首页> 外国专利> Polisustituidos Derivatives of 2 - aryl - 6 - phenyl imidazo 1,2-a pyridines, Pharmaceutical compositions containing the same, Preparation Process, Intermediates for the synthesis and use in the Treatment or prevention of diseases involving nuclear receptors such as NURR 1

Polisustituidos Derivatives of 2 - aryl - 6 - phenyl imidazo 1,2-a pyridines, Pharmaceutical compositions containing the same, Preparation Process, Intermediates for the synthesis and use in the Treatment or prevention of diseases involving nuclear receptors such as NURR 1

机译:2-芳基-6-苯基咪唑并[1,2-a]吡啶的Polisustituidos衍生物,包含该衍生物的药物组合物,制备方法,用于合成或用于治疗或预防涉及核受体(如NURR 1)的疾病的中间体

摘要

Claim 1: compounds of the formula (1) wherein R1 represents a phenyl group or a naphthyl Group, these two groups may be optionally substituted with one or more Atoms or groups are chosen independently of each other between the Halogen Atoms or groups, as follows: Rent - 10 haloalquilo C1 C1, C1 - alkoxy - 10, 10, 10 tioalquilo haloalcoxi C1, C1 - 10, - S (o) alkyl C1 - 10- S (or C1) 2 - alkyl - 10, cyano, Nitro, hydroxyl, hidroxialquileno C1 - 10, 10 - nrarb alquileno C1 C1 - alkoxy -, 10 - alquileno C1 - 10 - Oxy, nrarb, conrarb, so2nrarb, nrccord, OC (or C1) nrarb, OCO - alkyl - 10 NRCC (O) ore, nrcso2re, alquileno C1 - aryl - aryl or heteroaryl monocyclic, 10,While the aryl or heteroaryl monocyclic eventually substituted with one or more substituents selected from Halogen, alkyl group C1 - 10 10 -, Halo - alkoxy alkyl C1, C1 -, Halo - C1 - 10 nrarb alkoxy, Nitro, hydroxyl, Oxo, cyano, or OCO - C1 - 10 alkyl; X represents 1 to 4 Substituent S identical or different from each other, selected from Hydrogen, halogen, alkyl of C1 - 10C1 - 10 nrarb, alkoxy, Nitro, cyano, alkyl C1 - 10 May be eventually replaced with one or More groups selected from Halogen, alkoxy C1 - 10 10 -, Halo - alkoxy C1, nrarb or hydroxyl; R represents in position 3, 5, 7 or 8 of imidazo [1,2-c 1 to 4] pyridine substituents identical Or different from one another, chosen from a Halogen, alkyl of C1 - 10 alkyl, Halo - C1 - 10Alkoxy C1 - 10; R2 and R3 represent, independently of one another, a hydrogen Atom, an alkyl group C1 - 10, eventually replaced with a RF Group, an aryl Group, eventually replaced with one or more substituents selected from Halogen, alkyl group C1 - 10 - 10 - C1 alkyl, halo C1, 10 alkoxy -, Halo - alkoxy C1 - 10, nrarb, hydroxylNitro or cyano; R2 and x can form along with the carbon Atoms that are linked to the carbon cycle from 5 to 7 carbon Atoms; R4 represents a hydrogen Atom, an alkyl group C1 - 10, eventually replaced with a RF Group, an aryl Group, eventually replaced with one or Rivers substituents selected from Halogen, alkyl group C1 - 10 10 -, Halo - alkoxy alkyl C1, C1 - 10Halo - C1 - 10 nrarb alkoxy, Nitro, hydroxyl, alkyl, cyano, C1 - 10 - (CO) - conrarb nrccord, OC (,, OR) nrarb, OCO alkyl C1 - 10 NRCC (OR) or aryl aryl ore, being eventually