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1. 发明申请

WO2012019015A3 METHODS AND COMPOSITIONS FOR THE TREATMENT OF MYELOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES 审中-公开
公开(公告)号：WO2012019015A3
公开(公告)日：2012-02-09
申请号：PCT/US2011/046609
申请日：2011-08-04
申请人： DECIPHERA PHARMACEUTICALS, LLC , FLYNN, Daniel L. , PETILLO, Peter A. , KAUFMAN, Michael D. , BOOTH, Richard John
发明人： FLYNN, Daniel L. , PETILLO, Peter A. , KAUFMAN, Michael D. , BOOTH, Richard John
IPC分类号： A61K31/50 , A61K31/497 , A61K31/505
摘要： Compounds for treatment of diseases caused by oncogenic forms, aberrant fusion and polymorphs of c-ABL, FLT -3, cMET, KDR, PDGFR, HER, RET, c-FMS, or c-KIT kinase or combination thereof.

2. 发明申请

WO2008140895A1 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：WO2008140895A1
公开(公告)日：2008-11-20
申请号：PCT/US2008/060855
申请日：2008-04-18
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： 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，原发性肿瘤部位转移，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，嗜酸性粒细胞增多症，胃肠道间质瘤，结肠癌，以过度增殖为特征的导致失明的眼部疾病，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，其异常融合蛋白及其多形体，或由c-Kit激酶引起的疾病，致癌其形式，其异常融合蛋白及其多晶型物。

3. 发明申请

WO2008046003A3 KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES 审中-公开
公开(公告)号：WO2008046003A3
公开(公告)日：2008-04-17
申请号：PCT/US2007/081098
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： A61K31/54 , A61K39/395
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.

4. 发明申请

WO2006081034A2 ANTI-INFLAMMATORY MEDICAMENTS 审中-公开
标题翻译：抗炎药物
公开(公告)号：WO2006081034A2
公开(公告)日：2006-08-03
申请号：PCT/US2005/047597
申请日：2005-12-23
申请人： DECIPHERA PHARMACEUTICALS, LLC , FLYNN, Daniel, L. , PETILLO, Peter, A.
发明人： FLYNN, Daniel, L. , PETILLO, Peter, A.
IPC分类号： G01N33/53
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，癌症和以高血管化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

