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1. 发明授权

US06803364B1 Il-5 inhibiting 6-azauracil derivatives 失效
标题翻译： 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. 发明申请

US20100173913A1 PYRIDO-AND PYRIMIDOPYRIMIDINE DERIVATIVES AS ANTI-PROLIFERATIVE AGENTS 有权
标题翻译：作为抗增生剂的吡咯并吡啶并吡啶衍生物
公开(公告)号：US20100173913A1
公开(公告)日：2010-07-08
申请号：US12724203
申请日：2010-03-15
申请人： Eddy Jean Edgard Freyne , Marc Willems , Pierre Henri Storck , Virginie Sophie Poncelet , Kristof Van Emelen , Peter Jacobus Johannes Antonius Buijnsters , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
发明人： Eddy Jean Edgard Freyne , Marc Willems , Pierre Henri Storck , Virginie Sophie Poncelet , Kristof Van Emelen , Peter Jacobus Johannes Antonius Buijnsters , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
IPC分类号： A61K31/529 , C07D498/18 , A61P35/00 , C07D487/18
CPC分类号： C07D498/16 , C07D471/04 , C07D487/04 , C07D487/16 , C07D487/22
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein a1-a2=a3-a4 represents a divalent radical selected from N—CH═CH—CH, N—CH═N—CH or CH—CH═N—CH; Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O— or —NR11—; X2 represents —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R4 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R11 represents hydrogen; R12 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R13 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.
摘要翻译：本发明涉及N-氧化物形式的化合物，其药学上可接受的加成盐和立体化学异构体，其中a1-a2 = a3-a4表示选自N-CH = CH-CH，N- CH = N-CH或CH-CH = N-CH; Z表示NH; Y表示-C3-9烷基 - ，-C1-5烷基-NR13-C1-5烷基 - ，C1-6烷基-NH-CO-或-CO-NH-C1-6烷基 - ; X1表示-O-或-NR11-; X2表示-C1-2烷基 - ， - O-C1-2烷基，-O-或-O-CH2-; R1表示氢或卤素; R 2表示氢，氰基，卤素，羟基羰基 - ，C 1-4烷氧基羰基 - ，Het 16 - 羰基 - 或Ar 5; R3表示氢; R 4表示羟基，C 1-4烷氧基 - ，Ar 4 -C 1-4烷氧基或R 4表示被一个或多个可能的两个或多个选自C 1-4烷氧基或Het 2-的取代基取代的C 1-4烷氧基; R11表示氢; R 12表示氢，C 1-4烷基 - 或C 1-4烷基 - 氧基 - 羰基 - ; R13表示Het14-C1-4烷基，特别是吗啉基-C 1-4烷基; Het2表示选自任选被C 1-4烷基，优选甲基取代的吗啉基或哌啶基的杂环; Het14代表吗啉基; Het16表示选自吗啉基或吡咯烷基的杂环; Ar4表示苯基; Ar 5表示任选被氰基取代的苯基。

