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。

公开(公告)号：US08940936B2

公开(公告)日：2015-01-27

申请号：US13880642

申请日：2011-10-17

申请人： Kyeong Lee ,  Mi Sun Won ,  Hwan Mook Kim ,  Song Kyu Park ,  Kiho Lee ,  Ki Hoon Lee ,  Chang Woo Lee ,  Jung Joon Lee ,  Kyung Sook Chung ,  Bo Kyung Kim ,  Yinglan Jin ,  Seung-hee Lee

发明人： Kyeong Lee ,  Mi Sun Won ,  Hwan Mook Kim ,  Song Kyu Park ,  Kiho Lee ,  Ki Hoon Lee ,  Chang Woo Lee ,  Jung Joon Lee ,  Kyung Sook Chung ,  Bo Kyung Kim ,  Yinglan Jin ,  Seung-hee Lee

IPC分类号： C07C233/07 ,  A61K31/167 ,  C07C235/28 ,  C07C311/16 ,  C07D295/088

CPC分类号： A61K31/5375 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  A61K31/167 ,  A61K31/196 ,  A61K31/24 ,  A61K31/34 ,  A61K31/40 ,  A61K31/417 ,  A61K31/4409 ,  C07C233/07 ,  C07C235/28 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C2603/74 ,  C07D295/088

摘要： The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity not by non-selective cytotoxicity but by inhibiting the activity of HIF-1, the transcription factor playing an important role in cancer cell growth and metastasis. Accordingly, the compound or the pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumors such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases.

摘要翻译： 本发明涉及抑制HF-1活性的化合物，其制备方法以及含有该化合物作为活性成分的药物组合物。 本发明的化合物通过非选择性细胞毒性表现出抗癌活性，但通过抑制HIF-1的活性，该转录因子在癌细胞生长和转移中起重要作用。 因此，根据本发明的化合物或其药学上可接受的盐抑制HIF-1活性，因此可以用作结肠癌，肝癌，胃癌和乳腺癌等实体瘤的治疗剂。 此外，根据本发明的化合物或其药学上可接受的盐可以用作用于糖尿病性视网膜病变或关节炎的治疗剂的活性成分，当HIF-1的缺氧诱导的VEGF表达增加时，可能变差。

公开(公告)号：US20130237542A1

公开(公告)日：2013-09-12

申请号：US13880642

申请日：2011-10-17

申请人： Kyeong Lee ,  Mi Sun Won ,  Hwan Mook Kim ,  Song Kyu Park ,  Kiho Lee ,  Ki Hoon Lee ,  Chang Woo Lee ,  Jung Joon Lee ,  Kyung Sook Chung ,  Bo Kyung Kim ,  Yinglan Jin ,  Seung-hee Lee

发明人： Kyeong Lee ,  Mi Sun Won ,  Hwan Mook Kim ,  Song Kyu Park ,  Kiho Lee ,  Ki Hoon Lee ,  Chang Woo Lee ,  Jung Joon Lee ,  Kyung Sook Chung ,  Bo Kyung Kim ,  Yinglan Jin ,  Seung-hee Lee

IPC分类号： C07C235/28 ,  C07D295/088 ,  C07C311/16

CPC分类号： A61K31/5375 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  A61K31/167 ,  A61K31/196 ,  A61K31/24 ,  A61K31/34 ,  A61K31/40 ,  A61K31/417 ,  A61K31/4409 ,  C07C233/07 ,  C07C235/28 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C2603/74 ,  C07D295/088

摘要： The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity not by non-selective cytotoxicity but by inhibiting the activity of HIF-1, the transcription factor playing an important role in cancer cell growth and metastasis. Accordingly, the compound or the pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumors such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases.

摘要翻译： 本发明涉及抑制HF-1活性的化合物，其制备方法以及含有该化合物作为活性成分的药物组合物。 本发明的化合物通过非选择性细胞毒性表现出抗癌活性，但通过抑制HIF-1的活性，该转录因子在癌细胞生长和转移中起重要作用。 因此，根据本发明的化合物或其药学上可接受的盐抑制HIF-1活性，因此可以用作结肠癌，肝癌，胃癌和乳腺癌等实体瘤的治疗剂。 此外，根据本发明的化合物或其药学上可接受的盐可以用作用于糖尿病性视网膜病变或关节炎的治疗剂的活性成分，当HIF-1的缺氧诱导的VEGF表达增加时，可能变差。

公开(公告)号：US07846963B2

公开(公告)日：2010-12-07

申请号：US10557085

申请日：2004-05-17

申请人： Yung Hee Kho ,  Gyoon Hee Han ,  Ho Jae Lee ,  Bum Woo Park ,  Hyo Kon Chun ,  Hwan Mook Kim ,  Song Kyu Park ,  Sang Bae Han ,  Dong Kyu Ryu ,  Tae Gyu Chun ,  Jin Ha Lee ,  Chang Woo Lee ,  Ki Hoon Lee ,  Hee Yoon Lee

