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1. 发明申请

WO2007071311A1 2 -PHENYLETHYLAMINO DERIVATIVES AS CALCIUM AND/OR SODIUM CHANNEL MODULATORS 审中-公开
标题翻译：作为钙和/或钠通道调节剂的2-苯乙烯胺衍生物
公开(公告)号：WO2007071311A1
公开(公告)日：2007-06-28
申请号：PCT/EP2006/011443
申请日：2006-11-29
申请人： NEWRON PHARMACEUTICALS S.P.A. , THALER, Florian , NAPOLETANO, Mauro , SABIDO-DAVID, Cibele , MORIGGI, Ermanno , CACCIA, Carla , FARAVELLI, Laura , RESTIVO, Alessandra , SALVATI, Patricia
发明人： THALER, Florian , NAPOLETANO, Mauro , SABIDO-DAVID, Cibele , MORIGGI, Ermanno , CACCIA, Carla , FARAVELLI, Laura , RESTIVO, Alessandra , SALVATI, Patricia
IPC分类号： C07D237/06 , C07D295/18 , C07D307/52 , C07D295/08 , C07D309/06 , C07D307/14 , C07D261/08 , C07D213/30 , C07D213/38 , A61K31/33 , A61K31/165 , A61P25/00 , A61P9/00 , A61P13/00 , A61P27/00
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, R, R 0 R 1 , R 2 , R 3 , and R 4 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，R 0，R 1，R 2，R 3和R 2 > 4 具有本说明书及其药学上可接受的盐中所定义的含义，含有它们作为活性成分的药物组合物及其作为钠和/或钙通道调节剂的用途，其可用于预防缓解和治愈多种病变，描述了上述机制已被描述为发挥病理作用的神经，精神，心血管，炎症，眼科，泌尿科和胃肠道疾病。

2. 发明申请

WO2005054189A1 N-ACYL-N'-BENZYL-ALKYLENDIAMINO DERIVATIVES 审中-公开
标题翻译： N-乙酰基-N'-苄基-L-鸟氨酸衍生物
公开(公告)号：WO2005054189A1
公开(公告)日：2005-06-16
申请号：PCT/EP2004/012834
申请日：2004-11-12
申请人： NEWRON PHARMACEUTICALS S.P.A. , THALER, Florian , SABIDO DAVID, Cibele, Maria , FARAVELLI, Laura , GAGLIARDI, Stefania , COLOMBO, Elena , SALVATI, Patricia
发明人： THALER, Florian , SABIDO DAVID, Cibele, Maria , FARAVELLI, Laura , GAGLIARDI, Stefania , COLOMBO, Elena , SALVATI, Patricia
IPC分类号： C07D207/267
CPC分类号： C07D207/27 , C07C233/36
摘要： This invention is related to compounds and use of N-Acyl-N'-benzyl-alkylendiamino derivatives of the following general formula (I), wherein A is a straight or branched C 2 -C 8 alkyl chain; X is a methylene, oxygen, sulphur or a NR 7 group; R 1 is a straight or branched C 1 -C 8 alkyl or C 3 -C 8 alkenylene or C 3 -C 8 alkynylene chain, optionally substituted with CF 3 , phenyl, phenoxy or naphthyl, the aromatic rings optionally substituted by one or more C 1 -C 4 alkyl, halogens, trifluoromethyl, hydroxy or C 1 -C 4 alkoxy groups; R 2 , R 3 are independently hydrogen, a C 1 -C 3 alkyl chain, halogen, trifluoromethyl, hydroxy or C 1 -C 4 alkoxy groups; R 4 , R 5 are independently hydrogen or C 1 -C 6 alkyl; R 6 is a hydrogen or a straight or branched C 1 -C 8 alkyl or linked to R 5 can form a five to seven membered lactam; R 7 is hydrogen or C 1 -C 6 alkyl; and the pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators 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：本发明涉及以下通式（I）的N-酰基-N'-苄基 - 烷基二氨基衍生物的化合物和用途，其中A为直链或支链C 2 -C 8烷基链; X是亚甲基，氧，硫或NR 7基团; R 1是任选被CF 3，苯基，苯氧基或萘基取代的直链或支链C 1 -C 8烷基或C 3 -C 8亚烯基或C 3 -C 8亚炔基，任选被一个或多个C 1 -C 4烷基取代的芳环，卤素，三氟甲基，羟基或C 1 -C 4烷氧基; R 2，R 3独立地是氢，C 1 -C 3烷基链，卤素，三氟甲基，羟基或C 1 -C 4烷氧基; R 4，R 5独立地是氢或C 1 -C 6烷基; R 6是氢或直链或支链C 1 -C 8烷基或连接至R 5可以形成5至7元的内酰胺; R 7是氢或C 1 -C 6烷基; 其作为钠和/或钙通道调节剂具有活性的药学上可接受的盐，因此可用于预防，减轻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，泌尿系统，代谢和胃肠道疾病，其中上述机制被描述为发挥病理作用。

