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。

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。

公开(公告)号：US20120220592A1

公开(公告)日：2012-08-30

申请号：US13359285

申请日：2012-01-26

申请人： Florian THALER ,  Mauro NAPOLETANO ,  Cibele SABIDO-DAVID ,  Ermanno MORIGGI ,  Carla CACCIA ,  Laura FARAVELLI ,  Alessandra RESTIVO ,  Patricia SALVATI

发明人： Florian THALER ,  Mauro NAPOLETANO ,  Cibele SABIDO-DAVID ,  Ermanno MORIGGI ,  Carla CACCIA ,  Laura FARAVELLI ,  Alessandra RESTIVO ,  Patricia SALVATI

IPC分类号： A61K31/165 ,  A61K31/433 ,  A61K31/44 ,  A61K31/445 ,  A61K31/5375 ,  A61P25/00 ,  A61P25/06 ,  A61P25/28 ,  A61P25/18 ,  A61P25/08 ,  A61P25/30 ,  A61P29/00 ,  A61P1/00 ,  A61P13/00 ,  A61P27/02 ,  A61P1/16 ,  A61P37/00 ,  A61P5/00 ,  A61P9/00 ,  A61K31/42

CPC分类号： C07D285/06 ,  C07C237/06 ,  C07C237/20 ,  C07C2601/02 ,  C07D211/58 ,  C07D213/30 ,  C07D213/38 ,  C07D213/64 ,  C07D231/12 ,  C07D233/64 ,  C07D261/12 ,  C07D295/185 ,  C07D307/14 ,  C07D307/52 ,  C07D333/20 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

摘要： 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.

摘要翻译： 提出了2-苯基乙基氨基取代的甲酰胺衍生物及其作为钠和/或钙通道调节剂用于预防，减轻和治愈广泛范围病理学的用途。

公开(公告)号：US20100197799A1

公开(公告)日：2010-08-05

申请号：US12760007

申请日：2010-04-14

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： A61K31/13 ,  C07C239/20 ,  A61P25/16 ,  A61P25/28

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

摘要： This invention is related to hydroxylamino derivatives of the following 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 the compounds and to pharmaceutical compositions containing them.

摘要翻译： 本发明涉及以下通式（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相关的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，涉及制备该化合物的方法和含有该化合物的药物组合物。

公开(公告)号：US07649005B2

公开(公告)日：2010-01-19

申请号：US10575627

申请日：2004-10-05

申请人： Patricia Salvati ,  Carla Caccia ,  Piero Melloni ,  Alessandra Restivo ,  Cibele Sabido David ,  Stefania Vallese

发明人： Patricia Salvati ,  Carla Caccia ,  Piero Melloni ,  Alessandra Restivo ,  Cibele Sabido David ,  Stefania Vallese

IPC分类号： A61K31/44 ,  C07D213/02

CPC分类号： C07D261/02 ,  A61K31/341 ,  A61K31/422 ,  A61K31/426 ,  C07D213/38 ,  C07D233/64 ,  C07D235/14 ,  C07D249/08 ,  C07D261/08 ,  C07D263/32 ,  C07D277/28 ,  C07D307/14 ,  C07D307/38 ,  C07D307/52 ,  C07D307/81 ,  C07D309/04 ,  C07D319/12 ,  C07D333/20

摘要： This invention is related to compounds of general formula (I) wherein X is oxygen or sulphur or a NR7 group; R1 is C3-C8 alkyl, or C1-C8 alkyl substituted by phenoxy or phenyl, both phenoxy or phenyl being optionally substituted by one or more fluoro, chloro, trifluoromethyl, C1-C6 alkyl, hydroxyl, C1-C6 alkoxy; R2, R3 are independently hydrogen, C1-C6 alkyl, halogen, trifluoromethyl, hydroxy or C1-C6 alkoxy; R4 is hydrogen, C1-C8 alkyl; R5, R6 are independently hydrogen, C1-C3 alkyl, optionally substituted by hydroxy or phenyl; R7 is hydrogen or straight or branched C1-C3 alkyl; Het is a five to seven membered, saturated or unsaturated heteromonocyclic or an eight to ten membered, saturated or unsaturated heterobicyclic group, containing one or more heteroatoms chosen independently from nitrogen, oxygen and sulphur, said mono- or bicyclic groups being optionally substituted by C1-C6alkyl, halogen, hydroxyl or C1-C6 alkoxy; and the pharmaceutically acceptable salts or prodrug thereof, that are active as sodium and/or calcium channel modulators and/or as selective MAO-B inhibitors and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.

