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1. 发明申请

WO2006108700A1 3-TRIAZOLYLTHIOALKYL-3-AZABICYCLO (3 - 1 - O) HEXANES AND THEIR USE AS DOPAMINE D3 RECEPTOR LIGANDS 审中-公开
标题翻译： 3-三唑基三唑-3-基亚氨基（3 - 1 - O）HEXANES及其作为DOPAMINE D3受体配体使用
公开(公告)号：WO2006108700A1
公开(公告)日：2006-10-19
申请号：PCT/EP2006/003553
申请日：2006-04-12
申请人： GLAXO GROUP LIMITED , ANDREOTTI, Daniele , CHECCHIA, Anna , HAMPRECHT, Dieter , MICHELI, Fabrizio
发明人： ANDREOTTI, Daniele , CHECCHIA, Anna , HAMPRECHT, Dieter , MICHELI, Fabrizio
IPC分类号： C07D403/12 , C07D413/12 , A61K31/4196 , A61K31/422 , A61P25/00
CPC分类号： C07D413/12 , C07D403/12
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein • R 1 is hydrogen or C 1-4 alkyl; • R 2 is C 1-4 alkyl; • R 3 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; • p is 0, 1 , 2, 3 or 4; and • R 4 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy and C 1-4 alkanoyl; • n is 0 or 1 ; wherein when R 4 is chlorine and p is 1 , such R 4 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and wherein, if n is 0, R 3 comprises at least one SF 5 group as a substituent; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐：其中R 1是氢或C 1-4烷基; R 2是C 1-4烷基; R 3是氢或苯基，杂环基，5或6元杂芳族基团或8至11元双环基团，其中任何基团任选被 1,2,3或4个选自以下的取代基：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1 -4个烷氧基，C 1-4烷酰基和SF 5; p是0，1，2，3或4; R 4和R 4独立地选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基 C 1-4烷氧基，卤代C 1-4烷氧基和C 1-4烷酰基; n为0或1; 其中当R 4为氯且p为1时，相对于与分子的其余部分的连接键，该R 4不在邻位; 并且其中，如果n是0，则R 3 3包含至少一个SF 5基团作为取代基; 其制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D 3受体的调节剂，例如。治疗药物依赖性，作为抗精神病药，治疗强迫性强迫症，早泄或认知障碍。

2. 发明申请

WO2006108701A1 3- (1,2,4-TRIAZOL-3YLALKYL) AZABRICLO (3.1.0) HEXANE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： 3-（1,2,4-TRIAZOL-3YLALKYL）AZABRICLO（3.1.0）作为DOPAMINE D3受体的调节剂的HEXANE衍生物
公开(公告)号：WO2006108701A1
公开(公告)日：2006-10-19
申请号：PCT/EP2006/003554
申请日：2006-04-12
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , CHECCHIA, Anna , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
发明人： BONANOMI, Giorgio , CHECCHIA, Anna , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
IPC分类号： C07D403/06 , C07D403/14 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/4196 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/501 , A61K31/497 , A61P25/00 , C07D409/14
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: wherein " G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl and indazolyl; " p is an integer ranging from 0 to 5; " R 1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5, or corresponds to a group R 5; " each R 2 is independently hydrogen, fluorine or C 1-4 alkyl; " n is 2, 3, 4, or 5; " R 3 is C 1-4 alkyl; " R 4 is hydrogen, or a C 1-4 alkyl group, a benzyl group, a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ;or R 4 is a -SR 6 group; " R 5 is selected from a group consisting of: isoxazolyl, -CH 2 -N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl and 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from a group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy and C 1-4 alkanoyl; " R 6 is C 1-4 alkyl or -CH 2 C 3-4 cycloalkyl; and when R 1 is chlorine and p is 1, such R 1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R 1 corresponds to R 5 , p is 1. processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐：其中“G选自：苯基，吡啶基，苯并噻唑基和吲唑基”; p是0-5的整数; “R 1”独立地选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5，或对应于基团R 5;每个R 2独立地是氢，氟或C 1-4烷基; “n为2,3,4或5;”R 3为C 1-4烷基; “R”4是氢或C 1-4烷基，苄基，苯基，杂环基，5或6元杂芳基或8至11元双环基团，其中任何基团任选被1,2,3或4个选自以下的取代基取代：卤素，氰基，C 1-4烷基，烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷基，烷酰基和SF 5;或R 4是-SR 6 C 6;选择“R 5” 由以下组成的组：异恶唑基，-CH 2 - N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基和2-吡咯烷基，并且这种基团任选被取代通过一个或两个选自以下的取代基：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4 - 烷氧基和C 1-4烷酰基; “R 6”是C 1-4烷基或-CH 2 -SO 3 -S-环烷基;当R 相对于与分子的其余部分的连接键，R 1不在氯原子的邻位存在这样的R 1，并且当R _{1 对应于R 5，p为1.它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D的调节剂 > 3受体，例如治疗药物依赖性，作为抗精神病药，治疗强迫性强迫症，早泄或认知障碍。}

