公开(公告)号：US20130079362A1

公开(公告)日：2013-03-28

申请号：US13590955

申请日：2012-08-21

申请人： Daniel L. Flynn ,  Peter A. Petillo ,  Michael D. Kaufman

发明人： Daniel L. Flynn ,  Peter A. Petillo ,  Michael D. Kaufman

IPC分类号： C07D413/04 ,  C07D401/14 ,  C07D403/04 ,  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。

公开(公告)号：US20120322834A1

公开(公告)日：2012-12-20

申请号：US13559170

申请日：2012-07-26

申请人： Daniel L. Flynn ,  Michael D. Kaufman

发明人： Daniel L. Flynn ,  Michael D. Kaufman

IPC分类号： A61K31/44 ,  A61P35/00 ,  C07D211/98

CPC分类号： C07D401/12 ,  A61K31/44 ,  A61K31/505 ,  C07D213/75 ,  C07D239/47

摘要： The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, stereoisomer, or tautomer thereof.

摘要翻译： 所公开的化合物可用于治疗哺乳动物癌症，特别是人类癌症。 公开了化合物，药物组合物和式I的方法：或其药学上可接受的盐，水合物，溶剂合物，对映异构体，立体异构体或其互变异构体。

公开(公告)号：US20120289540A1

公开(公告)日：2012-11-15

申请号：US13445435

申请日：2012-04-12

申请人： Daniel L. Flynn ,  Peter A. Petillo ,  Michael D. Kaufman ,  William C. Patt

发明人： Daniel L. Flynn ,  Peter A. Petillo ,  Michael D. Kaufman ,  William C. Patt

IPC分类号： A61K31/4375 ,  A61P35/04 ,  A61P9/00 ,  A61P19/02 ,  A61P11/00 ,  A61P35/00 ,  A61P29/00

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。

公开(公告)号：US20120225057A1

公开(公告)日：2012-09-06

申请号：US13228288

申请日：2011-09-08

申请人： Daniel L. Flynn ,  Michael D. Kaufman

发明人： Daniel L. Flynn ,  Michael D. Kaufman

IPC分类号： A61K31/4709 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/437 ,  A61K31/498 ,  A61K31/454 ,  A61K31/5025 ,  A61P35/02 ,  A61P35/00 ,  A61P35/04 ,  A61P27/02 ,  A61P37/00 ,  A61P29/00 ,  A61P25/00 ,  A61P19/04 ,  A61P11/06 ,  A61P19/02 ,  A61P19/06 ,  A61P31/00 ,  A61P11/00 ,  A61P9/10 ,  A61P17/06 ,  A61P19/08 ,  A61P37/06 ,  A61P1/00 ,  A61P1/04 ,  A61K39/395 ,  A61K38/16 ,  C12N9/99 ,  A61K31/4725

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： Compounds of the present invention, alone and in combination with other active agents, find utility in the treatment of hyperproliferative diseases, mammalian cancers and especially human cancers including but not limited to for example malignant melanomas, myeloproliferative diseases, chronic myelogenous leukemia, acute lymphocytic leukemia, a disease caused by c-ABL kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.

摘要翻译： 本发明的单独和与其它活性剂组合的化合物可用于治疗过度增殖性疾病，哺乳动物癌症，特别是人类癌症，包括但不限于恶性黑素瘤，骨髓增生性疾病，慢性骨髓性白血病，急性淋巴细胞性白血病 ，由c-ABL激酶，其致癌形式，异常融合蛋白和其多态性引起的疾病。

公开(公告)号：US07790756B2

公开(公告)日：2010-09-07

申请号：US11870388

申请日：2007-10-10

申请人： Daniel L. Flynn ,  Peter A Petillo ,  Michael D Kaufman

发明人： Daniel L. Flynn ,  Peter A Petillo ,  Michael D Kaufman

IPC分类号： A61K31/44

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。

公开(公告)号：US07666895B2

公开(公告)日：2010-02-23

申请号：US11450850

申请日：2006-06-09

申请人： Daniel L. Flynn ,  Peter A. Petillo

发明人： Daniel L. Flynn ,  Peter A. Petillo

IPC分类号： A61K31/415 ,  A61K31/41 ,  C12N9/96

CPC分类号： C07D239/42 ,  C07D295/10 ,  C07D401/04 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

摘要： Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.

公开(公告)号：US20080269254A1

公开(公告)日：2008-10-30

申请号：US12105350

申请日：2008-04-18

申请人： Daniel L. Flynn ,  Peter A. Petillo ,  Michael D. Kaufman

发明人： Daniel L. Flynn ,  Peter A. Petillo ,  Michael D. Kaufman

IPC分类号： A61K31/506 ,  C07D403/14 ,  A61P35/04 ,  A61P3/00 ,  A61P11/00 ,  A61P27/00 ,  C07D413/14

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.

公开(公告)号：US20080113967A1

公开(公告)日：2008-05-15

申请号：US11963740

申请日：2007-12-21

申请人： Daniel Flynn ,  Peter Petillo

发明人： Daniel Flynn ,  Peter Petillo

IPC分类号： A61K31/4155 ,  C07D231/38 ,  A61K31/415 ,  A61K31/506 ,  C07D401/14 ,  C07D401/12 ,  A61K31/4439 ,  A61K31/519 ,  C07D471/04 ,  A61K31/4709 ,  C07D401/02 ,  A61K31/4725 ,  C07D403/02 ,  A61K31/55 ,  A61K31/496 ,  A61K31/5377 ,  C07D413/02 ,  C07D409/02

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, hyperproliferative diseases, cancer, and diseases characterized by hyper-vascularization are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein, abl kinase protein, ber-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，癌症和以血管新生血管瘤为特征的疾病的方法。 在优选的实施方案中，调节p38激酶蛋白，abl激酶蛋白，ber-abl激酶蛋白，braf激酶蛋白，VEGFR激酶蛋白或PDGFR激酶蛋白的激活状态包括使所述激酶蛋白与新化合物接触的步骤。