引入δ-选择性化合物1和2(DS1,化合物22; DS2,化合物16)作为含δ的GABA A型受体(GABA A R)的功能选择性调节剂。在我们手中,用重组GABA A R和化合物22进行的[ 3 H] EBOB结合实验没有显示δ选择性的证据,尽管就效力而言,对α4β3δ和α6β2/3δ受体的偏爱程度最低。为了描述δ偏好的结构决定因素,我们合成了DS1和DS2的25个导数,并研究了它们的构效关系(SAR)。我们的衍生品四个表现出对α6β3δ受体的选择性(29,38,39和41)。对于所有这些化合物,使它们与化合物22区别开的主要因素是其苯甲酰胺基对位的变异。但是,当在GABA存在下测试时,两种化合物(29和39)显示出对另外几种GABA A R的影响。新合成的化合物仍将用作研究α6β3δ受体的有用工具。
Methods and Compositions for Treatment of Scleritis and Related Disorders
申请人:Bedard Patricia W.
公开号:US20080125454A1
公开(公告)日:2008-05-29
The present teachings relate to the field of anti-inflammatory substances and more particularly to compounds that are useful for the treatment of scleritis, a scleritis symptom, or a scleritis-related disorder. In one aspect, methods of treating scleritis, a scleritis symptom, or a scleritis-related disorder generally include administering to a subject a compound of Formula I:
or a pharmaceutically acceptable salt, hydrate or ester thereof, wherein W
1
, W
2
, R
1
, L, X, Y, Z, and n
1
are defined as described herein.
Thieno [2,3-B] pyridine-5-carbonitriles as protein kinase inhibitors
申请人:Boschelli H. Diane
公开号:US20070082880A1
公开(公告)日:2007-04-12
Disclosed are compounds of Formula I:
wherein R
1
, R
2
, R
3
, R
4
, and X, are defined hereinbefore in the specification, which can be useful in the treatment of autoimmune and inflammatory diseases, and processes for producing said compounds.
Novel one-pot pseudo four component reaction: expeditious synthesis of functionalized imidazo[1,2-a]pyridines
作者:Haleh Sanaeishoar、Roya Nazarpour、Fouad Mohave
DOI:10.1039/c5ra10891h
日期:——
A new and efficient one-pot synthesis of imidazo[1,2-a] pyridines is described. A C-3 imine substituent was installed on the imidazopyridine framework under mild conditions to form the corresponding products in good to excellent yields.
Process for the synthesis of compounds for selectin inhibition
申请人:Wang Youchu
公开号:US20070082923A1
公开(公告)日:2007-04-12
The present teachings relate to the field of anti-inflammatory substances, and more particularly to the preparation of compounds that act as antagonists of the mammalian adhesion proteins known as selecting. In some embodiments, the present teachings provide methods for preparing compounds for treating selectin-mediated disorders that have the formula VI:
wherein R
1
, R
2
, R
3
, p, and q are defined herein.
A compound having GPR52 agonist activity or a salt thereof is provided.
The compound can be provided as a preventive/therapeutic agent for schizophrenia or the like. The compound is represented by the following formula:
wherein
A represents —CONR
a
— or —NR
a
CO—,
R
a
represents a hydrogen atom or the like,
B represents a hydrogen atom or the like,
a ring Cy1 represents a six-membered aromatic ring which may have one or more substituents in addition to a group represented by -A-B,
a ring Cy2 represents a six-membered ring which may be substituted with a halogen atom or the like,
a ring Cy3 represents a five- or six-membered ring which may have one or more substituents;
X represents C
1-2
alkylene or the like,
m represents an integer of 0 to 2, and
a ring Cy4 represents a six-membered aromatic ring which may have one or more substituents.