摘要:
Piperidine derivatives, process for obtaining them and pharmaceutical compositions containing them, of formula ##STR1## used as neurokinin receptor antagonists, which are, in particular, useful for the treatment of all substance P- and neurokinin-dependent pathologies.
摘要:
Piperidine derivatives, process for obtaining them and pharmaceutical compositions containing them, of formula ##STR1## used as neurokinin receptor antagonists, which are, in particular, useful for the treatment of all substance P- and neurokinin-dependent pathologies.
摘要:
Piperidine derivatives, process for obtaining them and pharmaceutical compositions containing them, of formula ##STR1## used as neurokinin receptor antagonists, which are, in particular, useful for the treatment of all substance P- and neurokinin-dependent pathologies.
摘要:
The invention concerns compounds of formula: ##STR1## in which Am.sup.+ represents a substituted 1-pyridylium radical, a substituted 3-thiazolylium radical, a substituted 1-pyridazinylium radical or a substituted 3-imidazolylium radical, and their salts with mineral or organic acids, whether in their optically pure or racemic form. The invention also concerns a process for the preparation of these compounds and pharmaceutical compositions containing them. Activity: antagonists of neurokinin receptors.
摘要:
Compounds of formula (I), a method for obtaining them and pharmaceutical compositions containing them are described. The compounds are useful as human NK.sub.3 receptor antagonists.
摘要:
The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from: A.sub.1) --O--CO-- A.sub.2) --CH.sub.2 --O--CO-- A.sub.3) --O--CH.sub.2 --CO-- A.sub.4) --O--CH.sub.2 --CH.sub.2 -- A.sub.5) --N(R.sub.1)--CO-- A.sub.6) --N(R.sub.1)--CO--CO-- A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 -- A.sub.8) --O--CH.sub.2 -- in which: R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; and Am is a nitrogen-containing heterocycle.
摘要:
The invention relates to quaternary basic amides of the formula ##STR1## in which Ar is an optionally substituted mono-, di- or tricyclic aromatic or heteroaromatic group; T is a direct bond, a hydroxymethylene group, an alkoxymethylene group in which the alkoxy group is C.sub.1 -C.sub.4, or a C.sub.1 -C.sub.5 -alkylene group; Ar' is an unsubstituted or mono- or poly-substituted phenyl, a thienyl, a benzothienyl, a naphthyl or an indolyl; R is hydrogen or a C.sub.1 -C.sub.4 -alkyl, or a C.sub.1 -C.sub.4 -.omega.-alkoxy(C.sub.2 -C.sub.4)alkyl, or a C.sub.2 -C.sub.4 -.omega.-alkanoyloxy (C.sub.1 -C.sub.4)alkyl;. Q is hydrogen; or else Q and R together form a 1,2-ethylene, 1,3-propylene or 1,4-butylene group; Am.sup..sym. is the radical ##STR2## in which X.sub.1, X.sub.2 and X.sub.3, together with the nitrogen atom to which they are bonded, form a 1-AZONIABICYCLO�2.2.1!HEPTANE optionally substituted by a phenyl or benzyl group; and A.sup..crclbar. is a pharmaceutically acceptable anion. These compounds are useful for the preparation of drugs intended for the treatment of pathological conditions involving the tachykinin system.
摘要:
The present invention relates to quaternary basic amides of the formula: ##STR1## These compounds are useful for the preparation of drugs intended for the treatment of pathological conditions involving the tachkinin system.
摘要:
The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycle.
摘要:
A compound of formula: in which:Ar represents a pyrid-2-yl or a phenyl which is unsubstituted or substituted by a halogen, a methyl or a (C.sub.1 -C.sub.4)alkoxy;R.sub.1 represents a methyl group;R.sub.11 represents hydrogen;or R.sub.1 and R.sub.11 together represent a --(CH.sub.2).sub.3 -- group;R.sub.2 represents a hydroxyl; a (C.sub.1 -C.sub.7)alkoxy; a (C.sub.1 -C.sub.7)acyloxy; a cyano; an --NR.sub.6 R.sub.7 group; an --NR.sub.3 COR.sub.4 group; an --NR.sub.3 COOR.sub.8 group; an --NR.sub.3 SO.sub.2 R.sub.9 group; an --NR.sub.3 CONR.sub.10 R.sub.12 group; a (C.sub.1 -C.sub.7)acyl group; a (C.sub.1 -C.sub.7)alkoxycarbonyl; a --CONR.sub.10 R.sub.12 group; a --CH.sub.2 OH group; a (C.sub.1 -C.sub.7)alkoxymethyl; a (C.sub.1 -C.sub.7)acyloxymethyl; a (C.sub.1 -C.sub.7)alkylaminocarbonyloxymethyl; a --CH.sub.2 NR.sub.13 R.sub.14 group; a --CH.sub.2 NR.sub.3 COR.sub.4 group; a --CH.sub.2 NR.sub.3 COOR.sub.8 group; a --CH.sub.2 NR.sub.3 SO.sub.2 R.sub.9 group; a --CH.sub.2 NR.sub.3 CONR.sub.10 R.sub.12 group; or R.sub.2 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring;or Ar and R.sub.2, together with the carbon atom to which they are attached, constitute a group of formula: ##STR1## Application: NK.sub.3 antagonists