4,5-Dimethyl-2H-pyridazin-3-one | 4591-71-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 4,5-Dimethyl-2H-pyridazin-3-one
• 英文别名: 4,5-Dimethylpyridazin-3(2h)-one；4,5-dimethyl-1H-pyridazin-6-one
• CAS: 4591-71-3
• 化学式: C₆H₈N₂O
• 分子量: 124.142
• InChiKey: FKRUSEKREOFROB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  41.5
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] PYRIDAZINONE DERIVATIVES AS PARP INHIBITORS<br/>[FR] DERIVÉS DE PYRIDAZINONE INHIBITEURS DE LA PARP
  申请人：ANGELETTI P IST RICHERCHE BIO

  公开号：WO2009063244A1

  公开（公告）日：2009-05-22

  The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinaldamage, skin senescence and UV-induced skin damage, and as chemo-or radiosensitizers for cancer treatment.

  本发明涉及式(I)化合物及其药用可接受的盐或互变异构体，它们是聚(ADP-核糖)聚合酶（PARP）的抑制剂，因此可用于治疗癌症、炎症性疾病、再灌注损伤、缺血情况、中风、肾衰竭、心血管疾病、非心血管疾病的血管疾病、糖尿病、神经退行性疾病、逆转录病毒感染、视网膜损伤、皮肤老化和紫外线诱导的皮肤损伤，并用作癌症治疗的化疗或放射敏化剂。
• DIARYLPYRIDAZINONE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF FOR THE TREATMENT OF HUMANS
  申请人：Dupont-Passelaigue Elisabeth

  公开号：US20130267520A1

  公开（公告）日：2013-10-10

  The present invention relates to diarylpyridazinone derivatives that block the potassium Kv channels (specifically the Kv1.5, Kv4.3, and Kv11.1 channels) and to the use thereof for the treatment of humans. Said compounds have the general formula (I), where R 1 and R 2 are simultaneously or independently one or more groupings such as: halogen, such as F, Br, Cl, a straight or branched C 1 -C 4 alkyl, hydroxy, a straight or branched C 1 -C 4 alkoxy, arylsulfonamido, in which the aryl is optionally replaced with a straight or branched C 1 -C 4 alkyl, or nitrile, as well as the various enantiomers and the mixtures thereof in any proportion, and the pharmaceutically acceptable salts thereof.

  本发明涉及一种阻断钾Kv通道（具体是Kv1.5、Kv4.3和Kv11.1通道）的二芳基吡啉二酮衍生物，以及其用于治疗人类的用途。所述化合物具有通式（I），其中R1和R2同时或独立地是卤素，如F、Br、Cl，直链或支链的C1-C4烷基，羟基，直链或支链的C1-C4烷氧基，芳基磺酰胺基，其中芳基可选地被直链或支链的C1-C4烷基取代，或腈，以及各种对映体和它们的任何比例的混合物，以及其药学上可接受的盐。
• AZABICYCLIC HETEROCYCLES AS CANNABINOID RECEPTOR MODULATORS
  申请人：Ewing William R.

  公开号：US20100029656A1

  公开（公告）日：2010-02-04

  The present application describes CB-1 inverse agonists according to Formula (I) and (Ia), pharmaceutical compositions comprising at least one compound according to Formula (I) or (Ia), and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula (I) or (Ia), both alone and in combination with one or more additional therapeutic agents. The preferred compounds have the general Formula (Ia), including all prodrugs, pharmaceutically acceptable salts and stereoisomer, thereof, wherein R 1 , R 2 , Ar 1 , Ar 2 are defined herein.

  本申请描述了按照公式（I）和（Ia）的CB-1逆激动剂，包括至少一种按照公式（I）或（Ia）的化合物的制药组合物，以及可选地使用按照公式（I）或（Ia）的化合物和一个或多个其他治疗剂进行治疗的方法，无论是单独使用还是与一个或多个其他治疗剂联合使用。首选化合物具有一般公式（Ia），包括所有前药、药学上可接受的盐和立体异构体，其中R1、R2、Ar1、Ar2在此定义。
• HETEROCYCLIC COMPOUNDS AND EXPANSION AGENTS FOR HEMATOPOIETIC STEM CELLS
  申请人：Nishino Taito

  公开号：US20120128640A1

  公开（公告）日：2012-05-24

  An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells useful for improvement in the efficiency of gene transfer into hematopoietic stem cells for gene therapy useful for treatment of various disorders is provided. An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells containing a compound represented by the formula (I) (wherein X, Y, Z, Ar 1 , R 1 , R 2 , R 3 , R 4 , R 5 , R6 and R 7 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof, which can expand hematopoietic stem cells and/or hematopoietic progenitor cells.

  提供一种用于改善基因治疗中将基因转移至造血干细胞以治疗各种疾病的血液干细胞和/或造血祖细胞扩张剂。该扩张剂包含由式(I)表示的化合物（其中X、Y、Z、Ar1、R1、R2、R3、R4、R5、R6和R7如描述中所定义）、该化合物的互变异构体、前药或药学上可接受的盐或其溶剂，能够扩张血液干细胞和/或造血祖细胞。
• HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS
  申请人：PFIZER INC.

  公开号：US20150196561A1

  公开（公告）日：2015-07-16

  The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), age-related cognitive decline, dementia, and Parkinson's disease.

  本发明部分提供了I式化合物及其药物可接受的盐；制备过程；用于制备的中间体；以及包含这些化合物或盐的组合物，以及它们用于治疗D1介导（或D1相关）疾病的用途，包括例如：精神分裂症（例如其认知和负性症状），认知障碍（例如与精神分裂症、AD、PD或药物治疗相关的认知障碍），年龄相关的认知衰退、痴呆和帕金森病。