179929-80-7

Upstream product

• 124-63-0 methanesulfonyl chloride 
• 155308-58-0 1-(3-isopropoxy-phenyl-acetyl)-3-(3,4-dichloro-phenyl)-3-(2-hydroxy-ethyl)-piperidine 

Relevant academic research and scientific papers

Synthesis and NK1 receptor antagonistic activity of (+)-1-acyl-3-(3,4- dichlorophenyl)-3-[2-(spiro-substituted piperidin-1'-yl)ethyl]piperidines

(±)-1-Acyl-3-(3,4-dichlorophenyl)-3-[2-(spiro-substituted piperidin- 1'-yl)ethyl]piperidines and their quaternary ammonium salts were prepared and evaluated for their NK1 receptor antagonistic activity. Some of these inhibited SP-induced contraction in guinea pig ileum with IC50 values at a level of 10-9 M and showed potent inhibitory activity against selective NK1 receptor agonist-induced bronchoconstriction in guinea pigs.

PIPERIDINE DERIVATIVES, PROCESS FOR OBTAINING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

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.

SALTS OF SUBSTITUTED NITROGENOUS HETEROAROMATIC COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

The invention concerns compounds of formula: STR1 in which Am + 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.

1-AZONIABICYCLO[2.2.1]HEPTANES, METHODS OF PREPARING THEM AND PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE PRESENT

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 1-C. sub.4, or a C 1-C 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 1-C. sub.4-alkyl, or a C 1-C 4-ω-alkoxy(C 2-C 4) alkyl, or a C 2-C 4-ω-alkanoyloxy (C 1-C 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 ⊕ is the radical STR2 in which X 1, X 2 and X 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 . 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.

1-AZONIABICYCLO[2.2.1] HEPTANES AND PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE PRESENT

The invention relates to quaternary basic amides of the formula STR1 in which Ar is an optionally substituted mono-, di-or tri-cyclic aromatic or heteroaromatic group;T is a direct bond, a hydroxymethylene group, an alkoxymethylene group in which the alkoxy group is C 1-C. sub.4, or a C 1-C 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 1-C 4-alkyl, or a ω-C 1-C. sub.4-alkoxy(C 2-C 4) alkyl, or a ω-C 2-C. sub.4-alkanoyloxy (C 1-C 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 ⊕ is the radical STR2 in which X 1, X 2 and X 3, together with the nitrogen atom to which they are bonded, form an azabicyclic or azatricyclic system optionally substituted by a phenyl or benzyl group; andA ? 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.