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公开(公告)号：US08314119B2
公开(公告)日：2012-11-20
申请号：US11935157
申请日：2007-11-05
申请人： Michael R. Schrimpf , Diana L. Nersesian , Kevin B. Sippy , Jianguo Ji , Tao Li , Marc Scanio , Lei Shi , Chih-Hung Lee , William H. Bunnelle , Geoff G. Z. Zhang , Paul J. Brackemeyer , Shuang Chen , Rodger F. Henry
发明人： Michael R. Schrimpf , Diana L. Nersesian , Kevin B. Sippy , Jianguo Ji , Tao Li , Marc Scanio , Lei Shi , Chih-Hung Lee , William H. Bunnelle , Geoff G. Z. Zhang , Paul J. Brackemeyer , Shuang Chen , Rodger F. Henry
IPC分类号： A61K31/439 , C07D221/22
CPC分类号： C07D471/18 , A61K31/095 , A61K31/439 , A61K31/444 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07C309/29 , C07D451/14 , C07D471/08 , C07F5/022
摘要： The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.
摘要翻译： 本发明涉及作为氮杂金刚烷衍生物的化合物，特别是醚取代或胺取代的氮杂金刚烷衍生物及其盐和前体药物，包含这些化合物的组合物，使用这些化合物和组合物的方法，制备这些化合物的方法以及在此过程中获得的中间体 。
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公开(公告)号：US20080167336A1
公开(公告)日：2008-07-10
申请号：US11935157
申请日：2007-11-05
申请人： Michael R. Schrimpf , Diana L. Nersesian , Kevin B. Sippy , Jianguo Ji , Tao Li , Marc Scanio , Lei Shi , Chih-Hung Lee , William H. Bunnelle , Geoff G.Z. Zhang , Paul J. Brackemeyer , Shuang Chen , Rodger F. Henry
发明人： Michael R. Schrimpf , Diana L. Nersesian , Kevin B. Sippy , Jianguo Ji , Tao Li , Marc Scanio , Lei Shi , Chih-Hung Lee , William H. Bunnelle , Geoff G.Z. Zhang , Paul J. Brackemeyer , Shuang Chen , Rodger F. Henry
IPC分类号： A61K31/439 , C07D471/08 , C07F5/02
CPC分类号： C07D471/18 , A61K31/095 , A61K31/439 , A61K31/444 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07C309/29 , C07D451/14 , C07D471/08 , C07F5/022
摘要： The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.
摘要翻译： 本发明涉及作为氮杂金刚烷衍生物的化合物，特别是醚取代或胺取代的氮杂金刚烷衍生物及其盐和前体药物，包含这些化合物的组合物，使用这些化合物和组合物的方法，制备这些化合物的方法以及在此过程中获得的中间体 。
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公开(公告)号：US09625475B2
公开(公告)日：2017-04-18
申请号：US12727723
申请日：2010-03-19
申请人： Michael R. Schrimpf , Chih-Hung Lee , Tao Li , Gregory A. Gfesser , Kathleen H. Mortell , Ramin Faghih , Diana L. Nersesian , Kevin B. Sippy , William H. Bunnelle , Marc Scanio , Lei Shi , Murali Gopalakrishnan , Diana L. Donnelly-Roberts , Min Hu
发明人： Michael R. Schrimpf , Chih-Hung Lee , Tao Li , Gregory A. Gfesser , Kathleen H. Mortell , Ramin Faghih , Diana L. Nersesian , Kevin B. Sippy , William H. Bunnelle , Marc Scanio , Lei Shi , Murali Gopalakrishnan , Diana L. Donnelly-Roberts , Min Hu
IPC分类号： A61K31/55 , C07D487/00 , C07D491/00 , C07D498/00 , C07D513/00 , C07D515/00 , G01N33/68 , C07D471/18 , C07D487/10 , G01N33/50
CPC分类号： G01N33/6896 , C07D471/18 , C07D487/10 , G01N33/5058 , G01N2800/2814 , G01N2800/30
摘要： The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
