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公开(公告)号:US06787535B2
公开(公告)日:2004-09-07
申请号:US10164660
申请日:2002-06-06
申请人: Colin Charles Beard , Robin Douglas Clark , Lawrence Emerson Fisher , Ralph New Harris, III , David Bruce Repke , David George Putman
发明人: Colin Charles Beard , Robin Douglas Clark , Lawrence Emerson Fisher , Ralph New Harris, III , David Bruce Repke , David George Putman
IPC分类号: A61K3133
CPC分类号: A61K31/405 , C07D209/30 , C07D401/04 , C07D401/12
摘要: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: wherein one of R5, R6 or R7 is a group of general Formula B, wherein W is a —CH— group or a nitrogen atom, and the other substituents are as defined herein; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
摘要翻译: 本发明涉及通常具有5-HT 6受体亲和性并由式I表示的化合物:其中R 5,R 6或R 7中的一个为通式B的基团,其中W为 -CH-基或氮原子,其它取代基如本文所定义; 或各异构体,异构体的外消旋或非外消旋混合物,或其药学上可接受的盐或溶剂合物。 本发明还涉及含有这些化合物的药物组合物,其用作治疗剂的方法及其制备方法。
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公开(公告)号:US07094778B2
公开(公告)日:2006-08-22
申请号:US10685124
申请日:2003-10-14
申请人: Charles Alois Dvorak , Lawrence Emerson Fisher , Keena Lynn Green , Ralph New Harris, III , Hans Maag , Anthony Prince , David Bruce Repke , Russell Stephen Stabler
发明人: Charles Alois Dvorak , Lawrence Emerson Fisher , Keena Lynn Green , Ralph New Harris, III , Hans Maag , Anthony Prince , David Bruce Repke , Russell Stephen Stabler
IPC分类号: A61K31/513 , C07D279/06 , C07D413/12 , C07D239/10 , C07D241/08
CPC分类号: C07D207/27 , A61K31/55 , A61K31/551 , A61K31/553 , C07D211/76 , C07D223/10 , C07D225/02 , C07D239/10 , C07D241/08 , C07D243/04 , C07D243/08 , C07D265/10 , C07D267/06 , C07D267/10 , C07D267/22 , C07D279/06 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14
摘要: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
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公开(公告)号:US07361648B2
公开(公告)日:2008-04-22
申请号:US11508581
申请日:2006-08-22
申请人: Charles Alois Dvorak , Lawrence Emerson Fisher , Keena Lynn Green , Ralph New Harris, III , Hans Maag , Anthony Prince , David Bruce Repke , Russell Stephen Stabler
发明人: Charles Alois Dvorak , Lawrence Emerson Fisher , Keena Lynn Green , Ralph New Harris, III , Hans Maag , Anthony Prince , David Bruce Repke , Russell Stephen Stabler
IPC分类号: A61K31/395 , A61K31/553 , A61K31/55
CPC分类号: C07D207/27 , A61K31/55 , A61K31/551 , A61K31/553 , C07D211/76 , C07D223/10 , C07D225/02 , C07D239/10 , C07D241/08 , C07D243/04 , C07D243/08 , C07D265/10 , C07D267/06 , C07D267/10 , C07D267/22 , C07D279/06 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14
摘要: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
摘要翻译: 本发明涉及通常为毒蕈碱性M2 / M3受体拮抗剂并由式I表示的化合物:其中X,Y和Z为O,S或NR 5,其它取代基为 在规范中定义; 和前药,各异构体,异构体的外消旋或非外消旋混合物及其药学上可接受的盐或溶剂合物。 本发明还涉及含有这些化合物的药物组合物及其用作治疗剂的方法。
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公开(公告)号:US06667301B2
公开(公告)日:2003-12-23
申请号:US09862286
申请日:2001-05-22
申请人: Charles Alois Dvorak , Lawrence Emerson Fisher , Keena Lynn Green , Ralph New Harris, III , Hans Maag , Anthony Prince , David Bruce Repke , Russell Stephen Stabler
发明人: Charles Alois Dvorak , Lawrence Emerson Fisher , Keena Lynn Green , Ralph New Harris, III , Hans Maag , Anthony Prince , David Bruce Repke , Russell Stephen Stabler
