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11. 发明申请

WO2006035061A1 HCV INHIBITING BI-CYCLIC PYRIMIDINES 审中-公开
标题翻译： HCV抑制双循环嘧啶
公开(公告)号：WO2006035061A1
公开(公告)日：2006-04-06
申请号：PCT/EP2005/054912
申请日：2005-09-29
申请人： TIBOTEC PHARMACEUTICALS LTD. , SIMMEN, Kenneth Alan , LIN, Tse-I , LENZ, Oliver , SURLERAUX, Dominique, Louis, Nestor, Ghislain , RABOISSON, Pierre, Jean-Marie, Bernard
发明人： SIMMEN, Kenneth Alan , LIN, Tse-I , LENZ, Oliver , SURLERAUX, Dominique, Louis, Nestor, Ghislain , RABOISSON, Pierre, Jean-Marie, Bernard
IPC分类号： A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/5377 , A61P1/16 , A61P31/14 , A61P35/00
CPC分类号： A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/5377 , Y02A50/385 , Y02A50/387
摘要： The present invention relates to the use of bi-cyclic pyrimidines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to processes for preparation of such pharmaceutical compositions. The present invention also concerns combinat ions of the present bi-cyclic pyrimidines with other anti-HCV agents.
摘要翻译：本发明涉及双环嘧啶作为HCV复制抑制剂的用途，以及它们在旨在治疗或对抗HCV感染的药物组合物中的用途。此外，本发明涉及这种药物组合物的制备方法。本发明还涉及本发明的双环嘧啶与其它抗HCV剂的组合离子。

12. 发明申请

WO2005111044A1 4-SUBSTITUTED-1,5-DIHYDRO-PYRIDO[3,2-B]INDOL-2-ONES 审中-公开
标题翻译： 4-取代的-1,5-二氢 - 吡啶并[3,2-b]吲哚-2-酮
公开(公告)号：WO2005111044A1
公开(公告)日：2005-11-24
申请号：PCT/EP2005/052265
申请日：2005-05-17
申请人： TIBOTEC PHARMACEUTICALS Ltd. , KESTELEYN, Bart, Rudolf, Romanie , VAN DE VREKEN, Wim , SURLERAUX, Dominique, Louis, Nestor, Ghislain , VENDEVILLE, Sandrine, Marie, Helene , RABOISSON, Pierre, Jean-Marie, Bernard , WIGERINCK, Piet, Tom, Bert, Paul , PEETERS, Annick, Ann
发明人： KESTELEYN, Bart, Rudolf, Romanie , VAN DE VREKEN, Wim , SURLERAUX, Dominique, Louis, Nestor, Ghislain , VENDEVILLE, Sandrine, Marie, Helene , RABOISSON, Pierre, Jean-Marie, Bernard , WIGERINCK, Piet, Tom, Bert, Paul , PEETERS, Annick, Ann
IPC分类号： C07D491/04
CPC分类号： C07D471/04 , C07D491/04 , C07D491/14
