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1. 发明申请

WO2008119773A1 AMIDE DERIVATIVES AS INHIBITORS OF ASPARTYL PROTEASES 审中-公开
标题翻译：作为ASPARTYL蛋白抑制剂的酰胺衍生物
公开(公告)号：WO2008119773A1
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053767
申请日：2008-03-28
申请人： MEDIVIR AB , KVARNSTRÖM, Ingemar , BÄCK, Marcus , SANDGREN, Veronica , OSCARSON, Stefan , BJÖRKLUND, Catarina , ROSENQUIST, Åsa , SAMUELSSON, Bertil , JOHANSSON, Per-Ola , DORANGE, Ismet
发明人： KVARNSTRÖM, Ingemar , BÄCK, Marcus , SANDGREN, Veronica , OSCARSON, Stefan , BJÖRKLUND, Catarina , ROSENQUIST, Åsa , SAMUELSSON, Bertil , JOHANSSON, Per-Ola , DORANGE, Ismet
IPC分类号： C07C311/07 , C07C311/08 , C07C237/22 , C07D207/26 , C07D213/56 , A61K31/18 , A61K31/16 , A61P25/28
CPC分类号： C07C311/08 , C07C237/22 , C07C311/07 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/26 , C07D213/56
摘要： The invention provides compounds of the formula (I). N-oxides, addition salts, quaternary amines, metal complexes, stereochemically isomeric forms and metabolites thereof, wherein W is H,C 1-C 6 alkyl, C 3-C 6 cycloalkyl, aryl or heterocyclyl; Q is aryl or heterocyclyl; A is a five or six membered saturated, partially unsaturated or aromatic ring; D is (II) or (III) the other variables are as defined in the specification. The compounds of the invention are inhibitors of BACE and are among other things useful for the treatment and/or prevention of conditions associated with BACE activity such as Alzheimer's disease.
摘要翻译：本发明提供式（I）化合物。 N-氧化物，加成盐，季胺，金属络合物，立体化学异构形式及其代谢物，其中W是H，C 1 -C 6烷基，C 3 -C 6环烷基，芳基或杂环基; Q是芳基或杂环基; A是五或六元饱和，部分不饱和或芳环; D是（II）或（III）其他变量如说明书中所定义。本发明的化合物是BACE的抑制剂，并且可用于治疗和/或预防与BACE活性相关的病症如阿尔茨海默氏病。

2. 发明申请

WO2008135488A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2008135488A1
公开(公告)日：2008-11-13
申请号：PCT/EP2008/055326
申请日：2008-04-30
申请人： MEDIVIR AB , BJÖRKLUND, Catarina , KVARNSTRÖM, Ingemar , AYESA, Susana , JOHANSSON, Per-Ola , DORANGE, Ismet , ERSMARK, Karolina , SAMUELSSON, Bertil , ROSENQUIST, Åsa
发明人： BJÖRKLUND, Catarina , KVARNSTRÖM, Ingemar , AYESA, Susana , JOHANSSON, Per-Ola , DORANGE, Ismet , ERSMARK, Karolina , SAMUELSSON, Bertil , ROSENQUIST, Åsa
IPC分类号： C07D267/00 , C07D313/00 , A61P25/28 , A61K31/365
CPC分类号： C07D313/00 , C07D267/00
摘要： The invention provides compounds of the formula (I) N-oxides, addition salts, quaternary amines, metal complexes, stereochemically isomeric forms and metabolites thereof, wherein G is-O-, -S(=O) r -, -CRdRd or -NRa-; W is H, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, aryl or heterocyclyl; L 1 is a bond, methyleneor ethylene; L 2 is CHR 1 ;or L 1 and L 2 together form CH=CH; L 3 is a bond, C(=O) or CH 2 ; V 1 and V 2 are independently a bond, NRa, CRdRd or O; R 1 is H, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 4 alkoxyC 1 -C 4 alkyl, C 1 -C 4 alkoxyC 1 -C 4 alkoxyC 1 -C 4 alkyl, C 0 -C 3 alkandiylcarbocyclyl or C 0 -C 3 alkandiylheterocyclyl; R 2b are both H, or the two R 2b together form=O; ring A is a five or six membered saturated, partially unsaturated or aromatic ring; and the other variables are as defined in the specification. The compounds of the invention are inhibitors of BACE and are among other things useful for the treatment and/or prevention of conditions associated with BACE activity such as Alzheimer´s disease.
摘要翻译：本发明提供式（I）的化合物N-氧化物，加成盐，季胺，金属配合物，立体化学异构形式及其代谢物，其中G是-O-，-S（= O） > - ，-CRdRd或-NRa-; W是H，C 1 -C 6烷基，C 3 -C 6 -C 6环烷基，芳基或杂环基; L 1是键，亚甲基或亚乙基; L 2是CHR 1或L 1和L 2一起形成CH = CH; L 3是一个键，C（= O）或CH 2; V 1和V 2独立地是键，NR a，CR d R d或O; R 1是H，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，烷氧基，C 1 -C 4烷氧基C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基， / SUB> -C _{4 烷氧基C _{1 -C _{4 烷氧基C _{1 -C ₄}}}}

