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1. 发明申请

WO2015069266A1 METHODS FOR INHIBITING TIE2 KINASE USEFUL IN THE TREATMENT OF CANCER 审中-公开
标题翻译：抑制TIE2激酶治疗癌症的方法
公开(公告)号：WO2015069266A1
公开(公告)日：2015-05-14
申请号：PCT/US2013/069005
申请日：2013-11-07
申请人： FLYNN, Daniel L. , KAUFMAN, Michael D. , SMITH, Bryan , RUDOLTZ, Marc S.
发明人： FLYNN, Daniel L. , KAUFMAN, Michael D. , SMITH, Bryan , RUDOLTZ, Marc S.
IPC分类号： A01N43/56 , A01N47/28 , C07D231/00
CPC分类号： A61K31/357 , A61K31/337 , A61K31/4709 , A61K45/06 , A61K2300/00
摘要： The present invention relates to methods of inhibiting TIE2 kinase useful in the treatment of tumor growth, invasiveness, intravasation, dissemination, metastasis, and immunosuppression. Specifically, the invention relates to methods of using 1-(3-tert-butyl-1-(quinolin-6-yl)-1Hpyrazol- 5-yl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea and salts thereof of Formula I.
摘要翻译：本发明涉及抑制TIE2激酶治疗肿瘤生长，侵袭，侵袭，传播，转移和免疫抑制的方法。具体地说，本发明涉及使用1-（3-叔丁基-1-（喹啉-6-基）-1H-吡唑-5-基）-3-（2-氟-4-（2-（甲基氨基甲酰基）吡啶-4-基氧基）苯基）脲及其盐。

2. 发明申请

WO2013036232A3 METHODS AND COMPOSITIONS FOR THE TREATMENT OF MYELOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES 审中-公开
标题翻译：治疗失语性疾病和其他增殖性疾病的方法和组合
公开(公告)号：WO2013036232A3
公开(公告)日：2014-03-27
申请号：PCT/US2011050856
申请日：2011-09-08
申请人： DECIPHERA PHARMACEUTICALS LLC , FLYNN DANIEL L , PETILLO PETER A , KAUFMAN MICHAEL D
发明人： FLYNN DANIEL L , PETILLO PETER A , KAUFMAN MICHAEL D
IPC分类号： A01N47/28 , A61K31/17
CPC分类号： A61K45/06 , A61K31/4709
摘要： Compounds of the present invention find utility in the treatment of hyperproliferative diseases, 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 secondary sites, myeloproliferative diseases, chronic myelogenous leukemia, acute lymphocytic leukemia, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, thyroid cancer, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, i.e. diabetic retinopathy and age-related macular degeneration, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, human inflammation, rheumatoid spondylitis, ostero-arthritis, asthma, gouty arthritis, sepsis, septic shock, endotoxic shock, Gram-negative sepsis, toxic shock syndrome, adult respiratory distress syndrome, stroke, reperfusion injury, neural trauma, neural ischemia, psoriasis, restenosis, chronic obstructive pulmonary disease, bone resorptive diseases, graft-versus-host reaction, Crohn's disease, ulcerative colitis, inflammatory bowel disease, pyresis, and combinations thereof, a disease caused by c-ABL kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, c-KIT kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, VEGFR kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, PDGFR kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, FLT-3 kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, TIE-2 kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, TRK kinases, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, c-MET kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by a HER 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，成胶质细胞瘤，卵巢癌，胰腺癌，前列腺癌，肺癌，乳腺癌，肾癌，宫颈癌原发性肿瘤部位继发部位的转移，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，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，甲状腺癌，眼病，过度增生导致失明，包括各种视网膜病变，即糖尿病性视网膜病变和年龄相关性黄斑变性，类风湿性关节炎，哮喘，慢性阻塞性肺病，人类炎症，类风湿性脊椎炎，ostero-关节炎，哮喘，痛风性关节炎，败血症，败血性休克，内毒素性休克，格拉 m阴性败血症，中毒性休克综合征，成人呼吸窘迫综合征，中风，再灌注损伤，神经创伤，神经缺血，牛皮癣，再狭窄，慢性阻塞性肺病，骨吸收性疾病，移植物抗宿主反应，克罗恩病，溃疡性结肠炎，炎症性肠病，发炎及其组合，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，c-KIT激酶，其致癌形式，异常融合蛋白及其多态性，VEGFR 激酶，其致癌形式，其异源融合蛋白及其多态性，PDGFR激酶，其致癌形式，异常融合蛋白及其多态性，FLT-3激酶，其致癌形式，异常融合蛋白及其多态性，TIE-2激酶，其致癌形式，异常融合蛋白和其多态性，TRK激酶，其致癌形式，异常fus 离子蛋白及其多晶型物，c-MET激酶，其致癌形式，异常融合蛋白及其多态性，或由HER激酶，其致癌形式，异常融合蛋白及其多态性引起的疾病。

