摘要:
Compounds of the general formula (I), wherein R is hydrogen, halogen, C₁₋₄alkyl, C₁₋₄alkoxy or a C₁₋₄acylamino group; and R₁ is hydrogen or a carboxyl-protective group, in the E and/or Z configuration, as well as their salts, show both a cytoprotective effect and anti-inflammatory action. Their toxicity is low.
摘要:
Known acrylic acid derivatives of formula wherein n is an integer of from 0 to 2, R represents a hydrogen, an alkaline or an alkaline earth metal atom, or a C₁₋₄alkyl-group, and R¹ represents a hydrogen or a halogen atom or a C₁₋₄-alkyl, a C₁₋₄alkoxy or a nitro group have useful pharmaceutical activities, in particular cytoprotective and optionally antiulcer activities. They can be used in the treatment and prevention of ulceration in the digestive tract of mammals, inclusive men.
摘要:
The present invention relates to a compound of formula (I) wherein R' represents methyl or a group of the formula R 3 -NH-/CH 2 ) 4 - wherein R 3 is hydrogen or a protective group compatible with the peptide bond, R 2 represents hydrogen, a protective group compatible with the peptide bond or a cation derived from an organic or inorganic base; pharmaceutically acceptable salts and diastereomers thereof. The compounds of the invention are useful for inhibiting the effect of the angiotensin-converting enzyme and they can be used in therapy as blood pressure reducing agents and for the treatment of cardiac failure and glaucoma.
摘要:
57 The present invention relates to optically active or racemic tetrahydro-1,2,4-oxadiazine-5-thione derivatives, to methods for their preparation, and pharmaceutical compositions containing the said compounds. Methods for the anticonvulsive treatment of mammals, especially human beings are described. The compounds of the formula I have similar activity to diphenyl hydantoin but their toxicity is much lower.
摘要:
The invention relates to new 1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizin-1-yl-alkanecarboxylic acid amides of the general formula (I), wherein R, and R 2 represent a hydrogen or halogen atom, or a hydroxyl, nitro or C 1-4 alkoxy group; R 3 and R 4 represent a hydrogen atom or a C 1-4 alkyl group; R 5 and R 6 represent a hydrogen atom, C 1-8 alkyl group, C 3-8 alkenyl or cycloalkyl group, aryl or aralkyl group, heteroaryl or heteroaralkyl goup containing oxygen, nitrogen or sulphur atom, all these goups being optionally substituted; or R 5 and R 6 together represent a,w-alkyl group, wherein one carbon atom may optionally be replaced by an oxygen or nitrogen atom; and G means a C 1-4 straight chained alkylidene group, as well as to their therapeutically useful acid addition salts and pharmaceutical compositions containing these compounds. Furthermore, the invention relates to a process for preparing these compounds and compositions. The compounds of the general formula (I) have valuable therapeutic properties, namely vasodilatory, spasmolytic, antiarrhythmic and gastrocytoprotective effects. The gastrocytoprotective effect is particularly important.
摘要:
The present invention relates to a compound of formula (I) wherein
R' represents methyl or a group of the formula R 3 -NH-/CH 2 ) 4 - wherein R 3 is hydrogen or a protective group compatible with the peptide bond, R 2 represents hydrogen, a protective group compatible with the peptide bond or a cation derived from an organic or inorganic base; pharmaceutically acceptable salts and diastereomers thereof.
The compounds of the invention are useful for inhibiting the effect of the angiotensin-converting enzyme and they can be used in therapy as blood pressure reducing agents and for the treatment of cardiac failure and glaucoma.
摘要:
The invention relates to fodder additives comprising a compound inducing the microsomal enzyme system of the liver, such as a compound of the formula (I) wherein
R i , R 2 and R 3 which may be the same or different represent hydrogen, halogen, trihalomethyl, or alkyl or alkoxy group each containing from 1 to 6 carbon atoms; R 4 is phenyl, dialkylaminocarbonyl or alkoxycarbonyl having from 1 to 6 carbon atoms in the alkyl and alkoxy moieties, respectively; R 5 is hydrogen or methyl, or together with R 4 and the nitrogen atom to which they are attached forms a heterocyclic ring having up to 8 members; n is an integer 1, 2, 3, 4 or 5; m is 0 or 1; a is 0 or 1,
with the proviso that if a = 0, R 1 is trihalomethyl and R 2 and R 3 both are hydrogen. The compounds are preferably used in amount of 0.5 to 99% by weight, in admixture with a conventional carrier and/or additive and optionally at least one further active ingredient conventionally used in the animal husbandry. The enzyme-inducing compounds used according to the invention accelerate the elimination of various xenobiotics metabolizing in the iiver.