发明人： Yung Hee Kho ,  Gyoon Hee Han ,  Ho Jae Lee ,  Bum Woo Park ,  Hyo Kon Chun ,  Hwan Mook Kim ,  Song Kyu Park ,  Sang Bae Han ,  Dong Kyu Ryu ,  Tae Gyu Chun ,  Jin Ha Lee ,  Chang Woo Lee ,  Ki Hoon Lee ,  Hee Yoon Lee

IPC分类号： A01N43/36 ,  A61K31/40 ,  C07D207/00 ,  C07D295/00 ,  C09B1/00

CPC分类号： C07D207/26 ,  C07D207/38 ,  C07D211/86 ,  C07D409/06

摘要： The present invention is related to new 2-oxo-cyclic compound the process for preparing them and a pharmaceutical composition comprising the same. The present invention provides a pharmaceutical composition for preventing and treating the inflammatory disease comprising the pain or inflammation caused by rheumatic disease, for example, rheumatoid arthritis, spondyloarthopathies, gout, osteoarthritis, systemic lupus erythematosus and juvenile arthritis, and inflammatory syndrome for example, from myositis, gingivitis, synovitis, ankylosing spondylitis, burstitis, burns and scar, inflammatory Crohn's disease, Types I diabetes. therefore, it can be used as the therapeutics for treating and preventing inflammatory diseases.

摘要翻译： 本发明涉及新的2-氧代环状化合物及其制备方法和包含其的药物组合物。 本发明提供了用于预防和治疗炎性疾病的药物组合物，其包括由风湿性疾病引起的疼痛或炎症，例如类风湿性关节炎，脊椎动物病变，痛风，骨关节炎，系统性红斑狼疮和幼年关节炎以及炎性综合征，例如， 肌炎，牙龈炎，滑膜炎，强直性脊柱炎，爆发性炎症，烧伤和瘢痕，炎性克罗恩病，I型糖尿病。 因此，它可以用作治疗和预防炎性疾病的治疗剂。

公开(公告)号：US07723376B2

公开(公告)日：2010-05-25

申请号：US10564653

申请日：2004-07-15

申请人： Hwan Mook Kim ,  Gyoon Hee Han ,  Song Kyu Park ,  Chang Woo Lee ,  Sang Bae Han ,  Ki Hoon Lee ,  Yung Hee Kho ,  Jin Hyuk Yang ,  Bum Woo Park ,  Hyang Woo Lee ,  Jeung Whan Han ,  Dong Kyu Ryu ,  Jin Ha Lee ,  Tae Gyu Chun ,  Yong Kee Kim ,  Hee Yoon Lee ,  Bong Yong Lee ,  Jeom Yong Kim ,  Ji Duck Kim ,  Kyunga Yu ,  Sun Young Kim

发明人： Hwan Mook Kim ,  Gyoon Hee Han ,  Song Kyu Park ,  Chang Woo Lee ,  Sang Bae Han ,  Ki Hoon Lee ,  Yung Hee Kho ,  Jin Hyuk Yang ,  Bum Woo Park ,  Hyang Woo Lee ,  Jeung Whan Han ,  Dong Kyu Ryu ,  Jin Ha Lee ,  Tae Gyu Chun ,  Yong Kee Kim ,  Hee Yoon Lee ,  Bong Yong Lee ,  Jeom Yong Kim ,  Ji Duck Kim ,  Kyunga Yu ,  Sun Young Kim

IPC分类号： A01N43/36

CPC分类号： A61K31/454 ,  A61K31/4015 ,  A61K31/4545 ,  C07D207/38 ,  C07D211/86 ,  C07D223/10 ,  C07D417/06

摘要： The present invention is related to novel use of 2-oxo-heterocyclic compounds having anticancer activity and the process for preparing them and a pharmaceutical composition comprising the same. The present invention provides a pharmaceutical composition for preventing and treating the cancer disease comprising lung cancer, bone cancer, pancreatic cancer, skin cancer, cancer of the head and neck, cutaneous or intraocular melanoma, uterine cancer, ovarian cancer, rectal cancer or cancer of the anal region, stomach cancer, colon cancer, breast cancer, gynecologic tumors, Hodgkin's disease, cancer of the esophagus, cancer of the small intestine, cancer of the endocrine system, sarcomas of soft tissues, cancer of the urethra, cancer of the penis, prostate cancer, chronic or acute leukemia, solid tumors of childhood, lymphocytic lymphonas, cancer of the bladder, cancer of the kidney or ureter, or neoplasms of the central nervous system, therefore, it can be used as the therapeutics for treating and preventing cancer diseases.

