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1. 发明授权

US07858646B2 Potentiators of glutamate receptors 有权
标题翻译：谷氨酸受体的增效剂
公开(公告)号：US07858646B2
公开(公告)日：2010-12-28
申请号：US11718446
申请日：2005-11-15
申请人： Thomas Daniel Aicher , Dana Rae Benesh , Maria-Jesus Blanco-Pillado , Guillermo S. Cortez , Todd Michael Groendyke , Albert Khilevich , James Allen Knobelsdorf , Fredrik Pehr Marmsäter , Jeffrey Michael Schkeryantz , Tony Pisal Tang
发明人： Thomas Daniel Aicher , Dana Rae Benesh , Maria-Jesus Blanco-Pillado , Guillermo S. Cortez , Todd Michael Groendyke , Albert Khilevich , James Allen Knobelsdorf , Fredrik Pehr Marmsäter , Jeffrey Michael Schkeryantz , Tony Pisal Tang
IPC分类号： C07D401/04 , C07D213/79 , A61K31/41 , A61K31/4439
CPC分类号： C07C229/60 , C07C317/44 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/70 , C07D213/79 , C07D213/80 , C07D213/84 , C07D213/85 , C07D257/04 , C07D401/04 , C07D401/12
摘要： The present invention provides compounds of formula (I); pharmaceutical compositions thereof, and methods of using the same, processes or preparing the same, and intermediates thereof.
摘要翻译：本发明提供式（I）化合物; 其药物组合物及其使用方法，方法或制备方法及其中间体。

2. 发明授权

US07291632B2 Substituted 2-carbonylamino-6-piperidinaminopyridines and substituted 1-carbonylamino-3-piperidinaminobenzenes as 5-HT1F agonists 有权
公开(公告)号：US07291632B2
公开(公告)日：2007-11-06
申请号：US10569109
申请日：2004-09-03
申请人： Maria-Jesus Blanco-Pillado , Michael Philip Cohen , Sandra Ann Filla , Kevin John Hudziak , Daniel Timothy Kohlman , Dana Rae Benesh , Frantz Victor , Yao-Chang Xu , Bai-Ping Ying , DeAnna Piatt Zacherl , Deyi Zhang , Brian Michael Mathes
发明人： Maria-Jesus Blanco-Pillado , Michael Philip Cohen , Sandra Ann Filla , Kevin John Hudziak , Daniel Timothy Kohlman , Dana Rae Benesh , Frantz Victor , Yao-Chang Xu , Bai-Ping Ying , DeAnna Piatt Zacherl , Deyi Zhang , Brian Michael Mathes
IPC分类号： A61K31/445 , C07D211/32 , C07D211/72 , C07D421/00
CPC分类号： C07D211/58 , A61K31/4468 , A61K31/4523 , C04B35/632 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14
摘要： The present invention relates to compounds of formula I: (I) or a pharmaceutically acceptable acid addition salt thereof, where; X is C(R3c═ or N═; R1 is C2–C6 alkyl, substituted C2–C6 alkyl, C3–C7 cycloalkyl, substituted C3–C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1–C3 n-alkyl, C3–C6 cycloalkyl-C1–C3 alkyl, or a group of formula II (II) provided that when R1 is C2–C6 alkyl or substituted C2–C6 alkyl, R2 is hydrogen or methyl; R3a, R3b, and, when X is C(R3c)═, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1–C3 alkyl; R5 is hydrogen, C1–C3 alkyl, or C3–C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1–C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal.

