6-Thienyl and 6-phenylimidazo[2,1-b]thiazoles as inhibitors of mitochondrial NADH dehydrogenase
摘要:
Starting from the potent inhibitory effect of the previously described 2 methyl-6-(2-thienyl)imidazo[2,1-b]thiazol on mitochondrial complex I, we prepared a series of derivatives in order to study the effect of a different substitution at the positions 2, 5 and 6. The replacement of the thienyl group at position 6 with a phenyl group does not modify the biological behaviour of the lead compound, whereas the shift of the methyl group from position 2 to position 5 yields a compound devoid of inhibitory effects. In both the 6-thienyl and 6-phenyl series, the lengthening of the chain at position 2 has provided useful information to outline the structural determinants of the ubiquinone antagonist action in imidazothiazole derivatives. (C) 1999 Editions scientifiques et medicales Elsevier SAS.
[EN] THIAZOLE COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS<br/>[FR] COMPOSES THIAZOLE UTILES POUR LE TRAITEMENT DES MALADIES NEURODEGENERATIVES
申请人:PFIZER PROD INC
公开号:WO2004033439A1
公开(公告)日:2004-04-22
The invention provides compounds of Formula (I): wherein R1, R2, R3, R4, R6, R7, and A are as defined. Compounds of Formula (I) have activity inhibiting production of Aß-peptide. The invention also provides pharmaceutical compositions and methods for treating diseases, for example Alzheimer's disease, in mammals comprising compounds of Formula (I).
2-Aminothiazole and its 5-substituted derivatives were obtained in one step from thiourea and an aldehyde by reaction with sulfuryl chloride, bromine, iodine or nitric acid.
通过与硫酰氯,溴,碘或硝酸反应,从硫脲和醛一步获得2-氨基噻唑及其5-取代的衍生物。
Thiazole compounds for treatment of neurodegenerative disorders
申请人:Pfizer Inc
公开号:US20040152747A1
公开(公告)日:2004-08-05
The invention provides compounds of Formula I:
1
wherein R
1
, R
2
, R
3
, R
4
, R
6
, R
7
, and A are as defined. Compounds of Formula I have activity inhibiting production of A&bgr;-peptide. The invention also provides pharmaceutical compositions and methods for treating diseases, for example Alzheimer's disease, in mammals comprising compounds of Formula I.
Novel benzamidine derivatives, process for the preparation thereof and pharmaceutical composition comprising the same
申请人:Lee Jin Soo
公开号:US20100240890A1
公开(公告)日:2010-09-23
The present invention relates to novel benzamidine derivatives, process for the preparation thereof and pharmaceutical composition comprising the same. The novel benzamidine derivatives of the present invention are useful for the prevention and treatment of osteoporosis, bone fractures and allergic inflammatory diseases.