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1. 发明申请

WO2004005256A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2004005256A2
公开(公告)日：2004-01-15
申请号：PCT/EP2003/007127
申请日：2003-07-02
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , CARDULLO, Francesca , DI FABIO, Romano , GIOVANNINI, Riccardo , PIGA, Elisabetta , TRANQUILLINI, Maria, Elvira
发明人： ALVARO, Giuseppe , CARDULLO, Francesca , DI FABIO, Romano , GIOVANNINI, Riccardo , PIGA, Elisabetta , TRANQUILLINI, Maria, Elvira
IPC分类号： C07D211/34
CPC分类号： C07D211/34 , C07D211/64 , C07D223/04 , C07D223/06
摘要： The present invention relates to cyclic amine derivatives of formula(I) (I)whereinR represents halogen, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy;R1 represents hydrogen, halogen, C3-7cycloalkyl, hydroxy, nitro, cyano or C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy;R2 represents hydrogen or C1-4 alkyl;R3 and R4 independently represent hydrogen, cyano, C1-4 alkyl or R3 together with R4 represents C3-7 cycloalkyl;R5 represents trifluoromethyl, S(O)t C 1-4 alkyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy, halogen or cyano;R6 represents hydrogen or (CH2)rR7;R7 represents hydrogen, C3-7 cycloalkyl, NH(C1-4alkylOC1-4alkoxy), NH(C1-4alkyl), N(C1-4alkyl)2 , OC(O)NR9R8 , NR8C(O)R9 or C(O)NR9R8;R9 and R8 independently represent hydrogen, C1-4 alkyl or C3-7 cycloalkyl; m represents zero or an integer from 1 to 4;n represents 1 or 2;p is zero or an integer from 1 to 3;q is an integer from 1 to 3;r is an integer from 1 to 4;t is 0 , 1 or 2 ;provided that when m is 0, p is 2, q , r and n represent 1, R1, R2,R3, R4, R5 and R7 are hydrogen and R is chlorine, R5 is not iodine; and pharmaceutically acceptable salts and solvates thereof; process for their preparation and their use in the treatment of conditions mediated by tackykinins and/or by selective inhibition of serotonin reuptake transporter protein .
摘要翻译：本发明涉及式（I）（I）的环胺衍生物，其中R代表卤素，C 1-4烷基，氰基，C 1-4烷氧基，三氟甲基或三氟甲氧基; R 1代表氢，卤素，氰基或C1-4烷基; R2代表氢或C1-4烷基; R3和R4独立地代表氢，氰基，C1-4烷基或R3 与R 4一起代表C 3-7环烷基; R 5代表三氟甲基，S（O）t C 1-4烷基，C 1-4烷基，C 1-4烷氧基，三氟甲氧基，卤素或氰基; R 6代表氢或（CH 2）r R 7; R 7 （C 1-4烷基），N（C 1-4烷基）2，OC（O）NR 9 R 8，NR 8 C（O）R 9或C（O）NR 9 R 8; R9和R8独立地表示氢，C1-4烷基或C3-7环烷基; m表示0或1至4的整数; n表示1或2; p为0或1至3的整数; q为1至3的整数; r为1至4的整数; t为0， 1或2;条件是当m为0时，p为2，q，r和n表示1，R1，R2，R3，R4，R5和R7是氢并且R是氯，R5不是碘; 及其药学上可接受的盐和溶剂合物; 它们的制备方法以及它们在治疗由粘着激肽介导的病症和/或通过选择性抑制血清素再摄取转运蛋白中的用途。

