N-hydroxyethyl-2-pyridone | 70987-71-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: N-hydroxyethyl-2-pyridone
• 英文别名: 1-(hydroxy-ethyl)-1H-pyridin-2-one；Pyridonyl-ethanol；1-(1-hydroxyethyl)pyridin-2-one
• CAS: 70987-71-2
• 化学式: C₇H₉NO₂
• 分子量: 139.154
• InChiKey: PJRLEMXBQBKRPG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  40.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  ethyl 2-(2-oxopyridin-1(2H)-yl)acetate 在 锂硼氢 作用下， 以 1,4-二氧六环 、 水 、 乙酸乙酯 为溶剂， 以41%的产率得到N-hydroxyethyl-2-pyridone
  参考文献：
  名称：

  Substituted vinyl pyridine derivative and drugs containing the same

  摘要：

  本发明涉及一种由以下式（1）表示的取代乙烯吡啶衍生物：##STR1##（其中R.sup.1代表氢原子、烷基等，R.sup.2代表烷基；R.sup.3和R.sup.4中的一个，二者不同，代表氢原子，另一个代表腈基，R.sup.5代表芳基或杂环芳基，X代表氧原子等，Q.sup.1、Q.sup.2和Q.sup.3中的一个代表氮原子，另外两个代表CH）；该衍生物的盐；以及含有该衍生物或盐作为活性成分的药物。由于具有强烈的PDE抑制作用和TNF-α产生抑制作用，该衍生物、盐和药物对于预防和治疗各种炎症性疾病和自身免疫性疾病非常有用。

  公开号：

  US05935977A1

文献信息

• Heterocyclic Compounds For Preventing And Treating Disorders Associated With Excessive Bone Loss
  申请人：Ono Mitsunori

  公开号：US20080058297A1

  公开（公告）日：2008-03-06

  This invention relates to pyrimidine compounds of formula (I), formula (I′), and formula (I″): and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , U, V, W, X, Y, Z, and n are defined herein. This invention also relates to compositions comprising these compounds and methods for using them. The compounds and compositions of this invention are useful to treat or prevent disorders associated with excessive bone loss, including, without limitation periodontal disease, non-malignant bone disorders (such as osteoporosis, Pagers-disease of bone, osteogenesis imperfecta, fibrous dysplasia, and primary hyperparathyroidism) estrogen deficiency, inflammatory bone loss, bone malignancy, arthritis, osteopetrosis, and certain cancer-related disorders (such as hypercalcemia of malignancy (HCM), osteolytic bone lesions of multiple myeloma and osteolytic bone metastases of breast cancer and other metastatic cancers).

  本发明涉及式(I)、式(I′)和式(I″)的嘧啶化合物，以及其药学上可接受的盐、溶剂合物、包合物和前药，其中R1、R2、R3、R4、R5、U、V、W、X、Y、Z和n在此处有定义。本发明还涉及包含这些化合物的组合物和使用它们的方法。本发明的化合物和组合物可用于治疗或预防与骨量过度流失相关的疾病，包括但不限于牙周病、非恶性骨疾病（如骨质疏松症、帕格氏骨病、遗传性骨发育不全、纤维性骨发育不良和原发性甲状旁腺功能亢进症）、雌激素缺乏、炎症性骨流失、骨恶性肿瘤、关节炎、骨质增生症以及某些与癌症相关的疾病（如恶性高钙血症、多发性骨髓瘤的溶骨性骨病变和乳腺癌及其他转移癌的溶骨性骨转移）。
• HETEROCYCLIC COMPOUNDS FOR PREVENTING AND TREATING DISORDERS ASSOCIATED WITH EXCESSIVE BONE LOSS
  申请人：Ono Mitsunori

  公开号：US20100120722A1

  公开（公告）日：2010-05-13

  This invention relates to pyrimidine compounds of formula (I), formula (I′), and formula (I″): and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , U, V, W, X, Y, Z, and n are defined herein. This invention also relates to compositions comprising these compounds and methods for using them. The compounds and compositions of this invention are useful to treat or prevent disorders associated with excessive bone loss, including, without limitation periodontal disease, non-malignant bone disorders (such as osteoporosis, Pagers-disease of bone, osteogenesis imperfecta, fibrous dysplasia, and primary hyperparathyroidism) estrogen deficiency, inflammatory bone loss, bone malignancy, arthritis, osteopetrosis, and certain cancer-related disorders (such as hypercalcemia of malignancy (HCM), osteolytic bone lesions of multiple myeloma and osteolytic bone metastases of breast cancer and other metastatic cancers).

