JENNIFER R. ALLEN,FANG HONG,PATRICIA TSAO - LOPEZ,PHILIP R. OLIVIERI,ZIHAO HUA,OLEG EPSTEIN,RYAN WHITE,JASON BROOKS HUMAN,KARINA ROMERO,LAURIE SCHENKEL,JOHN STELLWAGEN,NURIA A. TAMAYO,XIAO MEI ZHENG
申请号:
ARP140100307
公开号:
AR095093A1
申请日:
2014.01.29
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
1. Requirement 1: a compound (1) with formula characteristics,O O O 1 stereoisomer, tauqianros, hydrate, solution or drug acceptable salt, wherein a83099 is cr83090 or N; a8310 is cr8310 or N; a83212 is cr831222 or N, but not more than one of a83099;A8310 and a831222 n; each R1,independently, it is H, F, Cl, C₁₋₆ alkyl,C₂₋₄ alkenyl,1. C 83228331 asphalt;CN, -CH₂O-C₁₋₆-alkyl,-O-alkyl C₁₋₆,-S (O) ₒ-C₁₋₆-alkyl,-NH-C₁₋₆-alkyl,-C (O) C₁₋₆ alkyl or C₃₋₆ cycloalkyl,where each of the C alqu alkyl portions,C₂₋₄ alkenyl,1. C 83228331 asphalt;C₃₋₆ cycloalkyl and C₁₋₆ alkyl of -CH₂O-C₁₋₆ alkyl,-O-alkyl C₁₋₆,-S (O) ₒ-C₁₋₆-alkyl,-NH-C₁₋₆-alkyl and -C (O) C₁₋₆-alkyl is optionally substituted with 1-4 substituents of F, oxo or OH; alternatively, each R¹ taken together with the carbon atom to which it is attached forms a spirocarbocyclic ring C₃₋₆ which optionally includes a hetero atom selected from O and N and which is optionally independently substituted with 1-4 substituents of F, OH, C₁₋₃ alkyl,C₁₋₃ alkoxy,a. C8322; o-lessor c83231;R2 is lease No. c83217c83318324,CH₂O-C₁₋₄ alkyl,CH₂OH, CH₂CN, C₃₋₆ cycloalkyl or CN, where each of C₁₋₄ alkyl,CH₂O-C₁₋₄-alkyl and C₃₋₆-cycloalkyl is optionally substituted with 1-4 F atoms; each R³,Independently, this is halo, lease No. c1832131, lease No. 832431,O-alkyl C alqu,CH₂O-C₁₋₄ alkyl,CH₂OH, haloalkyl C₁₋₄,cyclopropyl or CN, where each of C₁₋₄-O-alkyl,CH₂O-C₁₋₄-alkyl and cyclopropyl is optionally substituted with 1-4 F atoms; each of R⁵,R8310 and r831222,independently, it is H, halo, haloalkyl, haloalkoxy, C₁₋₄-alkyl,CN, OH, O-C₁₋₄-alkyl,S (O) -alquilo CNH-C₁₋₄-alkyl or C (O) C₁₋₄-alkyl;R⁷ is -NH-R⁹,-NHC (3DO) -R-C (3DO) NH-R-O-R⁹ or -S-R⁹;R⁹ is acetyl, C₁₋₆ alkyl,C₂₋₄ alkenyl,C₂₋₄-alkynyl or a 5-, 6- or 7-membered monocyclic or fully or partially unsaturated ring consisting of carbon atoms, where said ring optionally includes 1-4 heteroatoms if monocyclic or 1 - 5 heteroatoms if bicyclic, where said heteroatoms are selected from O, N or S,