发明名称 |
HIV inhibiting bicyclic pyrimidine derivatives |
摘要 |
HIV replication inhibitors of formula;
wherein
-a1=a2-a3=a4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b1=b2-b3=b4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—;n and m is 0-4,R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl;R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(═O)pR6; C(═NH)R6;R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH═N—NH—C(═O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X—R7;R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7; —X—R7;R4 is halo; OH; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7;-A-B— is —CR5═N—, —N═N—, —CH2—CH2—, —CS—NH—, —CO—NH—, —CH═CH—; and the use of these compounds for the prevention or the treatment of HIV infection. |
申请公布号 |
US9487518(B2) |
申请公布日期 |
2016.11.08 |
申请号 |
US201213410779 |
申请日期 |
2012.03.02 |
申请人 |
Janssen Sciences Ireland UC |
发明人 |
Guillemont Jerôme Emile Georges;Paugam Mikaël;Delest Bruno Francois Marie;Heeres Jan;Lewi Paulus Joannes;Janssen Paul Adriaan Jan |
分类号 |
C07D487/04;A61K31/519;C07D473/00;C07D473/34;A61P31/18;A61K31/52 |
主分类号 |
C07D487/04 |
代理机构 |
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代理人 |
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主权项 |
1. A compound of formulawherein R2a is cyano, R3 is ethenyl substituted with cyano, R4 is —CH3 or halo, and -A-B— is a radical —N═N— (c-2), N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof. |
地址 |
Little Island, Co Cork IE |