IPC分类号: C07D24108
CPC分类号: C07D207/27 , A61K31/55 , A61K31/551 , A61K31/553 , C07D211/76 , C07D223/10 , C07D225/02 , C07D239/10 , C07D241/08 , C07D243/04 , C07D243/08 , C07D265/10 , C07D267/06 , C07D267/10 , C07D267/22 , C07D279/06 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14
摘要: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
摘要翻译: 本发明涉及通常为毒蕈碱性M2 / M3受体拮抗剂并由式I表示的化合物:其中X,Y和Z为O,S或NR 5,其它取代基如说明书中所定义; 和前药,各异构体,异构体的外消旋或非外消旋混合物及其药学上可接受的盐或溶剂合物。 本发明还涉及含有这些化合物的药物组合物及其用作治疗剂的方法。
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公开(公告)号:US06518460B2
公开(公告)日:2003-02-11
申请号:US10142824
申请日:2002-05-08
IPC分类号: C07C32307
CPC分类号: C07D309/08 , C07C319/14 , C07C319/20 , C07C323/20
摘要: This invention provides processes for the preparation of a compound of Formula I: Y—C(═O)—C(R1)(R2)—CH2—S(O)nR3 wherein: Y is hydroxy or XONX, where each X is independently hydrogen, lower alkyl or lower acyl; R1 is hydrogen or lower alkyl; R2 is hydrogen, lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, or R1 and R2 together with the carbon atom to which they are attached form a cycloalkyl or heterocyclo group; R3 is aryl; and n is 0, 1 or 2. The invention also provides novel aryl haloalkyl sulfide intermediates useful for the preparation of compounds of Formula I and novel methods of preparing aryl alkyl sulfides.
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公开(公告)号:US06451804B1
公开(公告)日:2002-09-17
申请号:US09693337
申请日:2000-10-20
申请人: James Patrick Dunn , Lawrence Emerson Fisher , David Michael Goldstein , William Harris , Christopher Huw Hill , Ian Edward David Smith , Teresa Rosanne Welch
发明人: James Patrick Dunn , Lawrence Emerson Fisher , David Michael Goldstein , William Harris , Christopher Huw Hill , Ian Edward David Smith , Teresa Rosanne Welch
IPC分类号: A61K31505
CPC分类号: C07D487/04
摘要: The invention provides compounds represented by the formula: wherein R1, R2, R3, R4, and n are as defined in the Summary of the Invention; and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
摘要翻译: 本发明提供由下式表示的化合物:其中R1,R2,R3,R4和n如发明概述中所定义; 和各异构体,异构体的外消旋或非外消旋混合物及其药学上可接受的盐。 本发明还涉及含有这些化合物的药物组合物,其用作治疗剂的方法及其制备方法。
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公开(公告)号:US09365494B2
公开(公告)日:2016-06-14
申请号:US13359329
申请日:2012-01-26
申请人: Kieran Durkin , Lawrence Emerson Fisher , Arthur Meili , Michaelangelo Scalone , Xianqing Shi , Justin Vitale
发明人: Kieran Durkin , Lawrence Emerson Fisher , Arthur Meili , Michaelangelo Scalone , Xianqing Shi , Justin Vitale
IPC分类号: C07C231/18 , B01J31/24 , C07C315/02 , C07C319/14 , C07C319/20 , B01J31/18
CPC分类号: C07C231/18 , B01J31/1805 , B01J31/24 , B01J31/2409 , B01J2231/645 , B01J2531/821 , C07B2200/07 , C07C315/02 , C07C319/14 , C07C319/20 , C07C2602/10 , C07C237/24 , C07C317/32 , C07C323/22 , C07C323/62 , C07C323/38 , C07C323/44
摘要: Methods for producing a compound of formula k1 or k2 by reducing a dihydronapthalene amide compound of formula i with hydrogen gas in the presence of a ruthenium catalyst of formula j1 or j2 Ru(Z)2(L) j1; Ru(E)(E′)(L)(D) j2; wherein m, n, Ar, Y, R1E, E′, D, Z and L are as defined herein.
