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    Hydroxylamine derivatives
    1.
    发明申请
    Hydroxylamine derivatives 有权
    羟胺衍生物

    公开(公告)号：US20070049643A1

    公开(公告)日：2007-03-01

    申请号：US10582141

    申请日：2004-12-10

    申请人： Carla Caccia ,  Laura Girola ,  Petra Kaltofen ,  Daniele Losi ,  Patricia Salvati ,  Enrico Selva ,  Florian Thaler

    发明人： Carla Caccia ,  Laura Girola ,  Petra Kaltofen ,  Daniele Losi ,  Patricia Salvati ,  Enrico Selva ,  Florian Thaler

    IPC分类号： A61K31/13

    CPC分类号： C07C239/20 ,  A61K31/13 ,  C07C239/12 ,  C07C2602/10

    摘要： This invention is related to hydroxylamino derivatives of the general formula (I) wherein n is 0, 1 or 2; R1 and R2, independently of each other, are H, OH or OCH3; R3 is H or CH3; R4 is H, C1-C3 straight or branched alkyl or, together with R3, forms a five to seven-membered carbocyclic ring; and R5 and R6, independently of each other, are H or C1-C5 straight or branched alkyl and the pharmaceutically acceptable salts or prodrug thereof, for the preparation of medicaments useful for the prevention, treatment and diagnosis of CNS degenerative disorders related to protein misfolding and/or misaggregation. The invention also relates to novel compounds included in formula (I), to a method for preparing said compounds and to pharmaceutical compositions containing them.

    摘要翻译： 本发明涉及通式（I）的羟基氨基衍生物，其中n为0,1或2; R 1和R 2彼此独立地是H，OH或OCH 3; R 3是H或CH 3 N; R 4是H，C 1 -C 3直链或支链烷基，或与R 3'一起形成 五至七元碳环; 和R 5和R 6彼此独立地是H或C 1 -C 5直链或 支链烷基及其药学上可接受的盐或前药，用于制备可用于预防，治疗和诊断与蛋白质错折叠和/或解聚相关的CNS退行性疾病的药物。 本发明还涉及式（I）中包括的新化合物，涉及制备所述化合物的方法和含有它们的药物组合物。

    Hydroxylamine derivatives
    2.
    发明授权
    Hydroxylamine derivatives 有权
    羟胺衍生物

    公开(公告)号：US07763751B2

    公开(公告)日：2010-07-27

    申请号：US10582141

    申请日：2004-12-10

    申请人： Carla Caccia ,  Laura Girola ,  Petra Karin Kaltofen ,  Daniele Losi ,  Patricia Salvati ,  Enrico Selva ,  Florian Thaler

    发明人： Carla Caccia ,  Laura Girola ,  Petra Karin Kaltofen ,  Daniele Losi ,  Patricia Salvati ,  Enrico Selva ,  Florian Thaler

    IPC分类号： C07C239/00 ,  A61K31/13

    CPC分类号： C07C239/20 ,  A61K31/13 ,  C07C239/12 ,  C07C2602/10

    摘要： This invention is related to hydroxylamino derivatives of the general formula (I) wherein n is 0, 1 or 2; R1 and R2, independently of each other, are H, OH or OCH3; R3 is H or CH3; R4 is H, C1-C3 straight or branched alkyl or, together with R3, forms a five to seven-membered carbocyclic ring; and R5 and R6, independently of each other, are H or C1-C5 straight or branched alkyl and the pharmaceutically acceptable salts or prodrug thereof, for the preparation of medicaments useful for the prevention, treatment and diagnosis of CNS degenerative disorders related to protein misfolding and/or misaggregation. The invention also relates to novel compounds included in formula (I), to a method for preparing said compounds and to pharmaceutical compositions containing them.