3. 发明申请

WO2007113232A1 AZABICYCLO [3. 1. 0] HEXYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： AZABICYCLO [3。作为DOPAMINE D3受体的调节剂的HEXYL衍生物
公开(公告)号：WO2007113232A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053074
申请日：2007-03-30
申请人： Glaxo Group Limited , BERTANI, Barbara , BONANOMI, Giorgio , CAPELLI, Anna Maria , CHECCHIA, Anna , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna , TERRENI, Silvia
发明人： BERTANI, Barbara , BONANOMI, Giorgio , CAPELLI, Anna Maria , CHECCHIA, Anna , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14 , A61K31/513 , A61P25/00
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to novel compounds of formula (I)' or a salt thereof: wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11 -membered heteroaryl bicyclic group; A is a group P1 or a group P2 Wherein p is an integer ranging from 0 to 5; R 1 is halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1- 4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 6 ; and when p is an integer ranging from 2 to 5, each R 1 may be the same or different; R 2 is hydrogen or C 1-4 alkyl; n is 3, 4, 5 or 6; R 6 is a moiety selected from the group consisting of: isoxazolyl, -CH 2 -N-pyrrolyl, 1,1 -dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such R 6 group is optionally substituted by one or two substituents selected from: halogen, cyano, C 1- 4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl; R 4 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C 1- 4 alkyl, C 3-7 cycloalkyl, haloC 1-4 alkyl, C 1-4- alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and NR'R"; or R 4 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic group is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl, haloC 1-4 alkoxy and SF 5 ; R 5 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, C 3-7 cycloalkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and NR'R"; or R 5 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; R 7 is hydrogen or C 1-2 alkyl; R' is H, C 1-4 alkyl or C 1-4 alkanoyl; R" is defined as R'; R' and R" taken together with the interconnecting nitrogen atom may form a 5-, 6- membered saturated or unsaturated heterocyclic ring; wherein at least one of R 4 and R 5 is hydrogen; and wherein only one R 2 group may be different from hydrogen; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中G选自：苯基，5-或6-元单环杂芳基或8-至11元杂芳基双环基团 A是基团P1或基团P2，其中p是0至5的整数; R 1是卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷基，烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5; 或对应于基团R 6; 并且当p是2至5的整数时，每个R 1可以相同或不同; R 2是氢或C 1-4烷基; n为3,4,5或6; R 6是选自以下的部分：异恶唑基，-CH 2 - N-吡咯基，1,1-二氧代-2-异噻唑烷基，噻吩基，噻唑基，吡啶基，2-吡咯烷酮基和这样的R 6 C 6基团任选地被一个或两个选自以下的取代基取代：卤素，氰基，C 1-4 - >一

