N-氰基-N'-(2-硝氧乙基)-3-吡啶甲脒甲烷磺酸盐 | 134431-49-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: N-氰基-N'-(2-硝氧乙基)-3-吡啶甲脒甲烷磺酸盐
• 英文名称: N-cyano-N'-(2-nitroxyethyl)-3-pyridinecarboximidamide methanesulfonate
• 英文别名: 2-[[(cyanoamino)-pyridin-3-ylmethylidene]amino]ethyl nitrate;methanesulfonic acid
• CAS: 134431-49-5
• 化学式: C10H13N5O6S
• 分子量: 331.31
• InChiKey: BIBJJSCMCXFMML-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.39
• 重原子数：
  22
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  179
• 氢给体数：
  2
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  N-cyano-N'-(2-nitroxyethyl)-3-pyridinecarboxamidine 生成 N-氰基-N'-(2-硝氧乙基)-3-吡啶甲脒甲烷磺酸盐
  参考文献：
  名称：

  Drugs Fut. 1994, 19, 546

  摘要：

  DOI：

文献信息

• Irrigation solution and method for inhibition of pain and inflammation
  申请人：Omeros Corporation

  公开号：EP1563838A2

  公开（公告）日：2005-08-17

  A method and solution for perioperatively inhibiting a variety of pain and inflammation, processes at wounds from general surgical procedures including oral/dental procedures. The solution preferably includes at least one α2- receptor agonist and, optionally, additional multiple pain and inflammation inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. The solution is applied by continuous irrigation of a wound during a surgical procedure for preemptive inhibition of pain and while avoiding undesirable side effects associated with oral, intramuscular, subcutaneous or intravenous application of larger doses of the agents. One preferred solution to inhibit pain and inflammation, includes an α2- receptor agonist, a serotonin2 antagonist, a serotonin3 antagonist, a histamine antagonist, a serotonin agonist, a cyclooxygenase inhibitor, a neurokinin1 antagonist, a neurokinin2 antagonist, a purinoceptor antagonist, an ATP-sensitive potassium channel opener, a calcium channel antagonist, a bradykinin1 antagonist, a bradykinin2 antagonist and a µ-opioid agonist.

  一种围手术期抑制包括口腔/牙科手术在内的一般外科手术伤口处各种疼痛和炎症过程的方法和溶液。该溶液最好包括至少一种α2-受体激动剂，另外还包括在生理载体（如生理盐水或乳酸林格氏液）中稀释浓度的多种疼痛和炎症抑制剂。该溶液可在手术过程中通过持续冲洗伤口来预先抑制疼痛，同时避免口服、肌肉注射、皮下注射或静脉注射大剂量药物所带来的不良副作用。一种优选的抑制疼痛和炎症的方案包括α2 受体激动剂、5-羟色胺2 拮抗剂、5-羟色胺3 拮抗剂、组胺拮抗剂、5-羟色胺激动剂、环氧化酶抑制剂、神经激肽1 拮抗剂、组胺拮抗剂、5-羟色胺激动剂、环氧化酶抑制剂、神经激肽 1 拮抗剂、神经激肽 2 拮抗剂、嘌呤受体拮抗剂、ATP 敏感性钾通道开放剂、钙通道拮抗剂、缓激肽 1 拮抗剂、缓激肽 2 拮抗剂和 µ 阿片类激动剂。
• Irrigation solution and use thereof for the perioperative inhibition of pain/inflammation and/or spasm at a vascular structure
  申请人：Omeros Corporation