    摘要翻译： 本发明涉及通式（I）的羟基氨基衍生物，其中n为0,1或2; R 1和R 2彼此独立地是H，OH或OCH 3; R3是H或CH3; R4是H，C1-C3直链或支链烷基，或与R3一起形成五至七元碳环; 和R5和R6彼此独立地是H或C 1 -C 5直链或支链烷基及其药学上可接受的盐或前药，用于制备用于预防，治疗和诊断与蛋白质错折叠有关的CNS退行性病症的药物 和/或散乱。 本发明还涉及式（I）中包括的新化合物，涉及制备所述化合物的方法和含有它们的药物组合物。

    USE OF (HALOBENZYLOXY) BENZYLAMINO-PROPANAMIDES FOR THE MANUFACTURE OF MEDICAMENTS ACTIVE AS SODIUM AND/OR CALCIUM CHANNEL SELECTIVE MODULATORS
    3.
    发明申请
    USE OF (HALOBENZYLOXY) BENZYLAMINO-PROPANAMIDES FOR THE MANUFACTURE OF MEDICAMENTS ACTIVE AS SODIUM AND/OR CALCIUM CHANNEL SELECTIVE MODULATORS 审中-公开
    （HALOBENZYLOXY）苯甲酰胺丙酰胺用于制备作为钠和/或钙通道选择性调节剂活性的药物的用途

    公开(公告)号：US20110184068A1

    公开(公告)日：2011-07-28

    申请号：US12939726

    申请日：2010-11-04

    申请人： Elena Barbanti ,  Florian Thaler ,  Carla Caccia ,  Ruggero Fariello ,  Patricia Salvati

    发明人： Elena Barbanti ,  Florian Thaler ,  Carla Caccia ,  Ruggero Fariello ,  Patricia Salvati

    IPC分类号： A61K31/167 ,  A61P25/04

    CPC分类号： C07C237/06 ,  A61K31/00 ,  A61K31/165 ,  A61K45/06 ,  A61K2300/00

    摘要： The invention relates to the use of selected (R)-2-[(halobenzyloxy)benzylamino]-propanamides and the pharmaceutically acceptable salts thereof for the manufacture of medicament, that are selectively active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, pain, migraine, periferal diseases, cardiovascular diseases, inflammatory processes affecting all body systems, disorders affecting skin and related tissues, disorders of the respiratory system, disorders of the immune and endocrinological systems, gastrointestinal, urogenital, metabolic and seizure disorders, where the above mechanisms have been described as playing a pathological role.

    摘要翻译： 本发明涉及选择的（R）-2 - [（卤代苄氧基）苄基氨基] - 丙酰胺及其药学上可接受的盐在制备药物中的用途，其作为钠和/或钙通道调节剂选择性活性， 预防，缓解和治愈各种病症，包括疼痛，偏头痛，周围疾病，心血管疾病，影响所有身体系统的炎症过程，影响皮肤和相关组织的疾病，呼吸系统疾病，免疫和内分泌系统疾病 ，胃肠道，泌尿生殖，代谢和发作障碍，其中上述机制被描述为发挥病理作用。

    Substituted Aminoalkyl- and Amidoalkyl-Benzopyran Derivatives
    9.
    发明申请
    Substituted Aminoalkyl- and Amidoalkyl-Benzopyran Derivatives 审中-公开
    取代的氨基烷基 - 和酰胺基 - 苯并吡喃衍生物

    公开(公告)号：US20090005436A1

    公开(公告)日：2009-01-01

    申请号：US11909095

    申请日：2006-02-22

    申请人： Angelo Carotti ,  Piero Melloni ,  Florian Thaler ,  Carla Caccia ,  Sara Maestroni ,  Patricia Salvati

    发明人： Angelo Carotti ,  Piero Melloni ,  Florian Thaler ,  Carla Caccia ,  Sara Maestroni ,  Patricia Salvati