5. 发明申请

US20100105668A1 Quinazoline derivatives 有权
标题翻译：喹唑啉衍生物
公开(公告)号：US20100105668A1
公开(公告)日：2010-04-29
申请号：US12624637
申请日：2009-11-24
申请人： Eddy Jean Edgard Freyne , Timothy Pietro Suren Perera , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Gaston Stanislas Marcella Diels , Werner Constant Johan Embrechts , Peter ten Holte , Frederik Jan Rita Rombouts , Carsten Schultz-Fademrecht
发明人： Eddy Jean Edgard Freyne , Timothy Pietro Suren Perera , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Gaston Stanislas Marcella Diels , Werner Constant Johan Embrechts , Peter ten Holte , Frederik Jan Rita Rombouts , Carsten Schultz-Fademrecht
IPC分类号： A61K31/541 , C07D239/70 , A61K31/517 , C07D413/02 , A61K31/5377 , C07D417/02 , C07C211/00 , C07D239/72
CPC分类号： C07D498/06 , C07C229/16 , C07C229/40 , C07D239/88 , C07D239/93 , C07D239/94
摘要： The present invention concerns the compounds of formula wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl-, —O—N═CH— or —C1-2alkyl-; R1 and R2 are hydrogen or halo; R3 are hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 are hydrogen or C1-4alkyl; R14 and R15 are hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 are hydrogen or C1-4alkyl optionally substituted with phenyl or hydroxy; R20 and R21 are hydrogen or C1-4alkyl optionally substituted with C1-4alkyloxy; Het20, Het21 and Het22 are a heterocycle selected from the group consisting pyrrolidinyl, 2-pyrrolidinonyl or piperidinyl optionally substituted with hydroxy.
摘要翻译：本发明涉及下式的化合物其中Z代表NH; Y代表任选被氨基，一或二（C 1-4烷基）氨基或C 1-4烷氧基羰基氨基 - ， - C 3-7烯基-CO-的氨基取代的-C 3-9烷基 - ， - C 2-9烯基 - ， - 氨基，一或二（C 1-4烷基）氨基 - 或C 1-4烷氧基羰基氨基 - ，C 1-5烷基-NR 13 -C 1-5烷基 - ， - C 1-5烷基-NR 14 -CO-C 1-5烷基 - C 1-6烷基-CO-NH - ， - C 1-5烷基-CO NR 15 -C 1-5烷基 - ， - C 1-3烷基-NH-CO-Het 20 - ， - C 1-2烷基-CO-Het 21 -CO-， - C 1-2烷基 -NH-CO-CR16R17-NH-，-C1-2烷基-CO-NH-CR18R19-CO-，-C1-2烷基-CO-NR20-C1-3烷基-CO-或-NR22-CO-C1-3烷基 - NH-; X1表示直接键，O或-O-C 1-2烷基 - ; -X 2表示直接键，-CO-C 1-2烷基 - ，NR 12，-NR 12 -C 1-2烷基 - ， - O-N = CH-或-C 1-2烷基 - ; R1和R2是氢或卤素; R3是氢; R4代表氢或C1-4烷氧基; R 12和R 13是氢或C 1-4烷基; R14和R15是氢; R 16和R 17各自独立地表示氢或C 1-4烷基; R 18和R 19是氢或任选被苯基或羟基取代的C 1-4烷基; R 20和R 21是氢或任选被C 1-4烷氧基取代的C 1-4烷基; Het20，Het21和Het22是选自吡咯烷基，2-吡咯烷基或任选被羟基取代的哌啶基的杂环。

6. 发明申请

US20080139601A1 3-Cyano-Quinoline Derivatives With Antiproliferative Activity 有权
公开(公告)号：US20080139601A1
公开(公告)日：2008-06-12
申请号：US10596509
申请日：2004-12-15
申请人： Eddy Jean Edgard Freyne , Peter Jacobus Johannes Antonius Buijnsters , Kristof Van Emelen , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
发明人： Eddy Jean Edgard Freyne , Peter Jacobus Johannes Antonius Buijnsters , Kristof Van Emelen , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
IPC分类号： A61K31/4745 , C07D487/02 , A61P35/00
CPC分类号： C07D215/54 , A61K31/4748 , C07D498/06
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR12—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O—; X2 represents a direct bond, —NR11—C1-2alkyl-, —NR11—CH2—, —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen, hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.

7. 发明申请

US20120035171A1 BICYCLIC HETEROCYCLYL DERIVATIVES AS FGFR KINASE INHIBITORS FOR THERAPEUTIC USE 有权
标题翻译：作为用于治疗用途的FGFR激酶抑制剂的双相间苯二酚衍生物
公开(公告)号：US20120035171A1
公开(公告)日：2012-02-09
申请号：US13264593
申请日：2010-04-15
申请人： Gordon Saxty , Valerio Berdini , Eddy Jean Edgard Freyne , Alexandra Papanikos , Pascal Benderitter , Werner Constant Johan Embrechts , Berthold Wroblowski , Rhalid Akkari
发明人： Gordon Saxty , Valerio Berdini , Eddy Jean Edgard Freyne , Alexandra Papanikos , Pascal Benderitter , Werner Constant Johan Embrechts , Berthold Wroblowski , Rhalid Akkari
IPC分类号： A61K31/5377 , A61P35/00 , A61K31/496 , A61K31/513 , C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
摘要翻译：本发明涉及式（I）的新的双环杂环基衍生物，包含所述化合物的药物组合物和所述化合物在治疗疾病中的用途，例如，癌症。

