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公开(公告)号：US20090099190A1
公开(公告)日：2009-04-16
申请号：US11854293
申请日：2007-09-12
IPC分类号： A61K31/4985 , C07D487/04 , A61K31/519 , A61P35/00 , A61P19/02 , A61P9/00 , A61P37/00 , A61P11/00 , A61P29/00 , C12N9/99 , C07D239/70
CPC分类号： C07D471/04 , C07D487/04
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： 本发明涉及可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，本发明涉及这样的化合物，激酶/化合物加合物，治疗疾病的方法和化合物的合成方法。 优选地，所述化合物可用于调节Raf激酶及其疾病多形体的激酶活性。 本发明的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，甲状腺乳头状癌，非小细胞肺癌和间皮瘤。 本发明的化合物还可用于治疗类风湿性关节炎和视网膜病变，包括糖尿病性视网膜神经病变和黄斑变性。
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公开(公告)号：US07897762B2
公开(公告)日：2011-03-01
申请号：US11854293
申请日：2007-09-12
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
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： 本发明涉及可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，本发明涉及这样的化合物，激酶/化合物加合物，治疗疾病的方法和化合物的合成方法。 优选地，所述化合物可用于调节Raf激酶及其疾病多形体的激酶活性。 本发明的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，甲状腺乳头状癌，非小细胞肺癌和间皮瘤。 本发明的化合物还可用于治疗类风湿性关节炎和视网膜病变，包括糖尿病性视网膜神经病变和黄斑变性。
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3.发明授权Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases 失效二氢吡啶并嘧啶基，二氢萘并吡啶基和可用作激酶抑制剂用于治疗增殖性疾病的相关化合物公开(公告)号：US08188113B2
公开(公告)日：2012-05-29
申请号：US11854354
申请日：2007-09-12
IPC分类号： C07D471/04 , A61K31/4375 , A61P35/00 , A61P29/00 , A61P19/00 , A61P11/00 , A61P9/00 , A61P37/00
CPC分类号： A61K31/4375 , A61K31/519 , C07D471/04
摘要： The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator 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. Preferably, 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： 本发明涉及新的二氢吡啶并嘧啶基，二氢萘并吡啶基和相关化合物，它们是可用于治疗各种疾病的激酶抑制剂和调节剂。 更具体地，本发明涉及这些化合物，激酶/化合物加合物，治疗疾病的方法和化合物的合成方法。 优选地，所述化合物可用于调节Raf激酶及其疾病多形体的激酶活性。 本发明的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，甲状腺乳头状癌，非小细胞肺癌和间皮瘤。 本发明的化合物还可用于治疗类风湿性关节炎和视网膜病变，包括糖尿病性视网膜神经病变和黄斑变性。
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公开(公告)号：US20120289540A1
公开(公告)日：2012-11-15
申请号：US13445435
申请日：2012-04-12
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： 本发明涉及可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，本发明涉及这样的化合物，激酶/化合物加合物，治疗疾病的方法和化合物的合成方法。 优选地，该化合物可用于调节Raf激酶的激酶活性及其疾病多形体。 本发明的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，甲状腺乳头状癌，非小细胞肺癌和间皮瘤。 本发明的化合物还可用于治疗类风湿性关节炎和视网膜病变，包括糖尿病性视网膜神经病变和黄斑变性。
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公开(公告)号：US08461179B1
公开(公告)日：2013-06-11
申请号：US13491394
申请日：2012-06-07
CPC分类号： A61K31/5377 , A01N43/42 , A61K31/4375 , A61K31/496 , C07D471/04
摘要： The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound.
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6.发明申请CYCLOPROPANE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES 有权环丙沙星和类似物展示抗癌和抗增生活性公开(公告)号：US20100120806A1
公开(公告)日：2010-05-13
申请号：US12608578
申请日：2009-10-29
IPC分类号： A61K31/4439 , C07D401/04 , C07D413/04 , C07D401/14 , C07D403/04 , A61K31/444 , A61K31/506 , A61P35/00 , A61P35/02 , A61P25/00 , A61P3/00
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.
