公开(公告)号：US08288423B2

公开(公告)日：2012-10-16

申请号：US12598010

申请日：2008-05-09

申请人： Young Lag Cho ,  Ho Young Song ,  Dae Yon Lee ,  Sung Yoon Baek ,  Sang Eun Chae ,  Sang Hui Jo ,  Yeon Ok Kim ,  Hyang Sook Lee ,  Ju Hyun Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

发明人： Young Lag Cho ,  Ho Young Song ,  Dae Yon Lee ,  Sung Yoon Baek ,  Sang Eun Chae ,  Sang Hui Jo ,  Yeon Ok Kim ,  Hyang Sook Lee ,  Ju Hyun Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

IPC分类号： A01N43/64 ,  A01N43/76 ,  A01N43/50 ,  A01N43/02 ,  A01N43/06 ,  A61K31/41 ,  A61K31/42 ,  A61K31/415 ,  A61K31/38

CPC分类号： C07D413/14

摘要： The present invention relates to novel oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof, and processes for preparing the same, and pharmaceutical compositions comprising the same. The oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof can be usefully employed as an anticoagulant for treating thromboembolism and tumors via inhibition of coagulation factor Xa.

摘要翻译： 本发明涉及具有环脒的新的恶唑烷酮衍生物及其前体药物，水合物，溶剂合物，异构体和药学上可接受的盐及其制备方法，以及包含其的药物组合物。 具有环脒的恶唑烷酮衍生物及其前体药物，水合物，溶剂合物，异构体和药学上可接受的盐可有效地用作通过抑制凝血因子Xa治疗血栓栓塞和肿瘤的抗凝血剂。

公开(公告)号：US20100184781A1

公开(公告)日：2010-07-22

申请号：US12598010

申请日：2008-05-09

申请人： Young Lag Cho ,  Ho Young Song ,  Dae Yon Lee ,  Sung Yoon Baek ,  Sang Eun Chae ,  Sang Hui Jo ,  Yeon Ok Kim ,  Hyang Sook Lee ,  Ju Hyun Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

发明人： Young Lag Cho ,  Ho Young Song ,  Dae Yon Lee ,  Sung Yoon Baek ,  Sang Eun Chae ,  Sang Hui Jo ,  Yeon Ok Kim ,  Hyang Sook Lee ,  Ju Hyun Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

IPC分类号： A61K31/506 ,  C07D413/14 ,  A61K31/422 ,  C07D409/14 ,  A61K31/4439 ,  A61P9/10 ,  A61P29/00 ,  A61P9/00

CPC分类号： C07D413/14

摘要： The present invention relates to novel oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof, and processes for preparing the same, and pharmaceutical compositions comprising the same. The oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof can be usefully employed as an anticoagulant for treating thromboembolism and tumors via inhibition of coagulation factor Xa.

摘要翻译： 本发明涉及具有环脒的新的恶唑烷酮衍生物及其前体药物，水合物，溶剂合物，异构体和药学上可接受的盐及其制备方法，以及包含其的药物组合物。 具有环脒的恶唑烷酮衍生物及其前体药物，水合物，溶剂合物，异构体和药学上可接受的盐可有效地用作通过抑制凝血因子Xa治疗血栓栓塞和肿瘤的抗凝血剂。

公开(公告)号：US20110112083A1

公开(公告)日：2011-05-12

申请号：US13002271

申请日：2009-06-05

申请人： Ho Young Song ,  Young Lag Cho ,  Dae Yon Lee ,  Hee Sock Park ,  Sung Yoon Baek ,  Sang Eun Chae ,  Sang Hui Jo ,  Yeon Ok Kim ,  Hyang Sook Lee ,  Ju Hyun Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

发明人： Ho Young Song ,  Young Lag Cho ,  Dae Yon Lee ,  Hee Sock Park ,  Sung Yoon Baek ,  Sang Eun Chae ,  Sang Hui Jo ,  Yeon Ok Kim ,  Hyang Sook Lee ,  Ju Hyun Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

IPC分类号： A61K31/5395 ,  C07D413/14 ,  C07D487/04 ,  A61K31/53 ,  A61P7/02 ,  A61P9/10 ,  A61P29/00 ,  A61P25/00 ,  A61P9/00 ,  A61P11/00

CPC分类号： C07D413/14 ,  C07D487/04

摘要： The present invention relates to novel oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group, pharmaceutically acceptable salts thereof, methods for preparing the same and pharmaceutical compositions comprising the same. The oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group or the pharmaceutically acceptable salts thereof can be effectively used for the treatment of thromboembolism and tumor as an anticoagulant based on the inhibition of factor Xa.

