公开(公告)号：US5670517A

公开(公告)日：1997-09-23

申请号：US659791

申请日：1996-06-06

Applicant: Nakyen Choy ,  Hoil Choi ,  Chi-Hyo Park ,  Young-Chan Son ,  Chang-Sun Lee ,  Heungsik Yoon ,  Sung-Chun Kim ,  Jong-Sung Koh ,  Chung-Ryeol Kim

Inventor： Nakyen Choy ,  Hoil Choi ,  Chi-Hyo Park ,  Young-Chan Son ,  Chang-Sun Lee ,  Heungsik Yoon ,  Sung-Chun Kim ,  Jong-Sung Koh ,  Chung-Ryeol Kim

IPC: A61K38/00 ,  C07D303/36 ,  C07D405/12 ,  C07K5/02 ,  A61K31/47 ,  A61K31/335 ,  C07D215/14 ,  C07D217/15

CPC classification number: C07D405/12 ,  C07D303/36 ,  C07K5/021 ,  A61K38/00

Abstract: The present invention relates to novel compounds of formula (I) which has inhibitory activities against human immunodeficiency virus ("HIV") protease, a process for the preparation thereof, and compositions for prevention or treatment of AIDS by HIV infection comprising the above compounds as active ingredients. ##STR1## wherein: R.sup.1 is an aromatic group, a nitrogen-containing aromatic group, C.sub.1-4 alkyl group optionally substituted with an aromatic group or a nitrogen-containing aromatic group, C.sub.1-4 alkoxy group optionally substituted with an aromatic group or a nitrogen-containing aromatic group; R.sup.2 is an amino acid residue or a C.sub.1-8 alkyl group substituted with a C.sub.1-4 alkylsulfonyl group; R.sup.3 is a C.sub.1-4 alkyl group optionally substituted with an aromatic group; R.sup.4 is hydrogen or a C.sub.1-2 alkyl group; R.sup.5 is a C.sub.1-10 alkyl group optionally substituted with an aromatic group; and n is 1 or 2.

Abstract translation: 本发明涉及对人体免疫缺陷病毒（“HIV”）蛋白酶具有抑制活性的新型式（I）化合物，其制备方法，以及用于通过HIV感染预防或治疗AIDS的组合物，其包含上述化合物作为 有效成分。 （I）其中：R1是芳基，含氮芳香基，任选被芳基或含氮芳基取代的C1-4烷基，任选被芳族取代的C 1-4烷氧基 基团或含氮芳族基团; R2是被C1-4烷基磺酰基取代的氨基酸残基或C1-8烷基; R3是任选被芳基取代的C 1-4烷基; R4是氢或C1-2烷基; R5是任选被芳基取代的C 1-10烷基; n为1或2。