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Isoindolinona derivatives as inhibitors of Akt and pirrolopiridinona
专利权人:
INCYTE CORPORATION
发明人:
申请号:
ARP120103803
公开号:
AR088320A1
申请日:
2012.10.12
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
This product provides synephrine and pyrethroid derivatives, as well as their ingredients and methods of use, which hinder the activities of SERINA / trenina quinasa (Akt) and help to treat diseases related to Akt activities, including cancer and other diseases. 1. Characteristic 1: a formula compound (1) or acceptable salt for pharmaceutical use, wherein X is n or cr83088;This is n / cr830909;Z is n or cr8310a,with the proviso that at least one of X, Y, and Z comprises a carbon atom; A is aryl C₆₋₁₀,5-10 membered heteroaryl, or C₃₋₇ cycloalkyl,In this regard, it should be noted that:5-10 membered heteroaryl, and C₃₋₇ cycloalkyl are each optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from Q; R¹ is H, F, Cl, Br, CN, C₁₋₆ alkyl,C₂₋₆ alkenyl,1. C 83228331 asphalt;haloalkyl C₁₋₆,cycloalkyl C₃₋₆,aryl C₆₋₁₀,4-6 membered heterocycloalkyl, or 5-10 membered heteroaryl, wherein said C₁₋₆ alkyl,C₂₋₆ alkenyl,1. C 83228331 asphalt;cycloalkyl C₃₋₆,aryl C₆₋₁₀,4-6 membered heterocycloalkyl, and 5-10 membered heteroaryl are each optionally substituted by 1, 2, or 3 substituents independently selected from Cy, halo, C₁₋₆-alkyl,C₂₋₆ alkenyl,1. C 83228331 asphalt;haloalkyl C₁₋₆,CN, ORᵃ,SR7491,C (O) RC (o) No. 7580; r74966;C (O) OROC (O) ROC (O) NR RNo. 7580; No. 74966;No. 7580; C (o) r7495;NR C (O) NR RNo. 7580; C (o) or74919;C (= No. 750101) No. 7580; r74966;NR C (3DNR) NR RS (O) RS (o) No. 7580; r74966;S (O) RNR S (O) RS (o) 8322; 7580; r74966;1. No more than one of the two or three alternatives is cy, two is h, and c832131 is leased;cycloalkyl C₃₋₆,O 4 to 6 members of the groupor R² and R³ together with the nitrogen atom to which they are both attached form a 4- to 6-membered heterocycloalkyl group optionally substituted by 1 or 2 substituents independently selected from RA; R⁴ is H, F, Cl, CN, or C₁₋₃ alkyl;R8309es h, F, Cl, CN, or c832131;R8310es h, F, Cl, CN, or c83231;R⁷ is C₁₋₃ alkyl;Q is a cy1 independent candidate,-L-Cy1,Halo, rented c83217c83
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