[EN] 6,7-DIHYDROPYRAZOLO[1,5-A]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS [FR] COMPOSÉS 6,7-DIHYDROPYRAZOLO[1,5-A] PYRAZIN-4(5H)-ONE ET LEUR UTILISATION COMME MODULATEURS ALLOSTÉRIQUES NÉGATIFS DES RÉCEPTEURS MGLUR2
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。)
[EN] FUSED BICYCLIC COMPOUNDS AS INHIBITORS FOR PI3 KINASE<br/>[FR] COMPOSÉS BICYCLIQUES FUSIONNÉS UTILISÉS COMME INHIBITEURS DE LA PI3 KINASE
申请人:MERCK SERONO SA
公开号:WO2010100144A1
公开(公告)日:2010-09-10
The invention relates to compounds of formula (I) for the regulation of phosphoinositides 3-kinases activity and related diseases.
该发明涉及用于调节磷脂酰肌醇3-激酶活性及相关疾病的化合物(I)的公式。
[EN] SUBSTITUTED BIPHENYL GPR40 MODULATORS<br/>[FR] MODULATEURS DU GPR40 À BIPHÉNYLE SUBSTITUÉ
申请人:AMGEN INC
公开号:WO2009048527A1
公开(公告)日:2009-04-16
The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
Patients susceptible to or suffering from central nervous system disorders (e.g., Alzheimer's disease, Parkinson's disease, Tourette's syndrome, attention deficit disorder or schizophrenia) are treated by administering an effective amount of an aryl substituted olefinic amine compound. Exemplary compounds include (E)-N-methyl-4-\x9b3-(5-benzyloxypyridin)yl!-3-buten-1-amine, (E)-N-methyl-4-\x9b3-(5-phenoxypyridin)yl!-3-buten-1-amine, and (E)-N-methyl-4-\x9b3-(5-phenylpyridin)yl!-3-buten-1-amine.
Pharmaceutical compositions for the treatment of conditions associated
申请人:——
公开号:US05811442A1
公开(公告)日:1998-09-22
Patients suffering from or susceptible to conditions of the vascular or circulatory system, particularly the microvasculature, which conditions are associated with decreased blood flow in regions of microcirculation (e.g., Raynaud's disease and Raynaud's phenomenon) are treated with pharmaceutical compositions incorporating an effective amount of an aryl substituted olefinic amine compound. The compounds incorporated into the pharmaceutical compositions of the present invention exhibit selective activity of to the .beta.2-containing nicotinic acetylcholine receptors and thereby yield beneficial therapeutic effects increasing vascular blood flow in regions of microcirculation.