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公开(公告)号：US5906985A
公开(公告)日：1999-05-25
申请号：US916028
申请日：1997-08-21
申请人： Stephen Richard Baker , Almudena Rubio Esteban , John Goldsworthy , Concepcion Pedregal Tercero
发明人： Stephen Richard Baker , Almudena Rubio Esteban , John Goldsworthy , Concepcion Pedregal Tercero
IPC分类号： A61K31/195 , A61P25/00 , A61P25/04 , C07C229/30 , C07C229/36 , C07C229/48 , A61K31/66
CPC分类号： C07C229/30 , Y02P20/55
摘要： Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and m is 1 or 2, R.sup.1 is hydrogen, C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, phenyl, naphthyl, C.sub.1-10 alkyl-phenyl, C.sub.2-10 alkenyl-phenyl or C.sub.2-10 alkynyl-phenyl, said phenyl and naphthyl groups being optionally substituted, R.sup.2 is hydrogen or a protecting group, and Q is an acidic group; or a salt or ester thereof.
摘要翻译： 下式的药物化合物，其中n为0,1或2，m为1或2，R1为氢，C1-10烷基，C2-10烯基，C2-10炔基，苯基，萘基，C1-10烷基 - 苯基 ，C 2-10烯基 - 苯基或C 2-10炔基 - 苯基，所述苯基和萘基任选被取代，R 2是氢或保护基，Q是酸性基团; 或其盐或酯。
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公开(公告)号：US5990165A
公开(公告)日：1999-11-23
申请号：US46445
申请日：1998-03-24
IPC分类号： A61K31/195 , A61K31/215 , A61P25/26 , C07C227/22 , C07C229/30 , C07C229/32 , C07C229/36 , C07C323/58
CPC分类号： C07C229/30 , C07C2101/08 , C07C2101/14 , Y02P20/55
摘要： A pharmaceutical compound of the formula: ##STR1## in which n is 1 or 2, R.sup.1 is --CO.sub.2 H, R.sup.2 is hydrogen or C.sub.1-4 alkyl andR.sup.3 is hydrogen, C.sub.1-10 alkyl, C.sub.2-10 alkenyl, optionally substituted phenyl, optionally substituted phenyl-C.sub.1-4 alkyl, optionally substituted phenyl C.sub.2-10 alkenyl,(optionally substituted phenyl).sub.2 -C.sub.1-4 alkyl, optionally substituted C.sub.3-7 cycloalkyl, optionally substituted C.sub.3-7 cycloalkyl-C.sub.1-4 alkyl or optionally substituted C.sub.3-7 cycloalkyl-C.sub.2-10 alkenyl, orR.sup.2 and R.sup.3, together with the carbon atom to which they are attached, form an optionally substituted C.sub.4-7 cycloalkyl group;or a salt or ester thereof other than the compounds .gamma.-propylidene-L-glutamic acid, .gamma.-ethylidene-L-glutamic acid and .gamma.-methylidene-L-glutamic acid.
摘要翻译： 下式的药物化合物：其中n为1或2，R 1为-CO 2 H，R 2为氢或C 1-4烷基，R 3为氢，C 1-10烷基，C 2-10烯基，任选取代的苯基，任选取代的苯基 -C 1-4烷基，任选取代的苯基C 2-10烯基，（任选取代的苯基）2 -C 1-4烷基，任选取代的C 3-7环烷基，任选取代的C 3-7环烷基-C 1-4烷基或任选取代的C 3-7 环烷基-C 2-10烯基，或者R 2和R 3与它们所连接的碳原子一起形成任选取代的C 4-7环烷基; 或其除了γ-亚丙基-L-谷氨酸，γ-亚乙基-L-谷氨酸和γ-亚甲基-L-谷氨酸的化合物的盐或酯。
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公开(公告)号：US5739164A
公开(公告)日：1998-04-14
申请号：US713624
申请日：1996-09-13
申请人： Jesus Ezquerra Carrera , Almudena Rubio Esteban , Andre Mann , Angele Schoenfelder , Darryle Darwin Schoepp , Concepcion Pedregal Tercero , Camille-Georges Wermuth
发明人： Jesus Ezquerra Carrera , Almudena Rubio Esteban , Andre Mann , Angele Schoenfelder , Darryle Darwin Schoepp , Concepcion Pedregal Tercero , Camille-Georges Wermuth
IPC分类号： A61K31/00 , A61K31/19 , A61K31/195 , A61K31/20 , A61K31/215 , A61K31/38 , A61K31/41 , A61P1/08 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07C229/36 , C07D257/04 , C07D333/24 , C07D409/06
CPC分类号： C07D257/04 , C07C229/36
摘要： Disclosed herein is a method of treating a disease of the central nervous system with a compound of the formula ##STR1## in which m is 0, 1 or 2, n and q are each 0 or 1 to 5, and p is 0 or 1, X is --CO.sub.2 H or tetrazolyl, Y is --CH.dbd.CH--, and Z is (i) phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted, (ii) --CHR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted, (iii) .dbd.CR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted, or (iv) ##STR2## where r is 0 or 1 to 3 and the phenyl rings are optionally substituted; provided that when Z is phenyl and m is 1, p is 1; and salts and esters thereof.
