SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS
申请人:GLAXOSMITHKLINE LLC
公开号:US20150152108A1
公开(公告)日:2015-06-04
The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
POLYCYCLIC COMPOUNDS AS LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
申请人:CLARK Ryan
公开号:US20110082164A1
公开(公告)日:2011-04-07
Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
[EN] DIARYLAMIDE-SPIRODIAMINE DERIVATIVE<br/>[FR] DÉRIVÉ DE DIARYLAMIDE-SPIRODIAMINE
申请人:BANYU PHARMA CO LTD
公开号:WO2010147234A1
公开(公告)日:2010-12-23
To provide a melanin concentrating hormone receptor antagonist useful as medicines for central system disorders, cardiovascular disorders and metabolic disorders. Provided is a compound of a formula (I): wherein R1a and R1b each are a hydrogen atom, etc.; R2 is a hydrogen atom, a C1-6 alkyl, etc.; Ar1 is a 6-membered aromatic carbocyclic group or a 6-membered aromatic nitrogen-containing heterocyclic group; Ar2 is a group to be formed by removing two hydrogen atoms from a 6-membered aromatic carbon ring, a 6-membered aromatic nitrogen-containing hetero ring, etc.; Ar3 is a mono- or bi-cyclic aromatic carbocyclic group or aromatic heterocyclic group; m1, m2, m3 and m4 are independently 0, 1, 2, 3 or 4, provided that the total of m1 and m2 is from 2 to 6, and the total of m3 and m4 is from 2 to 6. The compound is useful as medicines for central system disorders, cardiovascular disorders and metabolic 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。)
Kinase Inhibitors
申请人:Wurster A. Julie
公开号:US20070032478A1
公开(公告)日:2007-02-08
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.