摘要:
The present invention relates to a composition containing at least one amidine derivative or carboxamide derivative of general formula (I) or (A) in combination with at least one compound chosen from steroids, corticoids or corticosteroids, wherein said composition is suitable for the preparation of a medicament.
摘要:
The invention concerns amidine derivatives of general formula (I) exhibiting an inhibitory activity of calpains and/or a trapping activity of reactive forms of oxygen.
摘要:
The invention relates to new derivatives of 2-(iminomethyl)amino-phenyl which are NO synthase inhibitors and can trap reactive oxygen species. These compounds can notably be used for the treatment of stroke, of neurodegenerative diseases and of ischemic or hemorragic cardiac of cerebral infarctions.These compounds include: N-{4-[({[4-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3-thiazol-2-yl]methyl}amino)methyl]phenyl}thiophene-2-carboximidamide; N-{3-[({[4-(3,5-di-tert-butyl-4-hydroxyphenyl-)-1,3-thiazol-2-yl]methyl}amino)methyl]phenyl}thiophene-2carboximidamide; N-(4-{[{[4-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3-thiazol-2-yl]methyl}(methyl)amino]methyl}phenyl)thiophene-2carboximidamide; N-[3-(}[3-(3,5-di-tert-butyl-4-hydroxyphenyl)propyl]amino}methyl) phenyl]thiophene-2carboximidamide; N-(3-{[(3,5-di-tert-butyl-4-hydroxybenzyl)amino]methyl}phenyl)thiophene-2-carboximidamide; N-[3-({[2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethyl]amino}methyl)phenyl]thiophene-2-carboximidamide; N-[3-({[3-(4-hydroxy-3,5-diisopropylphenyl)propyl]amino}methyl)phenyl]thiophene -2-carboximidamide; N-(3-{[(4-hydroxy-3,5-diisopropylbenzyl)amino]phenyl)thiophene-2- carboximidamide; N-[3-({[2-(4-hydroxy-3,5-diisopropylphenyl)ethyl]amino}methyl) phenyl]thiophene-2-carboximidamide; N-2-(3,5-di-tert-butyl-4-hydroxybenzoyl)-N-1(4-(4-{[imino(thien-2-yl) methyl]amino}phenyl)-L-leucinamide; and pharmaceutically acceptable salts thereof.
摘要:
Thiaxozle, oxazole, imidazole, isoxazole and isoxazoline compounds of the formula wherein Het is thiazole, oxazole, imidazole, isoxazole or isoxazoline, n is an integer from 0 to 6, A is selected from the various optionally substituted aromatic radicals defined in the specification, B is hydrogen, alkyl or phenyl, R1 and R2 are independently hydrogen, alkyl or cycloalkyl or R1 and R2 taken together with the carbon atom which carries them, form a carbocycle with 3 to 7 members and Ω is —NH46R47 or —OR48, R46 and R47 are independently hydrogen, alkyl, cycloalkyl or —(CH2)kCOOR51, R51 is alkyl or haloalkyl and R48 is hydrogen or alkyl having advantageous pharmacological properties which allow their use in therapeutics, for treating neurodegenerative disorders or pain.
摘要:
A compound of the formula wherein the substituents are defined as in the specification and their pharmaceutically acceptable salts having NOS and ROS activity.
摘要:
Phenylpiperazine derivatives having high affinity for the &agr;1-adrenoreceptor and pharmaceutical compositions containing them. Also disclosed is a method of using the such derivatives to treat benign prostatic hyperplasia.
摘要:
The present invention relates to a composition containing at least one amidine derivative or carboxamide derivative of general formula (I) or (A) in combination with at least one compound chosen from steroids, corticoids or corticosteroids, wherein said composition is suitable for the preparation of a medicament.