摘要翻译： 本发明涉及通式（I）的化合物，其中X是氧或硫或NR 7基团; R 1是C 3 -C 8烷基或被苯氧基或苯基取代的C 1 -C 8烷基，苯氧基或苯基任选被一个或多个氟，氯，三氟甲基，C 1 -C 6烷基，羟基，C 1 -C 6烷氧基取代; R2，R3独立地是氢，C1-C6烷基，卤素，三氟甲基，羟基或C1-C6烷氧基; R4是氢，C1-C8烷基; R5，R6独立地为氢，任选被羟基或苯基取代的C 1 -C 3烷基; R 7是氢或直链或支链C 1 -C 3烷基; Het是五至七元饱和或不饱和杂单环或八至十元饱和或不饱和杂双环基团，其含有一个或多个独立地选自氮，氧和硫的杂原子，所述单 - 或双环基团任选被C 1 -C 1-6烷基，卤素，羟基或C 1 -C 6烷氧基; 其作为钠和/或钙通道调节剂和/或作为选择性MAO-B抑制剂是有活性的，因此可用于预防，缓解和治愈广泛范围的病症，包括但不限于 神经，精神，心血管，炎症，眼科，泌尿，代谢和胃肠疾病，其中上述机制已被描述为发挥病理作用。

公开(公告)号：US20080319057A1

公开(公告)日：2008-12-25

申请号：US12158491

申请日：2006-11-29

申请人： Florian Thaler ,  Mauro Napoletano ,  Cibele Sabido-David ,  Ermanno Moriggi ,  Carla Caccia ,  Laura Faravelli ,  Alessandra Restivo ,  Patricia Salvati

发明人： Florian Thaler ,  Mauro Napoletano ,  Cibele Sabido-David ,  Ermanno Moriggi ,  Carla Caccia ,  Laura Faravelli ,  Alessandra Restivo ,  Patricia Salvati

IPC分类号： A61K31/341 ,  C07C237/20 ,  A61K31/165 ,  C07D307/54

CPC分类号： C07D285/06 ,  C07C237/06 ,  C07C237/20 ,  C07C2601/02 ,  C07D211/58 ,  C07D213/30 ,  C07D213/38 ,  C07D213/64 ,  C07D231/12 ,  C07D233/64 ,  C07D261/12 ,  C07D295/185 ,  C07D307/14 ,  C07D307/52 ,  C07D333/20 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

摘要： 2-Phenylethylamino substituted carboxamide derivatives of formula (I); wherein J, W, R0, R1, R2, R3, and R4 have the meanings as defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urology, and gastrointestinal diseases where the above mechanisms have been described as playing a pathological role, are described.

摘要翻译： 式（I）的2-苯基乙基氨基取代的甲酰胺衍生物; 其中J，W，R 0，R 1，R 2，R 3和R 4具有如本说明书中所定义的含义及其药学上可接受的盐，含有它们作为活性成分的药物组合物及其作为钠和/或钙通道调节剂用于预防 描述了将上述机制描述为发挥病理作用的各种病症，包括神经，精神，心血管，炎症，眼科，泌尿科和胃肠疾病。

公开(公告)号：US20060116329A1

公开(公告)日：2006-06-01

申请号：US10536307

申请日：2003-11-25

申请人： Luca Benatti ,  Ruggero Fariello ,  Patricia Salvati ,  Roberto Pellicciari ,  Carla Caccia

发明人： Luca Benatti ,  Ruggero Fariello ,  Patricia Salvati ,  Roberto Pellicciari ,  Carla Caccia

IPC分类号： A61K31/7052 ,  A61K31/381 ,  C07D333/38

CPC分类号： C07D333/28

摘要： Compounds of formula (I) wherein R is hydroxy, linear or branched C1-C6 alkoxy, phenoxy, benzyloxy, a group —N(R1R2) wherein R1 is hydrogen, linear or branched C1-C4 alkyl, benzyl, phenyl and R2 is hydrogen or linear or branched C1-C4 alkyl, or R is a glycoside residue or a primary alkoxy residue from ascorbic acid, optionally having one or more hydroxy groups alkylated or acylated by linear or branched C1-C4 alkyl or acyl groups; X is a halogen atom and n 1 or 2 are long lasting inhibitors of kynurenine 3-monooxygenase (KMO) and potent glutamate (GLU) release inhibitors.

