-
1.发明公开CYCLOPROPANE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES 有权CYCLOPROPANAMIDE和模拟具有抗癌特性和抗增殖特性
公开(公告)号：EP2365752A1
公开(公告)日：2011-09-21
申请号：EP09824132.6
申请日：2009-10-29
IPC分类号： A01N43/90 , A01N55/02 , A61K31/555
CPC分类号： C07D413/04 , A61K31/555 , C07D401/04 , C07D401/14 , C07D403/04
摘要： Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-α kinase, PDGFR-β kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.
-
公开(公告)号：EP1907411A2
公开(公告)日：2008-04-09
申请号：EP06786910.7
申请日：2006-07-10
IPC分类号： C07K1/00
CPC分类号： C07K14/4702 , C12N9/1205
摘要： New methods for the rational identification of molecules capable of interacting with specific naturally occurring proteins are provided, in order to yield new pharmacologically important compounds and treatment modalities. Broadly, the method comprises the steps of identifying a switch control ligand forming a part of a particular protein of interest, and also identifying a complemental switch control pocket forming a part of the protein and which interacts with said switch control ligand. The ligand interacts in vivo with Hie pocket to regulate the conformation and biological activity of the protein such that the protein assumes a first conformation and a first biological activity, upon the ligand-pocket interaction, and assumes a second, different conformation and biological activity in the absence of the ligand-pocket interaction. Next, respective samples of said protein in the first and second conformations are provided, and these are screened against one or more candidate molecules by contacting the molecules and the samples. Thereupon, small molecules which bind with the protein at the region of the pocket maybe identified. Novel protein-modulator adducts and methods of altering protein activity are also provided.
-
3.发明授权CYCLOPROPANE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES 有权CYCLOPROPANAMIDE和模拟具有抗癌特性和抗增殖特性
公开(公告)号：EP2365752B1
公开(公告)日：2014-09-24
申请号：EP09824132.6
申请日：2009-10-29
IPC分类号： A61K31/555 , C07D401/04 , C07D401/14 , C07D403/04 , A01N43/90 , A01N55/02 , A61P25/28 , A61P19/00 , A61P35/00 , A61P3/00 , A61P37/08
CPC分类号： C07D413/04 , A61K31/555 , C07D401/04 , C07D401/14 , C07D403/04
-
4.发明公开KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES 审中-公开激酶抑制剂用于治疗增生性疾病和其他增殖性疾病
公开(公告)号：EP2146717A1
公开(公告)日：2010-01-27
申请号：EP08746294.1
申请日：2008-04-18
IPC分类号： A61K31/506 , A61K31/517 , A61K31/426 , A61K31/433 , A61P35/00 , C07D401/14 , C07D403/14
CPC分类号： C07D401/14 , C07D413/14 , C07D417/14
摘要： Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, leukemias, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.
摘要翻译： 本发明化合物可用于治疗哺乳动物癌症，特别是人类癌症，包括但不限于恶性肿瘤，黑素瘤，成胶质细胞瘤，卵巢癌，胰腺癌，前列腺癌，肺癌，乳腺癌，肾癌，宫颈癌，转移瘤 原发性肿瘤位点，骨髓增殖性疾病，白血病，乳头状甲状腺癌，非小细胞肺癌，间皮瘤，嗜酸性粒细胞增多综合征，胃肠道间质瘤，结肠癌，以过度增殖为特征的眼病，导致包括各种视网膜病，类风湿性关节炎，哮喘，慢性 肥大细胞白血病，由c-Abl激酶引起的疾病，其致癌形式，其异常融合蛋白及其多形体，或由c-Kit激酶引起的疾病，其致癌形式，其异常融合蛋白和 多晶型物。
-
5.发明公开
公开(公告)号：EP2146716A1
公开(公告)日：2010-01-27
申请号：EP08746279.2
申请日：2008-04-18
IPC分类号： A61K31/506 , A61K31/517 , A61K31/426 , A61K31/433 , A61P35/00 , C07D401/14 , C07D403/14
CPC分类号： C07D401/14 , C07D413/14 , C07D417/14
摘要： Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, leukemias, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.
-
公开(公告)号：EP2063897A2
公开(公告)日：2009-06-03
申请号：EP07842438.9
申请日：2007-09-13
IPC分类号： A61K31/54 , A61K39/395
CPC分类号： A61K31/4375 , A61K31/519 , C07D471/04
摘要： The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
摘要翻译： 本发明涉及用于治疗各种疾病的新型激酶抑制剂和调节剂化合物。 更具体地说，本发明涉及这样的化合物，激酶/化合物加合物，治疗疾病的方法以及合成该化合物的方法。 优选地，所述化合物可用于调节Raf激酶及其疾病多晶型物的激酶活性。 本发明化合物可用于治疗哺乳动物癌症，特别是人类癌症，包括但不限于恶性黑素瘤，结肠直肠癌，卵巢癌，乳头状甲状腺癌，非小细胞肺癌和间皮瘤。 本发明化合物还可用于治疗类风湿性关节炎和视网膜病，包括糖尿病视网膜神经病和黄斑变性。
-
公开(公告)号：EP1835934A2
公开(公告)日：2007-09-26
申请号：EP05855777.8
申请日：2005-12-23
IPC分类号： A61K39/395
CPC分类号： C07D231/40 , C07D209/46 , C07D231/38 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Novel compounds and methods of using those compounds for the treatment of inflammatory conditions, immunological disorders, hyperproliferative diseases, cancer, and diseases characterized by hyper-vascularization are provided. In a preferred embodiment, modulation of the activation state of kinases, including p38 kinase protein, abl kinase protein, bcr-abl kinase protein, braf kinase protein, VEGFR kinase protein, or PDGFR kinase protein, comprises the step of contacting said kinase protein with the novel compounds.