  公开号：EP1609477A1

  公开（公告）日：2005-12-28

  A method and solution for perioperatively inhibiting a variety of pain and inflammation and spasm processes at a vascular structure during an intervascular procedure. The solution includes multiple pain and inflammation inhibitory agents and spasm inhibitory agents in a physiologic base, such as saline or lactated Ringer's solution. Depending on the application, the pain and inflammation agents included in the solution may include: (1) serotonin receptor antagonists; (2) serotonin receptor agonists; (3) histamine receptor antagonists; (4) bradykinin receptor antagonists: (5) kallikrein inhibitors; (6) tachykinin receptor antagonists, including neurokinin1 and neurokinin2 receptor subtype antagonists; (7) calcitonin gene-related peptide (CGRP) receptor antagonists; (8) interleukin receptor antagonists; (9) inhibitors of enzymes active in the synthetic pathway for arachadonic acid metabolites, including (a) phospholipase inhibitors, including PLA2 isoform and PLCγ isoform inhibitors, (b) cyclooxygenase inhibitors, and (c) lipooxygenase inhibitors; (10) prostanoid receptor antagonists including eicosanoid EP-1 and EP-2 receptor subtype antagonists and thromboxane receptor subtype antagonists; (11) leukotriene receptor antagonists including leukotriene B4 and D4 receptor subtype antagonists; (12) opioid receptor agonists, including mu-opiate, delta-opiate, and kappa-opiate receptor subtype agonists; (13) purinoceptor agonists and antagonists including P2X receptor antagonists and P2Y receptor agonists; (14) adenosine triphosphate (ATP) sensitive potassium channel openers; and (15) calcium channel antagonists. Suitable anti-inflammatory/anti-pain agents which also act as anti-spasm agents include serotonin receptor antagonists, tachykinin receptor antagonists, ATP-sensitive potassium channel openers and calcium channel antagonists. Other agents which may be utilized in the solution specifically for their anti-spasm properties including endothelin receptor antagonists and the nitric oxyde donors (enzyme activators). The solution is used to continuously irrigate a wound during an operative/interventional procedure for preemptive inhibition of pain and inflammation, as well as vascular and smooth muscle spasm, while avoiding undesirable side effects associated with oral, intramuscular or intravenous application of larger doses of the agents. The solution is useful for intravascular procedures.

  一种方法和溶液，用于在血管间手术期间围手术期抑制血管结构的各种疼痛、炎症和痉挛过程。该溶液包括生理基质（如生理盐水或乳酸林格氏液）中的多种疼痛和炎症抑制剂及痉挛抑制剂。根据不同的应用，溶液中包含的止痛和炎症抑制剂可包括(1) 血清素受体拮抗剂； (2) 血清素受体激动剂； (3) 组胺受体拮抗剂； (4) 缓激肽受体拮抗剂：(5) 降凝血酶抑制剂；(6) 速激肽受体拮抗剂，包括神经激肽 1 和神经激肽 2 受体亚型拮抗剂；(7) 降钙素基因相关肽（CGRP）受体拮抗剂；(8) 白细胞介素受体拮抗剂；(9) 花生四烯酸代谢物合成途径中活性酶的抑制剂，包括：(a) 磷脂酶抑制剂，包括 PLA2 同工酶和 PLCγ 同工酶抑制剂；(b) 环氧化酶抑制剂；(c) 脂氧化酶抑制剂；(10) 类固醇受体拮抗剂，包括类二十烷酸 EP-1 和 EP-2 受体亚型拮抗剂和血栓素受体亚型拮抗剂； (11) 白三烯受体拮抗剂，包括白三烯 B4 和 D4 受体亚型拮抗剂；(12) 阿片受体激动剂，包括μ-阿片、δ-阿片和卡帕-阿片受体亚型激动剂； (13) 嘌呤受体激动剂和拮抗剂，包括 P2X 受体拮抗剂和 P2Y 受体激动剂； (14) 对三磷酸腺苷（ATP）敏感的钾通道开放剂；以及 (15) 钙通道拮抗剂。合适的消炎/止痛剂也可作为抗痉挛剂，包括血清素受体拮抗剂、速激肽受体拮抗剂、ATP 敏感性钾通道开放剂和钙通道拮抗剂。溶液中可使用的其他抗痉挛药剂包括内皮素受体拮抗剂和一氧化氮供体（酶激活剂）。该溶液用于在手术/介入治疗过程中持续冲洗伤口，以预先抑制疼痛和炎症以及血管和平滑肌痉挛，同时避免口服、肌肉注射或静脉注射大剂量药剂所带来的不良副作用。该溶液适用于血管内手术。
• Peptides comprising non-natural amino acids and methods of making and using the same
  申请人：Longevity Biotech, Inc.

