公开(公告)号：US20070270466A1

公开(公告)日：2007-11-22

申请号：US11810388

申请日：2007-06-04

申请人： Maria-Jesus Blanco-Pillado ,  Michael Cohen ,  Sandra Filla ,  Kevin Hudziak ,  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 Hudziak ,  Daniel Kohlman ,  Dana Benesh ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Zacherl ,  Deyi Zhang ,  Brian Mathes

IPC分类号： A61K31/4468 ,  A61K31/4523 ,  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.

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.

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。

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。

公开(公告)号：US20070010558A1

公开(公告)日：2007-01-11

申请号：US10581164

申请日：2004-12-06

申请人： Dana Benesh ,  Maria-Jesus Blanco-Pillado

发明人： Dana Benesh ,  Maria-Jesus Blanco-Pillado

IPC分类号： A61K31/4436 ,  A61K31/4433 ,  A61K31/4415 ,  C07D409/02 ,  C07D405/02 ,  C07D213/78

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 ，公开了预防或改善肥胖症和相关疾病。

公开(公告)号：US20060166987A1

公开(公告)日：2006-07-27

申请号：US10544286

申请日：2004-03-01

申请人： Dana Benesh ,  Maria Blanco-Pillado ,  Charles Mitch ,  Kumiko Takeuchi

发明人： Dana Benesh ,  Maria Blanco-Pillado ,  Charles Mitch ,  Kumiko Takeuchi

IPC分类号： A61K31/5377 ,  A61K31/426 ,  A61K31/381 ,  C07D333/34 ,  C07D277/36

CPC分类号： C07D277/34 ,  C07D307/58 ,  C07D333/32

摘要： A compound of the formula I: (I) wherein the variables are as described herein, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixture thereof, formulations and methods of use thereof are disclosed.

摘要翻译： 公开了其中变量如本文所述的式I化合物或其药学上可接受的盐，溶剂合物，对映异构体，外消旋物，非对映异构体或其混合物，其制剂及其使用方法。