4-Methyl-isochinolin-3-ol | 7697-67-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 英文名称: 4-Methyl-isochinolin-3-ol
• 英文别名: 4-methylisoquinolin-3-ol；3(2H)-Isoquinolinone, 4-methyl-；4-methyl-2H-isoquinolin-3-one
• CAS: 7697-67-8
• 化学式: C₁₀H₉NO
• 分子量: 159.188
• InChiKey: QRWCYONTZZFFJZ-UHFFFAOYSA-N

物化性质

• 沸点：
  507.3±23.0 °C(Predicted)
• 密度：
  1.18±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  1

安全信息

• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

反应信息

• 作为反应物：
  描述：

  4-Methyl-isochinolin-3-ol 、 甲基丙烯酸甲酯 以 甲苯 为溶剂， 反应 48.0h， 生成 、
  参考文献：
  名称：

  Tricyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof

  摘要：

  提供了一种新型的非甾体化合物，可用于治疗与糖皮质激素受体、AP-1和/或NF-κB活性调节相关的疾病，包括肥胖、糖尿病、炎症和免疫性疾病，并具有以下结构的化学式（I）或其立体异构体或前药或其药用可接受盐，其中B、J、K、Z、R、Ra、Rb、Rc、Rd、Rq、Rw、m和n在此处被定义。还提供了包含所述化合物的药物组合物和治疗肥胖、糖尿病以及炎症或免疫相关疾病的方法。

  公开号：

  US20050187242A1
• 作为产物：
  描述：

  N-苄基-2-氧丙酰胺 在 硫酸 、 氨 作用下， 以 水 为溶剂， 反应 3.0h， 以77%的产率得到4-Methyl-isochinolin-3-ol
  参考文献：
  名称：

  Tricyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof

  摘要：

  提供了一种新型的非甾体化合物，可用于治疗与糖皮质激素受体、AP-1和/或NF-κB活性调节相关的疾病，包括肥胖、糖尿病、炎症和免疫性疾病，并具有以下结构的化学式（I）或其立体异构体或前药或其药用可接受盐，其中B、J、K、Z、R、Ra、Rb、Rc、Rd、Rq、Rw、m和n在此处被定义。还提供了包含所述化合物的药物组合物和治疗肥胖、糖尿病以及炎症或免疫相关疾病的方法。

  公开号：

  US20050187242A1

文献信息

• 2-AMINOPYRIDINE KINASE INHIBITORS
  申请人：Steinig Arno G.

  公开号：US20090197862A1

  公开（公告）日：2009-08-06

  2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The present invention is further directed to a method of treating a patient having a condition which is mediated by protein kinase activity by administering to the patient a therapeutically effective amount of the above-mentioned pharmaceutical composition.

  具有Formula I结构的2-氨基吡啶化合物，以及这些化合物的药用可接受的盐。Formula I的化合物抑制动物（包括人类）中的酪氨酸激酶酶活性，并可用于治疗和/或预防各种疾病和病况。特别地，本文披露的化合物是激酶抑制剂，特别是但不限于KDR、Tie-2、Flt3、FGFR3、Ab1、Aurora A、c-Src、IGF-1R、ALK、c-MET、RON、PAK1、PAK2和TAK1，并可用于治疗增生性疾病，如但不限于癌症。本发明还涉及一种包含Formula I化合物的药物组合物，或其药用可接受的盐，以及药用可接受的载体的药物组合物。本发明还涉及一种通过向患有由蛋白激酶活性介导的病症的患者投与上述药物组合物的治疗方法。
• [EN] HETEROCYCLIC MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kappaB ACTIVITY AND USE THEREOF<br/>[FR] MODULATEURS HETEROCYCLIQUES DU RECEPTEUR GLUCOCORTICOIDE AP-1, ET/OU ACTIVITE NF-20050811US5569655ADORITY JR JOHN A [US], et al19961029AASee references of EP 1711488A4
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2005073221A1

  公开（公告）日：2005-08-11

  Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of Formula (I) or stereoisomers or prodrugs or solvates or pharmaceutically acceptable salts thereof, wherein A, B, J, K, Z, R, Ra, Rb, Rc, and Rd, are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.

  提供了一种新型的非甾体化合物，可用于治疗与糖皮质激素受体、AP-1和/或NF-κB活性调节相关的疾病，包括肥胖、糖尿病、炎症和免疫性疾病，并具有如下结构的化学式（I）或其立体异构体、前药、溶剂合物或其药用可接受的盐，其中A、B、J、K、Z、R、Ra、Rb、Rc和Rd在此有所定义。还提供了包含该化合物的药物组合物和治疗肥胖、糖尿病以及炎症或免疫相关疾病的方法。
• 2-aminopyridine kinase inhibitors
  申请人：OSI Pharmaceuticals, LLC

  公开号：US08178668B2

  公开（公告）日：2012-05-15

  2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The present invention is further directed to a method of treating a patient having a condition which is mediated by protein kinase activity by administering to the patient a therapeutically effective amount of the above-mentioned pharmaceutical composition.

  具有I式结构的2-氨基吡啶化合物，以及这些化合物的药学上可接受的盐。I式化合物抑制动物（包括人类）中的酪氨酸激酶酶活性，并在治疗和/或预防各种疾病和病况方面有用。特别地，本文披露的化合物是激酶抑制剂，特别是但不限于KDR，Tie-2，Flt3，FGFR3，Ab1，Aurora A，c-Src，IGF-1R，ALK，c-MET，RON，PAK1，PAK2和TAK1，并可用于治疗增殖性疾病，例如但不限于癌症。本发明还涉及一种制备药物组合物的方法，该组合物包括I式化合物或其药学上可接受的盐的治疗有效量以及药学上可接受的载体。本发明还涉及一种通过向患有蛋白激酶活性介导的病症的患者投与上述药物组合物的治疗方法。
• TRICYCLIC MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF
  申请人：Weinstein S. David

  公开号：US20070270453A1

  公开（公告）日：2007-11-22

  Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein B, J, K, Z, R, R a , R b , R c , R d , R q , R w , m and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
• US7253283B2
  申请人：——

  公开号：US7253283B2

  公开（公告）日：2007-08-07