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1. 发明申请

WO2003042228A1 MACROLIDES 审中-公开
标题翻译：大环内酯类
公开(公告)号：WO2003042228A1
公开(公告)日：2003-05-22
申请号：PCT/GB2002/005101
申请日：2002-11-13
申请人： GLAXO GROUP LIMITED , PLIVA D.D. , ALIHODZIC, Sulejman , ANDREOTTI, Daniele , BERDIK, Andrea , BIENTINESI, Ilaria , BIONDI, Stefano , CIRACO, Manuela , DAMIANI, Federica , DJEREK, Marko , DUMIC, Miljenko , ERAKOVIC, Vesna , HUTINEC, Antun , LAZAREVSKI, Gorjana , LOCIURO, Sergio , MARSIC, Natasa , MARUSIC-ISTUK, Zorica , MUTAK, Stjepan , PAIO, Alfredo , PAVLOVIC, Drazen , QUAGLIA, Anna , SCHOENFELD, Wolfgang , STIMAC, Vlado , TIBASCO, Jessica
发明人： ALIHODZIC, Sulejman , ANDREOTTI, Daniele , BERDIK, Andrea , BIENTINESI, Ilaria , BIONDI, Stefano , CIRACO, Manuela , DAMIANI, Federica , DJEREK, Marko , DUMIC, Miljenko , ERAKOVIC, Vesna , HUTINEC, Antun , LAZAREVSKI, Gorjana , LOCIURO, Sergio , MARSIC, Natasa , MARUSIC-ISTUK, Zorica , MUTAK, Stjepan , PAIO, Alfredo , PAVLOVIC, Drazen , QUAGLIA, Anna , SCHOENFELD, Wolfgang , STIMAC, Vlado , TIBASCO, Jessica
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： The present invention relates to 14 or 15 membered macrolides substitued at the 4" position of formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.
摘要翻译：本发明涉及在式（I）的4“位取代的14或15元大环内酯及其药学上可接受的盐和溶剂化物，其制备方法及其在治疗或预防人体全身或局部细菌感染中的用途或动物体。

2. 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

3. 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。

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