2. 发明申请

WO2005049600A1 BETA-LACTAMS FOR TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：用于治疗CNS疾病的BETA-LACTAMS
公开(公告)号：WO2005049600A1
公开(公告)日：2005-06-02
申请号：PCT/EP2004/012772
申请日：2004-11-10
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , DI FABIO, Romano , GIOVANNINI, Riccardo , PAIO, Alfredo , TRANQUILLINI, Maria, Elvira , MATTIOLI, Lucia
发明人： ALVARO, Giuseppe , DI FABIO, Romano , GIOVANNINI, Riccardo , PAIO, Alfredo , TRANQUILLINI, Maria, Elvira , MATTIOLI, Lucia
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： The present invention relates to novel compounds of formula (I) wherein ---- represents a single or a double bond; R represents a radical selected from formulae i), ii), iii) and iv) in which R 1 is halogen, cyano, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethyl or trifluoromethoxy and p is zero or an integer from 1 to 3; R 2 represents hydrogen or C 1-4 alkyl; R 3 represents hydrogen, hydroxy or C 1-4 alkyl; R 4 represents hydrogen or R 4 together with R 3 represents =0 or =CH 2 ; R 5 represents phenyl, naphthyl, a 9 to 10 membered fused bicyclic heterocyclic group or a 5 or 6 membered heteroaryl group, wherein said groups are optionally substituted by 1 to 3 groups independently selected from trifluoromethyl, C 1-4 alkyl, hydroxy, cyano, C 1-4 alkoxy, trifluoromethoxy, halogen or S(O)qC 1-4 alkyl; R 6 and R 7 independently represent hydrogen, cyano, C 1-4 alkyl; R 8 is (CH 2 )rR 10 ; R 9 represents hydrogen, halogen, C 3-7 cycloalkyl, hydroxy, nitro, cyano or C 1-4 alkyl optionally substituted by one or two groups selected from halogen, cyano, hydroxy or C 1-4 alkoxy; R 10 represents hydrogen or C 3-7 cycloalkyl; n represents 1 or 2; q is 0, 1 or 2; r is 0 or an integer from 1 to 4; or a pharmaceutically acceptable salt or a solvate thereof, process for their preparation and their use in the treatment of conditions mediated by tackykinins and/or by selective inhibition of the serotonin reuptake transporter protein.
摘要翻译：本发明涉及式（I）的新化合物，其中----表示单键或双键; R表示选自式i），ii），iii）和iv）中的基团，其中R 1为卤素，氰基，C 1-4烷基，C 1-4烷氧基，三氟甲基或三氟甲氧基，p为0或1至3的整数 ; R2代表氢或C1-4烷基; R3表示氢，羟基或C1-4烷基; R4表示氢或R4，R3表示= 0或= CH2; R5表示苯基，萘基，9至10元稠合双环杂环基或5或6元杂芳基，其中所述基团任选被1至3个独立地选自三氟甲基，C 1-4烷基，羟基，氰基，C 1-4烷氧基，三氟甲氧基，卤素或S（O）qC 1-4烷基; R6和R7独立地表示氢，氰基，C1-4烷基; R8为（CH2）rR10; R9代表氢，卤素，C3-7环烷基，羟基，硝基，氰基或任选被一个或两个选自卤素，氰基，羟基或C 1-4烷氧基的基团取代的C 1-4烷基; R 10表示氢或C 3-7环烷基; n表示1或2; q是0,1或2; r为0或1至4的整数; 或其药学上可接受的盐或溶剂合物，其制备方法及其用于治疗由粘蛋白介导的病症和/或通过选择性抑制5-羟色胺再摄取转运蛋白。

3. 发明申请

WO2003066635A1 PIPERIDINE DERIVATIVES 审中-公开
标题翻译：哌啶衍生物
公开(公告)号：WO2003066635A1
公开(公告)日：2003-08-14
申请号：PCT/EP2003/001308
申请日：2003-02-10
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , DI FABIO, Romano , TRANQUILLINI, Maria, Elvira , SPADA, Simone
发明人： ALVARO, Giuseppe , DI FABIO, Romano , TRANQUILLINI, Maria, Elvira , SPADA, Simone
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/445
摘要： The present invention relates to piperidine derivatives of formula (I): R represents halogen or C 1-4 alkyl; R 1 represents C 1-4 alkyl; R 2 or R 3 independently represent hydrogen or C 1-4 alkyl; R 4 represents trifluoromethyl, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethoxy or halogen; R 5 represents hydrogen , C 1-4 alkyl or C 3-7 cycloalkyl; R 6 is hydrogen and R 7 is a radical of formula (W): R 6 is a radical of formula (W) and R 7 is hydrogen; X represents CH 2 , NR 5 or O; Y represents Nitrogen and Z is CH or Y represents CH and Z is Nitrogen; A represents C(O) or S(O)q, provided that when Y is nitrogen and Z is CH, A is not S(O)q; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; p and q are independently an integer from 1 to 2; and pharmaceutically acceptable salts and solvates thereof. The process for their preparation and their use in the treatment of condition mediated by tachykinins.
摘要翻译：本发明涉及式（I）的哌啶衍生物：R代表卤素或C 1-4烷基; R1表示C1-4烷基; R2或R3独立地表示氢或C1-4烷基; R 4表示三氟甲基，C 1-4烷基，C 1-4烷氧基，三氟甲氧基或卤素; R5代表氢，C1-4烷基或C3-7环烷基; R6是氢，R7是式（W）的基团：R6是式（W）的基团，R7是氢; X表示CH 2，NR 5或O; Y表示氮，Z表示CH或Y表示CH，Z表示氮; A表示C（O）或S（O）q，条件是当Y为氮且Z为CH时，A不为S（O）q; m为0或1〜3的整数; n为1〜3的整数， p和q独立地为1至2的整数; 及其药学上可接受的盐和溶剂化物。其制备方法及其用于治疗由速激肽介导的病症。

