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1. 发明授权

US09062056B2 Aza-benzimidazolone Chymase inhibitors 有权
标题翻译：氮杂 - 苯并咪唑酮胃促胰酶抑制剂
公开(公告)号：US09062056B2
公开(公告)日：2015-06-23
申请号：US13062749
申请日：2009-08-25
申请人： Michel Jose Emmanuel , Xin Guo , Jin Mi Kim , Ho Yin Lo , Peter Allen Nemoto , Kevin Chungeng Qian
发明人： Michel Jose Emmanuel , Xin Guo , Jin Mi Kim , Ho Yin Lo , Peter Allen Nemoto , Kevin Chungeng Qian
IPC分类号： C07D471/04 , C07D487/04
CPC分类号： C07D487/04 , C07D471/04
摘要： Disclosed are small molecule inhibitors of the formula (I): and the pharmaceutical compositions thereof and processes of making the same. The compounds are useful in treating various diseases and conditions involving chymase.
摘要翻译：公开了式（I）的小分子抑制剂及其药物组合物及其制备方法。该化合物可用于治疗涉及胃促胰酶的各种疾病和病症。

2. 发明申请

US20110104741A1 Screening Method for Inhibitors of Cancer Cell Invasion and Screening System Thereof 审中-公开
标题翻译：癌细胞侵袭抑制剂筛选方法及筛选方法
公开(公告)号：US20110104741A1
公开(公告)日：2011-05-05
申请号：US13000483
申请日：2008-12-24
申请人： Da-Woon Jung , Jin Mi Kim , Zhong Min Che , Young-Tae Chang
发明人： Da-Woon Jung , Jin Mi Kim , Zhong Min Che , Young-Tae Chang
IPC分类号： C12Q1/02 , C12M1/34
CPC分类号： G01N33/5011 , G01N33/5044
摘要： This invention relates to a screening method for an inhibitor to cancer cell invasion, comprising the steps of: (a) co-culturing cancer cells and a carcinoma-associated fibroblasts (CAFs) in a multi-chamber containing a upper-chamber, a lower-chamber and a porous filter separating the upper-chamber from the lower-chamber; in which each cancer cells and CAFs is inoculated into the upper-chamber and the lower-chamber of the multi-chamber, and then a candidate is added to the upper-chamber; and (b) measuring the number of cancer cells passing the porous filter. According to the screening system and screening method using the same, the inhibitor to cancer cell invasion is able to be screened in a high-throughput manner.
摘要翻译：本发明涉及一种抑制剂对癌细胞侵袭的筛选方法，其特征在于包括以下步骤：（a）在含有上室，下部的多室中共同培养癌细胞和癌相关成纤维细胞（CAF） - 室和将上室与下室分离的多孔过滤器; 其中将每个癌细胞和CAF接种到多室的上室和下室中，然后将候选物加入到上室中; 和（b）测量通过多孔过滤器的癌细胞的数量。根据使用其的筛选系统和筛选方法，能够以高通量的方式筛选癌细胞侵袭抑制剂。

3. 发明授权

US07345074B2 Derivatives of [6,7-dihydro-5H-imidazol[1,2-a]imidazole-3-sulfonylamino]-propionamide 有权
标题翻译： [6,7-二氢-5H-咪唑并[1,2-a]咪唑-3-磺酰基氨基] - 丙酰胺的衍生物
公开(公告)号：US07345074B2
公开(公告)日：2008-03-18
申请号：US10969105
申请日：2004-10-20
申请人： Terence Alfred Kelly , Jin Mi Kim , René Marc Lemieux
发明人： Terence Alfred Kelly , Jin Mi Kim , René Marc Lemieux
IPC分类号： A61K31/4166 , C07D235/02 , C07D403/02
CPC分类号： A61K31/4166 , A61K31/506 , A61K31/5355 , C07D487/04
摘要： Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
摘要翻译： [6,7-二氢-5H-咪唑并[1,2-a]咪唑-3-磺酰氨基] - 丙酰胺的衍生物，其对CAM和白细胞整合素的相互作用具有良好的抑制作用，因此可用于治疗炎性疾病。

4. 发明授权

US06852748B1 Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide 有权
标题翻译： [6,7-二氢-5H-咪唑并[1,2-a]咪唑-3-磺酰基] - 吡咯烷-2-甲酸酰胺的衍生物
公开(公告)号：US06852748B1
公开(公告)日：2005-02-08
申请号：US10685638
申请日：2003-10-15
申请人： Terence Alfred Kelly , Jin Mi Kim , René Marc Lemieux , Matt Aaron Tschantz
发明人： Terence Alfred Kelly , Jin Mi Kim , René Marc Lemieux , Matt Aaron Tschantz
IPC分类号： A61K31/4166 , A61K31/4188 , A61K31/5375 , A61P29/00 , C07D235/02 , C07D403/12 , C07D413/02 , C07D487/04
CPC分类号： C07D487/04 , A61K31/4188
摘要： Derivatives of 6,7-dihydro-5H-imidazo[1,2-α]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
摘要翻译： 6,7-二氢-5H-咪唑并[1,2-α]咪唑-3-磺酰基] - 吡咯烷-2-甲酸酰胺的衍生物，其对CAM和白血球素蛋白的相互作用具有良好的抑制作用，因此可用于治疗炎症性疾病。

