[Benzotriazol-1-yl(dimethylamino)methylidene]-dimethylazanium

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并三唑类
• 英文名称: [Benzotriazol-1-yl(dimethylamino)methylidene]-dimethylazanium
• 化学式: C11H16N5+
• 分子量: 218.28
• InChiKey: KFTDPOJLGIWVEI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  37
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] MACROCYCLIC QUINAZOLINE DERIVATIVES AS ANTIPROLIFERATIVE AGENTS<br/>[FR] DERIVES DE QUINAZOLINE MACROCYCLIQUE UTILISES COMME AGENTS ANTIPROLIFERATIFS
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2004105765A1

  公开（公告）日：2004-12-09

  The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents O, CH2, NH or S; in particular Z represents NH; Y represents -C3-9alkyl-, -C3-9alkenyl-, -C3-9alkynyl-, -C3-7alkyl-CO-NH- optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4 alkyloxycarbonylamino-, -C3-7alkenyl-CO-NH- optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-oxy-C1-5alkyl-, -C1-5alkyl NR13-, -C1-5alkyl-, -C1-5alkyl-NR14-CO-C1-5alkyl-, -C1-5alkyl-CO NR15-C1-5alkyl-, -C1-6alkyl-CO-NH-, -C1-6alkyl-NH-CO-, -C1-3alkyl-NH-CS-Het20-, -C1-3alkyl-NH-CO-Het20-, -C1-2alkyl-CO-Het21-CO-, -Het22-CH2-CO-NH-C1-3alkyl-, -CO-NH-C1-6alkyl-, -NH-CO-C1-6alkyl-, -CO-C1-7alkyl-, -C1-7alkyl-CO-, -C1-6alkyl-CO-C1-6alkyl-, -C1-2alkyl-NH-CO-CR16R17-NH-, -C1-2alkyl-CO-NH-CR18R19-CO-, -C1-2alkyl-CO-NR20-C1-3alkyl-CO-, C1-2alkyl-NR21-CH2-CO-NH-C1-3alkyl-, or -NR22-CO-C1-3alkyl-NH-; X1 represents a direct bond, O or -O-C1-2alkyl-, CO, -CO-C1-2alkyl-, NR11, -NR11-C1-2alkyl-, CH2-, -O-N=CH- or -C1-2alkyl-; X2 represents a direct bond, O, -O-C1-2alkyl-, CO, -CO-C1-2alkyl-, NR12, -NR12-C1-2alkyl-, -CH2-, -O-N=CH- or -C1-2alkyl-. The growth inhibitory effect anti-tumour activity of the present compounds has been demonstrated in vitro, in enzymatic assays on the receptor tyrosine kinase EGFR.

  本发明涉及公式（I）的化合物，其N-氧化物形式，药用可接受的加合物盐及其立体化异构形式，其中Z代表O、CH2、NH或S；特别是Z代表NH；Y代表-C3-9烷基，-C3-9烯基，-C3-9炔基，-C3-7烷基-CO-NH-（可选择地被氨基，单或双（C1-4烷基）氨基或C1-4烷氧羰氨基取代），-C3-7烯基-CO-NH-（可选择地被氨基，单或双（C1-4烷基）氨基或C1-4烷氧羰氨基取代），C1-5烷氧基-C1-5烷基，-C1-5烷基-NR13-，-C1-5烷基，-C1-5烷基-NR14-CO-C1-5烷基，-C1-5烷基-CO NR15-C1-5烷基，-C1-6烷基-CO-NH-，-C1-6烷基-NH-CO-，-C1-3烷基-NH-CS-Het20-，-C1-3烷基-NH-CO-Het20-，-C1-2烷基-CO-Het21-CO-，-Het22-CH2-CO-NH-C1-3烷基-，-CO-NH-C1-6烷基-，-NH-CO-C1-6烷基-，-CO-C1-7烷基-，-C1-7烷基-CO-，-C1-6烷基-CO-C1-6烷基-，-C1-2烷基-NH-CO-CR16R17-NH-，-C1-2烷基-CO-NH-CR18R19-CO-，-C1-2烷基-CO-NR20-C1-3烷基-CO-，C1-2烷基-NR21-CH2-CO-NH-C1-3烷基-，或-NR22-CO-C1-3烷基-NH-；X1代表直接键，O或-O-C1-2烷基-，CO，-CO-C1-2烷基-，NR11，-NR11-C1-2烷基-，CH2-，-O-N=CH-或-C1-2烷基-；X2代表直接键，O，-O-C1-2烷基-，CO，-CO-C1-2烷基-，NR12，-NR12-C1-2烷基-，-CH2-，-O-N=CH-或-C1-2烷基-。本发明化合物的生长抑制效应和抗肿瘤活性已在体外实验中，在EGFR受体酪氨酸激酶的酶促活性测定中得到证明。
• [EN] TRYPANOSOMES INHIBITORS<br/>[FR] INHIBITEURS DE TRYPANOSOMES
  申请人：HOFFMANN LA ROCHE

