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公开(公告)号：US08183254B2
公开(公告)日：2012-05-22
申请号：US12454210
申请日：2009-05-14
申请人： Humberto Bartolome Arzeno , James Patrick Dunn , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Alam Jahangir , Wylie Solang Palmer , Deborah Carol Reuter , Tania Silva , Parcharee Tivitmahaisoon , Teresa Alejandra Trejo-Martin , Shao-Yong Wu
发明人： Humberto Bartolome Arzeno , James Patrick Dunn , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Alam Jahangir , Wylie Solang Palmer , Deborah Carol Reuter , Tania Silva , Parcharee Tivitmahaisoon , Teresa Alejandra Trejo-Martin , Shao-Yong Wu
IPC分类号： C07D401/14 , A61K31/506
CPC分类号： C07D401/14
摘要： The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula I: wherein m, n, p, q, Q, r, R1, R2, R3, X, X1, X2, X3, X4, X5, Y1, Y2, Z1 and Z2 are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
摘要翻译： 本发明涉及JNK抑制剂的前药以及用于抑制JNK和治疗JNK介导的病症的相应方法，制剂和组合物。 本申请公开了如下式I所述的JNK抑制剂的前药：其中m，n，p，q，Q，r，R1，R2，R3，X，X1，X2，X3，X4，X5，Y1， Z1和Z2如本文所定义。 本文公开的化合物和组合物可用于调节JNK的活性并治疗与JNK活性相关的疾病。 公开了用于抑制JNK和治疗JNK介导的病症等的方法和制剂，以及本文公开的化合物，以及制备所述化合物的方法和相应的组合物。
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公开(公告)号：US20090318484A1
公开(公告)日：2009-12-24
申请号：US12454210
申请日：2009-05-14
申请人： Humberto Bartolome Arzeno , James Patrick Dunn , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Alam Jahangir , Wylie Solang Palmer , Deborah Carol Reuter , Tania Silva , Parcharee Tivitmanhaisoon , Teresa Alejandra Trejo-Martin , Shao-Yong Wu
发明人： Humberto Bartolome Arzeno , James Patrick Dunn , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Alam Jahangir , Wylie Solang Palmer , Deborah Carol Reuter , Tania Silva , Parcharee Tivitmanhaisoon , Teresa Alejandra Trejo-Martin , Shao-Yong Wu
IPC分类号： A61K31/506 , C07D413/14 , A61P19/02 , A61P3/04 , A61P25/16 , A61P25/28
CPC分类号： C07D401/14
摘要： The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula I: wherein m, n, p, q, Q, r, R1, R2, R3, X, X1, X2, X3, X4, X5, Y1, Y2, Z1 and Z2 areas defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
摘要翻译： 本发明涉及JNK抑制剂的前药以及用于抑制JNK和治疗JNK介导的病症的相应方法，制剂和组合物。 本申请公开了如下式I所述的JNK抑制剂的前药：其中m，n，p，q，Q，r，R1，R2，R3，X，X1，X2，X3，X4，X5，Y1， Z1和Z2区域。 本文公开的化合物和组合物可用于调节JNK的活性并治疗与JNK活性相关的疾病。 公开了用于抑制JNK和治疗JNK介导的病症等的方法和制剂，以及本文公开的化合物，以及制备所述化合物的方法和相应的组合物。
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公开(公告)号：US06573218B1
公开(公告)日：2003-06-03
申请号：US09786816
申请日：2001-07-05
IPC分类号： C07D23116
CPC分类号： C07D239/54 , A01N43/54 , A01N43/76 , A01N43/84 , A01N43/90 , C07D263/56 , C07D413/04 , C07D471/04 , C07D487/04
摘要： A compound of the formula (Ia): or its salts, in which the variables are as described in the disclosure; herbicidal compositions of said compounds, herbicidal processes using said compounds, defoliant processes using said compounds, and processes for preparing said compounds.
摘要翻译： 式（Ia）化合物或其盐，其中变量如本公开所述; 所述化合物的除草组合物，使用所述化合物的除草方法，使用所述化合物的脱叶法，以及制备所述化合物的方法。
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4.发明授权Substituted benzene compounds, process for their preparation, and herbicidal and defoliant compositions containing them 失效取代的苯化合物，其制备方法和含有它们的除草和脱叶组合物公开(公告)号：US06545161B2
公开(公告)日：2003-04-08
申请号：US09930149
申请日：2001-08-16
IPC分类号： C07D24808
CPC分类号： C07D209/48 , A01N37/32 , A01N37/34 , A01N43/40 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/64 , A01N43/653 , A01N43/713 , A01N43/90 , A01N47/06 , A01N47/20 , A01N47/22 , A01N47/24 , A01N47/30 , A01N47/34 , C07C211/52 , C07C217/84 , C07D231/16 , C07D237/14 , C07D239/54 , C07D239/553 , C07D249/12 , C07D257/04 , C07D471/04 , C07D487/04
摘要： Novel herbicidal and defoliant substituted aniline derived compounds represented by general structure (I) are described. W, X, Y, Z, and Q are as defined in the disclosure. Also described are the processes for the manufacture of these compounds and agriculturally suitable compositions containing these as active ingredients which are useful as herbicides for general or selective pre-emergent or post-emergent control of undesired plant species and defoliants at very low concentrations of these biologically active compounds.
