公开(公告)号：US06653443B2

公开(公告)日：2003-11-25

申请号：US10118575

申请日：2002-04-08

Applicant: Hui Zhang ,  Roger J. Pomerantz ,  Bin Yang

Inventor： Hui Zhang ,  Roger J. Pomerantz ,  Bin Yang

IPC: A61K3804

CPC classification number: C07K14/005 ,  A61K38/00 ,  C12N2740/16322 ,  Y10S530/826

Abstract: One approach to treating individuals infected with HIV-1 is to administer to such individuals compounds that directly interfere with and intervene in the machinery by which HIV-1 replicates itself within human cells. Although the specific role of HIV-1 viral protein Vif in the viral life cycle is not known, the vif gene is essential for the pathogenic replication of lentiviruses in vivo. The present invention relates to a method for treating an individual exposed to or infected with HIV-1. Individuals identified as being exposed to or infected by HIV-1 are administered a therapeutically effective amount of one or more compounds that inhibit or prevent replication of said HIV-1 by interfering with the replicative or other essential functions of HIV-1 viral protein Vif, by interactively blocking the multimerization domain of Vif, thereby preventing multimerization of Vif protein, which is important for Vif function in the lentivirus life cycle. In preferred embodiments, the compound or compounds that interactively block the multimerization domain of Vif are Vif antagonists. Pharmaceutical compositions comprising these compounds are also disclosed.

Abstract translation: 治疗感染HIV-1的个体的一种方法是向这些个体施用直接干扰和干预HIV-1在人细胞内自身复制的机制的化合物。 虽然HIV-1病毒蛋白Vif在病毒生命周期中的具体作用尚不清楚，但vif基因对于体内慢病毒的致病性复制至关重要。 本发明涉及用于治疗暴露于或感染HIV-1的个体的方法。 鉴定为暴露于HIV-1或感染HIV-1的个体被施用治疗有效量的一种或多种化合物，其通过干扰HIV-1病毒蛋白Vif的复制或其它基本功能来抑制或阻止所述HIV-1的复制， 通过交互阻断Vif的多聚化结构域，从而防止Vif蛋白的多聚化，这对于慢病毒生命周期中的Vif功能是重要的。 在优选的实施方案中，交互式阻断Vif的多聚化结构域的化合物是Vif拮抗剂。 还公开了包含这些化合物的药物组合物。

公开(公告)号：US06406735B2

公开(公告)日：2002-06-18

申请号：US09255010

申请日：1999-02-22

Applicant: Hermann Stein ,  Klaus Viardot ,  Bin Yang

Inventor： Hermann Stein ,  Klaus Viardot ,  Bin Yang

IPC: A23L127

CPC classification number: C07C403/24 ,  A23L5/44

Abstract: A process for the preparation of a pulverous preparation having a finely divided carotenoid, retinoid or natural colorant is provided, which process comprises the steps of: a) forming a suspension of the active ingredient in a water-immiscible organic solvent optionally containing an antioxidant and/or an oil; b) feeding the suspension of step a) to a heat exchanger; c) heating the suspension to 100-250° C., whereby the residence time in the heat exchanger is less than 5 sec to provide a solution; d) rapidly mixing the solution of step c) with an aqueous solution of a swellable colloid and optionally a stabilizer such that the resulting mixture is at a temperature in the range of 20-100° C.; e) removing the organic solvent; and f) converting the dispersion of step e) into a pulverous preparation; where steps b) to f) are carried out continuously and in sequence.

Abstract translation: 提供了一种制备具有细碎的类胡萝卜素，类视色素或天然色素的粉末制剂的方法，该方法包括以下步骤：a）将活性成分在任选含有抗氧化剂的水不混溶性有机溶剂中形成悬浮液， /或油; b）将步骤a）的悬浮液进料到热交换器; c）将悬浮液加热至100-250℃，由此在热交换器中的停留时间小于5秒以提供溶液; d）将步骤c）的溶液与可溶胀胶体和任选的稳定剂的水溶液快速混合，使得所得混合物的温度在20-100℃的范围内; e）除去有机溶剂; 和f）将步骤e）的分散体转化成粉末制剂;其中步骤b）至f）连续且顺序地进行。