摘要： 4-substituted 1,5-dihydro-pyrido[3,2-b]indol-2-ones of formula (I): the N -oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein n is 1, 2 or 3; R 1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N -hydroxymethanimidamidyl, mono- or di(C 1-4 alkyl)methanimidamidyl, Het 1 or Het 2 ; X is NR 2 , O, S, SO, SO 2 ; R 2 is hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 3-7 cycloalkyl, which are optionally substituted; R 2 is aryl substituted with -COOR 4 ; or R 2 is: (b-1); (b-2); -C p H 2p -CH(OR 14 )-C q H 2q -R 15 (b-3); -CH 2 -CH 2 -(O-CH 2 -CH 2 ) m -OR 14 (b-4); -CH 2 -CH 2 -(O-CH 2 -CH 2 ) m -NR 5a R 5b (b-5); -a 1 =a 2 -a 3 =a 4 - is -CH=CH-CH=CH-; -N=CH-CH=CH-; -CH=N-CH=CH-; -CH=CH-N=CH-; -CH=CH-CH=N-; wherein hydrogen atoms in (c-1) - (c-5) may be replaced by certain radicals; R 3 is obtionally substituted phenyl or a monocyclic or bicyclic aromatic heterocyclic ring system that can be substituted; R 21 is halo, hydroxy, amino, carboxyl, C 1-6 alkyl, C 3-7 cycloalkyl, arylC 1-6 alkyl, formyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonylo xy, -C(=O)-NR 13 R 14 ; C 1-6 alkyloxy, arylC 1-6 alkyloxy, polyhaloC 1-6 alkyloxy, amino, mono or di(C 1-6 alkyl)amino, formylamino, C 1-6 alkylcarbonylamino, C 1-6 alkylsulfo nylamino, mercapto, C 1-6 alkylthio, arylthio, aryloxy, arylC 1-6 alkylthio, C 1-6 alkylsulfynyl, C 1-6 alkylsulfo nyl, aryl, arylamino, Het 1 , Het 2 .
摘要翻译：式（I）的4-取代的1,5-二氢吡啶并[3,2-b]吲哚-2-酮：N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物，其中n 是1，2或3; R 1是氢，氰基，卤素，取代的羰基，甲亚氨基酰胺基，N-羟基甲酰亚胺基，单或二（C 1-4烷基）甲酰亚胺基，Het1或Het2; X是NR 2，O，S，SO，SO 2; R 2是氢，C 1-10烷基，C 2-10烯基，C 3-7环烷基，其任选被取代; R 2是被-COOR 4取代的芳基; 或R 2为：（b-1）; （B-2）; -CpH2p-CH（OR 14）-C≡H2q-R 15（b-3）; -CH 2 -CH 2 - （O-CH 2 -CH 2）m -OR 14（b-4）; -CH 2 CH 2 - （O-CH2-CH2）M-NR <5A> - [R <5B>（B-5）; -a 1 = a 2 -a 3 = a 4 - 是-CH = CH-CH = CH-; -N = CH-CH = CH-; -CH = N-CH = CH-; -CH = CH-N = CH-; -CH = CH-CH = N-; 其中（c-1） - （c-5）中的氢原子可被某些基团取代; R 3是被取代的苯基或可被取代的单环或双环芳族杂环体系; R 21是卤素，羟基，氨基，羧基，C 1-6烷基，C 3-7环烷基，芳基C 1-6烷基，甲酰基，C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基氧基，-C（= O）-NR 13 > - [R <14>; C 1-6烷氧基，芳基C 1-6烷氧基，多卤代C 1-6烷氧基，氨基，单或二（C 1-6烷基）氨基，甲酰氨基，C 1-6烷基羰基氨基，C 1-6烷基磺酰基氨基，巯基，C 1-6烷硫基，芳硫基，芳氧基，芳基C 1-6烷硫基， -6-烷基亚磺酰基，C 1-6烷基磺酰基，芳基，芳基氨基，Het 1，Het 2。

