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11. 发明申请

US20060116329A1 Halothenoyl-cyclopropane-1-carboxylic acid derivatives 审中-公开
标题翻译：卤代苯甲酰基 - 环丙烷-1-羧酸衍生物
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。

12. 发明申请

US20070049643A1 Hydroxylamine derivatives 有权
标题翻译：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。

13. 发明授权

US08278485B2 Process for the production of 2-[4-(3- and 2-fluorobenzyloxy) benzylamino] propanamides 有权
标题翻译：制备2- [4-（3-和2-氟苄氧基）苄氨基]丙酰胺的方法
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。

14. 发明授权

US5874457A Imidazolylalkyl derivatives of imidazo�1,5-a!indol-3-one 失效
标题翻译：咪唑并[1,5-a]吲哚-3-酮的咪唑基烷基衍生物
公开(公告)号：US5874457A
公开(公告)日：1999-02-23
申请号：US578550
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： A61K31/415 , A61K31/4188 , A61P1/00 , A61P1/08 , A61P1/12 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/36 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04 , Y02P20/55
摘要： Novel 5-HT.sub.3 receptor antagonist compounds having following formula (I) ##STR1## wherein n is 1, 2 or 3;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;R.sub.3 is an imidazolyl group of formula ##STR2## wherein each of R.sub.8 and R.sub.10 which may be the same or different is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.9 is hydrogen, C.sub.1 -C.sub.6 alkyl or a nitrogen protecting group; and the pharmaceutically acceptable salts thereof, are disclosed.
摘要翻译： PCT No.PCT / EP95 / 01651 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。出版物WO95 / 32204 日期：1995年11月30日具有下式（I）的新型5-HT 3受体拮抗剂化合物其中n为1,2或3; 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，其中R 4和R 5各自独立地为氢，C 1 -C 6烷基，甲酰基或C 2 -C 6烷酰基的C 1 -C 6烷氧羰基，硝基，-N（R 4 R 5）或（R6R7）N-SO2基团，其中R6和R7各自独立地为氢或C1-C6烷基; R 3是式（I）的咪唑基，其中R 8和R 10各自可以相同或不同，是氢或C 1 -C 6烷基，R 9是氢，C 1 -C 6烷基或氮保护基; 及其药学上可接受的盐。

15. 发明授权

US08076515B2 Process for the production of 2-[4-(3- and 2-fluorobenzyloxy) benzylamino] propanamides 有权
标题翻译：制备2- [4-（3-和2-氟苄氧基）苄氨基]丙酰胺的方法
公开(公告)号：US08076515B2
公开(公告)日：2011-12-13
申请号：US12338825
申请日：2008-12-18
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。

16. 发明授权

US07763751B2 Hydroxylamine derivatives 有权
标题翻译：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。

17. 发明申请

US20090156678A1 PROCESS FOR THE PRODUCTION OF 2-[4-(3- AND 2-FLUOROBENZYLOXY) BENZYLAMINO] PROPANAMIDES 有权
标题翻译：生产2- [4-（3-和2-氟代苄基）苯甲酰胺]丙酰胺的方法
公开(公告)号：US20090156678A1
公开(公告)日：2009-06-18
申请号：US12338825
申请日：2008-12-18
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： A61K31/195 , C07C237/14 , A61K31/165 , A61P25/00 , A61P29/00
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。

18. 发明授权

US5783574A Imidazolylakyl derivatives of imidazo �5,1-c!�1,4!benzoxazin-1-one process for their preparation 失效
标题翻译：咪唑并[5,1-c] [1,4]苯并恶嗪-1-酮的咪唑基]甲基衍生物的制备方法
公开(公告)号：US5783574A
公开(公告)日：1998-07-21
申请号：US578549
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： A61K31/535 , A61K31/5383 , A61P1/00 , A61P1/08 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/36 , A61P43/00 , C07D498/04
CPC分类号： C07D498/04 , Y02P20/55
摘要： Novel 5-HT.sub.3 receptor antagonist compounds having following formula (I) ##STR1## wherein n is 1, 2 or 3; 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 R6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.3 is an imidazolyl group of formula ##STR2## wherein each of R.sub.8 and R.sub.10 which may be the same or different is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.9 is hydrogen, C.sub.1 -C.sub.6 alkyl or a nitrogen protecting group; and the pharmaceutically acceptable salts thereof, are disclosed.
摘要翻译： PCT No.PCT / EP95 / 01650 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 / 32208 PCT 日期：1995年11月30日具有下式（I）的新型5-HT 3受体拮抗剂化合物其中n为1,2或3; 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，其中R 4和R 5各自独立地为氢，C 1 -C 6烷基，甲酰基或C 2 -C 6烷酰基的C 1 -C 6烷氧羰基，硝基，-N（R 4 R 5）或（R6R7）N-SO2基团，其中R6和R7各自独立地为氢或C1-C6烷基; R 3是式A的咪唑基a）其中R 8和R 10可以相同或不同的是氢或C 1 -C 6烷基，R 9是氢，C 1 -C 6烷基或氮保护组; 及其药学上可接受的盐。

19. 发明授权

US06284896B1 Abeo-ergoline derivatives as 5HT1A ligands 失效
标题翻译：二氢麦角灵衍生物作为5HT1A配体
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。

20. 发明授权

US5424328A Phenyl-imidazolidinone derivatives 失效
标题翻译：苯基咪唑啉酮衍生物
公开(公告)号：US5424328A
公开(公告)日：1995-06-13
申请号：US144514
申请日：1993-11-02
申请人： Mario Varasi , Franco Heidempergher , Carla Caccia , Claudio Arrigoni
发明人： Mario Varasi , Franco Heidempergher , Carla Caccia , Claudio Arrigoni
IPC分类号： C07D403/06 , A61K31/415 , A61K31/4178 , A61P1/00 , A61P1/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/20 , A61P25/26 , C07D233/32 , C07D233/54 , C07D233/56 , C07D233/61 , C07D401/06
CPC分类号： C07D233/64 , Y02P20/55
摘要： The invention relates to new derivatives of 1-imidazolylalkyl-3-phenyl-imidazolidin-2-ones of general formula (I) ##STR1## wherein n is 1, 2 or 3; 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; R.sub.3 is an imidazolyl group of formula ##STR2## wherein each of R.sub.8 and R.sub.10 which may be the same or different is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.9 is hydrogen, C.sub.1 -C.sub.6 alkyl or a nitrogen protecting group, or pharmaceutically acceptable salts thereof, which are useful in the treatment of CNS disorders, such as, e.g., anxiety and psychosis, and in the treatment of gut motility disorders, and/or emesis.
摘要翻译：本发明涉及通式（I）的单咪唑烷基-3-苯基 - 咪唑烷-2-酮的新衍生物，其中n为1,2或3; 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，其中R 4和R 5各自独立地是C 1 -C 6烷基甲酰基或C 2 -C 6烷酰基的C 1 -C 6烷氧基羰基，硝基，-N（R 4 R 5）或（R6R7）N-SO2基团，其中R6和R7各自独立地为氢或C1-C6烷基; R3是式IMAMA的咪唑基，其中R 8和R 10可以相同或不同的是氢或C 1 -C 6烷基，R 9是氢，C 1 -C 6烷基或氮保护基，或其药学上可接受的盐，其可用于治疗中枢神经系统疾病，例如焦虑和精神病，以及肠道运动障碍和/或呕吐的治疗。

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