公开(公告)号：US5773468A

公开(公告)日：1998-06-30

申请号：US572402

申请日：1995-12-14

申请人： Sung Chun Kim ,  Young Chan Son ,  Ho Il Choi ,  Heungsik Yoon ,  Chi Hyo Park ,  Nakyen Choy ,  Chang Sun Lee ,  Jong Sung Koh ,  Kwang Yul Moon ,  Won Hee Jung ,  Chung Ryeol Kim

发明人： Sung Chun Kim ,  Young Chan Son ,  Ho Il Choi ,  Heungsik Yoon ,  Chi Hyo Park ,  Nakyen Choy ,  Chang Sun Lee ,  Jong Sung Koh ,  Kwang Yul Moon ,  Won Hee Jung ,  Chung Ryeol Kim

IPC分类号： A61K38/00 ,  C07D303/46 ,  A01N43/20 ,  A01N31/34

CPC分类号： C07D303/46 ,  A61K38/00

摘要： The present invention relates to a novel compound of formula (I) and pharmaceutically acceptable salts, hydrates and solvates thereof which is an irreversible HIV protease inhibitor; a process for the preparation thereof; and a pharmaceutical composition containing the compound as an active ingredient which is useful for treating or preventing diseases caused by HIV infection. ##STR1##

摘要翻译： 本发明涉及新的式（I）化合物及其药学上可接受的盐，水合物和溶剂化物，其是不可逆的HIV蛋白酶抑制剂; 其制备方法; 以及含有该化合物作为活性成分的药物组合物，其可用于治疗或预防由HIV感染引起的疾病。 （一）

公开(公告)号：US5696134A

公开(公告)日：1997-12-09

申请号：US473877

申请日：1995-06-07

申请人： Heungsik Yoon ,  Nakyen Choy ,  Sung Chun Kim ,  Ho Il Choi ,  Young Chan Son ,  Chi Hyo Park ,  Kwang-Yul Moon ,  Wonhee Jung ,  Chung Ryeol Kim ,  Chang Sun Lee ,  Jong Sung Koh ,  Sang Soo Kim

发明人： Heungsik Yoon ,  Nakyen Choy ,  Sung Chun Kim ,  Ho Il Choi ,  Young Chan Son ,  Chi Hyo Park ,  Kwang-Yul Moon ,  Wonhee Jung ,  Chung Ryeol Kim ,  Chang Sun Lee ,  Jong Sung Koh ,  Sang Soo Kim

IPC分类号： A61K38/00 ,  C07K5/02 ,  A61K31/44 ,  A61K31/47

CPC分类号： C07K5/0207 ,  A61K38/00

摘要： Novel cis-epoxide compounds of formula (I) are useful for treating or preventing diseases caused by HIV infection: ##STR1## wherein A, B, R.sub.1 to R.sub.4 and n have the same meanings as defined in the specification. The novel HIV protease inhibitor of the formula (I) has a specific structure to form a stable bonding with the enzyme active site, which entails a highly enhanced irreversible inhibition against HIV protease.

摘要翻译： 式（I）的新型顺式环氧化合物可用于治疗或预防由HIV感染引起的疾病：其中A，B，R 1至R 4和n具有与说明书中所定义相同的含义。 式（I）的新型HIV蛋白酶抑制剂具有与酶活性位点形成稳定结合的特定结构，这对HIV蛋白酶具有高度的不可逆抑制作用。

公开(公告)号：US06747050B1

公开(公告)日：2004-06-08

申请号：US10088288

申请日：2002-03-15

申请人： Eunice Eun-Kyeong Kim ,  Mi-Jeong Park ,  Tae-Hee Lee ,  Hye-Kyung Chang ,  Tae-Kyo Park ,  Chang-Yuil Kang ,  Young-Myeong Kim ,  Kwang-Yul Moon ,  Young-Leem Oh ,  Chang-Hee Min ,  Hyun-Ho Chung

发明人： Eunice Eun-Kyeong Kim ,  Mi-Jeong Park ,  Tae-Hee Lee ,  Hye-Kyung Chang ,  Tae-Kyo Park ,  Chang-Yuil Kang ,  Young-Myeong Kim ,  Kwang-Yul Moon ,  Young-Leem Oh ,  Chang-Hee Min ,  Hyun-Ho Chung

IPC分类号： A61K3142

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D261/18 ,  C07D413/12

摘要： The present invention provides to an isoxazoline derivative of formula (I), the pharmaceutically acceptable salts, esters and stereochemically isomeric forms thereof, and the use of the derivative in inhibiting the activity of caspases. The present invention also provides a pharmaceutical composition for preventing inflammation and apoptosis which comprise the isoxazoline derivative, pharmaceutically acceptable salts, esters and stereochemically isomeric forms thereof and the process for preparing the same. The derivative according to the present invention can be effectively used in treating diseases due to caspases, such as, for example the disease in which cells are abnormally died, dementia, cerebral stroke, AIDS, diabetes, gastric ulcer, hepatic injury by hepatitis, sepsis, organ transplantation rejection reaction and anti-inflammation.

摘要翻译： 本发明提供了式（I）的异恶唑啉衍生物，其药学上可接受的盐，酯和立体化学异构形式，以及该衍生物在抑制胱天蛋白酶活性方面的用途。 本发明还提供了包含异恶唑啉衍生物，其药学上可接受的盐，酯和立体化学异构形式的用于预防炎症和细胞凋亡的药物组合物及其制备方法。 根据本发明的衍生物可以有效地用于治疗由于胱天蛋白酶引起的疾病，例如细胞异常死亡的疾病，痴呆，脑卒中，艾滋病，糖尿病，胃溃疡，肝炎肝损伤，败血症 器官移植排斥反应和抗炎。

公开(公告)号：US06307059B1

公开(公告)日：2001-10-23

申请号：US09623214

申请日：2000-08-30

申请人： Jay Hyok Chang ,  Won Sup Kim ,  Tae Hee Lee ,  Kwang Yul Moon

发明人： Jay Hyok Chang ,  Won Sup Kim ,  Tae Hee Lee ,  Kwang Yul Moon

IPC分类号： C07D20722

CPC分类号： C07D471/04 ,  C07D207/22 ,  C07D207/24 ,  C07D207/36 ,  Y02P20/55

摘要： A process for preparing a compound of formula (1) in which P1 and P2 are protecting groups; comprising a) reaction of a compound of formula (5) wherein P1 is as defined for formula (1); with a Raney-nickel catalyst in a solvent under hydrogen to produce a compound of formula (6) wherein P1 is as defined for formula (1); b) protecting the amino group to produce a compound of formula (7) wherein P1 and P2 are as defined for formula (1); and c) selective reduction of the double bond to produce the compound of formula (1).

摘要翻译： 制备式（1）化合物的方法，其中P1和P2为保护基; 包括a）其中P1如式（1）所定义的式（5）化合物的反应; 用阮内镍催化剂在溶剂中在氢气下制备式（6）化合物，其中P1如式（1）所定义; b）保护氨基以产生其中P1和P2如式（1）所定义的式（7）化合物; 和c）选择性还原双键以制备式（1）化合物。