摘要翻译： 式（I）的化合物，其中R是羟基，直链或支链C 1 -C 6烷氧基，苯氧基，苄氧基，-N（R 1， 其中R 1是氢，直链或支链C 1 -C 4烷基，C 1 -C 4烷基， 苄基，苯基和R 2是氢或直链或支链C 1 -C 4烷基，或R是糖苷残基或伯烷氧基 任选具有一个或多个由直链或支链C 1 -C 4烷基或酰基烷基化或酰化的羟基的抗坏血酸残基; X是卤素原子，n 1或2是犬尿苷3-单加氧酶（KMO）和强力谷氨酸（GLU）释放抑制剂的长效抑制剂。

公开(公告)号：US06284896B1

公开(公告)日：2001-09-04

申请号：US08998867

申请日：1997-12-29

申请人： Sergio Mantegani ,  Tiziano Bandiera ,  Enzo Brambilla ,  Carla Caccia ,  Nicola Carfagna

发明人： Sergio Mantegani ,  Tiziano Bandiera ,  Enzo Brambilla ,  Carla Caccia ,  Nicola Carfagna

IPC分类号： C07D48706

CPC分类号： C07D487/06

摘要： There are provided compounds of formula (I), wherein R1 is a hydrogen, chlorine or bromine atom or a methyl, methylthio, hydroxy, cyano or carboxamido group; R2 is C1-C3 alkyl or an alkyl group; R3 and R4 are independently a hydrogen atom, a C1-C5 alkyl group, a C3-C5 alkenyl group, a C5-C6 cycloalkyl C1-C3 alkyl group, a phenyl-C3-C5 alkenyl or phenyl group: which groups are optionally substituted by C1-C3 alkyl, C1-C3 alkoxy, triflouromethyl, hydroxy or amino group; or a group of formula (a), wherein R6 is hydrogen atom or a C1-C3 alkyl group and R7 is a phenyl group, a substituted phenyl group as described above or a heterocyclic ring, R5 is a hydrogen or bromine atom or an organic residue and R is H or an organic residue, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmaceutical compositions comprising them are also provided.

摘要翻译： 提供式（I）化合物，其中R 1是氢，氯或溴原子或甲基，甲硫基，羟基，氰基或甲酰氨基; R2是C1-C3烷基或烷基; R3和R4独立地是氢原子，C1-C5烷基，C3-C5烯基，C5-C6环烷基C1-C3烷基，苯基-C3-C5链烯基或苯基：这些基团是任选取代的 C 1 -C 3烷基，C 1 -C 3烷氧基，三氟甲基，羟基或氨基; 或式（a）的基团，其中R6是氢原子或C1-C3烷基，R7是苯基，如上所述的取代苯基或杂环，R5是氢或溴原子或有机 残基，R为H或有机残基，或其药学上可接受的盐。 还提供了其制备方法和包含它们的药物组合物。

公开(公告)号：US08278485B2

公开(公告)日：2012-10-02

申请号：US13288891

申请日：2011-11-03

申请人： Elena Barbanti ,  Carla Caccia ,  Patricia Salvati ,  Francesco Velardi ,  Tiziano Ruffilli ,  Luigi Bogogna

发明人： Elena Barbanti ,  Carla Caccia ,  Patricia Salvati ,  Francesco Velardi ,  Tiziano Ruffilli ,  Luigi Bogogna

IPC分类号： C07C231/12 ,  C07C233/09 ,  A61K31/165

CPC分类号： C07C231/12 ,  C07C231/18 ,  C07C237/06

摘要： A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]propanamides and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight.The process is carried out by submitting the Schiff bases intermediates 2-[4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to catalytic hydrogenation in the presence of a heterogeneous catalyst in a protic organic solvent.

摘要翻译： 一种获得治疗活性的2- [4-（3-和2-（氟苄氧基）苄氨基]丙酰胺及其与药学上可接受的酸的高纯度程度的盐，特别是二苄基衍生物杂质含量低于0.03％的方法， 优选低于0.01重量％，该方法通过将席夫碱中间体2- [4-（3-和2-氟苄氧基）亚苄基氨基]丙酰胺在质子有机溶剂中的非均相催化剂存在下进行催化氢化来进行 。

公开(公告)号：US20080096965A1

公开(公告)日：2008-04-24

申请号：US11574751

申请日：2005-07-28

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

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

IPC分类号： A61K31/195 ,  A61P29/00

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 assodium 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）苄氨基] - 丙酰胺及其药学上可接受的盐在制备药物中的用途，所述药物是选择性活性的脯氨酸和/或钙通道调节剂，因此可用于预防 ，减轻和治愈各种病症，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病症，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。