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    Il-5 inhibiting 6-azauracil derivatives
    1.
    发明授权
    Il-5 inhibiting 6-azauracil derivatives 失效
    Il-5抑制6-氮尿嘧啶衍生物

    公开(公告)号：US06498158B1

    公开(公告)日：2002-12-24

    申请号：US09856626

    申请日：2001-05-22

    申请人： Jean Fernand Armand Lacrampe ,  Yannick Ligny ,  Eddy Jean Edgard Freyne ,  Frederik Dirk Deroose

    发明人： Jean Fernand Armand Lacrampe ,  Yannick Ligny ,  Eddy Jean Edgard Freyne ,  Frederik Dirk Deroose

    IPC分类号： C07D253075

    CPC分类号： C07D253/075 ,  C07D405/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14

    摘要： The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 3; q is 0 to 4; —A—B— represents —(CH2)r—, —(CH2)t—O—, —(CH2)t—S(═O)u— or —(CH2)t—NR3—; r is 2 to 4; t is 1 to 3; u is 0 to 2; X1 is O, S, NR3 or a direct bond; R1 and R4 are C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or substituted C1-4alkyl; R2 is aryl, Het1, C3-7cycloalkyl, cyano, optionally substituted C1-6alkyl, —C(═Q)—X2—R15; R3 is hydrogen or C1-4alkyl; R15 is hydrogen, optionally substituted C1-6alkyl, C3-7cycloalkyl, aryl; where X2 is a direct bond, R15 may also be halo or Het1; where X2 is NR5, R15 may also be hydroxy; where X2 is C(═O)—NH—NH or NH—NH—C(═O), R15 may be replaced by R11; Q is O, S or NR3; X2 is O, S, NR5, C(═O)—NH—NH, NH—NH—C(═O) or a direct bond; R5 is hydrogen, C1-6alkyl, C1-6alkyloxy or arylC1-6alkyl; R6 is a sulfonyl or sulfinyl derivative; R7 and R8 are independently hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl containing moiety, C3-7cycloalkyl, —Y-C1-4alkanediyl-C(═O)—O—R14, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, formyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, C1-4alkanediyl-C(═O)—O—R14, —C(═O)—O—R14, —Y-C1-4alkanediyl-C(═0)—O—R14, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3, Het4 and C(═O)Het3; aryl is optionally substituted phenyl; Het1, Het2, Het3 and Het4 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

    摘要翻译： 本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐和立体化学异构形式，其中p为0-3; q为0〜4; -A-B-表示 - （CH 2）r - ， - （CH 2）t -O-， - （CH 2）t -S（= O）u - 或 - （CH 2）t -NR 3 - ; r为2〜4; t为1〜3; 你是0到2; X1是O，S，NR3或直接键; R 1和R 4是C 1-6烷基，卤素，多卤代C 1-6烷基，羟基，巯基，C 1-6烷氧基，C 1-6烷硫基，C 1-6烷基羰氧基，芳基，氰基，硝基，Het 3，R 6，NR 7 R 8或取代的C 1-4烷基; R 2是芳基，Het 1，C 3-7环烷基，氰基，任选取代的C 1-6烷基，-C（= Q）-X 2 -R 15; R3是氢或C1-4烷基; R 15是氢，任选取代的C 1-6烷基，C 3-7环烷基，芳基; 其中X2是直接键，R15也可以是卤素或Het1; 其中X2是NR5，R15也可以是羟基; 其中X 2是C（= O）-NH-NH或NH-NH-C（= O），R 15可以被R 11取代; Q是O，S或NR 3; X2是O，S，NR5，C（= O）-NH-NH，NH-NH-C（= O）或直接键; R5是氢，C1-6烷基，C1-6烷氧基或芳基C1-6烷基; R6是磺酰基或亚磺酰基衍生物; R 7和R 8独立地为氢，任选取代的C 1-4烷基，芳基，含羰基部分，C 3-7环烷基，-Y-C 1-4烷二基-C（= O）-O-R 14，Het 3

    IL-5 inhibiting 6-azauracil derivatives
    3.
    发明授权
    IL-5 inhibiting 6-azauracil derivatives 失效
    IL-5抑制6-氮尿嘧啶衍生物

    公开(公告)号：US06469001B1

    公开(公告)日：2002-10-22

    申请号：US09856625

    申请日：2001-05-22

    申请人： Eddy Jean Edgard Freyne ,  Frederik Dirk Deroose ,  Davy Petrus Franciscus Maria Petit ,  Jean Fernand Armand Lacrampe

    发明人： Eddy Jean Edgard Freyne ,  Frederik Dirk Deroose ,  Davy Petrus Franciscus Maria Petit ,  Jean Fernand Armand Lacrampe

