摘要:
.alpha.-(2,6-dimethyl-4-carboxyphenyl)-2-methyl-5-(1-imidazolyl)-benzenemethanol, pharmaceutically acceptable metal salts forms thereof, acid addition salt forms thereof, amino acid addition salt forms thereof, hydrate forms thereof and mixtures thereof.Such compounds have inhibitory activities on biosynthesis of thromboxane A.sub.2, inhibitory activities on platelet aggregation, vasodilative activities and protective effects against liver disorders.
摘要:
An imidazole derivative of the formula: ##STR1## wherein each of R.sup.1 and R.sup.4 is a hydrogen atom or a lower alkyl group; each of R.sup.2 and R.sup.3 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an aralkyloxy group, a nitro group or an amino group; A is --O--, --S--, --CH.dbd.CH-- pr --CH.dbd.N--; Z is an aryl group, a thienyl group, a pyridyl group or a furyl group, in which definition these aromatic (heterocyclic) rings may have 1 to 3 substituents, each substituent being independently selected from a halogen atom, a lower alkyl group, a cyclic alkyl group, a lower alkoxy group, a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group, a carboxy-lower-alkoxy group, a di-lower-alkylamino-lower-alkoxy group and a nitro group; and a pharmaceutically acceptable acid addition salt thereof, a method for preparing the same and a pharmaceutical composition containing such compound. Such compounds have inhibitory activities on biosynthesis of thromboxane A.sub.2, inhibitory activities on platelet aggregation, vasodilative activities and protective effects on liver disorders.
摘要:
Compounds of the formula: ##SPC1##WhereinOf X.sup.1 and X.sup.2 is a hydrogen atom, a halogen atom or an alkyl group having 1 to 4 carbon atoms;R.sup.1 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, an alkynyl group having 2 to 4 carbon atoms or a group -B.sup.1 -R.sup.3 (wherein B.sup.1 is an alkylene group having 1 to 4 carbon atoms, and R.sup.3 is a carboxyl group, an alkoxycarbonyl group in which the alkoxy moiety has 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a di-alkyl-amino group in which each alkyl moiety has 1 to 4 carbon atoms);R.sup.2 is an alkyl group having 1 to 4 carbon atoms or a group -B.sup.2 -R.sup.4 (wherein B.sup.2 is an alkylene group having 2 to 4 carbon atoms, and R.sup.4 is a carboxyl group or a di-alkyl-amino group in which each alkyl moiety has 1 to 4 carbon atoms);A is a methylene group or a carbonyl group;Y is an oxygen atom, a sulfur atom or an alkyl-imino group in which the alkyl moiety has 1 to 4 carbon atoms; andRing P is a pyridine ring; andPharmaceutically acceptable salts thereof are disclosed.They are useful as anti-inflammatory agents, analgesics, antipyretics and antirheumatics.
摘要:
Pyridine derivatives of the formula: ##STR1## or pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represents hydrogen atom or lower alkyl group, or R.sup.1 and R.sup.2, or R.sup.3 and R.sup.4 together with the adjacent nitrogen atom form a heterocycle, A.sup.1 and A.sup.2 are the same or different and each represents alkylene or hydroxy-substituted alkylene group, Y.sup.1 and Y.sup.2 are the same or different and each represents oxygen or sulfur atom, and Z represents ##STR2## These compounds show pharmacological activities such as potentiating activity for leukocyte phagocytosis, potentiating activity for macrophage phagocytosis, potentiating activity for the production of rosette forming cells in the spleen and anti-adjuvant arthritis activity, and are useful as medicines.
摘要:
1H-Tetrazole derivatives of the formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein the ring P is pyridine ring; A is carbonyl, methylene or C.sub.2-4 alkylidene; Y is oxygen, sulfur or --N(R.sup.1)-- wherein R.sup.1 is hydrogen or C.sub.1-4 alkyl; each of X.sup.1 and X.sup.2 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl or substituted phenyl, any substitutent on the phenyl being halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethy; and R is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, hydroxy-C.sub.1-4 alkyl, C.sub.1-4 alkoxy-C.sub.1-4 alkyl, carboxy-C.sub.1-4 alkyl, C.sub.1-4 alkoxycarbonyl-C.sub.1-4 alkyl or substituted or unsubstituted amino-C.sub.1-4 alkyl, any substituted amino being C.sub.1-4 alkyl- or di-C.sub.1-4 alkyl-amino, piperidino, 1-pyrrolidinyl, morpholino, 1-piperazinyl and 4-C.sub.1-4 alkyl-1-piperazinyl; are useful as antiallergic agents.
摘要:
Substituted alkanoic acids and derivatives thereof of the formula: ##SPC1##Wherein each of X.sup.1 and X.sup.2 is a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms; each of R.sup.1 and R.sup.2 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; A is a carbonyl group, a methylene group or an alkylidene group having 2 to 4 carbon atoms; Y is --O--, --S-- or --N(R)-- [wherein R is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms]; Z is OH or Q--B--N(R.sup.3)(R.sup.4) [wherein Q is O (oxygen atom) or NH, B is an alkylene group having 1 to 4 carbon atoms and each of R.sup.3 and R.sup.4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, or R.sup.3 and R.sup.4 together with the adjacent nitrogen atom form a saturated heterocycle selected from the group consisting of pyrrolidine, piperidine, morpholine, piperazine and piperazine substituted by an alkyl group having 1 to 4 carbon atoms at the 4-position]; and ring P represents a pyridine or a pyridine N-oxide ring; and pharmaceutically acceptable salts thereof are useful as antirheumatics, analgesics, antipyretics and anti-inflammatory agents.
摘要:
Heterocyclic compounds of the formula: ##SPC1##Wherein A is a carbonyl group, a methylene group or an alkylidene group having 2 to 4 carbon atoms; B is an oxygen atom, a sulfur atom or --N(R')-- (wherein R' is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms); each of R.sup.1 and R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a phenyl group which may be substituted by a halogen atom, an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms; X is an alkyl group having 1 to 4 carbon atoms, a cycloalkyl group having 3 to 6 carbon atoms or OM (wherein M is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, a metal atom or NH.sub.4); and ring P represents a pyridine ring, are useful as anti-allergic agents.
摘要:
A novel pyridine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a salt thereof which exhibit inhibitory activity or prolylendopeptidase and a pharmaceutical use thereof are disclosed.
摘要:
Benzopyranopyridineacetic acid ester compounds of the formula: ##STR1## wherein R.sup.1, and R.sup.2 and R.sup.3 independently represent hydrogen or C.sub.1-4 alkyl; and n is 1 or 2, and their pharmaceutical use are disclosed.These compounds possess antiinflammatory, analgesic and antipyretic activities with less adverse action on the gastrointestinal tract.
摘要:
A pyrazolopyridine compound of the formula: ##STR1## or a salt thereof, wherein each symbol is as defined in the specification. Said compounds exhibit antiinflammatory, analgesic, antipyretic, antiallergic, antiarthritic, antirheumatic activities or inhibitory activities on platelet aggregation.