3. 发明申请

WO2005040138A1 SUBSTITUTED BENZYLAMINOALKYLENE HETEROCYCLES 审中-公开
标题翻译：取代的苯甲酰氨基烯烃杂环化合物
公开(公告)号：WO2005040138A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/011104
申请日：2004-10-05
申请人： NEWRON PHARMACEUTICALS S.P.A. , SALVATI, Patricia , CACCIA, Carla , MELLONI, Piero , RESTIVO, Alessandra , SABIDO DAVID, Cibele , VALLESE, Stefania
发明人： SALVATI, Patricia , CACCIA, Carla , MELLONI, Piero , RESTIVO, Alessandra , SABIDO DAVID, Cibele , VALLESE, Stefania
IPC分类号： C07D261/02
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 NR 7 group; R 1 is C 3 -C 8 alkyl, or C 1 -C 8 alkyl substituted by phenoxy or phenyl, both phenoxy or phenyl being optionally substituted by one or more fluoro, chloro, trifluoromethyl, C 1 -C 6 alkyl, hydroxyl, C 1 -C 6 alkoxy; R 2 , R 3 are independently hydrogen, C 1 -C 6 alkyl, halogen, trifluoromethyl, hydroxy or C 1 -C 6 alkoxy; R 4 is hydrogen, C 1 -C 8 alkyl; R 5 , R 6 are independently hydrogen, C 1 -C 3 alkyl, optionally substituted by hydroxy or phenyl; R 7 is hydrogen or straight or branched C 1 -C 3 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 C 1 -C 6 alkyl, halogen, hydroxyl or C 1 -C 6 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; R 2，R 3独立地是氢，C 1 -C 6烷基，卤素，三氟甲基，羟基或C 1 -C 6烷氧基; R 4是氢，C 1 -C 8烷基; R 5，R 6独立地是氢，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抑制剂具有活性，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。

4. 发明申请

WO2008151702A1 SUBSTITUTED 2- [2- (PHENYL) ETHYLAMINO] ALKANEAMIDE DERIVATIVES AND THEIR USE AS SODIUM AND/OR CALCIUM CHANNEL MODULATORS 审中-公开
标题翻译：取代的2- [2-（苯基）乙酰胺]烷基胺衍生物及其作为钠和/或钙通道调节剂的用途
公开(公告)号：WO2008151702A1
公开(公告)日：2008-12-18
申请号：PCT/EP2008/003848
申请日：2008-05-14
申请人： NEWRON PHARMACEUTICALS S.P.A. , MELLONI, Piero , RESTIVO, Alessandra , IZZO, Emanuela , FRANCISCONI, Simona , COLOMBO, Elena , SABIDO-DAVID, Cibele
发明人： MELLONI, Piero , RESTIVO, Alessandra , IZZO, Emanuela , FRANCISCONI, Simona , COLOMBO, Elena , SABIDO-DAVID, Cibele
IPC分类号： C07C237/06 , A61K31/165 , C07D295/182
CPC分类号： A61K31/381 , A61K31/137 , A61K31/165 , A61K31/40 , A61K31/4515 , A61K31/519 , A61K31/5513 , C07C237/06 , C07C237/08 , C07C237/20 , C07C317/28 , C07C321/26 , C07C323/25 , C07C327/42 , C07C327/44 , C07D207/16 , C07D295/182 , C07D333/20
摘要： Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives of formula (I) wherein X, Y, Z, R, R 1 , R 2 , R 3 , R' 3 , R 4 , R 5 , R 6 , R 7 have the meanings 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, but not limited to, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
摘要翻译：其中X，Y，Z，R，R 1，R 2，R 3，R'3，R 4，R 5，R 6，R 7的取代的式（I）的2- [2-（苯基）乙基氨基]烷酰胺衍生物具有含有它们作为活性成分的药物组合物及其作为钠和/或钙通道调节剂的用途，可用于预防，减轻和治愈广泛范围的病症，包括但不限于神经学，认知功能，精神病学，炎症，泌尿生殖和胃肠道疾病，其中上述机制已被描述为发挥病理作用。