3. 发明申请

US20110034511A1 SUBSTITUTED 2-CARBONYLAMINO-6-PIPERIDINAMINOPYRIDINES AND SUBSTITUTED 1-CARBONYLAMINO-3-PIPERIDINAMINOBENZENES AS 5-HT1F AGONISTS 审中-公开
标题翻译：取代的2-碳酰氨基-6-哌啶氨基吡啶和取代的1-碳代氨基-3-哌啶甲酰苯胺作为5-HT1F激动剂
公开(公告)号：US20110034511A1
公开(公告)日：2011-02-10
申请号：US12892433
申请日：2010-09-28
申请人： Maria-Jesus Blanco-Pillado , Michael Philip Cohen , Sandra Ann Filla , Kevin John Hudziak , Daniel Timothy Kohlman , Dana Rae Benesh , Frantz Victor , Yao-Chang Xu , Bai-Ping Ying , DeAnna Piatt Zacherl , Deyi Zhang , Brian Michael Mathes
发明人： Maria-Jesus Blanco-Pillado , Michael Philip Cohen , Sandra Ann Filla , Kevin John Hudziak , Daniel Timothy Kohlman , Dana Rae Benesh , Frantz Victor , Yao-Chang Xu , Bai-Ping Ying , DeAnna Piatt Zacherl , Deyi Zhang , Brian Michael Mathes
IPC分类号： A61K31/4468 , C07D211/58 , C07D401/06 , C07D409/12 , C07D401/12 , C07D401/14 , A61K31/454 , A61K31/4545 , A61P25/06
CPC分类号： C07D211/58 , A61K31/4468 , A61K31/4523 , C04B35/632 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14
摘要： The present invention relates to compounds of formula I: or a pharmaceutically acceptable acid addition salt thereof, wherein X is C(R3c)═ or N═; R1 is C2-C6 alkyl, substituted C2-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 n-alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II provided that when R1 is C2-C6 alkyl or substituted C2-C6 alkyl, R2 is hydrogen or methyl; R3a, R3b and, when X is —C(R3c)═, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1-C3 alkyl; R5 is hydrogen, C1-C3 alkyl, or C3-C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal.
摘要翻译：本发明涉及式I化合物或其药学上可接受的酸加成盐，其中X为C（R3c）=或N =; R 1是C 2 -C 6烷基，取代的C 2 -C 6烷基，C 3 -C 7环烷基，取代的C 3 -C 7环烷基，苯基，取代的苯基，杂环或取代的杂环; R 2是氢，C 1 -C 3正烷基，C 3 -C 6环烷基-C 1 -C 3烷基或式II基团，条件是当R 1是C 2 -C 6烷基或取代的C 2 -C 6烷基时，R 2是氢或甲基; R3a，R3b，并且当X是-C（R3c）= R3c时，R3c各自独立地为氢，氟或甲基，条件是R3a，R3b和R3c中不超过一个可以不是氢; R4是氢或C1-C3烷基; R5是氢，C1-C3烷基或C3-C6环烷基羰基，条件是当R3a不是氢时，R5是氢; R6是氢或C1-C6烷基; n为1〜6的整数。本发明的化合物可用于活化5HT1F受体，抑制神经元蛋白质外渗，以及治疗或预防哺乳动物偏头痛。

4. 发明授权

US07196100B2 Opioid receptor antagonists 有权
标题翻译：阿片受体拮抗剂
公开(公告)号：US07196100B2
公开(公告)日：2007-03-27
申请号：US10581164
申请日：2004-12-06
申请人： Dana Rae Benesh , Maria-Jesus Blanco-Pillado
发明人： Dana Rae Benesh , Maria-Jesus Blanco-Pillado
IPC分类号： A61K31/445 , A61K31/165 , A61K31/44 , A61K31/435 , C07D211/68
CPC分类号： C07C235/46 , C07C2601/14 , C07D211/46 , C07D213/80 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12
摘要： A compound of the formula (I) wherein the variables X1 to X5, R1 to R7 including R3′, E, q, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed
摘要翻译：式（I）的化合物，其中变量X 1至X 5，R 1至R 7，包括R 3'，E，q，v，y，z，A和B如上所述，或其药学上可接受的盐，溶剂合物，对映异构体，外消旋体，非对映异构体或其混合物，可用于治疗公布了预防或改善肥胖及相关疾病

5. 发明授权

US07803813B2 Substituted 2-carbonylamino-6-piperidinaminopyridines and substituted 1-carbonylamino-3-piperidinaminobenzenes as 5-HT1F agonists 有权
标题翻译：取代的2-羰基氨基-6-哌啶基氨基吡啶和取代的1-羰基氨基-3-哌啶基氨基苯作为5-HT1F激动剂
公开(公告)号：US07803813B2
公开(公告)日：2010-09-28
申请号：US11810388
申请日：2007-06-04
申请人： Maria-Jesus Blanco-Pillado , Dana Rae Benesh
发明人： Maria-Jesus Blanco-Pillado , Dana Rae Benesh
IPC分类号： A61K31/445 , C07D211/56
CPC分类号： C07D211/58 , A61K31/4468 , A61K31/4523 , C04B35/632 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14
摘要： The present invention relates to compounds of formula I: or a pharmaceutically acceptable acid addition salt thereof, wherein X is C(R3c)═ or N═; R1 is C2-C6 alkyl, substituted C2-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 n-alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II provided that when R1 is C2-C6 alkyl or substituted C2-C6 alkyl, R2 is hydrogen or methyl; R3a, R3b and, when X is —C(R3c)═, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1-C3 alkyl; R5 is hydrogen, C1-C3 alkyl, or C3-C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal.
摘要翻译：本发明涉及式I化合物或其药学上可接受的酸加成盐，其中X为C（R3c）=或N =; R 1是C 2 -C 6烷基，取代的C 2 -C 6烷基，C 3 -C 7环烷基，取代的C 3 -C 7环烷基，苯基，取代的苯基，杂环或取代的杂环; R 2是氢，C 1 -C 3正烷基，C 3 -C 6环烷基-C 1 -C 3烷基或式II基团，条件是当R 1是C 2 -C 6烷基或取代的C 2 -C 6烷基时，R 2是氢或甲基; R3a，R3b，并且当X是-C（R3c）= R3c时，R3c各自独立地为氢，氟或甲基，条件是R3a，R3b和R3c中不超过一个可以不是氢; R4是氢或C1-C3烷基; R5是氢，C1-C3烷基或C3-C6环烷基羰基，条件是当R3a不是氢时，R5是氢; R6是氢或C1-C6烷基; n为1〜6的整数。本发明的化合物可用于活化5HT1F受体，抑制神经元蛋白质外渗，以及治疗或预防哺乳动物偏头痛。

