C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 295/16 (2006.01) A61K 31/155 (2006.01) A61K 31/395 (2006.01) C07C 257/18 (2006.01) C07C 257/20 (2006.01) C07C 279/20 (2006.01) C07D 211/16 (2006.01) C07D 211/40 (2006.01) C07D 211/42 (2006.01) C07D 211/44 (2006.01) C07D 211/46 (2006.01) C07D 211/74 (2006.01) C07D 213/75 (2006.01) C07D 265/02 (2006.01) C07D 277/04 (2006.01) C07D 295/195 (2006.01) C07D 295/215 (2006.01) C07D 295/28 (2006.01) C07D 401/12 (2006.01) C07D 491/113 (2006.01)
Patent
CA 2203850
This invention relates to a novel class of partial or full muscarinic receptor agonists, intermediates for their preparation, and pharmaceutical compositions for the treatment or prevention of diseases, the treatment or prevention of which is mediated by muscarinic receptor agonism. They are compounds of the invention of formula I (see fig.I) wherein, preferably, X is NR4R5 and R4 and R5 are taken together with the nitrogen atom to which they are attached to form an optionally substituted (five to nine)-membered saturated heterocyclic ring selected from piperidine, pyrrolidine, thiomorpholine, hexametheneimine, morpholine, thiazolidine and 1,2-tetrahydrooxazine; Y is N or CH; Z is pyridyl or phenyl optionally substituted with from one to three substituents independently selected from the group consisting of (C1-C6)alkyl, halo, hydroxy, (C1-C6)alkoxy, amino, (C1-C6)alkylamino, di(C1-C6)alkylamino and trifluoromethoxy; R2 is phenyl optionally substituted with halo, hydroxy, fluoro or methoxy; and R3 is phenyl optionally substituted with from one to three substituents independently selected from the group consisting of (C1-C6)alkyl, halo, hydroxy, (C1-C6)alkoxy, amino,
Nouvelle classe d'agonistes partiels ou totaux du récepteur muscarinique; intermédiaires pour leur préparation; compositions pharmaceutiques pour le traitement et la prévention de maladies, via des agonistes de ce récepteur. Il s'agit de composés de formule I (voir fig. I) dans laquelle, de préférence, X est NR4R5 et R4 et R5 sont regroupés avec l'atome d'zote auquel ils sont liés pour former un hétérocyle saturé, de 5 à 9 chaînons avec substitution facultative, choisi parmi les hétérocycles pipéridine, pyrrolidine, thiomorpholine, hexaméthèneimine, morpholine, thiazolidine 1,2-tétrahydrooxazine; Y est N ou CH; Z est un pyridyle ou un phényle, avec substitution facultative par un à trois substituants, choisis independamment l'un de l'autre parmi les groupes alkyle (C1-C6), halo, hydroxy, alcoxy (C1-C6), amino, alkylamino (C1-C6), dialkyl(C1-C6)amino et trifluorométhoxy; R2 est un phényle avec substitution faculative par un groupe halo, hydroxy, fluoro ou méthoxy; R3 est un phényle avec substitution facultative par un à trois substituants choisis indépendamment l'un de l'autre parmi les groupes alkyle (C1-C6), halo, hydroxy, alcoxy (C1-C6) et amino.
Liston Dane R.
Nowakowski Jolanta
Villalobos Anabella
Yohannes Daniel
Pfizer Inc.
Smart & Biggar
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