5-methyl-1-(2-trimethylsilanyl-ethoxymethyl)-1H-imidazole-2-carboxylic acid ethyl ester | 954125-10-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 5-methyl-1-(2-trimethylsilanyl-ethoxymethyl)-1H-imidazole-2-carboxylic acid ethyl ester
• 英文别名: ethyl 5-methyl-1-{[2-(trimethylsilyl)ethoxy]methyl}-1H-imidazole-2-carboxylate；ethyl 5-methyl-1-(2-trimethylsilylethoxymethyl)imidazole-2-carboxylate
• CAS: 954125-10-1
• 化学式: C₁₃H₂₄N₂O₃Si
• 分子量: 284.431
• InChiKey: XLTVNVKCXMHLBC-UHFFFAOYSA-N

物化性质

• 沸点：
  362.1±52.0 °C(Predicted)
• 密度：
  1.03±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.68
• 重原子数：
  19
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.69
• 拓扑面积：
  53.4
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-methyl-1-(2-trimethylsilanyl-ethoxymethyl)-1H-imidazole-2-carboxylic acid ethyl ester 在 氢氧化钾 作用下， 以 乙醇 、 水 为溶剂， 反应 1.0h， 生成 5-methyl-1-(2-trimethylsilanyl-ethoxymethyl)-1H-imidazole-2-carboxylic acid potassium salt
  参考文献：
  名称：

  INHIBITORS OF C-FMS KINASE

  摘要：

  该发明涉及以下式I的化合物：其中Z、X、J、R2和W如规范中所述，以及其溶剂合物、水合物、互变异构体和药用可接受的盐，这些化合物抑制蛋白酪氨酸激酶，特别是c-fms激酶。提供了治疗自身免疫疾病的方法；以及具有炎症成分的疾病；治疗卵巢癌、子宫癌、乳腺癌、结肠癌、胃癌、毛细胞白血病和非小细胞肺癌的转移；以及治疗疼痛，包括肿瘤转移或骨关节炎引起的骨骼疼痛，或内脏、炎症和神经源性疼痛；以及骨质疏松症、Paget病和其他骨吸收导致发病率的疾病，包括关节炎、假体失败、破骨性肉瘤、骨髓瘤和肿瘤转移至骨骼的方法，使用式I的化合物也提供了。

  公开号：

  US20070249649A1
• 作为产物：
  描述：

  氰基甲酸乙酯 在 正丁基锂 作用下， 以 四氢呋喃 、 环己烷 为溶剂， 反应 10.5h， 以38%的产率得到5-methyl-1-(2-trimethylsilanyl-ethoxymethyl)-1H-imidazole-2-carboxylic acid ethyl ester
  参考文献：
  名称：

  INHIBITORS OF C-FMS KINASE

  摘要：

  本发明涉及式I化合物：其中Z、X、J、R2和W在说明书中规定，以及抑制蛋白酪氨酸激酶，尤其是c-fms激酶的溶剂化物、水合物、互变异构体和药用盐。治疗自身免疫病；和治疗具有炎症成分的疾病；治疗来自卵巢癌、子宫癌、乳腺癌、前列腺癌、肺癌、结肠癌、胃癌、毛细胞白血病的转移；和治疗疼痛，包括由肿瘤转移或骨关节炎引起的骨骼疼痛，或内脏、炎症性和神经性疼痛；以及骨质疏松症、佩吉特病，以及骨吸收介导病状的其它疾病，包括类风湿性关节炎、其它形式的炎症性关节炎、骨关节炎、假体失败、溶骨肉瘤、骨髓瘤和骨转移瘤，也提供了式I化合物。

  公开号：

  US20070249593A1

文献信息

• Inhibitors of C-FMS Kinase
  申请人：Illig Carl R.

  公开号：US20080275031A1

  公开（公告）日：2008-11-06

  The invention is directed to compounds of Formula I: wherein Z, X, J, R 2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

  本发明涉及公式I的化合物：其中Z，X，J，R2和W在规范中设置，以及其溶剂化物，水合物，互变异构体和药学上可接受的盐，该化合物抑制蛋白酪氨酸激酶，特别是c-fms激酶。本发明还提供了使用公式I化合物治疗自身免疫性疾病和具有炎症成分的疾病的方法；治疗卵巢癌，子宫癌，乳腺癌，前列腺癌，肺癌，结肠癌，胃癌，毛细胞白血病的转移；以及治疗疼痛，包括由肿瘤转移或骨关节炎引起的骨骼疼痛，或脏器，炎症和神经源性疼痛；以及骨质疏松症，帕吉特氏病和其他骨吸收介导发病率的疾病，包括类风湿性关节炎和其他形式的炎性关节炎，骨关节炎，假体失败，骨溶性肉瘤，骨髓瘤和肿瘤转移至骨骼的公式I化合物。
• Inhibitors of c-fms kinase
  申请人：Janssen Pharmaceutica, N.V.

  公开号：US07414050B2

  公开（公告）日：2008-08-19

  The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

  本发明涉及一类式I的化合物：其中Z、X、J、R2和W在规范中列出，以及其溶剂化物、水合物、互变异构体和药学上可接受的盐，该化合物抑制蛋白酪氨酸激酶，特别是c-fms激酶。本发明还提供了使用式I化合物治疗自身免疫性疾病和具有炎症成分的疾病；治疗卵巢癌、子宫癌、乳腺癌、前列腺癌、肺癌、结肠癌、胃癌、毛细胞白血病引起的转移；以及治疗疼痛，包括肿瘤转移或骨关节炎引起的骨骼疼痛，或内脏、炎症和神经性疼痛；以及骨质疏松症、帕吉特病和其他骨吸收介导的疾病，包括类风湿性关节炎和其他形式的炎症性关节炎、骨关节炎、假体失效、骨溶性肉瘤、骨髓瘤和转移至骨骼的肿瘤。
• Inhibitors of C-FMS kinase
  申请人：Janssen Pharmaceutica, N.V.

  公开号：US07973035B2

  公开（公告）日：2011-07-05

  The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

  本发明涉及式I的化合物：其中Z、X、J、R2和W在规范中列出，以及其溶剂化物、水合物、互变异构体和药学上可接受的盐，其抑制蛋白酪氨酸激酶，尤其是c-fms激酶。本发明还提供了使用式I化合物治疗自身免疫性疾病和带有炎症成分的疾病的方法；治疗卵巢癌、子宫癌、乳腺癌、前列腺癌、肺癌、结肠癌、胃癌、毛细胞白血病的转移；以及治疗疼痛，包括肿瘤转移或骨关节炎引起的骨骼疼痛，或内脏、炎症和神经源性疼痛；以及骨质疏松症、帕吉特病和其他骨吸收介导的疾病，包括类风湿性关节炎和其他形式的炎症性关节炎、骨关节炎、假体失效、骨溶性肉瘤、骨髓瘤和转移至骨骼的肿瘤。
• [EN] CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF<br/>[FR] MODULATEURS DE CALPAIN ET LEURS UTILISATIONS THÉRAPEUTIQUES
  申请人：BLADE THERAPEUTICS INC

  公开号：WO2018064119A8

  公开（公告）日：2019-04-25
• IMIDAZOLE CARBONYL COMPOUND
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP2226322B1

  公开（公告）日：2015-01-21