发明名称 4-PYRIDINONETRIAZINE DERIVATIVES AS HIV INTEGRASE INHIBITORS
摘要 The present invention relates to 4-Pyridinonetriazine Derivatives of Formula (I); and pharmaceutically acceptable salts thereof, wherein A, X, Y, R1, R2, R3 and R5 are as defined herein. The present invention also relates to compositions comprising at least one 4-Pyridinonetriazine Derivative, and methods of using the 4-Pyridinonetriazine Derivatives for treating or preventing HIV infection in a subject.;
申请公布号 US2015329539(A1) 申请公布日期 2015.11.19
申请号 US201314652580 申请日期 2013.12.12
申请人 Merck Sharp & Dohme Corp. 发明人 Embrey Mark W.;Graham Thomas H.;Walji Abbas;Waddell Sherman T.;Yu Tao;Zhang Yonglian;Liu Wensheng;Coleman Paul J.;Wai John;Steele Thomas;Di Marco Christina
分类号 C07D471/04;C07D471/10;C07D471/20;A61K45/06;A61K31/675;C07D471/14;A61K31/55;A61K31/4985;A61K31/53;C07F9/6521 主分类号 C07D471/04
代理机构 代理人
主权项 1. A compound having the formula: or a pharmaceutically acceptable salt or prodrug thereof, wherein: A is —NHC(O)— or 5 or 6-membered monocyclic heteroaryl;X is C1-C3 alkylene;Y is O, —C(R8)2— or —N(R4)—;R1 is C1-C6 alkyl, C3-C7 cycloalkyl or —(C1-C4 alkylene)-O—(C1-C6 alkyl);R2 is selected from H, C1-C6 alkyl, C1-C6 hydroxyalkyl, —(C1-C6 alkylene)p-C(O)OR6, —(C1-C6 alkylene)p-C(O)R6, —(C1-C6 alkylene)p-C(O)N(R9)2, C3-C7 cycloalkyl, 5 or 6-membered monocyclic heterocycloalkyl, 5 or 6-membered monocyclic heteroaryl and —(C1-C4 alkylene)-O—(C1-C6 alkyl), wherein said C3-C7 cycloalkyl group, said 5 or 6-membered monocyclic heteroaryl group and said 5 or 6-membered monocyclic heterocycloalkyl group can be optionally substituted with R7;R3 is selected from H, C1-C6 alkyl, C3-C7 cycloalkyl, 5 or 6-membered monocyclic heterocycloalkyl and —(C1-C4 alkylene)-O—(C1-C6 alkyl), wherein said C3-C7 cycloalkyl group and said 5 or 6-membered monocyclic heterocycloalkyl group can be optionally substituted with one or more groups selected from R7, or R2 and R3, together with the common carbon atom to which they are both attached, can optionally join to form a spirocyclic C3-C7 cycloalkyl group or a a spirocyclic C3-C7 cycloalkenyl group, wherein said spirocyclic C3-C7 cycloalkyl group and said spirocyclic C3-C7 cycloalkenyl group can be optionally substituted with one or more groups selected from R7, and wherein said spirocyclic C3-C7 cycloalkyl group can be fused to another ring, selected from C3-C7 cycloalkyl, 3 to 8-membered monocyclic heterocycloalkyl and 5 or 6-membered monocyclic heteroaryl, and wherein said spirocyclic C3-C7 cycloalkyl group can form a spirocyclic ring system with a C3-C7 cycloalkyl group or a 3 to 8-membered monocyclic heterocycloalkyl group, or R1 and R3, together with the carbon atoms to which they are attached, can optionally join to form a 3 to 8-membered monocyclic heterocycloalkyl group, which can be optionally substituted with one or more groups selected from R7;R4 is selected from H, C1-C6 alkyl, —SO2R6, —C(O)R6, —(C1-C6 alkylene)p-C(O)N(R9)2, and —(C2-C4 alkylene)-O—(C1-C6 alkyl);R5 represents up to 3 optional substitutents, each independently selected from halo, C1-C6 alkyl, —O—(C1-C6 alkyl) and C1-C6 haloalkyl; andeach occurrence of R6 is independently selected from C1-C6 alkyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, phenyl, 3 to 8-membered monocyclic heterocycloalkyl or 6-membered monocyclic heteroaryl and 8 to 10-membered bicyclic heteroaryl, wherein said C3-C7 cycloalkyl group, said phenyl group, said 5 or 6-membered monocyclic heteroaryl group and said 8 to 10-membered bicyclic heteroaryl group can be optionally substituted with R7;each occurrence of R7 is independently selected from halo, C1-C6 alkyl, C1-C6 haloalkyl, 3 to 8-membered monocyclic heterocycloalkyl, 6 to 10-membered bicyclic heterocycloalkyl, —O—(C1-C6 alkyl), —O—(C6-C10 aryl), —O—(C1-C6 alkylene)-O—(C1-C6 alkyl), —O—(C1-C6 haloalkyl), —O—(C1-C6 alkylene)-O—(C1-C6 alkylene)-O—(C1-C6 alkyl), —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)2, —S(O)2—(C1-C6 alkyl), —NHS(O)2—(C1-C6 alkyl), —OC(O)—(C1-C6 haloalkyl), —(C1-C6 alkylene)p-C(O)OR6, —(C1-C6 alkylene)p-C(O)R6, —(C1-C6 alkylene)p-C(O)N(R9)2, C1-C6 hydroxyalkyl, —P(O)(OR11)2, and —CN;each occurrence of R8 is independently selected from H, C1-C6 alkyl, C3-C7 cycloalkyl, 3 to 8-membered monocyclic heterocycloalkyl and 5 or 6-membered monocyclic heteroaryl;each occurrence of R9 is independently selected from H, C1-C6 alkyl, C3-C7 cycloalkyl, —(C1-C6 alkylene)-N(R9)2, C1-C6 haloalkyl, —C(O)O(C1-C6 alkyl), —(C1-C6 alkylene)p-R10 and —(C1-C6 alkylene)-O—(C1-C6 alkyl);each occurrence of R10 is independently selected from H, C1-C6 alkyl, C3-C7 cycloalkyl, 5 or 6-membered monocyclic heteroaryl and 3 to 8-membered monocyclic heterocycloalkyl;each occurrence of R1 is independently selected from H and C1-C6 alkyl; andeach occurrence of p is independently 0 or 1.
地址 Rahway NJ US