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11. 发明申请

US20120088759A1 THIAZOLIDIN-4-ONE AND [1,3]-THIAZINAN-4-ONE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：噻吗啉-4-酮和[1,3] - 噻嗪-4-酮化合物作为OREXIN受体拮抗剂
公开(公告)号：US20120088759A1
公开(公告)日：2012-04-12
申请号：US13319774
申请日：2010-05-11
申请人： Hamed Aissaoui , Christoph Boss , Christine Brotschi , Markus Gude , John Gatfield , Romain Siegrist , Thierry Sifferlen , Jodi T. Williams
发明人： Hamed Aissaoui , Christoph Boss , Christine Brotschi , Markus Gude , John Gatfield , Romain Siegrist , Thierry Sifferlen , Jodi T. Williams
IPC分类号： A61K31/54 , C07D277/34 , C07D417/12 , A61K31/506 , A61K31/4439 , A61K31/426 , A61K31/498 , A61P25/22 , A61P25/00 , C07D417/10 , C07D417/04 , C07D279/06 , A61K31/501 , A61K31/427 , A61K31/4709 , A61K31/541 , A61P25/20 , A61P25/18 , C07D277/14
CPC分类号： C07D277/14 , C07D417/04
摘要： The present invention relates to thiazolidin-4-one and [1,3]-thiazinan-4-one compounds of formula (I) wherein X, Y, R3 and R4 are as described in the description, or pharmaceutically acceptable salts thereof, for the prevention or treatment of diseases related to the orexin system. The present invention also relates to novel thiazolidin-4-one compounds of formula (II) and their use as pharmaceuticals, pharmaceutical compositions containing one or more compounds of formula (II), and especially their use as orexin receptor antagonists.
摘要翻译：本发明涉及式（I）的噻唑烷-4-酮和[1,3]噻嗪-4-酮化合物，其中X，Y，R 3和R 4如说明书中所述或其药学上可接受的盐，用于预防或治疗与食欲素系统有关的疾病。本发明还涉及式（II）的新型噻唑烷-4-酮化合物及其作为药物的用途，含有一种或多种式（II）化合物的药物组合物，特别是其作为食欲素受体拮抗剂的用途。

12. 发明申请

US20110166170A1 SYNTHESIS OF AVRAINVILLAMIDE, STEPHACIDIN B, AND ANALOGUES THEREOF 审中-公开
标题翻译：阿维菌素，去甲胆碱B及其类似物的合成
公开(公告)号：US20110166170A1
公开(公告)日：2011-07-07
申请号：US12913091
申请日：2010-10-27
申请人： Andrew G. Myers , Seth B. Herzon , Jeremy Earle Wulff , Romain Siegrist , Jakub Svenda , Matthew Allen Zajac
发明人： Andrew G. Myers , Seth B. Herzon , Jeremy Earle Wulff , Romain Siegrist , Jakub Svenda , Matthew Allen Zajac
IPC分类号： A61K31/437 , C07D487/04 , C07D471/22 , C07D209/56 , C07D209/82 , A61K31/407 , A61K31/403 , A61P35/00
CPC分类号： C07D209/88 , C07D471/22 , C07D491/052 , C07D491/22 , C07D495/22
摘要： The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The α,β-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores. The compounds of the invention may be used in the treatment of diseases such as cancer, autoimmune diseases, and bacterial infection.
摘要翻译：提供了天然产物，维生素A和抗抑郁素B的合成。显示出avrainvillamide及其3-亚烷基-3H-吲哚-1-氧化物核心的α，bgr-不饱和硝酮官能团共价和可逆地键合到基于杂原子的亲核试剂。这种能力可以允许这些分子结合活性位点亲核试剂，并且可以为设计有效和选择性酶抑制剂提供依据。已经报道了丙氨酰维他命和其二聚杀生物素蛋白B都具有抗增殖活性，据报道，抗谷氨酰胺具有抗多药耐药细菌的抗微生物活性。已经发现Avrainvillamide靶向细胞骨架连接膜蛋白（CLIMP-63），从而防止细胞发生有丝分裂。本发明提供这些天然产物以及这些天然产物及其功能核心的类似物的合成。本发明的化合物可用于治疗诸如癌症，自身免疫性疾病和细菌感染等疾病。