13. 发明申请

WO2005110411A1 COMBINATIONS OF SUBSTITUTED 1-PHENYL-1,5-DIHYDRO-PYRIDO- [3,2-B] INDOL-2-ONES AND OTHER HIV INHIBITORS 审中-公开
标题翻译：取代的1-苯基-1,5-二氢吡喃并[3,2-B]吲哚-2-酮和其他HIV抑制剂的组合
公开(公告)号：WO2005110411A1
公开(公告)日：2005-11-24
申请号：PCT/EP2005/052266
申请日：2005-05-17
申请人： TIBOTEC PHARMACEUTICALS LTD. , 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
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
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; R 1 is H, CN, halo, aminoC(=O), C(=O)OH, C 1-4 alkyloxyC(=O), C 1-4 alkylC(=O), mono- or di(C 1-4 alkyl)aminoC(=O), arylaminoC(=O), N -(aryl)- N -(C 1-4 alkyl)aminoC(=O), methanimidamidyl, N -hydroxy-methanimidamidyl, mono- or di(C 1-4 alkyl)methanimidamidyl, Het 1 or Het 2 ; R 2 is H, C 1-10 alkyl, C 2-10 alkenyl, C 3-7 cycloalkyl, wherein said C 1-10 alkyl, C 2-10 alkenyl and C 3-7 cycloalkyl may be optionally substituted; R 3 is nitro, cyano, amino, halo, hydroxy, C 1-4 alkyloxy, hydroxyC(=O), aminoC(=O), C 1-4 alkyloxyC(=O), mono- or di(C 1-4 alkyl)aminoC(=O), C 1-4 alkylC(=O), methanimidamidyl, mono- or di(C 1-4 alkyl)methanimidamidyl, N -hydroxy-methanimidamidyl or Het 1 ; 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.
摘要翻译：本发明涉及包含式（I）化合物的组合; N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯或代谢物，其中n为1,2或3; R 1是H，CN，卤素，氨基C（= 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） O），芳基氨基C（= O），N-（芳基）-N-（C 1-4烷基）氨基C（= O），甲亚氨基酰胺基，N-羟基 - 甲亚胺基酰胺基，单或二（C 1-4烷基）甲酰胺基，Het1或 HET 2; R 2是H，C 1-10烷基，C 2-10烯基，C 3-7环烷基，其中所述C 1-10烷基，C 2-10烯基和C 3-7环烷基可以任选被取代; 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）氨基C（= O），C 1-4烷基C（= O），甲亚氨基亚氨基，单或二（C 1-4烷基）甲亚氨基酰胺基，N-羟基 - 甲亚胺酰氨基或Het1; 和另一种HIV抑制剂。本发明还涉及包含式（I）化合物和另一种HIV抑制剂的产品，作为用于同时，分别或顺序用于治疗逆转录病毒感染如HIV感染的组合制剂，特别是用于治疗多发性感染的感染，耐药性逆转录病毒