5. 发明申请

WO2012019015A2 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：WO2012019015A2
公开(公告)日：2012-02-09
申请号：PCT/US2011046609
申请日：2011-08-04
申请人： DECIPHERA PHARMACEUTICALS LLC , FLYNN DANIEL L , PETILLO PETER A , KAUFMAN MICHAEL D , BOOTH RICHARD JOHN
发明人： FLYNN DANIEL L , PETILLO PETER A , KAUFMAN MICHAEL D , BOOTH RICHARD JOHN
IPC分类号： A61K39/395 , A61K31/454 , A61K31/506 , A61K31/519 , A61P11/00 , A61P19/00 , A61P35/00
CPC分类号： A61K31/454 , A61K31/506 , A61K31/519
摘要： Compounds of the present invention find utility in the treatment of hyperproliferative diseases, including autoimmune diseases and other diseases characterized by hypervascularization or proliferation of myeloid, mast cells, fibroblasts, synoviocytes, or monocytes; mammalian cancers and especially human cancers including but not limited to melanomas; a disease caused by c-ABL kinase, oncogenic forms thereof, aberrant fusion proteins thereof including BCR-ABL kinase and polymorphs thereof; a disease caused by FLT-3 kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof; a disease caused by cMET kinase, oncogenic forms thereof, aberrant fusion proteins thereof including TPR-MET; a disease caused by KDR kinase or PDGFR kinases; a disease caused by HER kinases, oncogenic forms thereof and polymorphs thereof; a disease caused by RET kinase, oncogenic forms thereof, aberrant fusion proteins thereof; a disease caused by c-FMS kinase, oncogenic forms thereof and polymorphs thereof; a disease caused by a c-KIT kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof; and diseases caused by any of the foregoing kinases, oncogenic forms thereof, and aberrant fusion proteins thereof, including but not limited to, chronic myelogenous leukemia, acute lymphocytic leukemia, acute myeloid leukemia, other myeloproliferative disorders, a disease caused by metastasis of primary solid tumors to secondary sites, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, mesothelioma, hypereosinophilic syndrome, a disease caused or maintained by pathological vascularization, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, i.e. diabetic retinopathy and age-related macular degeneration, non small cell lung cancer, breast cancers, kidney cancers, colon cancers, cervical carcinomas, papillary thyroid carcinoma, melanomas, autoimmune diseases including rheumatoid arthritis, multiple sclerosis, lupus, asthma, 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, bone cancer, graft-versus-host reaction, Chron's disease, ulcerative colitis, inflammatory bowel disease, pyresis, gastrointestinal stromal tumors, mastocytosis, mast cell leukemia, and combinations thereof.
摘要翻译：本发明的化合物可用于治疗过度增殖性疾病，包括自身免疫疾病和其它特征在于骨髓，肥大细胞，成纤维细胞，滑膜细胞或单核细胞的高血管形成或增殖的疾病; 哺乳动物癌症，特别是人类癌症，包括但不限于黑素瘤; 由c-ABL激酶，其致癌形式引起的疾病，异常融合蛋白，包括BCR-ABL激酶及其多态性; 由FLT-3激酶，其致癌形式，异常融合蛋白及其多态性引起的疾病; 由cMET激酶引起的疾病，其致癌形式，异常融合蛋白，包括TPR-MET; 由KDR激酶或PDGFR激酶引起的疾病; 由HER激酶，其致癌形式及其多晶型物引起的疾病; 由RET激酶，其致癌形式，异常融合蛋白引起的疾病; 由c-FMS激酶，其致癌形式及其多形体引起的疾病; 由c-KIT激酶，其致癌形式，异常融合蛋白及其多态性引起的疾病; 以及由上述激酶，其致癌形式及其异常融合蛋白引起的疾病，包括但不限于慢性骨髓性白血病，急性淋巴细胞性白血病，急性骨髓性白血病，其他骨髓增生性疾病，由原发性转移引起的疾病肿瘤到继发部位，胶质母细胞瘤，卵巢癌，胰腺癌，前列腺癌，肺癌，间皮瘤，嗜酸性粒细胞综合征，由病理性血管形成引起或维持的疾病，以过度增生为特征的眼病，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黄斑变性，非小细胞肺癌，乳腺癌，肾癌，结肠癌，宫颈癌，甲状腺乳头状癌，黑素瘤，自身免疫性疾病，包括类风湿性关节炎，多发性硬化症，狼疮，哮喘，人类炎症，类风湿性脊椎炎，关节炎，哮喘，痛风脓毒病，败血症，败血症休克，内毒素休克，革兰氏阴性败血症，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，克隆氏病，溃疡性结肠炎，炎症性肠病，胃肠道间质瘤，肥大细胞增多症，肥大细胞白血病及其组合。

6. 发明申请

WO2008033999A3 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：WO2008033999A3
公开(公告)日：2008-08-07
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。

7. 发明申请

WO2007008917A2 MODULATION OF PROTEIN FUNCTIONALITIES 审中-公开
标题翻译：蛋白质功能调节
公开(公告)号：WO2007008917A2
公开(公告)日：2007-01-18
申请号：PCT/US2006/026920
申请日：2006-07-10
申请人： DECIPHERA PHARMACEUTICALS, LLC , FLYNN, Daniel, L. , PETILLO, Peter, A.
发明人： FLYNN, Daniel, L. , PETILLO, Peter, A.
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.
摘要翻译：提供了用于合理鉴定能够与特定天然存在的蛋白质相互作用的分子的新方法，以产生新的药理学上重要的化合物和治疗方式。广泛地，该方法包括鉴定形成特定目的蛋白质的一部分的开关控制配体，以及鉴定形成蛋白质的一部分并与所述开关对照配体相互作用的互补开关控制袋。配体与Hie口袋相互作用以调节蛋白质的构象和生物活性，使得蛋白质在配体 - 口袋相互作用时呈现第一构象和第一生物学活性，并呈现第二种不同的构象和生物学活性没有配体 - 口袋相互作用。接下来，提供第一和第二构象中的所述蛋白质的各个样品，并且通过使分子和样品接触将它们与一种或多种候选分子进行筛选。因此，可以鉴定在口袋区域与蛋白质结合的小分子。还提供了新的蛋白质调节剂加合物和改变蛋白质活性的方法。