  公开号：WO2017089389A1

  公开（公告）日：2017-06-01

  The invention relates to a compound of formula (I) wherein R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used in the treatment of Human African TRypanosomiasis.

  本发明涉及一种化合物，其化学式为(I)，其中R1和R2的定义如说明书和权利要求书中所述。化合物(I)可用于治疗人类非洲锥虫病。
• DEUTERATED AMINOGLYCIDAL COMPOUNDS
  申请人：Gant Thomas G.

  公开号：US20090182057A1

  公开（公告）日：2009-07-16

  Provided herein are substituted aminoglycidyl compounds of Formula (1), processes of preparation, and pharmaceutical compositions thereof and methods of their use for treating, preventing, or ameliorating one or more symptoms of a social anxiety disorder, an anxiety disorder, hyperthyroidism, tremor, glaucoma, hypertension, coronary artery bypass graft, chronic stable angina, atrial arrhythmia, migraine, bleeding esophageal varices, hypertrophic subaortic stenosis, heart failure, post-myocardial infarction, decreased left ventricular function after recent myocardial infarction, and/or any disorder ameliorated by beta adrenergic receptor modulators.

  本文提供了一种式子为（1）的取代氨基环氧丙烷化合物，其制备方法，以及其制药组合物和用于治疗、预防或缓解社交焦虑症、焦虑症、甲状腺功能亢进、震颤、青光眼、高血压、冠状动脉搭桥手术、慢性稳定型心绞痛、心房心动过速、偏头痛、食管静脉曲张出血、肥厚性主动脉瓣下狭窄、心力衰竭、心肌梗死后、近期心肌梗死后左心室功能下降和/或任何通过β肾上腺素能受体调节剂缓解的疾病的治疗方法。
• Synthesis of carbon acid amides
  申请人：Synthacon GmbH

  公开号：EP1801086A1

  公开（公告）日：2007-06-27

  The present invention relates to a process for producing carbon acid amides, in particular peptides, whereby the carbon acid amide bond is formed by an activated carboxylic acid and an amine component in a continuous flow. The described process provides an efficient synthesis method for the formation of carbon acid amides, and is applicable even for large scale synthesis ranging from several grams to even more than 100 kg of products.

  本发明涉及一种生产碳酸酰胺，特别是肽的工艺，其中碳酸酰胺键由活化的羧酸和胺组分在连续流中形成。所述工艺为碳酸酰胺的形成提供了一种高效的合成方法，甚至适用于从几克到甚至超过 100 公斤产品的大规模合成。
• PROCESS FOR SYNTHESIS OF MUCIN-TYPE PEPTIDES AND MUC1-RELATED GLYCOPEPTIDES
  申请人：SHIONOGI & CO., LTD.

  公开号：EP1801118A1

  公开（公告）日：2007-06-27

  The invention aims at providing novel compounds useful as primer in producing mucin-type glycopeptides which are useful in a wide field including materials for biochemical research, drugs, and food and the production of which was difficult in the prior art; and a process for the production of glycopeptides by using the primers. The aim is attained by providing novel glycopeptide derivatives (represented by the general formula (I)) which each bear an aldehyde or ketone group at the end and each contain an amino acid residue cleavable with a protease; and an easy and simple process for the production of glycopeptides by using the derivative as the primer.

  本发明旨在提供可用作生产粘蛋白型糖肽的引物的新型化合物，该引物可用于广泛的领域，包括生化研究材料、药物和食品，在现有技术中很难生产；以及使用该引物生产糖肽的工艺。为达到上述目的，本发明提供了新型糖肽衍生物（通式(I)表示），其末端各含有一个醛基或酮基，且各含有一个可被蛋白酶裂解的氨基酸残基；以及一种使用该衍生物作为引物生产糖肽的简单易行的工艺。