14. 发明申请

WO2003097616A1 BROADSPECTRUM SUBSTITUTED BENZISOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 审中-公开
标题翻译： BROADSPECTRUM取代苯唑沙芬磺酰胺艾滋病毒蛋白酶抑制剂
公开(公告)号：WO2003097616A1
公开(公告)日：2003-11-27
申请号：PCT/EP2003/050173
申请日：2003-05-16
申请人： TIBOTEC PHARMACEUTICALS LTD , SURLERAUX, Dominique, Louis, Nestor, Ghislain , VERGOUWEN, Bernhard, Joanna, Bernard , DE KOCK, Herman, Augustinus
发明人： SURLERAUX, Dominique, Louis, Nestor, Ghislain , VERGOUWEN, Bernhard, Joanna, Bernard , DE KOCK, Herman, Augustinus
IPC分类号： C07D261/20
CPC分类号： C07D413/12 , C07D261/20 , C07D417/12 , C07D493/04
摘要： The present invention concerns the compounds having the formula N- oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs esters and metabolites thereof. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.
摘要翻译：本发明涉及具有式N-氧化物，盐，立体异构形式，外消旋混合物，前药酯及其代谢物的化合物。它还涉及它们作为广谱的HIV蛋白酶抑制剂，其制备方法以及药物组合物和包含它们的诊断试剂盒的用途。它还涉及与另一种抗逆转录病毒剂的组合，以及它们在测定中用作参考化合物或作为试剂。

