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PDE TV INHIBITING 2-CYANOIMINOIMIDAZOLE DERIVATIVES

机译:PDE TV抑制2-氰基亚氨基咪唑衍生物

摘要

The present invention concerns 2-cyanoiminoimidazole derivatives having formula (I) the N-oxide forms, the pharmaceuticallyacceptable addition salts and the stereochemically isomeric forms thereof, wherein R[err] and R[err] each independently are hydrogen; C[err]alkyl;difluoromethyl; trifluoromethyl; C[err]cycloakyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatomsselected from oxygen, sulfur or nitrogen; indanyl; 6,7-dihydro-5H-cyclopentapyridinyl; bicyclo[2,2,1]-2-heptenyl; bicyclo[2.2.1]heptanyl;C[err]-alkylsulfonyl; arylsulfonyl; or substituted C[err]alkyl; R[err] is hydrogen, halo or C[err]alkyloxy; R[err] is hydrogen; halo; C[err]alkyl;trifluoromethyl; -C[err]cycloalkyl; carboxyl; C[err]alkyloxycarbonyl; C[err]cycloalkylaminocarbonyl; aryl; Het[err]; or substituted C[err]alkyl; orR[err] is -O-R[err] or -NH-R[err]; R[err] is hydrogen, halo, hydroxy, C[err]alkyl or C[err]alkyloxy; R[err] is a hydrogen or C[err]alkyl; or R[err] and R[err], or R[err] andR[err] taken together may form a bivalent radical; -A-B- is -CR[err]-CR[err]- or -CHR[err]-CHR[err]-; L is hydrogen; C[err]alkyl; C[err]alkylcarbonyl;C[err]alkyloxycarbonyl; substituted C[err]alkyl; C[err]alkenyl; substituted C[err]alkenyl; piperidinyl; substituted piperidinyl; C[err]alkylsulfonyl orarylsulfonyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds offormula (I) and pharmaceutical compositions thereof.
机译:本发明涉及具有式(I)的N-氧化物形式的2-氰基氨基咪唑衍生物,可接受的加成盐及其立体化学异构形式,其中R [err]和R [err]各自独立地是氢; C [err]烷基;二氟甲基三氟甲基; C [err]环烷基;含有一个或两个杂原子的饱和5元,6元或7元杂环选自氧,硫或氮;茚满基; 6,7-二氢-5H-环戊啶基;双环[2,2,1] -2-庚烯基;双环[2.2.1]庚基;C [err]-烷基磺酰基;芳基磺酰基;或取代的C [err]烷基; R [err]为氢,卤素或C [err]烷氧基; R [err]是氢;光环; C [err]烷基;三氟甲基; -C [err]环烷基;羧基; C [err]烷氧基羰基; C [err]环烷基氨基羰基;芳基Het [err];或取代的C [err]烷基;要么R [err]是-O-R [err]或-NH-R [err]; R [err]是氢,卤素,羟基,C [err]烷基或C [err]烷氧基; R [err]是氢或C [err]烷基;或R [err]和R [err],或R [err]和R [err]一起可以形成二价基团; -A-B-是-CR [err] -CR [err]-或-CHR [err] -CHR [err]-; L是氢; C [err]烷基; C [err]烷基羰基;C [err]烷氧基羰基;取代的C [err]烷基; C [err]烯基;取代的C [err]烯基;哌啶基;取代的哌啶基; C [err]烷基磺酰基或芳基磺酰基;具有PDE IV和细胞因子抑制活性。本发明还涉及制备以下化合物的方法式(I)及其药物组合物。

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