摘要:
A phosphodiesterase IV inhibiting cathecol derivatives of the general formula I: ##STR1## or a pharmaceutically acceptable salt thereof in which R1 is C.sub.1-7 alkyl; C.sub.3-7 cycloalkane; phenyl optionally substituted with lower alkyl lower alkoxy, nitro or halogen; pyrimidine optionally substituted with lower alkyl, lower alkoxy, nitro or halogen; or pyridine optionally substituted with lower alkyl, lower alkoxy, nitro or halogen; X, Y and Z are each independently oxygen, nitrogen or sulfur optionally substituted with C.sub.1-7 alkyl, C.sub.3-7 cycloalkane or phenyl; W is oxygen or sulfur is disclosed. In addition, a process for producing the compound of the general formula I and a pharmaceutical composition containing pharmaceutically effective amount of the compound of the general formula I are disclosed.
摘要:
Novel 4,5-diamino pyrimidine derivatives are described by the following general formula I: in which X is a direct bond, C1-4 alkylene, C1-4 alkyleneoxy, C1-4 alkoxyphenyl or phenyl C1-4 alkylene; Y is a direct bond or C1-2 alkyl, R1 is (i) 5-15 membered cyclic or fused heterocompound which includes one or two atoms selected from a group consisting of nitrogen, oxygen and sulfur and which is substituted with one or two substituents selected from a group consisting of hydrogen, halogen, nitro, hydroxy, C1-6 alkyl, C3-6 alkenyl and halogen C1-4 alkoxy, (ii) C4-10 carbocyclic compound or (iii) hydroxy C1-4 alkoxy, R2 is 5-15 membered cyclic or fused heterocompound which includes one or two nitrogen atoms and, optionally, one oxygen or sulfur atom, and which is substituted with one or two substituents selected from a group consisting of hydrogen, hydroxy, halogen, nitro, hydroxy C1-5 alkyl, C1-6 alkyl, C3-6 alkenyl and halogen C1-4 alkoxy; R3 is hydrogen, in which R4 and R5 are each independently selected from a group consisting of hydroxy, C1-6 alkyl, C3-7 cycloalkyl, C3-6 alkenyl, halogen C1-6 alkyl, halogen C2-6 alkenyl and C1-4alkoxy or R4 and R5 represent each independently in which R6 is selected from a group consisting of hydrogen, hydroxy, C1-6 alkyl, C3-6 alkenyl, halogen C1-6 alkyl, halogen, nitro and C1-4 alkoxy.
摘要:
The present invention provides novel cathecol hydrazone derivatives of formula (I) or pharmaceutically acceptable salts thereof, wherein R1 is C1-7 alkyl or C3-7 cycloalkyl; R2 is hydrogen, hydroxy, C1-5 alkyl or —CH2CH2C(═O)NH2; R3 and R4 are independently hydrogen, C1-7 alkyl, —C(═X)—R5, or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one or two selected from a group consisting of halogen, C1-6 alkoxy, nitro, trifluoromethyl, C1-6 alkyl and carboxyl, or R3 and R4 are directly bonded by C3-4 containing oxygen, sulfur or nitrogen to form a heterocyclic ring, X is oxygen, sulfur or NH and R5 is C1-7 alkyl, —NHR6, CONH2 or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one selected from a group consisting of halogen, C1-6 alkoxy, nitrile, trifluoromethyl, C1-6 alkyl and carboxyl, and R6 is hydrogen, hydroxy, NH2, C1-5 alkoxy, C1-5 alkyl, pyridyl or phenyl.
摘要:
The present invention relates to a composition for treatment and prevention of cardiovascular diseases, containing an extract of Lindera obtusiloba. More particularly, the extract of Lindera obtusiloba strongly inhibits NAD(P)H oxidases, which are the main cause of vascular diseases, and at the same time, regulates contraction and relaxation of vascular smooth muscles to manifest a potent vasorelaxant effect, thereby improving the blood pressure regulation and vascular endothelial dysfunction. Therefore, a composition containing this as an active ingredient can be usefully utilized as a pharmaceutical product or health functional food product for the prevention and treatment of cardiovascular diseases.
摘要:
The present invention relates to a composition for treatment and prevention of cardiovascular diseases, containing an extract of Lindera obtusiloba. More particularly, the extract of Lindera obtusiloba strongly inhibits NAD(P)H oxidases, which are the main cause of vascular diseases, and at the same time, regulates contraction and relaxation of vascular smooth muscles to manifest a potent vasorelaxant effect, thereby improving the blood pressure regulation and vascular endothelial dysfunction. Therefore, a composition containing this as an active ingredient can be usefully utilized as a pharmaceutical product or health functional food product for the prevention and treatment of cardiovascular diseases.