15. 发明申请

WO2003076413A1 BROADSPECTRUM SUBSTITUTED BENZIMIDAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 审中-公开
标题翻译： BROADSPECTRUM取代苯并咪唑磺酰胺艾滋病毒蛋白酶抑制剂
公开(公告)号：WO2003076413A1
公开(公告)日：2003-09-18
申请号：PCT/EP2003/050057
申请日：2003-03-12
申请人： TIBOTEC PHARMACEUTICALS LTD , SURLERAUX, Dominique, Louis, Nestor, Ghislain , WIGERINCK, Piet, Tom, Bert, Paul , VOETS, Marieke, Christiane, Johanna , VENDEVILLE, Sandrine, Marie, Helene , DE KOCK, Herman, Augustinus , VERGOUWEN, Bernhard, Joanna, Bernard
发明人： SURLERAUX, Dominique, Louis, Nestor, Ghislain , WIGERINCK, Piet, Tom, Bert, Paul , VOETS, Marieke, Christiane, Johanna , VENDEVILLE, Sandrine, Marie, Helene , DE KOCK, Herman, Augustinus , VERGOUWEN, Bernhard, Joanna, Bernard
IPC分类号： C07D235/32
CPC分类号： C07D401/12 , A61K31/415 , C07D235/30 , C07D235/32 , C07D405/12 , C07D413/12 , C07D417/12 , C07D493/04
摘要： The present invention concerns the compounds having the formula (I), wherein N -oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R 1 and R 8 each are H, optionally substituted C 1-6 alkyl, C 2-6 alkenyl, C 3-7 cycloalkyl, aryl, Het 1 , Het 2 ; R 1 may also be a radical of formula (R 11a R 11b )NC(R 10a R l0b )CR 9 -; t is 0, 1 or 2; R 2 is H or C 1-6 alkyl; L is -C(=O)-, -O-C(=O)-, -NR 8 -C(=O)-, -O-C 1-6 alkanediyl-C(=O)-, -NR 8 -C 1-6 alkanediyl-C(=O)-, -S(=O) 2 -, -O-S(=O) 2 -, -NR 8 -S(=O) 2 ; R 3 is C 1-6 alkyl, aryl, C 3-7 cycloalkyl, C 3-7 cycloalkylC 1-4 alkyl, or arylC 1-4 alkyl; R 4 is H, C 1-4 alkylOC(=O), carboxyl, aminoC(=O), mono- or di(C 1-4 alkyl)aminoC(=O), C 3-7 cycloalkyl, C 2-6 alkenyl, C 2-6 alkynyl or optionally substituted C 1-6 alkyl; A is C 1-6 alkanediyl, -C(=O)-, -C(=S)-, -S(=O) 2 -, C 1-6 alkanediyl-C(=O)-, C 1-6 alkanediyl-C(=S)- or C 1-6 alkanediyl-S(=O) 2 -; R 5 is H, OH, C 1-6 alkyl, Het 1 C 1-6 alkyl, Het 2 C 1-6 alkyl, optionally substituted amino-C 1-6 alkyl; R 6 is C 1-6 alkylO, Het 1 , Het 1 O, Het 2 , Het 2 O, aryl, arylO, C 1-6 alkyloxycarbonylamino or amino; and in case _ A- is other than C 1-6 alkanediyl then R 6 may also be C 1-6 alkyl, Het 1 C 1-4 alkyl, Het 1 OC 1-4 alkyl, Het 2 C 1-4 alkyl, Het 2 OC 1-4 alkyl, arylC 1-4 alkyl, arylOC 1-4 alkyl or aminoC 1-4 alkyl; whereby each of the amino groups in the definition of R 6 may optionally be substituted; R 5 and _ A-R 6 taken together with the nitrogen atom to which they are attached may also form Het 1 or Het 2 , R 12 , is H, - NH 2 , _ NR 5 AR 6 , - C 1-6 alkyl or alkyl-W-R 14 , wherein said alkyl is optionally substituted with halogen, hydroxy, aryl, heteroaryl, Het 1 , Het 2 , or amino wherein said amino is optionally mono- or di-substituted with C 1-4 alkyl and R 13 is H, C 1-6 -alkyl, optionally substituted by aryl, Het 1 , Het 2 , hydroxy, halogen, amino whereby the amino group may be optionally be mono- or di-substituted with C 1-4 alkyl.
摘要翻译：本发明涉及具有式（I）的化合物，其中N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物，其中R 1和R 8各自为H，任选取代的C 1-6烷基，C 2-6烯基，C 3-7环烷基，芳基，Het1，Het2; R1也可以是式（R11aR11b）NC（R10aR10b）CR9-的基团; t为0,1或2; R2是H或C1-6烷基; L是-C（= O） - ， - OC（= O） - ， - NR 8 -C（= O） - ， - O-C 1-6烷二基-C（= O） - ， - NR 8 -C 1-6烷二基-C （= O） - ， - S（= O）2 - ， - OS（= O）2 - ， - NR 8 -S（= O）2; R 3是C 1-6烷基，芳基，C 3-7环烷基，C 3-7环烷基C 1-4烷基或芳基C 1-4烷基; R 4是H，C 1-4烷基OC（= O），羧基，氨基C（= O），单或二（C 1-4烷基）氨基C（= O），C 3-7环烷基，C 2-6烯基，C 2-6炔基或任选取代的C 1 1-6; A是C 1-6烷二基，-C（= O） - ， - C（= S） - ， - S（= O）2 - ，C 1-6烷二基-C（= O） - ，C 1-6烷二基-C S） - 或C 1-6烷二基-S（= O）2 - ; R5是H，OH，C1-6烷基，Het1C1-6烷基，Het2C1-6烷基，任选取代的氨基-C 1-6烷基; R 6是C 1-6烷基O，Het 1，Het 10，Het 2，Het 2 O，芳基，芳基O，C 1-6烷氧基羰基氨基或氨基; 并且在_A-不是C 1-6烷二基的情况下，R 6还可以是C 1-6烷基，Het 1 C 1-4烷基，Het 1 OC 1-4烷基，Het 2 C 1-4烷基，Het 2 OC 1-4烷基，芳基C 1-4烷基，芳基OC 1-4烷基或氨基C 1-4烷基; 其中R6的定义中的每个氨基可任选被取代; R5和_A-R6与它们所连接的氮原子一起也可以形成Het1或Het2，R12，是H，-NH2，_NR5AR6，C1-6烷基或烷基-W-R14，其中所述烷基任选被取代卤素，羟基，芳基，杂芳基，Het1，Het2或氨基，其中所述氨基任选被C 1-4烷基单取代或二取代，R 13为H，任选被芳基，Het1，Het2，羟基，卤素，氨基，其中氨基可以任选被C 1-4烷基单取代或二取代。

