Compounds 4 - 4 - phenyl - 2 - 1H imidazole il piperidine substituted, their prodrugs and Pharmaceutical compositions comprising these Compounds, and use of such compounds and Pharmaceutical compositions for the preparation of medicines

摘要

4-phenyl-4 - [1h-imidazol-2-il] derivative pyridine, alternative formula (1),Acid group acceptable on acid salt or medicine, its stereochemical isomer form, its ceramic form, and its oxide form, wherein: a = B is an excimer with bivalent P bond, X is a covalent bond, CH2 - or CH2CH2 -;R1 is hydrogen, alkyloxy, alkylcarbonyloxy, Ar-oxy, Het-oxy, Ar-carbonyloxy, Het-carbonyloxy, Ar-alkyloxy, Het-alkyloxy, alkyl, polyhaloalkyl, alkyloxyalkyl, Ar-alkyl, Het-alkyl, Ar, Het, thio, alkylthio, Ar-thio, Het-thio or NR9R10 where each of R9 and R10 is independently hydrogen, alkyl, Ar, Ar-alkyl, Het, Het-alkyl, alkyl-carbonyl, Ar-carbonyl, Het-carbonyl or alkyloxycarbonylalkyl; or A = B and R1 together, form an optionally substituted semiaromatic or aromatic carbocyclic or heterocyclic Het2 or Het3 radical; R2 is hydroxy, alkyloxy, alkylcarbonyloxy, phenyloxy, phenylcarbonyloxy, halo, cyano, alkyl, polyhaloalkyl, alkyloxyalkyl,Thyroid, carboxi, lcarnia, ocyclohexarbonilo, aminocarbonilo, mono-o dialaminocarbonilo, fenilo, nitro, amino, mono-o dialamino, TiO o codio; R3 is asphalt, AR, AR codilo, AR alquenilo, het, het codilo, het alquenilo; R4, R5 is hydrogen, asphalt, carboxi, aminoboxi, PVC, halogen or oxy; P is an integer equal to zero, 1, 2 or 3; tar is a directly saturated or scattered saturated radical hydrocarbon, containing 1 to 6 carbon atoms, or a cyclic saturated / or cyclic hydrocarbon (cyclopentyl compound), containing 3 to 7 carbon atoms,O is a cyclic saturated hydrocarbon group with 3 to 7 carbon atoms attached to 1 to 6 carbon atoms of a direct saturated or branched group, each of which can be replaced by aminobenzene, nitro group, uncle, hydroxyl group, oxo, cyanogen, thyroid or carboxi; Beryllium is a radical tar with one or more double links; AR is a cycle selected between groups consisting of phenyl and northwest group, each of which can be selectively replaced by one or more substitutes, each of which is independently selected from the group consisting of hydrogen, hydrocarbon and phenyl. Phenyl carbide polyacylhalide cyanide1. Tar, polyalkylhaloalkyl, alkylacyloxy, methylrice, haloformate, anthrax, tar, tar, tar, alkyl, aminobenzene, monkey - or dialectical carbide, phenyl, phenyl, nitrobenzene, aminobenzene, monkey - or diallamine, uncle, asphalt or so2-ch3; halogenation is an alternative selected from the fluorine, chlorine, bromine and iodine groups; Polyacyloxy is a direct or diffuse hydrocarbon radical with 1 to 6 carbon atoms, or a cyclic saturated hydrocarbon radical with 3 to 7 carbon atoms, one or more of which is replaced by one or more halogen atoms; het is a heterocyclic radical selected from het1, het group. And Het3,Het1 is a monoperiodic heteromorphic arifa radical selected from pirrolidini, dioxillo, imidazolidini, pirazolidini, piperidinilo, dioxilo, morfoline, ditienilo, tiomorfolini, piperaznilo, piperaznilo, tiomorfolini, piperaznilo and tetrahydrofuran, etc. het2 is a semi aromatic monoperiodic heteromorphic radical selected from this population. It is composed of 2H pirrolilo, pirrolilinilo, pyridine dimethyl ether, pyridine dimethyl ether, pyridine dimethyl ether and pyridine dimethyl ether. Hett3 is a single cycle aromatic radical substance, which is composed of pyridinol, pyridine diene, pyridine diene, pyridine diene, pyridine dienyl, pyridine isol, pyridine isol and trioctyl ester;Or one of the heterocyclic aromatic hormones selected from the following groups: quinoolinil, quinoxaline, indolilo, benzimidazolino, benzoxazolilo, benisoxazolilo, benzotiazollo, benisotiazolilo, benzofuranie and benzotienilo; each single ring and double ring heterocyclic radicalism can be selectively replaced by carbon. And / or heteromorphic atoms with halogenation, hydrogen group, asphalt, asphalt, AR, asphalt or pyridine. These compounds are selective, non opioid drugs for the treatment of various painful disorders. Its chemical composition, including the pharmaceutical composition of these derivatives, has also been published,And these derivatives or drug compounds are used in drug production.