2-azaniumyl-6-[(2-chlorophenyl)methoxycarbonylamino]hexanoate

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-azaniumyl-6-[(2-chlorophenyl)methoxycarbonylamino]hexanoate
• 化学式: C14H19ClN2O4
• 分子量: 314.76
• InChiKey: YCQVFPIEKSYHFI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  21
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  102
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• [EN] INHIBITORS OF GROWTH FACTOR ACTIVATION ENZYMES<br/>[FR] INHIBITEURS D'ENZYMES D'ACTIVATION DE FACTEUR DE CROISSANCE
  申请人：UNIV WASHINGTON

  公开号：WO2016144654A1

  公开（公告）日：2016-09-15

  The present invention generally relates to compounds that are useful for inhibiting one or more of hepatocyte growth factor activator, matriptase, hepsin, Factor Xa, or thrombin. The present invention also relates to various methods of using the inhibitor compounds including treating a malignancy, a pre-malignant condition, or cancer by administering an effective amount of the inhibitor to a subject in need thereof.

  本发明通常涉及对抑制肝细胞生长因子激活剂、麦曲丝蛋白、赫普星、Xa因子或凝血酶等的化合物有用的化合物。本发明还涉及使用抑制剂化合物的各种方法，包括通过向需要的受试者施用有效量的抑制剂来治疗恶性肿瘤、癌前病变或癌症。
• [EN] COMPOUNDS AND METHODS FOR TREATING CANCER, VIRAL INFECTIONS, AND ALLERGIC CONDITIONS<br/>[FR] COMPOSÉS ET MÉTHODES DE TRAITEMENT DU CANCER, D'INFECTIONS VIRALES ET D'AFFECTIONS ALLERGIQUES
  申请人：JANETKA JAMES

  公开号：WO2020264187A1

  公开（公告）日：2020-12-30

  The present invention generally relates to compounds that are useful for inhibiting one or more trypsin-like S1 serine proteases, HGFA, matriptase, hepsin, KLK5 and/or TMPRSS2 as well as cysteine proteases including trypsin-like cysteine proteases (e.g. Cathepsin B). The present invention also relates to various methods of using the inhibitor compounds to treat or prevent viral infections, including those caused by coronaviruses and influenza, conditions associated with KLK5, various malignancies, pre-malignant conditions, and cancer.

  本发明通常涉及一种用于抑制一个或多个类似胰蛋白酶的S1丝氨酸蛋白酶，HGFA、matriptase、hepsin、KLK5和/或TMPRSS2以及胱氨酸蛋白酶包括类似胰蛋白酶的胱氨酸蛋白酶（例如Cathepsin B）的化合物。本发明还涉及使用这些抑制剂化合物治疗或预防病毒感染的各种方法，包括由冠状病毒和流感病毒引起的感染，与KLK5相关的疾病、各种恶性肿瘤、癌前病变和癌症。
• Polypeptides
  申请人：IMPERIAL CHEMICAL INDUSTRIES PLC

  公开号：EP0315367A2

  公开（公告）日：1989-05-10

  The invention relates to a polypeptide of formula I:- wherein each of the generic terms is disclosed in full in the specification and includes:-R1 is (2-6C)alkanoyl or (1-4C)alkoxycarbonyl; A1 is a direct link to A2, or is Gly or Arg; A2 is a direct link to A3, or is Gly or Pro; A3 is a direct link to A4, or is Lys or Lys(Z); A4 is His or D-His; A5 is Trp or MeTrp; A6 is Ala or MeAla; A7 is Val or MeVal; A8 is Gly or Sar; A9 is His or MeHis; and Q is a group of the formula -A10.R2 in which A10 is Leu or D-Leu and R2 is hydroxy, amino, (1-3C)alkylamino or (1-3C)alkoxy; or Q is (1-6C)alkoxy or (1-10C)-alkylamino; provided that when R1 is acetyl and -A4-A5-A6-A7-A8-A9-Q is -His-Trp-Ala-Val-Gly-His-Leu-NH2 then -A1-A2-A3- is not a direct link to His. The compounds possess antagonist properties against bombesin-like peptides and are of value in the treatment of malignant disease in warm-blooded animals.

  本发明涉及式 I 的多肽 其中各通式在说明书中已全部公开，包括-R1是(2-6C)烷酰基或(1-4C)烷氧羰基；A1是与A2的直接连接，或者是Gly或Arg；A2是与A3的直接连接，或者是Gly或Pro；A3是与A4的直接连接，或者是Lys或Lys(Z)；A4 是 His 或 D-His；A5 是 Trp 或 MeTrp；A6 是 Ala 或 MeAla；A7 是 Val 或 MeVal；A8 是 Gly 或 Sar；A9 是 His 或 MeHis；以及 Q 是式 -A10 的基团。其中 A10 是 Leu 或 D-Leu，R2 是羟基、氨基、(1-3C)烷基氨基或(1-3C)烷氧基；或 Q 是(1-6C)烷氧基或(1-10C)-烷基氨基； 条件是当 R1 为乙酰基且-A4-A5-A6-A7-A8-A9-Q 为-His-Trp-Ala-Val-Gly-His-Leu-NH2 时，-A1-A2-A3- 不是与 His 的直接连接。 这些化合物具有拮抗蚕豆蛋白样肽的特性，在治疗温血动物的恶性疾病方面具有重要价值。
• Inhibitors of growth factor activation enzymes
  申请人：Janetka James W.

  公开号：US11130780B2

  公开（公告）日：2021-09-28

  The present invention generally relates to compounds that are useful for inhibiting one or more of hepatocyte growth factor activator, matriptase, hepsin, Factor Xa, or thrombin. The present invention also relates to various methods of using the inhibitor compounds including treating a malignancy, a pre-malignant condition, or cancer by administering an effective amount of the inhibitor to a subject in need thereof.

  本发明一般涉及可用于抑制一种或多种肝细胞生长因子激活剂、淀粉酶、肝素、Xa因子或凝血酶的化合物。 本发明还涉及使用抑制剂化合物的各种方法，包括通过向有需要的受试者施用有效量的抑制剂来治疗恶性肿瘤、恶性肿瘤前期病症或癌症。
• INHIBITORS OF GROWTH FACTOR ACTIVATION ENZYMES
  申请人：Janetka James W.

  公开号：US20180066015A1

  公开（公告）日：2018-03-08

  The present invention generally relates to compounds that are useful for inhibiting one or more of hepatocyte growth factor activator, matriptase, hepsin, Factor Xa, or thrombin. The present invention also relates to various methods of using the inhibitor compounds including treating a malignancy, a pre-malignant condition, or cancer by administering an effective amount of the inhibitor to a subject in need thereof.