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1. 发明申请

US20090312349A1 ANTI-INFLAMMATORY MEDICAMENTS 审中-公开
标题翻译：抗炎药物
公开(公告)号：US20090312349A1
公开(公告)日：2009-12-17
申请号：US11721026
申请日：2005-12-23
申请人： Daniel L. Flynn , Peter A. Petillo
发明人： Daniel L. Flynn , Peter A. Petillo
IPC分类号： A61K31/519 , C07D401/12 , A61K31/4439 , C07D471/04 , A61P35/00 , C12N9/12
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. In 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，bcr-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。

2. 发明申请

US20080299639A1 Anti-inflammatory medicaments 失效
公开(公告)号：US20080299639A1
公开(公告)日：2008-12-04
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： C12N9/12
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.

3. 发明授权

US07342037B2 Anti-inflammatory medicaments 失效
公开(公告)号：US07342037B2
公开(公告)日：2008-03-11
申请号：US11450840
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： A61K31/4155 , A61K31/4196 , A61K31/433 , A61K31/5377 , A61K31/422 , C07D231/40 , C07D263/06 , C07D413/10 , C07D285/06 , C07D249/12
CPC分类号： A61K31/4184 , A61K31/426 , A61K31/4745 , A61K31/496 , A61K31/517 , A61K31/53 , A61K31/5377 , C07C271/56 , C07C2601/10 , C07D231/38 , C07D231/40 , C07D285/10 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/10 , C07D413/14 , C07D417/10 , 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.

4. 发明授权

US07144911B2 Anti-inflammatory medicaments 失效
公开(公告)号：US07144911B2
公开(公告)日：2006-12-05
申请号：US10746460
申请日：2003-12-24
申请人： Daniel L. Flynn , Peter A. Petillo
发明人： Daniel L. Flynn , Peter A. Petillo
IPC分类号： C07D231/40 , A61K31/4155 , A61K31/4196 , C07D263/06 , C07D413/10 , C07D285/06 , C07D249/12 , A61K31/433 , A61K31/5377 , A61K31/422
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.

5. 发明授权

US08486951B2 Cyclopropane amides and analogs exhibiting anti-cancer and anti-proliferative activities 失效
标题翻译：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
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： 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。

6. 发明授权

US08278331B2 N-acyl ureas exhibiting anti-cancer and anti-proliferative activities 有权
标题翻译：表现出抗癌和抗增殖活性的N-酰基脲
公开(公告)号：US08278331B2
公开(公告)日：2012-10-02
申请号：US12608578
申请日：2009-10-29
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： 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。

7. 发明授权

US08143293B2 Kinase inhibitors useful for the treatment of myleoprolific diseases and other proliferative diseases 失效
标题翻译：激酶抑制剂可用于治疗myleoprolific疾病和其他增殖性疾病
公开(公告)号：US08143293B2
公开(公告)日：2012-03-27
申请号：US12105408
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： A61K31/44 , C07D417/00 , C07D401/00
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, mastocyclosis, 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，乳腺增生症，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，以及其多晶型。

8. 发明申请

US20090105230A1 Anti-inflammatory medicaments 审中-公开
公开(公告)号：US20090105230A1
公开(公告)日：2009-04-23
申请号：US11450842
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： A61K31/4155 , C07D231/38 , C07D403/10 , C07D417/10 , C07D403/12 , C07D471/08 , A61K31/439 , A61K31/5377 , A61K31/506 , A61K31/427 , A61K31/4709 , A61K31/541 , A61K31/422 , C07D413/10 , C12N9/12 , A61P29/00 , A61K31/4196 , A61K31/433
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.

9. 发明申请

US20090099190A1 Kinase inhibitors useful for the treatment of proliferative diseases 失效
标题翻译：可用于治疗增殖性疾病的激酶抑制剂
公开(公告)号：US20090099190A1
公开(公告)日：2009-04-16
申请号：US11854293
申请日：2007-09-12
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： A61K31/4985 , 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。

10. 发明申请

US20080261965A1 KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFIC DISEASES AND OTHER PROLIFERATIVE DISEASES 失效
标题翻译：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：US20080261965A1
公开(公告)日：2008-10-23
申请号：US12105408
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： A61K31/5383 , A61K31/4439 , C07D413/14 , A61P35/00 , C07D498/04 , C07D401/04
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, mastocyclosis, 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，乳腺增生症，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，以及其多晶型。

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