16. 发明申请

WO2002083657A2 BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOTHIAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 审中-公开
标题翻译： BROADSPECTRUM 2-（取代氨基） - 苯并噻唑磺酰胺HIV蛋白酶抑制剂
公开(公告)号：WO2002083657A2
公开(公告)日：2002-10-24
申请号：PCT/EP2002/001788
申请日：2002-02-14
申请人： TIBOTEC PHARMACEUTICALS LTD. , SURLERAUX, Dominique, Louis, Nestor, Ghislain , WIGERINCK, Piet, Tom, Bert, Paul , GETMAN, Daniel , VERSCHUEREN, Wim, Gaston , VENDEVILLE, Sandrine , DE BETHUNE, Marie-Pierre , DE KERPEL, Jan, Octaaf, Antoon , MOORS, Samuel, Leo, Christiaan , DE KOCK, Herman, Augustinus , VOETS, Marieke, Christiane, Johanna
发明人： SURLERAUX, Dominique, Louis, Nestor, Ghislain , WIGERINCK, Piet, Tom, Bert, Paul , GETMAN, Daniel , VERSCHUEREN, Wim, Gaston , VENDEVILLE, Sandrine , DE BETHUNE, Marie-Pierre , DE KERPEL, Jan, Octaaf, Antoon , MOORS, Samuel, Leo, Christiaan , DE KOCK, Herman, Augustinus , VOETS, Marieke, Christiane, Johanna
IPC分类号： C07D277/82
CPC分类号： C07D417/12 , C07D277/82
摘要： The present invention concerns the compounds having the formula (I), N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R 1 and R 8 each are H, optionally substituted C 1-6 alkyl, C 2 -6alkenyl, C 3-7 cycloalkyl, aryl, Het 1 , Het 2 ; R 1 may also be a radical of formula (R 11a R 11b )NC(R 10aR10b )CR 9- ; t is 0, 1 or 2; R 2 is H or C 1-6 alkyl; L is -C(=O)-, -O-C(=O)-, -NR 8 -C(=O)-, -O-C 1-6 alkanediyl-C(=O)-, -NR 8 -C 1 -6?alkanediyl-C(=O)-, -S(=O)2-, -O-S(=O) 2- , -NR8-S(=O) 2 ; R3 is C 1-6 alkyl, aryl, C 3-7 cycloalkyl, C 3-7 cycloalkylC 1-4 alkyl, or arylC 1-4 alkyl; R 4 is H, C 1-4 alkylOC(=O), carboxyl, aminoC(=O), mono- or di(C 1-4 alkyl)aminoC(=O), C 3-7 cycloalkyl, C 2-6 alkenyl, C 2-6 alkynyl or optionally substituted C 1-6 alkyl; A is C 1-6 alkanediyl, -C(=O)-, -C(=S)-, -S(=O) 2- , C 1-6 alkanediyl-C(=O)-, C 1-6 alkanediyl-C(=S)- or C 1-6 alkanediyl-S(=O) 2- ; R 5 is H, OH, C 1-6 alkyl, Het 1 C 1-6 alkyl, Het 2 C 1-6 alkyl, optionally substituted aminoC 1-6 alkyl; R 6 is C 1-6 alkylO, Het 1 , Het 1O , Het 2 , Het 2 O, aryl, arylO, C 1-6 alkyloxycarbonylamino or amino; and in case -A- is other than C 1-6 alkanediyl then R 6 may also be C 1-6 alkyl, Het 1 C 1-4 alkyl, Het 1 OC 1-4 alkyl, Het 2 C 1-4 alkyl, Het 2 OC 1-4 alkyl, arylC 1-4 alkyl, arylOC 1-4 alkyl or aminoC 1-4 alkyl; whereby each of the amino groups in the definition of R 6 may optionally be substituted; R 5 and -A-R 6 taken together with the nitrogen atom to which they are attached may also form Het 1 or Het 2 . It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.
摘要翻译：本发明涉及具有式（I），N-氧化物，盐，立体异构体形式，外消旋混合物，前药，酯和代谢物的化合物，其中R 1>和R 8各自为H，任选取代的C> 1-6烷基，C 2 < - 6烯基，C 3-7环烷基，芳基，Het 1，Het 2， R1也可以是式（R11aR11b）NC（R10aR10b）CR9-的基团; t为0,1或2; R2是H或C1-6烷基; L是-C（= O） - ， - OC（= O） - ， - NR 8 -C（= O） - ， - O-C 1-6烷二基-C（= O） - ， - NR 8 -C 1-6烷基 -C（= O） - ， - S（= O）2 - ， - O（O）2 - ， - NR 8 -S（= O） R 3是C 1-6烷基，芳基，C 3-7环烷基，C 3-7环烷基C 1-4 - 烷基或芳基C 1-4 - 烷基; R 4是H，C 1-4，烷基OC（= O），羧基，氨基C（= O），单或二（C 1-4）烷基氨基C（= O） 7 <环烷基，C 2-6>烯基，C 2-6炔基或任选取代的C 1-6烷基; A是C 1-6烷基，-C（= O） - ， - C（= S） - ， - S（= O）2 2-，C 1-6烷基-C（= O） - ，C> 1-6 <烷二基-C（= S） - 或C 1-6>烷二基-S（= O）2 - R 5是H，OH，C 1-6烷基，Het 1 C 1-6烷基，Het 2 C 1-6烷基，任选取代的氨基C 1-6烷基; R 6是C 1-6烷基O，Het 1，Het 10，Het 2，Het 2 O，芳基，芳基O，C 1-6烷氧基羰基氨基或氨基; 并且在-A-不是C 1-6烷二基的情况下，则R 6也可以是C 1-6烷基，Het 1 C 1-4烷基，Het 1 OC 1-4烷基，Het 2 C 1-4烷基， C 1-4烷基，芳基C 1-4烷基，芳基OC 1-4烷基或氨基C 1-4烷基; 其中R 6定义中的每个氨基可以任选被取代; R 5和-A-R 6与它们所连接的氮原子一起也可以形成Het 1或Het 2。它还涉及它们作为广谱的HIV蛋白酶抑制剂，其制备方法以及药物组合物和包含它们的诊断试剂盒的用途。它还涉及与另一种抗逆转录病毒剂的组合，以及它们在测定中用作参考化合物或作为试剂。