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公开(公告)号：US09063126B2
公开(公告)日：2015-06-23
申请号：US12568085
申请日：2009-09-28
申请人： Michael R. Schrimpf , Chih-Hung Lee , Tao Li , Gregory A. Gfesser , Kathleen H. Mortell , Ramin Faghih , Diana L. Nersesian , Kevin B. Sippy , William H. Bunnelle , Marc Scanio , Lei Shi , Murali Gopalakrishnan , Diana L. Donnelly-Roberts , Min Hu
发明人： Michael R. Schrimpf , Chih-Hung Lee , Tao Li , Gregory A. Gfesser , Kathleen H. Mortell , Ramin Faghih , Diana L. Nersesian , Kevin B. Sippy , William H. Bunnelle , Marc Scanio , Lei Shi , Murali Gopalakrishnan , Diana L. Donnelly-Roberts , Min Hu
IPC分类号： A61K31/439 , C07D471/08 , G01N33/50 , C07D471/18 , C07D487/10 , C07D487/18 , G01N33/68
CPC分类号： G01N33/5058 , C07D471/18 , C07D487/10 , C07D487/18 , G01N33/6896 , G01N2800/28 , G01N2800/30
摘要： The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
摘要翻译： 本申请涉及式（I），（II），（III），（IV），（V）或（VI）的吲哚和二氢吲哚衍生物，其中a，R1，R2，R3，R4，R5， V，W，X，Y和Z如说明书中所定义。 本申请还涉及包含这些化合物的组合物，以及使用这些化合物和组合物治疗疾病状况的方法，以及鉴定这些化合物的方法。
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公开(公告)号：US20100249105A1
公开(公告)日：2010-09-30
申请号：US12727723
申请日：2010-03-19
申请人： Michael R. Schrimpf , Chih-Hung Lee , Tao Li , Gregory A. Gfesser , Kathleen H. Mortell , Ramin Faghih , Diana L. Nersesian , Kevin B. Sippy , William H. Bunnelle , Marc Scanio , Lei Shi , Murali Gopalakrishnan , Diana L. Donnelly-Roberts , Min Hu
发明人： Michael R. Schrimpf , Chih-Hung Lee , Tao Li , Gregory A. Gfesser , Kathleen H. Mortell , Ramin Faghih , Diana L. Nersesian , Kevin B. Sippy , William H. Bunnelle , Marc Scanio , Lei Shi , Murali Gopalakrishnan , Diana L. Donnelly-Roberts , Min Hu
IPC分类号： A61K31/55 , A61P25/28 , A61P25/16 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/02 , C07D487/04 , A61K31/439 , C07D471/00
CPC分类号： G01N33/6896 , C07D471/18 , C07D487/10 , G01N33/5058 , G01N2800/2814 , G01N2800/30
摘要： The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
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公开(公告)号：US20100087471A1
公开(公告)日：2010-04-08
申请号：US12568085
申请日：2009-09-28
申请人： Michael R. Schrimpf , Chih-Hung Lee , Tao Li , Gregory A. Gfesser , Kathleen H. Mortell , Ramin Faghih , Diana L. Nersesian , Kevin B. Sippy , William H. Bunnelle , Marc Scanio , Lei Shi , Murali Gopalakrishnan , Diana L. Donnelly-Roberts , Min Hu
发明人： Michael R. Schrimpf , Chih-Hung Lee , Tao Li , Gregory A. Gfesser , Kathleen H. Mortell , Ramin Faghih , Diana L. Nersesian , Kevin B. Sippy , William H. Bunnelle , Marc Scanio , Lei Shi , Murali Gopalakrishnan , Diana L. Donnelly-Roberts , Min Hu
IPC分类号： A61K31/439 , C12Q1/02 , C07D471/08
CPC分类号： G01N33/5058 , C07D471/18 , C07D487/10 , C07D487/18 , G01N33/6896 , G01N2800/28 , G01N2800/30
摘要： The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
