公开(公告)号：US5962474A

公开(公告)日：1999-10-05

申请号：US977526

申请日：1997-11-24

申请人： James Edmund Audia ,  Bruce Anthony Dressman ,  James Joseph Droste ,  James Erwin Fritz ,  Stephen Warren Kaldor ,  Daniel James Koch ,  Joseph Herman Krushinski, Jr. ,  Jeffrey Scott Nissen ,  Vincent Patrick Rocco ,  John Mehnert Schaus ,  Dennis Charles Thompson

发明人： James Edmund Audia ,  Bruce Anthony Dressman ,  James Joseph Droste ,  James Erwin Fritz ,  Stephen Warren Kaldor ,  Daniel James Koch ,  Joseph Herman Krushinski, Jr. ,  Jeffrey Scott Nissen ,  Vincent Patrick Rocco ,  John Mehnert Schaus ,  Dennis Charles Thompson

IPC分类号： A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/47 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  A61P25/00 ,  A61P43/00 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D417/14 ,  A61K31/40

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D407/14 ,  C07D409/14 ,  Y02P20/582

摘要： This invention provides novel 5-HT.sub.1F agonists of Formula I ##STR1## where A--B, R,R.sup.1 and X are as defined in the specification, which are useful for the treatment of migraine and associated disorders.

摘要翻译： 本发明提供式I的新型5-HT1F激动剂，其中A-B，R，R 1和X如说明书中所定义，其可用于治疗偏头痛及相关疾病。

公开(公告)号：US5708008A

公开(公告)日：1998-01-13

申请号：US619783

申请日：1996-03-20

申请人： James Edmund Audia ,  Bruce Anthony Dressman ,  James Joseph Droste ,  James Erwin Fritz ,  Stephen Warren Kaldor ,  Daniel James Koch ,  Joseph Herman Krushinski, Jr. ,  Jeffrey Scott Nissen ,  Vincent Patrick Rocco ,  John Mehnert Schaus ,  Dennis Charles Thompson

发明人： James Edmund Audia ,  Bruce Anthony Dressman ,  James Joseph Droste ,  James Erwin Fritz ,  Stephen Warren Kaldor ,  Daniel James Koch ,  Joseph Herman Krushinski, Jr. ,  Jeffrey Scott Nissen ,  Vincent Patrick Rocco ,  John Mehnert Schaus ,  Dennis Charles Thompson

IPC分类号： A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/47 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  A61P25/00 ,  A61P43/00 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D417/14

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D407/14 ,  C07D409/14 ,  Y02P20/582

摘要： This invention provides novel 5-HT.sub.1F agonists of Formula I ##STR1## where A--B, R, R.sup.1 and X are as defined in the specification, which are useful for the treatment of migraine and associated disorders.

摘要翻译： 本发明提供式I的新型5-HT1F激动剂，其中A-B，R，R 1和X如说明书中所定义，其可用于治疗偏头痛及相关疾病。

公开(公告)号：US07214673B2

公开(公告)日：2007-05-08

申请号：US10505805

申请日：2003-03-17

申请人： Thomas Daniel Aicher ,  Zhaogen Chen ,  Joseph Herman Krushinski, Jr. ,  Yvan Le Huerou ,  Marta Maria Pineiro-Nunez ,  Kevin Michael Ruley ,  John Mehnert Schaus ,  Dennis Charles Thompson ,  David Edward Tupper ,  Ying Chen ,  Margaret Mary Faul ,  Vincent Patrick Rocco

发明人： Thomas Daniel Aicher ,  Zhaogen Chen ,  Joseph Herman Krushinski, Jr. ,  Yvan Le Huerou ,  Marta Maria Pineiro-Nunez ,  Kevin Michael Ruley ,  John Mehnert Schaus ,  Dennis Charles Thompson ,  David Edward Tupper ,  Ying Chen ,  Margaret Mary Faul ,  Vincent Patrick Rocco