5. 发明申请

WO2005054178A1 CYCLOPENTYL DERIVATIVES 审中-公开
标题翻译：环戊二烯衍生物
公开(公告)号：WO2005054178A1
公开(公告)日：2005-06-16
申请号：PCT/EP2004/012835
申请日：2004-11-12
申请人： NEWRON PHARMACEUTICALS S.p.A. , MELLONI, Piero , SABIDO DAVID, Cibele, Maria , RESTIVO, Alessandra , FORLANI, Roberto , SALVATI, Patricia
发明人： MELLONI, Piero , SABIDO DAVID, Cibele, Maria , RESTIVO, Alessandra , FORLANI, Roberto , SALVATI, Patricia
IPC分类号： C07C237/24
CPC分类号： C07C237/24 , C07C2601/08
摘要： This invention is related to novel cyclopentyl derivatives of the following general Formula (I), wherein X is methylene, oxygen, sulphur or a NR 7 group; R 1 is a straight or branched C 1 -C 8 alkyl or C 3 -C 8 alkenylene or C 3 -C 8 alkynylene chain, optionally substituted with CF 3 , phenyl, phenoxy or naphthyl, the aromatic rings optionally substituted by one or more C 1 -C 4 alkyl, halogens, trifluoromethyl, hydroxy or C 1 -C 4 alkoxy groups; R 2 , R 3 are independently hydrogen, a C 1 -C 3 alkyl chain, halogen, trifluoromethyl, hydroxy or C 1 -C 4 alkoxy groups; R 4 , R 5, R 6 , R 7 are independently hydrogen or C 1 -C 6 alkyl; and the pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefor 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：本发明涉及以下通式（I）的新环戊基衍生物，其中X为亚甲基，氧，硫或NR 7基团; R 1是任选被CF 3，苯基，苯氧基或萘基取代的直链或支链C 1 -C 8烷基或C 3 -C 8亚烯基或C 3 -C 8亚炔基，任选被一个或多个C 1 -C 4烷基取代的芳环，卤素，三氟甲基，羟基或C 1 -C 4烷氧基; R 2，R 3独立地是氢，C 1 -C 3烷基链，卤素，三氟甲基，羟基或C 1 -C 4烷氧基; R 4，R 5，R 6，R 7独立地是氢或C 1 -C 6烷基; 其作为钠和/或钙通道调节剂具有活性的药学上可接受的盐，其可用于预防，减轻和治愈广泛范围的病症，包括但不限于神经性，精神病学，心血管疾病，炎症性，眼科，泌尿系统，代谢和胃肠道疾病，其中上述机制被描述为发挥病理作用。

