8,8-dioxo-8λ⁶-thia-bicyclo[3.2.1]octan-3-one | 19677-50-0

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 8,8-dioxo-8λ⁶-thia-bicyclo[3.2.1]octan-3-one
• 英文别名: 8lambda6-Thiabicyclo[3.2.1]octane-3,8,8-trione；8,8-dioxo-8λ6-thiabicyclo[3.2.1]octan-3-one
• CAS: 19677-50-0
• 化学式: C₇H₁₀O₃S
• 分子量: 174.221
• InChiKey: FDQGOPRXAOUROX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  59.6
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• INHIBITORS OF C-FMS KINASE
  申请人：Illig Carl R.

  公开号：US20070249680A1

  公开（公告）日：2007-10-25

  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.

  本发明涉及式I化合物：其中Z、X、J、R2和W如规范中所述，以及其溶剂化物、水合物、互变异构体和药学上可接受的盐，其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、骨髓瘤和肿瘤转移至骨骼。
• US8859602B2
  申请人：——

  公开号：US8859602B2

  公开（公告）日：2014-10-14
• US9394289B2
  申请人：——

  公开号：US9394289B2

  公开（公告）日：2016-07-19
• [EN] INHIBITORS OF C-FMS KINASE<br/>[FR] INHIBITEURS DE LA C-FMS KINASE
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2007124319A1

  公开（公告）日：2007-11-01

  [EN] 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.
  [FR] L'invention porte sur des composés de formule (I) dans laquelle Z, X, J, R2 et W sont tels que définis dans la description, ainsi que sur des solvates, des hydrates, des tautomères et des sels de ceux-ci acceptables d'un point de vue pharmaceutique qui inhibent des protéines tyrosine kinases, notamment la c-fms kinase. L'invention porte également sur des méthodes de traitement de maladies auto-immunes, et de maladies ayant une composante inflammatoire; sur des méthodes de traitement de la métastase du cancer des ovaires, du cancer utérin, du cancer du sein, du cancer du côlon, du cancer de l'estomac, de la leucémie à tricholeucocytes, de l'épithélioma du poumon à grandes cellules; et sur des méthodes de traitement de la douleur, y compris la douleur osseuse provoquée par la métastase tumorale ou l'ostéoarthrite ou la douleur viscérale, inflammatoire et neurogénique. Ces méthodes permettent de traiter également l'ostéoporose, la maladie de Paget et d'autres maladies dans lesquelles la résorption osseuse induit une morbidité, telles que l'arthrite, la défaillance de prothèse, l'ostéosarcome, le myélome et la métastase tumorale sur l'os, ces méthodes utilisant les composés de formule (I) de l'invention.