DEMARTINO, MICHAEL P.,迪麦提诺 麦可,迪麥提諾 麥可,GUAN, AMY HUIPING,关慧萍,關慧萍,迪麦提诺 麦可,迪麥提諾 麥可
申请号：
TW104129876
公开号：
TW201625534A
申请日:
2015.09.10
申请国别(地区):
TW
年份:
2016
代理人:
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.本發明係關於轉染重排(RET)激酶抑制劑之新穎化合物、包含彼等之醫藥組成物、其製備方法，以及其單獨或組合用於正常化胃腸敏感、蠕動力及/或分泌，及/或腹部病症或疾病之治療上用途，及/或治療與RET機能障礙有關的或其中調節RET活性可能具有治療利益的相關疾病，包括(但不限於)所有分類的腸躁症(IBS)，包括腹瀉型、便祕型或交替型、功能性腹脹、功能性便秘、功能性腹瀉、非特定之功能性腸道疾病、功能性腹痛症候群、慢性特發性便秘、功能性食道病症、功能性胃十二指腸病症、功能性肛門直腸疼痛、發炎性腸道疾病、增生性疾病例如非小細胞肺癌、肝細胞癌、結腸直腸癌、甲狀腺髓質癌、濾泡性甲狀腺癌、甲狀腺未分化癌、乳突性甲狀腺癌、腦腫瘤、腹膜腔癌、實體腫瘤、其他肺癌、頭頸癌、神經膠質瘤、神經母細胞瘤、馮希伯-林島氏症(Von Hippel-Lindau Syndrome)及腎腫瘤、乳癌、輸卵管癌、卵巢癌、過渡細胞癌、前列腺癌、食道及胃食道連接
