摘要:
The invention relates to Δ¹⁴-16α,17-dihydroxypregnane derivatives of general formula (I),
wherein A represents a hydrogen atom, or hydroxyl or trifluoroacetoxy group; X represents a hydrogen or halogen atom with the proviso that if A is a hydrogen atom, X is also a hydrogen atom; R represents a hydrogen atom, a benzoyl or C₁₋₈ alkanoyl group; and --- represents a single or double bond between the two adjacent carbon atoms, as well as pharmaceutical compositions containing these compounds and a process for their preparation. The compounds of general formula (I) possess valuable antiinflammatory effects and thus may be used as active ingredients in antiinflammatory pharmaceutical compositions. They may also be useful in the preparation of other therapeutically useful steroid derivatives.
摘要:
Novel acrylic amide derivative of the formula wherein R¹ represents a hydrogen or a halogen atom or a C₁₋₄alkyl, a C₁₋₄alkoxy or a nitro group. n is an integer of 0 to 2, A represents an amino acid residue derived from a naturally occuring amino acid or an antipode thereof which is connected to the acrylic acyl residue through its amino group; or a residue derived from thiazolidinecarboxylic acid connected to the acrylic acyl group through its nitrogen, or a derivative of the above residues wherein any free carboxy group is esterified with a C₁₋₄alkyl group or is amidated; or A represents a group of formula wherein R₂ is a hydrogen atom or a phenyl, a C₁₋₄alkyl or a C₁₋₄alkoxycarbonyl group, and their salts which have interesting cytoprotective and antiulcer activities are provided. A process is also described for the preparation of said compounds.
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 invention relates to novel Δ¹⁴-16α,17-dihydroxy-pregnane-16,17-cyclic aldehyde acetal and -cyclic ketone ketal derivatives of general formula (I),
wherein A stands for hydrogen or hydroxyl group; X stands for hydrogen or halogen with the proviso that if A is hydrogen, then X also means hydrogen; R stands for hydrogen,benzoyl or C₁ ⁻ ₈alkanoyl group; R¹ and R², which are the same or different, stand for hydrogen or a C₁ ⁻ ₄alkyl group; or one of R¹ and R² is hydrogen and the other is phenyl group; or R¹ and R² together form a C₄ ⁻ ₅alkylene group; --- means a single or double bond between two adjacent carbon atoms, as well as pharmaceutical compositions containing these compounds and a process for their preparation. The compounds of general formula (I) possess a very strong antiinflammatory effect and only week harmful side effect. Thus, they can be used as active ingredients of antiinflammatory pharmaceutical compositions being useful in the therapy.
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:
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.
摘要:
Novel acrylic amide derivative of the formula wherein R¹ represents a hydrogen or a halogen atom or a C₁₋₄alkyl, a C₁₋₄alkoxy or a nitro group. n is an integer of 0 to 2, A represents an amino acid residue derived from a naturally occuring amino acid or an antipode thereof which is connected to the acrylic acyl residue through its amino group; or a residue derived from thiazolidinecarboxylic acid connected to the acrylic acyl group through its nitrogen, or a derivative of the above residues wherein any free carboxy group is esterified with a C₁₋₄alkyl group or is amidated; or A represents a group of formula wherein R₂ is a hydrogen atom or a phenyl, a C₁₋₄alkyl or a C₁₋₄alkoxycarbonyl group, and their salts which have interesting cytoprotective and antiulcer activities are provided. A process is also described for the preparation of said compounds.