3. 发明申请

WO2013184119A1 DIHYDRONAPHTHYRIDINES AND RELATED COMPOUNDS USEFUL AS KINASE INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
标题翻译：用作治疗增殖性疾病的激酶抑制剂的二氢萘啶和相关化合物
公开(公告)号：WO2013184119A1
公开(公告)日：2013-12-12
申请号：PCT/US2012/041378
申请日：2012-06-07
申请人： FLYNN, Daniel L. , KAUFMAN, Michael D.
发明人： FLYNN, Daniel L. , KAUFMAN, Michael D.
IPC分类号： A61K31/4375
CPC分类号： C07D471/04 , A61K31/4375
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. The present invention discloses the unexpected utility of compounds that inhibit cKIT kinase across a broad range of c-KIT mutations, including complex occurrences of primary mutations (KIT exon 9 or 11) and secondary KIT mutations (exons 13, 14, 17 and 18) that may arise in individual, refractory GIST patients. Also unexpected is the utility of compounds of the present invention to inhibit the problematic exon 17 D816V c-KIT mutation, for which there is currently no effective therapy.
摘要翻译：本发明涉及二氢萘并及其相关化合物; 包含有效量的二氢萘并或相关化合物的组合物; 以及治疗或预防增殖性疾病的方法，包括施用有效量的二氢萘并吡啶或相关化合物。本发明公开了在广泛的c-KIT突变中抑制cKIT激酶的化合物的意想不到的效用，包括复发性原发突变（KIT外显子9或11）和次级KIT突变（外显子13,14,17和18）可能在个体耐火GIST患者中出现。也是意想不到的是本发明化合物用于抑制问题的外显子17D816V c-KIT突变的用途，目前没有有效的治疗。

4. 发明申请

WO2011056260A1 IMPROVED VIBRATING DENTAL DEVICES 审中-公开
标题翻译：改进的振动牙科装置
公开(公告)号：WO2011056260A1
公开(公告)日：2011-05-12
申请号：PCT/US2010/034303
申请日：2010-05-11
申请人： SPAULDING, Glen , LING, Jeremy , KAUFMAN, Michael E. , LOWE, Michael K. , ORTHOACCEL TECHNOLOGIES, INC.
发明人： SPAULDING, Glen , LING, Jeremy , KAUFMAN, Michael E. , LOWE, Michael K.
IPC分类号： A61C7/06
CPC分类号： A61C7/008 , A61C1/0015 , A61C7/00 , A61C7/002 , A61C7/08 , A61C7/12 , A61C2204/005
摘要： A variety of improvements to the vibrating devices for dental remodeling are provided, including improved bite plate designs that accomodate common patient bite structure, a connector for a bite plate, a sizing tray for same, as well as better motors providing improved performance characteristics for an extraoral vibrator, and a completely intraoral vibrating dental plate with very thin cross section.
摘要翻译：提供了用于牙齿重塑的振动装置的各种改进，包括改进的咬合板设计以适应常见的患者咬合结构，用于咬合板的连接器，用于其的定型托盘，以及更好的马达，其为口外振动器和具有非常薄横截面的完全口腔内振动的牙板。