-
8.发明公开KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES 审中-公开激酶抑制剂用于治疗增生性疾病和其他增殖性疾病
公开(公告)号：EP2148677A1
公开(公告)日：2010-02-03
申请号：EP08746333.7
申请日：2008-04-18
IPC分类号： A61K31/519 , A61K31/444 , C07D239/70 , C07D401/12
CPC分类号： C07D401/14 , C07D413/14 , C07D417/14
摘要： Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers. breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, a disease caused by c-Met kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by a Raf kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.
摘要翻译： 本发明化合物可用于治疗哺乳动物癌症，特别是人类癌症，包括但不限于恶性黑素瘤，实体瘤，成胶质细胞瘤，卵巢癌，胰腺癌，前列腺癌，肺癌。 乳腺癌，肾癌，肝癌，宫颈癌，原发性肿瘤部位的转移，骨髓增殖性疾病，慢性骨髓性白血病，白血病，乳头状甲状腺癌，非小细胞肺癌，间皮瘤，嗜酸性粒细胞增多综合征，胃肠道间质瘤，结肠癌， 以过度增殖为特征的眼病包括各种视网膜病，糖尿病视网膜病，类风湿性关节炎，哮喘，慢性阻塞性肺病，肥大细胞增多症，肥大细胞白血病，由c-Abl激酶引起的疾病，其致癌形式，其异常融合蛋白和多晶型物 由c-Kit激酶引起的疾病，其致癌形式，其异常融合蛋白及其多形体，由c-Met激酶引起的疾病，其致癌形式，其异常融合蛋白及其多晶型，或由 Raf激酶，其致癌形式，其异常融合蛋白， d多晶型物。
-
9.发明公开KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES 审中-公开激酶抑制剂用于治疗增生性疾病和其他增殖性疾病
公开(公告)号：EP2146718A1
公开(公告)日：2010-01-27
申请号：EP08746306.3
申请日：2008-04-18
IPC分类号： A61K31/506 , A61K31/517 , A61K31/426 , A61K31/433 , A61P35/00 , C07D401/14 , C07D403/14
CPC分类号： C07D401/14 , C07D413/14 , C07D417/14
摘要： Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, leukemias, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocyctosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.
摘要翻译： 本发明化合物可用于治疗哺乳动物癌症，特别是人类癌症，包括但不限于恶性肿瘤，黑素瘤，成胶质细胞瘤，卵巢癌，胰腺癌，前列腺癌，肺癌，乳腺癌，肾癌，宫颈癌，转移瘤 原发性肿瘤位点，骨髓增殖性疾病，白血病，乳头状甲状腺癌，非小细胞肺癌，间皮瘤，嗜酸性粒细胞增多综合征，胃肠道间质瘤，结肠癌，以过度增殖为特征的眼病，导致包括各种视网膜病，类风湿性关节炎，哮喘，慢性 阻塞性肺病，肥大细胞增多症，肥大细胞白血病，由c-Abl激酶引起的疾病，其致癌形式，其异常融合蛋白及其多态性，或由c-Kit激酶引起的疾病，致癌形式，其异常融合蛋白和 多晶型物。
-
公开(公告)号：EP1836173A2
公开(公告)日：2007-09-26
申请号：EP05857260.3
申请日：2005-12-23
IPC分类号： C07D231/40 , C07D263/06 , C07D413/10 , C07D285/06 , C07D249/12 , A61K31/4155 , A61K31/4196 , A61K31/433 , A61K31/5377 , A61K31/422
CPC分类号： C07D487/04 , C07D209/46 , C07D231/40 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/14 , C07D413/10 , C07D417/10 , C07D417/12 , C07D417/14 , C12Q1/485
摘要： Novel compounds and methods of using those compounds for the treatment of inflammatory conditions, hyperproliferative diseases, cancer, and diseases characterized by hyper-vascularization are provided. ][n a preferred embodiment, modulation of the activation state of p38 kinase protein, abl kinase protein, bcr-abl kinase protein, braf kinase protein, VEGFR kinase protein, or PDGFR kinase protein comprises the step of contacting said kinase protein with the novel compounds.
摘要翻译： 提供了新型化合物和使用这些化合物治疗炎性病症，过度增殖性疾病，癌症和以高血管形成为特征的疾病的方法。 在优选实施方案中，调节p38激酶蛋白，abl激酶蛋白，bcr-abl激酶蛋白，braf激酶蛋白，VEGFR激酶蛋白或PDGFR激酶蛋白的活化状态包括使所述激酶蛋白与新化合物接触的步骤 。
-
-
-
-
-
-
-
-
-
搜索结果
11 条记录 (耗时 0.026 秒)