摘要翻译: 在式j1或j2 Ru(Z)2(L)j1的钌催化剂存在下,用氢气还原式I的二氢萘酰胺化合物,制备式k1或k2化合物的方法; Ru(E)(E')(L)(D)j2; 其中m,n,Ar,Y,R1E,E',D,Z和L如本文所定义。
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公开(公告)号:US5932595A
公开(公告)日:1999-08-03
申请号:US769049
申请日:1996-12-18
申请人: Steven Lee Bender , Chris Allen Broka , Jeffrey Allen Campbell , Arlindo Lucas Castelhano , Lawrence Emerson Fisher , Robert Than Hendricks , Keshab Sarma
发明人: Steven Lee Bender , Chris Allen Broka , Jeffrey Allen Campbell , Arlindo Lucas Castelhano , Lawrence Emerson Fisher , Robert Than Hendricks , Keshab Sarma
IPC分类号: C07D333/34 , A61K31/00 , A61K31/10 , A61K31/165 , A61K31/18 , A61K31/185 , A61K31/34 , A61K31/341 , A61K31/35 , A61K31/351 , A61K31/38 , A61K31/381 , A61K31/382 , A61K31/44 , A61K31/4402 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61P1/00 , A61P1/02 , A61P3/00 , A61P5/00 , A61P19/00 , A61P19/10 , A61P27/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07C259/06 , C07C315/02 , C07C317/44 , C07C323/51 , C07D211/54 , C07D213/64 , C07D213/643 , C07D307/14 , C07D309/08 , C07D335/02 , C07D401/04 , C07D401/06 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , A01N43/40 , A01N37/10 , A01N43/36 , C07C233/00 , C07D207/00 , C07D211/08 , C07D333/32 , C07C415/00
CPC分类号: C07D213/643 , C07D211/54 , C07D309/08 , C07D401/06 , C07D407/12 , C07D409/12 , C07D413/12 , Y10S514/825 , Y10S514/885 , Y10S514/90 , Y10S514/903
摘要: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.
摘要翻译: 本发明涉及式I化合物:基质金属蛋白酶抑制剂,含有它们的药物组合物,其使用方法和制备这些化合物的方法。
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公开(公告)号:US06420573B1
公开(公告)日:2002-07-16
申请号:US09991143
申请日:2001-11-09
IPC分类号: C07D30906
CPC分类号: C07D309/08 , C07C319/14 , C07C319/20 , C07C323/20
摘要: This invention provides processes for the preparation of a compound of Formula I: Y—C(═O)—C(R1)(R2)—CH2—S(O)nR3 wherein: Y is hydroxy or XONX, where each X is independently hydrogen, lower alkyl or lower acyl; R1 is hydrogen or lower alkyl; R2 is hydrogen, lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, or R1 and R2 together with the carbon atom to which they are attached form a cycloalkyl or heterocyclo group; R3 is aryl; and n is 0, 1 or 2. The invention also provides novel aryl haloalkyl sulfide intermediates useful for the preparation of compounds of Formula I and novel methods of preparing aryl alkyl sulfides.
摘要翻译: 本发明提供制备式I化合物的方法:其中:Y是羟基或XONX,其中每个X独立地是氢,低级烷基或低级酰基; R 1是氢或低级烷基; R 2是氢,低级烷基,芳基 ,芳烷基,环烷基,环烷基烷基或R 1和R 2与它们所连接的碳原子一起形成环烷基或杂环基; R 3为芳基; 和n为0,1或2.本发明还提供了可用于制备式I化合物的新型芳基卤代烷基硫化物中间体和制备芳基烷基硫化物的新方法。
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公开(公告)号:US06342639B1
公开(公告)日:2002-01-29
申请号:US09335447
申请日:1999-06-17
IPC分类号: C07C32106
CPC分类号: C07D309/08 , C07C319/14 , C07C319/20 , C07C323/20
摘要: This invention provides processes for the preparation of a compound of Formula I: Y—C(═O—C(R1)(R2)—CH2—S(O)nR3 wherein: Y is hydroxy or XONX, where each X is independently hydrogen, lower alkyl or lower acyl; R1 is hydrogen or lower alkyl; R2 is hydrogen, lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, or R1 and R2 together with the carbon atom to which they are attached form a cycloalkyl or heterocyclo group; R3 is aryl; and n is 0, 1 or 2. The invention also provides novel aryl haloalkyl sulfide intermediates useful for the preparation of compounds of Formula I and novel methods of preparing aryl alkyl sulfides.
摘要翻译: 本发明提供制备式I化合物的方法:其中:Y是羟基或XONX,其中每个X独立地是氢,低级烷基或低级酰基; R 1是氢或低级烷基; R 2是氢,低级烷基,芳基 ,芳烷基,环烷基,环烷基烷基或R 1和R 2与它们所连接的碳原子一起形成环烷基或杂环基; R 3为芳基; 和n为0,1或2.本发明还提供了可用于制备式I化合物的新型芳基卤代烷基硫化物中间体和制备芳基烷基硫化物的新方法。
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