摘要翻译： 本发明涉及具有环状偕胺肟或环状氨基腙基的新的恶唑烷酮衍生物，其药学上可接受的盐，其制备方法和包含其的药物组合物。 具有环偕胺肟或环状氨基腙基的恶唑烷酮衍生物或其药学上可接受的盐可以有效地用于基于对因子Xa的抑制作为抗凝血剂治疗血栓栓塞和肿瘤。

公开(公告)号：US08178525B2

公开(公告)日：2012-05-15

申请号：US13002271

申请日：2009-06-05

申请人： Ho Young Song ,  Young Lag Cho ,  Dae Yon Lee ,  Hee Sock Park ,  Sung Yoon Baek ,  Sang Eun Chae ,  Sang Hui Jo ,  Yeon Ok Kim ,  Hyang Sook Lee ,  Ju Hyun Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

发明人： Ho Young Song ,  Young Lag Cho ,  Dae Yon Lee ,  Hee Sock Park ,  Sung Yoon Baek ,  Sang Eun Chae ,  Sang Hui Jo ,  Yeon Ok Kim ,  Hyang Sook Lee ,  Ju Hyun Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

IPC分类号： C07D413/12 ,  C07D413/14 ,  C07D487/04 ,  A61K31/5395 ,  A61K31/53

CPC分类号： C07D413/14 ,  C07D487/04

摘要： Disclosed are novel oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group, pharmaceutically acceptable salts thereof, methods for preparing the same and pharmaceutical compositions containing the same. The oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group or the pharmaceutically acceptable salts thereof can be effectively used for the treatment of thromboembolism and tumor as an anticoagulant based on the inhibition of factor Xa.

摘要翻译： 公开了具有环状偕胺肟或环状氨基腙基团的新型恶唑烷酮衍生物，其药学上可接受的盐，其制备方法和含有它们的药物组合物。 具有环偕胺肟或环状氨基腙基的恶唑烷酮衍生物或其药学上可接受的盐可以有效地用于基于对因子Xa的抑制作为抗凝血剂治疗血栓栓塞和肿瘤。

公开(公告)号：US08809541B2

公开(公告)日：2014-08-19

申请号：US13818355

申请日：2011-08-25

申请人： Hyung Sub Gwak ,  Yong Zu Kim ,  Uk Il Kim ,  Byeong Deog Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Joung Yul Yun ,  Dae Yon Lee ,  Hyang Sook Lee ,  Jeong Eun Jeon ,  Se Kyoo Jeong ,  Hyung Mook Choi

发明人： Hyung Sub Gwak ,  Yong Zu Kim ,  Uk Il Kim ,  Byeong Deog Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Joung Yul Yun ,  Dae Yon Lee ,  Hyang Sook Lee ,  Jeong Eun Jeon ,  Se Kyoo Jeong ,  Hyung Mook Choi

IPC分类号： A61K31/497 ,  C07D211/32 ,  A61Q19/00 ,  A61K8/49 ,  C07D471/04 ,  C07D235/08

CPC分类号： C07D235/08 ,  A61K8/4946 ,  A61Q19/00 ,  A61Q19/007 ,  A61Q19/008 ,  C07D471/04

摘要： Provided are heterocyclic compounds, having effects of treating and preventing inflammatory diseases and treating skin wounds, and particularly, exhibiting effects of recovering disrupted skin barriers, mitigating inflammation, and pruritus. Also, a composition containing the compound as an effective component can be used to mitigate various inflammatory diseases and protease activated receptor-2 (PAR-2)-overexpressed diseases, and can be particularly used as a composition having an anti-inflammatory function in inflammatory skin diseases including atopic dermatitis and the like, by inhibiting PAR-2 activity.

摘要翻译： 提供具有治疗和预防炎性疾病和治疗皮肤伤口的作用的杂环化合物，特别是显示恢复破坏的皮肤屏障，减轻炎症和瘙痒的作用。 此外，含有该化合物作为有效成分的组合物可用于缓解各种炎性疾病和蛋白酶活化受体-2（PAR-2） - 去表达疾病，并且可特别用作具有炎性功能的组合物 皮肤病，包括特应性皮炎等，通过抑制PAR-2活性。