  本发明涉及式(I)、式(I′)和式(I″)的嘧啶化合物，以及其药学上可接受的盐、溶剂化合物、笼合物和前药，其中R1、R2、R3、R4、R5、U、V、W、X、Y、Z和n在此被定义。本发明还涉及包含这些化合物的组合物和使用它们的方法。本发明的化合物和组合物可用于治疗或预防与过度骨质流失相关的疾病，包括但不限于牙周病、非恶性骨疾病（如骨质疏松症、骨的Pagers病、不完全性骨发育不良、纤维性骨发育异常和原发性甲状旁腺功能亢进症）、雌激素缺乏、炎症性骨流失、骨恶性肿瘤、关节炎、骨质硬化和某些与癌症相关的疾病（如恶性高钙血症（HCM）、多发性骨髓瘤的溶骨性骨病变和乳腺癌和其他转移性癌症的溶骨性骨转移）。
• Pyrimidine compounds
  申请人：——

  公开号：US20040024206A1

  公开（公告）日：2004-02-05

  This invention features pyrimidine compounds of formula (I): 1 R 1 is 2 , in which one of R a and R b is H or alkyl, and the other is aryl or heteroaryl optionally substituted with R d and R e m ; each of R 2 and R 4 is H; R 3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R 5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NR c ; Y is covalent bond, CH 2 , C(O), C═N—R c , C═N—OR c , C═N—SR c , O, S, S(O), S(O 2 ), or NR c ; Z is N or CH; one of U and V is N, and the other is CR c ; and W is O, S, S(O), S(O 2 ), NR c , or NC(O)R c ; in which R c is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R d is halogen, CN, alkyl alkyloxy, alkylcarbonyl, alkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, hydroxyalkyl, alkylamino, or alkylaminocarbonyl; R e is halogen, CN, hydroxyl, alkyl, aryl, heteroaryl, alkoxyl, aryloxyl, or heteroaryloxyl; and m is 0, 1, 2, 3, or 4. The pyrimidine compounds can be used to treat an IL-12 overproduction-related disorder (e.g., rheumatoid arthritis, sepsis, Crohn's disease, multiple sclerosis, psoriasis, or insulin-dependent diabetes mellitus).

  本发明涉及式（I）的嘧啶化合物： 其中1R1是2，其中Ra和Rb中的一个是H或烷基，另一个是芳基或杂芳基，可选地被Rd和Rem取代；R2和R4中的每一个都是H；R3是H、烷基、芳基、杂芳基、环烷基、杂环烷基或烷基羰基；R5是H或烷基；n为0、1、2、3、4、5或6；X为NRc；Y为共价键、CH2、C（O）、C≡N—Rc、C≡N—ORc、C≡N—SRc、O、S、S（O）、S（O2）或NRc；Z为N或CH；U和V中的一个是N，另一个是CRc；W为O、S、S（O）、S（O2）、NRc或NC（O）Rc；其中Rc是H、烷基、芳基、杂芳基、环烷基、杂环烷基或烷基羰基；Rd是卤素、CN、烷基氧基、烷基羰基、烷氧基羰基、芳氧基羰基、杂芳氧基羰基、羟基烷基、烷基氨基或烷基氨基羰基；Re是卤素、CN、羟基、烷基、芳基、杂芳基、烷氧基、芳氧基或杂芳氧基；m为0、1、2、3或4。这些嘧啶化合物可用于治疗与IL-12过度产生相关的疾病（例如，类风湿性关节炎、败血症、克罗恩病、多发性硬化症、银屑病或胰岛素依赖性糖尿病）。
• SUBSTITUTED VINYLPYRIDINE DERIVATIVES AND DRUGS CONTAINING THE SAME
  申请人：SS Pharmaceutical Co., Ltd.

  公开号：EP0882714A1

  公开（公告）日：1998-12-09

  The present invention relates to a substituted vinylpyridine derivative represented by the following formula (1): (wherein R1 represents a hydrogen atom, an alkyl group, etc., R2 represents an alkyl group; one of R3 and R4, which are different from each other, represents a hydrogen atom and the other represents a nitrile group, R5 represents an aryl group or a heteroaryl group, X represents an oxygen atom, etc., and one of Q1, Q2, and Q3 represents a nitrogen atom and the other two represent CH); a salt of the derivative; and a drug containing the derivative or salt as the active ingredient. Due to strong PDE inhibitory action and TNF-α production inhibitory action, the derivative, salt, and drug are useful for the prevention and treatment of a wide variety of inflammatory diseases and autoimmune diseases.

  本发明涉及由下式(1)代表的取代乙烯基吡啶衍生物： (其中R1代表氢原子、烷基等，R2代表烷基；R3和R4互不相同，其中一个代表氢原子，另一个代表腈基，R5代表芳基或杂芳基，X代表氧原子等，Q1、Q2和Q3中的一个代表氮原子，另两个代表CH）；该衍生物的盐；以及含有该衍生物或盐作为活性成分的药物。由于具有很强的 PDE 抑制作用和 TNF-α 生成抑制作用，衍生物、盐和药物可用于预防和治疗多种炎症性疾病和自身免疫性疾病。
• Process for the preparation of hydroxybenzoic benzyl esters
  申请人：——

  公开号：US20030053964A1

  公开（公告）日：2003-03-20

  The invention relates to the preparation of hydroxybenzoic benzyl esters by reacting benzyl chloride with hydroxybenzoic acids in the presence of one or more amides.

  本发明涉及在一种或多种酰胺存在下，通过氯化苄与羟基苯甲酸反应制备羟基苯甲酸苄酯。