6. 发明授权

US07608629B2 (Piperidinyloxy)phenyl, (piperidinyloxy)pyridinyl, (piperidinylsulfanyl)phenyl and (piperidinylsulfanyl)pyridinyl compounds as 5-HT1F agonists 失效
标题翻译：（哌啶基氧基）苯基，（哌啶基氧基）吡啶基，（哌啶基硫烷基）苯基和（哌啶基硫烷基）吡啶基化合物作为5-HT1F激动剂
公开(公告)号：US07608629B2
公开(公告)日：2009-10-27
申请号：US10552131
申请日：2004-04-14
申请人： Maria-Jesus Blanco-Pillado , Dana Rae Benesh , Sandra Ann Filla , Kevin John Hudziak , Brian Michael Mathes , Daniel Timothy Kohlman , Bai-Ping Ying , Deyi Zhang , Yao-Chang Xu
发明人： Maria-Jesus Blanco-Pillado , Dana Rae Benesh , Sandra Ann Filla , Kevin John Hudziak , Brian Michael Mathes , Daniel Timothy Kohlman , Bai-Ping Ying , Deyi Zhang , Yao-Chang Xu
IPC分类号： A61K31/4545 , C07D401/14
CPC分类号： C07D401/12 , C07D211/44 , C07D211/46 , C07D211/54 , C07D401/14 , C07D409/12 , C07D409/14
摘要： The present invention relates to compounds of formula 1: and pharmaceutically acceptable acid addition sails thereof. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or preverition of migraine in mammals, particularly humans.
摘要翻译：本发明涉及式1的化合物及其药学上可接受的酸加成口。本发明的化合物可用于激活5-HT1F受体，抑制神经元蛋白质外渗，以及在哺乳动物，特别是人中治疗或预防偏头痛。

7. 发明申请

US20080096930A1 Potentiators Of Glutamate Receptors 有权
标题翻译：谷氨酸受体的药剂
公开(公告)号：US20080096930A1
公开(公告)日：2008-04-24
申请号：US11718446
申请日：2005-11-15
申请人： Thomas Aicher , Dana Benesh , Maria-Jesus Blanco-Pillado , Guillermo Cortez , Todd Groendyke , Albert Khilevich , James Knobelsdorf , Fredrik Marmsater , Jeffrey Schkeryantz , Tony Tang
发明人： Thomas Aicher , Dana Benesh , Maria-Jesus Blanco-Pillado , Guillermo Cortez , Todd Groendyke , Albert Khilevich , James Knobelsdorf , Fredrik Marmsater , Jeffrey Schkeryantz , Tony Tang
IPC分类号： A61K31/4439 , A61K31/41 , A61P25/06 , C07D213/79 , C07D401/04 , C07D257/04 , C07D213/70 , A61K31/44
CPC分类号： C07C229/60 , C07C317/44 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/70 , C07D213/79 , C07D213/80 , C07D213/84 , C07D213/85 , C07D257/04 , C07D401/04 , C07D401/12
摘要： The present invention provides compounds of formula (I); pharmaceutical compositions thereof, and methods of using the same, processes or preparing the same, and intermediates thereof.
摘要翻译：本发明提供式（I）化合物; 其药物组合物及其使用方法，方法或制备方法及其中间体。

