公开(公告)号：US07384934B2

公开(公告)日：2008-06-10

申请号：US10523147

申请日：2003-07-28

申请人： Thomas Daniel Aicher ,  Zhaogen Chen ,  Yvan LeHuerou ,  Fionna Mitchell Martin ,  Marta Maria Pineiro-Nunez ,  Vincent Patrick Rocco ,  Kevin Michael Ruley ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  David Edward Tupper

发明人： Thomas Daniel Aicher ,  Zhaogen Chen ,  Yvan LeHuerou ,  Fionna Mitchell Martin ,  Marta Maria Pineiro-Nunez ,  Vincent Patrick Rocco ,  Kevin Michael Ruley ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  David Edward Tupper

IPC分类号： C07D403/04 ,  C07D495/04 ,  C07D513/04 ,  A61K31/55 ,  A61P25/18

CPC分类号： C07D403/04 ,  C07D495/04 ,  C07D513/04

摘要： Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C1-4) alkylene or hydroxy substituted (C1-4) alkylene; X is oxygen or sulfur; R1 is hydrogen, (C1-6) fluroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, or —CN; R2 is H, halogen, (C1-6) fluoroalkyl, (C1-6) cycloalkyl, OR4, SR4, NO2, CN, COR4, C(O)OR4, CONR5R6, NR5R6, SO2NR5R6, NR5COR4, NR5SO2R4, optionally substituted aromatic, or (C1-6) alkyl, wherein (C1-6) alkyl is unsubstituted or substituted with a hydroxy group; R3 is hydrogen (C1-6) fluoroalkyl, (C2-6) alkenyl, Ar, (C1-4)alkyl-Ar, or (C1-4) alkyl wherein (C1-4) alkyly is unsubstituted or substituted with a phenyl; R4 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic, R7 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic; Ar is optionally substituted phenyl, napthyl, monocyclic heteroaromatic or bicyclic heteroaromatic; Z1 and Z2 are independently selected from hydrogen, halogen, (C1-6) alkyl, (C1-6) fluoroalkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, NR8R9, and optionally substituted aromatic; and all salts, solvates, optical and geometric isomers, and crystalline forms thereof. Also, described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treatment of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I)

公开(公告)号：US20100120785A1

公开(公告)日：2010-05-13

申请号：US12597255

申请日：2008-05-07

申请人： Valentina O. Badescu ,  Anne Marie Camp ,  Barry Peter Clark ,  Michael Philip Cohen ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Sarah Lynne Hellman ,  Michael Philip Mazanetz ,  Marta Maria Pineiro-Nunez ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  Maria Ann Whatton

发明人： Valentina O. Badescu ,  Anne Marie Camp ,  Barry Peter Clark ,  Michael Philip Cohen ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Sarah Lynne Hellman ,  Michael Philip Mazanetz ,  Marta Maria Pineiro-Nunez ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  Maria Ann Whatton

IPC分类号： A61K31/497 ,  C07D241/02 ,  A61P25/06

CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine, persistent pain, and anxiety: where A and B are each independently C(H)═ or N═, provided that at least one of A and B is —N═, n is 1-3, m is 0-3, and R14 are as defined herein.

摘要翻译： 本发明提供式I的选择性5-HT7受体拮抗剂化合物及其在治疗偏头痛，持续性疼痛和焦虑中的用途：其中A和B各自独立地为C（H）=或N =，条件是至少一种 A和B为-N =，n为1-3，m为0-3，R 14如本文所定义。

公开(公告)号：US08202873B2

公开(公告)日：2012-06-19

申请号：US12597255

申请日：2008-05-07

申请人： Valentina O. Badescu ,  Anne Marie Camp ,  Barry Peter Clark ,  Michael Philip Cohen ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Sarah Lynne Hellman ,  Michael Philip Mazanetz ,  Marta Maria Pineiro-Nunez ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  Maria Ann Whatton

发明人： Valentina O. Badescu ,  Anne Marie Camp ,  Barry Peter Clark ,  Michael Philip Cohen ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Sarah Lynne Hellman ,  Michael Philip Mazanetz ,  Marta Maria Pineiro-Nunez ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  Maria Ann Whatton

IPC分类号： A61K31/4965

CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine, persistent pain, and anxiety: where A and B are each independently —C(H)═ or —N═, provided that at least one of A and B is —N═, n is 1-3, m is 0-3, and R1-4 are as defined herein.