摘要翻译： 本发明涉及具有抗癌活性的2-氧代杂环化合物及其制备方法的新用途以及包含其的药物组合物。 本发明提供了用于预防和治疗包括肺癌，骨癌，胰腺癌，皮肤癌，头颈癌，皮肤或眼内黑素瘤，子宫癌，卵巢癌，直肠癌或癌症的癌症疾病的药物组合物 肛门区域，胃癌，结肠癌，乳腺癌，妇科肿瘤，霍奇金病，食道癌，小肠癌，内分泌系统癌，软组织肉瘤，尿道癌，阴茎癌 ，前列腺癌，慢性或急性白血病，儿童实体瘤，淋巴细胞淋巴管，膀胱癌，肾或输尿管癌，或中枢神经系统肿瘤，因此可用作治疗和预防的治疗剂 癌症疾病

公开(公告)号：US20090042872A1

公开(公告)日：2009-02-12

申请号：US12087474

申请日：2006-12-08

申请人： Seong Eon Ryu ,  Seung Jun Kim ,  Dae Gwin Jeong ,  Sang Hyeup Lee ,  Suk Kyeong Jung ,  Hwan Mook Kim ,  Song Kyu Park ,  Ki Ho Lee ,  Chang Woo Lee ,  Joong-Kwon Choi ,  Jin Hee Ahn

发明人： Seong Eon Ryu ,  Seung Jun Kim ,  Dae Gwin Jeong ,  Sang Hyeup Lee ,  Suk Kyeong Jung ,  Hwan Mook Kim ,  Song Kyu Park ,  Ki Ho Lee ,  Chang Woo Lee ,  Joong-Kwon Choi ,  Jin Hee Ahn

IPC分类号： A61K31/426 ,  C07D277/04 ,  C07D413/12 ,  A61K31/538 ,  A61P3/10 ,  A61P35/00 ,  A61P3/04 ,  A61K31/5377 ,  C07D265/34

CPC分类号： C07D277/20 ,  C07D417/12

摘要： Disclosed herein are rhodanine derivatives, a method for the preparation thereof, and a pharmaceutical composition containing the same. The rhodanine derivatives have inhibitory activity against protein phosphatases (PPase) such as PTP1B, Prl-3, LAR, CD45, Cdc25A, Cdc25B, Cdc25C, Yop, PP1 and VHR, and can be applied for the prevention and treatment of PPase-caused diseases, including autoimmune diseases, diabetes, impaired glucose intolerance, insulin resistance, obesity, cancers, etc. when the inhibitory activity thereof is modulated.

摘要翻译： 本文公开了绕丹宁衍生物，其制备方法和含有它们的药物组合物。 罗丹明衍生物对PTP1B，Prl-3，LAR，CD45，Cdc25A，Cdc25B，Cdc25C，Yop，PP1和VHR等蛋白磷酸酶（PPase）具有抑制活性，可用于预防和治疗PPase引起的疾病 包括自身免疫性疾病，糖尿病，葡萄糖耐受不良，胰岛素抵抗，肥胖，癌症等。

公开(公告)号：US08148541B2

公开(公告)日：2012-04-03

申请号：US12087474

申请日：2006-12-08

申请人： Seong Eon Ryu ,  Seung Jun Kim ,  Dae Gwin Jeong ,  Sang Hyeup Lee ,  Suk Kyeong Jung ,  Hwan Mook Kim ,  Song Kyu Park ,  Ki Ho Lee ,  Chang Woo Lee ,  Joong-Kwon Choi ,  Jin Hee Ahn

发明人： Seong Eon Ryu ,  Seung Jun Kim ,  Dae Gwin Jeong ,  Sang Hyeup Lee ,  Suk Kyeong Jung ,  Hwan Mook Kim ,  Song Kyu Park ,  Ki Ho Lee ,  Chang Woo Lee ,  Joong-Kwon Choi ,  Jin Hee Ahn

IPC分类号： C07D277/04 ,  C07D417/02 ,  C07D413/02 ,  A61K31/535 ,  A61K31/497 ,  A61K31/425

CPC分类号： C07D277/20 ,  C07D417/12

摘要： Disclosed herein are rhodanine derivatives, a method for the preparation thereof, and a pharmaceutical composition containing the same. The rhodanine derivatives have inhibitory activity against protein phosphatases (PPase) such as PTP1B, Prl-3, LAR, CD45, Cdc25A, Cdc25B, Cdc25C, Yop, PP1 and VHR, and can be applied for the prevention and treatment of PPase-caused diseases, including autoimmune diseases, diabetes, impaired glucose intolerance, insulin resistance, obesity, cancers, etc. when the inhibitory activity thereof is modulated.

摘要翻译： 本文公开了绕丹宁衍生物，其制备方法和含有它们的药物组合物。 罗丹明衍生物对PTP1B，Prl-3，LAR，CD45，Cdc25A，Cdc25B，Cdc25C，Yop，PP1和VHR等蛋白磷酸酶（PPase）具有抑制活性，可用于预防和治疗PPase引起的疾病 包括自身免疫性疾病，糖尿病，葡萄糖耐受不良，胰岛素抵抗，肥胖，癌症等。