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1. 发明申请

US20130231488A1 PROCESS FOR PREPARING 2-HYDROXYPHENYL ALKENYL BENZOTRIAZOLE COMPOUNDS; USE OF THE SAID COMPOUNDS OBTAINED VIA THE PROCESS IN THE SYNTHESIS OF SILOXANE COMPOUNDS CONTAINING A 2-HYDROXYPHENYLBENZOTRIAZOLE FUNCTION 有权
标题翻译：制备2-羟基苯甲醛苯并噻唑化合物的方法; 使用通过合成含有2-羟基苯并噻唑功能的硅氧烷化合物的方法获得的该化合物
公开(公告)号：US20130231488A1
公开(公告)日：2013-09-05
申请号：US13814539
申请日：2010-10-25
申请人： Herve Richard , Jinzhu Xu , Patricio Guerreiro , Yuan Wang , Jianping Guo
发明人： Herve Richard , Jinzhu Xu , Patricio Guerreiro , Yuan Wang , Jianping Guo
IPC分类号： C07F7/08 , C07D249/20
CPC分类号： C07F7/0879 , C07D249/20 , C07F7/0838
摘要： The process for preparing 2-hydroxyphenyl alkenyl benzotriazole compounds and the process for preparing siloxane compounds containing 2-hydroxyphenyl benzotriazole function are disclosed.
摘要翻译：公开了制备2-羟基苯基烯基苯并三唑化合物的方法和制备含有2-羟基苯基苯并三唑功能的硅氧烷化合物的方法。

2. 发明申请

US20120309743A1 THIOLACTAMS AND USES THEREOF 有权
标题翻译： THIOLACTATA及其用途
公开(公告)号：US20120309743A1
公开(公告)日：2012-12-06
申请号：US13570486
申请日：2012-08-09
申请人： Indu T. Bharathan , Matthew Duffey , Amy Elder , Jianping Guo , Gang Li , Dominic Reynolds , Francois Soucy , Tricia J. Vos
发明人： Indu T. Bharathan , Matthew Duffey , Amy Elder , Jianping Guo , Gang Li , Dominic Reynolds , Francois Soucy , Tricia J. Vos
IPC分类号： A61K31/55 , A61P35/00 , A61N5/10 , A61P37/00 , A61P29/00 , A61P35/02 , C07D487/04 , A61P25/28
CPC分类号： C07D213/75 , A61K31/55 , A61N5/10 , C07D215/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D471/04 , C07D487/04
摘要： This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
摘要翻译：本发明提供式I化合物：其中R 1，R 2，R 3，R 4，R 5和R 6如说明书中所述。这些化合物是PLK的抑制剂，因此可用于治疗增殖性，炎性或心血管疾病。

3. 发明授权

US08268992B2 Thiolactams and uses thereof 有权
标题翻译：硫醇内酰胺及其用途
公开(公告)号：US08268992B2
公开(公告)日：2012-09-18
申请号：US13173161
申请日：2011-06-30
申请人： Indu T. Bharathan , Matthew Duffey , Amy Elder , Jianping Guo , Gang Li , Dominic Reynolds , Francois Soucy , Tricia J. Vos
发明人： Indu T. Bharathan , Matthew Duffey , Amy Elder , Jianping Guo , Gang Li , Dominic Reynolds , Francois Soucy , Tricia J. Vos
IPC分类号： C07D487/04
CPC分类号： C07D213/75 , A61K31/55 , A61N5/10 , C07D215/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D471/04 , C07D487/04
摘要： This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
摘要翻译：本发明提供式I化合物：其中R 1，R 2，R 3，R 4，R 5和R 6如说明书中所述。这些化合物是PLK的抑制剂，因此可用于治疗增殖性，炎性或心血管疾病。

4. 发明申请

US20100179126A1 THIOLACTAMS AND USES THEREOF 有权
标题翻译： THIOLACTATA及其用途
公开(公告)号：US20100179126A1
公开(公告)日：2010-07-15
申请号：US12631144
申请日：2009-12-04
申请人： Indu T. Bharathan , Matthew Duffey , Amy Elder , Jianping Guo , Gang Li , Dominic Reynolds , Francois Soucy , Tricia J. Vos
发明人： Indu T. Bharathan , Matthew Duffey , Amy Elder , Jianping Guo , Gang Li , Dominic Reynolds , Francois Soucy , Tricia J. Vos
IPC分类号： A61K31/55 , C07D487/04 , A61P25/28 , A61P29/00 , A61P37/00 , A61P35/02 , A61P35/00
CPC分类号： C07D213/75 , A61K31/55 , A61N5/10 , C07D215/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D471/04 , C07D487/04
摘要： This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
摘要翻译：本发明提供式I化合物：其中R 1，R 2，R 3，R 4，R 5和R 6如说明书中所述。这些化合物是PLK的抑制剂，因此可用于治疗增殖性，炎性或心血管疾病。

