摘要:
Novel compounds, 3,5-di-tert-butylstyrene derivatives and their salts, are disclosed, which derivatives are represented by the general formula: ##STR1## wherein R.sup.1 stands for an acyloxy group represented by R.sup.3 COO (R.sup.3 is a hydrogen atom or an alkyl group with C.sub.1 -C.sub.6), an alkoxyl group of R.sub.4 O (R.sup.4 is an alkyl group with C.sub.1 -C.sub.4), a hydroxyl group, or a hydrogen atom; R.sup.2 stands for ##STR2## (R.sup.5 is a hydrogen atom or an alkyl group with C.sub.1 -C.sub.3 and X.sup.1 is CH.sub.2 or an oxygen atom), ##STR3## (R.sup.5 and X.sup.1 are each the same as defined above), or ##STR4## (X.sup.2 is an oxygen or sulfur atom). There are also disclosed an anti-inflammatory, analgesic, and antipyretic pharmaceutical composition and an anti-platelet aggregation pharmaceutical composition, both pharmaceutical compositions comprising the foregoing 3,5-di-tert-butylstyrene derivative or its pharmaceutically acceptable salt as an active ingredient in association with pharmaceutical excipients.
摘要:
A new anti-inflammatory, analgesic, and antipyretic pharmaceutical composition is disclosed which contains a 3,5-di-tert-butyl-4-hydroxystyrene derivative of the formula: ##STR1## wherein R.sup.1 stands for a group represented by COR.sup.3 [R.sup.3 denotes a group of OR.sup.4 (R.sup.4 is a hydrogen atom or an alkyl group with C.sub.1 .about.C.sub.4), an alkyl group with C.sub.1 .about.C.sub.3, a phenyl group, or an amino group], a nitro group, or an alkylsulfonyl group represented by SO.sub.2 R.sup.5 (R.sup.5 is an alkyl group with C.sub.1 .about.C.sub.3); and R.sup.2 stands for a hydrogen atom, an alkyl group with C.sub.1 .about.C.sub.4, a hydroxyalkyl group with C.sub.1 .about.C.sub.4, a cyano group, or an acyl group represented by COR.sup.6 (R.sup.6 is an alkyl group with C.sub.1 .about.C.sub.3),or its pharmaceutically acceptable salt as an active ingredient in association with pharmaceutical excipients. The pharmaceutical composition has excellent anti-inflammatory, analgesic, and antipyretic activities and low toxicity.
摘要:
A hydroxystyrene derivative represented by the formula (I): ##STR1## wherein when R.sup.1 and R.sup.2 : phenyl group, benzyl group or phenethyl group, or R.sup.1 : R.sup.5 O- (R.sup.5 : H, a C.sub.1 to C.sub.5 alkyl group or benzyl group) and R.sup.2 : benzyl group or PhSCH.sub.2, R.sup.3 and R.sup.4 are taken together to represent --CONH--CS--S--, ##STR2## (X.sup.1 : H, a halogen, methyl group, ethyl group, R.sup.7 O-- (R.sup.7 : methyl or ethyl group), nitro group, aminosulfonyl group or amino group, m.sup.1 : 1 or 2), pyridyl group, furyl group or thienyl group, n.sup.1 : an integer of 0 to 3); when R.sup.1 and R.sup.2 : phenyl group, benzyl group or phenethyl group, or R.sup.1 : R.sup.5 O-- (R.sup.5 : as defined above) and R.sup.2 : benzyl group, R.sup.3 : cyano group and R.sup.4 : a carbamoyl group, or R.sup.3 and R.sup.4 are taken together to represent --CO--Y--CH.sub.2 CH.sub.2 -- (Y: O or --NH--) or ##STR3## and when R.sup.1 and R.sup.2 : a C.sub.1 to C.sub.3 alkyl group, R.sup.3 and R.sup.4 are taken together to represent ##STR4## (n.sup.1, R.sup.6 : as defined above), or a salt thereof. The hydroxystyrene derivative or a salt thereof is a compound which is useful as an active ingredient of an antiallergic agent, a 5-lipoxygenase inhibiting agent, an antibacterial agent, a tyrosine kinase inhibiting agent, an ultraviolet absorber or a reverse transcriptase inhibiting agent, and also is useful as an intermediate for preparing various organic compounds.