5. 发明授权

US06844360B2 Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide 有权
公开(公告)号：US06844360B2
公开(公告)日：2005-01-18
申请号：US10686073
申请日：2003-10-15
申请人： Terence Alfred Kelly , Jin Mi Kim , René Marc Lemieux
发明人： Terence Alfred Kelly , Jin Mi Kim , René Marc Lemieux
IPC分类号： A61P37/00 , C07D487/04 , A61K31/4166 , C07D235/02 , C07D403/02
CPC分类号： A61K31/4166 , A61K31/506 , A61K31/5355 , C07D487/04
摘要： Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.

6. 发明授权

US09150556B2 Benzimidazolone chymase inhibitors 有权
标题翻译：苯并咪唑酮胃促胰酶抑制剂
公开(公告)号：US09150556B2
公开(公告)日：2015-10-06
申请号：US12596152
申请日：2008-05-15
申请人： Asitha Abeywardane , Brian Nicholas Cook , Stephane De Lombaert , Michel Jose Emmanuel , Xin Guo , Ming-Hong Hao , Jin Mi Kim , Ho Yin Lo , Chuk Chui Man , Tina Marie Morwick , Peter Allen Nemoto , Kevin Chungeng Qian , Hidenori Takahashi , Steven John Taylor
发明人： Asitha Abeywardane , Brian Nicholas Cook , Stephane De Lombaert , Michel Jose Emmanuel , Xin Guo , Ming-Hong Hao , Jin Mi Kim , Ho Yin Lo , Chuk Chui Man , Tina Marie Morwick , Peter Allen Nemoto , Kevin Chungeng Qian , Hidenori Takahashi , Steven John Taylor
IPC分类号： C07D235/26 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04
CPC分类号： C07D409/06 , C07D235/26 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04
摘要： Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase.
摘要翻译：公开了可用于治疗涉及胃促胰酶的各种疾病和病症的小分子抑制剂。

7. 发明授权

US07670602B2 Concatameric immunoadhesion molecule 有权
标题翻译：共聚蛋白免疫粘附分子
公开(公告)号：US07670602B2
公开(公告)日：2010-03-02
申请号：US11739288
申请日：2007-04-24
申请人： Yong-Hoon Chung , Ji-Woong Han , Hye-Ja Lee , Eun-Yong Choi , Jin-Mi Kim
发明人： Yong-Hoon Chung , Ji-Woong Han , Hye-Ja Lee , Eun-Yong Choi , Jin-Mi Kim
IPC分类号： A61K39/395
CPC分类号： C07K14/70507 , A61K2039/505 , C07K14/70521 , C07K14/7151 , C07K2319/00 , C07K2319/30
摘要： Disclosed are concatameric proteins comprising two soluble domains, in which the C-terminus of a soluble domain of a biologically active protein is linked to the N-terminus of an identical soluble domain or a distinct soluble domain of a biologically active protein. Also, the present invention discloses dimeric proteins formed by formation of intermolecular disulfide bonds at the hinge region of two monomeric proteins formed by linkage of a concatamer of two identical soluble extracellular regions of proteins involving immune response to an Fc fragment of an immunoglobulin molecule, their glycosylated proteins, DNA constructs encoding the monomeric proteins, recombinant expression plasmids containing the DNA construct, host cells transformed or transfected with the recombinant expression plasmids, and a method of preparing the dimeric proteins by culturing the host cells. Further, the present invention discloses pharmaceutical or diagnostic compositions comprising the dimeric protein or its glycosylated form.
摘要翻译：公开了包含两个可溶性结构域的连续蛋白质，其中生物活性蛋白质的可溶性结构域的C末端与生物活性蛋白质的相同可溶性结构域或不同可溶性结构域的N末端连接。此外，本发明公开了通过在两个单体蛋白的铰链区上形成分子间二硫键而形成的二聚体蛋白，该两个单体蛋白是通过将免疫应答涉及免疫应答的两个相同的可溶胞外区的连接体与免疫球蛋白分子的Fc片段糖基化蛋白质，编码单体蛋白的DNA构建体，含有DNA构建体的重组表达质粒，用重组表达质粒转化或转染的宿主细胞，以及通过培养宿主细胞制备二聚体蛋白质的方法。此外，本发明公开了包含二聚体蛋白质或其糖基化形式的药物或诊断组合物。

