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    2-amino-4,5-trisubstituted thiazolyl derivatives
    1.
    发明授权
    2-amino-4,5-trisubstituted thiazolyl derivatives 有权
    2-氨基-4,5-三取代噻唑基衍生物

    公开(公告)号：US07232838B2

    公开(公告)日：2007-06-19

    申请号：US10486819

    申请日：2002-08-09

    申请人： Christopher John Love ,  Guy Rosalia Eugeen Van Lommen ,  Julien Georges Pierre-Olivier Doyon ,  Jean-Pierre André Marc Bongartz ,  Marcel Jozef Maria Van der AA ,  Robert Jozef Maria Hendrickx ,  Peter Jacobus Johannes Antonius Buijnsters ,  Ludwig Paul Cooymans ,  Nele Vandermaesen ,  Erwin Coesemans ,  Gustaaf Maria Boeckx

    发明人： Christopher John Love ,  Guy Rosalia Eugeen Van Lommen ,  Julien Georges Pierre-Olivier Doyon ,  Jean-Pierre André Marc Bongartz ,  Marcel Jozef Maria Van der AA ,  Robert Jozef Maria Hendrickx ,  Peter Jacobus Johannes Antonius Buijnsters ,  Ludwig Paul Cooymans ,  Nele Vandermaesen ,  Erwin Coesemans ,  Gustaaf Maria Boeckx

    IPC分类号： A61K31/425 ,  C07D277/00 ,  C07D277/20

    CPC分类号： C07D417/04 ,  C07D277/42 ,  C07D471/04

    摘要： This invention concerns the use of a compound of formula (I′), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxy -carbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(═O)2—; mono- or di(C1-6alkyl)aminoS(═O)2; —C(═N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula (b-1), (b-2), or (b-3), L is optionally substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of inflammatory and/or auto-immune diseases mediated through TNF-α and/or IL-12

    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，季胺及其立体化学异构体形式的用途，其中Z是卤素; C 1-6烷基; C 1-6烷基羰基; C 1-6烷氧基羰基; 氨基羰基; 用羟基，羧基，氰基，氨基，被哌啶取代的氨基，被C 1-4烷基取代的哌啶基取代的氨基，单或二（ C 1-6烷基）氨基，氨基羰基，一或二（C 1-6烷基）氨基羰基，C 1-6烷氧基羰基， C 1-6烷基氧基，哌啶基，哌嗪基，吗啉基，硫代吗啉基; 多卤代1-4烷基; 氰基; 氨基; 单或二（C 1-6烷基）氨基羰基; C 1-6烷氧基羰基; C 1-6烷基羰基氧基; 氨基-S（-O）2 - ; 单或二（C 1-6烷基）氨基S（-O）2; -C（-N-R x X）NR z R z Z; Q为任选取代的C 3-6环烷基，苯基，吡啶基，嘧啶基，吡嗪基，哒嗪基，苯并噻唑基，苯并恶唑基，苯并咪唑基，吲唑基或咪唑并吡啶基，或Q为式（b-1） ，（b-2）或（b-3）中，L是任选取代的苯基或任选取代的单环5或6元部分饱和或芳族杂环或双环部分饱和或芳族杂环; 芳基是任选取代的苯基; 用于制备用于预防或治疗通过TNF-α和/或IL-12介导的炎症和/或自身免疫疾病的药物

    Angiogenesis inhibiting 5-substituted-1,2,4,-thiadiazolyl derivatives
    2.
    发明授权
    Angiogenesis inhibiting 5-substituted-1,2,4,-thiadiazolyl derivatives 失效
    血管发生抑制5-取代-1,2,4-噻二唑衍生物

    公开(公告)号：US06833369B2

    公开(公告)日：2004-12-21

    申请号：US09998975

    申请日：2001-10-19

    申请人： Raymond Antoine Stokbroekx ,  Marc André Ceusters ,  Marcel Jozef Maria Van der Aa ,  Marcel Gerebernus Maria Luyckx ,  Marc Willems ,  Robert W. Tuman

    发明人： Raymond Antoine Stokbroekx ,  Marc André Ceusters ,  Marcel Jozef Maria Van der Aa ,  Marcel Gerebernus Maria Luyckx ,  Marc Willems ,  Robert W. Tuman