3. 发明申请

WO2010042030A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2010042030A1
公开(公告)日：2010-04-15
申请号：PCT/SE2009/051105
申请日：2009-10-05
申请人： MEDIVIR AB , LUNDBERG, Stina , AYESA, Susana , BELDA, Oscar , DORANGE, Ismet , ERSMARK, Karolina , HAMMER, Kristin , JOHANSSON, Per-Ola , LINDSTRÖM, Stefan , ROSENQUIST, Åsa , SAMUELSSON, Bertil , BÄCK, Marcus , KVARNSTRÖM, Ingemar , WÅNGSELL, Fredrik , BJÖRKLUND, Katarina
发明人： LUNDBERG, Stina , AYESA, Susana , BELDA, Oscar , DORANGE, Ismet , ERSMARK, Karolina , HAMMER, Kristin , JOHANSSON, Per-Ola , LINDSTRÖM, Stefan , ROSENQUIST, Åsa , SAMUELSSON, Bertil , BÄCK, Marcus , KVARNSTRÖM, Ingemar , WÅNGSELL, Fredrik , BJÖRKLUND, Katarina
IPC分类号： C07D213/75 , A61K31/195 , A61K31/455 , A61P25/28 , C07C229/38 , C07D207/26 , C07D263/20 , C07D279/02 , C07D285/06
CPC分类号： C07D213/81 , C07C233/78 , C07C237/34 , C07C309/66 , C07C311/08 , C07C311/16 , C07D207/27 , C07D263/22 , C07D277/28 , C07D279/02 , C07D285/10 , C07D295/26 , C07D401/12 , C07D417/12
摘要： A compound of formula (I): N-oxides, addition salts, quaternary amines metal complexes stereochemically isomeric forms and metabolites thereof, wherein A is CR 1 or N; D is H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or Q is C 2 -C 6 alkenyl, C 2 -Cealkynyl, aryl or heterocyclyl; W is H, Ci-Cealkyl, C 2 -C 6 alkenyl, haloC 1 -C 3 alkyl, hydroxyC 1 -C 3 alkyl, C 3 -C 6 Cy cloalkyl, aryl or heterocyclyl; one of X' and X" is H or CH 3 , the other is C 1 -C 3 alkyl, F, OH, NRaRb, CF 3 or N 3 ; or X' and X" are both F; Y is a bond, CH 2 , NRa, O, CH 2 CH 2 , CH 2 NRa, CH 2 O or S(=O) r ; Z is O, S(=O) r or NRa; the other variables are as defined in the specification. The compounds of the invention are inhibitors of BACE and are among other things useful for the treatment and/or prevention of conditions associated with BACE activity such as Alzheimer's disease.
摘要翻译：式（I）的化合物：N-氧化物，加成盐，季胺金属络合物立体化学异构形式及其代谢物，其中A是CR 1或N; D是H，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或Q是C 2 -C 6烯基，C 2 -C 6炔基，芳基或杂环基; W是H，C 1 -C 6烷基，C 2 -C 6烯基，卤代C 1 -C 3烷基，羟基C 1 -C 3烷基，C 3 -C 6环烷基，芳基或杂环基; X'和X“之一是H或CH3，另一个是C 1 -C 3烷基，F，OH，NR a R b，CF 3或N 3;或X'和X”均为F; Y是键，CH2，NRa，O，CH2CH2，CH2NRa，CH2O或S（= O）r; Z是O，S（= O）r或NR a; 其他变量如规范中所定义。本发明的化合物是BACE的抑制剂，并且可用于治疗和/或预防与BACE活性相关的病症如阿尔茨海默氏病。

