1-[(3S)-3-methylpyrrolidin-1-yl]prop-2-en-1-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 1-[(3S)-3-methylpyrrolidin-1-yl]prop-2-en-1-one
• 化学式: C₈H₁₃NO
• 分子量: 139.19
• InChiKey: LDJYZHYUFLLNFK-ZETCQYMHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  1

文献信息

• INHIBITORS OF BRUTON'S TYROSINE KINASE
  申请人：Pharmacyclics, Inc.

  公开号：US20140142123A1

  公开（公告）日：2014-05-22

  Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

  本文披露了一些与布鲁顿酪氨酸激酶（Btk）形成共价键的化合物。还描述了Btk的不可逆抑制剂。本文披露了制备这些化合物的方法。还披露了包括这些化合物的药物组合物。披露了使用Btk抑制剂的方法，单独或与其他治疗剂一起，用于治疗自身免疫疾病或病况，异种免疫疾病或病况，癌症，包括淋巴瘤和炎症性疾病或病况。
• SUBSTITUTED NICOTINIMIDE INHIBITORS OF BTK AND THEIR PREPARATION AND USE IN THE TREATMENT OF CANCER, INFLAMMATION AND AUTOIMMUNE DISEASE
  申请人：BEIJING SYNERCARE PHARMA TECH CO., LTD.

  公开号：US20160237075A1

  公开（公告）日：2016-08-18

  Compounds of Formula I, as shown below and defined herein: and pharmaceutically acceptable salts, syntheses, intermediates, formulations, and methods of treating diseases including cancer, inflammation, and autoimmune disease mediated at least in part by Bruton's Tyrosine Kinase (BTK).

  化学式为I的化合物，如下所示，其定义如下：以及药学上可接受的盐，合成物，中间体，制剂和治疗疾病的方法，包括由布鲁顿酪氨酸激酶（BTK）介导的癌症，炎症和自身免疫疾病。
• INHIBITORS OF FIBROBLAST GROWTH FACTOR RECEPTOR AND USE THEREOF
  申请人：Nanjing Transthera Biosciences Co. Ltd.

  公开号：EP3508482A1

  公开（公告）日：2019-07-10

  Provided are an irreversible inhibitor of a fibroblast growth factor receptor (FGFR) as indicated by formula I, a pharmaceutically acceptable salt, a stereoisomer, a pharmaceutical preparation, a pharmaceutical composition and an application thereof. R1, R2, R3, R4, ring A, Ar, ring B and warhead are as defined in the specification. The compound has high-efficiency and high-selectivity inhibition of a fibroblast growth factor receptor and can be applied to treatment of abnormal FGF/FGFR-mediated diseases, in particular the treatment of cancers.

  本发明提供了一种如式 I 所示的成纤维细胞生长因子受体（FGFR）不可逆抑制剂、一种药学上可接受的盐、一种立体异构体、一种药物制剂、一种药物组合物及其应用。R1、R2、R3、R4、环 A、Ar、环 B 和弹头如说明书中所定义。该化合物对成纤维细胞生长因子受体具有高效率和高选择性的抑制作用，可应用于治疗异常的FGF/FGFR介导的疾病，特别是癌症的治疗。
• THIAZOLYL-CONTAINING COMPOUNDS FOR TREATING PROLIFERATIVE DISEASES
  申请人：Dana-Farber Cancer Institute

  公开号：EP3715346A1

  公开（公告）日：2020-09-30

  The present disclosure provides thiazolyl-containing compounds of Formula (II). The compounds described herein may be able to inhibit protein kinases (e.g., Src family kinases (e.g., hemopoietic cell kinase (HCK)), Bruton's tyrosine kinase (BTK)) and may be useful in treating and/or preventing proliferative diseases (e.g., myelodysplasia, leukemia, lymphoma (e.g., Waldenstrom's macroglobulinemia)) and in inducing apoptosis in a cell (e.g., malignant blood cell). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.

  本公开提供了式(II)的含噻唑化合物。本文所述化合物可抑制蛋白激酶（如 Src 家族激酶（如造血细胞激酶 (HCK)）、布鲁顿酪氨酸激酶 (BTK)），可用于治疗和/或预防增殖性疾病（如、骨髓增生异常、白血病、淋巴瘤（如瓦尔登斯特罗姆氏巨球蛋白血症））和诱导细胞（如恶性血细胞）凋亡。本公开还提供了包括或使用本文所述化合物的药物组合物、试剂盒、方法和用途。
• Aminopyridazinone compounds as protein kinase inhibitors
  申请人：Jiangsu Hengrui Medicine Co., Ltd.

  公开号：US10323037B2

  公开（公告）日：2019-06-18

  The present disclosure provides a compound of formula (I) and the use thereof for the therapeutic treatment of human cancers including B-cell lymphoma and autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, and multiple sclerosis.

  本公开提供了一种式（I）化合物及其在人类癌症（包括 B 细胞淋巴瘤）和自身免疫性疾病（如类风湿性关节炎、系统性红斑狼疮和多发性硬化症）治疗中的用途。