17. 发明申请

WO2008037784A1 QUINOLINONE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：WO2008037784A1
公开(公告)日：2008-04-03
申请号：PCT/EP2007/060289
申请日：2007-09-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , KESTELEYN, Bart Rudolf Romanie , SURLERAUX, Dominique Louis Nestor Ghislain , HACHÉ, Geerwin Yvonne Paul
发明人： KESTELEYN, Bart Rudolf Romanie , SURLERAUX, Dominique Louis Nestor Ghislain , HACHÉ, Geerwin Yvonne Paul
IPC分类号： C07D215/54 , C07D401/04 , C07D401/12 , A61K31/4741 , A61K31/4704 , A61K31/4709 , A61K31/436 , A61K31/4375 , A61P31/00 , C07D221/12 , C07D413/04 , C07D409/04 , C07D417/04
CPC分类号： C07D215/54 , C07D221/12 , C07D401/04 , C07D401/12 , C07D409/04 , C07D413/04 , C07D417/04 , C07F9/60 , C07F9/65685
摘要： HIV inhibitory compounds of formula (I) including the stereoisomeric forms thereof, the pharmaceutically acceptable salts, and pharmaceutically acceptable solvates thereof; wherein R 1 is cyano; R 2 is H, C 1-6 alkyl, trifluoromethyl, amino, mono- or di-C 1-6 alkylamino, C 1-6 alkylamino wherein the C 1-6 alkyl group can be substituted; X 1 is CH or N; R 3 is phenyl or pyridyl, each unsubstituted or substituted; R 4 is H, C 1-6 alkyl, (C 1-6 alkylcarbonyla mino)C 1-6 alkyl-, Ar, potionally substituted thienyl, furanyl, pyridyl, pyrimidyl, pyrazinyl, pyrrolyl, pyrazolyl, imidazolyl, triazo lyl, oxazolyl, thiazolyl, halo, trifluoromethyl, hydroxy, C 1-6 alkyloxy, -OPO(OH) 2 , amino, aminocarbonyl, cyano, -Y 1 -R 6 , -Y 1 -Alk-R 6 , or -Y 1 -Alk-Y 2 -R 7 ; R 5 is H, halo, hydroxy or C 1-6 alkyloxy; or R 4 and R 5 form -O-CH 2 -O-; Y 1 is O or NR 8 ; Y 2 is O or NR 9 ; Alk is bivalent C 1-6 alkyl; R 6 is pyrrolidinyl, piperidinyl, morpho linyl, piperazinyl, 4-C 1 -6 alkylpiperazinyl, 4-(C 1-6 alkylcarbonyl)piperazinyl, pyridyl, or imidazolyl; R 7 is H, C 1-6 alkyl, hydroxyC 1 -6 alkyl, C 1 -6 alkylcarbonyl; R 8 and R 9 are H or C 1-6 alkyl; Ar is optionally substituted phenyl; pharmaceut ical compositions comprising the above compounds (I) as active ingredient.
摘要翻译：包括其立体异构形式的式（I）的HIV抑制化合物，其药学上可接受的盐和药学上可接受的溶剂合物; 其中R 1是氰基; R 2是H，C 1-6烷基，三氟甲基，氨基，一或二-C 1-6烷基氨基，C _{C 1-6烷基氨基，其中C 1-6烷基可以被取代; X 1是CH或N; R 3是苯基或吡啶基，各自是未取代或取代的; R 4是H，C 1-6烷基，（C 1-6烷基羰基氨基）C 1-6 吡唑基，吡唑基，吡唑基，咪唑基，三唑基，恶唑基，噻唑基，卤素，三氟甲基，羟基，C 1-6烷基氧基， -OPO（OH）2，氨基，氨基羰基，氰基，-Y-1-R 6，-Y 1 O / > -Alk-R 6或-Y 1 -Alk-Y 2 -R 7; R 5是H，卤素，羟基或C 1-6烷氧基; 或R 4和R 5形式-O-CH 2 -O-; Y 1是O或NR 8; Y 2是O或NR 9; Alk是二价C 1-6烷基; R 6是吡咯烷基，哌啶基，吗啉基，哌嗪基，4-C 1-16烷基哌嗪基，4-（C 1-6烷基羰基）哌嗪基，吡啶基或咪唑基; R 7是H，C 1-6烷基，羟基C 1-6烷基，C 1〜}

18. 发明申请

WO2007060249A1 AMINOPHENYLSULFONAMIDE DERIVATIVES AS HIV PROTEASE INHIBITOR 审中-公开
标题翻译：氨基酚磺酰胺衍生物作为HIV蛋白酶抑制剂
公开(公告)号：WO2007060249A1
公开(公告)日：2007-05-31
申请号：PCT/EP2006/068983
申请日：2006-11-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , DE KOCK, Herman Augustinus , JONCKERS, Tim Hugo Maria , LAST, Stefaan Julien , BOONANTS, Paul Jozef Gabriel Maria , SURLERAUX, Dominique Louis Nestor Ghislain , WIGERINCK, Piet Tom Bert Paul
发明人： DE KOCK, Herman Augustinus , JONCKERS, Tim Hugo Maria , LAST, Stefaan Julien , BOONANTS, Paul Jozef Gabriel Maria , SURLERAUX, Dominique Louis Nestor Ghislain , WIGERINCK, Piet Tom Bert Paul
IPC分类号： C07D401/04 , A61K31/34 , A61P31/18
CPC分类号： C07D493/04
摘要： The present invention concerns substituted aminophenylsulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present substituted aminophenylsulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.
摘要翻译：本发明涉及取代的氨基苯基磺酰胺化合物及其衍生物，它们作为蛋白酶抑制剂的用途，特别是作为广谱的HIV蛋白酶抑制剂，其制备方法以及包含它们的药物组合物和诊断试剂盒。本发明还涉及本发明的取代氨基苯基磺酰胺化合物和其衍生物与另一种抗逆转录病毒剂的组合。它还涉及它们在测定中作为参考化合物或作为试剂的用途。

