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公开(公告)号：US5424328A
公开(公告)日：1995-06-13
申请号：US144514
申请日：1993-11-02
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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2.发明授权Derivatives of substituted imidazo benzoxazin-1-one and process for their preparation 失效取代的咪唑并苯并恶嗪-1-酮的衍生物及其制备方法
公开(公告)号：US5364854A
公开(公告)日：1994-11-15
申请号：US70860
申请日：1993-06-03
IPC分类号： A61K31/535 , A61P25/26 , C07D498/04 , C07D519/00 , C07D487/04 , A61K35/00
CPC分类号： C07D519/00 , Y10S514/872
摘要： Derivatives of 2,3,3a,4-tetrahydro-2-azabicyclo alkyl-1H-imidazo[5,1,-c][1,4]benzoxazin-1-one are provided of general formula (I) ##STR1## in which inter alia R.sub.3 represents ##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, which are useful in the treatment of CNS disorders, gut motility disorders, emesis and migraine, as cognition activators, anti-drug addiction agents and analgesic.
摘要翻译： 2,3,3a，4-四氢-2-氮杂双环烷基-1H-咪唑并[5,1，-c] [1,4]苯并恶嗪-1-酮的衍生物由通式（I）提供。 I），其中特别是R3表示
其中n是1或2的整数，R8是氢，未被取代或被苯基，C 2 -C 4烯基，C 2 -C 4炔基，甲酰基或C 2 -C 6取代的C 1 -C 6烷基 烷酰基; 及其药学上可接受的盐，其可用于治疗CNS障碍，肠蠕动障碍，呕吐和偏头痛，作为认知激活剂，抗药成瘾剂和止痛剂。 -
3.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
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：US5874457A
公开(公告)日：1999-02-23
申请号：US578550
申请日：1996-01-24
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。
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5.发明授权Imidazolylakyl derivatives of imidazo �5,1-c!�1,4!benzoxazin-1-one process for their preparation 失效咪唑并[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
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。
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公开(公告)号：US06087371A
公开(公告)日：2000-07-11
申请号：US125108
申请日：1998-08-17
IPC分类号： C07D457/00 , C07D457/02 , A61K37/437 , C07D471/04
CPC分类号： C07D457/02 , C07D457/00
摘要： Ergoline derivative having formula (I) wherein R.sub.1 is hydrogen atom or C.sub.1-4 alkyl group; R.sub.2 is hydrogen, chlorine, or bromine atom, methyl or C.sub.1-4 alkylthio group; n is 0, 1 or 2; the substituent at position 8 is in .alpha. or .beta. configuration; Het represents an aromatic 5-membered heterocyclic ring, said ring having three heteroatoms which are the same or different and which are selected from the group consisting of sulfur, oxygen and nitrogen atom and X is hydrogen, chlorine or bromine or fluorine atom, or a pharmaceutically acceptable acid addition salt thereof are active at the Central Nervous System level. A process for their preparation is also described, as are pharmaceutical compositions containing them. ##STR1##
摘要翻译： PCT No.PCT / EP97 / 00582 Sec。 371日期1998年8月17日 102（e）日期1998年8月17日PCT 1997年2月7日提交PCT公布。 公开号WO97 / 30050 PCT 日期：1997年8月21日具有式（I）的衍生物，其中R 1为氢原子或C 1-4烷基; R2是氢，氯或溴原子，甲基或C1-4烷硫基; n为0,1或2; 位置8处的取代基是α或β构型; Het表示芳族5元杂环，所述环具有三个相同或不同的杂原子，选自硫，氧和氮原子，X是氢，氯或溴或氟原子，或 其药学上可接受的酸加成盐在中枢神经系统水平上是有活性的。 还描述了其制备方法，以及含有它们的药物组合物。
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7.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
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。
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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。
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9.发明申请2-Phenylethylamino Derivatives as Calcium and/or Sodium Channel Modulators 有权2-苯基乙基氨基衍生物作为钙和/或钠通道调节剂公开(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。
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公开(公告)号：US20060116329A1
公开(公告)日：2006-06-01
申请号：US10536307
申请日：2003-11-25
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。
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