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1. 发明专利

IL186852D0 BENZOIC ACID DERIVATIVES THAT ARE MODULATORS OR AGONISTS OF GLYR 未知
公开(公告)号：IL186852D0
公开(公告)日：2008-02-09
申请号：IL18685207
申请日：2007-10-22
申请人： ASTRAZENECA AB , NIKLAS PLOBECK , MARKUS HAEBERLEIN , GYBACK HELENA , JONASSON CATRIN , KIHLSTROM JACOB , MOLIN HAKAN DECEASED , HETTMAN ANDREAS , VIKLUND JENNY , YNGVE ULRIKA
IPC分类号： C07C20100101
摘要： Compounds of formula I, wherein R1, Z, Y, M and R2 are as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical composition containing the same, methods of using the same for therapeutic purposes and methods of making the same.

2. 发明申请

US20090192190A1 Benzoic Acid Derivatives that are Modulators or Agonists of GlyR 审中-公开
标题翻译：作为GlyR的调节剂或激动剂的苯甲酸衍生物
公开(公告)号：US20090192190A1
公开(公告)日：2009-07-30
申请号：US11912552
申请日：2006-05-08
申请人： Helena Gyback , Markus Haeberlein , Catrin Jonasson , Jacob Kihlstrom , Hakan Molin , Berit Molin , Niklas Plobeck , Andreas Hettman , Jenny Viklund , Ulrika Yngve
发明人： Helena Gyback , Markus Haeberlein , Catrin Jonasson , Jacob Kihlstrom , Hakan Molin , Berit Molin , Niklas Plobeck , Andreas Hettman , Jenny Viklund , Ulrika Yngve
IPC分类号： A61K31/47 , C07C65/01 , A61K31/192 , A61K31/44 , C07D213/70 , C07D215/14 , A61P25/00
CPC分类号： C07C323/62 , C07C65/105 , C07C65/24 , C07C65/40 , C07C205/45 , C07C229/64 , C07C251/48 , C07C255/57 , C07C317/46 , C07C2601/14 , C07D213/32 , C07D213/34 , C07D213/55 , C07D213/70 , C07D215/14 , C07D217/16 , C07D241/42 , C07D271/06 , C07D277/36 , C07D277/64 , C07D295/155 , C07D307/80 , C07D309/04 , C07D333/60
摘要： Compounds of formula I, wherein R1, Z, Y, M and R2 are as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical composition containing the same, methods of using the same for therapeutic purposes and methods of making the same.
摘要翻译：式I的化合物，其中R 1，Z，Y，M和R 2如说明书中所定义，其药学上可接受的盐，含有该化合物的药物组合物，其用于治疗目的的方法及其制备方法。

3. 发明申请

US20070270435A1 Novel Compounds 失效
标题翻译：新型化合物
公开(公告)号：US20070270435A1
公开(公告)日：2007-11-22
申请号：US11743824
申请日：2007-05-03
申请人： William Brown , Christopher Walpole , Niklas Plobeck , Thomas Hudzik
发明人： William Brown , Christopher Walpole , Niklas Plobeck , Thomas Hudzik
IPC分类号： A61K31/496 , A61P25/24 , A61P43/00 , C07D295/00
CPC分类号： C07D295/155 , C07D233/24 , C07D307/52 , C07D333/20
摘要： The invention relates to at least one compound of general formula I wherein R1 is phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, or pyridine N-oxide, where each R1 phenyl and R1 heteroaromatic ring may optionally and independently be substituted by 1, 2 or 3 substituents selected from CF3, methyl, iodo, bromo, fluoro, and chloro; R2 is independently selected from ethyl and isopropyl; R3 is hydrogen or fluoro; R4 is —NH2 or —NHSO2R5; and R5 is hydrogen, —CF3, or C1-C6 alkyl, or pharmaceutically acceptable salts thereof, at least one process for making at least one compound in accordance with Formula I; at least one method for treating at least one δ receptor associated condition with at least one compound in accordance with Formula I; and at least one pharmaceutical composition comprising at least one compound in accordance with Formula I.
摘要翻译：本发明涉及至少一种通式I的化合物，其中R 1是苯基，吡啶基，噻吩基，呋喃基，咪唑基，吡咯基，三唑基，噻唑基或吡啶N-氧化物，其中每个R 0 > 1苯基和R 1 - 杂芳环可以任选地和独立地被1,2或3个选自CF 3，甲基，碘，溴，氟和氯; R 2独立地选自乙基和异丙基; R 3是氢或氟; R 4是-NH 2或-NHSO 2 R 5; 和R 5是氢，-CF 3或C 1 -C 6烷基，或其药学上可接受的盐至少一种根据式I制备至少一种化合物的方法; 用至少一种根据式I的化合物治疗至少一种δ受体相关病症的方法; 和包含至少一种根据式I的化合物的至少一种药物组合物。

