D-tyrosine ; hydrochloride

• 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
• 英文名称: D-tyrosine ; hydrochloride
• 英文别名: D-Tyrosin; Hydrochlorid；(R)-2-amino-3-(4-hydroxyphenyl)propionic acid hydrochloride；(2R)-2-amino-3-(4-hydroxyphenyl)propanoic acid;hydrochloride
• 化学式: C₉H₁₁NO₃*ClH
• 分子量: 217.652
• InChiKey: JJWFIVDAMOFNPS-DDWIOCJRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.77
• 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：
  83.6
• 氢给体数：
  4
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  氯化亚砜 、 D-tyrosine ; hydrochloride 、 甲醇 在 ice water 、 异丙醚 作用下， 反应 3.17h， 以to give (R)-2-amino-3-(4-hydroxyphenyl)propionic acid methyl ester hydrochloride (33.9 g)的产率得到D-酪氨酸甲酯盐酸盐
  参考文献：
  名称：

  Aminoalcohol derivatives and their use as beta 3 adrenergic agonists

  摘要：

  化合物的式子(I)：其中X1是键或—OCH2—；X2是—(CH2)n—，其中n为1、2或3；X3是键、—O—、—S—、—OCH2—或—NH—；R1是苯基或吡啶基，每个基团可能有一个或两个取代基，所选的取代基包括羟基、卤素等；R2是氢、(较低)烷氧羰基等；R3是羟基(较低)烷基、卤代(较低)烷基等；R4是芳基或不饱和杂环基，每个基团可能有一个或两个取代基，所选的取代基包括较低烷基、羟基、氨基甲酰基、卤素、较低烷氧等；以及其盐，其用作药物。

  公开号：

  US20050043358A1
• 作为产物：
  描述：

  DL-酪氨酸甲酯盐酸盐 在 Aspergillus niger lipase 、 sodium acetate buffer 作用下， 生成 L-酪氨酸盐酸盐 、 D-tyrosine ; hydrochloride
  参考文献：
  名称：

  Empirical rules for the enantiopreference of lipase from Aspergillus niger toward secondary alcohols and carboxylic acids, especially α-amino acids

  摘要：

  Lipase from Aspergillus niger (ANL, Amano lipase AP) catalyzes enantioselective hydrolysis and acylation reactions. To aid in the design of new applications of this lipase, we propose two empirical rules that predict which enantiomer reacts faster. For secondary alcohols, a rule proposed previously for other lipases also works for ANL, but with lower reliability (77%, 37 of 48 examples). For carboxylic acids, we examined both crude and partially-purified ANL because commercial ANL contains contaminating hydrolases. Partial purification removed a contaminating amidase and increased the enantioselectivity of ANL toward many alpha-amino acids, including cyclic amino acids. Unlike other lipases, ANL readily accepts positively-charged substrates and shows the highest enantioselectivity toward alpha-amino acids. Although a rule based on the sizes of the substituents could not predict the fast-reacting enantiomer, a rule limited to alpha-amino acids did predict the fast-reacting enantiomer. We estimate that the charged alpha-amino group contributes a factor of 40-100 (Delta Delta G double dagger=2.2-2.7 kcal/mol) to the enantioselectivity of ANL towards carboxylic acids. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0957-4166(97)00524-7

文献信息

• [EN] CHEMICAL COMPOUNDS<br/>[FR] COMPOSÉS CHIMIQUES
  申请人：NODTHERA LTD

  公开号：WO2018167468A1

  公开（公告）日：2018-09-20

  The present disclosure relates to compounds of Formula (I): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein inhibit the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inter alia autoinflammatory and autoimmune diseases and cancers.

  本公开涉及式(I)的化合物及其药用可接受的盐、药物组合物、使用方法和制备方法。本文披露的化合物通过抑制炎症小体来抑制IL-1家族细胞因子的成熟，可用于治疗涉及炎症小体活性的疾病，如自身炎症和自身免疫疾病以及癌症等。
• TYROSINE HYDROXYLASE INHIBITORS FOR USE IN TREATING CANCER
  申请人：Tyme, Inc.

  公开号：EP3488848A1

  公开（公告）日：2019-05-29

  The invention relates to a pharmaceutical composition comprising: a tyrosine hydroxylase inhibitor; and melanin, a melanin promoter, or a combination thereof. The invention also relates to a tyrosine hydroxylase inhibitor that is a-methyl-DL-tyrosine for use in treating cancer. Pharmaceutical compositions and kits including a tyrosine hydroxylase inhibitor; melanin, a melanin promoter, or a combination thereof; a p450 3A4 promoter; and a leucine aminopeptidase inhibitor are also provided. Also provided is the treatment of cancer in a subject, comprising administering an effective amount of a tyrosine hydroxylase inhibitor, a melanin promoter, a p450 3A4 promoter, and a leucine aminopeptidase inhibitor to the subject in need thereof. Also provided are means of reducing cell proliferation in a subject comprising administering an effective amount of a tyrosine hydroxylase inhibitor, a melanin promoter, a p450 3A4 promoter, and a leucine aminopeptidase inhibitor to the subject in need thereof.