摘要翻译： 本申请涉及式（I），（II），（III），（IV），（V）或（VI）的吲哚和二氢吲哚衍生物，其中a，R1，R2，R3，R4，R5， V，W，X，Y和Z如说明书中所定义。 本申请还涉及包含这些化合物的组合物，以及使用这些化合物和组合物治疗疾病状况的方法，以及鉴定这些化合物的方法。
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公开(公告)号：US07399765B2
公开(公告)日：2008-07-15
申请号：US10942035
申请日：2004-09-16
申请人： William H. Bunnelle , Jianguo Ji , Tao Li , Jennifer M. Pace , Karin R. Tietje , Kathleen H. Mortell , Diana L. Nersesian , Michael R. Schrimpf
发明人： William H. Bunnelle , Jianguo Ji , Tao Li , Jennifer M. Pace , Karin R. Tietje , Kathleen H. Mortell , Diana L. Nersesian , Michael R. Schrimpf
IPC分类号： A61K31/501 , A61K31/5025 , A61K31/4427 , A61K31/42 , A61K31/4436 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D471/04 , C07D491/04 , C07D498/04 , C07D513/04 , C07D515/04 , A61P29/00 , C07D231/12 , C07D417/04 , C07D285/08 , C07D285/12 , C07D239/42 , C07D263/34 , C07D413/02 , C07D413/14 , C07D271/107 , C07D487/04 , C07D215/12 , C07D261/12 , C07D401/14 , C07D413/04 , C07D23/56 , A61K31/41 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/4245 , A61K31/441 , A61K31/422 , A61K31/4155
CPC分类号： A61K31/501 , A61K31/4178 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/53
摘要： Compounds of formula (I) Z-Ar1—Ar2 (I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.
摘要翻译： 式（I）化合物<？in-line-formula description =“In-line Formulas”end =“lead”？> Z-Ar 1 -Ar 2 I）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中Z是二氮杂双环胺，Ar 1是5或6元芳环 和Ar 2 2选自未取代或取代的5或6元杂芳基环; 未取代或取代的双环杂芳基环; 3,4-（亚甲二氧基）苯基; 咔唑基; 四氢咔唑基; 萘基; 和苯基; 其中苯基在间位或对位被0,1,2或3个取代基取代。 该化合物可用于治疗由α7nAChR配体预防或改善的病症或病症。 还公开了包含式（I）化合物和使用这些化合物和组合物的方法的药物组合物。
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公开(公告)号：US07365193B2
公开(公告)日：2008-04-29
申请号：US11051437
申请日：2005-02-04
申请人： Michael R. Schrimpf , Kevin B. Sippy , Jianguo Ji , Tao Li , Jennifer M. Frost , Clark A. Briggs , William H. Bunnelle
发明人： Michael R. Schrimpf , Kevin B. Sippy , Jianguo Ji , Tao Li , Jennifer M. Frost , Clark A. Briggs , William H. Bunnelle
IPC分类号： C07D245/00 , A01N43/00 , A61K31/33 , A61K31/397 , A61K31/407
CPC分类号： C07D453/02 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/14 , C07D209/88 , C07D211/14 , C07D243/08 , C07D333/76 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D451/06 , C07D487/04 , C07D487/08
摘要： Compounds of formula (I) wherein A and B are amine-substituted sidechains, Y1 and Y2 form various tricyclic cores, Xa and Xb are C, CH, or N, as defined herein, and Rx is an optional substituent. Compounds and compositions of formula (I) are contemplated as well as methods for treating conditions or disorders prevented by or ameliorated by α7nAChR ligands that encompass compounds of formula (I) and other tricyclic derivatives. Methods of using amino-substituted tricyclic derivatives also are described herein.
