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    Azabicyclo (3, 1, 0) hexan derivatives useful as modulators of dopamine D3 receptors
    3.
    发明授权
    Azabicyclo (3, 1, 0) hexan derivatives useful as modulators of dopamine D3 receptors 失效
    可用作多巴胺D3受体调节剂的氮杂双环（3,1,0）己烷衍生物

    公开(公告)号：US07745458B2

    公开(公告)日：2010-06-29

    申请号：US12064123

    申请日：2006-08-18

    申请人： Luca Arista ,  Anna Checchia ,  Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli

    发明人： Luca Arista ,  Anna Checchia ,  Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli

    IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D239/00 ,  C07D239/02 ,  C07D261/04 ,  C07D261/14 ,  C07D233/00 ,  C07D233/14 ,  C07D233/60

    CPC分类号： C07D403/06 ,  C07D403/12

    摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: p is 0, 1, 2, 3, 4 or 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; n is 3 or 4; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is —CH2—, —O— or —S—; Z may be —CH— or N; A is a group P or P1, wherein P is and P1 is and Y is hydrogen, —OH, C1-4alkyl, haloC1-4alkyl, 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, C1-4alkoxy and haloC1-4alkoxy; 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 substance 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：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; R2是氢或C1-4烷基; n为2或3; X是-CH 2 - ， - O-或-S-; Z可以是-CH-或N; A是P或P1基团，其中P是和P1是且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; 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D3受体的调节剂。 治疗物质相关疾病，作为抗精神病药物早泄或认知障碍。

    AZABICYCLO (3, 1, 0) HEXAN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS
    4.
    发明申请
    AZABICYCLO (3, 1, 0) HEXAN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS 失效
    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：US20090221618A1

    公开(公告)日：2009-09-03

    申请号：US12064123

    申请日：2006-08-18

    申请人： Luca Arista ,  Anna Checchia ,  Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli

    发明人： Luca Arista ,  Anna Checchia ,  Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli

    IPC分类号： A61K31/506 ,  C07D403/06

    CPC分类号： C07D403/06 ,  C07D403/12

    摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: p is 0, 1, 2, 3, 4 or 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; n is 3 or 4; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is —CH2—, —O— or —S—; Z may be —CH— or N; A is a group P or P1, wherein P is and P1 is ; and Y is hydrogen, —OH, C1-4alkyl, haloC1-4alkyl, 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, C1-4alkoxy and haloC1-4alkoxy; 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 substance 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：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; R2是氢或C1-4烷基; n为2或3; X是-CH 2 - ， - O-或-S-; Z可以是-CH-或N; A是P或P1组，其中P和P1是; 并且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; 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D3受体的调节剂。 治疗物质相关疾病，作为抗精神病药物早泄或认知障碍。

    Process for the production of ramoplanin-like amide derivatives
    6.
    发明授权
    Process for the production of ramoplanin-like amide derivatives 有权
    拉莫拉宁类酰胺衍生物的制备方法

    公开(公告)号：US07169890B2

    公开(公告)日：2007-01-30

    申请号：US10505881

    申请日：2003-02-26

    申请人： Romeo Ciabatti ,  Sonia Maffioli ,  Anna Checchia ,  Gabriella Romano ,  Gianpaolo Candiani ,  Gianbattista Panzone

    发明人： Romeo Ciabatti ,  Sonia Maffioli ,  Anna Checchia ,  Gabriella Romano ,  Gianpaolo Candiani ,  Gianbattista Panzone

    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 form 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。 其中烃基R不同的新化合物形成了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。

    3-triazolylthiaalkyl-3-azabicyclo (3-1-O) hexanes and their use as dopamine D3 receptor ligands
    7.
    发明授权
    3-triazolylthiaalkyl-3-azabicyclo (3-1-O) hexanes and their use as dopamine D3 receptor ligands 失效
    3-三唑基硫杂烷基-3-氮杂双环（3-1-O）己烷及其作为多巴胺D3受体配体的用途

    公开(公告)号：US07803820B2

    公开(公告)日：2010-09-28

    申请号：US11911035

    申请日：2006-04-12

    申请人： Daniele Andreotti ,  Anna Checchia ,  Dieter Hamprecht ,  Fabrizio Micheli

    发明人： Daniele Andreotti ,  Anna Checchia ,  Dieter Hamprecht ,  Fabrizio Micheli

    IPC分类号： A61K31/41 ,  C07D249/08 ,  C07D257/00

    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 R1 is hydrogen or C1-4alkyl; R2 is C1-4alkyl; R3 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, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl and SF5; p is 0, 1, 2, 3 or 4; and R4 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy and C1-4alkanoyl; n is 0 or 1; wherein when R4 is chlorine and p is 1, such R4 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, R3 comprises at least one SF5 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 D3 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; R2是C1-4烷基; R 3为氢或苯基，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个取代基取代 选自卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基和SF 5; p是0，1，2，3或4; 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为氯并且p为1时，相对于与分子的其余部分的连接键，该R 4不存在于邻位; 并且其中，如果n为0，则R 3包含至少一个SF 5基团作为取代基; 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，治疗强迫性强迫症，早泄或认知障碍。

    3-Triazolylthiaalkyl-3-Azabicyclo (3-1-O) Hexanes and Their Use as Dopamine D3 Receptor Ligands
    9.
    发明申请
    3-Triazolylthiaalkyl-3-Azabicyclo (3-1-O) Hexanes and Their Use as Dopamine D3 Receptor Ligands 失效
    3-三唑基硫杂烷基-3-氮杂双环（3-1-O）己烷及其作为多巴胺D3受体配体的用途

    公开(公告)号：US20080176917A1

    公开(公告)日：2008-07-24

    申请号：US11911035

    申请日：2006-04-12

    申请人： Daniele Andreotti ,  Anna Checchia ,  Dieter Hamprecht ,  Fabrizio Micheli

    发明人： Daniele Andreotti ,  Anna Checchia ,  Dieter Hamprecht ,  Fabrizio Micheli

    IPC分类号： A61K31/4196 ,  C07D209/52 ,  A61K31/403 ,  A61P25/18 ,  C07D249/12

    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 R1 is hydrogen or C1-4alkyl; R2 is C1-4alkyl; R3 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, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl and SF5; p is 0, 1, 2, 3 or 4; and R4 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy and C1-4alkanoyl; n is 0 or 1; wherein when R4 is chlorine and p is 1, such R4 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, R3 comprises at least one SF5 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 D3 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，相对于与分子其余部分的连接键，该R 4不在邻位; 并且其中，如果n为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。

    Process for the production of ramoplanin-like amide derivatives
    10.
    发明申请
    Process for the production of ramoplanin-like amide derivatives 有权
    拉莫拉宁类酰胺衍生物的制备方法

    公开(公告)号：US20050106691A1

    公开(公告)日：2005-05-19

    申请号：US10505881

    申请日：2003-02-26

    申请人： Romeo Ciabatti ,  Sonia Maffiolt ,  Anna Checchia ,  Gabriella Romano ,  Gianpaolo Candiani ,  Gianbattista Panzone

    发明人： Romeo Ciabatti ,  Sonia Maffiolt ,  Anna Checchia ,  Gabriella Romano ,  Gianpaolo Candiani ,  Gianbattista Panzone

    IPC分类号： A61K38/00 ,  A61P31/04 ,  C07K7/08 ,  C07K7/56 ,  C07K9/00 ,  C07K11/02 ,  C12P13/00

    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 form 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。 其中烃基R不同的新化合物形成了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。