8. 发明申请

US20060287363A1 Substituted 2-carbonylamino-6-piperidinaminopyridines and substituted 1-carbonylamino-3-piperidinaminobenzenes as 5-ht 1f agonists 有权
公开(公告)号：US20060287363A1
公开(公告)日：2006-12-21
申请号：US10569109
申请日：2004-09-03
申请人： Maria-Jesus Blanco-Pillado , Michael Cohen , Sandra Filla , Kevin Hudzlak , Daniel Kohlman , Dana Benesh , Frantz Victor , Yao-Chang Xu , Bai-Ping Ying , DeAnna Zacherl , Deyi Zhang , Brian Mathes
发明人： Maria-Jesus Blanco-Pillado , Michael Cohen , Sandra Filla , Kevin Hudzlak , Daniel Kohlman , Dana Benesh , Frantz Victor , Yao-Chang Xu , Bai-Ping Ying , DeAnna Zacherl , Deyi Zhang , Brian Mathes
IPC分类号： A61K31/4545 , A61K31/454 , C07D403/14
CPC分类号： C07D211/58 , A61K31/4468 , A61K31/4523 , C04B35/632 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14
摘要： The present invention relates to compounds of formula I: (I) or a pharmaceutically acceptable acid addition salt thereof, where; X is C(R3c═ or N═; R1 is C2-C6 alkyl, substituted C2-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 n-alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II (II) provided that when R1 is C2-C6 alkyl or substituted C2-C6 alkyl, R2 is hydrogen or methyl; R3a, R3b, and, when X is C(R3c)═, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1-C3 alkyl; R5 is hydrogen, C1-C3 alkyl, or C3-C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal.

9. 发明申请

US20060211734A1 (Piperidinyloxy)phenyl, (piperidinyloxy)pyridinyl, (piperidinylsulfanyl)phenyl and (piperidinylsulfanyl)pyridinyl compounds as 5-ht1f agonists 失效
标题翻译：（哌啶基氧基）苯基，（哌啶基氧基）吡啶基，（哌啶基硫烷基）苯基和（哌啶基硫烷基）吡啶基化合物作为5-ht1f激动剂
公开(公告)号：US20060211734A1
公开(公告)日：2006-09-21
申请号：US10552131
申请日：2004-04-14
申请人： Maria-Jesus Blanco-Pillado , Dana Benesh , Sandra Filla , Kevin Hudziak , Brian Mathes , Daniel Kohlman , Bai-Ping Ying , Deyl Zhang , Yao-Chang Xu
发明人： Maria-Jesus Blanco-Pillado , Dana Benesh , Sandra Filla , Kevin Hudziak , Brian Mathes , Daniel Kohlman , Bai-Ping Ying , Deyl Zhang , Yao-Chang Xu
IPC分类号： A61K31/4545 , A61K31/454 , C07D401/14 , C07D403/14
CPC分类号： C07D401/12 , C07D211/44 , C07D211/46 , C07D211/54 , C07D401/14 , C07D409/12 , C07D409/14
摘要： The present invention relates to compounds of formula 1: and pharmaceutically acceptable acid addition sails thereof. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or preverition of migraine in mammals, particularly humans.
摘要翻译：本发明涉及式1的化合物及其药学上可接受的酸加成口。本发明的化合物可用于激活5-HT 1F受体，抑制神经元蛋白质外渗，以及在哺乳动物，特别是人中治疗或预防偏头痛。

10. 发明申请

US20080255152A1 DIARYL ETHERS AS OPIOID RECEPTOR ANTAGONISTS 有权
标题翻译： DIARYL ETHERS作为阿片受体拮抗剂
公开(公告)号：US20080255152A1
公开(公告)日：2008-10-16
申请号：US12052994
申请日：2008-03-21
申请人： Maria-Jesus Blanco-Pillado , Mark Donald Chappell , Marta Garcia De La Torre , Nuria Diaz Buezo , James Erwin Fritz , William Glen Holloway , James Edward Matt , Charies Howard Mitch , Concepcion Pedregal-Tercero , Steven James Quimby , Miles Goodman Siegel , Dana Rae Smith , Russell Dean Stucky , Kumiko Takeuchi , Elizabeth Marie Thomas , Chad Nolan Wolfe
发明人： Maria-Jesus Blanco-Pillado , Mark Donald Chappell , Marta Garcia De La Torre , Nuria Diaz Buezo , James Erwin Fritz , William Glen Holloway , James Edward Matt , Charies Howard Mitch , Concepcion Pedregal-Tercero , Steven James Quimby , Miles Goodman Siegel , Dana Rae Smith , Russell Dean Stucky , Kumiko Takeuchi , Elizabeth Marie Thomas , Chad Nolan Wolfe
IPC分类号： A61K31/497
CPC分类号： C07D213/643 , C07C235/46 , C07D213/38 , C07D213/64 , C07D213/78 , C07D213/81 , C07D213/82 , C07D217/02 , C07D217/04 , C07D237/24 , C07D239/34 , C07D241/24 , C07D307/14 , C07D307/52 , C07D333/20 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： A compound of the formula (I) wherein the variables X1 to X10, R1 to R7 including R3′, E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.
摘要翻译：式（I）的化合物，其中变量X 1至X 10，R 1至R 7，包括R 3，E，V，Y，Z，A和B如上所述，或其药学上可接受的盐，溶剂合物，对映异构体，外消旋体，非对映体或其混合物，可用于治疗，预防或改善肥胖及相关疾病。

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