公开(公告)号：US20130165652A1

公开(公告)日：2013-06-27

申请号：US13818420

申请日：2011-08-25

申请人： Hyung Sub Gwak ,  Yong Zu Kim ,  Uk Il Kim ,  Byeong Deog Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Joung Yul Yun ,  Dae Yon Lee ,  Hyang Sook Lee ,  Jeong Eun Jeon ,  Se Kyoo Jeong ,  Hyung Mook Choi

发明人： Hyung Sub Gwak ,  Yong Zu Kim ,  Uk Il Kim ,  Byeong Deog Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Joung Yul Yun ,  Dae Yon Lee ,  Hyang Sook Lee ,  Jeong Eun Jeon ,  Se Kyoo Jeong ,  Hyung Mook Choi

IPC分类号： C07D471/04

CPC分类号： C07D235/08 ,  A61K8/4946 ,  A61Q19/00 ,  A61Q19/007 ,  A61Q19/008 ,  C07D471/04

摘要： The heterocyclic compound according to the present invention may treat and prevent inflammatory diseases and heal skin wounds, and particularly, have effects of recovering damaged skin barrier, reducing inflammation and pruritus in inflammatory skin diseases. In addition, the composition containing the compound according to the present invention as an active ingredient may be used to alleviate various inflammatory diseases and diseases in which PAR-2 is excessively expressed, and particularly, the composition may inhibit activity of PAR-2 in skin, such that the composition may be used as a composition having anti-inflammatory function in inflammatory skin diseases including atopic dermatitis, or the like.

摘要翻译： 根据本发明的杂环化合物可以治疗和预防炎性疾病并愈合皮肤伤口，特别是具有恢复受损的皮肤屏障，减少炎性皮肤疾病中的炎症和瘙痒的作用。 此外，含有本发明化合物作为活性成分的组合物可以用于缓和各种炎性疾病和PAR-2过度表达的疾病，特别是该组合物可抑制PAR-2在皮肤中的活性 ，使得该组合物可以用作具有抗炎功能的组合物，所述炎性皮肤病包括特应性皮炎等。

公开(公告)号：US20130158047A1

公开(公告)日：2013-06-20

申请号：US13818355

申请日：2011-08-25

申请人： Hyung Sub Gwak ,  Yong Zu Kim ,  Uk Il Kim ,  Byeong Deog Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Joung Yul Yun ,  Dae Yon Lee ,  Hyang Sook Lee ,  Jeong Eun Jeon ,  Se Kyoo Jeong ,  Hyung Mook Choi

发明人： Hyung Sub Gwak ,  Yong Zu Kim ,  Uk Il Kim ,  Byeong Deog Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Joung Yul Yun ,  Dae Yon Lee ,  Hyang Sook Lee ,  Jeong Eun Jeon ,  Se Kyoo Jeong ,  Hyung Mook Choi

IPC分类号： C07D235/08

CPC分类号： C07D235/08 ,  A61K8/4946 ,  A61Q19/00 ,  A61Q19/007 ,  A61Q19/008 ,  C07D471/04

摘要： Provided are heterocyclic compounds, having effects of treating and preventing inflammatory diseases and treating skin wounds, and particularly, exhibiting effects of recovering disrupted skin barriers, mitigating inflammation, and pruritus. Also, a composition containing the compound as an effective component can be used to mitigate various inflammatory diseases and protease activated receptor-2 (PAR-2)-overexpressed diseases, and can be particularly used as a composition having an anti-inflammatory function in inflammatory skin diseases including atopic dermatitis and the like, by inhibiting PAR-2 activity.

摘要翻译： 提供具有治疗和预防炎性疾病和治疗皮肤伤口的作用的杂环化合物，特别是显示恢复破坏的皮肤屏障，减轻炎症和瘙痒的作用。 此外，含有该化合物作为有效成分的组合物可用于缓解各种炎性疾病和蛋白酶活化受体-2（PAR-2） - 去表达疾病，并且可特别用作具有炎性功能的组合物 皮肤病，包括特应性皮炎等，通过抑制PAR-2活性。

公开(公告)号：US07652152B2

公开(公告)日：2010-01-26

申请号：US11996011

申请日：2006-07-19

申请人： Kyoung Rok Roh ,  Ji Sang Yoo ,  Jong Won Jang ,  Dae Yon Lee

发明人： Kyoung Rok Roh ,  Ji Sang Yoo ,  Jong Won Jang ,  Dae Yon Lee

IPC分类号： C07D207/12

CPC分类号： C07D207/12 ,  Y02P20/55

摘要： A method of preparing optically pure (S)-3-hydroxypyrrolidine is disclosed. The present invention provides a method of economically and industrially preparing optically and chemically pure (S)-3-hydroxypyrrolidine, through a process comprising introducing an amine protecting group by using optically pure 4-amino-(S)-2-hydroxybutylic acid as a starting material, reducing a carboxylic acid group into a primary alcohol, removing the amine protecting group to form an amine salt, halogenating the primary alcohol, and amine cyclization; and through a simple purification process, i.e., distillation under reduced pressure. As another method, the present invention provides a method of preparing optically and chemically pure (S)-3-hydroxypyrrolidine, through a process comprising esterifying optically pure 4-amino-(S)-2-hydroxybutylic acid as a starting material, lactam cyclization, and reduction.

