哌氟替索 | 54341-02-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻喃类
• 中文名称: 哌氟替索
• 中文别名: 氟噻吡醇；匹鲁克素
• 英文名称: Piflutixolum
• 英文别名: 2-[1-[(3E)-3-[6-fluoro-2-(trifluoromethyl)thioxanthen-9-ylidene]propyl]piperidin-4-yl]ethanol
• CAS: 54341-02-5
• 化学式: C₂₄H₂₅F₄NOS
• 分子量: 451.5
• InChiKey: CCUOZZURYIZOKX-FQJNFEMKSA-N

物化性质

• 沸点：
  529.7±50.0 °C(Predicted)
• 密度：
  1.306±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.9
• 重原子数：
  31
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  48.8
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• 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。
• COMPOSITIONS AND METHODS FOR TREATMENT OF VIRAL DISEASES
  申请人：Johansen Lisa M.

  公开号：US20100009970A1

  公开（公告）日：2010-01-14

  The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E) and the agent or combination of agents includes sertraline, a sertraline analog, UK-416244, or a UK-416244 analog. Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease.

  本发明涉及用于治疗病毒性疾病的组合物、方法和试剂盒。在某些实施方式中，病毒性疾病是由单链RNA病毒、黄病毒科病毒或肝病毒引起的。在特定实施方式中，病毒性疾病是病毒性肝炎（例如甲型肝炎、乙型肝炎、丙型肝炎、丁型肝炎、戊型肝炎），药剂或药剂组合包括舍曲林、舍曲林类似物、UK-416244或UK-416244类似物。还包括用于鉴定可用于治疗病毒性疾病的新化合物的筛选方法。
• Conjugated psychotropic drugs and uses thereof
  申请人：——

  公开号：US20040242570A1

  公开（公告）日：2004-12-02

  Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.

  本发明揭示了精神药物和有机酸的新型化学结合物，其在治疗精神病和/或增生性疾病和疾病以及作为化学增敏剂中的应用，所述的有机酸被选择用于减少由精神药物引起的副作用和/或发挥抗增殖活性。同时，本发明还揭示了这些化合物的合成方法。
• CONJUGATES COMPRISING A GABA- OR GLYCINE COMPOUND, PHARMACEUTICAL COMPOSITIONS AND COMBINATIONS THEREOF AND THEIR USE IN TREATING CNS DISORDERS
  申请人：Nudelman Abraham

  公开号：US20090304584A1

  公开（公告）日：2009-12-10

  Conjugates of a gamma-aminobutyric acid (GABA) compound or a glycine compound and an analgesic drug are disclosed. Further disclosed are pharmaceutical compositions containing these conjugates and uses thereof in the treatment of CNS-associated diseases or disorders, optionally in combination with a psychotropic drug.

  本发明揭示了伽玛-氨基丁酸(GABA)化合物或甘氨酸化合物和镇痛药物的共轭物。此外，还揭示了包含这些共轭物的制药组合物以及在治疗与中枢神经系统相关的疾病或障碍方面的用途，可选择与精神药物联合使用。
• NOVEL CONJUGATES FOR TREATING NEURODEGENERATIVE DISEASES AND DISORDERS
  申请人：STEIN Gideon

  公开号：US20120277310A1

  公开（公告）日：2012-11-01

  A conjugate comprising L-DOPA covalently linked to at least one γ-aminobutyric acid (GABA) moiety, an ester and/or an addition salt thereof are disclosed, as well as uses thereof for treating a neurodegenerative disease or disorder.

  本发明揭示了一种共轭物，包括L-DOPA与至少一种γ-氨基丁酸（GABA）基团共价连接，以及它的酯和/或加成盐，以及它们在治疗神经退行性疾病或障碍方面的用途。