4. 发明授权

US06696447B2 Hydroxyphenyl-piperazinyl-methyl-benzamide derivatives for the treatment of pain 失效
标题翻译：羟苯基 - 哌嗪基 - 甲基 - 苯甲酰胺衍生物用于治疗疼痛
公开(公告)号：US06696447B2
公开(公告)日：2004-02-24
申请号：US10240037
申请日：2002-09-27
申请人： William Brown , Niklas Plobeck , Christopher Walpole
发明人： William Brown , Niklas Plobeck , Christopher Walpole
IPC分类号： A61K31496
CPC分类号： C07D295/155 , C07D307/52 , C07D333/20
摘要： The present application describes compounds of general formula I where R1 is selected from any one of pyridinyl, thienyl, furanyl, imidazolyl, and triazolyl; and where each R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the heteroaromatic ring may take place in any position on the ring system. The invention also includes enantiomers, salts and pharmaceutical compositions containing the compounds. The compounds may be used in treating patients for pain.
摘要翻译：本申请描述了通式I的化合物，其中R 1选自吡啶基，噻吩基，呋喃基，咪唑基和三唑基中的任一个;并且其中每个R 1杂芳环可以任选和独立地被1,2取代或3个选自直链和支链C 1 -C 6烷基，NO 2，CF 3，C 1 -C 6烷氧基，氯，氟，溴和碘的取代基。杂芳环上的取代可以在环系统上的任何位置进行。本发明还包括含有这些化合物的对映异构体，盐和药物组合物。该化合物可用于治疗患者的疼痛。

5. 发明申请

US20070299087A1 New Compounds 319 审中-公开
标题翻译：新化合物319
公开(公告)号：US20070299087A1
公开(公告)日：2007-12-27
申请号：US11761131
申请日：2007-06-11
申请人： Stefan Berg , Jorg Holenz , Katharina Hogdin , Karin Kolmodin , Niklas Plobeck , Didier Rotticci , Fernando Sehgelmeble
发明人： Stefan Berg , Jorg Holenz , Katharina Hogdin , Karin Kolmodin , Niklas Plobeck , Didier Rotticci , Fernando Sehgelmeble
IPC分类号： C07D487/02 , A61K31/519 , C12N5/00 , A61P25/00
CPC分类号： C07D487/04
摘要： This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译：本发明涉及具有以下结构式I的新化合物及其药学上可接受的盐，组合物和使用方法。这些新化合物提供了认知障碍，阿尔茨海默病，神经变性和痴呆症的治疗或预防。

6. 发明申请

US20070254890A1 4(Phenyl-Piperazinyl-Methyl) Benzamide Derivatives and Their Use for the Treatment of Pain or Gastrointestinal Disorders 失效
标题翻译： 4（苯基 - 哌嗪基 - 甲基）苯甲酰胺衍生物及其用于治疗疼痛或胃肠道疾病
公开(公告)号：US20070254890A1
公开(公告)日：2007-11-01
申请号：US11774935
申请日：2007-07-09
申请人： William Brown , Andrew Griffin , Paul Jones , Daniel Page , Niklas Plobeck , Christopher Walpole
发明人： William Brown , Andrew Griffin , Paul Jones , Daniel Page , Niklas Plobeck , Christopher Walpole
IPC分类号： A61K31/4965 , A61P1/00
CPC分类号： C07D213/38 , C07D215/12 , C07D233/64 , C07D277/28 , C07D295/155 , C07D307/52 , C07D333/20
摘要： Compounds of general formula: wherein R1, R2 and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
摘要翻译：其中R 1，R 2和R 3的通式如本说明书中所定义，以及其盐，对映体和制备包含该化合物的药物组合物。它们可用于治疗，特别是治疗疼痛。

7. 发明申请

US20060167004A1 4(Phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders 失效
标题翻译： 4（苯基 - 哌嗪基 - 甲基）苯甲酰胺衍生物及其用于治疗疼痛或胃肠道疾病的用途
公开(公告)号：US20060167004A1
公开(公告)日：2006-07-27
申请号：US10533744
申请日：2003-11-05
申请人： Willliam Brown , Andrew Griffin , Niklas Plobeck , Christopher Walpole
发明人： Willliam Brown , Andrew Griffin , Niklas Plobeck , Christopher Walpole
IPC分类号： A61K31/496 , A61K31/495 , C07D417/02 , C07D409/02 , C07D403/02
CPC分类号： C07D295/155 , C07D307/52
摘要： Compounds of general formula: wherein R1 and R2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
摘要翻译：制备其中R 1和R 2的化合物如说明书中所定义，以及其盐，对映异构体和包含该化合物的药物组合物。它们可用于治疗，特别是治疗疼痛。

