4,6-Dichlor-5-isopropylpyrimidin | 89938-06-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 4,6-Dichlor-5-isopropylpyrimidin
• 英文别名: 4,6-dichloro-5-isopropyl-pyrimidine；4,6-Dichloro-5-(propan-2-yl)pyrimidine；4,6-dichloro-5-propan-2-ylpyrimidine
• CAS: 89938-06-7
• 化学式: C₇H₈Cl₂N₂
• mdl: MFCD18844158
• 分子量: 191.06
• InChiKey: WGEQNVJAKYNYTM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.428
• 拓扑面积：
  25.8
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  L-4-(N,N-dimethylcarbamyloxy)phenylalanine tert-butyl ester 、 4,6-Dichlor-5-isopropylpyrimidin 在 二异戊胺 作用下， 以 乙醇 为溶剂， 反应 48.0h， 生成
  参考文献：
  名称：

  [EN] STEROID SPARING AGENTS AND THEIR USE
  [FR] AGENTS DE PRESERVATION DE STEROIDES ET LEURS PROCEDES D'UTILISATION

  摘要：

  公开号：

  WO2005097162A3
• 作为产物：
  描述：

  5-isopropyl-1H-pyrimidine-4,6-dione 在 N,N-二甲基苯胺 、 三氯氧磷 作用下， 反应 3.0h， 生成 4,6-Dichlor-5-isopropylpyrimidin
  参考文献：
  名称：

  [EN] STEROID SPARING AGENTS AND THEIR USE
  [FR] AGENTS DE PRESERVATION DE STEROIDES ET LEURS PROCEDES D'UTILISATION

  摘要：

  公开号：

  WO2005097162A3

文献信息

• Steroid sparing agents and methods of using same
  申请人：Lieberburg Ivan

  公开号：US20060004019A1

  公开（公告）日：2006-01-05

  This invention relates generally to methods of treatment of inflammatory bowel diseases (IBD), asthma, multiple schlerosis (MS), rheumatoid arthritis (RA), graft vs. host disease (GVHD), host vs. graft disease, and various spondyloarthropathies, comprising administering a steroid sparing immunoglobulin or small molecule composition to a patient in need thereof. The invention also relates generally to combination therapies for the treatment of these conditions.

  本发明涉及治疗炎症性肠病(IBD)、哮喘、多发性硬化症(MS)、类风湿性关节炎(RA)、移植物抗宿主病(GVHD)、宿主抗移植物病以及各种脊柱关节病的方法，包括向需要治疗的患者投予一种节省类固醇的免疫球蛋白或小分子组合物。本发明还涉及治疗这些疾病的联合疗法。
• Heteroaryl, heterocyclic and aryl compounds which inhibit leukocyte adhesion mediated by VLA-4
  申请人：——

  公开号：US20030125324A1

  公开（公告）日：2003-07-03

  Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

  本发明涉及一种可以结合VLA-4的化合物。其中一些化合物还可以抑制白细胞粘附，特别是通过VLA-4介导的白细胞粘附。这些化合物在哺乳动物患者（例如人类）的炎症性疾病治疗中非常有用，例如哮喘、阿尔茨海默病、动脉硬化、艾滋病痴呆、糖尿病、炎症性肠病、类风湿性关节炎、组织移植、肿瘤转移和心肌缺血。这些化合物还可以用于治疗多发性硬化等炎症性脑部疾病。
• Heteroaryl, heterocyclic and aryl compounds which inhibit leukocyte adhesion mediated byVLA-4
  申请人：——

  公开号：US20030139402A1

  公开（公告）日：2003-07-24

  Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

  本发明涉及一种与VLA-4结合的化合物。其中某些化合物还抑制白细胞粘附，特别是由VLA-4介导的白细胞粘附。这样的化合物可用于治疗哺乳动物患者（例如人类）的炎症性疾病，例如哮喘、阿尔茨海默病、动脉硬化、艾滋病痴呆、糖尿病、炎症性肠病、类风湿性关节炎、组织移植、肿瘤转移和心肌缺血。这些化合物还可以用于治疗多发性硬化等炎症性脑疾病。
• Methods and compositions for treating rheumatoid arthritis
  申请人：Yednock A. Theodore

  公开号：US20050065192A1

  公开（公告）日：2005-03-24

  This application relates to methods and compositions for treating rheumatoid arthritis by administering a combination therapy comprising methotrexate and an antibody to alpha-4 integrin or an immunologically active antigen binding fragment in therapeutically effective amounts. The application also relates generally to methods and compositions for treating rheumatoid arthritis by administering a combination therapy comprising methotrexate and small molecule alpha-4 integrin antagonist that inhibits the alpha-4 integrin (α4 integrin) interaction with VCAM-1. The invention further relates to methods of preparing the compounds and methods of using the compounds and compositions.

  本申请涉及通过以治疗有效剂量给予甲氨蝶呤和α-4整合素抗体或免疫活性抗原结合片段的联合治疗方法和组合物，治疗类风湿性关节炎。该申请还涉及通过以治疗有效剂量给予甲氨蝶呤和小分子α-4整合素拮抗剂的联合治疗方法和组合物，该拮抗剂抑制α-4整合素（α4整合素）与VCAM-1的相互作用，通常涉及制备化合物的方法和使用化合物和组合物的方法。
• IMIDAZOL (1,2-A)PYRIDINES AND RELATED COMPOUNDS WITH ACTIVITY AT CANNABINOID CB2 RECEPTORS
  申请人：Olsson Roger

  公开号：US20110206607A1

  公开（公告）日：2011-08-25

  Disclosed herein are compounds of Formula (I), or a pharmaceutically acceptable salt, ester, amide, thereof; and methods of modulating the activity of a cannabinoid CB2 receptor comprising contacting a compound of Formula I with the cannabinoid CB2 receptor. Also disclosed are methods of imaging of a tissue by positron emission tomography, the method comprising administering to the subject a compound of Formula I, wherein the compound comprises a radioisotope. Also disclosed are methods of measuring the relative concentration of cannabinoid CB2 receptors in tissue of a subject, by using a compound of Formula I which comprises a radioisotope. In addition, method of diagnosing a disorder in a subject are disclosed.

  本文公开了I式化合物，或其药学上可接受的盐、酯、酰胺等；以及调节大麻素CB2受体活性的方法，包括将I式化合物与大麻素CB2受体接触。还公开了通过正电子发射断层扫描成像组织的方法，该方法包括向受试者注射I式化合物，其中该化合物包含放射性同位素。还公开了通过使用含有放射性同位素的I式化合物来测量受试者组织中大麻素CB2受体的相对浓度的方法。此外，还公开了一种诊断受试者疾病的方法。