公开(公告)号：US06310070B1

公开(公告)日：2001-10-30

申请号：US09462861

申请日：2000-04-28

申请人： Akihisa Yokoyama ,  Sumitsugu Kisanuki ,  Yoshikazu Matsuda ,  Junko Matsui ,  Yoshiaki Isobe

发明人： Akihisa Yokoyama ,  Sumitsugu Kisanuki ,  Yoshikazu Matsuda ,  Junko Matsui ,  Yoshiaki Isobe

IPC分类号： C07D47330

CPC分类号： C07D473/30

摘要： A novel purine derivative exhibiting an effect to control inflammatory symptoms characteristic to nephritis and a medicine comprising this compound as an effective ingredient are provided. The compound is represented by the following general formula (I), wherein R1 is a hydrocarbon group having 17 or less carbon atoms and R2 is a hydrocarbon group having 16 or less carbon atoms, wherein one or more CH2 g roups in the hydrocarbon group which 7013 do not directly bind with the carbon atom at 2 or 7 position of the purine ring replaced are by carbonyl groups, sulfonyl groups, O, or S and/or one or more CH groups in the hydrocarbon group which do not directly bind with the carbon atom at 2 or 7 position of the purine ring are replaced by N, C-halogen, or C—C≡N, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明提供了具有控制肾炎特征性炎症症状的效果的新型嘌呤衍生物和含有该化合物作为有效成分的药物。 该化合物由以下通式（I）表示，其中R 1是具有17个或更少碳原子的烃基，R 2是具有16个或更少碳原子的烃基，其中一个或多个在烃基中的CH 2 7013不与嘌呤环的2或7位的碳原子直接结合，所取代的碳原子是羰基，磺酰基，O或S和/或烃基中一个或多个不与直接键合的CH基团 嘌呤环2或7位的碳原子被N，C-卤素或CC = N取代，或其药学上可接受的盐。

公开(公告)号：US5644028A

公开(公告)日：1997-07-01

申请号：US364707

申请日：1994-12-28

申请人： Tsutomu Mimoto ,  Sumitsugu Kisanuki ,  Osamu Takahashi ,  Yoshiaki Kiso

发明人： Tsutomu Mimoto ,  Sumitsugu Kisanuki ,  Osamu Takahashi ,  Yoshiaki Kiso

IPC分类号： C07C319/14 ,  C07C323/59 ,  C07D277/06 ,  C07D417/12 ,  C07K1/02 ,  C07K1/08 ,  C07K1/10 ,  C07K5/083

CPC分类号： C07D417/12 ,  C07C319/14 ,  C07D277/06

摘要： A process for producing peptide derivatives of formula (1) or salts thereof: ##STR1## which comprises condensation of peptide derivative of formula (2): ##STR2## with carboxylic acid of formula (3): ##STR3## or condensation of a peptide derivative of formula (4): ##STR4## with a protected amino acid of formula (5'): ##STR5## wherein R.sup.1 and R.sup.2 are a lower alkyl group or hydrogen atom, R.sup.3 is a lower alkyl group, X is a methylthiomethyl, methanesulfonylmethyl, carbamoylmethyl, or a lower alkyl group, Ar is an aryl or heteroaryl group, and A.sup.4 is Ar--O--CH.sub.2 --CO. The peptide derivatives and salts thereof are useful as the human immunodeficiency virus (HIV) protease inhibitors.

摘要翻译： （1）的肽衍生物或其盐的制备方法：包括式（2）的肽衍生物与式（3）的羧酸缩合的式（1）：IMA图 （3）或式（4）的肽衍生物与式（5'）的保护的氨基酸的缩合：其中R 1和R 2是低级烷基 或氢原子，R3是低级烷基，X是甲硫基甲基，甲磺酰基甲基，氨基甲酰基甲基或低级烷基，Ar是芳基或杂芳基，A4是Ar-O-CH2-CO。 肽衍生物及其盐可用作人类免疫缺陷病毒（HIV）蛋白酶抑制剂。