5. 发明申请

US20130204006A1 PROCESS FOR PREPARING 2-HYDROXYPHENYL BENZOTRIAZOLE SILOXANE COMPOUNDS 有权
标题翻译：制备2-羟基苯并噻唑硅氧烷化合物的方法
公开(公告)号：US20130204006A1
公开(公告)日：2013-08-08
申请号：US13814592
申请日：2010-10-25
申请人： Herve Richard , Patricio Guerreiro , Jianping Guo , Wensheng Tang
发明人： Herve Richard , Patricio Guerreiro , Jianping Guo , Wensheng Tang
IPC分类号： C07F7/08
CPC分类号： C07F7/0879 , C07D249/20 , C07F7/0838
摘要： A process for preparing a siloxane compound comprising a 2-hydroxyphenyl benzotriazole function which comprises at least one step in which a reaction for hydrosilylation of a compound 2-hydroxyphenyl benzotriazole comprising a substituent having a terminal double bond with a siloxane compound comprising an SiH function is carried out in the presence of a catalyst and of at least one volatile organic solvent corresponding to one of formula (VII) or (VIII). in which R4 and R5, which may be identical or different, represent a linear or branched C1-C4 alkyl radical, with the proviso that the sum of the carbons of R4 and R5 is less than or equal to 6; y is and integer between 1 and 3; R6 which may be identical or different, are linear or branched C1-C3 alkyl radicals, with the proviso that the sum of the carbons of R6 is less than or equal to 6 is disclosed.
摘要翻译：一种制备包含2-羟基苯基苯并三唑功能的硅氧烷化合物的方法，其包含至少一个步骤，其中包含具有末端双键的取代基的化合物2-羟基苯基苯并三唑与包含SiH官能团的硅氧烷化合物的氢化硅烷化反应是在催化剂和对应于式（VII）或（VIII）之一的至少一种挥发性有机溶剂的存在下进行。其中可以相同或不同的R 4和R 5表示直链或支链C 1 -C 4烷基，条件是R 4和R 5的碳的总和小于或等于6; y为1和3之间的整数; 可以相同或不同的R 6是直链或支链C 1 -C 3烷基，条件是R6的碳原子总数小于或等于6。

6. 发明授权

US07998952B2 Thiolactams and uses thereof 有权
标题翻译：硫醇内酰胺及其用途
公开(公告)号：US07998952B2
公开(公告)日：2011-08-16
申请号：US12631144
申请日：2009-12-04
申请人： Indu T. Bharathan , Matthew Duffey , Amy Elder , Jianping Guo , Gang Li , Dominic Reynolds , Francois Soucy , Tricia J. Vos
发明人： Indu T. Bharathan , Matthew Duffey , Amy Elder , Jianping Guo , Gang Li , Dominic Reynolds , Francois Soucy , Tricia J. Vos
IPC分类号： C07D487/04 , A61K31/55
CPC分类号： C07D213/75 , A61K31/55 , A61N5/10 , C07D215/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D471/04 , C07D487/04
摘要： This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
摘要翻译：本发明提供式I化合物：其中R 1，R 2，R 3，R 4，R 5和R 6如说明书中所述。这些化合物是PLK的抑制剂，因此可用于治疗增殖性，炎性或心血管疾病。

7. 发明授权

US09447123B2 Process for preparing 2-hydroxyphenyl alkenyl benzotriazole compounds; use of the said compounds obtained via the process in the synthesis of siloxane compounds containing a 2-hydroxyphenylbenzotriazole function 有权
标题翻译： 2-羟基苯基烯基苯并三唑化合物的制备方法; 在合成含有2-羟基苯基苯并三唑功能的硅氧烷化合物中使用通过该方法获得的所述化合物
公开(公告)号：US09447123B2
公开(公告)日：2016-09-20
申请号：US13814539
申请日：2010-10-25
申请人： Herve Richard , Jinzhu Xu , Patricio Guerreiro , Yuan Wang , Jianping Guo
发明人： Herve Richard , Jinzhu Xu , Patricio Guerreiro , Yuan Wang , Jianping Guo
IPC分类号： C07F7/08 , C07D249/20
CPC分类号： C07F7/0879 , C07D249/20 , C07F7/0838
摘要： The process for preparing 2-hydroxyphenyl alkenyl benzotriazole compounds and the process for preparing siloxane compounds containing 2-hydroxyphenyl benzotriazole function are disclosed.
摘要翻译：公开了制备2-羟基苯基烯基苯并三唑化合物的方法和制备含有2-羟基苯基苯并三唑功能的硅氧烷化合物的方法。

