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1. 发明申请

WO2008049901A1 USE OF A MT KINASE INHIBITOR FOR TREATING OR PREVENTING BRAIN CANCER 审中-公开
标题翻译：使用MT激酶抑制剂治疗或预防脑癌
公开(公告)号：WO2008049901A1
公开(公告)日：2008-05-02
申请号：PCT/EP2007/061498
申请日：2007-10-25
申请人： JANSSEN PHARMACEUTICA NV , PERERA, Timothy Pietro Suren , PAGE, Martin John , JANICOT, Michel Marie François , FREYNE, Eddy Jean Edgard
发明人： PERERA, Timothy Pietro Suren , PAGE, Martin John , JANICOT, Michel Marie François , FREYNE, Eddy Jean Edgard
IPC分类号： A61K31/519 , A61P35/00
CPC分类号： A61K31/519
摘要： The present invention is concerned with the finding that some the macrocyclic quinazoline derivative 4,6-ethanediylidenepyrimido[4,5- b ][6,1,12]benzoxadiazacyclo-pentadecine, 17-bromo-8,9,10,11,12,13,14,19-octahydro-20-methoxy-13-methyl-, described as compound 22 in PCT publication WO2004/105765, is useful in the manufacture of a medicament for the treatment or prevention of a primary brain cancer or brain metastasis. It accordingly provides methods for treating, preventing, delaying or mitigating brain cancer, or for preventing or slowing proliferation of cells of brain origin.
摘要翻译：本发明涉及一些大环喹唑啉衍生物4,6-乙二亚甲基嘧啶并[4,5-b] [6,1,12]苯并二氮杂环十五碳烯，17-溴-8,9,10,11,12 在PCT公开WO2004 / 105765中描述为化合物22的13,14,19-八氢-20-甲氧基-13-甲基，可用于制备用于治疗或预防原发性脑癌或脑转移的药物。因此，它提供了治疗，预防，延迟或减轻脑癌或预防或减缓脑源性细胞增殖的方法。

3. 发明申请

WO2009016132A1 PYRROLOPYRIMIDINES 审中-公开
标题翻译：的吡咯
公开(公告)号：WO2009016132A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/059833
申请日：2008-07-25
申请人： JANSSEN PHARMACEUTICA NV , DIELS, Gaston Stanislas Marcella , TEN HOLTE, Peter , FREYNE, Eddy Jean Edgard , GRAND-PERRET, Thierry Andre Regis , VAN EMELEN, Kristof , EMBRECHTS, Werner Constant Johan , BONNET, Pascal Ghislain André
发明人： DIELS, Gaston Stanislas Marcella , TEN HOLTE, Peter , FREYNE, Eddy Jean Edgard , GRAND-PERRET, Thierry Andre Regis , VAN EMELEN, Kristof , EMBRECHTS, Werner Constant Johan , BONNET, Pascal Ghislain André
IPC分类号： C07D487/08 , C07D498/08 , A61K31/529 , A61P35/02
CPC分类号： C07D498/08 , C07D487/08
摘要： The present invention relates to compounds or pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to compounds that are polo-like kinase (PLKs) inhibitors useful for the treatment of disease states mediated by PLK, especially PLK4, in particular such compounds that are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumour growth, rheumatoid arthritis, restenosis and atherosclerosis.
摘要翻译：本发明涉及其化合物或药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途。本发明特别涉及可用于治疗由PLK，特别是PLK4介导的疾病状态的polo样激酶（PLK）抑制剂的化合物，特别是可用于治疗涉及异常细胞增殖的病理过程的此类化合物，如肿瘤生长，类风湿关节炎，再狭窄和动脉粥样硬化。