4. 发明申请

WO2010107384A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2010107384A1
公开(公告)日：2010-09-23
申请号：PCT/SE2010/050307
申请日：2010-03-19
申请人： MEDIVIR AB , AYESA, Susana , BELDA, Oscar , DORANGE, Ismet , ERSMARK, Karolina , JOHANSSON, Per-Ola , LUNDGREN, Stina , ROSENQUIST, Åsa , SAMUELSSON, Bertil , WIKTELIUS, Daniel , WÄHLING, Horst
发明人： AYESA, Susana , BELDA, Oscar , DORANGE, Ismet , ERSMARK, Karolina , JOHANSSON, Per-Ola , LUNDGREN, Stina , ROSENQUIST, Åsa , SAMUELSSON, Bertil , WIKTELIUS, Daniel , WÄHLING, Horst
IPC分类号： C07D213/81 , A61K31/166 , A61K31/18 , A61K31/402 , A61K31/426 , A61K31/44 , A61K31/4439 , A61K31/444 , A61P25/28 , C07C237/34 , C07C311/08 , C07D207/08 , C07D277/28 , C07D401/06 , C07D417/12
CPC分类号： C07C311/08 , C07C237/34 , C07C2601/02 , C07C2601/04 , C07D207/08 , C07D213/81 , C07D277/28 , C07D401/06 , C07D417/12
摘要： A compound of formula (I) N-oxides, addition salts, quaternary amines metal complexes stereochemically isomeric forms and metabolites thereof, wherein A is CR 1 Or N; formula (A) or formula (B) D is H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, G is NR 10 or O Q is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 Cycloalkyl, aryl or heterocyclyl; W is H, C 1 -C 6 alkyl, C 3 -C 6 Cycloalkyl, CH 2 F, CHF 2 or CF 3 ; one of X' and X" is H or CH 3 , the other is C 1 -C 3 alkyl, F, OH, NRaRb, CF 3 or N 3 ; or X' and X" are both F; Y is NRd or O; Z is O, NRa, CHRd, CF 2 or S(=0)r or a bond; the other variables are as defined in the specification. The compounds of the invention are inhibitors of BACE and are among other things useful for the treatment and/or prevention of conditions associated with BACE activity such as Alzheimer's disease.
摘要翻译：式（I）的化合物N-氧化物，加成盐，季胺金属络合物立体化学异构形式及其代谢物，其中A是CR 1或N; 式（A）或式（B）D是H，C1-C6烷基，C2-C6链烯基，C2-C6炔基，G是NR10或OQ是C1-C6烷基，C2-C6链烯基，C2-C6炔基，C3-C6环烷基，芳基或杂环基 ; W是H，C 1 -C 6烷基，C 3 -C 6环烷基，CH 2 F，CHF 2或CF 3; X'和X“之一是H或CH3，另一个是C 1 -C 3烷基，F，OH，NR a R b，CF 3或N 3;或X'和X”均为F; Y为NRd或O; Z是O，NR a，CHR d，CF 2或S（= O）r或键; 其他变量如规范中所定义。本发明的化合物是BACE的抑制剂，并且可用于治疗和/或预防与BACE活性相关的病症如阿尔茨海默氏病。

