专利检索 ap:("Thomas Daniel Aicher" OR "Zhaogen Chen" OR "Yvan LeHuerou" OR "Fionna Mitchell Martin" OR "Marta Maria Pineiro-Nunez" OR "Vincent Patrick Rocco" OR "Kevin Michael Ruley" OR "John Mehnert Schaus" OR "Patrick Gianpietro Spinazze" OR "David Edward Tupper") AND inv:"Marta Maria Pineiro-Nunez" 第 1 页

1.

发明授权
Piperazine substituted aryl benzodiazepines 有权

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)

2.

发明授权
Piperazine substituted aryl benzodiazepines and their use as dopamine receptor antagonists for the treatment of psychotic disorders 失效

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).

3.

发明申请
2-[4-(PYRAZOL-4-YLALKYL)PIPERAZIN-1-YL]-3-PHENYL PYRAZINES AND PYRIDINES AND 3-[4-(PYRAZOL-4-YLALKYL)PIPERAZIN-1-YL]-2-PHENYL PYRIDINES AS 5-HT7 RECEPTOR ANTAGONISTS 有权
标题翻译： 2- [4-（吡唑-4-基）乙基]哌嗪-1-基] -3-苯基吡咯并吡啶和3- [4-（吡唑-4-基）乙基]哌嗪-1-基] -2-苯基吡啶 5-HT7受体拮抗剂

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。

4.

发明授权
2-[4-(pyrazol-4-ylalkyl)piperazin-1-yl]-3-phenyl pyrazines as 5-HT7 receptor antagonists 有权
标题翻译： 2- [4-（吡唑-4-基烷基）哌嗪-1-基] -3-苯基吡嗪，为5-HT 7受体拮抗剂

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。