发明授权
- 专利标题: 4,5-dihydro-isoxazole derivatives and their pharmaceutical use
- 专利标题(中): 4,5-二氢异恶唑衍生物及其药物用途
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申请号: US09807149申请日: 2001-04-06
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公开(公告)号: US06583141B1公开(公告)日: 2003-06-24
- 发明人: Eddy Jean Edgard Freyne , José Ignacio Andrés-Gil , Frederik Dirk Deroose , Davy Petrus Franciscus Maria Petit , Maria Encarnacion Matesanz-Ballesteros , Rosa Maria Alvarez Escobar
- 申请人: Eddy Jean Edgard Freyne , José Ignacio Andrés-Gil , Frederik Dirk Deroose , Davy Petrus Franciscus Maria Petit , Maria Encarnacion Matesanz-Ballesteros , Rosa Maria Alvarez Escobar
- 优先权: EP98203394 19981009
- 主分类号: C07D41304
- IPC分类号: C07D41304
摘要:
The present invention is concerned with the compounds of formula wherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; —A1═A2—A3═A4— is a pyridinylidene, pyridazinylidene, pyrimidinylidene, pyrazinylidene or phenylidene; B represents an amide, ketone or oxadiazole; D represents Ar or Het; Q represents a covalent direct bond or a ketone, —N—, —O—, —CR5R6—, amide ethenyl, imine, sulfonyl, sulfinyl, 3-oxobutenyl, pyrazole, isoxazole or thiazole; L represents Ar or Het; R1 represents hydrogen, halo, hydroxy, C(2-6)alkenyl, C(2-6)alkynyl, C(3-6)cycloalkyl, C(3-6)cycloalkenyl, cyano, guanidine, nitro, NR17R18, an optionally substituted C(1-6)alkyl or C(1-6)alkyloxy; R2 and R3 each independently represent hydrogen, halo, C(1-6)alkyloxy or an optionally substituted C(1-6)alkyl; R5 and R6 each independently represent hydrogen, hydroxy, halo, an optionally substituted C(1-6)alkyl, C(2-6)alkenyl, C(2-6)alkynyl, C(3-6)cycloalkyl, C(3-6)cycloalkenyl, C(1-6)alkyloxy, cyano, (C═O)R25, (C═O)OR16, (SO2)R16, aminocarbonyloxy, aminoC(1-6)alkyl, NR17R18, N3, Ar or Het; or R5 and R6 together with the carbon atom to which they are attached, form an Ar or Het; Ar represents an optionally substituted C(6-14)aryl; Het represents an optionally substituted C(1-14)heterocycle; or a N-oxide, pharmaceutically acceptable addition salt, quaternary amine or stereochemically isomeric form thereof; the processes for their preparation and compositions comprising them. It further relates to their use as a medicine.
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