    IPC分类号： A61K31496

    CPC分类号： C07D213/83 ,  A61K31/454 ,  C07D241/26 ,  C07D285/08 ,  C07D285/135 ,  C07D295/155 ,  C07D417/04 ,  C07D417/12

    摘要： This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1NH—, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 is hydrogen, C1-6alkyl, amino, aminocarbonyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl, C1-6alkylcarbonylamino, hydroxy or C1-6alkyloxy; R3, R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; is Ar2, Ar2CH2— or Het2; Ar1 and Ar2 optionally substituted phenyl; Het1 and Het2 are optionally substituted monocyclic heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中X是CH或N; R 1是氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，单或二（C 1-6烷基）氨基，Ar 1，Ar 1 NH-，C 3-6环烷基，羟甲基或 苄氧基甲基 R 2是氢，C 1-6烷基，氨基，氨基羰基，一或二（C 1-6烷基）氨基，C 1-6烷氧基羰基，C 1-6烷基羰基氨基，羟基或C 1-6烷氧基; R 3，R 4和R 5各自独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，三氟甲基，硝基，氨基，氰基，叠氮基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基 C 1-6烷氧基羰基或Het 1; Ar 2，Ar 2 CH 2 - 或Het 2; Ar 1和Ar 2任选取代的苯基; Het 1和Het 2是任选取代的单环杂环; 具有血管生成抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

    Angiogenesis inhibiting 5-substituted-1,2,4-thiadiazolyl derivatives
    6.
    发明授权
    Angiogenesis inhibiting 5-substituted-1,2,4-thiadiazolyl derivatives 失效
    血管发生抑制5-取代-1,2,4-噻二唑衍生物

    公开(公告)号：US07208503B2

    公开(公告)日：2007-04-24

    申请号：US10387703

    申请日：2003-03-13

    申请人： Raymond Antoine Stokbroekx ,  Marc André Ceusters ,  Marcel Jozef Maria Van der Aa ,  Marcel Gerebernus Maria Luyckx ,  Marc Willems ,  Robert W. Tuman

    发明人： Raymond Antoine Stokbroekx ,  Marc André Ceusters ,  Marcel Jozef Maria Van der Aa ,  Marcel Gerebernus Maria Luyckx ,  Marc Willems ,  Robert W. Tuman

    IPC分类号： A01N43/40 ,  A61K31/445 ,  C07D211/68

    CPC分类号： C07D285/08 ,  A61K31/454 ,  A61K31/496 ,  C07D285/135 ,  C07D417/04

    摘要： This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1NH—, C3-6cycloalkyl, hydroxymethyl or benzoyloxymethyl; R2 is hydrogen, C1-6alkyl, amino, aminocarbonyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl, C1-6alkylcarbonylamino, hydroxy or C1-6alkyloxy; R3, R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; is Ar2, Ar2CH2— or Het2; Ar1 and Ar2 optionally substituted phenyl; Het1 and Het2 are optionally substituted monocyclic heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中X是CH或N; R 1是氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基 ，氨基，单或二（C 1-6烷基）氨基，Ar 1，Ar 1，NH 3，C 3 -6个环烷基，羟甲基或苯甲酰氧基甲基; R 2是氢，C 1-6烷基，氨基，氨基羰基，一或二（C 1-6烷基）氨基，C C 1-6烷氧基羰基，C 1-6烷基羰基氨基，羟基或C 1-6烷氧基; R 3，R 4和R 5各自独立地选自氢，卤素，C 1-6烷基 C 1-6烷氧基，三氟甲基，硝基，氨基，氰基，叠氮基，C 1-6烷基氧基C 1-6烷基，C 1〜 C 1-6烷硫基，C 1-6烷氧基羰基或Het 1; 是Ar 2，Ar 2，CH 2或Het 2; Ar 1和Ar 2任选取代的苯基; Het 1和H 2 2是任选取代的单环杂环; 具有血管生成抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

    Angiogenesis inhibiting thiadiazolyl pyridazine derivatives
    8.
    发明授权
    Angiogenesis inhibiting thiadiazolyl pyridazine derivatives 失效
    血管发生抑制噻二唑基哒嗪衍生物

    公开(公告)号：US06265407B1

    公开(公告)日：2001-07-24

    申请号：US09446495

    申请日：2000-08-14

    申请人： Raymond Antoine Stokbroekx ,  Marc André Ceusters ,  Marcel Jozef Maria Van der Aa ,  Marcel Gerebernus Maria Luyckx ,  Marc Willems ,  Robert W. Tuman

    发明人： Raymond Antoine Stokbroekx ,  Marc André Ceusters ,  Marcel Jozef Maria Van der Aa ,  Marcel Gerebernus Maria Luyckx ,  Marc Willems ,  Robert W. Tuman