5. 发明申请

WO2008033999A8 KINASE INHIBITORS USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
标题翻译：用于治疗增殖性疾病的激素抑制剂
公开(公告)号：WO2008033999A8
公开(公告)日：2009-11-05
申请号：PCT/US2007078394
申请日：2007-09-13
申请人： DECIPHERA PHARMACEUTICALS LLC , FLYNN DANIEL L , PETILLO PETER A , KAUFMAN MICHAEL D , PATT WILLIAM C
发明人： FLYNN DANIEL L , PETILLO PETER A , KAUFMAN MICHAEL D , PATT WILLIAM C
IPC分类号： A61K31/54
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. 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。

6. 发明申请

WO2008046003A2 KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES 审中-公开
标题翻译：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：WO2008046003A2
公开(公告)日：2008-04-17
申请号：PCT/US2007081098
申请日：2007-10-11
申请人： DECIPHERA PHARMACEUTICALS LLC , PETILLO PETER A , KAUFMAN MICHAEL D , FLYNN DANIEL L
发明人： PETILLO PETER A , KAUFMAN MICHAEL D , FLYNN DANIEL L
IPC分类号： A61K31/44 , A61K31/47 , A61K31/505 , A61P35/00 , C07D213/00 , C07D215/00 , C07D239/02
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型化合物。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，并入或使用所述化合物。优选的化合物是式Ia-Iww中列出的活性小分子。

7. 发明申请

WO2008033999A2 KINASE INHIBITORS USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
标题翻译：激酶抑制剂用于治疗增殖性疾病
公开(公告)号：WO2008033999A2
公开(公告)日：2008-03-20
申请号：PCT/US2007/078394
申请日：2007-09-13
申请人： DECIPHERA PHARMACEUTICALS, LLC , FLYNN, Daniel, L. , PETILLO, Peter, A. , KAUFMAN, Michael, D. , PATT, William, C.
发明人： FLYNN, Daniel, L. , PETILLO, Peter, A. , KAUFMAN, Michael, D. , PATT, William, C.
IPC分类号： A61K31/4375 , A61K31/519 , A61P1/00 , A61P11/00 , A61P17/06 , A61P19/02 , A61P35/00 , A61P37/00
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。本发明的化合物还可用于治疗类风湿性关节炎和视网膜病，包括糖尿病性视网膜神经病和黄斑变性。

8. 发明申请

WO2005079378A2 SYNTHETIC TECHNIQUES AND INTERMEDIATES FOR POLYHYDROXY DIENYL LACTONES AND MIMICS THEREOF 审中-公开
标题翻译：合成技术和中间体的聚羟基二烯基酯及其制备方法
公开(公告)号：WO2005079378A2
公开(公告)日：2005-09-01
申请号：PCT/US2005/004643
申请日：2005-02-11
申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA , SMITH, Amos, B., III , QUI, Yuping , KAUFMAN, Michael , ARIMOTO, Hirokazu , JONES, David, R. , KOBAYASHI, Kaoru , BEAUCHAMP, Thomas, J.
发明人： SMITH, Amos, B., III , QUI, Yuping , KAUFMAN, Michael , ARIMOTO, Hirokazu , JONES, David, R. , KOBAYASHI, Kaoru , BEAUCHAMP, Thomas, J.
IPC分类号： C07C271/12 , C07D213/30 , C07D263/22 , C07D303/16 , C07D309/10 , C07D309/30 , C07D309/32 , C07D319/06 , C07D339/08 , C07D407/06 , C07D413/06 , C07D413/12 , C07D417/06 , C07F7/18 , C07F9/54
CPC分类号： C07C271/12 , C07B2200/07 , C07D213/30 , C07D263/22 , C07D303/16 , C07D309/10 , C07D309/30 , C07D309/32 , C07D319/06 , C07D339/08 , C07D407/06 , C07D413/06 , C07D413/12 , C07D417/06 , C07F7/1852 , C07F7/1856 , C07F7/1892 , C07F9/5428 , C07F9/5442
摘要： Synthetic methods and intermediates useful in the preparation of lactone containing compounds such as discodermolide and compounds which mimic the chemical or biological activity of discodermolide are provided.
摘要翻译：提供了可用于制备含内酯化合物如discodermolide的合成方法和中间体以及模拟discodermolide的化学或生物活性的化合物。

