Specific AKT3 activator and uses thereofCompositions and methods of selectively activating Akt3 are provided.A compound according to formula i:or a pharmaceutically acceptable enantiomer, salt or solvate thereof, wherein:rings a, b and c are independently six-membered aryl or n-containing heteroaryl monocyclic or bicyclic ring systems containing zero or more n-atoms, such as phenyl, pyridine, pyrimidine, pyridazine, pyrazine, triazine, quinoline, quinazoline, isoquinoline, naphthalene, naphthyridine, indole, isoindole, cinnoline, phthalazine, quinoxaline, pteridine, purine, and benzimidazole.r1is selected from- (c)1-c30) alkyl, - (c)3-c12) -cycloalkyl, - (c)3-c12) -heterocycloalkyl, - (c)6-c20) -aryl or- (c)3-c20) -heteroaryl, optionally substituted with one or more substituents selected from: - (c)1-c12) alkyl, - (c)3-c12) -cycloalkyl, - (c)3-c12) -heterocycloalkyl, -o- (c)1-c12) -alkyl, -o- (c)1-c12) -alkyl- (c)6-c20) -aryl, -o- (c)3-c12) -cycloalkyl, -s- (c)1-c12) -alkyl, -s- (c)3-c12) -cycloalkyl, -coo- (c)1-c12) -alkyl, -coo- (c)3-c12) -cycloalkyl, -conh- (c)1-c12) -alkyl, -conh- (c)3-c12) -cycloalkyl, -co- (c)1-c12) -alkyl, -co- (c)3-c12) -cycloalkyl, -n- [ (c)1-c12) -alkyl radical]2、-(c6-c20) -aryl, - (c)6-c20) -aryl- (c)1-c12) alkyl, - (c)6-c20) -aryl-o- (c)1-c12) alkyl, - (c)3-c20) -heteroaryl, - (c)3-c20) -heteroaryl- (c)1-c12) alkyl, - (c)3-c20) -heteroaryl-o- (c)1-c12) -alkyl, -cooh, -oh, -sh, -so3h、-cn、-nh2or halogen;x, y and z are independently selected from the group consisting of ═ o, -nh, -s, -n- (c)1-c30) -alkyl or- (c)1-c30) -an aryl group;r2is selected from- (c)1-c30) -alkyl, ═ o, -oh, -so2-so or-soch3(ii) a and isr3is selected from- (c)1-c30) alkyl, - (c)3-c12) -cycloalkyl, - (c)3-c12) -heterocycloalkyl, - (c)6-c20) -aryl or- (c)3-c20) -heteroaryl, optionally substituted with one or more substituents selected from: - (c)1-c12) alkyl, - (c)3-c12) -cycloalkyl, - (c)3-c12) -heterocycloalkyl, -o- (c)1-c12) -alkyl, -o- (c)1-c12) -alkyl- (c)6-c20) -aryl, -o- (c)3-c12) -cycloalkyl, -s- (c)1-c12) -alkyl, -s- (c)3-c12) -cycloalkyl, -coo- (c)1-c12) -alkyl, -coo- (c)3-c12) -cycloalkyl, -conh- (c)1-c12) -alkyl, -conh- (c)3-c12) -cycloalkyl, -co- (c)1-c12) -alkyl, -co- (c)3-c12) -cycloalkyl, -n- [ (c)1-c12) -alkyl radical]2、-(c6-c20) -aryl, - (c)6-c20) -aryl- (c)1-c12) alkyl, - (c)6-c20) -aryl-o- (c)1-c12) alkyl, - (c)3-c20) -heteroaryl, - (c)3-c20) -heteroaryl- (c)1-c12) alkyl, - (c)3-c20) -heteroaryl-o- (c)1-c12) -alkyl, -cooh, -oh, -sh, -so3h、-cn、-nh2or a halogen.