摘要翻译： 本发明提供式I的选择性5-HT7受体拮抗剂化合物及其在治疗偏头痛，持续性疼痛和焦虑中的用途：其中A和B各自独立地为-C（H）=或-N =，条件是在 A和B中的至少一个为-N =，n为1-3，m为0-3，R1-4如本文所定义。

公开(公告)号：US06844344B2

公开(公告)日：2005-01-18

申请号：US10148658

申请日：2000-12-06

申请人： John Xiaoqiang He ,  Nicholas Allan Honigschmidt ,  Todd Jonathan Kohn ,  Vincent Patrick Rocco ,  Patrick Gianpietro Spinazze ,  Kumiko Takeuchi

发明人： John Xiaoqiang He ,  Nicholas Allan Honigschmidt ,  Todd Jonathan Kohn ,  Vincent Patrick Rocco ,  Patrick Gianpietro Spinazze ,  Kumiko Takeuchi

IPC分类号： A61P25/24 ,  A61P25/34 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14 ,  C07D413/14 ,  A61K31/4545 ,  C07D401/14

CPC分类号： C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14

摘要： The present invention provides compounds of formula (I) which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine

摘要翻译： 本发明提供式（I）化合物，其可用于治疗抑郁症，焦虑症和减轻由于使用烟草或尼古丁而引起的部分戒断或症状

公开(公告)号：US07087635B2

公开(公告)日：2006-08-08

申请号：US11082106

申请日：2005-03-16

申请人： Daniel Jon Sall ,  Jolie Anne Bastian ,  Cynthia Darshini Jesudason ,  Don Richard Finley ,  Freddie Craig Stevens ,  Vincent Patrick Rocco ,  Patrick Gianpietro Spinazze ,  John Xiaoqiang He ,  John Arnold Werner ,  William George Trankle ,  Andrew Michael Ratz ,  Theo Schotten ,  Gerd Reuhter

发明人： Daniel Jon Sall ,  Jolie Anne Bastian ,  Cynthia Darshini Jesudason ,  Don Richard Finley ,  Freddie Craig Stevens ,  Vincent Patrick Rocco ,  Patrick Gianpietro Spinazze ,  John Xiaoqiang He ,  John Arnold Werner ,  William George Trankle ,  Andrew Michael Ratz ,  Theo Schotten ,  Gerd Reuhter

IPC分类号： A61K31/40 ,  A61K31/38 ,  C07D209/54 ,  C07D317/08 ,  C07D409/00

CPC分类号： C07D231/12 ,  C07D209/34 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14

摘要： The present invention relates to a β3 adrenergic receptor agonist of formula I: or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.

摘要翻译： 本发明涉及式I的β3肾上腺素能受体激动剂：或其药用盐; 其能够增加细胞中的脂肪分解和能量消耗，因此可用于治疗2型糖尿病和/或肥胖症。

公开(公告)号：US06911463B2

公开(公告)日：2005-06-28

申请号：US10486508

申请日：2002-08-06

申请人： Daniel Jon Sall ,  Jolie Anne Bastian ,  Cynthia Darshini Jesudason ,  Theo Schotten ,  Gerd Reuhter ,  Don Richard Finley ,  Freddie Craig Stevens ,  Vincent Patrick Rocco ,  Patrick Gianpietro Spinazze ,  John Xiaoqiang He ,  John Arnold Werner ,  William George Trankle ,  Andrew Michael Ratz

发明人： Daniel Jon Sall ,  Jolie Anne Bastian ,  Cynthia Darshini Jesudason ,  Theo Schotten ,  Gerd Reuhter ,  Don Richard Finley ,  Freddie Craig Stevens ,  Vincent Patrick Rocco ,  Patrick Gianpietro Spinazze ,  John Xiaoqiang He ,  John Arnold Werner ,  William George Trankle ,  Andrew Michael Ratz

IPC分类号： A01N41/12 ,  A61K31/4045 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/497 ,  A61P3/04 ,  A61P3/10 ,  C07D209/34 ,  C07D209/96 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14 ,  C07D521/00 ,  A61K31/4035 ,  A61K31/425 ,  C07D209/44 ,  C07D209/54

CPC分类号： C07D231/12 ,  C07D209/34 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14

摘要： The present invention relates to a β3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.