摘要:
A hydroxystyrene derivative represented by the formula (I): ##STR1## wherein when R.sup.1 and R.sup.2 : phenyl group, benzyl group or phenethyl group, or R.sup.1 : R.sup.5 O-- (R.sup.5 : H, a C.sub.1 to C.sub.5 alkyl group or benzyl group) and R.sup.2 : benzyl group or PhSCH.sub.2, R.sup.3 and R.sup.4 are taken together to represent --CONH--CS--S--, ##STR2## (X.sup.1 : H, a halogen, methyl group, ethyl group, R.sup.7 O-- (R.sup.7 : methyl or ethyl group), nitro group, aminosulfonyl group or amino group, m.sup.1 : 1 or 2), pyridyl group, furyl group or thienyl group, n.sup.1 : an integer of 0 to 3); when R.sup.1 and R.sup.2 : phenyl group, benzyl group or phenethyl group, or R.sup.1 : R.sup.5 O-- (R.sup.5 : as defined above) and R.sup.2 : benzyl group, R.sup.3 : cyano group and R.sup.4 : a carbamoyl group, or R.sup.3 and R.sup.4 are taken together to represent --CO--Y--CH.sub.2 CH.sub.2 -- (Y: O or --NH--) or ##STR3## and when R.sup.1 and R.sup.2 : a C.sub.1 to C.sub.3 alkyl group, R.sup.3 and R.sup.4 are taken together to represent ##STR4## (n.sup.1, R.sup.6 : as defined above), or a salt thereof. The hydroxystyrene derivative or a salt thereof is a compound which is useful as an active ingredient of an antiallergic agent, a 5-lipoxygenase inhibiting agent, an antibacterial agent, a tyrosine kinase inhibiting agent, an ultraviolet absorber or a reverse transcriptase inhibiting agent, and also is useful as an intermediate for preparing various organic compounds.
摘要:
A hydroxystyrene derivative represented by the formula (I): ##STR1## wherein when R.sup.1 and R.sup.2 : phenyl group, benzyl group or phenethyl group, or R.sup.1 : R.sup.5 O-- (R.sup.5 : H, a C.sub.1 to C.sub.5 alkyl group or benzyl group) and R.sup.2 : benzyl group or PhSCH.sub.2, R.sup.3 and R.sup.4 are taken together to represent --CONH--CS--S--, ##STR2## (X.sup.1 : H, a halogen, methyl group, ethyl group, R.sup.7 O-- (R.sup.7 : methyl or ethyl group), nitro group, aminosulfonyl group or amino group, m.sup.1 : 1 or 2), pyridyl group, furyl group or thienyl group, n.sup.1 : an integer of 0 to 3); when R.sup.1 and R.sup.2 : phenyl group, benzyl group or phenethyl group, or R.sup.1 : R.sup.5 O-- (R.sup.5 : as defined above) and R.sup.2 : benzyl group, R.sup.3 : cyano group and R.sup.4 : a carbamoyl group, or R.sup.3 and R.sup.4 are taken together to represent --CO--Y--CH.sub.2 CH.sub.2 -- (Y: O or --NH--) or ##STR3## and when R.sup.1 and R.sup.2 : a C.sub.1 to C.sub.3 alkyl group, R.sup.3 and R.sup.4 are taken together to represent ##STR4## (n.sup.1, R.sup.6 : as defined above), or a salt thereof. The hydroxystyrene derivative or a salt thereof is a compound which is useful as an active ingredient of an antiallergic agent, a 5-lipoxygenase inhibiting agent, an antibacterial agent, a tryosine kinase inhibiting agent, an ultraviolet absorber or a reverse transcriptase inhibiting agent, and also is useful as an intermediate for preparing various organic compounds.
