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公开(公告)号:US08507724B2
公开(公告)日:2013-08-13
申请号:US13133569
申请日:2009-12-09
申请人: Martin Leuwer , Paul O'Neill , Neil Berry , Gertrud Haeseler
发明人: Martin Leuwer , Paul O'Neill , Neil Berry , Gertrud Haeseler
IPC分类号: C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00 , C07C39/12 , C07C43/20
CPC分类号: C07C39/367 , C07C39/15 , C07C43/23 , C07C235/46
摘要: The present invention concerns compounds derived from the anaethetic propofol. The compounds may be useful in the treatment of pain, particularly, but not exclusively, chronic pain and central pain sensitisation.
摘要翻译: 本发明涉及衍生自异步异丙酚的化合物。 该化合物可用于治疗疼痛,特别是但不限于,慢性疼痛和中枢性疼痛敏化。
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公开(公告)号:US20120029235A1
公开(公告)日:2012-02-02
申请号:US13133569
申请日:2009-12-09
申请人: Martin Leuwer , Paul O'Neill , Neil Berry , Gertrud Haeseler
发明人: Martin Leuwer , Paul O'Neill , Neil Berry , Gertrud Haeseler
IPC分类号: C07C39/367 , C07C39/15 , C07C43/23 , C07C233/65
CPC分类号: C07C39/367 , C07C39/15 , C07C43/23 , C07C235/46
摘要: The present invention concerns compounds derived from the anaethetic propofol. The compounds may be useful in the treatment of pain, particularly, but not exclusively, chronic pain and central pain sensitisation.
摘要翻译: 本发明涉及衍生自异步异丙酚的化合物。 该化合物可用于治疗疼痛,特别是但不限于,慢性疼痛和中枢性疼痛敏化。
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公开(公告)号:US07485669B2
公开(公告)日:2009-02-03
申请号:US10416632
申请日:2001-11-13
申请人: Gertrud Haeseler , Martin Leuwer
发明人: Gertrud Haeseler , Martin Leuwer
IPC分类号: A01N31/00 , A01M31/08 , A61K31/045 , A61K31/05
CPC分类号: A61K8/498 , A61K8/347 , A61K8/4973 , A61K31/05 , A61K31/055 , A61K31/35 , A61K31/352 , A61K2800/28 , A61Q19/00
摘要: The invention relates to a pharmaceutical composition comprising at least one phenol derivative represented by formula (I) wherein R1 represents a hydrogen atom, a halogen atom or a hydrocarbon group containing up to 12 carbon atoms; R2 represents a hydrogen atom or a C1-C7 alkyl group; wherein R1 and R2 may optionally form a carbocyclic 5- or 6-membered ring; R3 represents a hydrogen atom, a halogen atom or a C1-C7alkyl group; R4 represents a hydrogen atom, a C1-C7 alkyl group or a halogen atom; R5 represents hydrogen atom, a halogen atom or a C1-C7 alkyl group; and R6 represents a hydrogen atom, a C1-C7 alkyl group or a C2 or C3 alkenyl group, under the proviso that R2 and R4 can only both represent a hydrogen atom if both R1 and R5 represent a C1-C7 alkyl group and R3 represents a halogen atom. The composition is particularly useful for the blockage of sodium channels and/or influencing the kinetics of sodium channels and thus can be used as local anesthetic, antidysrhythmic, anticonvulsant/antiepilepticand spasmolytic.
摘要翻译: 本发明涉及包含至少一种由式(I)表示的苯酚衍生物的药物组合物,其中R 1表示氢原子,卤素原子或含有至多12个碳原子的烃基; R2表示氢原子或C1-C7烷基; 其中R1和R2可以任选地形成碳环5或6元环; R3表示氢原子,卤素原子或C1-C7烷基; R4表示氢原子,C1-C7烷基或卤素原子; R5代表氢原子,卤素原子或C1-C7烷基; 并且R 6表示氢原子,C 1 -C 7烷基或C 2或C 3烯基,条件是如果R 1和R 5均表示C 1 -C 7烷基,则R 2和R 4只能表示氢原子,并且R 3表示 卤素原子。 该组合物特别可用于阻断钠通道和/或影响钠通道的动力学,因此可用作局部麻醉剂,抗心律失常药,抗惊厥药/抗癫痫药和解痉药。
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公开(公告)号:US20070142477A1
公开(公告)日:2007-06-21
申请号:US11612623
申请日:2006-12-19
申请人: Martin Leuwer , Gertrud Haeseler , Jeremy Lambert , Delia Belelli
发明人: Martin Leuwer , Gertrud Haeseler , Jeremy Lambert , Delia Belelli
IPC分类号: A61K31/16 , A61K31/135 , A61K31/05
CPC分类号: A61K31/055
摘要: The present invention concerns compounds derived from the anaesthetic propofol that are useful as analgesics and methods of using the same. The compounds act as co-activators of strychnine-sensitive glycine receptors and may have greater activity at those glycine receptors than at GABAA.
摘要翻译: 本发明涉及可用作镇痛药的麻醉丙泊酚衍生的化合物及其使用方法。 化合物作为士的宁敏感的甘氨酸受体的共激活剂,并且在那些甘氨酸受体上可能具有比在GABA A A处更强的活性。
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