5. 发明申请

WO2007014921A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒大肠杆菌抑制剂
公开(公告)号：WO2007014921A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064815
申请日：2006-07-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , DORANGE, Ismet , VENDEVILLE, Sandrine Marie Helene , SURLERAUX, Dominique Louis Nestor Ghislain , TAHRI, Abdellah , SIMONNET, Yvan , VAN DE VREKEN, Wim , HU, Lili , SIMMEN, Kenneth Alan , NILSSON, Karl Magnus , SAMUELSSON, Bengt Bertil , ROSENQUIST, Åsa Annica Kristina , WALLBERG, Hans Kristian
发明人： RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , DORANGE, Ismet , VENDEVILLE, Sandrine Marie Helene , SURLERAUX, Dominique Louis Nestor Ghislain , TAHRI, Abdellah , SIMONNET, Yvan , VAN DE VREKEN, Wim , HU, Lili , SIMMEN, Kenneth Alan , NILSSON, Karl Magnus , SAMUELSSON, Bengt Bertil , ROSENQUIST, Åsa Annica Kristina , WALLBERG, Hans Kristian
IPC分类号： C07D401/14 , C07K5/078 , A61K31/4725 , A61P31/14
CPC分类号： C07D401/14 , C07D401/12 , C07D417/14 , C07D487/04 , C07K5/06191
摘要： Inhibitors of HCV replication of formula (I) and the N -oxides, salts, and stereoisomers thereof, wherein X is N, CH and where X bears a double bond it is C; R 1 is -OR 5 , -NH-SO 2 R 6 ; 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, or C 3-7 cycloalkyl; R 4 is isoquinolinyl optionally substituted with one, two or three substituents each independently selected from C 1-6 alkyl, C 1-6 alkoxy, hydroxy, halo, polyhalo- C 1-6 alkyl, polyhaloC 1-6 alkoxy, amino, mono- or diC 1-6 alkylamino, mono- or DiC 1-6 alkylaminocarbonyl, C 1-6 alkylcarbonyl-amino, aryl, and Het; n is 3, 4, 5, or 6; each dashed line (represented by ) represents an optional double bond; R 5 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 6 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; each aryl is phenyl optionally substituted with one, two or three substituents; and each Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently 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复制抑制剂及其N-氧化物，盐和立体异构体，其中X为N，CH，X为双键时为C; R 1是-OR 5，-NH-SO 2 R 6; 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，或 ç_{3-7 环烷基; R 4是任选地被一个，两个或三个独立地选自C 1-6烷基，C 1-6 - 烷氧基，羟基，卤素，多卤代-C 1-6烷基，多卤C 1-6烷氧基，氨基，单或二C 1-6烷基氨基，单或二C 1-6烷基氨基羰基，C 1-6烷基羰基 - 氨基，芳基和Het; n为3,4,5或6; 每个虚线（代表）表示任选的双键; R 5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 6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; 每个芳基是任选被一个，两个或三个取代基取代的苯基; 并且每个Het是含有1至4个各自独立地选自氮，氧和硫的杂原子的5或6元饱和，部分不饱和或完全不饱和的杂环，并且任选地被一个，两个或三个取代基取代; 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。}