8. 发明授权

US08772272B2 Pyrido-and pyrimidopyrimidine derivatives as anti-proliferative agents 有权
标题翻译：吡啶并嘧啶并嘧啶衍生物作为抗增殖剂
公开(公告)号：US08772272B2
公开(公告)日：2014-07-08
申请号：US12724203
申请日：2010-03-15
申请人： Eddy Jean Edgard Freyne , Marc Willems , Pierre Henri Storck , Virginie Sophie Poncelet , Kristof Van Emelen , Peter Jacobus Johnnes Antonius Buijnsters , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
发明人： Eddy Jean Edgard Freyne , Marc Willems , Pierre Henri Storck , Virginie Sophie Poncelet , Kristof Van Emelen , Peter Jacobus Johnnes Antonius Buijnsters , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
IPC分类号： A61K31/33 , A61K31/519 , C07D487/00 , C07D487/18
CPC分类号： C07D498/16 , C07D471/04 , C07D487/04 , C07D487/16 , C07D487/22
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein a1-a2=a3-a4 represents a divalent radical selected from N—CH═CH—CH, N—CH═N—CH or CH—CH═N—CH; Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O— or —NR11—; X2 represents —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R4 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R11 represents hydrogen; R12 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R13 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.
摘要翻译：本发明涉及N-氧化物形式的化合物，其药学上可接受的加成盐和立体化学异构体，其中a1-a2 = a3-a4表示选自N-CH = CH-CH，N- CH = N-CH或CH-CH = N-CH; Z表示NH; Y表示-C3-9烷基 - ，-C1-5烷基-NR13-C1-5烷基 - ，C1-6烷基-NH-CO-或-CO-NH-C1-6烷基 - ; X1表示-O-或-NR11-; X2表示-C1-2烷基 - ， - O-C1-2烷基，-O-或-O-CH2-; R1表示氢或卤素; R 2表示氢，氰基，卤素，羟基羰基 - ，C 1-4烷氧基羰基 - ，Het 16 - 羰基 - 或Ar 5; R3表示氢; R 4表示羟基，C 1-4烷氧基 - ，Ar 4 -C 1-4烷氧基或R 4表示被一个或多个可能的两个或多个选自C 1-4烷氧基或Het 2-的取代基取代的C 1-4烷氧基; R11表示氢; R 12表示氢，C 1-4烷基 - 或C 1-4烷基 - 氧基 - 羰基 - ; R13表示Het14-C1-4烷基，特别是吗啉基-C 1-4烷基; Het2表示选自任选被C 1-4烷基，优选甲基取代的吗啉基或哌啶基的杂环; Het14代表吗啉基; Het16表示选自吗啉基或吡咯烷基的杂环; Ar4表示苯基; Ar 5表示任选被氰基取代的苯基。

9. 发明授权

US08148388B2 2,4 (4,6) pyrimidine derivatives 有权
标题翻译： 2,4（4,6）嘧啶衍生物
公开(公告)号：US08148388B2
公开(公告)日：2012-04-03
申请号：US11720681
申请日：2005-12-08
申请人： Eddy Jean Edgard Freyne , Marc Willems , Werner Constant Johan Embrechts , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Frederik Jan Rita Rombouts
发明人： Eddy Jean Edgard Freyne , Marc Willems , Werner Constant Johan Embrechts , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Frederik Jan Rita Rombouts
IPC分类号： A01N43/54 , A61K31/505 , C07D471/00 , C07D487/00 , C07D491/00 , C07D239/02
CPC分类号： C07D487/18 , C07D487/08 , C07D487/22 , C07D498/08 , C07D498/18
摘要： The present invention is drawn to 2,4 (4,6) pyrimidine derived macrocyclcs, pharmaceutical compositions thereof, and methods of making said compounds. The compounds disclosed herein are inhibitors of EGF receptor tyrosine kinases and are useful for treating cell proliferative disorders, including atherosclerosis, restenosis, and cancer.
摘要翻译：本发明涉及2,4（4,6）个嘧啶衍生的大环内酯，其药物组合物，以及制备所述化合物的方法。本文公开的化合物是EGF受体酪氨酸激酶的抑制剂，并且可用于治疗细胞增殖性疾病，包括动脉粥样硬化，再狭窄和癌症。

