首页> 外国专利> QUINOLINE-4-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS NEUROKININ 3(NK-3)-AND NEUROKININ 2(NK-2) RECEPTOR ANTAGONISTS

QUINOLINE-4-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS NEUROKININ 3(NK-3)-AND NEUROKININ 2(NK-2) RECEPTOR ANTAGONISTS

机译:QUINOLINE-4-羧酰胺衍生物,其制备及其作为神经激肽3(NK-3)和神经激肽2(NK-2)受体拮抗剂的用途

摘要

A compound of formula (I): or a salt thereof, or a solvate thereof, wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or an optionally substituted single or fused ring aromatic heterocyclic group; R is C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, optionally substituted phenyl or phenyl C1-6 alkyl, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C1-6 alkyl, amino C1-6 alkyl, C1-6 alkylaminoalkyl, di C1-6 alkylaminoalkyl, C1-6 acylaminoalkyl, C1-6 alkoxyalkyl, C1-6 alkylcarbonyl, carboxy, C1-6 alkoxycarbonyl, C1-6 alkoxycarbonyl C1-6 alkyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di C1-6 alkylaminocarbonyl, halogeno C1-6 alkyl; or R is a group -(CH2)p- wherein p is 2 or 3 which group forms a ring with a carbon atom of Ar; R1 represents hydrogen or up to four optional subtitutents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino or mono- and di-C1-6 alkylamino; R2 represents hydrogen, C1-6-alkyl, hydroxy, halogen, cyano, amino, mono- or di-C1-6-alkylamino, alkylsulphonylamino, mono- or di-C1-6-alkanoylamino wherein any alkyl group is optionally substituted with an amino group or with a mono- or di-alkylamino group, or R2 is a moiety -X-(CH2)n-Y wherein X is a bond or -O- and n is an integer in the range of from 1 to 5 providing that when X is -O- n is only an integer from 2 to 5 and Y represents a group NY1Y2 wherein Y1 and Y2 are independently selected from hydrogen, C1-6-alkyl, C1-6-alkenyl, aryl or aryl-C1-6-alkyl or Y is hydroxy, halogen or an optionally substituted N-linked single or fused ring, heterocyclic group, R3 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R
机译:式(I)的化合物:或其盐或它们的溶剂化物,其中,Ar为任选取代的芳基或C5-7环链二烯基,或任选取代的单环或稠环芳族杂环基; R为C 1-6烷基,C 3-7环烷基,C 3-7环烷基烷基,任选取代的苯基或苯基C 1-6烷基,任选取代的五元杂芳族环,其包含至多四个选自O和N的杂原子,羟基C 1-6烷基,氨基C 1-6烷基,C 1-6烷基氨基烷基,二C 1-6烷基氨基烷基,C 1-6酰基氨基烷基,C 1-6烷氧基烷基,C 1-6烷基羰基,羧基,C 1-6烷氧基羰基,C 1-6烷氧基羰基C 1-6烷基,氨基羰基,C 1-6烷基氨基羰基,二C 1-6烷基氨基羰基,卤代C 1-6烷基; R是基团-(CH 2)p-,其中p是2或3,该基团与Ar的碳原子形成环。 R 1代表氢或最多四个选自以下的取代基:C 1-6烷基,C 1-6烯基,芳基,C 1-6烷氧基,羟基,卤素,硝基,氰基,羧基,羧酰胺基,磺酰胺基,C 1-6烷氧基羰基,三氟甲基,酰氧基,邻苯二甲酰亚胺基,氨基或单-和二-C 1-6烷基氨基; R 2代表氢,C 1-6-烷基,羟基,卤素,氰基,氨基,单-或二-C 1-6-烷基氨基,烷基磺酰基氨基,单-或二-C 1-6-烷酰基氨基,其中任何烷基任选地被一个或多个氨基或具有单或二烷基氨基的基团,或R2为-X-(CH2)nY部分,其中X为键或-O-,n为1至5的整数,条件是当X为-O-n仅为2至5的整数,且Y表示基团NY1Y2,其中Y1和Y2独立地选自氢,C1-6-烷基,C1-6-烯基,芳基或芳基-C1-6-烷基或Y为羟基,卤素或任选取代的N-连接的单环或稠环,杂环基,R 3为支链或直链C 1-6烷基,C 3-7环烷基,C 4-7环烷基烷基,任选取代的芳基或任选取代的单或稠环芳族杂环基;和R

著录项

  • 公开/公告号HU9901016A3

    专利类型

  • 公开/公告日2002-01-28

    原文格式PDF

  • 申请/专利号HU19990001016

  • 发明设计人

    申请日1996-11-22

  • 分类号C07D215/52;C07D401/12;C07D487/04;C07D401/06;A61K31/47;

  • 国家 HU

  • 入库时间 2022-08-22 00:45:05

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