13. 发明申请

US20110105514A1 5,6,7,8-TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE COMPOUNDS 审中-公开
标题翻译： 5,6,7,8-四氢-1H-咪唑并[1,5-A]吡嗪化合物
公开(公告)号：US20110105514A1
公开(公告)日：2011-05-05
申请号：US13000201
申请日：2009-06-24
申请人： Hamed Aissaoui , Christoph Boss , Ralf Koberstein , Romain Siegrist , Thierry Sifferlen
发明人： Hamed Aissaoui , Christoph Boss , Ralf Koberstein , Romain Siegrist , Thierry Sifferlen
IPC分类号： A61K31/4985 , C07D487/04 , A61P25/00 , A61P25/30
CPC分类号： C07D487/04
摘要： The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I) wherein R1, R2, R3, and R4 are as described n the description, to salts, especially pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments; especially as orexin receptor antagonists.
摘要翻译：本发明涉及式（I）的5,6,7,8-四氢 - 咪唑并[1,5-a]吡嗪衍生物，其中R 1，R 2，R 3和R 4如在描述中所述，可接受的盐，以及这些化合物作为药物的用途; 特别是作为食欲素受体拮抗剂。

14. 发明申请

US20110105491A1 THIAZOLIDINE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：噻唑烷化合物作为OREXIN受体拮抗剂
公开(公告)号：US20110105491A1
公开(公告)日：2011-05-05
申请号：US13002365
申请日：2009-07-07
申请人： Hamed Aissaoui , Christoph Boss , Julien Hazemann , Ralf Koberstein , Romain Siegrist , Thierry Sifferlen
发明人： Hamed Aissaoui , Christoph Boss , Julien Hazemann , Ralf Koberstein , Romain Siegrist , Thierry Sifferlen
IPC分类号： A61K31/538 , C07D417/14 , C07D513/04 , C07D471/04 , C07D417/10 , A61K31/427 , A61K31/429 , A61K31/437 , A61K31/4245 , A61K31/433 , A61K31/498 , A61K31/4439 , A61K31/4375 , A61K31/497 , A61P25/20 , A61P25/30 , A61P25/00 , A61P25/18 , A61P25/32
CPC分类号： C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04
摘要： The invention relates to thiazolidine derivatives of the formula (I) wherein A, B, and R1 are as described in the description, to salts, especially pharmaceutically acceptable salts, of such compounds and to their use as medicaments, especially as orexin receptor antagonists.
摘要翻译：本发明涉及式（I）的噻唑烷衍生物，其中A，B和R 1如描述中所述，这些化合物的盐，特别是药学上可接受的盐，以及它们作为药物，特别是作为食欲素受体拮抗剂的用途。

