发明名称 CHEMOKINE RECEPTOR BINDING HETEROCYCLIC COMPOUNDS WITH ENHANCED EFFICACY
摘要 The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
申请公布号 US2016228413(A1) 申请公布日期 2016.08.11
申请号 US201615018698 申请日期 2016.02.08
申请人 Genzyme Corporation 发明人 BRIDGER Gary J.;SKERLJ Renato T.;KALLER Al;HARWIG Curtis;BOGUCKI David Earl;WILSON Trevor R.;CRAWFORD Jason B.;MCEACHERN Ernest J.;ATSMA Bem;NAN Siqiao;ZHOU Yuanxi;SCHOLS Dominique;SMITH Christopher Dennis;DIFLURI Maria Rosario
分类号 A61K31/4184;A61K31/4709;C07D401/12;C07D235/14;A61K31/5377;A61K31/506;C07D403/12;A61K31/4985;C07D491/052;A61K31/436;C07D471/04;C07D471/06;A61K31/497;A61K31/4725;A61K31/502;C07D401/14 主分类号 A61K31/4184
代理机构 代理人
主权项 1. A method to enhance the population of progenitor and/or stem cells in a subject, the method comprising: administering to said subject a compound of the formulaor the salts or pro-drug forms thereof; and including any stereoisomeric forms thereof wherein: X and Y are independently N or CR1; Z is S, O, NR1, or CR12; each R1-R6 is independently H or a noninterfering substituent; n1 is 0-4; n2 is 0-1, wherein the * signifies C≡C may be substituted for CR5═CR5; n3 is 0-4; wherein n1+n2+n3 is greater than or equal to 2; b is 0-2; wherein the following combinations of R groups may be coupled to generate a ring, which ring may be saturated or unsaturated: R2+R2, one R2+R3, R3+one R4, R4+R4, one R5+another R5, one R5+one R6, and R6+R6; wherein the ring may not be aromatic when the participants in ring formation are two R5; and wherein when n2 is 1, neither n1 nor n3 can be 0; in an amount effective to elevate said progenitor and/or stem cell population in said subject.
地址 Cambridge MA US