6. 发明申请

WO2005054206A1 HISTIDINE DERIVATIVES 审中-公开
公开(公告)号：WO2005054206A1
公开(公告)日：2005-06-16
申请号：PCT/EP2004/012944
申请日：2004-11-15
申请人： NEWRON PHARMACEUTICALS S.P.A. , MELLONI, Piero , SABIDO DAVID, Cibele, Maria , FARAVELLI, Laura , MAESTRONI, Sara , DONDIO, Giulio , SALVATI, Patricia
发明人： MELLONI, Piero , SABIDO DAVID, Cibele, Maria , FARAVELLI, Laura , MAESTRONI, Sara , DONDIO, Giulio , SALVATI, Patricia
IPC分类号： C07D233/64
CPC分类号： C07D233/64
摘要： This invention is related to novel histidine derivatives of the following general formula (I), wherein X is methylene, oxygen, sulphur or a NR 8 group; R 1 is a straight or branched C 1 -C 8 alkyl or C 3 -C 8 alkenylene or C 3 -C 8 alkynylene chain, optionally substituted with CF 3 , phenyl, phenoxy or naphthyl, the aromatic rings optionally substituted by one or more C 1 -C 4 alkyl, halogens, trifluoromethyl, hydroxy or C 1 -C 4 alkoxy groups; R 2 , R 3 are independently hydrogen, a C 1 -C 3 alkyl chain, halogen, trifluoromethyl, hydroxy or C 1 -C 4 alkoxy groups; R 4 , R 5 , R 6 , R 7 , R 8 are independently hydrogen or C 1 -C 4 alkyl; and the pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, psychiatric, cardiovascular, inflammatory, ophtalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
摘要翻译：本发明涉及以下通式（I）的新型组氨酸衍生物，其中X为亚甲基，氧，硫或NR 8基团; R 1是任选被CF 3，苯基，苯氧基或萘基取代的直链或支链C 1 -C 8烷基或C 3 -C 8亚烯基或C 3 -C 8亚炔基，任选被一个或多个C 1 -C 4烷基取代的芳环，卤素，三氟甲基，羟基或C 1 -C 4烷氧基; R 2，R 3独立地是氢，C 1 -C 3烷基链，卤素，三氟甲基，羟基或C 1 -C 4烷氧基; R 4，R 5，R 6，R 7，R 8独立地是氢或C 1 -C 4烷基; 其作为钠和/或钙通道调节剂具有活性的药学上可接受的盐，因此可用于预防，减轻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，眼底，泌尿系统，代谢和胃肠道疾病，其中上述机制被描述为发挥病理作用。

7. 发明申请

WO2005054190A1 3-AMINOPYRROLIDONE DERIVATIVES 审中-公开
标题翻译： 3-氨基吡咯烷酮衍生物
公开(公告)号：WO2005054190A1
公开(公告)日：2005-06-16
申请号：PCT/EP2004/012957
申请日：2004-11-16
申请人： NEWRON PHARMACEUTICALS S.p.A. , THALER, Florian , SABIDO DAVID, Cibele, Maria , MAESTRONI, Sara , RAVEGLIA, Luca, Francesco , SALVATI, Patricia
发明人： THALER, Florian , SABIDO DAVID, Cibele, Maria , MAESTRONI, Sara , RAVEGLIA, Luca, Francesco , SALVATI, Patricia
IPC分类号： C07D207/273
CPC分类号： C07D207/273 , A61K31/4015 , A61K31/4412 , A61K31/55 , C07D211/76
摘要： This invention is related to compounds and use of 3-aminopyrrolidone derivatives and analogues of the following general formula (I), wherein m is an integer from 1 to 3; X is methylene, oxygen, sulphur or a NR 6 group; R 1 is a straight or branched C 1 -C 8 alkyl or C 3 -C 8 alkenylene or C 3 -C 8 alkynylene chain, optionally substituted with CF 3 , phenyl, phenoxy or naphthyl, or phenyl the aromatic rings optionally substituted by one or more C 1 -C 4 alkyl, halogens, trifluoromethyl, hydroxy or C 1 -C 4 alkoxy groups; R 2 , R 3 are independently hydrogen, a C 1 -C 3 alkyl chain, halogen, trifluoromethyl, hydroxy or C 1 -C 4 alkoxy groups; R 4 , R 5 , R 6 are independently hydrogen or C 1 -C 6 alkyl; and the pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
摘要翻译：本发明涉及以下通式（I）的3-氨基吡咯烷酮衍生物和类似物的化合物和用途，其中m为1至3的整数; X是亚甲基，氧，硫或NR 6基团; R 1是任选被CF 3，苯基，苯氧基或萘基取代的直链或支链C 1 -C 8烷基或C 3 -C 8亚烯基或C 3 -C 8亚炔基链，或苯基，任选被一个或多个C 1 -C 4 烷基，卤素，三氟甲基，羟基或C 1 -C 4烷氧基; R 2，R 3独立地是氢，C 1 -C 3烷基链，卤素，三氟甲基，羟基或C 1 -C 4烷氧基; R 4，R 5，R 6独立地是氢或C 1 -C 6烷基; 和其药学上可接受的盐，其作为钠和/或钙通道调节剂是有活性的，因此可用于预防，缓解和治愈广泛范围的病理学，包括但不限于心血管，炎症，眼科，泌尿，代谢和胃肠道疾病其中上述机制被描述为发挥病理作用。