특이적 AKT3 활성제 및 이의 용도Akt3을 선택적으로 활성화하는 조성물 및 방법이 제공된다. 하기 식 I에 따른 화합물: [이미지]또는 이들의 약제학적으로 허용가능한 거울상이성질체, 염, 또는 용매화물로서, 식 중:고리 A, B, 및 C 는 페닐, 피리딘, 피리미딘, 피리다진, 피라진, 트리아진, 퀴놀린, 퀴나졸린, 이소퀴놀린, 나프탈렌, 나프티리딘, 인돌, 이소인돌, 시놀린, 프탈라진, 퀴녹살린, 프테리딘, 퓨린, 및 벤즈이미다졸과 같이 독립적으로 0개 또는 그보다 많은 N-원자를 함유하는 6-원 아릴 또는 N-함유 헤테로아릴 단환 또는 이환형 고리계이고,R1 은 -(C1-C12)-알킬, -(C3-C12)-사이클로알킬, -(C3-C12)-헤테로사이클로알킬, -O-(C1-C12)-알킬, -O-(C1-C12)-알킬-(C6-C20)-아릴, -O-(C3-C12)-사이클로알킬, -S-(C1-C12)-알킬, -S-(C3-C12)-사이클로알킬, -COO-(C1-C12)-알킬, -COO-(C3-C12)-사이클로알킬, -CONH-(C1-C12)-알킬, -CONH-(C3-C12)-사이클로알킬, -CO-(C1-C12)-알킬, -CO-(C3-C12)-사이클로알킬, -N-[(C1-C12)-알킬]2, -(C6-C20)-아릴, -(C6-C20)-아릴-(C1-C12)-알킬, -(C6-C20)-아릴-O-(C1-C12)-알킬, -(C3-C20)-헤테로아릴, -(C3-C20)-헤테로아릴-(C1-C12)-알킬, -(C3-C20)-헤테로아릴-O-(C1-C12)-알킬, -COOH, -OH, -SH, -SO3H, -CN, -NH2, 또는 할로겐으로부터 선택된 하나 이상의 치환체에 의해 선택적으로 치환된 -(C1-C30)-알킬, -(C3-C12)-사이클로알킬, -(C3-C12)-헤테로사이클로알킬, -(C6-C20)-아릴, 또는 -(C3-C20)-헤테로아릴 기들로부터 선택되고;X, Y, 및 Z 는 독립적으로 =O, -NH, -S, -N-(C1-C30)-알킬, 또는 -(C1-C30)-아릴로부터 선택되고;R2 는 -(C1-C30)-알킬, =O, -OH, -SO2, -SO, 또는 -SOCH3 으로부터 선택되고; 그리고R3 은 -(C1-C12)-알킬, -(C3-C12)-사이클로알킬, -(C3-C12)-헤테로사이클로알킬, -O-(C1-C12)-알킬, -O-(C1-C12)-알킬-(C6-C20)-아릴, -O-(C3-C12)-사이클로알킬, -S-(C1-C12)-알킬, -S-(C3-C12)-사이클로알킬, -COO-(C1-C12)-알킬, -COO-(C3-C12)-사이클로알킬, -CONH-(C1-C12)-알킬, -CONH-(C3-C12)-사이클로알킬, -CO-(C1-C12)-알킬, -CO-(C3-C12)-사이클로알킬, -N-[(C1-C12)-알킬]2, -(C6-C20)-아릴, -(C6-C20)-아릴-(C1-C12)-알킬, -(C6-C20)-아릴-O-(C1-C12)-알킬, -(C3-C20)-헤테로아릴, -(C3-C20)-헤테로아릴-(C1-C12)-알킬, -(C3-C20)-헤테로아릴-O-(C1-C12)-알킬, -COOH, -OH, -SH, -SO3H, -CN, -NH2, 또는 할로겐으로부터 선택된 하나 이상의 치환체에 의해 선택적으로 치환된 -(C1-C30)-알킬, -(C3-C12)-사이클로알킬, -(C3-C12)-헤테로사이클로알킬, -(C6-C20)-아릴, 또는 -(C3-C20)-헤테로아릴 기들로부터 선택되는, 화합물.