3-(Aminomethyl)-5-methylpyridin-2-amine | 1173998-64-5

• 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: 3-(Aminomethyl)-5-methylpyridin-2-amine
• CAS: 1173998-64-5
• 化学式: C₇H₁₁N₃
• 分子量: 137.184
• InChiKey: IKBGMCCWUSQWNT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 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：
  64.9
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-(Aminomethyl)-5-methylpyridin-2-amine 、 硫代异氰酸苯酯 在 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 生成
  参考文献：
  名称：

  Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2)

  摘要：

  Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas are described as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). These compounds demonstrate potent in vitro activity against the enzyme with IC50 values as low as 15 nM, and suppress expression of TNF alpha in THP-1 cells and in vivo in an acute inflammation model in mice. The synthesis, structure-activity relationship (SAR), and biological evaluation of these compounds are discussed. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.04.088

文献信息

• [EN] SUBSTITUTED PYRIDINE DERIVATIVES AS FABI INHIBITORS<br/>[FR] DÉRIVÉS DE PYRIDINE SUBSTITUÉS EN TANT QU'INHIBITEURS DE FABI
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2013080222A1

  公开（公告）日：2013-06-06

  The present invention provides substituted pyridine derivatives of formula (I), which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors. Formula(I) in which R1 to R5 and L have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage anti-bacterial agents, more particularly FabI inhibitors. The present invention also provides methods for synthesizing and administering the FabI inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明提供了式(I)的取代吡啶衍生物，其可能作为抗细菌剂，特别是FabI抑制剂，具有治疗用途。式(I)中，R1至R5和L具有说明书中给出的含义，以及用于治疗和预防疾病或失调的药用可接受盐，特别是在有优势使用抗细菌剂，尤其是FabI抑制剂的疾病或失调中的用途。本发明还提供了合成和管理FabI抑制剂化合物的方法。本发明还提供了包含至少一种FabI抑制剂化合物和用于其的药用可接受载体、稀释剂或助剂的药物制剂。
• N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
  申请人：Hanney Barbara

  公开号：US20070225229A1

  公开（公告）日：2007-09-27

  Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

  结构式I的化合物以组织选择性的方式调节雄激素受体（AR）。这些化合物对于增强肌肉张力的作用和治疗由雄激素缺乏引起或可以通过雄激素治疗改善的疾病（包括骨质疏松症、骨质疏松、糖皮质激素诱导的骨质疏松症、牙周病、骨折、骨重建手术后的骨损伤、肌肉萎缩、虚弱、老化皮肤、男性性腺功能减退、女性绝经后症状、动脉硬化、高胆固醇血症、高脂血症、肥胖症、再生障碍性贫血和其他造血系统疾病、炎性关节炎和关节修复、艾滋病浪费综合症、前列腺癌、良性前列腺增生、腹部脂肪堆积、代谢综合征、2型糖尿病、癌症消瘦、阿尔茨海默病、肌肉萎缩症、认知能力下降、性功能障碍、睡眠呼吸暂停、抑郁症、早发性卵巢功能衰竭和自身免疫性疾病等）具有用途，可以单独使用或与其他活性剂联合使用。
• US7268153B2
  申请人：——

  公开号：US7268153B2

  公开（公告）日：2007-09-11
• US7763659B2
  申请人：——

  公开号：US7763659B2

  公开（公告）日：2010-07-27
• Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2)
  作者：Songnian Lin、Matthew Lombardo、Sunita Malkani、Jeffrey J. Hale、Sander G. Mills、Kevin Chapman、James E. Thompson、Wen Xiao Zhang、Ruixiu Wang、Rose M. Cubbon、Edward A. O’Neill、Silvi Luell、Ester Carballo-Jane、Lihu Yang

  DOI：10.1016/j.bmcl.2009.04.088

  日期：2009.6

  Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas are described as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). These compounds demonstrate potent in vitro activity against the enzyme with IC50 values as low as 15 nM, and suppress expression of TNF alpha in THP-1 cells and in vivo in an acute inflammation model in mice. The synthesis, structure-activity relationship (SAR), and biological evaluation of these compounds are discussed. (C) 2009 Elsevier Ltd. All rights reserved.