摘要翻译： 本发明涉及式（I）的β3肾上腺素能受体激动剂; 或其药学盐; 其能够增加细胞中的脂肪分解和能量消耗，因此可用于治疗2型糖尿病和/或肥胖症。

公开(公告)号：US07208505B2

公开(公告)日：2007-04-24

申请号：US10486867

申请日：2002-08-06

申请人： Daniel Jon Sall ,  Jolie Anne Bastian ,  Rushad Eruch Karanjawala ,  Cynthia Darshini Jesudason ,  Theo Schotten ,  Britta Evers ,  Gerd Reuhter ,  Don Richard Finley ,  Freddie Craig Stevens ,  Vincent Patrick Rocco ,  Patrick Gianpietro Spinazze ,  John Xiaoqiang He ,  John Arnold Werner ,  William George Trankle ,  Andrew Michael Ratz

发明人： Daniel Jon Sall ,  Jolie Anne Bastian ,  Rushad Eruch Karanjawala ,  Cynthia Darshini Jesudason ,  Theo Schotten ,  Britta Evers ,  Gerd Reuhter ,  Don Richard Finley ,  Freddie Craig Stevens ,  Vincent Patrick Rocco ,  Patrick Gianpietro Spinazze ,  John Xiaoqiang He ,  John Arnold Werner ,  William George Trankle ,  Andrew Michael Ratz

IPC分类号： C07D209/14 ,  C07D213/64 ,  A61K31/404 ,  A61K31/422 ,  A61K31/444

CPC分类号： C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

摘要： The present invention relates to a β3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful, e.g., for treating Type 2 diabetes and/or obesity

摘要翻译： 本发明涉及式（I）的β3肾上腺素能受体激动剂; 或其药学盐; 其能够增加细胞中的脂肪分解和能量消耗，因此可用于例如治疗2型糖尿病和/或肥胖症

公开(公告)号：US07144898B2

公开(公告)日：2006-12-05

申请号：US10149476

申请日：2000-12-06

申请人： Marvin Martin Hansen ,  John Xiaoqiang He ,  Nicholas Allan Honigschmidt ,  Daniel James Koch ,  Todd Jonathan Kohn ,  Vincent Patrick Rocco ,  Patrick Gianpietro Spinazze ,  Kumiko Takeuchi

发明人： Marvin Martin Hansen ,  John Xiaoqiang He ,  Nicholas Allan Honigschmidt ,  Daniel James Koch ,  Todd Jonathan Kohn ,  Vincent Patrick Rocco ,  Patrick Gianpietro Spinazze ,  Kumiko Takeuchi

IPC分类号： A11K31/445

CPC分类号： C07D401/12 ,  C07D409/14 ,  C07D417/14

摘要： The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.

摘要翻译： 本发明提供了式（I）化合物：其可用于治疗抑郁，焦虑和减轻由于使用烟草或尼古丁引起的部分戒断引起的症状。

公开(公告)号：US06835733B2

公开(公告)日：2004-12-28

申请号：US10148768

申请日：2002-09-09

申请人： John Xiaoqiang He ,  Nicholas Allan Honigschmidt ,  Todd Jonathan Kohn ,  Vincent Patrick Rocco ,  Patrick Gianpietro Spinazze ,  Kumiko Takeuchi

发明人： John Xiaoqiang He ,  Nicholas Allan Honigschmidt ,  Todd Jonathan Kohn ,  Vincent Patrick Rocco ,  Patrick Gianpietro Spinazze ,  Kumiko Takeuchi

IPC分类号： C07D40514

CPC分类号： C07D451/02

摘要： The present invention provides compounds of formula (I) which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.

公开(公告)号：US06784180B2

公开(公告)日：2004-08-31

申请号：US10148655

申请日：2002-09-09

申请人： John Xiaoqiang He ,  Nicholas Allan Honigschmidt ,  Todd Jonathan Kohn ,  Vincent Patrick Rocco ,  Patrick Gianpietro Spinazze ,  Kumiko Takeuchi

发明人： John Xiaoqiang He ,  Nicholas Allan Honigschmidt ,  Todd Jonathan Kohn ,  Vincent Patrick Rocco ,  Patrick Gianpietro Spinazze ,  Kumiko Takeuchi

IPC分类号： C07D40904

CPC分类号： C07D409/12 ,  C07D409/14 ,  C07D417/04

摘要： The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.

摘要翻译： 本发明提供了式（I）化合物：其可用于治疗抑郁，焦虑和减轻由于使用烟草或尼古丁引起的部分戒断引起的症状。