首页> 外国专利> NOVEL DERIVATIVES OF IMIDAZOLE OR TRIAZOLE, METHOD OF OBTAINING THEM THEIR APPLICATION IN PRODUCTION OF A PHARMACOLOGICAL AGENT, PHARMACOLOGICAL AGENT AS SUCH AND METHOD OF OBTAINING SUCH PHARMACOLOGICAL AGENT

NOVEL DERIVATIVES OF IMIDAZOLE OR TRIAZOLE, METHOD OF OBTAINING THEM THEIR APPLICATION IN PRODUCTION OF A PHARMACOLOGICAL AGENT, PHARMACOLOGICAL AGENT AS SUCH AND METHOD OF OBTAINING SUCH PHARMACOLOGICAL AGENT

机译:咪唑或三唑的新衍生物,获得它们的方法在生产药理剂中的用途,作为这样的药理剂和获得该药理剂的方法

摘要

The present invention relates to compounds of the general formula CHEM wherein R1 - R4 signify independently hydrogen, -CF3, -OCF3, OCHF2, -OCH2F, lower alkyl, lower alkoxy, halogen, hydroxy, phenyl, benzyl, amino, nitro, pyrrol-1-yl, lower alkyl-sulfonyl, lower alkyl-sulfanyl, cyano or benzyloxy; or R2 and R3 may be together -O-(CH2)2-O-, -O-CH2-O-, -O-(CH2)2-, -(CH2)3- or -CH=CH-CH=CH-; X signifies -N=, -N(R8)- or -CH=; Y signifies -N=, =N-, -N(R8)- or -CH=; wherein one of X or Y has to be nitrogen; R5 signifies the group CHEM wherein R6 and R7 signify independently from each other hydrogen, lower alkyl, -C(O)-lower alkyl, hydroxy-lower alkyl, lower alkenyl, -C(O)CH2OH or R6 and R7 may be together with the N-atom -(CH2)n-, -(CH2)2-O-(CH2)2-, -CH2-CH=CH-CH2, -CH2-CH OC(O)CH3­-(CH2)2, -CH2-CH NHC(O)CH3­-(CH2)2, -O-(CH2)3-, -CH2-CH(OCH3)-(CH2)2-, -CH2-CH(halogen)-(CH2)2-, -(CH2)2-CH(O-phenyl)-(CH2)2-, -(CH2)2-N(CHO)-(CH2)2-, -(CH2)2-N(COCH3)-(CH2)2-, -CH2-CH(OH)-(CH2)3-, -(CH2)2-CH(OH)-(CH2)2- or -(CH2)2-N(benzyl)-CH2)2-; n signifies 3 to 5; and R8 signifies hydrogen, lower alkyl, lower alkenyl, lower alkinyl, -(CH2)m-O-lower alkyl, -(CH2)m-OH, -(CH2)m-CHF2, -(CH2)m-CH2F, -(CH2)m-C(O)-lower alkyl, - (CH2)m-C(O)O-lower alkyl, -(CH2)m-CH(OH)-lower alkyl, -(CH2)m-CH(OH)-(CH2)mOH, -(CH2)m-C6H5, which phenyl ring is optionally substituted by lower alkyl, lower alkoxy or hydroxy, -(CH2)m-C(=CH2)-lower alkyl, - (CH2)m-cycloalkyl, -(CH2)m-CN, -(CH2)m-pyridin-4-yl, -(CH2)m-pyridin-3-yl or - (CH2)m-pyridin-2-yl; m signifies 0 to 4; and to their pharmaceutically acceptable acid addition salts. These compounds may be used for the treatment of diseases related to the NMDA receptor subtype selective blockers.
机译:本发明涉及通式的化合物,其中R 1 -R 4独立地表示氢,-CF 3,-OCF 3,OCHF 2,-OCH 2 F,低级烷基,低级烷氧基,卤素,羟基,苯基,苄基,氨基,硝基,吡咯-1-基,低级烷基磺酰基,低级烷基硫烷基,氰基或苄氧基;或R 2和R 3可以一起是-O-(CH 2)2 -O-,-O-CH 2 -O-,-O-(CH 2)2-,-(CH 2)3-或-CH。 = CH-CH = CH-; X表示-N =,-N(R <8>)-或-CH =; Y表示-N =,= N-,-N(R 8)-或-CH =;其中X或Y之一必须是氮; R 5表示基团,其中R 6和R 7彼此独立地表示氢,低级烷基,-C(O)-低级烷基,羟基-低级烷基,低级烯基,-C( O)CH 2 OH或R 6和R 7可与N原子-(CH2)n-,-(CH2)2-O-(CH2)2-,-CH2-CH = CH-CH2一起,-CH2-CH OC(O)CH3-(CH2)2,-CH2-CH NHC(O)CH3-(CH2)2,-O-(CH2)3-,-CH2-CH(OCH3)-(CH2 )2-,-CH2-CH(卤素)-(CH2)2-,-(CH2)2-CH(O-苯基)-(CH2)2-,-(CH2)2-N(CHO)-(CH2 )2-,-(CH2)2-N(COCH3)-(CH2)2-,-CH2-CH(OH)-(CH2)3-,-(CH2)2-CH(OH)-(CH2)2 -或-(CH2)2-N(苄基)-CH2)2-; n表示3至5; R 8表示氢,低级烷基,低级烯基,低级炔基,-(CH2)mO-低级烷基,-(CH2)m-OH,-(CH2)m-CHF2,-(CH2)m-CH2F, -(CH2)mC(O)-低级烷基,-(CH2)mC(O)O-低级烷基,-(CH2)m-CH(OH)-低级烷基,-(CH2)m-CH(OH)- (CH 2)m OH,-(CH 2)m -C 6 H 5,其中苯环任选地被低级烷基,低级烷氧基或羟基取代,-(CH 2)m C(= CH 2)-低级烷基,-(CH 2)m-环烷基,- (CH2)m-CN,-(CH2)m-吡啶-4-基,-(CH2)m-吡啶-3-基或-(CH2)m-吡啶-2-基; m表示0到4;以及它们的药学上可接受的酸加成盐。这些化合物可用于治疗与NMDA受体亚型选择性阻滞剂有关的疾病。

著录项

  • 公开/公告号PL341616A1

    专利类型

  • 公开/公告日2001-01-29

    原文格式PDF

  • 申请/专利权人 F.HOFFMANN-LA ROCHE AG;

    申请/专利号PL20000341616

  • 发明设计人

    申请日2000-07-21

  • 分类号C07D233/64;C07D249/08;C07D401/10;C07D403/10;C07D405/10;A61K31/4164;A61K31/4178;A61K31/4196;A61P25/24;A61P25/28;

  • 国家 PL

  • 入库时间 2022-08-22 01:24:05

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