摘要翻译： 描述了由通式（I）表示的新型除草和脱落取代的苯胺衍生化合物。 W，X，Y，Z和Q如本公开所定义。 还描述了制备这些化合物的方法和含有这些作为活性成分的农业合适的组合物的方法，其可用作除草剂，用于在这些生物学非常低的浓度下用于一般或选择性芽前或出苗后控制不期望的植物物种和脱叶剂 活性化合物。
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5.发明授权Substituted benzene compounds, process for their preparation, and herbicidal and defoliant compositions containing them 有权取代的苯化合物，其制备方法和含有它们的除草和脱叶组合物公开(公告)号：US06355799B1
公开(公告)日：2002-03-12
申请号：US09530373
申请日：2000-04-27
IPC分类号： C07D23902
CPC分类号： C07D209/48 , A01N37/32 , A01N37/34 , A01N43/40 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/64 , A01N43/653 , A01N43/713 , A01N43/90 , A01N47/06 , A01N47/20 , A01N47/22 , A01N47/24 , A01N47/30 , A01N47/34 , C07C211/52 , C07C217/84 , C07D231/16 , C07D237/14 , C07D239/54 , C07D239/553 , C07D249/12 , C07D257/04 , C07D471/04 , C07D487/04
摘要： Novel herbicidal and defoliant substituted aniline derived compounds represented by general structure (I) are described. W, X, Y, Z, and Q are as defined in the disclosure. Also described are the processes for the manufacture of these compounds and agriculturally suitable compositions containing these as active ingredients which are useful as herbicides for general or selective pre-emergent or post-emergent control of undesired plant species and defoliants at very low concentrations of these biologically active compounds.
摘要翻译： 描述了由通式（I）表示的新型除草和脱落取代的苯胺衍生化合物。 W，X，Y，Z和Q如本公开所定义。 还描述了制备这些化合物的方法和含有这些作为活性成分的农业合适的组合物的方法，其可用作除草剂，用于在这些生物学非常低的浓度下用于一般或选择性芽前或出苗后控制不期望的植物物种和脱叶剂 活性化合物。
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6.发明授权Diaryl ethers and processes for their preparation and herbicidal and desiccant compositions containing them 失效二芳基醚及其制备方法和含有它们的除草和干燥剂组合物公开(公告)号：US06303543B1
公开(公告)日：2001-10-16
申请号：US09570911
申请日：2000-05-15
申请人： David A. Pulman , Bai-Ping Ying , Shao-Yong Wu , Sandeep Gupta , Masamitsu Tsukamoto , Takahiro Haga
发明人： David A. Pulman , Bai-Ping Ying , Shao-Yong Wu , Sandeep Gupta , Masamitsu Tsukamoto , Takahiro Haga
IPC分类号： C07D23156
CPC分类号： C07D231/20 , A01N43/50 , A01N43/52 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/653 , A01N43/66 , A01N43/713 , A01N43/76 , A01N43/80 , A01N43/90 , C07D231/18 , A01N2300/00 , A01N47/36 , A01N47/06 , A01N43/10 , A01N37/22
摘要： A compound represented by the formula (I) or its salt and herbicidal and desiccant use thereof: wherein X, Y are independently hydrogen, halogen, cyano, nito, or (C1-6)haloalkyl; Z is oxygen or sulfur; and
摘要翻译： 由式（I）表示的化合物或其盐和除草和干燥剂的用途：其中X，Y独立地是氢，卤素，氰基，硝基或（C 1-6）卤代烷基; Z是氧或硫; 和
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7.发明授权公开(公告)号：US08101665B2
公开(公告)日：2012-01-24
申请号：US12316946
申请日：2008-12-17
IPC分类号： A01N31/18 , A01N31/00 , A61K31/165 , A61K31/095 , C07C321/00 , C07C323/00 , C07C318/00
CPC分类号： C07B59/001 , C07B2200/05 , C07C319/06 , C07C319/14 , C07C319/20 , C07C319/24 , C07C323/60 , C07C323/56
摘要： Methods for preparing tritium or deuterium labeled thiorphan comprising reacting a compound of formula j wherein m is from 1 to 5 and X is halo, with Z2 wherein Z is tritium or deuterium, in the presence of a catalyst, to form a compound of formula k wherein n is from 1 to 5, provided that n is less than or equal to m.
