45515-22-8Relevant academic research and scientific papers
Pyrazole compounds and their use as antidiabetes agents
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, (2008/06/13)
The present invention provides a pyrazole compound that has liver glycogen phosphorylase inhibitory activity and is useful as a therapeutic or prophylactic agent for diabetes, the pyrazole compound represented by the following general formula (I): wherein Ring Q represents an aryl or heteroaromatic group, R1 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group or a C1-6 alkoxy group, R2 represents a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or an azido group, R3 represents a halogen atom, a hydroxyl group, a C1-6 alkyl group, a halo C1-6 alkyl group, a C1-6 alkoxy group, an azido group, an amino group, an acylamino group or a C1-6 alkylsulfonylamino group, R4 and R5 are identical with or different from each other and represent a hydrogen atom, a substituted or unsubstituted C1-6 alkyl group, a C3-8 cycloalkyl group, a substituted or unsubstituted saturated heterocyclic group, a substituted or unsubstituted aryl group, a C7-14 aralkyl group, a heteroaromatic group, or the like, or a pharmacologically acceptable salt thereof.
PYRAZOLE COMPOUND AND THERAPEUTIC AGENT FOR DIABETES COMPRISING THE SAME
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Page/Page column 252, (2008/06/13)
A pyrazole compound represented by the general formula (I) or a salt thereof which has a hepatic glycogen phosphorylase inhibitory activity and therefore is useful as a therapeutic or prophylactic agent for diabetes or a pharmacologically salt thereof : wherein the ring Q represents an aryl group or an aromatic heterocyclic group; R1 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group or a C1-6 alkoxy group; R2 represents a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or an azide group; R3 represents a halogen atom, a hydroxyl group, a C1-6 alkyl group, a halo-C1-6 alkyl group, a C1-6 alkoxy group, an azide group, an amino group, an acylamino group or a C1-6 alkylsulfonylamino group; R4 and R5 independently represent a hydrogen atom, a C1-6 alkyl group which may be substituted, a a C3-8 cycloalkyl group, a saturated heterocyclic group which may be substituted, an aryl group which may be substituted, a C7-14 aralkyl group, an aromatic heterocyclic group or the like.
Synthesis of oxazolyl-substituted morpholinium salts
Boulos, John,Stujenske, Christina
, p. 443 - 445 (2007/10/03)
Morpholinium salts coupled to oxazolyl moieties have been synthesized via nucleophilic substitution of a series of oxazolyl chlorides with morpholine. The oxazole moieties were first synthesized and then coupled with morpholine. The corresponding hydrochloride and methyl iodide salts were obtained, purified, characterized and then tested for muscarinic receptor binding affinity. Biological test results from MDS Pharma Services revealed no significant muscarinic receptor affinity.