4. 发明申请

WO2007022934A3 AZABICYCLO (3, 1, 0) HEXAN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： AZ Y Y O O O O O S S S S S S S S S S S S S S S S S S S S S S
公开(公告)号：WO2007022934A3
公开(公告)日：2007-05-10
申请号：PCT/EP2006008201
申请日：2006-08-18
申请人： GLAXO GROUP LTD , ARISTA LUCA , CHECCHIA ANNA , GENTILE GABRIELLA , HAMPRECHT DIETER , MICHELI FABRIZIO
发明人： ARISTA LUCA , CHECCHIA ANNA , GENTILE GABRIELLA , HAMPRECHT DIETER , MICHELI FABRIZIO
IPC分类号： C07D403/06 , A61K31/12 , A61K31/403 , A61P25/00 , C07D403/12
CPC分类号： C07D403/06 , C07D403/12
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: Formula (I), wherein: p is 0, 1, 2, 3, 4 or 5; R 1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; n is 3 or 4; R 2 is hydrogen or C 1-4 alkyl; n is 2 or 3; X is -CH 2 -, -O- or -S-; Z may be -CH- or N; A is a group P or P1, wherein P is Formula (Ia) and P1 is Formula (Ib); and Y is hydrogen, -OH, C 1-4 alkyl, haloC 1-4 alkyl, phenyl or a heteroaromatic group, wherein the phenyl and the heteroaromatic group are optionally substituted by one or two substituents selected from a group consisting of C1-4alkyl, haloC1-4alkyl, C 1-4 alkoxy and haloC 1-4 alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat substace related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（I）化合物或其盐：式（I），其中：p为0,1,2,3,4或5; R 1独立地选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基， C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5; n为3或4; R 2是氢或C 1-4烷基; n为2或3; X是-CH 2 - ， - O-或-S-; Z可以是-CH-或N; A是基团P或P1，其中P是式（Ia），P1是式（Ib）; 和Y是氢，-OH，C 1-4烷基，卤代C 1-4烷基，苯基或杂芳基，其中苯基和杂芳基任选被取代选自一个或两个选自C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基和卤代C 1-4烷氧基的取代基; 其制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D 3受体的调节剂，例如。治疗类别相关疾病，作为抗精神病药物早泄或认知障碍。

5. 发明申请

WO2006133946A1 AZAB I CYCLO [3 . 1 . 0] HEXANE DERIVATIVES AS DOPAMIN D3 RECEPTOR MODULATORS 审中-公开
标题翻译： AZAB I CYCLO [3。 1。 0] HEXANE衍生物作为DOPAMIN D3受体调节剂
公开(公告)号：WO2006133946A1
公开(公告)日：2006-12-21
申请号：PCT/EP2006/005768
申请日：2006-06-13
申请人： GLAXO GROUP LIMITED , ARISTA, Luca , CARDULLO, Francesca , CHECCHIA, Anna , HAMPRECHT, Dieter , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
发明人： ARISTA, Luca , CARDULLO, Francesca , CHECCHIA, Anna , HAMPRECHT, Dieter , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D413/14 , C07D401/14 , A61K31/435 , A61K31/41 , A61P25/00
CPC分类号： C07D417/14 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: (I), processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐：（I）其制备方法，用于这些方法的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D的调节剂 > 3个受体，例如治疗药物依赖性，作为抗精神病药，治疗强迫性强迫症，早泄或认知障碍。

6. 发明申请

WO2007113260A1 AZABICYCLO [3. 1. O] HEXYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： AZABICYCLO [3。作为DOPAMINE D3受体的调节剂的HEXYL衍生物
公开(公告)号：WO2007113260A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053117
申请日：2007-03-30
申请人： GLAXO GROUP LIMITED , BERTANI, Barbara , CHECCHIA, Anna , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TERRENI, Silvia
发明人： BERTANI, Barbara , CHECCHIA, Anna , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TERRENI, Silvia
IPC分类号： C07D401/14 , C07D403/06 , C07D405/14 , A61K31/513 , A61P25/00
CPC分类号： C07D401/14 , C07D403/06 , C07D405/14
摘要： The present invention relates to novel compounds or pharmaceutically acceptable saltsthereof: wherein G is selected from a group consisting of : phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; A is a group P wherein P is p is an integer ranging from 0 to 5; Rl, R2, R3, R4,R5 and R7 are as defined in the claims, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
摘要翻译：本发明涉及新化合物或其药学上可接受的盐衍生物：其中G选自：苯基，5-或6-元单环杂芳基或8-至11元杂芳基双环基; A为基团P，其中P为p为0至5的整数; R 1，R 2，R 3，R 4，R 5和R 7如权利要求书中所定义，其制备方法，在这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D3受体的调节剂。治疗药物依赖性，作为抗精神病药，治疗强迫性强迫性疾病或早泄。