    IPC分类号： C07D253075

    CPC分类号： C07D253/075 ,  C07D417/10

    摘要： The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 3; q is 0 to 5; —A—B— is —(CH2)r—, —(CH2)t—O—, —(CH2)t—S(═O)u— or —(CH2)t—NR3—; r is 2 to 4; t is 1 to 3; u is 0 to 2; X1 is O, S, NR3 or a direct bond; R1 and R4 are C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or C1-4alkyl substituted with Het3, R6 or NR7R8; R2 represents aryl, Het1, C3-7cycloalkyl, cyano, C1-6alkyl, —C(═Q)—X2—R15 or C1-6alkyl substituted with one or two substituents selected from hydroxy, cyano, amino, mono- or di(C1-4alkyl)amino, C1-6alkyloxy, C1-6alkylsulfonyloxy, C1-6alkyloxycarbonyl, C3-7cycloalkyl, aryl, aryloxy, arylthio, Het1, Het1 oxy, Het1 thio and —C(═Q)—X2—R15; R3 is hydrogen or C1-4alkyl; R15 is hydrogen, optionally substituted C1-6alkyl, C3-7cycloallcyl, aryl; where X2 is a direct bond, R15 is also halo or Het1; where X2 is NR5, R15 is also hydroxy; where X2 is C(═O)—NH—NH or NH—NH—C(═O), R15 is replaced by R11; R5 is hydrogen, C1-6alkyl, C1-6alkyloxy or arylC1-6alkyl; Q is O, S or NR3; X2 is O, S, NR5, C(═O)—NH—NH, NH—NH—C(═O) or a direct bond; R6 is a sulfonyl or sulfinyl derivative; R7 and R8 are independently hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl containing moiety, C3-7cycloalkyl, —Y—C1-4alkanediyl—C(═O)—O—R14, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, formyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, C1-4alkanediyl—C(═O)—O—R14, —C(═O)—O—R14,. —Y—C1-4alkanediyl—C(═O)—O—R14, aryl, aryloxy, arcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3, Het4 and C(═O)Het3; aryl is optionally substituted phenyl; Het1, Het2, Het3 and Het4 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

    摘要翻译： 本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐和立体化学异构形式，其中p为0-3; q为0〜5; -A-B-是 - （CH 2）r - ， - （CH 2）t -O-， - （CH 2）t -S（= O）u - 或 - （CH 2）t -NR 3 - ; r为2〜4; t为1〜3; 你是0到2; X1是O，S，NR3或直接键; R 1和R 4是C 1-6烷基，卤素，多卤代C 1-6烷基，羟基，巯基，C 1-6烷氧基，C 1-6烷硫基，C 1-6烷基羰基氧基，芳基，氰基，硝基，Het 3，R 6，NR 7 R 8或被Het 3， 或NR7R8; R 2表示芳基，Het 1，C 3-7环烷基，氰基，C 1-6烷基，-C（= Q）-X 2 -R 15或被一个或两个选自羟基，氰基，氨基，单 - 或二 1-4烷基）氨基，C 1-6烷氧基，C 1-6烷基磺酰氧基，C 1-6烷氧基羰基，C 3-7环烷基，芳基，芳氧基，芳硫基，Het 1，Het 1氧基，Het 1硫基和-C（= Q）-X 2 -R 15; R3是氢或C1-4烷基; R 15是氢，任选取代的C 1-6烷基，C 3-7环烷基，芳基; 其中X2是直接键，R15也是卤素或Het1; 其中X2是NR5，R15也是羟基; 其中X2是C（= O）-NH-NH或NH-NH-C（= O），R15被R11代替; R5是氢，C1-6烷基，

    Il-5 inhibiting 6-azauracil derivatives
    5.
    发明授权
    Il-5 inhibiting 6-azauracil derivatives 失效
    Il-5抑制6-氮尿嘧啶衍生物

    公开(公告)号：US06803364B1

    公开(公告)日：2004-10-12

    申请号：US09868384

    申请日：2001-08-29

    申请人： Eddy Jean Edgard Freyne ,  Frederik Dirk Deroose ,  Jean Fernand Armand Lacrampe ,  Werner Constant Johan Embrechts ,  Jerome Michel Claude Fortin

    发明人： Eddy Jean Edgard Freyne ,  Frederik Dirk Deroose ,  Jean Fernand Armand Lacrampe ,  Werner Constant Johan Embrechts ,  Jerome Michel Claude Fortin