4. 发明申请

WO2003066589A1 PIPERIDYLCARBOXAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF TACHYKINIM-MEDIATED DISEASES 审中-公开
标题翻译：哌啶甲酰胺衍生物及其在治疗TACHYKINIM介导性疾病中的应用
公开(公告)号：WO2003066589A1
公开(公告)日：2003-08-14
申请号：PCT/GB2003/000499
申请日：2003-02-05
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , PAIO, Alfredo , PONTIROLI, Alessandro , SPADA, Simone , TRANQUILLINI, Maria, Elvira
发明人： ALVARO, Giuseppe , PAIO, Alfredo , PONTIROLI, Alessandro , SPADA, Simone , TRANQUILLINI, Maria, Elvira
IPC分类号： C07D211/58
CPC分类号： C07D401/04 , C07D211/58 , C07D405/12
摘要： The present invention relates to piperidine derivatives of formula (I) wherein R represents halogen or C 1-4 alkyl; R 1 represents hydrogen or C 1-4 alkyl; R 2 represents hydrogen , C 1-4 alkyl or R 2 together with R 3 represents C 3-7 cycloalkyl; R 3 represents hydrogen, C 1-4 alkyl, C 3-7 cycloalkyl or C 3-6 alkenyl; or R 1 and R 3 together with nitrogen and carbon atom to which they are attached respectively represent a 5 to 6 membered heterocyclic group; R 4 represents trifluoromethyl, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethoxy or halogen; R is hydrogen and R is NR 7 R 8 or R 5 is NR 8 R 9 and R 6 is hydrogen; R 7 represents hydrogen or C 1-4 alkyl or R 7 and R 8 together with nitrogen to which they are attached are a saturated 5 to 7 membered heterocyclic group containing oxygen; R 8 represents hydrogen, phenyl, C 3-7 cycloalkyl, (CH2)pC(O)NR 10 R 11 , a saturated 5 to 7 membered heterocyclic group containing 1 to 3 heteroatoms selected from oxygen, sulphur and nitrogen and optionally substituted by C 1-4 alkyl, S(O) 2 C 1-4 alkyl or C(O) C 1-4 alkyl, a 5 membered heteroaryl group containing 1 to 3 heteroatoms selected from oxygen, sulphur and nitrogen and optionally substituted by C 1-4 alkyl S(O) 2 C 1-4 alkyl or C(O) C 1-4 alkyl or R 8 represents a 6 membered heteroaryl group containing 1 to 3 nitrogen atoms and optionally substituted by C 1-4 alkyl, S(O) 2 C 1-4 alkyl or C(O) C 1-4 alkyl; or R 8 is a C 1-6 alkyl group optionally substituted by one or two groups selected from fluorine, phenyl(optionally substituted by C 1-4 alkyl, C(O) C 1-4 alkyl or halogen), =O, C 3-7 cycloalkyl, hydroxy, amino, dimethylamino, aminocarbonyl, C 1-4 alkoxy or trifluoromethyl; R 9 is hydrogen, C 1-4 alkyl or R 9 and R 8 together with nitrogen to which they are attached are a 5 to 7 membered heterocyclic group optionally containing another heroatom selected from oxygen, sulphur and nitrogen and optionally substituted by one or two groups selected from C 1-4 alkyl, =O, S(O) 2 C 1-4 alkyl, C(O) C 3-7 cycloalkyl or C(O) C 1-4 alkyl; R 10 and R 11 are independently hydrogen or C 1-4 alkyl group; X represents a nitrogen atom and Y is CH or X represents CH and Y is nitrogen;m is zero or an integer from 1 to 3; n is an integer from 1 to 3; p is zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof; the process for their preparation and their use in the treatment of conditions mediated by tachykinins.
摘要翻译：本发明涉及式I的哌啶衍生物，其中R表示卤素或C 1-4烷基R 1表示氢或C 1-4烷基R 2表示氢，C 1-4烷基或R 2与R 3表示C 3-7环烷基R 3表示氢，C 1 -4-烷基，C 3-7环烷基或C 3-6烯基或R 1和R 3与它们所连接的氮原子和碳原子分别表示5至6元杂环基，R 4表示三氟甲基，C 1-4烷基，C 1-4烷氧基，三氟甲氧基或卤素R是氢，R是NR7R8或R5是NR8R9，R6是氢，R7代表氢或C1-4烷基或R7和R8与它们所连接的氮一起是含有氧的饱和5至7元杂环基 R 8表示氢，苯基，C 3-7环烷基，CH 2 pCONR 10 R 11，饱和5至7元杂环基，其含有1-3个选自氧，硫和氮的杂原子，且任选被C 1-4烷基，SO 2 C 1-4烷基或 CO C 1-4烷基，含有1至3个选自氧，硫和氮的杂原子并且任选被C 1-4烷基SO 2 C 1-4烷基或CO C 1-4烷基取代的5元杂芳基或R 8表示含有 1至3个氮原子，任选被C 1-4烷基，SO 2 C 1-4烷基或CO C 1-4烷基取代，或R 8是任选被一个或两个选自氟取代的C1-6烷基，被氟取代，被C1-4烷基取代烷基，CO C 1-4烷基或卤素，= O，C 3-7环烷基，羟基，氨基，二甲基氨基，氨基羰基，C 1-4烷氧基或三氟甲基R 9是氢，C 1-4烷基或R 9和R 8与它们任选地含有选自氧，硫和氮的另一个主原子，并且任选被一个或两个选自C 1-4烷基，O，SO 2 C 1-4烷基，CO C 3-7环烷基或基团的基团取代的5至7元杂环基， CO C 1-4烷基R 10和R 11独立地是氢或C 1-4烷基基团X表示氮原子，Y表示CH或X表示CH，Y表示氮