  公开号：US10543255B2

  公开（公告）日：2020-01-28

  This invention relates to novel compositions comprising analogs of naturally occurring polypeptides, wherein the analog comprises an α-amino acid and at least one β-amino acid. Administration of the compositions may be used for effecting treatment or prevention of a plurality of disease states caused by dysfunctional biochemical or biological pathways. The compositions and methods of this invention are particularly useful to identify novel therapeutic modulators of in-vivo receptor activity with extended half-lives and relevant bioactivity as compared to the naturally translated polypeptides upon which the analogs are derived.

  本发明涉及由天然多肽类似物组成的新型组合物，其中类似物包括一种α-氨基酸和至少一种β-氨基酸。给药组合物可用于治疗或预防由生化或生物途径功能障碍引起的多种疾病状态。本发明的组合物和方法特别适用于鉴定体内受体活性的新型治疗调节剂，与天然翻译的多肽相比，本发明的类似物具有更长的半衰期和相关的生物活性。
• Highly active polypeptides and methods of making and using the same
  申请人：Longevity Biotech, Inc.

  公开号：US10772934B2

  公开（公告）日：2020-09-15

  This invention relates to novel compositions comprising analogs of naturally occurring polypeptides, wherein the analog comprises an α-amino acid and at least one β-amino acid. Administration of the compositions may be used for effecting treatment or prevention of a plurality of disease states caused by dysfunctional biochemical or biological pathways. The compositions and methods of this invention are particularly useful to identify novel therapeutic modulators of in-vivo receptor activity with extended half-lives and relevant bioactivity as compared to the naturally translated polypeptides upon which the analogs are derived.

  本发明涉及由天然多肽类似物组成的新型组合物，其中类似物包括一种α-氨基酸和至少一种β-氨基酸。给药组合物可用于治疗或预防由生化或生物途径功能障碍引起的多种疾病状态。本发明的组合物和方法特别适用于鉴定体内受体活性的新型治疗调节剂，与天然翻译的多肽相比，本发明的类似物具有更长的半衰期和相关的生物活性。
• Surgical irrigation solution and method for inhibition of pain and inflammation
  申请人：Omeros Medical Systems, Inc.

  公开号：US20010044616A1

  公开（公告）日：2001-11-22

  A method and solution for perioperatively inhibiting a variety of pain and inflammation processes at wounds from general surgical procedures including oral/dental procedures. The solution preferably includes multiple pain and inflammation inhibitory at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. The solution is applied by continuous irrigation of a wound during a surgical procedure for preemptive inhibition of pain and while avoiding undesirable side effects associated with oral, intramuscular, subcutaneous or intravenous application of larger doses of the agents. One preferred solution to inhibit pain and inflammation includes a serotonin 2 antagonist, a serotonin 3 antagonist, a histamine antagonist, a serotonin agonist, a cyclooxygenase inhibitor, a neurokinin 1 antagonist, a neurokinin 2 antagonist, a purinoceptor antagonist, an ATP-sensitive potassium channel opener, a calcium channel antagonist, a bradykinin 1 antagonist, a bradykinin 2 antagonist and a &mgr;-opioid agonist.

  一种围手术期抑制一般外科手术（包括口腔/牙科手术）伤口处各种疼痛和炎症过程的方法和溶液。该溶液优选在生理载体（如生理盐水或乳酸林格氏液）中加入多种稀释浓度的疼痛和炎症抑制剂。该溶液可在手术过程中通过持续冲洗伤口来预先抑制疼痛，同时避免口服、肌肉注射、皮下注射或静脉注射大剂量制剂所带来的不良副作用。抑制疼痛和炎症的一种首选方案包括血清素 2 拮抗剂、血清素 3 拮抗剂、组胺拮抗剂、血清素激动剂、环氧化酶抑制剂、神经激肽 1 拮抗剂、神经激肽 2 拮抗剂、嘌呤受体拮抗剂、ATP 敏感性钾通道开放剂、钙通道拮抗剂、缓激肽 1 拮抗剂、缓激肽 2 拮抗剂和阿片激动剂。