6. 发明申请

WO2008068272A2 ANTIBACTERIAL QUINOLINE DERIVATIVES 审中-公开
标题翻译：抗生素喹啉衍生物
公开(公告)号：WO2008068272A2
公开(公告)日：2008-06-12
申请号：PCT/EP2007/063319
申请日：2007-12-04
申请人： JANSSEN PHARMACEUTICA N.V. , GUILLEMONT, Jérôme, Emile, Georges , DORANGE, Ismet , LANÇOIS, David, Francis, Alain , VILLALGORDO-SOTO, José, Manuel , SIMONNET, Yvan, René, Ferdinand , MOTTE, Magali, Madeleine, Simone , ANDRIES, Koenraad, Jozef, Lodewijk, Marcel , KOUL, Anil
发明人： GUILLEMONT, Jérôme, Emile, Georges , DORANGE, Ismet , LANÇOIS, David, Francis, Alain , VILLALGORDO-SOTO, José, Manuel , SIMONNET, Yvan, René, Ferdinand , MOTTE, Magali, Madeleine, Simone , ANDRIES, Koenraad, Jozef, Lodewijk, Marcel , KOUL, Anil
IPC分类号： C07D215/22 , C07D401/12 , C07D487/08 , A61K31/47 , C07D401/14 , C07D417/06
CPC分类号： C07D401/06 , C07D215/227 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D417/06 , C07D487/08
摘要： The present invention relates to novel subst ituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a pharmaceutically acceptable salt thereof, a N -oxide form thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or composit ions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
摘要翻译：本发明涉及根据通式（Ia）或式（Ib）的新的取代的喹啉衍生物：包括其任何立体化学异构形式，其药学上可接受的盐，其N-氧化物形式或其溶剂合物。所要求保护的化合物可用于治疗细菌感染。还要求保护的是包含药学上可接受的载体和作为活性成分的治疗有效量的所要求保护的化合物的组合物，所要求保护的化合物或复合离子在制备用于治疗细菌感染和方法的药物中的用途用于制备所要求保护的化合物。

7. 发明申请

WO2008068267A1 ANTIBACTERIAL QUINOLINE DERIVATIVES 审中-公开
标题翻译：抗菌喹啉衍生物
公开(公告)号：WO2008068267A1
公开(公告)日：2008-06-12
申请号：PCT/EP2007/063313
申请日：2007-12-04
申请人： JANSSEN PHARMACEUTICA N.V. , GUILLEMONT, Jérôme, Emile, Georges , LANÇOIS, David, Francis, Alain , DORANGE, Ismet , ANDRIES, Koenraad, Jozef, Lodewijk, Marcel , KOUL, Anil
发明人： GUILLEMONT, Jérôme, Emile, Georges , LANÇOIS, David, Francis, Alain , DORANGE, Ismet , ANDRIES, Koenraad, Jozef, Lodewijk, Marcel , KOUL, Anil
IPC分类号： C07D215/14 , C07D401/04 , C07D413/04 , C07D417/04 , A61K31/496 , A61P31/04
CPC分类号： C07D215/14 , C07D401/04 , C07D413/04 , C07D417/04
摘要： The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a N -oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or composit ions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
摘要翻译：本发明涉及根据通式（Ia）或式（Ib）的新型取代的喹啉衍生物：包括其任何立体化学异构形式，其N-氧化物，其药学上可接受的盐或其溶剂化物。要求保护的化合物可用于治疗细菌感染。还要求保护一种组合物，其包含药学上可接受的载体和作为活性成分的治疗有效量的要求保护的化合物，所要求保护的化合物或组合物在制备用于治疗细菌感染的药物中的用途和方法用于制备要求保护的化合物。

