Ago-allosteric modulators of human glucagon-like peptide 2 receptor
摘要:
Glucagon-like peptide 2 (GLP-2) is an intestinotropic peptide that binds to GLP-2 receptor (GLP-2R), a class-B G protein-coupled receptor (GPCR). Few synthetic agonists have been reported so far for class-B GPCRs. Here, we report the first scaffold compounds of ago-allosteric modulators for human GLP-2R, derived from methyl 2-{[(2Z)-2-(2,5-dichlorothiophen-3-yl)-2-(hydroxyimino) ethyl] sulfanyl}benzoate (compound 1). (C) 2012 Elsevier Ltd. All rights reserved.
The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
There is provided a morpholine derivative represented by General Formula [1A] or a salt thereof.
(In the formula, a ring A represents a ring represented by General Formula [I]; * represents a bonding position; Z
2
represents CH or the like; Z
1
represents CR
6
or the like; R
6
represents a hydrogen atom or the like; X
1
represents CHR
7
or the like; R
7
represents a hydrogen atom or the like; X
2
represents CH
2
or the like; R
1
and R
2
are the same as or different from each other, and each of R
1
and R
2
represents a hydrogen atom or the like; R
3
, R
4
, and R
5
are the same as or different from each other, and each of R
3
, R
4
, and R
5
represents a hydrogen atom, NR
a
R
b
, or the like; and each of R
a
and R
b
represents a hydrogen atom, a C
1-8
alkyl group which may have a substituent, or the like.)
提供一种由通用式[1A]表示的吗啉衍生物或其盐。
(在该式中,环A代表由通用式[I]表示的环;*代表连接位置;Z
2
代表CH或类似物;Z
1
代表CR
6
或类似物;R
6
代表氢原子或类似物;X
1
代表CHR
7
或类似物;R
7
代表氢原子或类似物;X
2
代表CH
2
或类似物;R
1
和R
2
相同或不同,且R
1
和R
2
中的每一个代表氢原子或类似物;R
3
,R
4
和R
5
相同或不同,且R
3
,R
4
和R
5
中的每一个代表氢原子,NR
a
R
b
或类似物;R
a
和R
b
中的每一个代表氢原子,可能具有取代基的C
1-8
烷基基团,或类似物。)
FUSED PYRIDINES AS KINASE INHIBITORS
申请人:BRISTOL-MYERS SQUIBB COMPANY
公开号:US20180141956A1
公开(公告)日:2018-05-24
The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
Fused Heterocyclic Compounds as Ion Channel Modulators
申请人:Kobayashi Tetsuya
公开号:US20120010192A1
公开(公告)日:2012-01-12
The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I:
wherein R
1
, R
2
, R
3
, R
4
, and R
5
are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
SUBSTITUTED SULPHONAMIDES FOR CONTROLLING ANIMAL PESTS
申请人:BAYER CROPSCIENCE AKTIENGESELLSCHAFT
公开号:US20200288710A1
公开(公告)日:2020-09-17
The present invention relates to the use of a compound of the general formula (I)
in which M and D have the meanings given in the description for controlling animal pests.