7. 发明申请

WO2007022934A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2007022934A2
公开(公告)日：2007-03-01
申请号：PCT/EP2006/008201
申请日：2006-08-18
申请人： GLAXO GROUP LIMITED , ARISTA, Luca , CHECCHIA, Anna , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio
发明人： ARISTA, Luca , CHECCHIA, Anna , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio
IPC分类号： C07D403/06 , C07D403/12
CPC分类号： C07D403/06 , C07D403/12
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: Formula (I), wherein: p is 0, 1, 2, 3, 4 or 5; R 1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; n is 3 or 4; R 2 is hydrogen or C 1-4 alkyl; n is 2 or 3; X is -CH 2 -, -O- or -S-; Z may be -CH- or N; A is a group P or P1, wherein P is Formula (Ia)and P1 is Formula (Ib) ; and Y is hydrogen, -OH, C 1-4 alkyl, haloC 1-4 alkyl, phenyl or a heteroaromatic group, wherein the phenyl and the heteroaromatic group are optionally substituted by one or two substituents selected from a group consisting of C1-4alkyl, haloC1-4alkyl, C 1-4 alkoxy and haloC 1-4 alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat substace related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（I）化合物或其盐：式（I），其中：p为0,1,2,3,4或5; R 1独立地选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基， C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5; n为3或4; R 2是氢或C 1-4烷基; n为2或3; X是-CH 2 - ， - O-或-S-; Z可以是-CH-或N; A是基团P或P1，其中P是式（Ia），P1是式（Ib）; 和Y是氢，-OH，C 1-4烷基，卤代C 1-4烷基，苯基或杂芳基，其中苯基和杂芳基任选被取代选自一个或两个选自C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基和卤代C 1-4烷氧基的取代基; 其制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D 3受体的调节剂，例如。治疗类别相关疾病，作为抗精神病药物早泄或认知障碍。

8. 发明申请

WO2003076460A1 A PROCESS FOR THE PRODUCTION OF RAMOPLANIN-LIKE AMIDE DERIVATIVES 审中-公开
标题翻译：用于生产类似兰普兰样酰胺衍生物的方法
公开(公告)号：WO2003076460A1
公开(公告)日：2003-09-18
申请号：PCT/EP2003/001961
申请日：2003-02-26
申请人： BIOSEARCH ITALIA S.p.A. , CIABATTI, Romeo , MAFFIOLI, Sonia , CHECCHIA, Anna , ROMANO', Gabriella , CANDIANI, Gianpaolo , PANZONE, Gianbattista
发明人： CIABATTI, Romeo , MAFFIOLI, Sonia , CHECCHIA, Anna , ROMANO', Gabriella , CANDIANI, Gianpaolo , PANZONE, Gianbattista
IPC分类号： C07K11/02
CPC分类号： C07K7/08 , C07K9/008
摘要： The invention regards a process for the production of ramoplanin-like derivatives of formula (I): RAMO-NC-CO-R (I), wherein the radical R represents a hydrocarbon radical and the portion RAMO-NH- represents deacylated ramoplanin, any of its factors or ramoplanose. The compound of Formula (I) are obtained by reacting a carboxylic acid R-COOH with deacylated ramoplanin, any of its factors or ramoplanose protected on the ornitine amino groups. New compounds wherein the hydrocarbon radical R is different from those characaterizing the ramoplanin and ramoplanose natural products and their tetrahydro-derivatives are calimed. The new compounds have the same or better antinfective activity, lower haemolytic effect and better tolerability profile than ramoplanin.
摘要翻译：本发明涉及制备式（I）的拉莫拉宁衍生物的方法：RAMO-NC-CO-R（I），其中基团R表示烃基，部分RAMO-NH-表示脱酰基拉莫拉宁，任何的因素或ramoplanose。式（I）化合物通过使羧酸R-COOH与脱酰基拉莫拉宁反应，其任何因子或在鸟氨酸上保护的拉米布糖反应得到。新的化合物，其中烃基R不同于拉莫拉宁和拉莫拉诺天然产物及其四氢衍生物的特征加压。新化合物与拉莫拉宁相比具有相同或更好的抗感染活性，较低的溶血作用和更好的耐受性。

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