19. 发明申请

WO2007014926A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译： HEPATITIS C病毒的大环境抑制剂
公开(公告)号：WO2007014926A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064820
申请日：2006-07-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , HU, Lili , VENDEVILLE, Sandrine Marie Helene , TAHRI, Abdellah , SURLERAUX, Dominique Louis Nestor Ghislain , SIMMEN, Kenneth Alan , NILSSON, Karl Magnus , SAMUELSSON, Bengt Bertil , ROSENQUIST, Åsa Annica Kristina , IVANOV, Vladimir , PELCMAN, Michael , BELFRAGE, Anna Karin Gertrud Linnea , JOHANSSON, Per-Ola Mikael
发明人： RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , HU, Lili , VENDEVILLE, Sandrine Marie Helene , TAHRI, Abdellah , SURLERAUX, Dominique Louis Nestor Ghislain , SIMMEN, Kenneth Alan , NILSSON, Karl Magnus , SAMUELSSON, Bengt Bertil , ROSENQUIST, Åsa Annica Kristina , IVANOV, Vladimir , PELCMAN, Michael , BELFRAGE, Anna Karin Gertrud Linnea , JOHANSSON, Per-Ola Mikael
IPC分类号： C07D487/04 , C07D245/04 , C07K5/078 , A61K38/05 , A61K31/33 , A61P31/14 , C07K5/06
CPC分类号： C07D487/04 , A61K31/427 , A61K31/4709 , A61K31/7056 , A61K38/05 , A61K38/212 , A61K45/06 , A61K47/60 , C07D245/04 , C07D277/56 , C07D401/14 , C07D417/04 , C07D417/14 , C07K5/06139 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/393
摘要： Inhibitors of HCV replication of formula (I) and the N -oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R 1 is -OR 7 , -NH-SO 2 R 8 ; R 2 is hydrogen, and where X is C or CH, R 2 may also be C 1-6 alkyl; R 3 is hydrogen, C 1-6 alkyl, C 1-6 alkoxyC 1-6 alkyl, C 3-7 cycloalkyl; R 4 is aryl or Het; n is 3, 4, 5, or 6; R 5 is halo, C 1-6 alkyl, hydroxy, C 1-6 alkoxy, phenyl, or Het; R 6 is C 1-6 alkoxy, or dimethylamino; R 7 is hydrogen; aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het; R 8 is aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three substituents ; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
摘要翻译：式（I）的HCV复制抑制剂和N-氧化物，盐和立体异构体，其中每个虚线表示任选的双键; X为N，CH，X为双键，C为C; R 1是-OR 7，-NH-SO 2 R 8; R 2是氢，并且其中X是C或CH，R 2也可以是C 1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基，C _{3-7 环烷基; R 4是芳基或Het; n为3,4,5或6; R 5为卤素，C 1-6烷基，羟基，C 1-6烷氧基，苯基或Het; R 6是C 1-6烷氧基或二甲基氨基; R 7是氢; 芳基; HET; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; R 8是芳基; HET; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; 芳基是任选被一个，两个或三个取代基取代的苯基; Het是含有1至4个选自氮，氧和硫的杂原子并且任选地被一个，两个或三个取代基取代的5或6元饱和，部分不饱和或完全不饱和的杂环。含有化合物（I）的药物组合物和制备化合物（I）的方法。还提供了式（I）的HCV抑制剂与利托那韦的生物可利用组合。}

20. 发明申请

WO2006120252A3 PYRIDO[2,3-D]PYRIMIDINES USEFUL AS HCV INHIBITORS, AND METHODS FOR THE PREPARATION THEREOF 审中-公开
公开(公告)号：WO2006120252A3
公开(公告)日：2006-11-16
申请号：PCT/EP2006/062290
申请日：2006-05-12
申请人： TIBOTEC PHARMACEUTICALS LTD. , SIMMEN, Kenneth Alan , SURLERAUX, Dominique Louis Nestor Ghislain , LIN, Tse-I , LENZ, Oliver , RABOISSON, Pierre Jean-Marie Bernard
发明人： SIMMEN, Kenneth Alan , SURLERAUX, Dominique Louis Nestor Ghislain , LIN, Tse-I , LENZ, Oliver , RABOISSON, Pierre Jean-Marie Bernard
IPC分类号： C07D471/04 , A61K31/519 , A61P31/14
摘要： The present invention relates to the use of pyrido[2,3-d]pyrimidines as inhibitors of 10 HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to pyrido- [2,3-d]pyrimidines co mpounds per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceut ical compositions co mprising them, and combinations of said compounds 15 with other anti-HCV agents.

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