4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridin-3-ol | 1093759-88-6

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridin-3-ol
• 英文别名: 1,2,4,5,6,7-hexahydropyrazolo[4,3-c]pyridin-3-one
• CAS: 1093759-88-6
• 化学式: C₆H₉N₃O
• mdl: MFCD11501667
• 分子量: 139.16
• InChiKey: AMUAVKXIRPMUBN-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：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  53.2
• 氢给体数：
  3
• 氢受体数：
  3

文献信息

• [EN] QUINOXALINE COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS À BASE DE QUINOXALINE ET LEURS UTILISATIONS
  申请人：MILLENNIUM PHARM INC

  公开号：WO2015161142A1

  公开（公告）日：2015-10-22

  This invention provides compounds of formula I and subsets thereof: wherein T, J, R, R4, Rq, o, RA, and RB and subsets thereof are as described in the specification. The compounds are inhibitors of NAMPT and are thus useful for treating cancer, inflammatory conditions, or T-cell mediated autoimmune disease.

  这项发明提供了公式I及其子集的化合物：其中T、J、R、R4、Rq、o、RA和RB以及其子集如规范中所述。这些化合物是NAMPT的抑制剂，因此可用于治疗癌症、炎症性疾病或T细胞介导的自身免疫疾病。
• [EN] INHIBITORS OF ARGINASE AND THEIR THERAPEUTIC APPLICATIONS<br/>[FR] INHIBITEURS D'ARGINASE ET LEURS APPLICATIONS THÉRAPEUTIQUES
  申请人：MARS INC

  公开号：WO2011133653A1

  公开（公告）日：2011-10-27

  Compounds according to Formula I and Formula II are potent inhibitors of Arginase I and II activity : Formule (I), (II) where R1, R2, R3, R4, R5, R6, R7, R8, R9, D, M, X, and Y are defined as set forth in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use for treating or preventing a disease or a condition associated with arginase activity.

  根据式I和式II，化合物是Arginase I和II活性的强效抑制剂：式(I)，(II)中的R1、R2、R3、R4、R5、R6、R7、R8、R9、D、M、X和Y的定义如规范所述。该发明还提供了这些化合物的药物组合物以及它们用于治疗或预防与Arginase活性相关的疾病或病况的方法。
• [EN] CCR5 MODULATORS FOR TREATING HIV<br/>[FR] MODULATEURS CCR5 POUR TRAITER LE VIH
  申请人：PURDUE RESEARCH FOUNDATION

  公开号：WO2011116287A1

  公开（公告）日：2011-09-22

  Compounds that modulate the CCR5 chemokine receptor, pharmaceutical compositions containing them, and uses therefor in the treatment of HIV and related diseases are described.

  本文描述了调节CCR5趋化因子受体的化合物、包含它们的制药组合物以及在治疗HIV和相关疾病方面的用途。
• INHIBITORS OF ARGINASE AND THEIR THERAPEUTIC APPLICATIONS
  申请人：Van Zandt Michael

  公开号：US20120083469A1

  公开（公告）日：2012-04-05

  Compounds according to Formula I and Formula II are potent inhibitors of Arginase I and II activity: where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , D, M, X, and Y are defined as set forth in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use for treating or preventing a disease or a condition associated with arginase activity.

  根据公式I和公式II的化合物是Arginase I和II活性的有效抑制剂：其中R1，R2，R3，R4，R5，R6，R7，R8，R9，D，M，X和Y的定义如规范中所述。该发明还提供了这些化合物的制药组合物和使用它们治疗或预防与Arginase活性相关的疾病或病况的方法。
• CYCLIC COMPOUNDS
  申请人：TANABE SEIYAKU CO., LTD.

  公开号：EP1277741A1

  公开（公告）日：2003-01-22

  1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof,    wherein X is =CH-or=N-, Y is-NH-, -NR4-, -S-, - O-, -CH=N-, -N=CH-, -N=N-, -CH=CH-, etc., R1 is a lower alkoxy group, an amino group, a heterocyclic ring containing N atom(s), or a hydroxy group substituted by a heterocyclic ring containing N atom(s) (each of which is optionally substituted), R2 is a lower alkylamino group which is optionally substituted by an aryl group, a lower alkoxy group which is optionally substituted by an aryl group, a lower alkoxy group substituted by an aromatic heterocyclic ring containing N atom(s), R3 is an aryl group, a heterocyclic ring containing N atom(s), a lower alkyl group, a lower alkoxy group, a cyclo lower alkoxy group, a hydroxy group substituted by a heterocyclic ring containing N atom(s), or an amino group (each of which is optionally substituted), and R3 and a substituent in Y may be combined to form a lactone ring.    The compound of the present invention has excellent selective PDE V inhibitory activity and therefore, is useful as a therapeutic or prophylactic drug for treating various diseases due to functional disorders on cGMP-signaling.

  1.式（I）的环状化合物或其药理学上可接受的盐、 其中 X 是 =CH-or=N-, Y 是-NH-、-NR4-、-S-、-O-、-CH=N-、-N=CH-、-N=N-、-CH=CH-等、R1 是低级烷氧基、氨基、含 N 原子的杂环或被含 N 原子的杂环取代的羟基（其中每一个都可选择被取代）， R2 是低级烷基氨基，可选择被芳基取代，低级烷氧基，可选择被芳基取代、R3 是芳基、含 N 原子的杂环、低级烷基、低级烷氧基、环低级烷氧基、被含 N 原子的杂环取代的羟基或氨基（其中每个基团都可选择被取代），R3 和 Y 中的一个取代基可结合形成一个内酯环。 本发明的化合物具有优异的选择性 PDE V 抑制活性，因此可用作治疗或预防药物，用于治疗因 cGMP 信号转导功能紊乱而引起的各种疾病。