发明名称 QUINAZOLINE COMPOUNDS
摘要 Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds.
申请公布号 US2016250215(A1) 申请公布日期 2016.09.01
申请号 US201514998042 申请日期 2015.12.23
申请人 Gilead Sciences, Inc. ;Institute of Organic Chemistry and Biochemistry of the AS CR, v.v.i. 发明人 BASZCZYNSKI Ondrej;DEJMEK Milan;HU Yunfeng Eric;JANSA Petr;LANSDON Eric;MACKMAN Richard L.;SIMON Petr
分类号 A61K31/517;C07D403/12;C07D239/95;C07D401/12;A61K45/06;C07D239/84 主分类号 A61K31/517
代理机构 代理人
主权项 1. A compound of formula (I): wherein Q is X1, X2, and X3 are each independently N or C(R11), provided that, at most 2 of X1, X2, and X3 are N; R1 is —H, —CN, —ORa, —C(O)ORa, halogen, C1-6alkyl, C3-10cycloalkyl, or C1-6heteroalkyl, wherein each C1-6alkyl, C3-10cycloalkyl, and C1-6heteroalkyl is optionally substituted with 1, 2, 3, 4, or 5 R12 groups, which may be same or different; R2 is —H, —CN, —ORa, —NRaRb, —C(O)ORa, halogen, C1-6alkyl, C3-10cycloalkyl, or C1-6 heteroalkyl, wherein each C1-6alkyl, C3-10cycloalkyl, and C1-6heteroalkyl is optionally substituted with 1, 2, 3, 4, or 5 R12 groups, which may be same or different; R3 is —H, —ORa, —SRa, —NRaRb, —NHC(O)NRaRb, C1-6alkyl, C3-10cycloalkyl, or C1-6 heteroalkyl, wherein each C1-6alkyl, C3-10cycloalkyl, and C1-6heteroalkyl is optionally substituted with 1, 2, 3, 4, or 5 R12 groups, which may be same or different; R4 is —H, —ORa, halogen, —NO2, —CN, —NRaRb, —NHC(O)NRaRb, —OC(O)NRaRb, —CH2C(O)NRaRb, C1-6alkyl, C3-10cycloalkyl, or C1-6 heteroalkyl, wherein each C1-6alkyl, C3-10cycloalkyl, and C1-6heteroalkyl is optionally substituted with 1, 2, 3, 4, or 5 R12 groups, which may be same or different; R5 is —H, —ORa, halogen, —NO2, —CN, —NRaRb, —NHC(O)NRaRb, —OC(O)NRaRb, —CH2C(O)NRaRb, C1-6alkyl, C3-10cycloalkyl, or C1-6heteroalkyl, wherein each C1-6alkyl, C3-10cycloalkyl, and C1-6heteroalkyl is optionally substituted with 1, 2, 3, 4, or 5 R12 groups, which may be same or different; R6 is —H, —ORa, halogen, —NO2, —CN, —NRaRb, —NHC(O)NRaRb, —OC(O)NRaRb, —CH2C(O)NRaRb, C1-6alkyl, C3-10cycloalkyl, or C1-6heteroalkyl, wherein each C1-6alkyl, C3-10cycloalkyl, and C1-6heteroalkyl is optionally substituted with 1, 2, 3, 4, or 5 R12 groups, which may be same or different; R7 is C1-6alkyl, C3-10cycloalkyl, C1-6heteroalkyl, halogen, —ORa, —CN, or —NO2, wherein each C1-6alkyl, C3-10cycloalkyl, and C1-6heteroalkyl is optionally substituted with 1, 2, 3, 4, or 5 R12 groups, which may be same or different; R8 is C1-6alkyl, C3-10cycloalkyl, C1-6heteroalkyl, halogen, —ORa, —CN, or —NO2, wherein each C1-6alkyl, C3-10cycloalkyl, and C1-6heteroalkyl is optionally substituted with 1, 2, 3, 4, or 5 R12 groups, which may be same or different; R9 is —H, C1-6alkyl, or C3-10cycloalkyl, wherein each C1-6alkyl and C3-10cycloalkyl is optionally substituted with 1, 2, 3, 4, or 5 R12 groups, which may be same or different; R10 is —H, C1-6alkyl, or C3-10cycloalkyl, wherein each C1-6alkyl and C3-10cycloalkyl is optionally substituted with 1, 2, 3, 4, or 5 R12 groups, which may be same or different; each R11 is independently —H, —CN, —ORa, —C(O)ORa, halogen, C1-6alkyl, C3-10cycloalkyl, or C1-6heteroalkyl, which may be same or different, wherein each C1-6alkyl, C3-10cycloalkyl, and C1-6heteroalkyl is optionally substituted with 1, 2, 3, 4, or 5 R12 groups, which may be same or different; each R12 is independently C1-6alkyl, C3-10cycloalkyl, C1-6heteroalkyl, 5-10 membered heterocyclyl, C6-10aryl, 5-10 membered heteroaryl, halogen, —ORa, —C(O)Ra, —C(O)ORa, —C(O)NRaRb, —OC(O)NRaRb, —NRaC(O)ORb, —SRa, —S(O)1-2Ra, —S(O)2F, —S(O)2NRaRb, —NRaS(O)2Rb, —N3, —CN, or —NO2; wherein each C1-6alkyl, C3-10cycloalkyl, C1-6heteroalkyl, and 5-10 membered heterocyclyl is optionally substituted with 1, 2, 3, 4, or 5 substituents selected from halogen, —ORa, —C(O)Ra, —C(O)ORa, —C(O)NRaRb, —OC(O)NRaRb, —NRaC(O)ORb, —SRa, —S(O)1-2Ra, —S(O)2F, —S(O)2NRaRb, —NRaS(O)2Rb, —N3, —CN, and —NO2, groups, which may be same or different; each Ra and Rb is independently —H, —NH2, C1-6alkyl, C3-10cycloalkyl, C1-6heteroalkyl, 5-10 membered heterocyclyl, C6-10aryl, or 5-10 membered heteroaryl, wherein each C1-6alkyl, C3-10cycloalkyl, C1-6heteroalkyl, 5-10 membered heterocyclyl, C6-10aryl, and 5-10 membered heteroaryl is optionally substituted with 1, 2, 3, 4, or 5 R13 groups, which may be same or different; or Ra and Rb together with the atoms to which they are attached form a 5-10 membered heterocycle; and each R13 is independently —CN, halogen, C1-6alkyl, C3-10cycloalkyl, C1-6heteroalkyl, or 5-10 membered heterocyclyl, or a tautomer or a pharmaceutically acceptable salt thereof.
地址 Foster City CA US