9. 发明申请

WO2005009975A3 BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS 审中-公开
标题翻译：苯并咪唑衍生物作为MEK抑制剂
公开(公告)号：WO2005009975A3
公开(公告)日：2005-04-07
申请号：PCT/IB2004002355
申请日：2004-07-12
申请人： WARNER LAMBERT CO , BARRETT STEPHAN DOUGLAS , FLAMME CATHLIN MARIE , KAUFMAN MICHAEL DAVID , MILBANK JARED BRUCE JOHN , TECLE HAILE , WARMUS JOSEPH SCOTT
发明人： BARRETT STEPHAN DOUGLAS , FLAMME CATHLIN MARIE , KAUFMAN MICHAEL DAVID , MILBANK JARED BRUCE JOHN , TECLE HAILE , WARMUS JOSEPH SCOTT
IPC分类号： A61P35/00 , C07D235/06 , C07D235/10 , C07D235/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/04 , A61K31/4184 , C07D235/08
CPC分类号： C07D235/06 , C07D235/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/04
摘要： The present invention relates to N-methyl-substituted benzamidazole derivatives of formula (I), as defined in the specification; pharmaceutical compositions and mehtod of use thereof,as inhibitors of MEK.
摘要翻译：本发明涉及如本说明书中定义的式（I）的N-甲基取代的苯并咪唑衍生物; 药物组合物及其用途，作为MEK的抑制剂。

10. 发明申请

WO2004026170A3 MECHANICALLY ATTACHED ELASTOMERIC COVER FOR PROSTHESIS 审中-公开
标题翻译：机械连接弹药保护套
公开(公告)号：WO2004026170A3
公开(公告)日：2004-06-10
申请号：PCT/IL0300748
申请日：2003-09-17
申请人： IMPLIANT LTD , ARNIN URI , TUVAL YOSSI , BENARY RAPHAEL , KAUFMAN MICHAEL EARL
发明人： ARNIN URI , TUVAL YOSSI , BENARY RAPHAEL , KAUFMAN MICHAEL EARL
IPC分类号： A61F2/00 , A61F2/28 , A61F2/30 , A61F2/32 , A61F2/34 , A61F2/36 , A61F2/38 , A61F2/40
CPC分类号： A61F2/4014 , A61F2/32 , A61F2/34 , A61F2/3609 , A61F2/3877 , A61F2/40 , A61F2/4081 , A61F2002/30014 , A61F2002/30016 , A61F2002/30069 , A61F2002/3007 , A61F2002/30125 , A61F2002/30332 , A61F2002/30378 , A61F2002/30405 , A61F2002/30433 , A61F2002/30434 , A61F2002/30441 , A61F2002/30451 , A61F2002/30487 , A61F2002/30495 , A61F2002/30563 , A61F2002/30589 , A61F2002/30604 , A61F2002/3065 , A61F2002/30673 , A61F2002/30757 , A61F2002/30797 , A61F2002/30808 , A61F2002/30822 , A61F2002/30827 , A61F2002/30892 , A61F2002/30934 , A61F2002/3611 , A61F2002/4018 , A61F2220/0025 , A61F2220/0033 , A61F2220/0041 , A61F2220/0058 , A61F2230/0008 , A61F2250/0018 , A61F2250/0019 , A61F2310/00011 , A61F2310/00179
摘要： A prosthetic orthopedic implant assembly including an implant body, and an elastomeric cover connected to the implant body by a mechanical fastener.
摘要翻译：一种假体矫形植入物组件，包括植入体，以及通过机械紧固件连接到植入物本体的弹性体盖。

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