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1. 发明公开

EP3191449A1 NOVEL COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS 有权
标题翻译：在转运（RET）抑制剂过程中重新配制的新化合物
公开(公告)号：EP3191449A1
公开(公告)日：2017-07-19
申请号：EP15840612.4
申请日：2015-09-10
申请人： GlaxoSmithKline Intellectual Property Development Limited
发明人： CHEUNG, Mui , DEMARTINO, Michael P. , EIDAM, Hilary Schenck , GUAN, Huiping Amy , QIN, Donghui , WU, Chengde , GONG, Zhen , YANG, Haiying , YU, Haiyu , ZHANG, Zhiliu
IPC分类号： C07D211/94 , C07D217/24 , C07D239/22 , A61K31/4412 , A61K31/4427 , A61P35/00 , A61P1/00 , A61P43/00
CPC分类号： C07D491/048 , C07B2200/13 , C07D213/64 , C07D213/65 , C07D213/69 , C07D213/75 , C07D217/24 , C07D221/00 , C07D221/04 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D471/04
摘要： This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.
摘要翻译：本发明涉及作为转染期间重排（RET）激酶抑制剂的新化合物，含有它们的药物组合物，其制备方法，以及它们单独或组合用于胃肠敏感性正常化的用途，（RET）功能障碍相关疾病相关的动力和/或分泌和/或腹部病症或疾病和/或治疗，或者RET活性的调节可能具有治疗益处，包括但不限于肠易激综合征（IBS）的所有分类，包括腹泻 - 功能性腹胀，功能性腹泻，非特异性功能性肠病，功能性腹痛综合征，慢性特发性便秘，功能性食管疾病，功能性胃十二指肠疾病，功能性肛门直肠疼痛，炎症性肠病，增殖性疾病疾病等如非小细胞肺癌，肝细胞癌，结直肠癌，甲状腺髓样癌，甲状腺滤泡癌，甲状腺未分化癌，乳头状甲状腺癌，脑肿瘤，腹腔癌，实体瘤，其他肺癌，头颈部癌，神经胶质瘤，神经母细胞瘤，Von Hippel-Lindau综合征和肾肿瘤，乳腺癌，输卵管癌，卵巢癌，移行细胞癌，前列腺癌，食管癌和胃食管连接癌，胆管癌，腺癌和RET激酶活性增加的任何恶性肿瘤。

2. 发明公开

EP3517526A1 NOVEL COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS 有权
公开(公告)号：EP3517526A1
公开(公告)日：2019-07-31
申请号：EP19160650.8
申请日：2015-09-09
申请人： GlaxoSmithKline Intellectual Property Development Limited
发明人： DEMARTINO, Michael P. , GUAN, Huiping Amy
IPC分类号： C07D213/69 , A61K31/4412 , A61P35/00
摘要： This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.

3. 发明公开

EP3790871A1 FURIN INHIBITORS 有权转让
公开(公告)号：EP3790871A1
公开(公告)日：2021-03-17
申请号：EP19725058.2
申请日：2019-05-10
申请人： GlaxoSmithKline Intellectual Property Development Limited
发明人： AXTEN, Jeffrey Michael , CHEUNG, Mui , DEMARTINO, Michael P. , GUAN, Huiping Amy , HU, Yan , MILLER, Aaron Bayne , QIN, Donghui , WU, Chengde , ZHANG, Zhiliu , LIN, Xiaojuan
IPC分类号： C07D401/14 , A61K31/44 , A61K31/4427 , C07D213/76 , C07D401/04 , C07D413/12

4. 发明授权

EP3517526B1 PYRIDINONES AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS 有权
公开(公告)号：EP3517526B1
公开(公告)日：2020-08-19
申请号：EP19160650.8
申请日：2015-09-09
申请人： GlaxoSmithKline Intellectual Property Development Limited
发明人： DEMARTINO, Michael P. , GUAN, Huiping Amy
IPC分类号： C07D213/69 , A61K31/4412 , A61P35/00

5. 发明授权

EP3191450B1 PYRIDONE DERIVATIVES AS REARRANGED DURING TRANSFECTION (RET) KINASE INHIBITORS 有权转让
公开(公告)号：EP3191450B1
公开(公告)日：2019-04-10
申请号：EP15767599.2
申请日：2015-09-09
申请人： GlaxoSmithKline Intellectual Property Development Limited
发明人： DEMARTINO, Michael P. , GUAN, Huiping Amy
IPC分类号： C07D213/69 , A61K31/4412 , A61P35/00

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