2,3-Dihydro-2-methyl-1H-2,4-diazainden | 16087-93-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: 2,3-Dihydro-2-methyl-1H-2,4-diazainden
• 英文别名: 6-methyl-6,7-dihydro-5H-pyrrolo[3,4-b]pyridine；6-Methyl-6,7-dihydro-5H-pyrrolo[3,4-b]pyridine；6-methyl-5,7-dihydropyrrolo[3,4-b]pyridine
• CAS: 16087-93-7
• 化学式: C₈H₁₀N₂
• 分子量: 134.181
• InChiKey: RYUNPOCFXODOBT-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：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  16.1
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF BROMODOMAIN-CONTAINING PROTEINS<br/>[FR] COMPOSÉS ET PROCÉDÉS POUR LA DÉGRADATION CIBLÉE DE PROTÉINES CONTENANT UN BROMODOMAINE
  申请人：ARVINAS INC

  公开号：WO2017030814A1

  公开（公告）日：2017-02-23

  The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.

  本发明涉及双功能化合物，其作为靶向泛素化的调节剂具有实用性，特别是根据本发明抑制各种多肽和其他蛋白质的化合物。具体而言，本发明涉及一端含有结合泛素连接酶的VHL配体，另一端含有结合靶蛋白的基团的化合物，使得靶蛋白靠近泛素连接酶以促使该蛋白的降解（和抑制）。根据本发明的化合物表现出与靶向多肽的降解/抑制一致的广泛的药理活性。
• [EN] HIV INTEGRASE INHIBITORS<br/>[FR] INHIBITEURS D'INTÉGRASE DU VIH
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2012078834A1

  公开（公告）日：2012-06-14

  The disclosure generally relates to the novel compounds of formula (I), including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

  该披露通常涉及到式（I）的新化合物，包括它们的盐，这些化合物抑制HIV整合酶并防止病毒整合到人类DNA中。这种作用使得这些化合物对治疗HIV感染和艾滋病有用。该发明还涵盖了用于治疗HIV感染者的药物组合物和方法。
• [EN] DIHYDROPYRIDAZINONES SUBSTITUTED WITH PHENYLUREAS<br/>[FR] DIHYDROPYRIDAZINONES SUBSTITUÉES PAR DES PHÉNYLURÉES
  申请人：BAYER PHARMA AG

  公开号：WO2018086703A1

  公开（公告）日：2018-05-17

  Compounds of formula (I) which are nicotinamide phosphoribosyltransferase (NAMPT) inhibitors and their use for the treatment of hyperproloferative diseases and/or disorders responsive to induction of cell death.

  式（I）的化合物是烟酰胺磷酸核糖转移酶（NAMPT）抑制剂，可用于治疗对诱导细胞死亡敏感的增生性疾病和/或紊乱。
• GLYCINE COMPOUND
  申请人：Yoshihara Kousei

  公开号：US20120184520A1

  公开（公告）日：2012-07-19

  [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that a compound of the present invention or a salt thereof exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. The present invention further relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound of the present invention or a salt thereof, and an excipient.

  本发明提供了一种化合物，该化合物可用作药物组合物的活性成分，特别是用于预防和/或治疗与VAP-1相关的疾病的药物组合物。 本发明的解决方案是，本发明者对具有VAP-1抑制活性的化合物进行了深入研究，结果发现本发明的化合物或其盐表现出优异的VAP-1抑制活性，并且对于预防和/或治疗与VAP-1相关的疾病，特别是糖尿病肾病或糖尿病黄斑水肿，具有用处，从而完成了本发明。本发明还涉及一种药物组合物，特别是用于预防和/或治疗与VAP-1相关的疾病的药物组合物，其包括本发明的化合物或其盐以及赋形剂。
• 8-AZABICYCLO[3.2.1]OCTANE-8-CARBOXAMIDE DERIVATIVE
  申请人：Horiuchi Yoshihiro

  公开号：US20120225876A1

  公开（公告）日：2012-09-06

  Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof (In the formula, A represents a group that is represented by formula (A-1); R 1a and R 1b may be the same or different and each independently represents a C 1-6 alkyl group which may be substituted by one to three halogen atoms; m and n each independently represents an integer of 0-5; X 1 represents a hydroxyl group or an aminocarbonyl group; Z 1 represents a single bond or the like; and R 2 represents an optionally substituted C 1-6 alkyl group, an optionally substituted C 6-10 aryl group or the like.)

  公开了一种由公式(1)表示的化合物或其药理可接受的盐(在公式中，A代表由公式(A-1)表示的基团；R1a和R1b可以相同或不同，每个独立地表示一个可以由一个到三个卤素原子取代的C1-6烷基；m和n各自独立地表示0-5之间的整数；X1代表羟基或氨基甲酰基；Z1代表单键等；R2代表一个可选地取代的C1-6烷基，一个可选地取代的C6-10芳基等)。