8. 发明申请

US20090011466A1 CONCATAMERIC IMMUNOADHESION MOLECULE 有权
标题翻译：综合免疫分子
公开(公告)号：US20090011466A1
公开(公告)日：2009-01-08
申请号：US11739288
申请日：2007-04-24
申请人： Yong-Hoon CHUNG , Ji-Woong HAN , Hye-Ja LEE , Eun-Yong CHOI , Jin-Mi KIM
发明人： Yong-Hoon CHUNG , Ji-Woong HAN , Hye-Ja LEE , Eun-Yong CHOI , Jin-Mi KIM
IPC分类号： C12P21/02 , C07K14/54 , C12N15/62 , C12N15/85 , C12N5/10
CPC分类号： C07K14/70507 , A61K2039/505 , C07K14/70521 , C07K14/7151 , C07K2319/00 , C07K2319/30
摘要： Disclosed are concatameric proteins comprising two soluble domains, in which the C-terminus of a soluble domain of a biologically active protein is linked to the N-terminus of an identical soluble domain or a distinct soluble domain of a biologically active protein. Also, the present invention discloses dimeric proteins formed by formation of intermolecular disulfide bonds at the hinge region of two monomeric proteins formed by linkage of a concatamer of two identical soluble extracellular regions of proteins involving immune response to an Fc fragment of an immunoglobulin molecule, their glycosylated proteins, DNA constructs encoding the monomeric proteins, recombinant expression plasmids containing the DNA construct, host cells transformed or transfected with the recombinant expression plasmids, and a method of preparing the dimeric proteins by culturing the host cells. Further, the present invention discloses pharmaceutical or diagnostic compositions comprising the dimeric protein or its glycosylated form.
摘要翻译：公开了包含两个可溶性结构域的连续蛋白质，其中生物活性蛋白质的可溶性结构域的C末端与生物活性蛋白质的相同可溶性结构域或不同可溶性结构域的N末端连接。此外，本发明公开了通过在两个单体蛋白的铰链区上形成分子间二硫键而形成的二聚体蛋白，该两个单体蛋白是通过将免疫应答涉及免疫应答的两个相同的可溶胞外区的连接体与免疫球蛋白分子的Fc片段糖基化蛋白质，编码单体蛋白的DNA构建体，含有DNA构建体的重组表达质粒，用重组表达质粒转化或转染的宿主细胞，以及通过培养宿主细胞制备二聚体蛋白质的方法。此外，本发明公开了包含二聚体蛋白质或其糖基化形式的药物或诊断组合物。

9. 发明授权

US07468382B2 Pyridine derivatives useful as inhibitors of PKC-theta 有权
标题翻译：可用作PKC-θ抑制剂的吡啶衍生物
公开(公告)号：US07468382B2
公开(公告)日：2008-12-23
申请号：US11277536
申请日：2006-03-27
申请人： Steven Richard Brunette , Jin Mi Kim , Rene′ Marc Lemieux , Matt Aaron Tschantz
发明人： Steven Richard Brunette , Jin Mi Kim , Rene′ Marc Lemieux , Matt Aaron Tschantz
IPC分类号： A01N43/40 , A61K31/44 , C07D211/72 , C07D211/84 , C07D213/00 , C07D213/72
CPC分类号： C07D213/74 , C07D213/82 , C07D213/85 , C07D401/12
摘要： Disclosed are novel compounds of formula (I): wherein R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
摘要翻译：公开了式（I）的新化合物：其中R 1，R 2和R 3如本文所定义，其可用作PKC-θ的抑制剂，因此可用于治疗通过该活性介导或维持的多种疾病和病症的PKC-θ，包括免疫学障碍和II型糖尿病。本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。

10. 发明授权

US07462637B2 Derivatives of [6,7-dihydro-5H-imidazo[1,2--a]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide 有权
标题翻译： [6,7-二氢-5H-咪唑并[1,2-a]咪唑-3-磺酰基] - 吡咯烷-2-甲酸酰胺的衍生物
公开(公告)号：US07462637B2
公开(公告)日：2008-12-09
申请号：US10969698
申请日：2004-10-20
申请人： Terence A. Kelly , Jin Mi Kim , René Marc Lemieux , Matt Aaron Tschantz
发明人： Terence A. Kelly , Jin Mi Kim , René Marc Lemieux , Matt Aaron Tschantz
IPC分类号： A61K31/4188 , A61K31/5375 , C07D235/02 , C07D403/12
CPC分类号： C07D487/04 , A61K31/4188
摘要： Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
摘要翻译： 6,7-二氢-5H-咪唑并[1,2-a]咪唑-3-磺酰基]吡咯烷-2-甲酸酰胺的衍生物，其对CAM和白血球素蛋白的相互作用具有良好的抑制作用，因此可用于治疗炎症性疾病。

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