4-(Condensed cyclicmethyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists
摘要:
Formula 1的化合物,其中变量的含义如规范中所定义的,是alpha2肾上腺素受体的激动剂。本公开的若干化合物是特异性或选择性地作用于alpha2B和/或alpha2C肾上腺素受体,而不是alpha2A肾上腺素受体。此外,一些所述的化合物几乎没有心血管和/或镇静作用,或者仅有极小的作用。Formula 1的化合物在哺乳动物中,包括人类,作为治疗对alpha2肾上腺素受体激动剂有响应的疾病和/或症状缓解的药物是有用的。具有无显著心血管和/或镇静作用的Formula 1的化合物可用于治疗疼痛和其他症状,具有最小的副作用。
PIPERAZINE DERIVATIVES FOR BLOCKING Cav2.2 CALCIUM CHANNELS
申请人:Heer Jag Paul
公开号:US20130072499A1
公开(公告)日:2013-03-21
The present invention relates to novel piperazine compounds; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Ca
v
2.2 calcium channels is beneficial and to treat diseases for which blocking the Ca
v
2.2 and Ca
v
3.2 calcium channels is beneficial, e.g. to treat pain.
本发明涉及新型哌嗪化合物;含有这些化合物的药物组合物;以及利用这些化合物在治疗中治疗阻断Ca
v
2.2钙通道有益的疾病,以及治疗阻断Ca
v
2.2和Ca
v
3.2钙通道有益的疾病,例如治疗疼痛。
[EN] TROPANE COMPOUNDS<br/>[FR] COMPOSÉS DE TROPANE
申请人:EXELIXIS INC
公开号:WO2009055077A1
公开(公告)日:2009-04-30
A compound according to Formula I or II: (I) or (II) wherein R1, R1b, R2, L1, and L2 and L2b are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
[EN] PIPERAZINE DERIVATIVES FOR BLOCKING Cav2.2 CALCIUM CHANNELS<br/>[FR] DÉRIVÉS DE PIPÉRAZINE POUR BLOQUER DES CANAUX CALCIQUES CAV2.2
申请人:CONVERGENCE PHARMACEUTICALS
公开号:WO2011086377A1
公开(公告)日:2011-07-21
The present invention relates to novel piperazine compounds; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial and to treat diseases for which blocking the Cav2.2 and Cav3.2 calcium channels is beneficial, e.g. to treat pain.
4-(Condensed cyclicmethyl)-imidazole-2-thiones acting as α2 adrenergic agonists
申请人:Allergan, Inc.
公开号:US07396849B2
公开(公告)日:2008-07-08
Compounds of Formula 1
where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.