摘要翻译： 其中A和B是胺取代的侧链，Y 1和Y 2的式（I）化合物形成各种三环核，X 1和 如本文所定义，C 1-6烷基是C，CH或N，并且R x是任选的取代基。 考虑式（I）的化合物和组合物以及用于治疗由包括式（I）化合物和其它三环衍生物的α7nAChR配体防止或改善的病症或病症的方法。 使用氨基取代的三环衍生物的方法也在本文中描述。
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公开(公告)号：US07951791B2
公开(公告)日：2011-05-31
申请号：US12046599
申请日：2008-03-12
申请人： Michael R. Schrimpf , Kevin B. Sippy , Jianguo Ji , Tao Li , Jennifer M. Frost , Clark A. Briggs , William H. Bunnelle
发明人： Michael R. Schrimpf , Kevin B. Sippy , Jianguo Ji , Tao Li , Jennifer M. Frost , Clark A. Briggs , William H. Bunnelle
IPC分类号： A01N43/00 , A01N43/62 , A61K31/33 , C07D245/00 , C07D487/00 , C07D243/00 , C07D491/00 , C07D498/00
CPC分类号： C07D453/02 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/14 , C07D209/88 , C07D211/14 , C07D243/08 , C07D333/76 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D451/06 , C07D487/04 , C07D487/08
摘要： Compounds of formula (I) wherein A and B are amine-substituted sidechains, Y1 and Y2 form various tricyclic cores, Xa and Xb are C, CH, or N, as defined herein, and Rx is an optional substituent. Compounds and compositions of formula (I) are contemplated as well as methods for treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands that encompass compounds of formula (I) and other tricyclic derivatives. Methods of using amino-substituted tricyclic derivatives also are described herein.
摘要翻译： 其中A和B是胺取代的侧链的式（I）化合物，Y1和Y2形成各种三环核，Xa和Xb是如本文所定义的C，CH或N，并且Rx是任选的取代基。 考虑式（I）的化合物和组合物以及用于治疗由包括式（I）化合物和其它三环衍生物的α7nAChR配体防止或改善的病症或病症的方法。 使用氨基取代的三环衍生物的方法也在本文中描述。
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公开(公告)号：US20080161281A1
公开(公告)日：2008-07-03
申请号：US12046599
申请日：2008-03-12
申请人： Michael R. Schrimpf , Kevin B. Sippy , Jianguo Ji , Tao Li , Jennifer M. Frost , Clark A. Briggs , William H. Bunnelle
发明人： Michael R. Schrimpf , Kevin B. Sippy , Jianguo Ji , Tao Li , Jennifer M. Frost , Clark A. Briggs , William H. Bunnelle
IPC分类号： A61K31/397 , C07D205/02 , C07D207/00 , A61K31/40 , C07D243/14 , A61K31/5513 , C07D333/52 , A61K31/381 , C07D209/82 , A61K31/403 , C07D221/00 , A61K31/445 , C07D295/00 , A61K31/496 , A61P25/00
CPC分类号： C07D453/02 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/14 , C07D209/88 , C07D211/14 , C07D243/08 , C07D333/76 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D451/06 , C07D487/04 , C07D487/08
摘要： Compounds of formula (I) wherein A and B are amine-substituted sidechains, Y1 and Y2 form various tricyclic cores, Xa and Xb are C, CH, or N, as defined herein, and Rx is an optional substituent. Compounds and compositions of formula (I) are contemplated as well as methods for treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands that encompass compounds of formula (I) and other tricyclic derivatives. Methods of using amino-substituted tricyclic derivatives also are described herein.
摘要翻译： 其中A和B是胺取代的侧链，Y 1和Y 2的式（I）化合物形成各种三环核，X 1和 如本文所定义，C 1-6烷基是C，CH或N，并且R x是任选的取代基。 考虑式（I）的化合物和组合物以及用于治疗由包括式（I）化合物和其它三环衍生物的α7nAChR配体防止或改善的病症或病症的方法。 使用氨基取代的三环衍生物的方法也在本文中描述。
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