公开(公告)号：EP1594870B1

公开(公告)日：2011-05-11

申请号：EP03811395.7

申请日：2003-11-14

申请人： Tibotec Pharmaceuticals

发明人： KESTELEYN, Bart, Rudolf, Romanie ,  VAN DE VREKEN, Wim ,  KINDERMANS, Natalie, Maria, Francisca ,  CANARD, Maxime, Francis, Jean-Marie, Ghislain ,  HERTOGS, Kurt ,  BETTENS, Eva ,  DE VROEY, Veronique, Corine, Paul ,  JOCHMANS, Dirk, Edward, Désiré ,  WIGERINCK, Piet Tom Bert Paul ,  TAHRI, Abdellah ,  WANG, Jing ,  SURLERAUX, Dominique Louis Nestor Ghislain

IPC分类号： A61K31/437 ,  A61P31/12 ,  C07D471/04

CPC分类号： C07D471/04

摘要： The present invention concerns the compounds of formula (1) (R3)n P(I) N O R1 R2 their N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites, wherein n is 1, 2 or 3; R1 is H, CN, halo, aminoC(=O), C(=O)OH, C1-4-alkyloxyC(=O), C1-4alkylC(='O), mono- or di(C1-4alkyl)aminoC(=O), arylaminoC(=O), N-(aryl)-N-(C1-4alkyl)aminoC(=O), methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; R2 is H, C1-10alkyl, C2-10allkenyl, C3-7cycloalkyl, wherein said C1-10alkyl,C2-10alkenyl and C3-7cycloalkyl may be optionally substituted; R3 is nitro, cyano, amino, halo, hydroxy,C1-4alkyloxy, hydroxyC(=O), aminoC(=O), C1-4alkyloxyC(=O), mono- or di(C1-4-alkyl)aminoC(=O), C1-4alkylC(=O), methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy methanimidamidyl or Het1; for use as a medicine. The invention further relates to a novel subgroup of the compounds of formula (I), and to compositions comprising compounds of formula (I).

公开(公告)号：EP1750708A1

公开(公告)日：2007-02-14

申请号：EP05747916.4

申请日：2005-05-17

申请人： Tibotec Pharmaceuticals Ltd.

发明人： KESTELEYN, Bart, Rudolf, Romanie ,  VAN DE VREKEN, Wim ,  KINDERMANS, Natalie, Maria, Francisca ,  CANARD, Maxime, Francis, Jean-Marie, Ghislain ,  HERTOGS, Kurt ,  BETTENS, Eva ,  DE VROEY, Veronique, Corine, Paul ,  JOCHMANS, Dirk, Edward, Désiré ,  WIGERINCK, Piet, Tom, Bert, Paul ,  WANG, Jing ,  TAHRI, Abdellah ,  SURLERAUX, Dominique, Louis, Nestor, Ghislain

IPC分类号： A61K31/475 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  A61P31/12 ,  A61P31/18

CPC分类号： A61K31/475 ,  A61K31/496 ,  A61K31/5377 ,  A61K2300/00

摘要： The present invention concerns combinations comprising a compound of formula (I); the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters or metabolites thereof, wherein n is 1, 2 or 3; R1 is H, CN, halo, aminoC(=O), C(=O)OH, C1-4alkyloxyC(=O), C1-4 alkylC(=O), mono- or di(C1-4alkyl)aminoC(=O), arylaminoC(=O), N-(aryl)-N-(C1-4 alkyl)aminoC(=O), methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; R2 is H, C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, wherein said C1-10alkyl, C2-10alkenyl and C3-7 cycloalkyl may be optionally substituted; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxyC(=O), aminoC(=O), C1-4alkyloxyC(=O), mono- or di(C1-4alkyl)aminoC(=O), C1-4alkylC(=O), methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1; and another HIV inhibitor. The invention also concerns products comprising a compound of formula (I) and another HIV inhibitor, as a combined preparation for simultaneous, separate or sequential use in treatment of retroviral infections such as HIV infection, in particular, in the treatment of infections with multi-drug resistant retroviruses.

公开(公告)号：EP1594870A1

公开(公告)日：2005-11-16

申请号：EP03811395.7

申请日：2003-11-14

申请人： Tibotec Pharmaceuticals Ltd.

发明人： KESTELEYN, Bart, Rudolf, Romanie ,  VAN DE VREKEN, Wim ,  KINDERMANS, Natalie, Maria, Francisca ,  CANARD, Maxime, Francis, Jean-Marie, Ghislain ,  HERTOGS, Kurt ,  BETTENS, Eva ,  DE VROEY, Veronique, Corine, Paul ,  JOCHMANS, Dirk, Edward, Désiré ,  WIGERINCK, Piet Tom Bert Paul ,  TAHRI, Abdellah ,  WANG, Jing ,  SURLERAUX, Dominique Louis Nestor Ghislain

IPC分类号： C07D471/00 ,  A61K31/437 ,  A61P31/12

CPC分类号： C07D471/04

摘要： The present invention concerns the compounds of formula (1) (R3)n P(I) N O R1 R2 their N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites, wherein n is 1, 2 or 3; R1 is H, CN, halo, aminoC(=O), C(=O)OH, C1-4-alkyloxyC(=O), C1-4alkylC(='O), mono- or di(C1-4alkyl)aminoC(=O), arylaminoC(=O), N-(aryl)-N-(C1-4alkyl)aminoC(=O), methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; R2 is H, C1-10alkyl, C2-10allkenyl, C3-7cycloalkyl, wherein said C1-10alkyl,C2-10alkenyl and C3-7cycloalkyl may be optionally substituted; R3 is nitro, cyano, amino, halo, hydroxy,C1-4alkyloxy, hydroxyC(=O), aminoC(=O), C1-4alkyloxyC(=O), mono- or di(C1-4-alkyl)aminoC(=O), C1-4alkylC(=O), methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy methanimidamidyl or Het1; for use as a medicine. The invention further relates to a novel subgroup of the compounds of formula (I), and to compositions comprising compounds of formula (I).

摘要翻译： 本发明涉及其N-氧化物，盐，立体异构体形式，外消旋混合物，前体药物，酯和代谢物的式（1）（R 3）n P（I）NR 1 R 2 R 2化合物，其中n是1,2或3; （= O），C（= O）OH，C 1-4烷氧基C（= O），C 1-4烷基C（= O），单或二（C 1-4烷基）氨基C （= O），芳基氨基C（= O），N-（芳基）-N-（C 1-4烷基）氨基C（= O），甲脒基，N-羟基甲脒基，单或二 或Het2; R2为H，C1-10烷基，C2-10链烯基，C3-7环烷基，其中所述C1-10烷基，C2-10链烯基和C3-7环烷基可以任选地被取代; R3是硝基，氰基，氨基，卤素，羟基，C1-4烷氧基，羟基C（= O），氨基C（= O），C1-4烷氧基C（= O），单 - 或二（C1-4-烷基） O），C 1-4烷基C（= O），甲脒基，单或二（C 1-4烷基）甲脒基，N-羟基甲脒基或Het 1; 用作药物。 本发明进一步涉及式（I）化合物的新亚组，并涉及包含式（I）化合物的组合物。