摘要翻译： 公开了制备光学纯的（S）-3-羟基吡咯烷的方法。 本发明提供了经济和工业上制备光学和化学纯的（S）-3-羟基吡咯烷的方法，其包括通过使用光学纯的4-氨基 - （S）-2-羟基丁酸作为 将羧酸基团还原成伯醇，除去胺保护基以形成胺盐，卤化伯醇和胺环化; 并通过简单的纯化方法，即减压蒸馏。 作为另一种方法，本发明提供了一种通过包括酯化光学纯的4-氨基 - （S）-2-羟基丁酸作为起始原料的方法制备光学和化学纯的（S）-3-羟基吡咯烷的方法，内酰胺环化 ，并减少。

公开(公告)号：US20080214837A1

公开(公告)日：2008-09-04

申请号：US11996011

申请日：2006-07-19

申请人： Kyoung Rok Roh ,  Ji Sang Yoo ,  Jong Won Jang ,  Dae Yon Lee

发明人： Kyoung Rok Roh ,  Ji Sang Yoo ,  Jong Won Jang ,  Dae Yon Lee

IPC分类号： C07D207/12

CPC分类号： C07D207/12 ,  Y02P20/55

摘要： A method of preparing optically pure (S)-3-hydroxypyrrolidine is disclosed. The present invention provides a method of economically and industrially preparing optically and chemically pure (S)-3-hydroxypyrrolidine, through a process comprising introducing an amine protecting group by using optically pure 4-amino-(S)-2-hydroxybutylic acid as a starting material, reducing a carboxylic acid group into a primary alcohol, removing the amine protecting group to form an amine salt, halogenating the primary alcohol, and amine cyclization; and through a simple purification process, i.e., distillation under reduced pressure. As another method, the present invention provides a method of preparing optically and chemically pure (S)-3-hydroxypyrrolidine, through a process comprising esterifying optically pure 4-amino-(S)-2-hydroxybutylic acid as a starting material, lactam cyclization, and reduction.

摘要翻译： 公开了制备光学纯的（S）-3-羟基吡咯烷的方法。 本发明提供了经济和工业上制备光学和化学纯的（S）-3-羟基吡咯烷的方法，其包括通过使用光学纯的4-氨基 - （S）-2-羟基丁酸作为 将羧酸基团还原成伯醇，除去胺保护基以形成胺盐，卤化伯醇和胺环化; 并通过简单的纯化方法，即减压蒸馏。 作为另一种方法，本发明提供了一种通过包括酯化光学纯的4-氨基 - （S）-2-羟基丁酸作为起始原料的方法制备光学和化学纯的（S）-3-羟基吡咯烷的方法，内酰胺环化 ，并减少。

公开(公告)号：US06353139B1

公开(公告)日：2002-03-05

申请号：US09792240

申请日：2001-02-26

申请人： Chul Ho Jun ,  Dae Yon Lee ,  Hyuk Lee ,  Jun Bae Hong

发明人： Chul Ho Jun ,  Dae Yon Lee ,  Hyuk Lee ,  Jun Bae Hong

IPC分类号： C07C4569

CPC分类号： C07C45/00 ,  C07F7/083

摘要： A method for preparing ketones has advantages of improving yields and reducing the time of the reactions due to high efficiency of catalysts. Ketones are prepared by reacting an aliphatic or an aromatic aldehyde with a vinyl olefin having an aliphatic or aromatic alkyl moiety in the presence of a transition metal catalyst, 2-aminopyridine catalyst, a primary amine and an acid, as catalysts and additives.

摘要翻译： 制备酮的方法具有提高产率和减少催化剂效率高的反应时间的优点。 酮是通过在过渡金属催化剂，2-氨基吡啶催化剂，伯胺和酸作为催化剂和添加剂的存在下使脂族或芳族醛与具有脂族或芳族烷基部分的乙烯基烯烃反应来制备的。