8. 发明申请

WO2007000435A1 QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：喹诺酮衍生物作为抗菌剂
公开(公告)号：WO2007000435A1
公开(公告)日：2007-01-04
申请号：PCT/EP2006/063553
申请日：2006-06-26
申请人： JANSSEN PHARMACEUTICA N.V. , ANDRIES, Koenraad, Jozef, Lodewijk, Marcel , KOUL, Anil , GUILLEMONT, Jérôme, Emile, Georges , LANÇOIS, David, Francis, Alain , MOTTE, Magali, Madeleine, Simone , DORANGE, Ismet , BACKX, Leo, Jacobus, Jozef , MEERPOEL, Lieven
发明人： ANDRIES, Koenraad, Jozef, Lodewijk, Marcel , KOUL, Anil , GUILLEMONT, Jérôme, Emile, Georges , LANÇOIS, David, Francis, Alain , MOTTE, Magali, Madeleine, Simone , DORANGE, Ismet , BACKX, Leo, Jacobus, Jozef , MEERPOEL, Lieven
IPC分类号： A61K31/47 , A61P31/04 , C07D215/22
CPC分类号： A61K31/47 , C07D215/227
摘要： Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N -oxide form thereof, wherein R 1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R 2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula ; R 3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 1, 2 or 3; R 4 and R 5 are hydrogen, alkyl or benzyl; or R 4 and R 5 together and including the N to which they are attached may form a ring; R 6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl ; or two vicinal R 6 radicals may be taken together to form a bivalent radical of formula - CH=CH-CH=CH-; r is 1, 2, 3, 4 or 5; R 7 is hydrogen, alkyl, Ar or Het; R 8 is hydrogen or alkyl; R 9 is oxo ; or R 8 and R 9 together form the radical -CH=CH-N=.
摘要翻译：使用化合物制造用于治疗细菌感染的药物，只要细菌感染不是分枝杆菌感染，所述化合物是式（Ia）或（Ib）的化合物，其药学上可接受的酸或碱加成其盐，其立体化学异构形式，其互变异构形式或其N-氧化物形式，其中R 1是氢，卤素，卤代烷基，氰基，羟基，Ar，Het，烷基，烷氧基，烷硫基，烷氧基烷基，烷硫基烷基，芳烷基或二（Ar）烷基; p为1,2,3或4; R 2是氢，羟基，巯基，烷氧基，烷氧基烷氧基，烷硫基，一或二（烷基）氨基或式的基团; R 3是烷基，Ar，Ar-烷基，Het或Het-烷基; q为1,2或3; R 4和R 5是氢，烷基或苄基; 或R 4和R 5一起并且包括它们所连接的N可以形成环; R 6是氢，卤素，卤代烷基，羟基，Ar，烷基，烷氧基，烷硫基，烷氧基烷基，烷硫基烷基，芳烷基或二（Ar）烷基; 或两个邻位R 6个基团可以一起形成式-CH = CH-CH = CH-的二价基团; r为1,2,3,4或5; R 7是氢，烷基，Ar或Het; R 8是氢或烷基; R 9是氧代; 或R 8和R 9一起形成基团-CH = CH-N =。

