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QUINUCLIDINE DERIVATIVES AS SUBSTANCE P ANTAGONISTS.
QUINUCLIDINE DERIVATIVES AS SUBSTANCE P ANTAGONISTS.
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机译:喹诺酮衍生物作为物质拮抗剂。
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摘要
Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of formula (I) and the pharmaceutically-acceptable salts thereof, wherein X1 is alkoxy or halosubstituted alkoxy; X2 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, halosubstitued alkyl, halosubstituted alkoxy, alkylamino, dialkylamino, alkylsulfonylamino (which may be substituted), N-alkyl-N-alkylsulfonylamino (which may be substituted), alkanoylamino (which may be substituted) or N-alkyl-N-alkanoylamino (which may be substituted); Ar1 and Ar2 are each, independently, thienyl, phenyl, fluorophenyl, chlorophenyl or bromophenyl; A is Y-(CH2)m-CH(R2)-(CH2)n-NR1-; R1 is hydrogen, alkyl, benzyl or -(CH2)p-Y; R2 is hydrogen, alkyl (which may be substituted), benzyl, 4-hydroxybenzyl, 3-indolylmethyl or -(CH2)p-Y; Y is -CN, -CH2Z or -COZ; Z is hydroxy, amino, alkoxy, alkylamino or dialkylamino; m, n and p are each, independently, 0, 1, 2 or 3; and R1 and R2 may be connected to form a ring.
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机译:用于治疗炎性疾病,中枢神经系统疾病和式(I)的其他疾病的化合物及其药学上可接受的盐,其中X 1为烷氧基或卤代烷氧基; X 2是氢,卤素,烷基,烯基,炔基,烷氧基,烷硫基,烷基亚磺酰基,烷基磺酰基,卤代烷基,卤代烷氧基,烷基氨基,二烷基氨基,烷基磺酰基氨基(可被取代),N-烷基-N-烷基磺酰基氨基(可以被取代),烷酰基氨基(可以被取代)或N-烷基-N-烷酰基氨基(可以被取代); Ar 1和Ar 2分别独立地是噻吩基,苯基,氟苯基,氯苯基或溴苯基; A为Y-(CH 2)m -CH(R 2)-(CH 2)n -NR 1-。 R 1为氢,烷基,苄基或-(CH 2)p -Y; R 2为氢,烷基(可被取代),苄基,4-羟基苄基,3-吲哚基甲基或-(CH 2)p -Y。 Y为-CN,-CH 2 Z或-COZ; Z为羟基,氨基,烷氧基,烷基氨基或二烷基氨基; m,n和p分别独立地为0、1、2或3; R 1和R 2可以连接形成环。
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