8. 发明授权

US08614337B2 S-5-substituent-N-2′-(thiophene-2-yl)ethyl-tetralin-2-amine or chiral acid salts thereof and use for preparing Rotigotine 有权
标题翻译： S-5-取代基-N-2' - （噻吩-2-基）乙基 - 四氢化萘-2-胺或其手性酸盐，用于制备罗替戈汀
公开(公告)号：US08614337B2
公开(公告)日：2013-12-24
申请号：US13394614
申请日：2010-09-07
申请人： Xungui He , Jianping Guo , Yanling Wang , Wensheng Tang , Xingzhong Zhang , Xuezhang Wang , Yuan Wang
发明人： Xungui He , Jianping Guo , Yanling Wang , Wensheng Tang , Xingzhong Zhang , Xuezhang Wang , Yuan Wang
IPC分类号： C07D333/20 , C07D333/22
CPC分类号： C07D333/20 , C07B57/00
摘要： The chiral compound S-5-substituted-N-2′-(thienyl-2-yl-)ethyl-tetralin-2-amine or its chiral acid salts and preparation method thereof are disclosed, and the method for preparing Rotigotine by using the chiral compound is also disclosed. Racemic 5-substituted-N-2′-(thien-2-yl-)ethyl-tetralin-2-amine (compound 1) is resolved by using a conventional chiral acid to obtain an optically pure chiral acid salt of S-5-substituted-N-2′-(thien-2-yl-)ethyl-tetralin-2-amine, which is then dissociated to obtain S-5-substituted-N-2′-(thien-2-yl-)ethyl-tetralin-2-amine (compound 2). The compound 2 or chiral acid salt thereof is alkylated and deprotected to produce rotigotine (compound 5).
摘要翻译：公开了手性化合物S-5-取代-N-2' - （噻吩基-2-基） - 乙基 - 四氢化萘-2-胺或其手性酸盐及其制备方法，还公开了手性化合物。通过使用常规的手性酸来拆分外消旋的5-取代的N-2' - （噻吩-2-基）乙基 - 四氢化萘-2-胺（化合物1），得到光学纯的手性酸S-5- 取代的N-2' - （噻吩-2-基）乙基 - 四氢化萘-2-胺，然后将其解离得到S-5-取代的N-2' - （噻吩-2-基）四氢化萘-2-胺（化合物2）。将化合物2或其手性酸式盐进行烷基化和脱保护，得到罗替戈汀（化合物5）。

9. 发明授权

US08507667B2 Thiolactams and uses thereof 有权
标题翻译：硫醇内酰胺及其用途
公开(公告)号：US08507667B2
公开(公告)日：2013-08-13
申请号：US13570486
申请日：2012-08-09
申请人： Indu T. Bharathan , Matthew O. Duffey , Amy M. Elder , Jianping Guo , Gang Li , Dominic Reynolds , Francois Soucy , Tricia J. Vos
发明人： Indu T. Bharathan , Matthew O. Duffey , Amy M. Elder , Jianping Guo , Gang Li , Dominic Reynolds , Francois Soucy , Tricia J. Vos
IPC分类号： C07D487/04
CPC分类号： C07D213/75 , A61K31/55 , A61N5/10 , C07D215/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D471/04 , C07D487/04
摘要： This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
摘要翻译：本发明提供式I化合物：其中R 1，R 2，R 3，R 4，R 5和R 6如说明书中所述。这些化合物是PLK的抑制剂，因此可用于治疗增殖性，炎性或心血管疾病。

10. 发明申请

US20120142732A1 HETEROARYLS AND USES THEREOF 有权
标题翻译： HETEROARYLS及其用途
公开(公告)号：US20120142732A1
公开(公告)日：2012-06-07
申请号：US13206671
申请日：2011-08-10
申请人： Courtney A. Cullis , Krista E. Granger , Jianping Guo , Masaaki Hirose , Gang Li , Miho Mizutani , Tricia J. Vos
发明人： Courtney A. Cullis , Krista E. Granger , Jianping Guo , Masaaki Hirose , Gang Li , Miho Mizutani , Tricia J. Vos
IPC分类号： A61K31/443 , C07D413/14 , A61K31/4439 , C07D413/04 , A61K31/422 , A61K31/444 , C07D405/14 , A61K31/4545 , C07D409/14 , A61P35/00 , A61P29/00 , A61P9/00 , A61P37/08 , A61P7/02 , A61P9/12 , A61P9/04 , C07D405/04
CPC分类号： A61K31/422 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04
摘要： This invention provides compounds of formula IA or IB: wherein HY, R1, R2, and G1, are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
摘要翻译：本发明提供式IA或IB的化合物：其中HY，R1，R2和G1如说明书中所述。这些化合物是VPS34和/或PI3K的抑制剂，因此可用于治疗增殖性，炎性或心血管疾病。

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