    IPC分类号： A61K31501

    CPC分类号： C07D417/04 ,  C07D417/14

    摘要： This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1—NH—, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 and R3 are hydrogen, or taken together may form a bivalent radical of formula —CH═CH—CH═CH—; R4, R5 and R6 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; or when R4 and R5 are adjacent to each other they may be taken together to form a radical of formula —CH═CH—CH═CH—; A is a bivalent radical of formula NR7, NR7—Alk1—X—, NR7—Alk1—X—Alk2—, O—Alk1—X—, O—Alk1—X—Alk2— or S—Alk1—X—; wherein X is a direct bond, —O—, —S—, C═O, —NR8— or Het2; R7 is hydrogen, C1-6alkyl or Ar2methyl; R8 is hydrogen, C1-6alkyl or Ar2methyl; Alk1 is C1-6alkanediyl; Alk2 is C1-4alkanediyl; Ar1 and Ar2 are optionally substituted phenyl; phenyl; Het1 and Het2 are optionally substituted heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中R 1是氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，单或二（C 1-6烷基 ）氨基，Ar1，Ar1-NH-，C3-6环烷基，羟甲基或苄氧基甲基; R2和R3是氢，或者可以一起形成式-CH = CH-CH = CH-的二价基团; R4，R5和R6各自独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，三氟甲基，硝基，氨基，氰基，叠氮基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基，C 1-6烷氧基羰基或Het 1; 或当R 4和R 5彼此相邻时，它们可以一起形成式-CH = CH-CH = CH-的基团; A是式NR7，NR7-Alk1-X，NR7-Alk1-X-Alk2-，O-Alk1-X，O-Alk1-X-Alk2-或S-Alk1-X-2的二价基; 其中X是直接键，-O - ， - S - ，C = O，-NR 8 - 或Het 2; R 7为氢，C 1-6烷基或Ar 2甲基; R8是氢，C1-6烷基或Ar2甲基; Alk1是C1-6烷二基; Alk2是C1-4烷二基; Ar1和Ar2是任选取代的苯基; 苯基; Het1和Het2是任选取代的杂环; 具有血管生成抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

    Angiogenesis inhibiting pyridazinamines
    9.
    发明授权
    Angiogenesis inhibiting pyridazinamines 失效
    血管发生抑制哒嗪胺

    公开(公告)号：US5985878A

    公开(公告)日：1999-11-16

    申请号：US119075

    申请日：1998-07-09

    申请人： Raymond Antoine Stokbroekx ,  Marcel Jozef Maria Van der Aa ,  Marc Willems ,  Lieven Meerpoel ,  Marcel Gerebernus Maria Luyckx ,  Robert Tuman

    发明人： Raymond Antoine Stokbroekx ,  Marcel Jozef Maria Van der Aa ,  Marc Willems ,  Lieven Meerpoel ,  Marcel Gerebernus Maria Luyckx ,  Robert Tuman

    IPC分类号： A61K31/00 ,  A61K31/50 ,  A61K31/501 ,  A61K31/505 ,  A61K31/517 ,  A61K31/529 ,  A61K31/55 ,  A61K31/551 ,  A61P9/00 ,  C07D417/04 ,  C07D417/14 ,  C07D451/02 ,  C07D471/08

    CPC分类号： C07D417/04 ,  C07D417/14

    摘要： This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; m is 2 or 3 and n is 1, 2 or 3; wherein 1 or 2 C-atoms of the CH.sub.2 groups of the ##STR1## moiety which may also contain one double bond, may be substituted with C.sub.1-6 alkyl, amino, aminocarbonyl, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkyloxycarbony, C.sub.1-6 alkylcarbonylamino, hydroxy or C.sub.1-6 alkyloxy; and/or 2 C-atoms of said CH.sub.2 groups may be bridged with C.sub.2-4 alkanediyl; R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, amino, mono- or di(C.sub.1-6 alkyl)amino, Ar, ArNH--, C.sub.3-6 cycloalkyl, hydroxymethyl or benzyloxymethyl; R.sup.2 and R.sup.3 are hydrogen, or taken together may form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH--; in case X represents CH then L is a radical L.sup.1, L.sup.2 or L.sup.3 ; or in case X represents N then L is a radical L.sup.2 or L.sup.3 ; L.sup.1 is Ar-C.sub.1-6 alkyloxy, Ar-oxy, Ar-thio, Ar-carbonylamino, di-Ar-methyloxy-, N-Ar-piperazinyl, N-Ar-homopiperazinyl, 2-benzimidazolinonyl, Ar--NR.sup.4 --, Ar-Alk-NR.sup.4 --, Ar--NR.sup.4 -Alk-NR.sup.5 -- or Het-NR.sup.4 --; L.sup.2 is Ar, Ar-carbonyl, Ar--CH.dbd.CH--CH.sub.2 --, naphtalenyl or Het; L.sup.3 is C.sub.1-6 alkyl substituted with one or two radicals selected from Ar, Ar-oxy, or Ar-thio, further optionally substituted with cyano or hydroxy; 2,2-dimethyl-1,2,3,4-tetrahydro-naphtalenyl; 2,2-dimethyl-1H-2,3-dihydroindenyl;Ar-piperidinyl or Ar--NR.sup.4 -Alk-; R.sup.4 and R.sup.5 are each independently selected from hydrogen or C.sub.1-6 alkyl; Alk is C.sub.1-6 alkanediyl; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中X是CH或N; m为2或3，n为1,2或3; 氨基，氨基羰基，一或二（C 1-6烷基）氨基，C 1-6烷氧基羰基，C 1 -C 6烷氧基羰基，C 1-6烷氧基羰基，C 1-6烷氧基羰基 -6-烷基羰基氨基，羟基或C 1-6烷氧基; 和/或所述CH 2基团的2个C原子可以与C 2-4烷二基桥接; R1是氢，C1-6烷基，C1-6烷氧基，C1-6烷硫基，氨基，一或二（C1-6烷基）氨基，Ar，ArNH-，C3-6环烷基，羟甲基或苄氧基甲基; R2和R3是氢，或者可以一起形成式-CH = CH-CH = CH-的二价基团; 在X表示CH的情况下，L是基团L 1，L 2或L 3; 或者在X表示N的情况下，则L是基团L2或L3; L 1是Ar-C 1-6烷氧基，Ar-氧基，Ar-硫代，Ar-羰基氨基，二-Ar-甲氧基 - ，N-Ar-哌嗪基，N-Ar-高哌嗪基，2-苯并咪唑啉酮基，Ar-NR4-， Alk-NR4-，Ar-NR4-Alk-NR5-或Het-NR4-; L2是Ar，Ar-羰基，Ar-CH = CH-CH 2 - ，萘基或Het; L3是被一个或两个选自Ar，Ar-氧基或Ar-硫基的基团取代的C 1-6烷基，进一步任选被氰基或羟基取代; 2,2-二甲基-1,2,3,4-四氢 - 萘基; 2,2-二甲基-1H-2,3-二氢茚基; Ar-哌啶基或Ar-NR4-Alk-; R 4和R 5各自独立地选自氢或C 1-6烷基; Alk是C1-6烷二基; 其制剂，含有它们的组合物及其作为药物的用途。

