公开(公告)号：US20080269296A1

公开(公告)日：2008-10-30

申请号：US12052972

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 ,  Charles 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 ,  Charles 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： A61K31/4433 ,  A61P25/32

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如所述，或其药学上可接受的盐，溶剂化物，对映体，外消旋物，非对映异构体或其混合物，其可用于治疗，预防或改善肥胖症和相关疾病。

公开(公告)号：US07381719B2

公开(公告)日：2008-06-03

申请号：US10526960

申请日：2003-09-17

申请人： Maria-Jesus Blanco-Pillado ,  Marta Garcia De La Torre ,  Nuria Diaz Buezo ,  William Glen Holloway ,  James Edward Matt ,  Charles Howard Mitch ,  Concepcion Pedregal-Tercero ,  Dana Rae Smith ,  Russell Dean Stucky ,  Kumiko Takeuchi

发明人： Maria-Jesus Blanco-Pillado ,  Marta Garcia De La Torre ,  Nuria Diaz Buezo ,  William Glen Holloway ,  James Edward Matt ,  Charles Howard Mitch ,  Concepcion Pedregal-Tercero ,  Dana Rae Smith ,  Russell Dean Stucky ,  Kumiko Takeuchi

IPC分类号： A61K31/54 ,  A61K31/535 ,  A61K31/50 ,  A61K31/497 ,  A61K31/4965 ,  C07D417/00 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D241/02 ,  C07D411/00 ,  C07D413/00 ,  C07D419/00

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

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。

公开(公告)号：US20060217372A1

公开(公告)日：2006-09-28

申请号：US10526960

申请日：2003-09-17

申请人： Maria-Jesus Blanco-Pillado ,  Mark Chappell ,  Marta De La Torre ,  Nuria Diaz Buezo ,  James Fritz ,  William Holloway ,  James Matt ,  Charles Mitch ,  Concepcion Pedregal-Tercero ,  Steven Wuimby ,  Miles Siegel ,  Dana Smith ,  Russell Stucky ,  Kumiko Takeuchi ,  Elizabeth Thomas ,  Chad Wolfe

发明人： Maria-Jesus Blanco-Pillado ,  Mark Chappell ,  Marta De La Torre ,  Nuria Diaz Buezo ,  James Fritz ,  William Holloway ,  James Matt ,  Charles Mitch ,  Concepcion Pedregal-Tercero ,  Steven Wuimby ,  Miles Siegel ,  Dana Smith ,  Russell Stucky ,  Kumiko Takeuchi ,  Elizabeth Thomas ,  Chad Wolfe

IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/501 ,  A61K31/506 ,  A61K31/497 ,  A61K31/496 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

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。

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.

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：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。

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

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。