10. 发明申请

US20100152174A1 MACROCYCLIC QUINAZOLE DERIVATIVES AND THEIR USE AS MTKI 审中-公开
标题翻译：大分子喹唑啉衍生物及其作为MTKI的用途
公开(公告)号：US20100152174A1
公开(公告)日：2010-06-17
申请号：US11720693
申请日：2005-12-08
申请人： Eddy Jean Edgard Freyne , Marc Willems , Peter Ten Holte , Alexandra Papanikos , Werner Constant John Embrechts , Pierre Henri Storck , Virginie Sophie Poncelet , Werner Constant Johan Embrechts , Pierre Henri Storck , Virginie Sophie Poncelet
发明人： Eddy Jean Edgard Freyne , Marc Willems , Peter Ten Holte , Alexandra Papanikos , Werner Constant John Embrechts , Pierre Henri Storck , Virginie Sophie Poncelet , Werner Constant Johan Embrechts , Pierre Henri Storck , Virginie Sophie Poncelet
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/517 , C07D498/04 , A61P35/00
CPC分类号： C07D498/06 , C07D498/08
摘要： The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-2alkyl-NR21—H2—CO—NH—C1-3alkyl- or —C1-2alkyl-NR23—CO—CR16R17—NH—; X1 represents O or —O—C1-2alkyl-; X2 represents a direct bond, C1-2alkyl, —CO—C1-2alkyl or NR12—C1-2alkyl; R1 represents hydrogen or halo; R2 represents halo, acetylene or Het1; R3 represents hydrogen or cyano; R4 represents Ar4—C1-4alkyloxy-, C1-4alkyloxy- or C1-4alkyloxy substituted with one or where possible two or more substituents selected from Het2, NR7R8, hydroxy and C1-4alkyloxy-C1-4alkyloxy-; R7 represents hydrogen or C1-4alkyl; R8 represents C1-4alkyl substituted with NR25R26 or C1-4alkylsulfonyl; R12 represents hydrogen or C1-4alkyl-; R13 represents Ar6-sulfonyl or C1-6alkyloxycarbonyl optionally substituted with phenyl; R16 and R17 represents hydrogen, C1-4alkyl or R16 and R17 taken together with the carbon atom to which they are attached from a C3-6cycloalkyl; R23 represents C1-4alkyl and R23 represents hydrogen when R16 and R17 taken together with the carbon atom to which they are attached from a C3-6cycloalkyl; R25, R26, R27 and R28 each independently represent hydrogen or C1-4alkylcarbonyl; Het1 represents 2-bora-1,3-dioxolanyl; Het represents piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl or 1,1-dioxothiomorpholinyl wherein said Het2 is optionally substituted with C1-4alkyloxycarbonyl or NR27R28—C1-4alkyl; Ar4 and Ar5 represents phenyl; Ar6 represents phenyl optionally substituted with nitro.
摘要翻译：本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中Z表示NH; Y表示-C3-9烷基，-C1-5烷基-NR13-C1-5烷基，-C1-5烷基-NR14-CO-C1-5烷基，-C1-2烷基-NR21-H2-CO-NH-C1-3烷基 - 或-C1-2烷基-NR23-CO-CR16R17-NH-; X 1表示O或-O-C 1-2烷基 - ; X2表示直接键，C1-2烷基，-CO-C1-2烷基或NR12-C1-2烷基; R1表示氢或卤素; R2代表卤代，乙炔或Het1; R3表示氢或氰基; R 4表示被一个或多个可能的两个或多个选自Het 2，NR 7 R 8，羟基和C 1-4烷氧基-C 1-4烷氧基 - 的取代基取代的Ar 4 -C 1-4烷氧基 - ，C 1-4烷氧基 - 或C 1-4烷氧基。 R7代表氢或C1-4烷基; R8表示被NR25R26或C1-4烷基磺酰基取代的C1-4烷基; R 12表示氢或C 1-4烷基 - ; R 13表示Ar 6 - 磺酰基或任选被苯基取代的C 1-6烷氧基羰基; R 16和R 17表示氢，C 1-4烷基或R 16和R 17与它们与C 3-6环烷基连接的碳原子一起; 当R 16和R 17与C 3-6环烷基连接的碳原子一起时，R 23表示C 1-4烷基，R 23表示氢; R 25，R 26，R 27和R 28各自独立地表示氢或C 1-4烷基羰基; Het1代表2-硼-1,3-二氧戊环基; Het表示哌啶基，哌嗪基，吗啉基，硫代吗啉基或1,1-二氧代硫代吗啉基，其中所述Het2任选被C 1-4烷氧基羰基或NR 27 R 28 -C 1-4烷基取代; Ar 4和Ar 5表示苯基; Ar 6表示任选被硝基取代的苯基。

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