8. 发明申请

WO2005040108A1 PROLINAMIDE DERIVATIVES AS SODIUM AND/OR CALCIUM CHANNEL BLOCKERS OR SELECTIVE MAO-B INHIBITORS 审中-公开
标题翻译：丙氨酰胺衍生物作为钠和/或钙通道阻断剂或选择性MAO-B抑制剂
公开(公告)号：WO2005040108A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/011105
申请日：2004-10-05
申请人： NEWRON PHARMACEUTICALS S.P.A. , CACCIA, Carla , LA PORTA, Elena , MAESTRONI, Sara , MELLONI, Piero , SABIDO DAVID, Cibele , SALVATI, Patricia
发明人： CACCIA, Carla , LA PORTA, Elena , MAESTRONI, Sara , MELLONI, Piero , SABIDO DAVID, Cibele , SALVATI, Patricia
IPC分类号： C07D207/16
CPC分类号： C07D401/12 , C07D207/16 , C07D211/60 , C07D223/06
摘要： This invention is related to novel prolinamide derivatives and analogues of general formula (I) wherein Q is C 3 -C 8 alkyl, or C 1 -C 8 alkyl substituted by phenoxy or saturated or unsaturated 5 to 7 membered ring optionally containing one or more heteroatoms chosen independently from nitrogen, oxygen or sulphur, the rings being optionally substituted by one or more halogen atoms, trifluoromethyl, C 1 -C 6 alkyl, hydroxyl, C 1 -C 6 alkoxy; X is an oxygen, sulphur or a NR 5 group; R, R 1 are independently hydrogen, C 1 -C 6 alkyl, halogen, trifluoromethyl, hydroxy or C 1 -C 6 alkoxy; R 2 is hydrogen or hydroxyl; R 3 R 4 R 5 are independently hydrogen or straight or branched C 1 -C 3 alkyl; n is an integer from 1 to 3 and a pharmaceutically acceptable salt or prodrug thereof, that areactive as sodium and/or calcium channel modulators and/or as selective MAOB 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：本发明涉及新的脯氨酰胺衍生物和通式（I）的类似物，其中Q为C 3 -C 8烷基或被苯氧基或饱和或不饱和5至7元环任选地含有一个或多个独立地选自以下的杂原子取代的C 1 -C 8烷基：氮，氧或硫，所述环任选被一个或多个卤素原子，三氟甲基，C 1 -C 6烷基，羟基，C 1 -C 6烷氧基取代; X是氧，硫或NR 5基团; R 1，R 2独立地是氢，C 1 -C 6烷基，卤素，三氟甲基，羟基或C 1 -C 6烷氧基; R 2是氢或羟基; R 3 R 4独立地是氢或直链或支链C 1 -C 3烷基; n是1至3的整数及其药学上可接受的盐或前药，其作为钠和/或钙通道调节剂和/或作为选择性MAOB抑制剂起作用，因此可用于预防，减轻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，泌尿系，代谢和胃肠道疾病，其中上述机制已被描述为发挥病理作用。

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