    IPC分类号： C07D25306

    CPC分类号： C07D253/075 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14

    摘要： The present invention is concerned with the compounds of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein p is 0 to 4; q is 0 to 5; X is O, S, NR3 or a direct bond; or —X—R2 is CN; R1 is H, OH, halo, NH2, mono- or di(C1-4alkyl)NH2, C1-6alkyl, C1-6alkylO, C3-7cycloalkyl, aryl, arylC1-6alkyl, NH2C1-4akyl, mono- or di(C1-4alkyl)NH2C1-4akyl or mono- or di(C1-4alkyl)NH2C1-4alkylNH2; R2 is aryl, Het1, optionally substituted C3-7cycloalkyl, optionally substituted C1-6alkyl; R3 is H or C1-4alkyl; R4 and R5 are —C(═O)—Z—R14, C1-6alkyl, halo, polyhaloC1-6alkyl, OH, mercapto, C1-6alkylO, C1-6alkylthio, C1-6alkylC(═O)O, aryl, cyano, nitro, Het3, R6, NR7R8 or C1-4alkyl substituted with —C(═O)—Z—R14, Het3, R6 or NR7R8; Z is O, S, NH, —CH2O or —CH2—S—; R14 is H, C1-20acyl, optionally substituted C1-20alkyl, optionally substituted C3-20alkenyl, C3-20alkynyl, C3-7cycloalkyl, polyhaloC1-20alkyl, Het5, phenyl; or R14 is an oxygen containing radical; aryl is optionally substituted phenyl; Het1, Het2, Het3 and Het5 are optionally substituted heterocycles; Het4 is a monocyclic heterocycle; provided however that R2 is other than NH2C(═O), C1-6alkylOC(═O)C1-6alkyl; and R11 is other than COOH, C1-4alkylOC(═O), NH2C(═O), C1-4alkylNH2C(═O), OHC1-4alkylNH2C(═O), C1-4alkylC(═O)NH2C(═O), C3-7cycloalkylNH2C(═O); and R7, R8, R9, R10, R12, R13, R15 and R16 are other than C1-4alkylC(═O)OC1-4alkylC(═O), OHC1-4alkylC(═O); and Het3 is other than a monocyclic heterocycle substituted with COOH or C1-4alkylOC(═O); and the compounds of formula (I) contain at least one —C(═O)—Z—R14 moiety: to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

    摘要翻译： 本发明涉及式（I）化合物，N-氧化物，药学上可接受的加成盐，季胺或其立体化学异构形式，其中p为0至4; q为0〜5; X是O，S，NR 3或直接键; 或-X-R 2为CN; R 1是H，OH，卤素，NH 2，单或二（C 1-4烷基）NH 2，C 1-6烷基，C 1-6烷基O，C 3-7环烷基，芳基，芳基C 1-6烷基，NH 2 C 1-4烷基，单或二 （C 1-4烷基）NH 2 C 1-4芳基或单或二（C 1-4烷基）NH 2 C 1-4烷基NH 2; R 2是芳基，Het 1，任选取代的C 3-7环烷基，任选取代的C 1-6烷基; R 3是H或C 1-4烷基; R 4和R 5是-C（= O）-ZR 14，C 1-6烷基，卤素，多卤代C 1-6烷基，OH，巯基，C 1-6烷基O，C 1-6烷硫基，C 1-6烷基C（= O ）O，芳基，氰基，硝基，Het 3，R 6，NR 7 R 8或被-C（= O）-ZR 14，Het 3取代的C 1-4烷基， R 6或NR 7 R 8; Z是O，S，NH，-CH 2 O或-CH 2 -S-; R 14是H，C 1-20酰基，任选取代的C 1-20烷基，任选取代的C 3-20烯基，C 3-20炔基，C 3-7环烷基，多卤代C 1-20烷基，Het 5，苯基; 或R 14是含氧基团; 芳基是任选取代的苯基; Het 1，Het 2，Het 3和Het 5是任选取代的杂环; Het 4是单环杂环; 但是R 2不是NH

    4,5-dihydro-isoxazole derivatives and their pharmaceutical use
    7.
    发明授权
    4,5-dihydro-isoxazole derivatives and their pharmaceutical use 失效
    4,5-二氢异恶唑衍生物及其药物用途

    公开(公告)号：US06583141B1

    公开(公告)日：2003-06-24

    申请号：US09807149

    申请日：2001-04-06

    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

    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

    IPC分类号： C07D41304

    CPC分类号： C07D413/04 ,  C07D261/04 ,  C07D413/14

    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.

    摘要翻译： 本发明涉及糠醛的化合物m，n和p各自独立地为0或1，q为0,1,2,3,4或5; -A1 = A2-A3 = A4-是亚吡啶基，哒嗪亚基，亚嘧啶亚基，亚吡嗪基或亚苯基; B代表酰胺，酮或恶二唑; D表示Ar或Het; Q表示共价直接键或酮，-N-，-O-，-CR5R6-，酰胺乙烯基，亚胺，磺酰基，亚磺酰基，3-氧代丁烯基，吡唑，异恶唑或噻唑; L表示Ar或Het; R1表示氢，卤素，羟基，C（2-6）烯基，C（2-6）炔基，C（3-6）环烷基，C（3-6）环烯基，氰基，胍，硝基，NR17R18， 取代的C（1-6）烷基或C（1-6）烷氧基; R2和R3各自独立地表示氢，卤素，C（1-6）烷氧基或任选取代的C 1-6烷基; R 5和R 6各自独立地表示氢，羟基，卤素，任选取代的C 1-6烷基，C（2-6）烯基，C（2-6）炔基，C（3-6）环烷基，C（3） -6）环烯基，C（1-6）烷氧基，氰基，（C = O）R25，（C = O）OR16，（SO2）R16，氨基羰基氧基，氨基C（1-6）烷基，NR17R18，N3，Ar或 Het; 或R 5和R 6与它们所连接的碳原子一起形成Ar或Het; Ar表示任选取代的C（6-14）芳基; Het表示任选取代的C（1-14）杂环; 或N-氧化物，药学上可接受的加成盐，季胺或其立体化学异构体形式; 其制备方法和包含它们的组合物。 它还涉及它们作为药物的用途。