  本发明涉及一种药物组合物，其中包含：酪氨酸羟化酶抑制剂；黑色素、黑色素促进剂或其组合。本发明还涉及一种用于治疗癌症的 a-甲基-DL-酪氨酸酪氨酸羟化酶抑制剂。还提供了包括酪氨酸羟化酶抑制剂、黑色素、黑色素促进剂或其组合、p450 3A4 促进剂和亮氨酸氨肽酶抑制剂的药物组合物和试剂盒。还提供了治疗受试者癌症的方法，包括向有需要的受试者施用有效量的酪氨酸羟化酶抑制剂、黑色素促进剂、p450 3A4 促进剂和亮氨酸氨肽酶抑制剂。还提供了减少受试者细胞增殖的方法，包括向有需要的受试者施用有效量的酪氨酸羟化酶抑制剂、黑色素促进剂、p450 3A4 促进剂和亮氨酸氨肽酶抑制剂。
• TYROSINE HYDROXYLASE INHIBITOR FOR TREATING INTESTINAL HYPERPERMEABILITY
  申请人：Hoffman, Steve

  公开号：EP3750555A1

  公开（公告）日：2020-12-16

  The present invention provides methods, compositions, and kits for treating intestinal hyperpermeability in a subject in need thereof, including conditions such as hyperglycemia and underlying diseases such as diabetes, autism, fibromyalgia, inflam -matory bowel disease (IBD), graft versus host disease (GVHD), HIV/ AIDS, multiple organ dysfunction syndrome, irritable bowel syndrome (IBS), celiac disease, eczema, psoriasis, acute pancreatitis, Parkinson's disease, depression, chronic fatigue syndrome, asthma, multiple sclerosis, arthritis, ankylosing spondylitis, nonalcoholic fatty liver disease, alcoholic cirrhosis, environmental en -teropathy, or kwashiorkor.

  本发明提供了用于治疗有需要的受试者肠道高渗透性的方法、组合物和试剂盒，包括高血糖症等病症和糖尿病、自闭症、纤维肌痛、炎症性肠病（IBD）、移植物抗宿主疾病（GVHD）、艾滋病病毒/艾滋病、多器官功能障碍综合征、肠易激综合征（IBS）、乳糜泻、湿疹、牛皮癣、急性胰腺炎、帕金森病、抑郁症、慢性疲劳综合征、慢性胰腺炎、帕金森病等潜在疾病、多器官功能障碍综合征、肠易激综合征（IBS）、乳糜泻、湿疹、银屑病、急性胰腺炎、帕金森病、抑郁症、慢性疲劳综合征、哮喘、多发性硬化症、关节炎、强直性脊柱炎、非酒精性脂肪肝、酒精性肝硬化、环境性肝炎或卡瓦氏病。
• Pharmaceutical compositions and methods
  申请人：Tyme, Inc.

  公开号：US10010590B2

  公开（公告）日：2018-07-03

  Pharmaceutical compositions and kits including a tyrosine hydroxylase inhibitor; melanin, a melanin promoter, or a combination thereof; a p450 3A4 promoter; and a leucine aminopeptidase inhibitor are provided. Also provided are methods of treating cancer in a subject, comprising administering an effective amount of a tyrosine hydroxylase inhibitor, a melanin promoter, a p450 3A4 promoter, and a leucine aminopeptidase inhibitor to the subject in need thereof. Also provided are methods of reducing cell proliferation in a subject comprising administering an effective amount of a tyrosine hydroxylase inhibitor, a melanin promoter, a p450 3A4 promoter, and a leucine aminopeptidase inhibitor to the subject in need thereof.

  提供了包括酪氨酸羟化酶抑制剂、黑色素、黑色素促进剂或其组合、p450 3A4 促进剂和亮氨酸氨肽酶抑制剂的药物组合物和试剂盒。还提供了治疗受试者癌症的方法，包括向有需要的受试者施用有效量的酪氨酸羟化酶抑制剂、黑色素启动子、p450 3A4启动子和亮氨酸氨肽酶抑制剂。还提供了减少受试者细胞增殖的方法，包括向有需要的受试者施用有效量的酪氨酸羟化酶抑制剂、黑色素促进剂、p450 3A4 促进剂和亮氨酸氨肽酶抑制剂。
• Compositions and methods for treating intestinal hyperpermeability
  申请人：Hoffman Steven

  公开号：US10085959B2

  公开（公告）日：2018-10-02

  The present invention provides methods, compositions, and kits for treating intestinal hyperpermeability in a subject in need thereof, including conditions such as hyperglycemia and underlying diseases such as diabetes, autism, fibromyalgia, inflammatory bowel disease (IBD), graft versus host disease (GVHD), HIV/AIDS, multiple organ dysfunction syndrome, irritable bowel syndrome (IBS), celiac disease, eczema, psoriasis, acute pancreatitis, Parkinson's disease, depression, chronic fatigue syndrome, asthma, multiple sclerosis, arthritis, ankylosing spondylitis, nonalcoholic fatty liver disease, alcoholic cirrhosis, environmental enteropathy, or kwashiorkor.

  本发明提供了用于治疗有需要的受试者肠道高渗透性的方法、组合物和试剂盒，包括高血糖症等病症和糖尿病、自闭症、纤维肌痛、炎症性肠病（IBD）、移植物抗宿主病（GVHD）、艾滋病毒/艾滋病、多器官功能障碍综合征、肠易激综合征（IBS）、乳糜泻、湿疹、牛皮癣、急性胰腺炎、帕金森病、抑郁症、慢性疲劳综合征等潜在疾病、多器官功能障碍综合征、肠易激综合征 (IBS)、乳糜泻、湿疹、牛皮癣、急性胰腺炎、帕金森病、抑郁症、慢性疲劳综合征、哮喘、多发性硬化症、关节炎、强直性脊柱炎、非酒精性脂肪肝、酒精性肝硬化、环境性肠病或卡瓦氏病。