15. 发明申请

US20090143581A1 SYNTHESIS OF AVRAINVILLAMIDE, STREPHACIDIN B, AND ANALOGUES THEREOF 失效
标题翻译：阿维菌素，去甲胆碱B及其类似物的合成
公开(公告)号：US20090143581A1
公开(公告)日：2009-06-04
申请号：US11908901
申请日：2006-03-17
申请人： Andrew G. Myers , Seth B. Herzon , Jeremy Earle Wulff , Romain Siegrist , Jakub Svenda , Matthew Alan Zajac
发明人： Andrew G. Myers , Seth B. Herzon , Jeremy Earle Wulff , Romain Siegrist , Jakub Svenda , Matthew Alan Zajac
IPC分类号： C07D471/22 , C07C45/61 , C07D209/56 , C07D491/052
CPC分类号： C07D209/88 , C07D471/22 , C07D491/052 , C07D491/22 , C07D495/22
摘要： The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The α,β-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores. The compounds of the invention may be used in the treatment of diseases such as cancer, autoimmune diseases, and bacterial infection.
摘要翻译：提供了天然产物，维生素A和抗抑郁素B的合成。显示出丙氨酰胺及其3-亚烷基-3H-吲哚-1-氧化物核心的α，β-不饱和硝酮官能团共价和可逆地键合到基于杂原子的亲核试剂。这种能力可以允许这些分子结合活性位点亲核试剂，并且可以为设计有效和选择性酶抑制剂提供依据。已经报道了丙氨酰维他命和其二聚杀生物素蛋白B都具有抗增殖活性，据报道，抗谷氨酰胺具有抗多药耐药细菌的抗微生物活性。已经发现Avrainvillamide靶向细胞骨架连接膜蛋白（CLIMP-63），从而防止细胞发生有丝分裂。本发明提供这些天然产物以及这些天然产物及其功能核心的类似物的合成。本发明的化合物可用于治疗诸如癌症，自身免疫性疾病和细菌感染等疾病。

16. 发明授权

US09096595B2 7-(heteroaryl-amino)-6,7,8,9-tetrahydropyrido[1,2-a]indol acetic acid derivatives and their use as prostaglandin D2 receptor modulators 有权
标题翻译： 7-（杂芳基 - 氨基）-6,7,8,9-四氢吡啶并[1,2-a]吲哚乙酸衍生物及其作为前列腺素D2受体调节剂的用途
公开(公告)号：US09096595B2
公开(公告)日：2015-08-04
申请号：US14111889
申请日：2012-04-13
申请人： Hamed Aissaoui , Christoph Boss , Jerome Gabillet , Sylvia Richard-Bildstein , Romain Siegrist
发明人： Hamed Aissaoui , Christoph Boss , Jerome Gabillet , Sylvia Richard-Bildstein , Romain Siegrist
IPC分类号： C07D471/04 , A61K31/437 , A61P37/08
CPC分类号： C07D471/04 , A61K31/437
摘要： The present invention relates to 7-(heteroaryl-amino)-6,7,8,9-tetrahydropyrido[1,2-a]indol acetic acid derivatives of the formula (I), wherein R1, R2, R3 and R4 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
摘要翻译：本发明涉及式（I）的7-（杂芳基 - 氨基）-6,7,8,9-四氢吡啶并[1,2-a]吲哚乙酸衍生物，其中R 1，R 2，R 3和R 4为描述及其作为前列腺素受体调节剂的用途，最特别地作为前列腺素D2受体调节剂用于治疗各种前列腺素介导的疾病和病症，含有这些化合物的药物组合物及其制备方法。

17. 发明申请

US20130109685A1 1-PHENYL-SUBSTITUTED HETEROCYCLYL DERIVATIVES AND THEIR USE AS PROSTAGLANDIN D2 RECEPTOR MODULATORS 有权
标题翻译： 1-苯基取代的杂环衍生物及其作为PROSTAGLANDIN D2受体调节剂的用途
公开(公告)号：US20130109685A1
公开(公告)日：2013-05-02
申请号：US13808857
申请日：2011-07-04
申请人： Hamed Aissaoui , Christoph Boss , Anja Valdenaire , Julien Pothier , Sylvia Richard-Bildstein , Philippe Risch , Romain Siegrist
发明人： Hamed Aissaoui , Christoph Boss , Anja Valdenaire , Julien Pothier , Sylvia Richard-Bildstein , Philippe Risch , Romain Siegrist
IPC分类号： C07D487/04 , C07D417/06 , C07D405/04 , C07D417/12 , C07D401/12 , C07D471/04 , C07D217/26 , C07D413/06
CPC分类号： C07D487/04 , A61K31/4035 , A61K31/472 , C07D209/44 , C07D217/16 , C07D217/26 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/04 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D417/12 , C07D471/04
摘要： The present invention relates to 1-phenyl-substituted heterocyclyl derivatives of the formula (I), wherein X, Y, Z, n, R1, R2, R3, R4, R5, R6, R7 and R10 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
摘要翻译：本发明涉及式（I）的1-苯基取代的杂环基衍生物，其中X，Y，Z，n，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 10如说明书和其用作前列腺素受体调节剂，最特别地作为前列腺素D2受体调节剂用于治疗各种前列腺素介导的疾病和病症，含有这些化合物的药物组合物及其制备方法。

