公开(公告)号：EP0708085A2

公开(公告)日：1996-04-24

申请号：EP95115938.3

申请日：1995-10-10

申请人： CIBA-GEIGY AG

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.

IPC分类号： C07C271/22 ,  A61K31/325 ,  C07C317/50 ,  C07D295/215 ,  C07D211/48 ,  C07D307/20 ,  C07D213/30

CPC分类号： C07D207/26 ,  A61K31/47 ,  A61K31/495 ,  C07C255/60 ,  C07C271/22 ,  C07C311/19 ,  C07C311/42 ,  C07C317/50 ,  C07C2601/14 ,  C07C2602/10 ,  C07D207/28 ,  C07D209/42 ,  C07D211/46 ,  C07D211/62 ,  C07D213/30 ,  C07D213/82 ,  C07D277/06 ,  C07D277/40 ,  C07D295/155 ,  C07D307/20 ,  C07D309/04 ,  C07D309/12 ,  C07D311/24 ,  C07D317/60 ,  A61K2300/00

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.

公开(公告)号：EP0708085A3

公开(公告)日：1997-10-08

申请号：EP95115938.3

申请日：1995-10-10

申请人： CIBA-GEIGY AG

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.

IPC分类号： C07C271/22 ,  A61K31/325 ,  C07C317/50 ,  C07D295/215 ,  C07D211/48 ,  C07D307/20 ,  C07D213/30

CPC分类号： C07D207/26 ,  A61K31/47 ,  A61K31/495 ,  C07C255/60 ,  C07C271/22 ,  C07C311/19 ,  C07C311/42 ,  C07C317/50 ,  C07C2601/14 ,  C07C2602/10 ,  C07D207/28 ,  C07D209/42 ,  C07D211/46 ,  C07D211/62 ,  C07D213/30 ,  C07D213/82 ,  C07D277/06 ,  C07D277/40 ,  C07D295/155 ,  C07D307/20 ,  C07D309/04 ,  C07D309/12 ,  C07D311/24 ,  C07D317/60 ,  A61K2300/00

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.