5-iodo-4-((2-(methyloxy)phenyl)oxy)-N-(4-(4-methyl-1-piperazinyl)phenyl)-2-pyrimidinamine | 835639-22-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 5-iodo-4-((2-(methyloxy)phenyl)oxy)-N-(4-(4-methyl-1-piperazinyl)phenyl)-2-pyrimidinamine
• 英文别名: 5-iodo-4-(2-methoxyphenoxy)-N-(4-(4-methylpiperazin-1-yl)phenyl)pyrimidin-2-amine；5-iodo-4-(2-methoxyphenoxy)-N-[4-(4-methylpiperazin-1-yl)phenyl]pyrimidin-2-amine
• CAS: 835639-22-0
• 化学式: C₂₂H₂₄IN₅O₂
• 分子量: 517.369
• InChiKey: ALVZQVNNASDEFA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  30
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  62.8
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• [EN] 2-AMINO-4-HYDROXY-5-PYRIMIDINECARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF T CELL ACTIVATION FOR THE TREATMENT OF INFLAMMATORY DISEASES<br/>[FR] DERIVES DE 2-AMINO-4-HYDROXY-5-PYRIMIDINOCARBOXAMIDE ET COMPOSES ASSOCIES SERVANT D'INHIBITEURS DE L'ACTIVATION DES LYMPHOCYTES T POUR LE TRAITEMENT DE MALADIES INFLAMMATOIRES
  申请人：AMGEN INC

  公开号：WO2005009443A1

  公开（公告）日：2005-02-03

  The present invention relates to pyrimidine or pyridine carboxamides or pharmaceutically-acceptable salts thereof. Also included is a method of treatment of inflammation, inhibition of T cell activation and proliferation, arthritis, rheumatoid arthritis, psoriatic arthritis, osteoarthritis, organ transplant, acute transplant or heterograft or homograft rejection, transplantation tolerance induction, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, including ulcerative colitis, Crohn's disease, lupus, contact hypersensitivity, delayed-type hypersensitivity, and gluten-sensitive enteropathy, type 1 diabetes, psoriasis, contact dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, glomerulonephritis, serum sickness, uticaria, allergic diseases, asthma, hayfever, allergic rhinitis, scleracielma, mycosis fungoides, dermatomyositis, alopecia areata, chronic actinic dermatitis, eczema, Behcet's disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary's syndrome, atopic dermatitis, systemic schlerosis, morphea, atopic dermatitis, colon carcinoma or thymoma in a mammal comprising administering a therapeutically-effective amount a compound as described above.

  本发明涉及嘧啶或吡啶甲酰胺或其药用可接受的盐。还包括一种治疗炎症、抑制T细胞激活和增殖、关节炎、类风湿性关节炎、银屑病关节炎、骨关节炎、器官移植、急性移植或异体移植或同种异体移植排斥、移植耐受性诱导、缺血或再灌注损伤、心肌梗死、中风、多发性硬化症、炎症性肠病，包括溃疡性结肠炎、克罗恩病、狼疮、接触超敏反应、迟发型超敏反应和谷蛋白敏感性肠病、1型糖尿病、银屑病、接触性皮炎、桥本甲状腺炎、舍格伦综合征、自身免疫性甲状腺功能亢进、阿狄森病、自身免疫多腺体病、自身免疫性脱发、恶性贫血、白癜风、自身免疫性垂体功能减退、吉兰-巴雷综合征、肾小球肾炎、血清病、荨麻疹、过敏性疾病、哮喘、花粉症、过敏性鼻炎、硬皮病、真菌病、皮肌炎、斑秃、慢性日光性皮炎、湿疹、贝赫切特病、掌跖脓疱病、脓皮病、塞扎里综合征、特应性皮炎、系统性硬化病、硬皮病、特应性皮炎、结肠癌或胸腺瘤的方法，包括施用如上所述的化合物的治疗有效量。
• Substituted heterocyclic compounds and methods of use
  申请人：Nunes J. Joseph

