Synthesis and structure–activity relationships of quaternary ammonium cephalosporins with 3-pyrazolylpyridinium derivatives
摘要:
Cephalosporins with 3-pyazolylpyridinium at C-3 position, which is supposed to exhibit synergic activity of ceftazidime and cefoselis, were synthesized and their antibacterial activity against Gram-positive and Gram-negative was inspected. (C) 2000 Elsevier Science Ltd. All rights reserved.
Synthesis and structure–activity relationships of quaternary ammonium cephalosporins with 3-pyrazolylpyridinium derivatives
摘要:
Cephalosporins with 3-pyazolylpyridinium at C-3 position, which is supposed to exhibit synergic activity of ceftazidime and cefoselis, were synthesized and their antibacterial activity against Gram-positive and Gram-negative was inspected. (C) 2000 Elsevier Science Ltd. All rights reserved.
[EN] 2, 6 BISHETEROARYL-4-AMINOPYRIMIDINES AS ADENOSINE RECEPTOR ANTAGONISTS<br/>[FR] 2, 6-BISHETEROARYL-4-AMINOPYRIMIDINES UTILISEES EN TANT QU'ANTAGONISTES DES RECEPTEURS DE L'ADENOSINE
申请人:ALMIRALL PRODESFARMA SA
公开号:WO2005058883A1
公开(公告)日:2005-06-30
4-Aminopyrimidine derivatives of formula (I) FORMULA heteroaryl groups, including pharmaceutically acceptable salts thereof, wherein R1 and R2 are adenosine A2A receptor antagonists useful in the treatment of movement disorders such as Parkinson's disease.
2,6 Bisheteroaryl-4-Aminopyrimidines as Adenosine Receptor Antagonists
申请人:Crespo Crespo Maria Isabel
公开号:US20080058356A1
公开(公告)日:2008-03-06
4-Aminopyrimidine derivatives of formula (I) FORMULA heteroaryl groups, including pharmaceutically acceptable salts thereof, wherein R
1
and R
2
are adenosine A
2A
receptor antagonists useful in the treatment of movement disorders such as Parkinson's disease.
The invention relates to 5-isothiazolamine derivatives having the formula
in which R1 is hydrogen, methyl, or ethyl, R2 and R3 are independently selected from hydrogen and alkyl, and the dotted line represents an optional bond, or a pharmaceutically acceptable acid addition salt thereof.
The compounds have α2-adrenergic agonistic properties with little cardiovascular side-effects and minimal or no dopaminergic and cholinergic activity.