    IPC分类号： A61K31/353 ,  C07D311/04 ,  A61P25/28

    CPC分类号： C07D311/16 ,  C07D311/58

    摘要： This invention is related to novel aminoalkyl- and amidoalkyl-benzopyran derivatives of the following general formula (I) wherein: the group  is a substituent in position 6 or 7 wherein: R is an aromatic mono- or bi-cyclic carbocyclic ring or a mono- or bi-cyclic heterocyclic ring radical, said rings being optionally substituted by one or two substituents selected from (C1-C5) straight or branched alkyl, (C1-C5) straight or branched alkoxy, hydroxy, halogen and trifluoromethyl; m is zero or an integer from 1 to 3; n, p, R1 and R2 are as herein indicated and R3 and R4 are both hydrogen or taken together represent an oxygen atom, and the pharmaceutically acceptable salts thereof. The compounds that are active as selective and reversible MAO-B inhibitors in vitro and in vivo, are useful as medicaments for the prevention and the treatment of CNS degenerative disorders.

    摘要翻译： 本发明涉及以下通式（I）的新型氨基烷基 - 和酰氨基烷基 - 苯并吡喃衍生物，其中：该基团是6或7位的取代基，其中：R是芳族单环或双环碳环或单 所述环任选被一个或两个选自（C1-C5）直链或支链烷基，（C1-C5）直链或支链烷氧基，羟基，卤素和三氟甲基的取代基取代; m为0或1〜3的整数; n，p，R1和R2如本文所示，R 3和R 4均为氢或一起代表氧原子，及其药学上可接受的盐。 在体外和体内作为选择性和可逆MAO-B抑制剂活性的化合物可用作预防和治疗CNS退行性疾病的药物。

    Azabicycloalkyl derivatives of imidazo[1,5-a]indol-3-one and process for their preparation
    10.
    发明授权
    Azabicycloalkyl derivatives of imidazo[1,5-a]indol-3-one and process for their preparation 失效
    咪唑并[1,5-a]吲哚-3-酮的氮杂双环烷基衍生物及其制备方法

    公开(公告)号：US5637596A

    公开(公告)日：1997-06-10

    申请号：US578548

    申请日：1996-01-24

    申请人： Mario Varasi ,  Franco Heidempergher ,  Carla Caccia ,  Patricia Salvati

    发明人： Mario Varasi ,  Franco Heidempergher ,  Carla Caccia ,  Patricia Salvati

    IPC分类号： A61K31/41 ,  A61K31/435 ,  A61K31/439 ,  A61K31/46 ,  A61P1/00 ,  A61P1/08 ,  A61P25/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28 ,  A61P25/36 ,  A61P43/00 ,  C07D451/04 ,  C07D451/14 ,  C07D453/02 ,  C07D519/00

    CPC分类号： C07D453/02 ,  C07D451/04 ,  C07D451/14

    摘要： Novel 5-HT.sub.3 receptor antagonist compounds having the general formula (I) ##STR1## wherein each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N(R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7)N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl; ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, are provided.

    摘要翻译： PCT No.PCT / EP95 / 01652 Sec。 371日期：1996年1月24日 102（e）日期1996年1月24日PCT 1995年5月2日PCT PCT。 公开号WO95 / 32209 日期1995年11月30日具有通式（I）的图像的新型5-HT 3受体拮抗剂化合物（I）其中R，R 1和R 2可以相同或不同，为氢，卤素，羟基，氰基 ，C 1 -C 6烷基，CF 3，C 1 -C 6烷氧基，C 1 -C 6烷硫基，甲酰基，C 2 -C 6烷酰基，羧基，C 1 -C 6烷氧羰基，硝基，-N（R 4 R 5） 是氢，C 1 -C 6烷基，甲酰基或C 2 -C 6烷酰基; 或（R6R7）N-SO2基团，其中R6和R7各自独立地为氢或C1-C6烷基; R3是a，a）或b）其中n是1或2的整数，R8是氢，未被取代或被苯基取代的C1-C6烷基，C2-C4烯基，C2-C4炔基， 或C 2 -C 6烷酰基; 及其药学上可接受的盐。