18. 发明申请

US20120101111A1 NOVEL OXAZOLIDINONE DERIVIATIVES 有权
标题翻译：新型氧杂环丁酮衍生物
公开(公告)号：US20120101111A1
公开(公告)日：2012-04-26
申请号：US13319780
申请日：2010-05-11
申请人： Hamed Aissaoui , Christoph Boss , Christine Brotschi , Markus Gude , Romain Siegrist , Thierry Sifferlen , Jodi T. Williams
发明人： Hamed Aissaoui , Christoph Boss , Christine Brotschi , Markus Gude , Romain Siegrist , Thierry Sifferlen , Jodi T. Williams
IPC分类号： A61K31/497 , A61K31/428 , A61K31/421 , C07D417/02 , A61P25/28 , C07D413/02 , A61P25/30 , A61P25/00 , A61P25/20 , A61P25/18 , A61K31/4439 , C07D263/18
CPC分类号： C07D263/18 , C07D263/56 , C07D413/06 , C07D413/10 , C07D417/06 , C07D417/10
摘要： The present invention relates to oxazolidinone derivatives of formula (I) wherein Y, R3 and R4 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.
摘要翻译：本发明涉及式（I）的恶唑烷酮衍生物，其中Y，R 3和R 4如本说明书所述，其制备方法，其药学上可接受的盐及其作为药物的用途，含有一种或多种化合物式（I），特别是它们作为食欲素受体拮抗剂的用途。

19. 发明申请

US20110212968A1 PHENETHYLAMIDE DERIVATIVES AND THEIR HETEROCYCLIC ANALOGUES 审中-公开
标题翻译：苯乙烯衍生物及其杂环类似物
公开(公告)号：US20110212968A1
公开(公告)日：2011-09-01
申请号：US13124233
申请日：2009-10-13
申请人： Hamed Aissaoui , Christoph Boss , Christine Brotschi , Ralf Koberstein , Romain Siegrist , Thierry Sifferlen , Daniel Trachsel , Jodi T. Williams
发明人： Hamed Aissaoui , Christoph Boss , Christine Brotschi , Ralf Koberstein , Romain Siegrist , Thierry Sifferlen , Daniel Trachsel , Jodi T. Williams
IPC分类号： A61K31/502 , A61K31/4965 , A61K31/437 , A61K31/44 , A61K31/4192 , A61K31/426 , A61K31/421 , C07D237/28 , C07D241/18 , C07D471/04 , C07D213/81 , C07D285/06 , C07D277/28 , C07D263/34 , A61P25/32 , A61P25/20 , A61P25/30 , A61P25/22 , A61P25/00 , A61P25/28
CPC分类号： C07D277/30 , C07D213/63 , C07D235/04 , C07D237/28 , C07D239/34 , C07D241/18 , C07D263/36 , C07D285/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , C07D417/14
摘要： The invention relates to novel phenethylamide derivatives and their wherein A, B, R1, R2 and R3 are as described in the application, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
摘要翻译：本发明涉及新的苯乙酰胺衍生物，其中A，B，R 1，R 2和R 3如本申请中所述，以及这些化合物或这些化合物的药学上可接受的盐作为药物，特别是食欲素受体拮抗剂

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