8. 发明授权

US06680321B1 Compounds with analgesic effect 失效
标题翻译：化合物具有镇痛作用
公开(公告)号：US06680321B1
公开(公告)日：2004-01-20
申请号：US09631116
申请日：2000-08-02
申请人： Edward Roberts , Niklas Plobeck , Claes Wahlestedt
发明人： Edward Roberts , Niklas Plobeck , Claes Wahlestedt
IPC分类号： A61K31495
CPC分类号： C07D295/185 , A61K31/495 , A61K31/496 , C07C2601/14 , C07D215/14 , C07D295/096 , C07D295/112 , C07D295/135 , C07D295/155 , C07D295/205 , C07D307/81
摘要： Compounds of the formula (I) as well as their pharmaceutically acceptable salts, and pharmaceutical compositions comprising the novel compounds. The novel compounds of the formula (I) are useful in the management of pain.
摘要翻译：式（I）化合物及其药学上可接受的盐，以及包含新化合物的药物组合物。式（I）的新化合物可用于治疗疼痛。

9. 发明授权

US07960389B2 4(phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders 失效
标题翻译： 4（苯基 - 哌嗪基 - 甲基）苯甲酰胺衍生物及其用于治疗疼痛或胃肠道疾病的用途
公开(公告)号：US07960389B2
公开(公告)日：2011-06-14
申请号：US11774935
申请日：2007-07-09
申请人： William Brown , Andrew Griffin , Paul Jones , Daniel Page , Niklas Plobeck , Christopher Walpole
发明人： William Brown , Andrew Griffin , Paul Jones , Daniel Page , Niklas Plobeck , Christopher Walpole
IPC分类号： A61K31/4965 , A61P25/22 , C07D295/03
CPC分类号： C07D213/38 , C07D215/12 , C07D233/64 , C07D277/28 , C07D295/155 , C07D307/52 , C07D333/20
摘要： Compounds of general formula: wherein R1, R2 and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
摘要翻译：制备通式如下的化合物：其中R 1，R 2和R 3如本说明书中所定义，以及其盐，对映异构体和包含该化合物的药物组合物。它们可用于治疗，特别是治疗疼痛。

10. 发明授权

US07915413B2 Compounds 失效
标题翻译：化合物
公开(公告)号：US07915413B2
公开(公告)日：2011-03-29
申请号：US11743824
申请日：2007-05-03
申请人： William Brown , Christopher Walpole , Niklas Plobeck
发明人： William Brown , Christopher Walpole , Niklas Plobeck
IPC分类号： C07D295/155 , C07D233/64 , C07D333/20 , C07D307/52
CPC分类号： C07D295/155 , C07D233/24 , C07D307/52 , C07D333/20
摘要： The invention relates to at least one compound of general formula I wherein R1 is phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, or pyridine N-oxide, where each R1 phenyl and R1 heteroaromatic ring may optionally and independently be substituted by 1, 2 or 3 substituents selected from CF3, methyl, iodo, bromo, fluoro, and chloro; R2 is independently selected from ethyl and isopropyl; R3 is hydrogen or fluoro; R4 is —NH2 or —NHSO2R5; and R5 is hydrogen, —CF3, or C1-C6 alkyl, or pharmaceutically acceptable salts thereof, at least one process for making at least one compound in accordance with Formula I; at least one method for treating at least one δ receptor associated condition with at least one compound in accordance with Formula I; and at least one pharmaceutical composition comprising at least one compound in accordance with Formula I.
摘要翻译：本发明涉及至少一种通式I的化合物，其中R 1是苯基，吡啶基，噻吩基，呋喃基，咪唑基，吡咯基，三唑基，噻唑基或吡啶N-氧化物，其中每个R 1苯基和R 1杂芳环可任选地和独立地是被1,2或3个选自CF 3，甲基，碘，溴，氟和氯的取代基取代; R2独立地选自乙基和异丙基; R3是氢或氟; R4是-NH2或-NHSO2R5; 和R 5是氢，-CF 3或C 1 -C 6烷基或其药学上可接受的盐，至少一种用于制备至少一种根据式I的化合物的方法; 用至少一种根据式I的化合物治疗至少一种δ受体相关病症的方法; 和包含至少一种根据式I的化合物的至少一种药物组合物。

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