发明名称 CENICRIVIROC FOR THE TREATMENT OF HIV-2 INFECTION
摘要 Cenicriviroc (CVC) is an orally active antagonist of ligand binding to C—C chemokine receptor type 5 (CCR5) and C—C chemokine receptor type 2 (CCR2). CVC blocks the binding of RANTES, MIP-1α, and MIP-1β to CCR5, and of MCP-1/CCL2 to CCR2. Methods of treating HIV-2 infection and related conditions comprising administration of CVC are provided herein.
申请公布号 US2017105969(A1) 申请公布日期 2017.04.20
申请号 US201515315477 申请日期 2015.06.02
申请人 Tobira Therapeutics, Inc. 发明人 LEFEBVRE Eric
分类号 A61K31/4178 主分类号 A61K31/4178
代理机构 代理人
主权项 1. A method of treating HIV-2 infectious disease in a patient in need of such treatment, comprising administering to the patient a therapeutically effective amount of a compound of formula (I):wherein R1 is a cyclic 5- to 6-membered ring which may be substituted; X1 is a bond; rings A and B, together with the variables a, b, E1, E2, E3, and E4, form a benzoazocine ring system; X2 is a bivalent chain group whose straight chain moiety is constituted of 1 to 4 atoms; Z1 is a bond or a bivalent cyclic group; Z2 is a bond or a bivalent group; and R2 is (1) an amino group which may be substituted and whose nitrogen atoms may be converted to quaternary ammonium or oxide,(2) a nitrogen-containing heterocyclic group which may be substituted, may contain a sulfur or oxygen atom as a ring constituent atom, and whose nitrogen atom may be converted to quaternary ammonium or oxide,(3) a group of the formula: wherein k is 0 or 1; when k is 0, the phosphorus atom may form a phosphonium salt; each of R5 and R6 is a hydrocarbon group which may be substituted, a hydroxy group or an amino group which may be substituted; and R5 and R6 may form a ring with the adjacent phosphorus atom,(4) an amidino group which may be substituted, or(5) a guanidino group which may be substituted;or a salt thereof, to a mammal in need thereof.
地址 South San Francisco CA US