摘要翻译： 本发明的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，原发性肿瘤部位转移，骨髓增生性疾病，慢性骨髓性白血病，白血病，甲状腺乳头状癌，非小细胞肺癌，间皮瘤，嗜酸性粒细胞综合征，胃肠道间质瘤，结肠癌，以过度增生为特征的眼部疾病 包括各种视网膜病变，糖尿病性视网膜病变，类风湿性关节炎，哮喘，慢性阻塞性肺疾病，肥大细胞增多症，肥大细胞白血病和由PDGFR-α激酶引起的疾病，PDGFR-＆bgr; 激酶，c-KIT激酶，cFMS激酶，c-MET激酶和致癌形式，异常融合蛋白和任何前述激酶的多态性。
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7.发明申请KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFIC DISEASES AND OTHER PROLIFERATIVE DISEASES 审中-公开用于治疗单纯性疾病和其他增殖性疾病的激酶抑制剂公开(公告)号：US20080261961A1
公开(公告)日：2008-10-23
申请号：US12105376
申请日：2008-04-18
IPC分类号： A61K31/4439 , C07D401/12 , C07D413/12 , C07D417/12 , A61K31/541 , A61P27/02 , A61P11/00 , A61P19/02 , A61P35/00 , A61K31/5377 , A61K31/496 , A61K31/4545
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： 本发明的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，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 原发性肿瘤部位，骨髓增生性疾病，白血病，甲状腺乳头状癌，非小细胞肺癌，间皮瘤，嗜酸性粒细胞综合征，胃肠道间质瘤，结肠癌，以过度增生为特征的眼部疾病导致失明，包括各种视网膜病变，类风湿关节炎，哮喘，慢性 阻塞性肺疾病，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，异常融合蛋白及其多形体，或由c-Kit激酶，其致癌形式，异常融合蛋白引起的疾病和 其多晶型。
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8.发明申请Kinase Inhibitors Useful for the Treatment of Myleoproliferative Diseases and other Proliferative Diseases 有权激酶抑制剂可用于治疗Myleopreiferative疾病和其他增生性疾病公开(公告)号：US20110136760A1
公开(公告)日：2011-06-09
申请号：US12829561
申请日：2010-07-02
IPC分类号： A61K31/695 , A61K31/44 , A61K31/4412 , A61K31/505 , A61K31/4439 , A61K31/4725 , A61K31/4155 , A61K31/4709 , A61K31/498 , A61P35/00 , A61P29/00 , A61P19/02 , A61P11/00 , A61P9/00 , C12N9/99
CPC分类号： C07D401/14 , C07D401/12 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present invention is concerned with novel compounds useful in the treatment of hyperproliferative diseases and mammalian cancers, especially human cancers. The invention also pertains to methods of modulating kinase activities, pharmaceutical compositions, and methods of treating individuals, incorporating or using the compounds. The preferred compounds are active small molecules set forth in formulae Ia-Iww.
摘要翻译： 本发明涉及可用于治疗过度增殖性疾病和哺乳动物癌症，特别是人类癌症的新化合物。 本发明还涉及调节激酶活性的方法，药物组合物和治疗个体的方法，掺入或使用该化合物。 优选的化合物是式Ia-Iww中所示的活性小分子。
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9.发明申请KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFIC DISEASES AND OTHER PROLIFERATIVE DISEASES 审中-公开用于治疗单纯性疾病和其他增殖性疾病的激酶抑制剂公开(公告)号：US20080269267A1
公开(公告)日：2008-10-30
申请号：US12105302
申请日：2008-04-18
IPC分类号： C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04 , A61K31/44 , A61K31/4439 , A61K31/506 , A61P35/00 , A61P3/00 , A61P11/00 , A61P19/02
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： 本发明的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，原发性肿瘤部位转移，骨髓增生性疾病，慢性髓细胞性白血病，白血病，甲状腺乳头状癌，非小细胞肺癌，间皮瘤，嗜酸性粒细胞综合征，胃肠道间质瘤，结肠癌，以过度增生为特征的眼部疾病导致失明 包括各种视网膜病变，糖尿病性视网膜病变，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，异常融合蛋白及其多态性， Kit激酶，其致癌形式，异常f 其诱发蛋白及其多态性，由c-Met激酶引起的疾病，其致癌形式，异常融合蛋白及其多形体，或由Raf激酶，其致癌形式，异常融合蛋白及其多形体引起的疾病。
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10.发明授权Cyclopropane amides and analogs exhibiting anti-cancer and anti-proliferative activities 失效表现出抗癌和抗增殖活性的环丙酰胺和类似物公开(公告)号：US08486951B2
公开(公告)日：2013-07-16
申请号：US13590955
申请日：2012-08-21
IPC分类号： A01N43/54 , C07D239/42 , C07D401/04
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, hypereosinophilia 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.
摘要翻译： 本发明的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，原发性肿瘤部位转移，骨髓增生性疾病，慢性骨髓性白血病，白血病，甲状腺乳头状癌，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，以过度增生为特征的眼部疾病 包括各种视网膜病变，糖尿病性视网膜病变，类风湿性关节炎，哮喘，慢性阻塞性肺病，肥大细胞增多症，肥大细胞白血病和由PDGFR-α激酶，PDGFR-β激酶，c-KIT激酶，cFMS激酶，c-MET引起的疾病 激酶和致癌形式，异常融合蛋白和任何前体的多态性 激酶。
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