已经进行了2-氨基-1-甲基-6-苯基咪唑并[4,5- b ]吡啶(PhIP),三个结构异构体和两个去苯基PhIP同类物的合成。使用鼠伤寒沙门氏菌菌株TA98在Ames试验中评估致突变力。与这些杂环胺中的结构特征相关的致突变力增加,从而允许苯基和咪唑并[4,5- b ]吡啶N 2-氨基取代基之间的共振延长。相比之下,PhIP异构体的取代不允许苯基参与其氨基咪唑共鸣杂合体,而去苯基同类物的诱变性比PhIP低86-234倍。
Heterobicyclic compounds of Formula (I):
or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, Huntington's Disease, and the like.
Formula (I)的杂环化合物:
或其药用可接受的盐、互变异构体或立体异构体,如规范中所定义,并含有它们的组合物,以及制备这种化合物的方法。本文还提供了通过抑制PDE10来治疗由此可治疗的疾病或疾病的方法,如肥胖症、非胰岛素依赖型糖尿病、精神分裂症、躁郁症、强迫症、亨廷顿病等。
Prokineticin 1 receptor antagonists
申请人:Coats Steven J.
公开号:US20080269225A1
公开(公告)日:2008-10-30
The present invention relates to certain novel compounds of Formula (I):
and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.
[EN] MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR 2<br/>[FR] MODULATEURS DU RÉCEPTEUR MÉTABOTROPIQUE DU GLUTAMATE 2
申请人:MASSACHUSETTS GEN HOSPITAL
公开号:WO2021155196A1
公开(公告)日:2021-08-05
The present application provides a compound of Formula: or a pharmaceutically acceptable salt thereof, wherein ring B, L1, ring A, L2, n, R1, R2, R3, R4, and X1 are as described herein. Pharmaceutical compositions comprising the compound, as well as the methods of making and using the compound, are also provided.
PROKINETICIN 1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PAIN
申请人:Flores Christopher M.
公开号:US20110319400A1
公开(公告)日:2011-12-29
Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows:
wherein A
1
, L
1
, D, and Q are defined herein.
The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I):
wherein the symbols are defined in the specification.