公开(公告)号：US08394799B2

公开(公告)日：2013-03-12

申请号：US12306319

申请日：2007-07-03

Applicant: Jung Joon Lee ,  Jeong-Hyung Lee ,  Kyeong Lee ,  Young-Soo Hong ,  B. K. Shanthaveerappa ,  Yinlan Jin ,  Jin Hwan Kim ,  Xuejun Jin

Inventor： Jung Joon Lee ,  Jeong-Hyung Lee ,  Kyeong Lee ,  Young-Soo Hong ,  B. K. Shanthaveerappa ,  Yinlan Jin ,  Jin Hwan Kim ,  Xuejun Jin

IPC: A61K31/5377 ,  A61K31/167 ,  A61K31/41 ,  A61K31/423 ,  A61P19/02 ,  C07C233/33 ,  C07D257/04 ,  C07D263/57 ,  C07D295/15

CPC classification number: C07C237/42 ,  C07C235/24 ,  C07C255/60 ,  C07C271/42 ,  C07C307/02 ,  C07C311/46 ,  C07C317/40 ,  C07C2603/74 ,  C07D213/38 ,  C07D213/75 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D235/12 ,  C07D257/04 ,  C07D263/56 ,  C07D307/52 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

Abstract: Disclosed herein are an HIF-1 inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient. The HIF-1 inhibitor shows anticancer activity thanks to the inhibition activity against HIF-1, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer; stomach cancer and breast cancer. Also, the compound having inhibition activity against HIF-1 is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HIF-1-mediated VEGF expression.

Abstract translation: 本文公开了HIF-1抑制剂，其制备方法和包含其作为活性成分的药物组合物。 HIF-1抑制剂由于对HIF-1的抑制活性而显示出抗癌活性，HIF-1是在癌症的生长和转移中起重要作用的转录因子，而不是一般的细胞毒性。 因此，HIF抑制剂及其药学上可接受的盐可以用作各种癌症如肝癌的治疗剂; 胃癌和乳腺癌。 此外，对HIF-1具有抑制活性的化合物可用于治疗由HIF-1介导的VEGF表达而恶化的糖尿病性视网膜病变和关节炎。

公开(公告)号：US20090306078A1

公开(公告)日：2009-12-10

申请号：US12306319

申请日：2007-07-03

Applicant: Jung Joon Lee ,  Jeong-Hyung Lee ,  Kyeong Lee ,  Young-Soo Hong ,  B.K. Shanthaveerappa ,  Yinlan Jin ,  Jin Hwan Kim ,  Xuejun Jin

Inventor： Jung Joon Lee ,  Jeong-Hyung Lee ,  Kyeong Lee ,  Young-Soo Hong ,  B.K. Shanthaveerappa ,  Yinlan Jin ,  Jin Hwan Kim ,  Xuejun Jin

IPC: A61K31/5377 ,  C07C233/33 ,  A61K31/167 ,  A61K31/41 ,  C07D257/04 ,  C07D295/15 ,  A61K31/423 ,  C07D263/57 ,  A61P19/02

CPC classification number: C07C237/42 ,  C07C235/24 ,  C07C255/60 ,  C07C271/42 ,  C07C307/02 ,  C07C311/46 ,  C07C317/40 ,  C07C2603/74 ,  C07D213/38 ,  C07D213/75 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D235/12 ,  C07D257/04 ,  C07D263/56 ,  C07D307/52 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

Abstract: Disclosed herein are an HIF-1 inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient. The HIF-1 inhibitor shows anticancer activity thanks to the inhibition activity against HIF-1, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer; stomach cancer and breast cancer. Also, the compound having inhibition activity against HIF-1 is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HIF-1-mediated VEGF expression.

Abstract translation: 本文公开了HIF-1抑制剂，其制备方法和包含其作为活性成分的药物组合物。 HIF-1抑制剂由于对HIF-1的抑制活性而显示出抗癌活性，HIF-1是在癌症的生长和转移中起重要作用的转录因子，而不是一般的细胞毒性。 因此，HIF抑制剂及其药学上可接受的盐可以用作各种癌症如肝癌的治疗剂; 胃癌和乳腺癌。 此外，对HIF-1具有抑制活性的化合物可用于治疗由HIF-1介导的VEGF表达而恶化的糖尿病性视网膜病变和关节炎。

公开(公告)号：USD978410S1

公开(公告)日：2023-02-14

申请号：US29843853

申请日：2022-06-24

Applicant: Xuejun Jin

Designer： Xuejun Jin

公开(公告)号：USD1063871S1

公开(公告)日：2025-02-25

申请号：US29975975

申请日：2024-12-03

Applicant: Xuejun Jin

Designer： Xuejun Jin

公开(公告)号：US20080248024A1

公开(公告)日：2008-10-09

申请号：US12039640

申请日：2008-02-28

Applicant: Jung Joon Lee ,  Jeong-Hyung Lee ,  Kyeong Lee ,  Young-Soo Hong ,  Xuejun Jin

Inventor： Jung Joon Lee ,  Jeong-Hyung Lee ,  Kyeong Lee ,  Young-Soo Hong ,  Xuejun Jin

IPC: A61K39/395 ,  A61P35/00 ,  A61K31/70 ,  G01N33/53 ,  A61P9/00 ,  A61P29/00 ,  C12Q1/68 ,  A61K38/02

CPC classification number: C07K16/18 ,  A61K38/1709 ,  C12N15/113 ,  C12N2310/14 ,  G01N33/57415 ,  G01N33/57434 ,  G01N33/57438 ,  G01N33/57446 ,  G01N33/6872 ,  G01N2333/4703 ,  G01N2510/00 ,  G01N2800/00

Abstract: The present invention relates to a use of ZFP91 based on the functions of ZFP91 (Zinc Finger Protein 91) and the interaction of ZFP91 with NF-κB (Nuclear factor kappa B) signal transduction pathway proteins, more precisely a method to inhibit the activation of NF-κB alternative pathway by regulating ZFP91 activation, to inhibit tumor growth by inhibiting the transcription factor HIF-1 (hypoxia inducible factor-1) activation, to inhibit cancer malignancy by inhibiting angiogenesis, or reversely a method to increase the activation of NF-κB alternative pathway or to increase angiogenesis by increasing activation of HIF-1. The method of regulating ZFP91 activation of the present invention can increase or reduce HIF-1α stability by increasing or reducing the activation of NF-κB alternative pathway, so that it can be effectively used for the development of an anticancer agent, a therapeutic agent for arthritis, a therapeutic agent for ulcerative colitis, an anti-inflammatory agent and an angiogenesis inducer.

Abstract translation: 本发明涉及基于ZFP91（锌指蛋白91）的功能和ZFP91与NF-κB（核因子κB）信号转导途径蛋白的相互作用的ZFP91的应用，更准确地说是抑制活化的方法 NF-κB通过调节ZFP91激活，通过抑制转录因子HIF-1（缺氧诱导因子-1）激活抑制肿瘤生长，通过抑制血管生成来抑制癌症恶性，或反向增加NF- kappaB替代途径或通过增加HIF-1的活化来增加血管生成。 调节本发明ZFP91活化的方法可以通过增加或减少NF-κB替代途径的活化来增加或降低HIF-1α的稳定性，从而可以有效地用于开发抗癌剂，治疗剂 关节炎，溃疡性结肠炎的治疗剂，抗炎剂和血管发生诱导剂。