公开(公告)号：US09421244B2

公开(公告)日：2016-08-23

申请号：US13638821

申请日：2011-04-04

申请人： Dae Jin Kim ,  Min Young Kim ,  Jin Sun Kim ,  Sung Hee Hong ,  Sung Youb Jung ,  Se Chang Kwon

发明人： Dae Jin Kim ,  Min Young Kim ,  Jin Sun Kim ,  Sung Hee Hong ,  Sung Youb Jung ,  Se Chang Kwon

IPC分类号： A61K38/21 ,  A61K47/48 ,  C07K14/565 ,  C07K19/00

CPC分类号： A61K38/215 ,  A61K47/68 ,  A61K47/6813 ,  A61K47/6835 ,  C07K14/565 ,  C07K19/00 ,  C07K2317/52 ,  C07K2317/732 ,  C07K2317/734 ,  C07K2319/30

摘要： The present invention relates to a long-acting interferon beta formulation having improved in vivo duration and stability, comprising an interferon beta conjugate that is prepared by covalently linking interferon beta with an immunoglobulin Fc region via a non-peptidyl polymer, and a preparation method thereof. The long-acting interferon beta formulation of the present invention maintains in vivo activity of interferon beta at a relatively high level and remarkably increases the serum half-life thereof, thereby being used for various diseases, for which interferon is efficacious.

摘要翻译： 本发明涉及具有改善的体内持续时间和稳定性的长效型干扰素β制剂，其包含通过非肽基聚合物共价连接干扰素β与免疫球蛋白Fc区制备的干扰素β偶联物及其制备方法 。 本发明的长效干扰素β配方维持干扰素β的体内活性在相当高的水平，并显着提高其血清半衰期，从而被用于干扰素有效的各种疾病。

公开(公告)号：US09061072B2

公开(公告)日：2015-06-23

申请号：US13809783

申请日：2011-07-14

申请人： Sung Hee Hong ,  Byung Sun Lee ,  Dae Seong Im ,  Jae Min Lee ,  Sung Min Bae ,  Se Chang Kwon

发明人： Sung Hee Hong ,  Byung Sun Lee ,  Dae Seong Im ,  Jae Min Lee ,  Sung Min Bae ,  Se Chang Kwon

IPC分类号： C07K17/06 ,  A61K39/00 ,  A61K47/48 ,  A61K9/00 ,  A61K9/08 ,  A61K38/27 ,  A61K47/26 ,  A61K47/12

CPC分类号： A61K47/48415 ,  A61K9/0019 ,  A61K9/08 ,  A61K38/27 ,  A61K47/12 ,  A61K47/26 ,  A61K47/60 ,  A61K47/68 ,  C07K2319/30

摘要： Disclosed is a liquid formulation of long-acting human growth hormone (hGH) conjugate, free of albumin, which can guarantee the stability of the long-acting hGH conjugate when stored over a long period of time, wherein the long-acting human growth hormone conjugate includes a human growth hormone linked to an immunoglobulin Fc region, and has a prolonged in vivo stability compared to the native form. The liquid formulation of hGH conjugate including a pH 5.0˜6.0 buffer, a sugar alcohol, a salt and a non-ionic surfactant is free of human serum albumin and other hazardous factors which are potentially contaminated with viruses, and can provide excellent storage stability customized for a long-acting hGH conjugate composed of an hGH polypeptide and an immunoglobulin Fc region which has higher molecular weight and in vivo durability, compared to the native.

摘要翻译： 公开了长效人生长激素（hGH）缀合物的液体制剂，其不含白蛋白，其可以长期保存长效hGH缀合物的稳定性，其中长效人生长激素 缀合物包括与免疫球蛋白Fc区连接的人生长激素，并且与天然形式相比具有延长的体内稳定性。 包含pH 5.0〜6.0缓冲液，糖醇，盐和非离子表面活性剂的hGH缀合物的液体制剂不含人血清白蛋白和潜在的病毒污染的其他有害因素，可提供优良的储存稳定性 对于由hGH多肽和具有较高分子量和体内耐久性的免疫球蛋白Fc区组成的长效hGH缀合物，与天然产物相比。

公开(公告)号：US20130115231A1

公开(公告)日：2013-05-09

申请号：US13809783

申请日：2011-07-14

申请人： Sung Hee Hong ,  Byung Sun Lee ,  Dae Seong Im ,  Jae Min Lee ,  Sung Min Bae ,  Se Chang Kwon