8. 发明申请

WO2006014290A3 ANTI-INFLAMMATORY MEDICAMENTS 审中-公开
标题翻译：抗炎药物
公开(公告)号：WO2006014290A3
公开(公告)日：2006-04-27
申请号：PCT/US2005023100
申请日：2005-06-30
申请人： DECIPHERA PHARMACEUTICALS LLC , FLYNN DANIEL L , PETILLO PETER A
发明人： FLYNN DANIEL L , PETILLO PETER A
IPC分类号： A61K31/4184 , A61K31/426 , A61K31/4745 , A61K31/496 , A61K31/517 , A61K31/53 , A61K31/5377 , C07D231/40 , C07D401/04 , C07D401/12 , C07D403/10 , C07D403/12 , C07D417/10 , C07D417/12 , C07D417/14 , C07D237/04
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.
摘要翻译：提供了新的化合物和使用这些化合物治疗炎性病症的方法。在优选的实施方案中，调节p38激酶蛋白的活化状态包括使激酶蛋白与新化合物接触的步骤。

9. 发明申请

WO2005024755A2 MEDICAMENTS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS OR DIABETES 审中-公开
标题翻译：治疗神经损伤性疾病或糖尿病的药物
公开(公告)号：WO2005024755A2
公开(公告)日：2005-03-17
申请号：PCT/US2004/011922
申请日：2004-04-15
申请人： DECIPHERA PHARMACEUTICALS, LLC. , FLYNN, Daniel, L. , PETILLO, Peter, A.
发明人： FLYNN, Daniel, L. , PETILLO, Peter, A.
IPC分类号： G09B1/00
CPC分类号： G09B1/00 , G09B19/02
摘要： Novel compounds and methods are provided for the treatment of human neurodegenerative diseases, diabetes, mental conditions, inflammatory diseases, strokes and cancers. The compounds are small molecule inhibitors of glycogen synthease kinase-3 proteins. GSK-3 kinase protein/small molecule inhibitor compound adducts are also described wherein the compounds are bonded to the kinase proteins at the region of a protein switch control pocket in order to alter the conformation and/or protein activity of the kinases.
摘要翻译：提供新的化合物和方法用于治疗人神经变性疾病，糖尿病，精神状况，炎性疾病，中风和癌症。这些化合物是糖原合成酶激酶-3蛋白的小分子抑制剂。还描述了GSK-3激酶蛋白/小分子抑制剂化合物加合物，其中化合物与蛋白质切换对照口袋区域的激酶蛋白结合，以改变激酶的构象和/或蛋白质活性。

10. 发明申请

WO2012075331A2 TISSUE IMPLANTABLE MICROBIOSENSOR 审中-公开
标题翻译：组织可植入式微生物传感器
公开(公告)号：WO2012075331A2
公开(公告)日：2012-06-07
申请号：PCT/US2011062951
申请日：2011-12-01
申请人： PINNACLE TECHNOLOGY INC , PETILLO PETER A , WILSON GEORGE S , WU JUDY Z , RICHTER MARK L , JOHNSON DAVID A , AILLON DANIEL V
发明人： PETILLO PETER A , WILSON GEORGE S , WU JUDY Z , RICHTER MARK L , JOHNSON DAVID A , AILLON DANIEL V
CPC分类号： A61B5/14865 , A61B5/14532 , A61B2562/12 , C25D7/00
摘要： A biosensor system comprises a capillary substrate, conductive electrode, and a plurality of nanoparticles having an enzyme deposited thereon formed in a cavity at one end of the capillary substrate. The substrate may have an optional reinforcing layer (which may be conductive or non-conductive) and optional insulating layer thereon. A cannula having an optional conductive layer, insulating layer, and reference electrode may also form part of the system.
摘要翻译：生物传感器系统包括毛细管基底，导电电极和在毛细管基底的一端形成在腔中的沉积有酶的多个纳米颗粒。衬底可以具有可选的增强层（其可以是导电的或不导电的）和其上的可选的绝缘层。具有可选导电层，绝缘层和参考电极的插管也可以形成系统的一部分。

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