6-Chlor-3-nitroso-pyridin | 63064-02-8

• 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: 6-Chlor-3-nitroso-pyridin
• 英文别名: 2-Chloro-5-nitrosopyridine
• CAS: 63064-02-8
• 化学式: C₅H₃ClN₂O
• 分子量: 142.545
• InChiKey: SYKAICBPZUNKGR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  42.3
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• SMALL MOLECULE INHIBITORS OF DYRK/CLK AND USES THEREOF
  申请人：Arizona Board of Regents on Behalf of the University of Arizona

  公开号：US20200039989A1

  公开（公告）日：2020-02-06

  This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a 6,5-heterocyclic structure (e.g., compounds having a imidazopyridine, imidazopyrimidine, imidazopyrazine, imidazopyridazine, imidazotriazine, benzoimidazole, benzotriazole, benzoisoxazole, purine, indazole, triazolotriazine, triazolopyridazine, triazolopyrimidine, triazolopyrazine, triazolotetrazine, triazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolopyridazine, pyrazolotriazine, pyrazolopyridine, isoxazolopyrazine, isoxazolopyrimidine, isoxazolopyrdiazine, isoxazolotriazine, or isoxalopyridine structure) which function as inhibitors of DYRK1A, DYRK1B, and Clk-1, and their use as therapeutics for the treatment of Alzheimer's disease, Down syndrome, diabetes, glioblastoma, autoimmune diseases, cancer (e.g., glioblastoma, prostate cancer), inflammatory disorders (e.g., airway inflammation), and other diseases.

  这项发明属于药物化学领域。具体来说，该发明涉及一类新型小分子，具有6,5-杂环结构（例如，具有咪唑吡啶、咪唑吡嘧啶、咪唑吡嗪、咪唑吡啶嗪、咪唑三嗪、苯并咪唑、苯并三唑、苯并异嗪、嘌呤、吲唑、三唑三嗪、三唑吡啶嗪、三唑吡嘧啶、三唑吡嗪、三唑四嗪、三唑吡啶、吡唑吡嗪、吡唑吡嘧啶、吡唑吡啶嗪、吡唑三嗪、吡唑吡啶、异嗪吡嗪、异嗪吡嘧啶、异嗪吡啶嗪、异嗪三嗪、或异嗪吡啶结构），其作为DYRK1A、DYRK1B和Clk-1的抑制剂，以及它们作为治疗阿尔茨海默病、唐氏综合征、糖尿病、胶质母细胞瘤、自身免疫疾病、癌症（例如，胶质母细胞瘤、前列腺癌）、炎症性疾病（例如，气道炎症）和其他疾病的治疗药物的用途。
• HETEROCYCLIC COMPOUNDS
  申请人：GAUL Christoph

  公开号：US20090203688A1

  公开（公告）日：2009-08-13

  The invention relates to compounds of formula I and salts thereof wherein the substituents are as defined in the specification, processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.

  该发明涉及公式I的化合物及其盐，其中取代基如规范中定义，以及其制备方法；含有这种化合物的药物，特别用于在一个或多个蛋白酪氨酸激酶介导的疾病中使用。
• Aminoethylaromatic Compounds Suitable For Treating Disorders That Respond To Modulation Of The Dopamine D3 Receptor
  申请人：Drescher Karla

  公开号：US20080096934A1

  公开（公告）日：2008-04-24

  The present invention relates to aromatic compounds of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical R a and wherein Ar may also carry 1 or 2 radicals R b ; X is N or CH; E is CR 6 R 7 or NR 3 ; R 1 is C 1 -C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C 4 -cycloalkylmethyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, fluorinated C 3 -C 4 -cycloalkylmethyl, fluorinated C 3 -C 4 -alkenyl, formyl or C 1 -C 3 -alkylcarbonyl; R 1a is H, C 1 -C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C 4 -cycloalkylmethyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, fluorinated C 3 -C 4 -cycloalkylmethyl, fluorinated C 3 -C 4 -alkenyl, or R 1a and R 2 together are (CH 2 ) n with n being 2, 3 or 4, or R 1a and R 2a together are (CH 2 ) n with n being 2, 3 or 4; R 2 and R 2a are are independently of each other H, C 1 -C 4 -alkyl or fluorinated C 1 -C 4 -alkyl or R 2a and R 2 together are (CH 2 ) m with m being 1, 2, 3, 4 or 5; R 3 is H or C 1 -C 4 -alkyl; R 6 , R 7 independently of each other are selected from H, fluorine, C 1 -C 4 -alkyl and fluorinated C 1 -C 4 -alkyl or together form a moiety (CH 2 ) p with p being 2, 3, 4 or 5; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

  本发明涉及式I的芳香族化合物，其中Ar是苯基或芳香族5-或6-成员C-连接的杂环基，其中Ar可以携带1个基团Ra，且Ar还可以携带1或2个基团Rb；X是N或CH；E是CR6R7或NR3；R1是C1-C4烷基、C3-C4环烷基、C3-C4环烷基甲基、C3-C4烯基、氟代C1-C4烷基、氟代C3-C4环烷基、氟代C3-C4环烷基甲基、氟代C3-C4烯基、甲酰基或C1-C3烷基羰基；R1a是H、C1-C4烷基、C3-C4环烷基、C3-C4环烷基甲基、C3-C4烯基、氟代C1-C4烷基、氟代C3-C4环烷基、氟代C3-C4环烷基甲基、氟代C3-C4烯基，或R1a和R2一起是(CH2)n，其中n为2、3或4，或R1a和R2a一起是(CH2)n，其中n为2、3或4；R2和R2a彼此独立地是H、C1-C4烷基或氟代C1-C4烷基，或者R2a和R2一起是(CH2)m，其中m为1、2、3、4或5；R3是H或C1-C4烷基；R6、R7彼此独立地选择自H、氟、C1-C4烷基和氟代C1-C4烷基，或者一起形成(CH2)p的基团，其中p为2、3、4或5；以及其生理耐受性酸盐。本发明还涉及使用式I的化合物或其药学上可接受的盐制备用于治疗易受多巴胺D3受体配体治疗的医疗疾病的制药组合物。
• Heterocyclyl-3-sulfonylazaindole or -azaindazole derivatives as 5-hydroxytryptamine-6 ligands
  申请人：Bernotas Charles Ronald

  公开号：US20080015201A1

  公开（公告）日：2008-01-17

  The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.

  本发明提供了一种I式化合物及其用于治疗与5-HT6受体相关或受其影响的中枢神经系统疾病的用途。
• C-Met Modulators and Method of Use
  申请人：Bannen Lynne Canne

  公开号：US20110077233A1

  公开（公告）日：2011-03-31

  The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

  本发明提供了用于调节蛋白激酶酶活性以调节细胞活动（如增殖、分化、程序性细胞死亡、迁移和化学侵袭）的化合物。更具体地，本发明提供了能够抑制、调节和/或调节激酶受体（特别是c-Met、KDF、c-Kit、flt-3和flt-4）信号转导通路的喹唑啉和喹啉，这些信号转导通路与上述细胞活动的变化有关，以及包含这些化合物的组合物和使用它们治疗激酶依赖性疾病和病况的方法。本发明还提供了制备上述化合物的方法和包含这些化合物的组合物。