艾才派硕 | 36067-73-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吖庚因类
• 中文名称: 艾才派硕
• 中文别名: 氮卓克唑
• 英文名称: azepexole
• 英文别名: 2-amino-6-ethyl-5,6,7,8-tetrahydro-4H-oxazolo[5,4-d]azepine；6-ethyl-4,5,7,8-tetrahydro-[1,3]oxazolo[4,5-d]azepin-2-amine
• CAS: 36067-73-9
• 化学式: C₉H₁₅N₃O
• mdl: MFCD00865941
• 分子量: 181.238
• InChiKey: ZNXAJGZPUQOEDZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.666
• 拓扑面积：
  55.3
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] POLYMERIC HYPERBRANCHED CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À DES EXCIPIENTS POLYMÉRIQUES HYPERBRANCHÉS
  申请人：ASCENDIS PHARMA AS

  公开号：WO2013024048A1

  公开（公告）日：2013-02-21

  The present invention relates to water-soluble carrier-linked prodrugs of formula (I),wherein POL is a polymeric moiety,each Hyp is independently a hyperbranched moiety,each moiety SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, m is 0 or 1, each n is independently an integer from 2 to 200 and each x is independently 0 or 1. It further relates to pharmaceutical compositions comprising said water- soluble carrier-linked prodrugs and methods of treatment.

  本发明涉及水溶性载体连接的前药，其化学式为（I），其中POL是聚合物基团，每个Hyp是独立的超支化基团，每个基团SP是独立的间隔基团，每个L是独立的可逆前药连接基团，m为0或1，每个n是独立的整数，范围从2到200，每个x是独立的0或1。此外，还涉及包含所述水溶性载体连接的前药的药物组合物和治疗方法。
• [EN] HIGH-LOADING WATER-SOLUBLE CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À DES EXCIPIENTS HYDROSOLUBLES DE FORTE CHARGE
  申请人：ASCENDIS PHARMA AS

  公开号：WO2013024047A1

  公开（公告）日：2013-02-21

  The present invention relates to water-soluble carrier-linked prodrugs of formula (I), wherein B, A and Hyp form the carrier, B is a branching core, each A is independently a poly(ethylene glycol)-based polymeric chain, each Hyp is independently a branched moiety, each SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, each D is independendly a biologically active moiety, each x is independently 0 or 1, each m is independently an integer of from 2 to 64, n is an integer from 3 to 32; or the pharmaceutically acceptable salt thereof. It further relates to pharmaceutical compositions comprising said water-soluble carrier-linked prodrugs, their use asmedicament or diagnostic, and methods of treatment.

  本发明涉及水溶性载体连接的前药，其化学式为(I)，其中B、A和Hyp形成载体，B是一个分支核心，每个A独立地是一条聚乙二醇基聚合链，每个Hyp独立地是一个分支基团，每个SP独立地是一个间隔基团，每个L独立地是一个可逆前药连接基团，每个D独立地是一个生物活性基团，每个x独立地为0或1，每个m独立地是从2到64的整数，n是从3到32的整数；或其药学上可接受的盐。进一步涉及包括所述水溶性载体连接的前药的药物组合物，其用作药物或诊断，以及治疗方法。
• [EN] RELEASABLE CONJUGATES<br/>[FR] CONJUGUÉS LIBÉRABLES
  申请人：QUIAPEG PHARMACEUTICALS AB

  公开号：WO2018163131A1

  公开（公告）日：2018-09-13

  The present application provides compounds of Formula (B), or pharmaceutically acceptable salts thereof, wherein D is a residue of a biologically active drug, which underdo hydrolysis under physiological conditions to release the biologically active drug and which are useful in the treatment of disorders that could be beneficially treated with the drug.

