DL-2,3-二氯苯丙氨酸

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: DL-2,3-二氯苯丙氨酸
• 英文名称: 2-Amino-3-(2,3-dichloro-phenyl)-propionic acid
• 英文别名: 2-azaniumyl-3-(2,3-dichlorophenyl)propanoate
• 化学式: C₉H₉Cl₂NO₂
• 分子量: 234.082
• InChiKey: NVDAAIHKUHFKOL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  63.3
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  diethyl 2-acetamido-2-[(2,3-dichlorophenyl)methyl]propanedioate 、 氢溴酸 以86%的产率得到
  参考文献：
  名称：

  TAYLOR, DAVID C.;WIGHTMAN, R. H.;WIGHTMAN, F.;WAND, A. J., BIOORG. CHEM., 15,(1987) N 4, 335-345

  摘要：

  DOI：

文献信息

• [EN] SUBSTITUTED PIPERAZINES AS MODULATORS OF THE MELANOCORTIN RECEPTOR<br/>[FR] PIPERAZINES SUBSTITUEES COMME MODULATEURS DU RECEPTEUR DE MELANOCORTINE
  申请人：AMGEN INC

  公开号：WO2003009850A1

  公开（公告）日：2003-02-06

  Selected substituted piperazine compounds are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving activation of the melanocortin receptor. The subject invention also relates to processes For making such compounds as well as to intermediates useful in such processes.

  选定的取代哌嗪化合物可用于预防和治疗疾病，如肥胖症等。该发明涵盖了新化合物、类似物、前药及其药学上可接受的盐、制药组合物以及用于预防和治疗涉及黑色素皮质素受体激活的疾病和其他疾病或病症的方法。该发明还涉及制造这些化合物的过程，以及在此类过程中有用的中间体。
• Renin inhibitors and methods for using same
  申请人：SCHERING CORPORATION

  公开号：EP0246381A1

  公开（公告）日：1987-11-25

  The rise in intraocular pressure associated with the use of steroidal anti-inflammatory drugs is controlled by use of a renin inhibitor.

  使用类固醇抗炎药会导致眼压升高，而使用肾素抑制剂则可控制眼压升高。
• Lipidated peptides for lowering blood glucose
  申请人：USTAV ORGANICKE CHEMIE A BIOCHEMIE AKADEMIE VED CR, V.V.I.

  公开号：US10350271B2

  公开（公告）日：2019-07-16

  Lipidated analogs of prolactin-releasing peptides (PrRP) and their use in controlling and lowering blood glucose in mammals is disclosed. Useful compounds included lipidated analogs of PrRP20 and PrRP31. Pharmacological effects are demonstrated both in vitro and in vivo. Peripheral administration of the lipidated peptides towers blood glucose levels. These treatments are applicable for treating impaired glucose tolerance (IGT), and glucose intolerance condition. The disclosed compounds have application in treating medical conditions including diabetes, pre-diabetes, eating disorders, and obesity.

  本研究公开了催乳素释放肽（PrRP）的脂化类似物及其在控制和降低哺乳动物血糖中的用途。有用的化合物包括 PrRP20 和 PrRP31 的脂化类似物。药理作用在体外和体内都得到了证实。外周给药脂化肽可降低血糖水平。这些疗法适用于治疗糖耐量受损（IGT）和葡萄糖不耐受症。所公开的化合物可用于治疗糖尿病、糖尿病前期、饮食失调和肥胖症等病症。
• Lipidated peptides as neuroprotective agents
  申请人：USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.

  公开号：US10751390B2

  公开（公告）日：2020-08-25

  Lipidated neuropeptides PrRP31, PrRP20, containing C14 to C16 fatty acid, and their analogs, wherein a sequence of IRPVGRF-NH2 at the C-terminus is variable in the site of isoleucine, valine and phenylalanine; said fatty acid is bound in position 1 or 11 for PrRP31 or its analog and in position 1 or 7 for PrRP20 or its analog; the bond comprises an amide bond between an amino acid having at least one free NH2 group and a carboxylic group of the fatty acid and alternatively includes also a binding through arm X2, which is a hydrophilic linker selected from a group comprising β-alanine, γ-aminobutyric acid or γ-glutamic acid; for use in the treatment and prevention of diseases, which are Alzheimer's disease (AD), Parkinson's disease (PD), cognitive impairment no dementia (CIND), brain trauma, and neurodegenerative changes and disorders.

  含 C14 至 C16 脂肪酸的脂质化神经肽 PrRP31、PrRP20 及其类似物，其中 C 端 IRPVGRF-NH2 序列在异亮氨酸、缬氨酸和苯丙氨酸部位可变；所述脂肪酸对 PrRP31 或其类似物而言结合在第 1 位或第 11 位，对 PrRP20 或其类似物而言结合在第 1 位或第 7 位；该键包括具有至少一个游离 NH2 基团的氨基酸与脂肪酸的羧基之间的酰胺键，或者还包括一个结合通臂 X2，该结合通臂是一种亲水连接体，选自包括 β-丙氨酸、γ-氨基丁酸或 γ-谷氨酸的组；用于治疗和预防疾病，这些疾病包括阿尔茨海默病（AD）、帕金森病（PD）、无认知障碍痴呆症（CIND）、脑外伤以及神经退行性病变和紊乱。
• Bicyclic peptide ligands specific for MT1-MMP
  申请人：BicycleRD Limited

  公开号：US10792368B1

  公开（公告）日：2020-10-06

  The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of membrane type 1 metalloprotease (MT1-MMP). The invention also describes drug conjugates comprising said peptides, conjugated to one or more effector and/or functional groups which have utility in imaging and targeted cancer therapy.

  本发明涉及与分子支架共价结合的多肽，其与支架的连接点之间有两个或多个肽环。特别是，本发明描述的多肽是膜 1 型金属蛋白酶（MT1-MMP）的高亲和力结合剂。本发明还描述了由上述肽组成的药物共轭物，这些药物共轭于一个或多个效应基团和/或功能基团，可用于成像和癌症靶向治疗。