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Compounds and compositions as inhibitors of the Protein Kinase C - Kit
专利权人:
IRM LLC
发明人:
JON CHRISTOPHER LOREN,VINCE YEH,XIAOLIN LI,XIAODONG LIU,VALENTINA MOLTENI,JULIET NABAKKA,BAO NGUYEN,HANK MICHAEL JAMES PETRASSI
申请号:
ARP120103222
公开号:
AR087752A1
申请日:
2012.08.31
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
Drug compounds and compounds that can be used as 500 protein inhibitors, and methods of using these compounds and of treating, alleviating or preventing conditions related to abnormal activity or deregulation of 500 enzymes are provided, 1. Abnormal activation of c-kit or c-kit and PDGFR (PDGFRA, PDGFRb) is involved. Claim 1: consists of formula (1) or formula (2),e. Or select acceptable salt of 1 and 83044 from h, halo and c83218331 asphalt;haloalkyl C₁₋₆,haloalkoxy C₁₋₆,deuterio alquilo C deuterado -CN - (CR) OR-C (O) R- (CR) C (3DO) ORR830404,- (CR) R- ((CR) O) R- (CR) O (CR) R- (CR) C (3DO) R-C (3DO) N (R)-OR⁴ and - (CR⁹₂) ₙCN; or m is 4 and R²⁰ is deuterium; R¹ is selected from C₁₋₆ alkyl and halo; each R¹¹ is independently selected from H, halo, and C₁₋₆ alkyl;L1 is a link, nh-o-c (= O) NH -;L es - (CR) --CHR⁶-,-(cr8313; 8322) - i.e. 8345;- en...- (CR) C (3DO) --C (= O) or (CR) 8313; - 832245; -,- (CR) OC (3DO) NR --(cr.8313;) - No. 834508; (= O) (cr.83313;) No. 8322245; -,- (CR⁹₂) ₙNR⁴C (= O) - or - (CR⁹₂) ₙNR⁴C (= O) O-;R2 is R3 or L3 cubic meters;R³ is selected from an unsubstituted C₃₋₈ cycloalkyl, a cyclobutanone, a cyclopentanone, and a C₃₋₈ substituted cycloalkyl, wherein the C² substituted cycloalkyl of R² is substituted by 1-4 substituents independently selected from alkyl C₁₋₆,halo, haloalkyl C₁₋₆,-Or83088,-CN -C (3DO) OR-C (3DO) R-C (3DO) R-C (3DO) OR- (CR) OR-O (CR) OR-C (3DO) O (CR) OR-N (R)= N-OR⁴,3DN-O- (CR) R-C (3DO) NR-8308; C (= O) or8308;-8308jc (= O) (cr8313); 832222). - 834508 or83088;-83088 (cr8313); 8322088;- 8308th;]-N (C (3DO) OR)=CH8322,3DCH (CR) ORR8322,- (CR) Ralcoxilo C deuterado -S (3DO) R-S (3DO) R-S (3DO) R-S (3DO) N (R)-S (3DO) NHC (3DO) OR-S (3DO) (CR) C (3DO) OR-S (3DO) (CR) ORa bonded spiro dioxolane, a bonded spiro dioxolane which is substituted by C₁₋₆-alkyl,1. Poly (diazo), syngas tetrahydrofuran, oxyethane, syngas cyclopentanone, syngas cyclopentadien, syngas Cyclopentanol, Jinqiao c8321;a 5-6 membered unsubstituted hete
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