发明名称 Compounds and compositions as TLR2 agonists
摘要 The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.
申请公布号 US9365506(B2) 申请公布日期 2016.06.14
申请号 US201414326957 申请日期 2014.07.09
申请人 NOVARTIS AG 发明人 Wu Tom Yao-Hsiang;Zou Yefen;Hoffman Timothy Z.;Pan Jianfeng
分类号 C07C53/00;C07C57/00;C07C59/00;C08G63/48;A61K31/21;C07C323/60;C07F9/38;C07D213/56;C07K5/00 主分类号 C07C53/00
代理机构 The Genomics Institute of the Novartis Research Foundation 代理人 The Genomics Institute of the Novartis Research Foundation ;Raymond Daniel E.
主权项 1. A compound of Formula (I), or pharmaceutically acceptable salt thereof: wherein: R1 is H, —C(O)—C7-C18alkyl or —C(O)—C1-C6alkyl;R2 is C7-C18alkyl;R3 is C7-C18alkyl;L1 is —CH2OC(O)—;L2 is —OC(O)—;R4 is -L3R5 or -L4R5;R5 is —P(O)(OR7)2, —NR7C(O)L3R8, —NR7C(O)L4R8, —OL3R6, —C(O)NR7L3R8, —C(O)NR7L4R8, —S(O)2OR7, —OS(O)2OR7, C1-C6alkyl, a C6aryl, a C10aryl, a C14aryl, 5 to 14 ring membered heteroaryl containing 1 to 3 heteroatoms selected from O, S and N, C3-C8cycloalkyl or a 5 to 6 ring membered heterocycloalkyl containing 1 to 3 heteroatoms selected from O, S and N, wherein the aryl, heteroaryl, cycloalkyl and heterocycloalkyl of R5 are each unsubstituted or the aryl, heteroaryl, cycloalkyl and heterocycloalkyl of R5 are each substituted with 1 to 3 substituents independently selected from —OR9, —OL3R6, —OL4R6, —OR7, and —C(O)OR7;L3 is a C1-C10alkylene, wherein the C1-C10alkylene of L3 is substituted with 1 to 4 R6 groups, or the C1-C10alkylene of L3 is substituted with 2 C1-C6alkyl groups on the same carbon atom which together, along with the carbon atom they are attached to, form a C3-C8cycloakyl;L4 is —((CR7R7)pO)q(CR10R10)p— or —(CR11R11)((CR7R7)pO)q(CR10R10)p—, wherein each R11 is a C1-C6alkyl groups which together, along with the carbon atom they are attached to, form a C3-C8cycloakyl;each R6 is independently selected from halo, —OR7, —N(R7)2, —C(O)N(R7)2, —P(O)(OR7)2, a C6aryl, a C10aryl and a C14aryl;each R7 is independently selected from H and C1-C6alkyl;R8 is —SR7, —C(O)OH, —P(O)(OR7)2, or a 5 to 6 ring membered heterocycloalkyl containing 1 to 3 heteroatoms selected from O and N;R9 is phenyl;each R19 is independently selected from H and halo;each p is independently selected from 1, 2, 3, 4, 5 and 6, andq is 1, 2, 3 or 4.
地址 Basel CH