发明人： Sung Hee Hong ,  Byung Sun Lee ,  Dae Seong Im ,  Jae Min Lee ,  Sung Min Bae ,  Se Chang Kwon

IPC分类号： A61K47/48

CPC分类号： A61K47/48415 ,  A61K9/0019 ,  A61K9/08 ,  A61K38/27 ,  A61K47/12 ,  A61K47/26 ,  A61K47/60 ,  A61K47/68 ,  C07K2319/30

摘要： Disclosed is a liquid formulation of long-acting human growth hormone (hGH) conjugate, free of albumin, which can guarantee the stability of the long-acting hGH conjugate when stored over a long period of time, wherein the long-acting human growth hormone conjugate includes a human growth hormone linked to an immunoglobulin Fc region, and has a prolonged in vivo stability compared to the native form. The liquid formulation of hGH conjugate including a pH 5.0˜6.0 buffer, a sugar alcohol, a salt and a non-ionic surfactant is free of human serum albumin and other hazardous factors which are potentially contaminated with viruses, and can provide excellent storage stability customized for a long-acting hGH conjugate composed of an hGH polypeptide and an immunoglobulin Fc region which has higher molecular weight and in vivo durability, compared to the native.

摘要翻译： 公开了长效人生长激素（hGH）缀合物的液体制剂，其不含白蛋白，其可以长期保存长效hGH缀合物的稳定性，其中长效人生长激素 缀合物包括与免疫球蛋白Fc区连接的人生长激素，并且与天然形式相比具有延长的体内稳定性。 包含pH 5.0〜6.0缓冲液，糖醇，盐和非离子表面活性剂的hGH缀合物的液体制剂不含人血清白蛋白和其他可能被病毒污染的危险因素，可以提供优良的储存稳定性 对于由hGH多肽和具有较高分子量和体内耐久性的免疫球蛋白Fc区组成的长效hGH缀合物，与天然产物相比。

公开(公告)号：US20100144708A1

公开(公告)日：2010-06-10

申请号：US12376889

申请日：2007-08-10

申请人： Gyoon Hee Han ,  Eun Hyun Choi ,  Jee Sun Yang ,  Sung Hee Hong ,  Myung Sook Kim ,  Mi Sun Won ,  Kyung Sook Chung ,  Dong Myung Kim ,  Hyang Sook Yoo ,  Hwan Mook Kim ,  Song Kyu Park ,  Ki Ho Lee ,  Chang Woo Lee ,  Youn Woong Choi ,  Yong Mi Jeong ,  Byung Gu Min

发明人： Gyoon Hee Han ,  Eun Hyun Choi ,  Jee Sun Yang ,  Sung Hee Hong ,  Myung Sook Kim ,  Mi Sun Won ,  Kyung Sook Chung ,  Dong Myung Kim ,  Hyang Sook Yoo ,  Hwan Mook Kim ,  Song Kyu Park ,  Ki Ho Lee ,  Chang Woo Lee ,  Youn Woong Choi ,  Yong Mi Jeong ,  Byung Gu Min

IPC分类号： A61K31/551 ,  C07D243/08 ,  C07D211/96 ,  A61K31/4965 ,  A61P35/04

CPC分类号： C07D295/185 ,  C07D243/08 ,  C07D295/26

摘要： The present invention relates to new heterocyclic compounds containing nitrogen atoms or pharmaceutically acceptable salts thereof, a process for the preparation thereof, and a pharmaceutical composition comprising the same for treatment of cancer. The compounds according to the present invention induce DNA damage due to reactive oxygen species to activate c-abl and p53, induce RhoB to generate apoptosis, and induce cell death by down-regulating Bcl2 involved in cell survival, which is generated by dysregulated signals via the mitochondria pathway, thereby inhibiting tumor cell growth and inducing apoptosis. Accordingly, the composition according to the present invention can be used to treat cancer.

摘要翻译： 本发明涉及含有氮原子的新的杂环化合物或其药学上可接受的盐，其制备方法和包含其的用于治疗癌症的药物组合物。 根据本发明的化合物诱导由于活性氧物质引起的DNA损伤以激活c-abl和p53，诱导RhoB产生凋亡，并通过下调参与细胞存活的Bcl2诱导细胞死亡，其由失调信号通过 线粒体途径，从而抑制肿瘤细胞生长并诱导细胞凋亡。 因此，本发明的组合物可用于治疗癌症。