摘要翻译： 制备氚或氘标记噻吩的方法，包括使式j化合物其中m为1至5，X为卤素，Z 2为Z为氚或氘，在催化剂存在下，形成式K化合物 其中n为1至5，条件是n小于或等于m。
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8.发明申请公开(公告)号：US20110319656A1
公开(公告)日：2011-12-29
申请号：US12316946
申请日：2008-12-17
IPC分类号： C07C235/74
CPC分类号： C07B59/001 , C07B2200/05 , C07C319/06 , C07C319/14 , C07C319/20 , C07C319/24 , C07C323/60 , C07C323/56
摘要： Methods for preparing tritium or deuterium labeled thiorphan comprising reacting a compound of formula i wherein m is from 1 to 5 and X is halo, with Z2 wherein Z is tritium or deuterium, in the presence of a catalyst, to form a compound of formula l wherein n is from 1 to 5, provided that n is less than or equal to m.
摘要翻译： 制备氚或氘标记的噻吩的方法包括使式I化合物其中m为1至5，X为卤素，Z 2为Z为氚或氘，在催化剂存在下，形成式I化合物 其中n为1至5，条件是n小于或等于m。
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9.发明授权Diaryl ethers and processes for their preparation and herbicidal and desiccant compositions containing them 失效二芳基醚及其制备方法和含有它们的除草和干燥剂组合物
公开(公告)号：US6121201A
公开(公告)日：2000-09-19
申请号：US159233
申请日：1998-09-23
申请人： David A. Pulman , Bai-Ping Ying , Shao-Yong Wu , Sandeep Gupta , Masamitsu Tsukamoto , Takahiro Haga
发明人： David A. Pulman , Bai-Ping Ying , Shao-Yong Wu , Sandeep Gupta , Masamitsu Tsukamoto , Takahiro Haga
IPC分类号： A01N43/50 , A01N43/52 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/653 , A01N43/66 , A01N43/713 , A01N43/76 , A01N43/80 , A01N43/90 , C07D231/18 , C07D231/20
CPC分类号： C07D231/20 , A01N43/50 , A01N43/52 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/653 , A01N43/66 , A01N43/713 , A01N43/76 , A01N43/80 , A01N43/90 , C07D231/18
摘要： A compound represented by the formula (I) or its salt and herbicidal and desiccant use thereof: ##STR1## wherein X, Y are independently hydrogen, halogen, cyano, nitro, or (C.sub.1-6)haloalkyl;Z is oxygen or sulfur; andQ is ##STR2##
摘要翻译： 由式（I）表示的化合物或其盐和除草和干燥剂的用途：其中X，Y独立地为氢，卤素，氰基，硝基或（C 1-6）卤代烷基; Z是氧或硫; 而Q是
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10.再颁专利Substituted benzene compounds, process for their preparation, and herbicidal and defoliant compositions containing them 失效取代的苯化合物，其制备方法和含有它们的除草和脱叶组合物公开(公告)号：USRE39590E1
公开(公告)日：2007-04-24
申请号：US10797936
申请日：2000-04-27
IPC分类号： C07D239/54 , A01N43/54
CPC分类号： C07D209/48 , A01N37/32 , A01N37/34 , A01N43/40 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/64 , A01N43/653 , A01N43/713 , A01N43/90 , A01N47/06 , A01N47/20 , A01N47/22 , A01N47/24 , A01N47/30 , A01N47/34 , C07C211/52 , C07C217/84 , C07D231/16 , C07D237/14 , C07D239/54 , C07D239/553 , C07D249/12 , C07D257/04 , C07D471/04 , C07D487/04
摘要： Novel herbicidal and defoliant substituted aniline derived compounds represented by general structure (I) are described. W, X, Y, Z, and Q are as defined in the disclosure. Also described are the processes for the manufacture of these compounds and agriculturally suitable compositions containing these as active ingredients which are useful as herbicides for general or selective pre-emergent or post-emergent control of undesired plant species and defoliants at very low concentrations of these biologically active compounds.
摘要翻译： 描述了由通式（I）表示的新型除草和脱落取代的苯胺衍生化合物。 W，X，Y，Z和Q如本公开所定义。 还描述了制备这些化合物的方法和含有这些作为活性成分的农业合适的组合物的方法，其可用作除草剂，用于在这些生物学非常低的浓度下用于一般或选择性芽前或出苗后控制不期望的植物物种和脱叶剂 活性化合物
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