摘要翻译： 本文公开了一种用式“IMAGE”的化合物治疗中枢神经系统疾病的方法，其中m为0,1或2，n和q各自为0或1至5，p为0或1 X是-CO 2 H或四唑基，Y是-CH = CH-，Z是（i）苯基，萘基或噻吩基，所述苯基，萘基和噻吩基任选被取代，（ii）-CHR 1 R 2，其中R 1和R 2各自是苯基 萘基或噻吩基，所述苯基，萘基和噻吩基任选被取代，（iii）= CR1R2，其中R1和R2各自为苯基，萘基或噻吩基，所述苯基，萘基和噻吩基任选被取代，或（iv） r为0或1至3，苯环任选被取代; 条件是当Z为苯基且m为1时，p为1; 及其盐和酯。
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公开(公告)号：US6069238A
公开(公告)日：2000-05-30
申请号：US342073
申请日：1999-06-28
申请人： Stephen Andrew Hitchcock , Chafiq Hamdouchi , Concepcion Sanchez-Martinez , Almudena Rubio Esteban
发明人： Stephen Andrew Hitchcock , Chafiq Hamdouchi , Concepcion Sanchez-Martinez , Almudena Rubio Esteban
CPC分类号： C07H19/01
摘要： An improved and a new synthetic route for the reparation of spirocyclic C-glycoside compounds having the following general structure are described. ##STR1## Novel derivatives of spirocyclic C-glycoside compounds are also disclosed which may be used as intermediates in the synthesis and evaluation of potential pharmaceutically active materials.
摘要翻译： 描述了用于修复具有以下一般结构的螺环C-糖苷化合物的改进和新的合成途径。 还公开了螺环C-糖苷化合物的新型衍生物，其可用作合成和评估潜在的药学活性物质的中间体。
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5.发明授权公开(公告)号：US08071776B2
公开(公告)日：2011-12-06
申请号：US11577508
申请日：2005-10-18
IPC分类号： C07D515/04 , A61K31/4365
CPC分类号： C07D495/04
摘要： The present invention relates to selective allosteric potentiators of the Formula (I): or pharmaceutically acceptable salts thereof, for the treatment of disorders associated with M4 muscarinic receptors.
摘要翻译： 本发明涉及用于治疗与M4毒蕈碱受体相关的病症的式（I）的选择性变构增效剂：或其药学上可接受的盐。
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6.发明申请公开(公告)号：US20090105244A1
公开(公告)日：2009-04-23
申请号：US11577508
申请日：2005-10-18
IPC分类号： A61K31/5377 , C07D495/04 , A61K31/496 , A61K31/4365
CPC分类号： C07D495/04
摘要： The present invention relates to selective allosteric potentiators of the Formula (I): or pharmaceutically acceptable salts thereof, for the treatment of disorders associated with M4 muscarinic receptors.
摘要翻译： 本发明涉及用于治疗与M4毒蕈碱受体相关的病症的式（I）的选择性变构增效剂：或其药学上可接受的盐。
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