5. 发明申请

WO2003015784A1 2-SUBSTITUTED 1-ARYLPIPERAZINES AS TACHYKININ ANTAGONISTS AND/OR SEROTONIN REUPTAKE INHIBITORS 审中-公开
标题翻译：作为TACHYKININ ANTAGONISTS和/或SERONONIN REUPTAKE抑制剂的2-取代的1-亚苄基
公开(公告)号：WO2003015784A1
公开(公告)日：2003-02-27
申请号：PCT/EP2002/009066
申请日：2002-08-13
申请人： GLAXO GROUP LIMITED , ALVARO, Guiseppe , JACK, Torquil, Iain, Maclean , TRANQUILLINI, Maria, Elvira
发明人： ALVARO, Guiseppe , JACK, Torquil, Iain, Maclean , TRANQUILLINI, Maria, Elvira
IPC分类号： A61K31/495
CPC分类号： C07D241/04
摘要： The present invention relates to piperazine derivatives of formula (I), wherein R represents halogen, C 1-4 alkyl, trifluoromethoxy or trifluoromethyl; R 1 is trifluoromethyl, C 1-4 alkyl, C 1-4 alkoxy, halogen or trifluoromethoxy; R 2 is hydrogen, C 1-4 alkyl or C 2-6 alkenyl; R 3 represents hydrogen or C 1-4 alkyl; n and m are independently 0 or an integer from 1 to 3; and pharmaceutically acceptable salts and solvates thereof, process for their preparation and their use in the treatment of condition mediated by tachykinins and/or by selective inhibition of the serotonin reuptake transporter protein.
摘要翻译：本发明涉及式（I）的哌嗪衍生物，其中R表示卤素，C 1-4烷基，三氟甲氧基或三氟甲基; R1是三氟甲基，C1-4烷基，C1-4烷氧基，卤素或三氟甲氧基; R2是氢，C1-4烷基或C2-6烯基; R3代表氢或C1-4烷基; n和m独立地为0或1至3的整数; 及其药学上可接受的盐和溶剂合物，其制备方法及其用于治疗由速激肽介导的病症和/或通过选择性抑制5-羟色胺再摄取转运蛋白。

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