摘要:
Benzodiazépines de formule dans laquelle R9 est hydrogène ou chlore, R10 est phényle éventuellement substitué, R11 est hydrogène, R12 est oxygène ou soufre, R13 est un groupe NH, Ar est aromatique ou hétéroaromatique comportant un ou deux cycles et dans laquelle, notamment, A est un pont éthylène ou triméthylène ; e est égal à 1 ou 2 ; qui sont antagonistes de la gastrine et ou antagonistes centraux de la cholecystokinine.
摘要:
Procédé de préparation des N-cycloalkylalkyle benzylamines de formule (I) : dans laquelle : R1 et R5 sont phényle R2 est alkyle R3 est hydrogène ou alkyle inférieur R4 est cycloalkyle -(CH)m m est 1 ou 2.
摘要:
Benzodiazépines de formule dans laquelle R₁ et R₂ sont H ou halogène, Ar est indolyle ou phényle et n est 2 ou 3, sont des antagonistes de la cholécystokinine.
摘要:
1. Claims (for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE) Aminoalcohols of formula see diagramm : EP0237366,P25,F1 in which R1 is lower alkyl and R2 is H or lower alkyl, R3 is H, lower alkyl, lower alkenyl, lower phenylalkyl or lower cycloalkylalkyl with 3 to 6 carbon atoms in the cycle or, when R2 is H, lower alkanoyl, lower phenylalkanoyl or cycloalkylcarbonyl having 3 to 6 carbon atoms in the cycle, or R2 and R3 form together with the nitrogen atom to which they are linked, a heterocycle saturated with 5 to 7 chain links which can have, as the second heteroatom not directly connected to the nitrogen atom, an oxygen, a sulphur or a nitrogen, the latter nitrogen heteroatom possibly carrying an alkyl substituent in C1 to C4 , and their acid addition salts. 1. Claims (for the Contracting States : AT, ES) Process for the preparation of aminoalcohols of formula see diagramm : EP0237366,P26,F2 in which R1 is lower alkyl and R2 is H or lower alkyl, R3 is H, lower alkyl, lower alkenyl, lower phenylalkyl or lower cycloalkylalkyl with 3 to 6 carbon atoms in the cycle, or when R2 is H, lower alkanoyl, lower phenylalkanoyl or cycloalkylcarbonyl having 3 to 6 carbon atoms in the cycle, or R2 and R3 form together with the nitrogen atom to which they are linked, a heterocycle saturated with 5 to 7 chain links and which can comprise, as the second heteroatom not directly linked with the nitrogen atom, an oxygen, a sulphur or a nitrogen, whereby said latter nitrogen heteroatom can carry an alkyl substituent in C1 to C4 and their acid addition salts, characterized in that it comprises : reducing an acid of formula see diagramm : EP0237366,P27,F1 by a boron or aluminium hydride to obtain compounds (la), in which R2 and R3 are hydrogen and for obtaining compounds (lb), in which NR2 R3 form a heterocycle performing a cyclization by reacting a compound (la) with a reagent of formula X-(CH2 )m -R5 -(CH2 )n -X' in which X and X', which can be the same or different, are halogen, R5 is a single valence bond and m and n are integers between 1 and 3, with m + n equal to or greater than 4 and equal to or less than 6, or R5 is an oxygen, a sulphur or NR6 , R6 being H or alkyl in C1 to C4 and m and n are integers between 1 and 3 with m + n equal to or higher than 3 and equal to or lower than 5 and for preparing compounds (lc), in which R3 is alkanoyl, phenylalkanoyl or cycloalkylcarbonyl, acylating a compound (la) with an acylating agent of formula R4 -COX, in which X is a halogen and R4 is the homolog immediately below R3 and for preparing compounds (ld), in which R2 is H and R3 is alkyl, alkenyl, phenylalkyl or cycloalkylalkyl, alkylating a compound (la) using an alkylating agent R3 -X, X being a halogen, or reducing a compound (lc) by a boron or aluminium hydride, or reducing a compound of formula see diagramm : EP0237366,P27,F2 by a boron or aluminium hydride and for preparing compounds (le), in which R2 is alkyl and R3 identical to R2 , reacting a compound (la) with an aldehyde of formula R4 CHO in the presence of formic acid and for preparing compounds (le) in which R2 is alkyl and R3 is alkyl, alkenyl, phenylalkyl or cycloalkylalkyl, reacting a compound (ld) with an aldehyde of formula R4 CHO in the presence of formic acid and, for preparing the acid addition salts, reacting the compounds (l) with an acid. 1. Claims (for the Contracting State GR) Aminoalcohols of formula see diagramm : EP0237366,P28,F1 in which R1 is lower alkyl and R2 is H or lower alkyl, R3 is H, lower alkyl, lower alkenyl, lower phenylalkyl or lower cycloalkylalkyl with 3 to 6 carbon atoms in the cycle or, when R2 is H, lower alkanoyl, lower phenylalkanoyl or cycloalkylcarbonyl having 3 to 6 carbon atoms in the cycle, or R2 and R3 form together with the nitrogen atom to which they are linked, a heterocycle saturated with 5 to 7 chain links which can have, as the second heteroatom not directly connected to the nitrogen atom, an oxygen, a sulphur or a nitrogen, the latter nitrogen heteroatom possibly carrying an alkyl substituent in C1 to C4 , and their acid addition salts.
摘要:
Aminoéthylimidazole de formule dans laquelle: R,est alcoyle inférieur; R 2 est un radical phényle ou phénoxy, éventuellement substitué par un atome d'halogène ou par un radical alcoxy inférieur; R 3 est un atome d'hydrogène ou un radical alcoyle inférieur; x, y et z ont pour valeur 0 ou 1, les valeurs de y et z ne pouvant toutefois être égales, et leurs sels d'addition avec des acides. Médicament cytoprotecteur.
摘要:
A method for resolving chiral hydantoins having general formula (I), wherein R1 is a lower alkyl radical having 1-5 carbon atoms in a linear or branched chain; and R2 is a phenyl radical which is optionally mono-, di- or trisubstituted by lower alkoxy or alkyl radicals or halogen atoms, which are the same or different, or a heteroaryl radical containing a ring of 5-7 links in which the only heteroatom is nitrogen, oxygen or sulphur, or else an aralkyl radical of which the alkyl portion includes one or two carbon atoms and the aryl ring is a phenyl group which is optionally mono-, di- or trisubstituted by lower alkoxy or alkyl radicals or halogen atoms which are the same or different. The hydantoin (I) to be resolved is dissolved in an alcohol or an alkaline solution, a specific proportion of an α-methylbenzylamine enantiomer is added to the solution thereby obtained, and the resulting diastereoisomer salt is isolated and treated with an acid solution to crystallize the hydantoin (I) enatiomer.
摘要:
Cette composition laxative à base de lactulose est préparée en mettant la composition sous la forme d'une gelée au moyen d'une pectine ayant un pourcentage des groupes carboxyliques estérifiés inférieur à 50 additionnée d'un sel de calcium et d'un agent d'ajustement du pH.