发明公开
- 专利标题: Antiviral ethers of aspartate protease substrate isosteres
- 专利标题(中): 天冬氨酸蛋白酶底物等排物的抗病毒醚
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申请号: EP95115938.3申请日: 1995-10-10
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公开(公告)号: EP0708085A3公开(公告)日: 1997-10-08
- 发明人: Bold, Guido, Dr. , Capraro, Hans-Georg, Dr. , Fässler, Alexander, Dr. , Lang, Marc, Dr. , Bhagwat, Shripad Subray, Dr. , Khanna, Satish Chandra, Dr. , Lazdins, Janis Karlis, Dr. , Mestan, Jürgen, Dr.
- 申请人: CIBA-GEIGY AG
- 申请人地址: Klybeckstrasse 141 CH-4002 Basel CH
- 专利权人: CIBA-GEIGY AG
- 当前专利权人: CIBA-GEIGY AG
- 当前专利权人地址: Klybeckstrasse 141 CH-4002 Basel CH
- 优先权: CH3140/94 19941019; CH2382/95 19950821
- 主分类号: C07C271/22
- IPC分类号: C07C271/22 ; A61K31/325 ; C07C317/50 ; C07D295/215 ; C07D211/48 ; C07D307/20 ; C07D213/30
摘要:
Antiretroviral compounds (which are effective, for example, against HIV) of the formula I
in which
R₁ is an acyl radical lower-alkoxy-lower-alkanoyl whose lower alkoxy radical is unsubstituted or is substituted by halogen, phenyl, lower alkoxy or a heterocyclic radical selected from piperidinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl, thiazolidinyl, thiazolyl, indolyl or 4H-1-benzopyranyl which is unsubstituted or substituted by oxo, hydroxyl, amino, lower alkyl, lower-alkoxycarbonyl and/or phenyl-lower-alkoxycarbonyl; lower alkanoyl which is unsubstituted or is substituted by one of the said unsubstituted or substituted heterocyclic radicals; arylcarbonyl or heterocyclylcarbonyl which are substituted by heterocyclyl or heterocyclyl-lower-alkyl; phenyl-lower-alkanoyl which is substituted by hydroxyl and lower alkyl; or arylsulfonyl;
or the residue of an amino acid which is defined in accordance with the description (and which may be acylated on the amino nitrogen by one of the abovementioned acyl radicals);
R₂ and R₃ are in each case cyclohexyl, cyclohexenyl, phenyl, naphthyl or tetrahydronaphthyl which are unsubstituted or substituted by lower alkyl, phenyl, cyanophenyl, phenyl-lower-alkyl, halogen, halo-lower-alkyl, cyano, hydroxyl, lower alkoxy, phenyl-lower-alkoxyl, pyridyl-lower-alkoxy, lower-alkoxy-lower-alkoxy, lower-alkoxycarbonyl-lower-alkoxy, carboxyl-lower-alkoxy, hydroxyl-lower-alkoxy, carbamoyl-lower-alkoxy, cyano-lower-alkoxy, and phenyl-lower-alkanesulfonyl which is unsubstituted or substituted by halogen;
R₄ is lower alkyl, cyclohexyl or phenyl; and R₅ is lower alkyl; and n is 1 or 2, or salts thereof, are novel.
in which
R₁ is an acyl radical lower-alkoxy-lower-alkanoyl whose lower alkoxy radical is unsubstituted or is substituted by halogen, phenyl, lower alkoxy or a heterocyclic radical selected from piperidinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl, thiazolidinyl, thiazolyl, indolyl or 4H-1-benzopyranyl which is unsubstituted or substituted by oxo, hydroxyl, amino, lower alkyl, lower-alkoxycarbonyl and/or phenyl-lower-alkoxycarbonyl; lower alkanoyl which is unsubstituted or is substituted by one of the said unsubstituted or substituted heterocyclic radicals; arylcarbonyl or heterocyclylcarbonyl which are substituted by heterocyclyl or heterocyclyl-lower-alkyl; phenyl-lower-alkanoyl which is substituted by hydroxyl and lower alkyl; or arylsulfonyl;
or the residue of an amino acid which is defined in accordance with the description (and which may be acylated on the amino nitrogen by one of the abovementioned acyl radicals);
R₂ and R₃ are in each case cyclohexyl, cyclohexenyl, phenyl, naphthyl or tetrahydronaphthyl which are unsubstituted or substituted by lower alkyl, phenyl, cyanophenyl, phenyl-lower-alkyl, halogen, halo-lower-alkyl, cyano, hydroxyl, lower alkoxy, phenyl-lower-alkoxyl, pyridyl-lower-alkoxy, lower-alkoxy-lower-alkoxy, lower-alkoxycarbonyl-lower-alkoxy, carboxyl-lower-alkoxy, hydroxyl-lower-alkoxy, carbamoyl-lower-alkoxy, cyano-lower-alkoxy, and phenyl-lower-alkanesulfonyl which is unsubstituted or substituted by halogen;
R₄ is lower alkyl, cyclohexyl or phenyl; and R₅ is lower alkyl; and n is 1 or 2, or salts thereof, are novel.
公开/授权文献
- EP0708085B1 Antiviral ethers of aspartate protease substrate isosteres 公开/授权日:2002-07-17
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