| 摘要 |
FIELD: chemistry. ^ SUBSTANCE: invention relates to the novel inhibitor of phosphodiesterase (PDE) IV and/or to the tumor necrosis factor (TNF) production inhibitor, which corresponds to the compound with formula (I), where R1 is: (1) mono- or di(inferior)alkylamino, (2) phenyl, (3) saturated or unsaturated 5-or 6-membered heteromonocyclic group, selected from a group which includes pyrrolidinyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, furanyl, thienyl and piridinyl, or (4) inferior alkyl not necessarily substituted with (i) inferior alkoxi or (ii) saturated 5- or 6-membered heteromonocyclic group, selected from the group, consisting of piperazinyl and morpholinyl, where the inferior alkoxi is not necessarily substituted with cyclo(inferior)alkyl or piridinyl, R2 corresponds to R7 or - A2R7 , where A2 is -(CH2)n- or -(CH=CH)m- [where n is an even number within 2 to 6, and m is an even number 1 or 2], and R7 is a hydrogen, inferior alkylsulfonyl, carboxy, etherificated carboxy or piridinyl; R3 is: (1) phenyl, not necessarily substituted with inferior alkyl, cyclo(inferior)alkyl, inferior alkoxi, halogen, cyano or carbamoyl; or (2) quinolinyl; or piridinyl, substituted with inferior alkyl, cyclo(inferior)alkyl, inferior alkoxi, carbamoyl or halogen, and R4 corresponds to the inferior alkyl, or its pharmaceutically acceptable salt. The application of the compound with formula is invented, for producing the therapeutic agent with the PDE IV and/or TNF production inhibiting activity and the pharmaceutical composition containing the effective amount of compounds with formula (I) mixed with the pharmaceutically acceptable carriers. The method for prevention and treatment of the diseases where the application of the PDE IV and/or TNF production inhibitor is considered to be reasonable, including the administration of the therapeutically effective amount of the compound with formula (I). The method for prevention and treatment of asthma, chronic obstructive pulmonary disease, fibrous disorders, acute and fulminant hepatitis, hepatic steatosis, chronic hepatitis, cirrhosis, autoimmune hepatitis, autoimmune inflammatory intestine disease, atopic dermatitis, Alzheimer's disease or viral infection, including the administration of the therapeutically or preventively effective amount of the compound with formula (I). ^ EFFECT: compound with the PDE IV and/or TNF production inhibiting activity. ^ 11 cl, 2 tbl, 672 ex |
