[EN] BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS [FR] DÉRIVÉS HÉTÉROCYCLIQUES BICYCLIQUES ET LEUR UTILISATION EN TANT QUE MODULATEURS DE GPR119
NOVEL DISUBSTITUTED 3,4-DIAMINO-3-CYCLOBUTENE-1,2-DIONE COMPOUNDS FOR USE IN THE TREATMENT OF CHEMOKINE-MEDIATED DISEASES
申请人:GALDERMA RESEARCH & DEVELOPMENT
公开号:US20140296254A1
公开(公告)日:2014-10-02
Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are described that correspond to general formula (I). Also described, are pharmaceutical compositions that include these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases.
A unique C(sp3)–H/C(sp3)–H dehydrocoupling of N-benzylimines with saturated heterocycles is described. Using super electron donor (SED) 2-azaallyl anions and aryl iodides as electron acceptors, single-electron-transfer (SET) generates an aryl radical. Hydrogen atom transfer (HAT) from saturated heterocycles or toluenes to the aryl radical generates alkyl radicals or benzylic radicals, respectively
The present invention relates to a compound represented by Formula (I):
(wherein Ar
1
represents an imidazolyl group which may be substituted with 1 to 3 substituents; Ar
2
represents a pyridinyl group, a pyrimidinyl group, or a phenyl group which may be substituted with 1 to 3 substituents; X
1
represents (1) —C≡C— or (2) a double bond etc. which may be substituted; R
1
and R
2
represent, for example, a C1-6 alkyl group or C3-8 cycloalkyl group which may be substituted)
or a pharmacologically acceptable salt thereof and to the use thereof as pharmaceutical agents. The object of the present invention is to find a therapeutic or preventive agent for diseases caused by Aβ. According to the present invention, a therapeutic or preventive agents for diseases caused by Aβ can be provided.
The present invention relates to a compound represented by Formula (I):
(wherein Ar
1
represents an imidazolyl group which may be substituted with 1 to 3 substituents; Ar
2
represents a pyridinyl group, a pyrimidinyl group, or a phenyl group which may be substituted with 1 to 3 substituents; X
1
represents (1) —C≡C— or (2) a double bond etc. which may be substituted; R
1
and R
2
represent, for example, a C1-6 alkyl group or C3-8 cycloalkyl group which may be substituted) or a pharmacologically acceptable salt thereof and to the use thereof as pharmaceutical agents.
Compounds of Formula I
wherein R
1
, A, R
2
, n, R
3
, m, R
4
, R
5
and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.