4-[3-(ethyl-methyl-amino)-propyl]-2-(4-methyl-piperidin-1-yl)-phenylamine | 954424-89-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 4-[3-(ethyl-methyl-amino)-propyl]-2-(4-methyl-piperidin-1-yl)-phenylamine
• 英文别名: 4-[3-[ethyl(methyl)amino]propyl]-2-(4-methylpiperidin-1-yl)aniline
• CAS: 954424-89-6
• 化学式: C₁₈H₃₁N₃
• 分子量: 289.464
• InChiKey: AOLFZWKFQRTJEC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  21
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  32.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-cyanofuran-2-carbonyl chloride 、 4-[3-(ethyl-methyl-amino)-propyl]-2-(4-methyl-piperidin-1-yl)-phenylamine 在 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 以45%的产率得到5-Cyano-furan-2-carboxylic acid [4-[3-(ethyl-methyl-amino)-propyl]-2-(4-methyl-piperidin-1-yl)-phenyl]-amide
  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

文献信息

• CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTICS DELIVERY
  申请人：Cheng Jianjun

  公开号：US20120283214A1

  公开（公告）日：2012-11-08

  The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

  本发明涉及一种新型治疗环糊精含聚合物组合物，设计为小分子治疗药物输送的载体及其制药组合物。这些含环糊精的聚合物改善了药物的稳定性和溶解性，并在体内使用时减少了小分子治疗药物的毒性。此外，通过从各种连接剂和靶向配体中选择，这些聚合物提供了治疗剂的可控释放方法。本发明还涉及使用上述治疗组合物治疗主体的方法。本发明还涉及用于制造、许可或分发包含或涉及上述聚合物的工具包的制药业务方法。
• Inhibitors of C-FMS kinase
  申请人：Illig Carl R.

  公开号：US08674100B2

  公开（公告）日：2014-03-18

  The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are as 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. The compounds of formula I are useful for treating a variety of disorders including autoimmune diseases such as rheumatoid arthritis, multiple sclerosis and psoriasis.

  本发明涉及I式化合物：其中Z，X，J，R2和W如规范所述，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。I式化合物对于治疗多种疾病包括自身免疫性疾病如类风湿性关节炎，多发性硬化症和牛皮癣等非常有用。
• Inhibitors of c-fms kinase
  申请人：Janssen Pharmaceutica NV

  公开号：US09221797B2

  公开（公告）日：2015-12-29

  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, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; 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 arthritis, 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在规范中说明，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的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、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，或者内脏、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：EP2687516A1

  公开（公告）日：2014-01-22

  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, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; 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 arthritis, 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如说明书所述，以及它们的溶解物、水合物、同系物和药学上可接受的盐，可抑制蛋白酪氨酸激酶，特别是c-fms激酶。治疗自身免疫性疾病的方法；治疗具有炎症成分的疾病的方法；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肺癌转移的方法；治疗疼痛的方法，包括由肿瘤转移或骨关节炎引起的骨骼疼痛，或内脏疼痛、炎症疼痛和神经源性疼痛；以及骨质疏松症、Paget 病和其他骨吸收介导发病的疾病，包括关节炎、假体失效、溶骨性肉瘤、骨髓瘤和肿瘤向骨骼转移，也提供了式 I 化合物。
• US8674100B2
  申请人：——

  公开号：US8674100B2

  公开（公告）日：2014-03-18