155308-39-7

Upstream product

• 155308-38-6 4-(3,4-dichloro-phenyl)-4-[2-(tetrahydro-pyran-2-yloxy)-ethyl]-pyrrolidin-2-one 
• 3218-49-3 3,4-dichloro-benzeneacetonitrile 
• 155308-37-5 3-cyano-3-(3,4-dichloro-phenyl)-5-(tetrahydro-pyran-2-yl-oxy)-pentanoic acid ethyl ester 
• 135936-16-2 α-[2-(Tetrahydropyran-2-yloxy)ethyl]-3,4-dichlorophenyl-acetonitrile 
• 17739-45-6 2-(2-bromoethoxy)tetrahydropyran 

Downstream Products

• 52423-89-9 3-(3,4-dichloro-phenyl)-3-(2-hydroxy-ethyl)-pyrrolidine 
• 193755-84-9 1-Benzoyl-3-(3,4-dichlorophenyl)-3-(formylmethyl)pyrrolidine 
• 167262-37-5 3-(3,4-dichloro-phenyl)-1-(benzoyl)-3-(2-hydroxy-ethyl)-pyrrolidine 
• 193755-82-7 1-Benzoyl-3-(3,4-dichlorophenyl)-3-(2-[tetrahydropyran-2-yloxy]ethyl)pyrrolidine 

Relevant academic research and scientific papers

4-Amino-2-(aryl)-butylbenzamides and their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK2) receptor

A library, evaluating a range of piperazines, piperidines and acyclic amines, as replacements for the 4-hydroxy-4-phenylpiperidine moiety in lead (1b) was prepared. These efforts identified the 4-((N)-benzimidazolone)piperidine analogue (2a) which was further optimised using classical single-compound synthesis to yield the 3-((N)-morpholino)azetidine (2j). Conformationally constrained analogues of (2j), generally offered no potency advantage in this particular series.

3-Azetidinylalkylpiperidines or -pyrrolidines as tachykinin antagonists

The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof. Such compounds and salts are tachykinin antagonists.

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.