where R-R4 represent hetero-aryl. The hetero-aryl is in form of a cyclic aromatic group with C5-C6 or a bicyclic group with C9-C10, which contain 1, 2 or 3 hetero atoms, independently O, S or N, or a residue of , R1-H, C1-C6-akyl, R2 and R3 independently CH3, -OCH3, F, Cl, Br, J, R4 - from 1 to 4 substitutes, -H, halogen, C1-C6alkyl, -CF3, -OCF3, -(CH2)n-OR5, -(CH2)n-NR5R6, -(CH2)n-NHSO2R5, -(CH2)n-NH(CH2)2NR5R6, -(CH2)n-NHC(O)NR5R7, -(CH2)n-NH(CH2)2OR5, or 1-piperazinyl; n - 0, 1, 2, 3; R5 and R6 - H, C1C3alkyl, R7-H, C1-C3alkyl, aminoalkyl C1-C3, or to their pharmaceutical salts. The compounds are antagonists of the nociceptin ORL-1 receptor.;EFFECT: obtaining of compounds that are useful in the treatment of cough.;10 cl, 22 ex, 1 tbl"/>
HETERO-ARYL DERIVATIVES AS SUPER LIGANDS FOR NOCICEPTIN ORL-1 RECEPTOR
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HETERO-ARYL DERIVATIVES AS SUPER LIGANDS FOR NOCICEPTIN ORL-1 RECEPTOR
HETERO-ARYL DERIVATIVES AS SUPER LIGANDS FOR NOCICEPTIN ORL-1 RECEPTOR
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机译：诺西派汀ORL-1受体的超级配体杂芳基衍生物
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摘要
FIELD: chemistry.;SUBSTANCE: invention pertains to new hetero-aryl derivatives of 8-azabicyclo-[3.2.1]-octan-3-ol with general formula I where R-R4 represent hetero-aryl. The hetero-aryl is in form of a cyclic aromatic group with C5-C6 or a bicyclic group with C9-C10, which contain 1, 2 or 3 hetero atoms, independently O, S or N, or a residue of , R1-H, C1-C6-akyl, R2 and R3 independently CH3, -OCH3, F, Cl, Br, J, R4 - from 1 to 4 substitutes, -H, halogen, C1-C6alkyl, -CF3, -OCF3, -(CH2)n-OR5, -(CH2)n-NR5R6, -(CH2)n-NHSO2R5, -(CH2)n-NH(CH2)2NR5R6, -(CH2)n-NHC(O)NR5R7, -(CH2)n-NH(CH2)2OR5, or 1-piperazinyl; n - 0, 1, 2, 3; R5 and R6 - H, C1C3alkyl, R7-H, C1-C3alkyl, aminoalkyl C1-C3, or to their pharmaceutical salts. The compounds are antagonists of the nociceptin ORL-1 receptor.;EFFECT: obtaining of compounds that are useful in the treatment of cough.;10 cl, 22 ex, 1 tbl
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机译：技术领域：本发明涉及具有通式I的8-氮杂双环-[[3.2.1]-辛烷-3-醇的新杂芳基衍生物。其中RR 4 表示杂芳基。杂芳基为带有C5-C6的环状芳族基团或带有C9-C10的双环基团，它们分别含有1、2或3个杂原子，分别为O，S或N，或“ 00000004.GIF” he =“ 14” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 18” />，R 1 -H，C 1 - C 6 -烷基，R 2 和R 3 独立地是CH 3 ，-OCH 3 ，F，Cl，Br，J，R 4 -从1至4个取代基-H，卤素，C 1 -C 6 烷基，-CF 3 ，-OCF 3 ，-（CH 2 ） n -OR 5 ，-（CH 2 ） n -NR 5 R 6 ，-（CH < Sub> 2 ） n -NHSO 2 R 5 ，-（CH 2 ） n -NH（CH 2 ） 2 NR 5 R 6 ，-（CH < Sub> 2 ） n -NHC（O）NR 5 R 7 ，-（CH 2 ） n -NH（CH 2 ） 2 OR 5 或1-哌嗪基; n-0、1、2、3; R 5 和R 6 -H，C 1 C 3 烷基，R 7 -H，C 1 -C 3 烷基，氨基烷基C 1 -C 3 或它们的药物盐。该化合物是伤害感受素ORL-1受体的拮抗剂。效果：获得可用于治疗咳嗽的化合物; 10 cl，22 ex，1 tbl
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