IPC分类号： A61P25/00 ,  A61K31/55 ,  C07D243/10

CPC分类号： C07D487/04 ,  C07D243/38 ,  C07D495/04 ,  C07D513/04

摘要： Described herein are antipyschotic compounds of formula (I) wherein, A is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S; Alk is (C1-4) alkylene optionally substituted with OH, methoxy, ethoxy, or F; Ar is optionally substituted phenyl, naphthyl, monocyclic heteroaromatic, or bicyclic heteroaromatic; R1 is hydrogen or (C1-4) alkyl optionally substituted with OH, OR3, or OCH2CH2OH, wherein R3 is (C1-2) alkyl; R2 is H, (C1-6) alkyl, halogen, fluorinated (C1-6) alkyl, OR4, SR4, NO2, CN, COR4, CONR5R6, SO2NR5R6, NR5R6, NR5COR4, NR5SO2R4, or optionally substituted phenyl, wherein R4 is hydrogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, or optionally substituted phenyl, R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl; Z is one or two substituents independently selected from hydrogen, halogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, SO2NR8R9, NR8SO2R7, NR8R9, or optionally substituted phenyl, wherein R7 is hydrogen, (C1-6) alkyl, fluorinated alkyl, or optionally substituted phenyl, R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl; and salts, solvates, and crystal 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 disorder, and pharmaceutical formulations of the compounds of formula (I).

公开(公告)号：US06864262B2

公开(公告)日：2005-03-08

申请号：US10432413

申请日：2001-11-16

申请人： John Mehnert Schaus ,  Dennis Charles Thompson ,  Karl Bruce Thor

发明人： John Mehnert Schaus ,  Dennis Charles Thompson ,  Karl Bruce Thor

IPC分类号： C07D295/12 ,  A61K31/495 ,  A61K45/06 ,  A61P13/10 ,  C07D295/135

CPC分类号： C07D295/135 ,  A61K31/495 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention provides a compound of the formula (I) and the pharmaceutically acceptable salts and solvates thereof, which is useful for treating bladder over-activity or urinary incontinence.

摘要翻译： 本发明提供式（I）化合物及其药学上可接受的盐和溶剂合物，其可用于治疗膀胱过度活动或尿失禁。

公开(公告)号：US06967201B1

公开(公告)日：2005-11-22

申请号：US10031312

申请日：2000-07-21

申请人： Karin Briner ,  Joseph Paul Burkhart ,  Timothy Paul Burkholder ,  Brian Eugene Cunningham ,  Matthew Joseph Fisher ,  William Harlan Gritton ,  Shawn Christopher Miller ,  Jeffrey Thomas Mullaney ,  Matthew Robert Reinhard ,  Dennis Charles Thompson ,  Leonard Larry Winneroski ,  Yanping Xu

发明人： Karin Briner ,  Joseph Paul Burkhart ,  Timothy Paul Burkholder ,  Brian Eugene Cunningham ,  Matthew Joseph Fisher ,  William Harlan Gritton ,  Shawn Christopher Miller ,  Jeffrey Thomas Mullaney ,  Matthew Robert Reinhard ,  Dennis Charles Thompson ,  Leonard Larry Winneroski ,  Yanping Xu

IPC分类号： A61K31/496 ,  A61K31/551 ,  A61P3/04 ,  A61P25/24 ,  A61P43/00 ,  C07D307/79 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12

CPC分类号： C07D307/79 ,  C07D405/04 ,  C07D405/12

摘要： The present invention provides serotonergic benzofurylpiperazines of Formula I: where: A is a piperazine of formula: and R, R1, R2, R3, R4, R5, R5′, R6, R6′, R7, R7′, R8, and R8′ are as described in the specification.

摘要翻译： 本发明提供式I的5-羟色胺苯并呋喃基哌嗪：其中：A是下式的哌嗪和R 1，R 1，R 2，R 3， R 4，R 5，R 5，R 6，R 6，R 6， R SUP，R 7，R 7，R 8和R 8'如上所述 规格。