首页> 外国专利> APPLICATION OF HETEROCYCLIC COMPOUNDS IN PRODUCTION OF A PHARMACEUTIC AGENT, NOVEL HETEROCYCLIC COMPOUNDS AND PHARMACEUTIC AGENT AS SUCH

APPLICATION OF HETEROCYCLIC COMPOUNDS IN PRODUCTION OF A PHARMACEUTIC AGENT, NOVEL HETEROCYCLIC COMPOUNDS AND PHARMACEUTIC AGENT AS SUCH

机译:杂环化合物在医药制剂生产中的应用,新型杂环化合物和医药制剂

摘要

Use of N-substituted pyrrolidone, imidazolidinone, oxazolidinone or thiazolidinone derivatives of formula (I), in all stereoisomer or mixture forms, or their salts is for inhibiting the adhesion and/or migration of leukocytes or inhibiting VLA-4 receptors is new. W = R1-A-CR13 or R1A-CH=C; Y = CO, CS or CH2; Z = O, S or CH2 etc.; A = 1-6C alkylene, 3-12C cycloalkylene, (1-6C), phenylene-(1-6C)alkyl, or the divalent residue of a 5- or 6-membered ring containing 1 or 2 N (optionally mono- or disubstituted) etc.; B = 1-6C alkylene (optionally substituted), 2-6C alkenylene, phenylene, phenylene-(1-3C) alkyl or (1-3C) alkylene-phenyl; D = CR2R3. NR3 or CH=CR3; E = tetrazolyl, SO3H etc.; R = H, alkyl, cycloalkyl, cycloalkylalkyl, Ar, Ar-alkyl, Het' or Het'-alkyl (where alkyl residues are optionally substituted); R1 = H, 1-10C alkyl (optionally fluorinated), cycloalkyl, cycloalkylalkyl, O or S etc.; R2 = H, alkyl, Ar, Ar-alkyl or 3-8C cycloalkyl; R3 = H, alkyl, Ar, Ar-alkyl, 3-8C cycloalkyl, alkenyl, alkynyl, alkenylcarbonyl, alkynylcarbonyl, pyridyl etc.; R13 = H, 1-6C alkyl, Ar-alkyl or 3-8C cycloalkyl; b, c, d, f = 0 or 1, but not all 0; e, g, h= 0-6; Ar = optionally substituted 6-14C aryl; Het' = optionally substituted heteroaryl; unless specified otherwise alkyl moieties have 1-8C, alkenyl or alkynyl moieties 2-8C, cycloalkyl moieties 3-12C and bi- or tri-cycloalkyl moieties 6-12C.
机译:以所有立体异构体或混合物形式使用式(I)的N-取代的吡咯烷酮,咪唑烷酮,恶唑烷酮或噻唑烷酮衍生物,或其盐用于抑制白细胞的粘附和/或迁移或抑制VLA-4受体是新的。 W = R1-A-CR13或R1A-CH = C; Y = CO,CS或CH2; Z = O,S或CH2等; A = 1-6C亚烷基,3-12C环亚烷基,(1-6C),亚苯基-(1-6C)烷基或含有1或2 N的5或6元环的二价残基(可选为单或二取代)等; B = 1-6C亚烷基(任选地被取代),2-6C亚烯基,亚苯基,亚苯基-(1-3C)烷基或(1-3C)亚烷基-苯基; D = CR2R3。 NR3或CH = CR3; E =四唑基,SO3H等; R = H,烷基,环烷基,环烷基烷基,Ar,Ar-烷基,Het'或Het'-烷基(其中烷基残基是任选取代的); R1 = H,1-10C烷基(任选地氟化),环烷基,环烷基烷基,O或S等; R2 = H,烷基,Ar,Ar-烷基或3-8C环烷基; R3 = H,烷基,Ar,Ar-烷基,3-8C环烷基,烯基,炔基,烯基羰基,炔基羰基,吡啶基等; R13 = H,1-6C烷基,Ar-烷基或3-8C环烷基; b,c,d,f = 0或1,但不全为0; e,g,h = 0-6; Ar =任选取代的6-14C芳基; Het'=任选取代的杂芳基;除非另有说明,否则烷基部分具有1-8C,烯基或炔基部分2-8C,环烷基部分3-12C和二或三环烷基部分6-12C。

著录项

  • 公开/公告号PL188042B1

    专利类型

  • 公开/公告日2004-11-30

    原文格式PDF

  • 申请/专利权人 HOECHST AG;

    申请/专利号PL19970323130

  • 申请日1997-11-15

  • 分类号C07D233/72;C07D403/10;C07K5/023;C07K5/117;A61K31/4015;A61K38/06;A61K38/07;A61P29/00;

  • 国家 PL

  • 入库时间 2022-08-21 22:16:46

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