isothiazol-3-yl-[5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-5,8-diazaspiro[2.6]nonan-8-yl]methanone | 1354625-78-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: isothiazol-3-yl-[5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-5,8-diazaspiro[2.6]nonan-8-yl]methanone
• 英文别名: [5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-5,8-diazaspiro[2.6]nonan-8-yl]-(1,2-thiazol-3-yl)methanone
• CAS: 1354625-78-7
• 化学式: C₁₇H₁₈N₆OS
• 分子量: 354.436
• InChiKey: HTLLKUXKXFDMTR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  25
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  106
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• [EN] NOVEL HOMOPIPERAZINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS AND PHARMACEUTICAL USE THEREOF<br/>[FR] NOUVEAUX DÉRIVÉS D'HOMOPIPÉRAZINE COMME INHIBITEURS DE PROTÉINES TYROSINE KINASES ET LEUR UTILISATION PHARMACEUTIQUE
  申请人：LEO PHARMA AS

  公开号：WO2012003829A1

  公开（公告）日：2012-01-12

  The invention relates to compounds of general formula (I) wherein R1,R2, R3, R4, m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use -alone or in combination with one or more other pharmaceutically active compounds- in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disesase, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.

  该发明涉及一般式(I)的化合物，其中R1、R2、R3、R4、m和n的定义如本文所述，以及其药学上可接受的盐、水合物或溶剂化合物，用于单独使用或与一个或多个其他药理活性化合物结合在一起进行治疗，作为JAK激酶和蛋白酪氨酸激酶抑制剂，用于预防、治疗或改善疾病及其并发症，包括例如牛皮癣、特应性皮炎、酒渣鼻、狼疮、多发性硬化、类风湿关节炎、I型糖尿病、哮喘、癌症、自身免疫性甲状腺疾病、溃疡性结肠炎、克罗恩病、阿尔茨海默病、白血病、眼疾病如糖尿病视网膜病变和黄斑变性以及其他自身免疫疾病和需要免疫抑制的适应症，例如器官移植。
• NOVEL HOMOPIPERAZINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS AND PHARMACEUTICAL USE THEREOF
  申请人：Nielsen Simon Felbdæk

  公开号：US20130172325A1

  公开（公告）日：2013-07-04

  The invention relates to compounds of general formula (I) wherein R 1 , R 2 , R 3 , R 4 , m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immuno-suppression would be desirable for example in organ transplantation.

  本发明涉及一般式（I）的化合物，其中R1、R2、R3、R4、m和n如本文所定义，并且其药物可接受的盐、水合物或溶剂化物，用于治疗，单独或与一个或多个其他药物活性化合物联合使用，作为JAK激酶和蛋白酪氨酸激酶抑制剂，用于预防、治疗或缓解疾病及其并发症，包括例如银屑病、特应性皮炎、酒渣鼻、红斑狼疮、多发性硬化症、类风湿性关节炎、1型糖尿病、哮喘、癌症、自身免疫性甲状腺疾病、溃疡性结肠炎、克隆病、阿尔茨海默病、白血病、眼部疾病如糖尿病视网膜病变和黄斑变性以及其他自身免疫性疾病和需要免疫抑制的指征，例如器官移植。
• US9586961B2
  申请人：——

  公开号：US9586961B2

  公开（公告）日：2017-03-07