  公开号：US20050209221A1

  公开（公告）日：2005-09-22

  The present invention relates to pyrimidine or pyridine carboxamides or pharmaceutically-acceptable salts thereof. Also included is a method of treatment of inflammation, inhibition of T cell activation and proliferation, arthritis, rheumatoid arthritis, psoriatic arthritis, osteoarthritis, organ transplant, acute transplant or heterograft or homograft rejection, transplantation tolerance induction, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, including ulcerative colitis, Crohn's disease, lupus, contact hypersensitivity, delayed-type hypersensitivity, and gluten-sensitive enteropathy, type 1 diabetes, psoriasis, contact dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, glomerulonephritis, serum sickness, uticaria, allergic diseases, asthma, hayfever, allergic rhinitis, scleracielma, mycosis fungoides, dermatomyositis, alopecia areata, chronic actinic dermatitis, eczema, Behcet's disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary's syndrome, atopic dermatitis, systemic schlerosis, morphea, atopic dermatitis, colon carcinoma or thymoma in a mammal comprising administering a therapeutically-effective amount a compound as described above.

  本发明涉及嘧啶或吡啶羧酰胺或其药学上可接受的盐。还包括一种治疗炎症、抑制T细胞激活和增殖、关节炎、类风湿性关节炎、银屑病性关节炎、骨关节炎、器官移植、急性移植或异种移植或同种移植排斥、移植耐受性诱导、缺血或再灌注损伤、心肌梗塞、中风、多发性硬化症、炎症性肠病（包括溃疡性结肠炎、克罗恩病）、狼疮、接触性超敏反应、迟发型超敏反应和对谷蛋白敏感的肠病、1型糖尿病、银屑病、接触性皮炎、桥本氏甲状腺炎、干燥综合症、自身免疫性甲状腺功能亢进症、亚当逊病、自身免疫性多腺体病、自身免疫性脱发症、恶性贫血、白癜风、自身免疫性垂体功能减退症、格林-巴利综合症、肾小球肾炎、血清病、荨麻疹、过敏性疾病、哮喘、花粉热、过敏性鼻炎、硬皮病、真菌性肿瘤、皮肌炎、斑秃、慢性光化性皮炎、湿疹、Behcet病、掌跖病性脓疱病、脓疱病、Sezary综合症、特应性皮炎、系统性硬化病、硬皮病、特应性皮炎、哺乳动物的结肠癌或胸腺瘤的方法，包括向其施用上述化合物的治疗剂量。
• Heteroaryl-substituted alkyne compounds and method of use
  申请人：Chaffee C. Stuart

  公开号：US20060217380A1

  公开（公告）日：2006-09-28

  The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A 1 , A 2 , A 3 , A 4 , R 1 and R 2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.

  本发明涉及一种新型化合物类别，可用于预防和治疗蛋白激酶介导的疾病，包括炎症、癌症和相关病症。该化合物具有一般式I，其中A1、A2、A3、A4、R1和R2如本文所定义。因此，本发明还涉及包含本发明化合物的制药组合物，使用本发明化合物和组合物预防和治疗激酶介导的疾病的方法，以及用于制备本发明化合物的中间体和过程。
• HETEROARYL-SUBSTITUTED ALKYNE COMPOUNDS AND METHOD OF USE
  申请人：Chaffee Stuart C.

  公开号：US20100160283A1

  公开（公告）日：2010-06-24

  The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A 1 , A 2 , A 3 , A 4 , R 1 and R 2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.

  本发明涉及一类新的化合物，用于预防和治疗蛋白激酶介导的疾病，包括炎症、癌症和相关疾病。该化合物具有一般式I，其中A1、A2、A3、A4、R1和R2的定义如本文所述。因此，本发明还涉及包括本发明化合物的制药组合物，使用本发明化合物和组合物预防和治疗激酶介导的疾病的方法，以及用于制备本发明化合物的中间体和过程。
• 2-AMINO-4-HYDROXY-5-PYRIMIDINCARBOXAMID DERIVATIVES AND RELATED COMPOUNDS AS T-CELL ACTIVATION INHIBITORS FOR THE TREATMENT OF INFLAMMATIONS
  申请人：AMGEN INC.

  公开号：EP1648464A1

  公开（公告）日：2006-04-26