SMALL MOLECULE CD4 MIMETICS PREVENT HIV TRANSMISSION INTO HOST CELLS
HIV infections
The compounds of the present invention can be used in preventing diseases related to HIV infections, such as AIDS. These compounds can exist as therapeutically acceptable salts and the pharmaceutical preparations can be made for systemic and non-systemic administration.
The present invention provides the compounds that are capable of disrupting HIV entry into the host cells. HIV entry into target cells involves the viral envelope glycoproteins, gp 120 and gp41, and host cell receptors, CD4 and the chemokine receptors (either CCR5 or CXCR4). CD4 contacts the gpl20 and creates ΓÇ£the Phe 43 cavity". The present invention provides the compounds that target the Phe 43 cavity to disrupt the HIV entry into the host cells. The invention relates to compounds of certain formula with optional substitutions. Such compounds act as inhibitors of HIV transmission by intercepting binding of the natural ligand CD4 and by prematurely triggering the envelope glycoproteins to undergo irreversible conformational changes that result in loss of functional competence of the virus.
Inventor: SODROSKI, Joseph | MADANI, Navid | SCHON, Arne | LA LONDE, Judith, M. | COURTER, Joel, R. | SOETA, Takahiro | NG, Danny | FREIRE, Ernesto | SMITH, Amos, B.
Priority Number: WO2010053583A3
IPC Current: C07D021134 | A61K0031435 | A61P003118 | C07D020504 | C07D023514 | C07D031710 | C07D040102 | C07D040302 | C07D041302 | C07D048704
Assignee Applicant: Dana-Farber Cancer Institute Inc. | Johns Hopkins University | University of Pennsylvania
Title: SMALL MOLECULE CD4 MIMETICS AND USES THEREOF | MIMÉTIQUES CD4 À PETITE MOLÉCULE ET LEURS UTILISATIONS
Usefulness: SMALL MOLECULE CD4 MIMETICS AND USES THEREOF | MIMÉTIQUES CD4 À PETITE MOLÉCULE ET LEURS UTILISATIONS
Summary: For activating human immunodeficiency virus (HIV) exterior envelope glycoprotein gp120; for inhibiting the progression of HIV infection; and for inhibiting transmission or progression of HIV to a cell (claimed).
Novelty: New heterocyclic compounds useful for activating human immunodeficiency virus exterior envelope glycoprotein, and for inhibiting transmission or progression of human immunodeficiency virus to a cell
诊断/治疗
人类免疫缺陷病毒
美国
