KNI-102(KNI-102) - 药物靶点：HIV-1 protease_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

HIV-1 protease

作用机制

HIV-1 protease抑制剂(HIV蛋白酶抑制剂)

治疗领域

免疫系统疾病感染泌尿生殖系统疾病

在研适应症-

非在研适应症

HIV感染

原研机构

Japan Energy, Inc.

在研机构-

非在研机构

Japan Energy, Inc.

最高研发阶段终止药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 KNI-102 相关的临床结果

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100 项与 KNI-102 相关的转化医学

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100 项与 KNI-102 相关的专利（医药）

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2

项与 KNI-102 相关的文献（医药）

1998-01-01·Chemical and Pharmaceutical Bulletin4区 · 医学

Synthesis of Dipeptide-Type Human Immunodeficiency Virus (HIV) Protease Inhibitors with a Binding Unit to GP120.

4区 · 医学

Article

作者: Nao Takayanagi ; Akira Asagarasu ; Kazuo Achiwa

Some dipeptide-type human immunodeficiency virus (HIV) protease inhibitors derived from KNI-102, with a N-carbomethoxycarbonylprolyl-phenylalanine benzyl ester (CPF) moiety as a binding site to gp120, were synthesized. Compounds 11a showed 7--100 times higher HIV protease-inhibitory activity (11a; IC50 = 0.90 microgram/ml, 1.1 microM) than the standard compound 3 or 4 (3; IC50 = 3.7 micrograms/ml, 7.7 microM, 4; IC50 = 75 micrograms/ml, 155 microM). Generally, the compounds substituted at the o-position of the phenoxyacetyl group 7a, 11a, 16a and 21a showed several times higher inhibitory activity than 3.

1991-01-01·Chemical and Pharmaceutical Bulletin4区 · 医学

KNI-102, a novel tripeptide HIV protease inhibitor containing allophenylnorstatine as a transition-state mimic.

4区 · 医学

Article

作者: Hattori, Naoko ; Kisanuki, Sumitsugu ; Mimoto, Tsutomu ; Tanaka, Shigeki ; Akaji, Kenichi ; Kiso, Yoshiaki ; Imai, Junya

HIV-1 protease inhibitors containing allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid]-Pro (syn diastereomer) as a transition-state mimic were established to be potent and highly selective. Z-Asn-Apns-Pro-NHBut (KNI-102) is the only tripeptide exhibiting substantial anti-HIV activity and may be of minimum size for potent, selective inhibition of HIV protease. Ready availability due to its simple chemical structure and stability should make it valuable for studies of the development of metabolically stable anti-AIDS drugs.

100 项与 KNI-102 相关的药物交易

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