N-hydroxy-L-arginine (NOHA)

• 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: N-hydroxy-L-arginine (NOHA)
• 英文别名: (2S)-5-(diaminomethylideneamino)-2-(hydroxyamino)pentanoic acid
• 化学式: C₆H₁₄N₄O₃
• 分子量: 190.2
• InChiKey: WQFIAVZQVYASHZ-BYPYZUCNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -4.2
• 重原子数：
  13
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  134
• 氢给体数：
  5
• 氢受体数：
  5

文献信息

• [EN] ARGINASE INHIBITORS AND METHODS OF USE<br/>[FR] INHIBITEURS D'ARGINASE ET PROCÉDÉS D'UTILISATION
  申请人：MERCK SHARP & DOHME

  公开号：WO2019177873A1

  公开（公告）日：2019-09-19

  Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.

  本文描述了化合物I的结构或其药用盐。化合物I作为精氨酸酶抑制剂，可用于预防、治疗或作为精氨酸酶相关疾病的治疗剂。
• Nitrosated and nitrosylated cyclooxygenase-2 inhibitors, compositions and methods of use
  申请人：——

  公开号：US20010041726A1

  公开（公告）日：2001-11-15

  The present invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or optionally, at least one therapeutic agent, such as, steroids, nonsteroidal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B 4 (LTB 4 ) receptor antagonists, leukotriene A 4 (LTA 4 ) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMGCoA) inhibitors, H antagonists, antineoplastic agents, antiplatelet agents, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhibitors, isoprostane inhibitors, and mixtures thereof. The present invention also provides novel compositions comprising at least one parent COX-2 inhibitor and at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The present invention also provides kits and methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity; and for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2.

  本发明描述了新颖的硝化和/或亚硝化环氧合酶2（COX-2）抑制剂以及包含至少一种硝化和/或亚硝化环氧合酶2（COX-2）抑制剂的新型组合物，以及可选地，至少一种捐赠、转移或释放一氧化氮、刺激内源性一氧化氮合成、提高内源性内皮源性舒张因子水平或是一氧化氮合酶底物的化合物，和/或可选地，至少一种治疗剂，如类固醇、非甾体抗炎化合物（NSAID）、5-脂氧合酶（5-LO）抑制剂、白三烯B4（LTB4）受体拮抗剂、白三烯A4（LTA4）水解酶抑制剂、5-HT激动剂、3-羟基-3-甲基戊二酰辅酶A（HMGCoA）抑制剂、H受体拮抗剂、抗肿瘤药物、抗血小板药物、解充血剂、利尿剂、镇静或非镇静抗组胺药、诱导型一氧化氮合酶抑制剂、阿片类药物、镇痛剂、幽门螺杆菌抑制剂、质子泵抑制剂、异前列腺素抑制剂以及其混合物。本发明还提供了包含至少一种母体COX-2抑制剂和至少一种一氧化氮供体的新型组合物，以及可选地，至少一种治疗剂。本发明还提供了用于治疗炎症、疼痛和发热的工具和方法；用于治疗和/或改善COX-2抑制剂的胃肠道特性；用于促进伤口愈合；用于治疗和/或预防肾毒性；以及用于治疗和/或预防由于环氧合酶-2水平升高而导致的其他疾病的工具和方法。
• DERIVATIVES OF N-ACYL-N'-PHENYLPIPERAZINE USEFUL (INTER ALIA) FOR THE PROPHYLAXIS OR TREATMENT OF DIABETES
  申请人：Kasai Shizuo

  公开号：US20120071489A1

  公开（公告）日：2012-03-22

  The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4.

  本发明涉及一种化合物，其化学式如下所示，其中每个符号如本说明书中所定义，该化合物具有优越的降低RBP4作用，并且可用作预防或治疗由RBP4增加介导的疾病或病况的药物组合物。
• Nitrosated proton pump inhibitors, compositions and methods of use
  申请人：NitroMed, Inc.

  公开号：US20040024014A1

  公开（公告）日：2004-02-05

  The invention describes novel nitrosated proton pump inhibitor compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated proton pump inhibitor compound, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating gastrointestinal disorders; facilitating ulcer healing; decreasing the recurrence of ulcers; improving gastroprotective properties, anti- Helicobacter pylori properties or antacid properties of proton pump inhibitors; decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds; treating bacterial infections and/or viral infections.

  该发明描述了新颖的亚硝化质子泵抑制剂化合物及其药用盐，以及包含至少一种亚硝化质子泵抑制剂化合物的新型组合物，以及可选地，至少一种捐赠、转移或释放一氧化氮、刺激内源性一氧化氮合成、提高内源性内皮源性舒张因子水平或是一氧化氮合酶底物的化合物，和/或至少一种治疗剂。该发明还提供了包含至少一种亚硝化质子泵抑制剂化合物和至少一种捐赠、转移或释放一氧化氮、提高内源性内皮源性舒张因子水平、刺激内源性一氧化氮合成或是一氧化氮合酶底物和/或至少一种治疗剂的新型组合物。该发明还提供了包含至少一种亚硝化质子泵抑制剂化合物，可选地至少一种一氧化氮供体和/或至少一种治疗剂的新型套装。该发明还提供了治疗胃肠道疾病的方法；促进溃疡愈合；减少溃疡复发；改善质子泵抑制剂的胃保护性能、抗幽门螺杆菌性能或抗酸性能；减少或减轻与非甾体类抗炎化合物使用相关的胃肠毒性；治疗细菌感染和/或病毒感染。
• N-phenpropylcuclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase
  申请人：——

  公开号：US20030105132A1

  公开（公告）日：2003-06-05

  The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R 1 is optionally substituted C 1-6 alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C 1-6 alkoxy, —NR 2 R 3 or —NR 4 SO 2 R 5 ; X is the linkage —(CH 2 ) n — or —(CH 2 ) q —O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C 1-4 alkoxy; hydroxy; hydroxy(C 1-3 alkyl); C 3-7 cycloalkyl; carbocyclyl; heterocyclyl; or by C 1-4 alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R 8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5 - or 6 -membered carbocyclic or heterocyclyic ring. 1

  该发明涉及用于治疗性功能障碍的化合物(I)的公式，其中R1是可选择取代的C1-6烷基，可选择取代的碳环烷基，可选择取代的杂环烷基，氢，C1-6烷氧基，—NR2R3或—NR4SO2R5；X是连接基—(CH2)n—或—( )q—O—（其中Y连接到氧原子）；其中连接基X中的一个或多个氢原子可以独立地被C1-4烷氧基，羟基，羟基(C1-3烷基)，C3-7环烷基，碳环烷基，杂环烷基或可选择取代的一个或多个氟或苯基的C1-4烷基替代；n为3、4、5、6或7；q为2、3、4、5或6；Y为苯基或吡啶基，每个基都可以被取代；或相邻碳原子上的两个R8基连同相互连接的碳原子可以形成一个可选择取代的5-或6-成员碳环或杂环环。