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Imidazo [1,2a] pyrazines and compositions that include them for the treatment of parasitic diseases
专利权人:
Novartis AG
发明人:
Chatterjee, Arnab,Nagle, Advait S.,Wu, Tao,Tully, David C.,Kuhen, Kelli
申请号:
ES14156496
公开号:
ES2574529T3
申请日:
2010.07.09
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound of Formula Ia: ** Formula ** in which: n is selected from 0, 1, 2, 3 and 4; m>; = 0 Ra is selected from -X3NR7R8, -X3OR8, -X3S (O) 0-2R8, -X3C (O) NR7R8, and benzyl optionally substituted with 1 to 3 radicals independently selected from halo, C1-4 alkyl, alkyl C1-4 halosubstituted, C1-4 alkoxy and C1-4 alkoxy halosubstituted; wherein X3 is selected from a bond and C1-4 alkylene; R1 is selected from -OR13, -C (O) OR13, -NR13R14, C6-10 aryl and a saturated, unsaturated or partially unsaturated 4-9 membered heterocyclic ring containing a maximum of three nitrogen atoms; wherein R13 is selected from hydrogen, C1-6 alkyl, halo-substituted C1-6 alkyl, hydroxy-substituted C1-6 alkyl, C6-10 aryl-C0-4 alkyl, C3-8 cycloalkyl-C0-4 alkyl, -X1NHC (O) R15, -X1C (NH) NHR15, -XiC (O) NHR15, -X1NHR15, -X1OR15, -C (O) R15 and -C (O) OR15; wherein X1 is selected from a bond and C1-4 alkylene; R15 is selected from hydrogen, C1-6 alkyl, halo-substituted C1-6 alkyl and benzyl; R14 is selected from hydrogen, C1-6 alkyl and hydroxy-substituted C1-6 alkyl; or R13 and R14 together with the nitrogen atom to which R13 and R14 are attached form a saturated, unsaturated or partially unsaturated 5-9 membered heterocyclic ring containing a maximum of three heteroatoms selected from N, NR30, S (O) 0 -2 and O; wherein R30 is selected from hydrogen and C1-6 alkyl; wherein said heterocyclic forms the combination of R13 and R14 is optionally substituted with 1-3 radicals independently selected from halo, hydroxy, C1-6 alkyl, aminosubstituted C1-6 alkyl and halosubstituted C1-6 alkyl; any aryl or heterocyclic of R1 is optionally substituted with 1-3 radicals independently selected from halo, C1-6 alkyl, halo- substituted C1-6 alkyl, C1-6 alkoxy and halosubstituted C1-6 alkoxy; R2 is selected from hydrogen, C1-6 alkyl, amino, C3-8 cycloalkyl-C0-4 alkyl, C6-10 aryl-C0-4 alkyl, halosubstituted C1-6 alkyl, hydroxy substituted C1-6 alkyl and heterocyclyl alkyl C0-4; wherein said heterocyclyl is
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