replaced with one or more substituents selected from Halogen an alkyl group C1 -, 10 -, Halo - alkoxy alkyl C1 C1 - 10, 10, Halo - C1 - 10 nrarb alkoxy, Nitro or cyano, hydroxyl, ra and RB are;Independently of one another, a hydrogen Atom, an alkyl group or C1 - 10 - 10 alquileno C1, aryl or aryl; or ra and RB are jointly, with the nitrogen atom of a group which takes them, azetidine, pyrrolidine, piperidine, morpholine, piperazine tiomorfolina azepine,,, homopiperazina. This group eventually substituted with an alkyl group C1 - 10Aryl or aryl alquileno C1 - 10; RC and Rd represent, independently of one another, a hydrogen Atom, an alkyl group or C1 - 10 - 10 alquileno C1, aryl, aryl, or RC and Rd together form a group alquileno C2 - 5; RE represents an alkyl group C1 - aryl - 10 alquileno C1 - 10, aryl or RC and re form Together; S a group alquileno C2 - 5; RF represents a Halogen Atom, an alkoxy Group C1 - 10Halo - C1 hydroxyl alkoxy -, cyano, 10, nrarb, C (o) nrarb, nrccord, OC (OR) nrarb, OCO - C1 - 10 nrccoore alkyl, aryl, so2nrarb, nrcso2re, alquileno C1 - 10, aryl, aryl eventually being replaced with one or more substituents selected from Halogen, an alkyl group C1 - 10 alkyl, Halo - C1 - 10 C1 10 alkoxy -, Halo - C1 - 10 nrarb, alkoxy, Nitro, hydroxyl,Cyano or OCO alkyl C1 - 10; in the form of a base or an Acid Addition Salt.
机译:权利要求1:式(1)的化合物,其中R1代表苯基或萘基,这两个基团可以任选地被一个或多个原子取代,或在卤素原子或基团之间彼此独立地选择,如下:租金-10卤代喹啉C1 C1,C1-烷氧基-10,10,10噻吩基卤代烷C1,C1-10,-S(o)烷基C1-10- S(或C1)2-烷基-10,氰基,硝基,羟基,Hidroxialquileno C1-10,10-nrarb Alquileno C1 C1-烷氧基-,10-Alquileno C1-10-Oxy,nrarb,conrarb,so2nrarb,nrccord,OC(或C1)nrarb,OCO-烷基-10 NRCC(O)矿石,nrcso2re,alquileno C1-芳基-芳基或杂芳基单环,10,而最终被一个或多个选自卤素,烷基C1-10 10-,卤代-烷氧基烷基C1,C1-的取代基取代的芳基或杂芳基单环卤代-C1-10 nrarb烷氧基,硝基,羟基,氧代,氰基或OCO-C1-10烷基; X代表1至4个彼此相同或不同的取代基S,选自氢,卤素,C1-10C1-10nrarb的烷基,烷氧基,硝基,氰基,烷基C1-10。最终可以被一个或多个选自以下的基团取代卤素,烷氧基C1-10 10-,卤代烷氧基C1,nrarb或羟基; R表示在咪唑基[1,2-c 1至4]吡啶取代基的3、5、7或8位彼此相同或不同,选自卤素,C1-10烷基的烷基,Halo-C1-10的烷氧基C1 -10; R 2和R 3彼此独立地代表氢原子,C 1-10的烷基,最终被RF基团,芳基取代,最终被一个或多个选自卤素,烷基C 1-10的取代基取代。 -C1烷基,卤代C1、10个烷氧基-,卤代-烷氧基C1-10,nrarb,羟基硝基或氰基; R2和x可以与与5至7个碳原子的碳循环相关的碳原子一起形成; R 4代表氢原子,烷基C1-10,最终被RF基团取代,芳基,最终被一个或一个选自卤素,烷基C1-10 10-,卤代-烷氧基烷基C1,C1的Rivers取代基取代-10卤代-C1-10 nrarb烷氧基,硝基,羟基,烷基,氰基,C1-10-(CO)-conrarb nrccord,OC(或OR)nrarb,OCO烷基C1-10 NRCC(OR)或芳基芳基矿石,最终被一个或多个选自卤素的取代基取代,烷基C 1-,10-,卤代-烷氧基烷基C 1 -C 10-10、10-卤代-C1-10 nrarb烷氧基,硝基或氰基,羟基,ra和RB是;彼此独立地为氢原子,烷基或C1-10-10alquileno C1,芳基或芳基;或ra和RB与带有氮原子的氮杂环丙烷,吡咯烷,哌啶,吗啉,哌嗪噻吗啉代氮杂环戊烷,高哌嗪合在一起。该基团最终被烷基C1-10芳基或芳基alquileno C1-10取代; RC和Rd彼此独立地代表氢原子,烷基或C1-10-10链烯基C1,芳基,芳基,或者RC和Rd一起形成链烯基C2-5; RE代表烷基C 1-芳基-10 Alquileno C1-10,芳基或RC并一起重整; S组alquileno C2-5; RF代表卤素原子,烷氧基C1-10卤代-C1羟基烷氧基-氰基,10,nrarb,C(o)nrarb,nrccord,OC(OR)nrarb,OCO-C1-10 nrccoore烷基,芳基,so2nrarb, nrcso2re,alquileno C1-10,芳基,最终被一个或多个选自卤素,烷基C1-10烷基,Halo-C1-10 C1 10烷氧基-,Halo-C1-10 nrarb,烷氧基,硝基的取代基取代的芳基,羟基,氰基或OCO烷基C 1-10;以碱或酸加成盐的形式存在。

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