摘要:
New N-substituted cyclic amines of formula: ##STR1## wherein: X, R.sub.1, R.sub.2 and R are as defined in the description, their optical and geometric isomers and physiologically tolerable salts thereof. The compounds of the invention are powerful PDE4 inhibitors and can be used therapeutically.
摘要:
A compound of general formula (I): ##STR1## in which: R.sub.1 represents alkyl,X represents oxygen, --CHR'-- or --CR'.dbd.,R' is chosen from hydrogen and alkyl,R.sub.2 represents optionally substituted alkyl as is defined in the description, cycloalkyl or polycycloalkyl as are defined in the description,R.sub.3 represents hydrogen or hydroxyl,Alk represents alkylene, andY is as defined in the description,and medicinal products containing the same are useful as PDE IV inhibitors.
摘要:
A compound selected from those of formula (1): ##STR1## wherein W represents aryl, arylalkyl, heteroaryl, or heteroarylalkyl, each being optionally substituted,R.sub.1 represents alkyl, alkenyl, alkynyl, aryl, cycloalkyl, arylalkyl, or cycloalkylalkyl, each being optionally substituted.R.sub.2 is as defined in the description,its isomers, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as anti-oxidation agents.
摘要:
A compound of formula (I): ##STR1## wherein: R.sub.1 represents unsubstituted or substituted cycloalkyl, phenyl, naphthyl, heterocyclic, alkyl or alkenyl,A represents a bond, oxygen, sulphur, a group ##STR2## a group ##STR3## or a group ##STR4## wherein Rc represents hydrogen, alkyl or cycloalkyl, R.sub.2 represents halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, cycloalkyl, formyl, carboxy, alkylcarbonyl, cycloalkylcarbonyl, alkoxycarbonyl, cycloalkyloxycarbonyl, optionally substituted carbamoyl, optionally substituted amino, formylamino, cyano, optionally substituted amidino, hydroxyaminomethyl, amide oxime, hydrazono, or a group selected from: ##STR5## wherein R.sub.21, R.sub.22 and R.sub.23 are as defined in the description, R.sub.3 represents hydrogen or alkyl, cycloalkyl or acyl,or ##STR6## together form the ring ##STR7## X is oxygen, sulphur, or NR", B is phenyl, Ra and Rb, which may be identical or different, each represents hydrogen, halogen, or alkyl, hydroxy, alkoxy, carboxy, polyhalogenoalkyl, cyano, nitro, alkoxycarbonyl, cycloalkyloxycarbonyl, amino, carbamoyl, sulfo, alkylsulfonyl, cycloalkylsulfonyl or aminosulfonyl, their isomers, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as PDE IV inhibitors.
摘要:
New benzopyrrolidinone compounds, which can be used as medicaments and correspond to the formula ##STR1## in which: either: R.sub.1 and R.sub.2 together represent, with the bond of the etherocycle to which they are attached, an optionally substituted benzene nucleus and, simultaneously, R.sub.3 and R.sub.4 are hydrogen, (C.sub.1 -C.sub.4)alkyl or (C.sub.5 -C.sub.6)cycloalkyl;or:R.sub.1 is hydrogen, R.sub.4 is a single bond and R.sub.2 and R.sub.3 together represent, with the bond of the heterocycle to which they are bonded, an optionally substituted benzene nucleus; andA is a straight or branched hydrocarbon chain having from 2 to 6 carbon atoms that is optionally substituted by hydroxy;X is a single bond, oxygen or sulphur; andY is hydrogen, halogen or (C.sub.1 -C.sub.5)alkyl or alkoxy.These new compounds and the physiologically tolerable salts thereof can be used therapeutically, especially in the treatment of bronchospastic disorders and inflammations in the ENT area.
摘要:
Compounds of formula: wherein: ALK represents an alkylene chain, W represents a group wherein R and R′ are as defined in the description. Medicinal products containing the same which are useful in treating cognitive disorders associated with cerebral aging or with neurodegenerative diseases.
摘要:
The compounds are trisubstituted triazines and pyrimidines useful for the suppressing the resistance of tumour cells to anti-cancer agents and for suppressing the resistance of parasites to anti-parasitic agents.A compound disclosed is 2,4-diallylamino-6-{4-[(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl) methylamino]piperidin-1-yl}-1,3,5-triazine.
摘要:
Polymethylene-imines of the formula: ##STR1## in which: A is a hydrocarbon radical from C.sub.3 to C.sub.5 in a straight or branched chain possibly containing one or two double bonds and possibly substituted by one or more hydroxy radicals;X is CH or nitrogen;n is zero, one or two;Y is oxygen or N--R.sub.1 in which R.sub.1 is hydrogen, alkyl from C.sub.1 to C.sub.5, alkenyl from C.sub.2 to C.sub.5, cycloalkyl or cycloalkenyl from C.sub.3 to C.sub.7, or acetyl;R is hydrogen, alkyl from C.sub.1 to C.sub.5, cycloalkyl from C.sub.5 to C.sub.7 or phenyl optionally substituted by one or more fluorine or chlorine; andB is hydrogen, alkyl from C.sub.1 to C.sub.5, alkenyl from C.sub.2 to C.sub.5, or phenyl, naphthyl, benzofuranyl, benzothienyl, benzodioxolyl, benzodioxanyl, benzodioxinyl, .DELTA.3-chromanyl, thiochromenyl or chromanyl, each optionally substituted by fluorine, chlorine, alkyl or alkoxy from C.sub.1 to C.sub.5 ; ora radical of the formula: ##STR2## in which: R.sub.2, R.sub.3 and R.sub.4 which may be the same or different, each represent hydrogen, or phenyl optionally substituted by fluorine or chlorine.These compounds and physiologically tolerable acid addition salts thereof may be used as medicines especially in the treatment of all kinds of tissular hypoxia.
摘要:
Piperidylbenzimidazolinone derivatives of the formula: ##STR1## in which: R.sub.1 is lower alkyl, phenyl, halophenyl, lower alkylphenyl, lower alkoxyphenyl, methylenedioxyphenyl, ethylenedioxyphenyl, thienyl, furyl or pyridyl.R.sub.2 is R'.sub.1 COO-- or R'.sub.1 --COO--CH.sub.2 -- in which R'.sub.1 has the same meanings as R.sub.1, R.sub.1 and R'.sub.1 being the same or different, or R.sub.3 NH-- in which R.sub.3 is formyl, acetyl mesyl, carbamoyl, sulfamoyl or ethoxalyl.Z is hydrogen, lower-alkyl or lower alkenyl, andT is hydrogen, lower alkyl or lower alkoxy.These compounds and physiologically tolerable acid addition salts thereof may be used as medicines especially in the treatment of autoimmune, allergic and antiinflammatory diseases and in the treatment of dyspnea especially asthmatic and bronchial dyspnea.
摘要:
A compound selected from those of formula (I): wherein m and n, which may be identical or different, each represent an integer from 0 to 2 inclusive, with the sum of the two integers being from 2 to 3 inclusive, p and q, which may be identical or different, each represent an integer from 0 to 2 inclusive, Alk represents an alkylene, alkenylene or alkynylene chain, X represents an oxygen atom, a sulphur atom or an —N(R)— group wherein R represents a hydrogen atom or an alkyl group, Y, Y′ and W are as defined in the description, its enantiomers, diastereoisomers, and addition salts thereof with one or more pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful for treating conditions associated with central histaminergic systems.