公开(公告)号：US10966966B2

公开(公告)日：2021-04-06

申请号：US17028640

申请日：2020-09-22

申请人： Deciphera Pharmaceuticals, LLC

发明人： Rodrigo Ruiz Soto ,  Oliver Rosen ,  Jama Pitman

IPC分类号： A61K31/4375 ,  A61P35/00

摘要： The present disclosure relates to methods of treating gastrointestinal stromal tumors to a subject in need thereof, comprising administering to the subject a therapeutically effective amount of ripretinib or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20210046059A1

公开(公告)日：2021-02-18

申请号：US17028640

申请日：2020-09-22

申请人： Deciphera Pharmaceuticals, LLC

发明人： Rodrigo Ruiz Soto ,  Oliver Rosen ,  Jama Pitman

IPC分类号： A61K31/4375 ,  A61P35/00

摘要： The present disclosure relates to methods of treating gastrointestinal stromal tumors to a subject in need thereof, comprising administering to the subject a therapeutically effective amount of ripretinib or a pharmaceutically acceptable salt thereof.

公开(公告)号：US09387202B2

公开(公告)日：2016-07-12

申请号：US14549125

申请日：2014-11-20

申请人： Deciphera Pharmaceuticals, LLC ,  Eli Lilly and Company

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

IPC分类号： A61K31/444 ,  C07D213/82

CPC分类号： A61K31/444 ,  C07D213/82

摘要： Compounds useful in the treatment of mammalian cancers and especially human cancers according to Formula I are disclosed. Pharmaceutical compositions and methods of treatment employing the compounds disclosed herein are also disclosed.

公开(公告)号：US09309224B2

公开(公告)日：2016-04-12

申请号：US14214179

申请日：2014-03-14

申请人： Deciphera Pharmaceuticals, LLC

发明人： Daniel L. Flynn ,  Timothy Malcolm Caldwell ,  Thiwanka Samarakoon ,  Lakshminarayana Vogeti ,  Michael D. Kaufman ,  William C. Patt ,  YuMi Ahn

IPC分类号： C07D213/65 ,  C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D493/08

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D493/08

摘要： Described are compounds of Formula 1 which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.

摘要翻译： 描述了通过抑制c-FMS（CSF-1R），c-KIT和/或PDGFR激酶在治疗癌症，自身免疫性疾病和代谢性骨骼疾病中有效的式1化合物。 这些化合物也可用于治疗由c-FMS，c-KIT或PDGFR激酶介导的其它哺乳动物疾病。

公开(公告)号：US20140275016A1

公开(公告)日：2014-09-18

申请号：US14214179

申请日：2014-03-14

申请人： Deciphera Pharmaceuticals, LLC

发明人： Daniel L. Flynn ,  Timothy Malcolm Caldwell ,  Thiwanka Samarakoon ,  Lakshminarayana Vogeti ,  Michael D. Kaufman ,  William C. Patt ,  YuMi Ahn

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D493/08 ,  C07D405/14

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D493/08

摘要： Described are compounds of Formula 1 which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.

摘要翻译： 描述了通过抑制c-FMS（CSF-1R），c-KIT和/或PDGFR激酶在治疗癌症，自身免疫性疾病和代谢性骨骼疾病中有用的式1化合物。 这些化合物也可用于治疗由c-FMS，c-KIT或PDGFR激酶介导的其它哺乳动物疾病。

公开(公告)号：US08461179B1

公开(公告)日：2013-06-11

申请号：US13491394

申请日：2012-06-07

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

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

IPC分类号： A01N43/42 ,  A61K31/44

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.

公开(公告)号：US08163756B2

公开(公告)日：2012-04-24

申请号：US11963740

申请日：2007-12-21

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

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

IPC分类号： C07D401/02 ,  A61K31/44

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。

公开(公告)号：US07897762B2

公开(公告)日：2011-03-01

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： A61K31/519 ,  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。

公开(公告)号：US07737283B2

公开(公告)日：2010-06-15

申请号：US11450849

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： C07D285/10 ,  C07D233/00 ,  A61K31/41 ,  A61K31/415 ,  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.

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。

公开(公告)号：US07531566B2

公开(公告)日：2009-05-12

申请号：US11336708

申请日：2006-01-20

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

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

IPC分类号： A61K31/415 ,  A61K31/54

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.