9. 发明申请

WO2006097534A1 1,3-DIHYDRO-BENZIMIDAZOL-2-YLIDENE AMINES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 审中-公开
标题翻译：作为呼吸道同种病毒复制的抑制剂的1,3-二氢苯并咪唑-2-基锂胺
公开(公告)号：WO2006097534A1
公开(公告)日：2006-09-21
申请号：PCT/EP2006/060852
申请日：2006-03-17
申请人： TIBOTEC PHARMACEUTICALS LTD , BONFANTI, Jean-François , FORTIN, Jérôme, Michel, Claude , DORANGE, Ismet
发明人： BONFANTI, Jean-François , FORTIN, Jérôme, Michel, Claude , DORANGE, Ismet
IPC分类号： C07D401/06 , C07D401/14 , A61K31/4184 , A61P11/00
CPC分类号： C07D401/06 , C07D235/30 , C07D401/14
摘要： Novel 1,3-dihydro-benzimidazo l-2-ylidene amine derivatives of formula (I) the addition salts and stereochemically iso meric forms wherein each Alk is C 1-6 alkanediyl; Q is hydrogen; C 1-6 alkyl subst ituted with one or two Ar 2 radicals; C 1-6 6alkyl subst ituted with quinolinyl, oxazolidinyl, thiazolidinyl, morpholinyl, thiomorpholinyl, or with pyrrolidinonyl; -CO-Ar 2 ; or Q is a radical of formula wherein t is 1, 2 or 3; R 4 is amino, mono-or di(C 1-6 alkyl)amino ; R 1 is Ar 2 , -CO-Ar 2 or a monocyclic or bicyclic heterocycle which may optionally be subst ituted; R 2 is as R 1 and additionally can be hydrogen; where Q is other than hydrogen, R 3 is hydrogen; and where Q is other than hydrogen, R 3 is a radical: (b) wherein R 6 is hydrogen, C 1-6 alkyl, substituted C 1-6 alkyl; R 7 , R 8 , R 9 are halo, cyano, C 1-6 alkyl, substituted C 1-6 alkyl, C 2-6 alkenyl, cyanoC 2-6 alkenyl, C 2-6 alkynyl, cyanoC 2 6 alkynyl, Ar1 1 , R 10a -O-, R 10a -S-, -N(R 5a R 5b ), R 10a -O-C(=O)-, N(R 5a R 5b )-C(=O)-, R 10a -C(=O)-NR 5b -, R 10b -C(=O)-O-; and R 8 and/or R 9 may also be hydrogen; which are RSV inhibitors. Compositions containing these compounds and processes for preparing these compounds and compositions.
摘要翻译：式（I）的新型1,3-二氢 - 苯并咪唑-1-基-2-亚基胺衍生物，其加成盐和立体化学异构体，其中每个Alk是C 1-6烷二基; Q是氢; 被一个或两个Ar 2基团取代的C 1-6烷基; 喹啉基，恶唑烷基，噻唑烷基，吗啉基，硫代吗啉基或与吡咯烷酮基反应的C 1-6-6烷基; -CO-的Ar ^{2 ; 或Q是式的基团，其中t是1,2或3; R 4是氨基，单 - 或二（C 1-6 - 烷基）氨基; R 1是Ar 2，-CO-Ar 2或可以任选被取代的单环或双环杂环; R 2是R 1，另外可以是氢; 其中Q不是氢，R 3是氢; 并且其中Q不是氢，R 3是自由基：（b）其中R 6是氢，C 1-6烷基，取代的C 1-6烷基; R 9，R 8，R 9是卤素，氰基，C 1-6烷基，取代的C 1 -C 6烷基， C 1-6亚烷基，C 2-6链烯基，氰基C 2-6烯基，C 2-6炔基，氰基C 2-6炔基，Ar 1，R 10a，-O-，R 10a，-S-， - N （R 5a，R 5b），R 10a -OC（= O） - ，N（R 5a）R 5 -C（= O） - ，R 10a -C（= O）-NR 5b， - R 10b， / SUP> C（= O）-O-; R 8和/或R 9也可以是氢; 其为RSV抑制剂。含有这些化合物的组合物和制备这些化合物和组合物的方法。}

10. 发明申请

WO2008068268A1 ANTIBACTERIAL QUINOLINE DERIVATIVES 审中-公开
标题翻译：抗生素喹啉衍生物
公开(公告)号：WO2008068268A1
公开(公告)日：2008-06-12
申请号：PCT/EP2007/063314
申请日：2007-12-04
申请人： JANSSEN PHARMACEUTICA N.V. , GUILLEMONT, Jérôme, Emile, Georges , DORANGE, Ismet , MOTTE, Magali, Madeleine, Simone , ANDRIES, Koenraad, Jozef, Lodewijk, Marcel , KOUL, Anil
发明人： GUILLEMONT, Jérôme, Emile, Georges , DORANGE, Ismet , MOTTE, Magali, Madeleine, Simone , ANDRIES, Koenraad, Jozef, Lodewijk, Marcel , KOUL, Anil
IPC分类号： C07D215/22 , C07D401/06 , C07D401/10 , C07D405/06 , C07D405/10 , C07D409/10 , A61K31/435 , A61P31/00
CPC分类号： C07D215/227 , C07D401/06 , C07D401/10 , C07D405/06 , C07D405/10 , C07D409/10
摘要： The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a N -oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or composit ions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
摘要翻译：本发明涉及根据通式（Ia）或式（Ib）的新的取代喹啉衍生物：包括其任何立体化学异构形式，其N-氧化物，其药学上可接受的盐或其溶剂合物。所要求保护的化合物可用于治疗细菌感染。还要求保护的是包含药学上可接受的载体和作为活性成分的治疗有效量的所要求保护的化合物的组合物，所要求保护的化合物或复合离子在制备用于治疗细菌感染和方法的药物中的用途用于制备所要求保护的化合物。

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