    Angiogenesis inhibiting thiadiazolyl pyridazine derivatives
    10.
    发明授权
    Angiogenesis inhibiting thiadiazolyl pyridazine derivatives 失效
    血管发生抑制噻二唑基哒嗪衍生物

    公开(公告)号：US06602873B2

    公开(公告)日：2003-08-05

    申请号：US09864594

    申请日：2001-05-24

    申请人： Raymond Antoine Stokbroekx ,  Marc André Ceusters ,  Marcel Jozef Maria Van der Aa ,  Marcel Gerebernus Maria Luyckx ,  Marc Willems ,  Robert W. Tuman

    发明人： Raymond Antoine Stokbroekx ,  Marc André Ceusters ,  Marcel Jozef Maria Van der Aa ,  Marcel Gerebernus Maria Luyckx ,  Marc Willems ,  Robert W. Tuman

    IPC分类号： A61K31501

    CPC分类号： C07D417/04 ,  C07D417/14

    摘要： This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1—NH—, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 and R3 are hydrogen, or taken together may form a bivalent radical of formula —CH═CH—CH═CH—; R4, R5 and R6 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; or when R4 and R5 are adjacent to each other they may be taken together to form a radical of formula —CH═CH—CH═CH—; A is a bivalent radical of formula NR7, NR7-Alk1-X-, NR7-Alk1-X-Alk2-, O-Alk1-X-, O-Alk1-X-Alk2- or S-Alk1-X-; wherein X is a direct bond, —O—, —S—, C═O, —NR8— or Het2; R7 is hydrogen, C1-6alkyl or Ar2methyl; R8 is hydrogen, C1-6alkyl or Ar2methyl; Alk1 is C1-6alkanediyl; Alk2 is C1-4alkanediyl; Ar1 and Ar2 are optionally substituted phenyl; phenyl; Het1 and Het2 are optionally substituted heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中R 1是氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，单或二（C 1-6烷基 ）氨基，Ar1，Ar1-NH-，C3-6环烷基，羟甲基或苄氧基甲基; R2和R3是氢，或者可以一起形成式-CH = CH-CH = CH-的二价基团; R4，R5和R6各自独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，三氟甲基，硝基，氨基，氰基，叠氮基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基，C 1-6烷氧基羰基或Het 1; 或当R 4和R 5彼此相邻时，它们可以一起形成式-CH = CH-CH = CH-的基团; A是式NR7，NR7-Alk1-X，NR7-Alk1-X-Alk2-，O-Alk1-X，O-Alk1-X-Alk2-或S-Alk1-X-2的二价基; 其中X是直接键，-O - ， - S - ，C = O，-NR 8 - 或Het 2; R 7为氢，C 1-6烷基或Ar 2甲基; R8是氢，C1-6烷基或Ar2甲基; Alk1是C1-6烷二基; Alk2是C1-4烷二基; Ar1和Ar2是任选取代的苯基; 苯基; Het1和Het2是任选取代的杂环; 具有血管生成抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。