摘要:
A hydroxystyrene derivative represented by the formula (I): ##STR1## Wherein when R.sup.1 and R.sup.2 : phenyl group, benzyl group or phenethyl group, or R.sup.1 : R.sup.5 O--(R.sup.5 : H, a C.sub.1 to C.sub.5 alkyl group or benzyl group) and R.sup.2 : benzyl group or PhSCH.sub.2, R.sup.3 and R.sup.4 are taken together to represent --CONH--CS--S--, ##STR2## (X.sub.1 : H, a halogen, methyl group, ethyl group, R.sup.7 O--(R.sup.7 : methyl or ethyl group), nitro group, aminosulfonyl group or amino group, m.sup.1 : 1 or 2), pyridyl group, furyl group or thienyl group, n.sup.1 : an integer of 0 to 3); when R.sup.1 and R.sup.2 : phenyl group, benzyl group or phenethyl group, or R.sup.1 : R.sup.5 O--(R.sup.5 : as defined above) and R.sup.2 : benzyl group, R.sup.3 : cyano group and R.sup.4 : a carbamoyl group, or R.sup.3 and R.sup.4 are taken together to represent --CO--Y--CH.sub.2 CH.sub.2 --(Y: O or --NH--) or ##STR3## and when R.sup.1 and R.sup.2 : a C.sub.1 to C.sub.3 alkyl group, R.sup.3 and R.sup.4 are taken together to represent ##STR4## (n.sup.1, R.sup.6 : as defined above), or a salt thereof. The hydroxystyrene derivative or a salt thereof is a compound which is useful as an active ingredient of an antiallergic agent, a 5-lipoxybenase inhibiting agent, an antibacterial agent, a tyrosine kinase inhibiting agent, an ultraviolet absorber or a reverse transcriptase inhibiting agent, and also is useful as an intermediate for preparing various organic compounds.
摘要:
A 3-phenylthiomethylstyrene derivative having the general formula (1): ##STR1## or salt thereof with a base, when X is hydroxyl group, R.sup.1 is hydrogen atom or R.sup.2 is hydrogen atom, a process for preparing the 3-phenylthiomethylstyrene derivative (1), and an antiallergic agent and a tyrosinekinase inhibiting agent containing the 3-phenylthiomethylstyrene derivative (1) as an effective component. The compound (1) of the present invention is a useful intermediate for preparing various organic compounds, and has excellent antiallergic and tyrosinekinase inhibiting activities.
摘要:
A method for treatment of diseases caused by Chlamydia infection is disclosed comprising administering a rifamycin of the formula (I): ##STR1## wherein R.sup.1 is hydrogen atom or acetyl, and X is oxygen, sulfur or a group NR, in which R is hydrogen, an alkyl group having 1 to 7 carbon atoms or a group of the formula (II): ##STR2## in which n is an integer of 1 to 3; or a physiologically acceptable salt thereof.
摘要:
Antibacterial compositions comprising (1) a rifamycin derivative represented by the formula (I) or its physiologically acceptable salt, and (2) a proton pump inhibitor (a) or a bismuth preparation (b) wherein the components (1) and (2) are used in such amounts as producing a synergistic effect against Helicobacter pylori, drugs and remedies for digestive organ diseases which contain the antibacterial compositions, process for producing them, and pharmaceutical preparations related to the antibacterial compositions. The compositions can be administered to patients with digestive diseases caused by infection of Helicobacter pylori in a smaller dose and at a lower administration frequency as compared with conventional remedies.
摘要:
A new antibiotic designated as auromomycin is prepared from the culture broth of Streptomyces macromomyceticus, a macromomycin-producing strain, as yellow crystals. Auromomycin is recovered in pure form from the culture broth by using hydrophobic chromatography with Octyl Sephalose CL-4B or Phenyl Sepharose CL-4B.