公开(公告)号：US08329684B2

公开(公告)日：2012-12-11

申请号：US13467019

申请日：2012-05-08

申请人： Young Lag Cho ,  Joung Yul Yun ,  Sang Eun Chae ,  Chul Soon Park ,  Hyang Sook Lee ,  Kyu Man Oh ,  Hye Jin Kang ,  Dae Hyuck Kang ,  Young Jae Yang ,  Hyun Jin Kwon ,  Tae Kyo Park ,  Sung Ho Woo ,  Young Zu Kim

发明人： Young Lag Cho ,  Joung Yul Yun ,  Sang Eun Chae ,  Chul Soon Park ,  Hyang Sook Lee ,  Kyu Man Oh ,  Hye Jin Kang ,  Dae Hyuck Kang ,  Young Jae Yang ,  Hyun Jin Kwon ,  Tae Kyo Park ,  Sung Ho Woo ,  Young Zu Kim

IPC分类号： A61K31/545 ,  C07D501/14

CPC分类号： C07D501/60 ,  C07D501/24 ,  C07D501/46

摘要： The present invention relates to novel cephalosporin derivatives represented by Chemical Formula 1. Wherein, X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. Compounds of the present invention are effective ingredients for the broad spectrum of antibiotic resistance, exhibit low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.

摘要翻译： 本发明涉及由化学式1表示的新型头孢菌素衍生物。其中，X，Y，L，R 1和R 2与本发明的描述中所定义相同。 本发明还涉及药物抗生素组合物，其包含由化学式1表示的新型胞孢素衍生物，其前药，其水合物，其溶剂合物，其异构体或其药学上可接受的盐作为有效成分。 本发明的化合物是广谱抗生素抗性的有效成分，表现出低毒性，特别是在革兰氏阴性细菌中，其可用于强抗微生物活性。

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。