1,4-Dimethyl-7-Azaindol | 27284-68-0

• 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: 1,4-Dimethyl-7-Azaindol
• 英文别名: 1,4-dimethyl-1H-pyrrolo[2,3-b]pyridine；1,4-dimethyl-1H-pyrrolo[2,3-b]pyridine；1,4-dimethylpyrrolo[2,3-b]pyridine
• CAS: 27284-68-0
• 化学式: C₉H₁₀N₂
• 分子量: 146.192
• InChiKey: GVCAIPDBXFIDQO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  17.8
• 氢给体数：
  0
• 氢受体数：
  1

文献信息

• [EN] DEUTERIUM-ENRICHED HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES ENRICHIS EN DEUTÉRIUM EN TANT QU'INHIBITEURS DE KINASES
  申请人：ASCEPION PHARMACEUTICALS INC

  公开号：WO2012028106A1

  公开（公告）日：2012-03-08

  The present invention provides deuterium-enriched heteroaryl-containing urea compounds (I) and use of the same for treating conditions mediated by protein kinase such as

  本发明提供了富含氘的杂环基脲化合物（I）以及利用这些化合物治疗由蛋白激酶介导的疾病的方法。
• [EN] DECAHYDROQUINOXALINE DERIVATIVES AND ANALOGS THEREOF<br/>[FR] DÉRIVÉS DE DÉCAHYDROQUINOXALINE ET LEURS ANALOGUES
  申请人：OTSUKA PHARMA CO LTD

  公开号：WO2013137479A1

  公开（公告）日：2013-09-19

  A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents -O- or -CH2-; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).

  通用式（1）表示的杂环化合物或其盐：其中m，l和n分别表示1或2的整数；X表示-O-或-CH2-；R1表示氢，较低的烷基基团，羟基较低的烷基基团，保护基或三较低烷氧基较低的烷基基团；R2和R3，相同或不同，各自独立地表示氢或较低的烷基基团；或R2和R3结合形成环-C3-C8烷基基团；R4表示芳香基团或杂环基团，其中芳香基团或杂环基团可能具有一个或多个任意取代基。
• [EN] HETEROCYCLIC COMPOUNDS FOR TREATING OR PREVENTING DISORDERS CAUSED BY REDUCED NEUROTRANSMISSION OF SEROTONIN, NOREPHNEPHRINE OR DOPAMINE.<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES POUR LE TRAITEMENT OU LA PRÉVENTION DE TROUBLES PROVOQUÉS PAR UNE NEUROTRANSMISSION RÉDUITE DE LA SÉROTONINE, DE LA NORÉPINEPHRINE OU DE LA DOPAMINE
  申请人：OTSUKA PHARMA CO LTD

  公开号：WO2012036253A1

  公开（公告）日：2012-03-22

  A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents -O- or -CH2-; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).

  通用式（1）表示的杂环化合物或其盐：其中m、l和n分别表示1或2的整数；X表示-O-或-CH2-；R1表示氢、较低的烷基基团、羟基较低的烷基基团、保护基或三较低烷氧基较低的烷基基团；R2和R3，相同或不同，各自独立地表示氢或较低的烷基基团；或R2和R3结合形成环-C3-C8烷基基团；R4表示芳香基团或杂环基团，其中芳香基团或杂环基团可能具有一个或多个任意取代基。
• [EN] HETEROCYCLIC COMPOUNDS AND METHODS OF USE<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES ET PROCÉDÉS D'UTILISATION
  申请人：INTEGRAL BIOSCIENCES PVT LTD

  公开号：WO2020012357A1

  公开（公告）日：2020-01-16

  The present invention discloses compounds useful in treatment of conditions associated with excessive activity of transforming growth factor beta (TGF-β), particularly type 1 or activin-like kinase 5 (ALK 5). Specifically the present invention discloses compound of formula (I) which exhibit inhibitory activity against ALK 5. Method of treating conditions associated with excessive activity (ALK 5) with such compound is disclosed. Uses thereof, pharmaceutical composition, and kits are also disclosed.

  本发明揭示了在治疗与转化生长因子β（TGF-β）过度活性相关的疾病中有用的化合物，特别是针对类型1或类活化激酶5（ALK 5）。具体来说，本发明揭示了具有对ALK 5具有抑制活性的化合物的结构式（I）。还公开了使用这种化合物治疗与过度活性（ALK 5）相关的疾病的方法。此外，还公开了这些化合物的用途、制药组合物和试剂盒。
• [EN] SOLUBLE GUANYLATE CYCLASE ACTIVATORS<br/>[FR] ACTIVATEURS DE GUANYLATE CYCLASE SOLUBLES
  申请人：MERCK SHARP & DOHME

  公开号：WO2011119518A1

  公开（公告）日：2011-09-29

  The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds are capable of modulating the body's production of cyclic guanosine monophosphate ("cGMP") and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.

  该发明涉及具有结构式（I）的化合物及其药用可接受盐，这些化合物是可溶性鸟苷酸环化酶激活剂。这些化合物能够调节人体对环鸟苷酸单磷酸（"cGMP"）的产生，并一般适用于治疗和预防与紊乱的cGMP平衡相关的疾病。这些化合物可用于治疗或预防心血管疾病、内皮功能障碍、舒张功能障碍、动脉粥样硬化、高血压、肺动脉高压、心绞痛、血栓形成、再狭窄、心肌梗死、中风、心功能不全、肺动脉高压、勃起功能障碍、支气管哮喘、慢性肾功能不全、糖尿病或肝硬化。