DERIVATIVES OF HETEROCYCLES WITH 5 MEMBERS, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS
申请人:CHABRIER DE LASSAUNIERE Pierre-Etienne
公开号:US20110172434A1
公开(公告)日:2011-07-14
The invention relates to thiazole, oxazole, imidazole, isoxazole and isoxazoline derivatives of general formula (I)
wherein Het is thiazole, oxazole, imidazole, isoxazole or isoxazoline, n is an integer from 0 to 6, A is notably selected from various optionally substituted aromatic radicals, B is notably hydrogen, alkyl or phenyl, R
1
and R
2
are notably independently hydrogen, alkyl or cycloalkyl and Ω is —NR
46
R
47
or —OR
48
, R
46
and R
47
are notably independently hydrogen, alkyl, cycloalkyl or —(CH
2
)
k
—COOR
51
, R
51
is notably alkyl or haloalkyl and R
48
is notably hydrogen or alkyl.
These compounds have advantageous pharmacological properties which allow their use in therapeutics, notably for treating neurodegenerative disorders or pain.
本发明涉及通式(I)的
噻唑,
噁唑,
咪唑,
异噁唑和
异噁唑啉衍
生物,其中Het为
噻唑,
噁唑,
咪唑,
异噁唑或
异噁唑啉,n为0至6的整数,A特别选择自各种可选取代的芳香基团,B特别为
氢,烷基或
苯基,R1和R2特别独立地为
氢,烷基或
环烷基,Ω为—NR46R47或—OR48,R46和R47特别独立地为
氢,烷基,
环烷基或—(
CH2)k—COOR51,R51特别为烷基或卤代烷基,R48特别为
氢或烷基。这些化合物具有有利的药理学性质,可以在治疗中使用,特别用于治疗神经退行性疾病或疼痛。