  本申请提供了化合物的公式（B），或其药用盐，其中D是生物活性药物的残留物，在生理条件下经过水解释放出生物活性药物，并且对可能受益于该药物治疗的疾病具有用处。
• [EN] PROTEIN CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À UN EXCIPIENT PROTÉIQUE
  申请人：ASCENDIS PHARMA AS

  公开号：WO2013024049A1

  公开（公告）日：2013-02-21

  The present invention relates to water-soluble protein carrier- linked prodrugs wherein the protein carrier comprises an amino acid sequence consisting of at least 100 amino acid residues forming random coil conformation and comprising alanine, serine and proline residues. It further relates to pharmaceutical compositions comprising said water-soluble protein carrier- linked prodrugs, their use as a medicament as well as methods of treatment and administration.

  本发明涉及水溶性蛋白载体连接的前药，其中蛋白载体包括至少100个氨基酸残基组成的氨基酸序列，形成随机卷曲构象，包括丙氨酸、丝氨酸和脯氨酸残基。还涉及包含上述水溶性蛋白载体连接的前药的药物组合物，它们作为药物的用途，以及治疗和管理的方法。
• Combination of adrenergic agonist and tricyclo-alkylamine for relieving chronic pain without adverse side effects
  申请人：——

  公开号：US20020177592A1

  公开（公告）日：2002-11-28

  This invention discloses that a combination of two drugs, from two different and previously unrelated categories, provides effective and long-lasting relief from neuropathic pain. Both drugs can be taken orally, in a convenient, painless, non-invasive manner that does not require injections. One drug in this combination is an &agr;2 adrenergic agonist, exemplified by clonidine. The other drug in the pain-relieving combination has a tri-cyclo-alkyl-amine (TCAA) structure. At least some TCAA drugs have antagonist (receptor-blocking) activity at two entirely different classes of neuronal receptors: the muscarinic subclass of acetylcholine (ACh) receptors, and the NMDA subclass of glutamate receptors. Such drugs include ethopropazine, normally used as an anti-cholinergic drug, and desipramine, normally used as an anti-depressant. Tests by the Applicants have shown that at least some TCAA drugs can relieve neuropathic pain to a limited extent, but at the doses required to relieve pain, they cause adverse side effects, and any pain relief is relatively brief and short-lived. However, when a TCAA drug such as ethopropazine is administered together with an &agr;2 adrenergic agonist such as clonidine, these drugs mutually potentiate one another's neuropathic pain-relieving action, and provide potent and sustained neuropathic pain relief, even when each agent is administered at a low dosage that is below its threshold for causing adverse side effects. Accordingly, this drug combination can provide safe and effective relief of neuropathic pain and possibly other types of chronic and/or intractable pain, at dosages which are so low that they do not pose serious risks of adverse side effects.

  这项发明揭示了两种药物的组合，来自两个不同且先前无关的类别，能够有效且持久地缓解神经痛。这两种药物可以口服，以方便、无痛、非侵入性的方式服用，无需注射。这种组合中的一种药物是α2肾上腺素受体激动剂，以克隆啶为例。缓解疼痛的另一种药物具有三环烷基胺（TCAA）结构。至少一些TCAA药物在两个完全不同的类别的神经受体上具有拮抗（受体阻断）活性：乙酰胆碱（ACh）受体的肌样亚类和谷氨酸受体的NMDA亚类。这些药物包括依托普拉辛，通常用作抗胆碱药物，以及地西泮，通常用作抗抑郁药物。申请人的测试显示，至少一些TCAA药物可以在一定程度上缓解神经痛，但在缓解疼痛所需的剂量下，它们会引起不良副作用，而且任何疼痛缓解都相对短暂。然而，当像依托普拉辛这样的TCAA药物与像克隆啶这样的α2肾上腺素受体激动剂一起使用时，这些药物相互增强彼此的神经痛缓解作用，并提供强效且持久的神经痛缓解，即使每种药物在低剂量下也能实现，低剂量低于引起不良副作用的阈值。因此，这种药物组合可以在剂量非常低的情况下提供神经痛和可能其他类型的慢性和/或难治性疼痛的安全有效缓解，不会带来严重的不良副作用风险。