, optionally substituted C2-C12 alkenyl, optionally substituted C2-C12 alkynyl, optionally substituted C1-C12 heteroalkyl, optionally substituted C3-C12 cycloalkyl, optionally substituted C2-C12 alkalo C6-C18 aryl and optionally substituted C1-C18 heteroaryl； ! each R5a and R5b is independently selected from the group consisting of H, halogen, C1-C12 alkyl, C1-C12 hydroxyalkyl and C1-C12 haloalkyl, or! one or more of R5a and R5b, taken together with one or more of R6, R7 and R8, and the atoms to which they are attached, form a part selected from the group consisting of optionally substituted C3-C12 cycloalkyl, optionally substituted C2-C12 heterocycloalkyl, optional substituted C6-C18 aryl and optionally substituted C1-C18 heteroaryl； ! R6, R7 and R8 are each independently selected from1. Способ понижающего регулирования активности MC5R или его фрагмента, аналога или функционального эквивалента, при котором MC5R или его фрагмент или аналог, или функциональный эквивалент подвергают воздействию соединения формулы (I): ! ! где Y представляет собой группу формулы -(CR9R10)n-； ! Х выбран из груп