4. 发明申请

WO2009118384A1 QUINAZOLINONE DERIVATIVES AS TUBULIN POLYMERIZATION INHIBITORS 审中-公开
标题翻译：喹唑啉酮衍生物作为管状聚氨酯抑制剂
公开(公告)号：WO2009118384A1
公开(公告)日：2009-10-01
申请号：PCT/EP2009/053604
申请日：2009-03-26
申请人： JANSSEN PHARMACEUTICA NV , FREYNE, Eddy Jean Edgard , MEVELLEC, Laurence Anne , VIALARD, Jorge Eduardo , MEYER, Christophe , PASQUIER, Elisabeth Thérèse Jeanne , BOURDREZ, Xavier Marc , ANGIBAUD, Patrick René
发明人： FREYNE, Eddy Jean Edgard , MEVELLEC, Laurence Anne , VIALARD, Jorge Eduardo , MEYER, Christophe , PASQUIER, Elisabeth Thérèse Jeanne , BOURDREZ, Xavier Marc , ANGIBAUD, Patrick René
IPC分类号： C07D239/80 , C07D401/06 , C07D417/06 , A61K31/517 , A61P35/00
CPC分类号： C07D239/80 , C07D401/06 , C07D417/06
摘要： The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , n, m and X have defined meanings.
摘要翻译：本发明提供式（I）化合物，其作为微管蛋白聚合抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中R1，R2，R3，R4，R5，R6，n，m和X具有定义含义。

5. 发明申请

WO2008107478A1 QUINOLINONE DERIVATIVES AS PARP AND TANK INHIBITORS 审中-公开
标题翻译：喹诺酮衍生物作为PARP和坦克抑制剂
公开(公告)号：WO2008107478A1
公开(公告)日：2008-09-12
申请号：PCT/EP2008/052764
申请日：2008-03-07
申请人： JANSSEN PHARMACEUTICA NV , VIALARD, Jorge Eduardo , ANGIBAUD, Patrick René , MEVELLEC, Laurence Anne , MEYER, Christophe , FREYNE, Eddy Jean Edgard , PILATTE, Isabelle Noëlle Constance , ROUX, Bruno , PASQUIER, Elisabeth Thérèse Jeanne , BOURDREZ, Xavier Marc , ADELINET, Christophe Denis , MARCONNET-DECRANE, Laurence Françoise Bernadette , MACRITCHIE, Jacqueline Anne , DUFFY, James Edward Stewart , OWENS, Andrew Pate , STORCK, Pierre-Henri , PONCELET, Virginie Sophie
发明人： VIALARD, Jorge Eduardo , ANGIBAUD, Patrick René , MEVELLEC, Laurence Anne , MEYER, Christophe , FREYNE, Eddy Jean Edgard , PILATTE, Isabelle Noëlle Constance , ROUX, Bruno , PASQUIER, Elisabeth Thérèse Jeanne , BOURDREZ, Xavier Marc , ADELINET, Christophe Denis , MARCONNET-DECRANE, Laurence Françoise Bernadette , MACRITCHIE, Jacqueline Anne , DUFFY, James Edward Stewart , OWENS, Andrew Pate , STORCK, Pierre-Henri , PONCELET, Virginie Sophie
IPC分类号： C07D215/22 , A61K31/4704
CPC分类号： C07D215/227 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： The present invention provides compounds of Formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , n, m and X have defined meanings.
摘要翻译：本发明提供式（I）化合物，它们作为PARP抑制剂的用途以及包含所述化合物的药物组合物，其中R 1，R 2， R 3，R 4，R 5，R 6，R 7，R 7，R 7， / sup>，n，m和X定义了含义。

6. 发明申请

WO2005012307A1 TRIAZOLOPYRIMIDINE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS 审中-公开
标题翻译：三氮唑嘧啶衍生物作为GLYCOGEN SYNTHASE激酶3抑制剂
公开(公告)号：WO2005012307A1
公开(公告)日：2005-02-10
申请号：PCT/EP2004/051455
申请日：2004-07-12
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy Jean Edgard , LOVE, Christopher John , COOYMANS, Ludwig Paul , VANDERMAESEN, Nele , BUIJNSTERS, Peter Jacobus Johannes Antonius , WILLEMS, Marc , EMBRECHTS, Werner Constant Johan
发明人： FREYNE, Eddy Jean Edgard , LOVE, Christopher John , COOYMANS, Ludwig Paul , VANDERMAESEN, Nele , BUIJNSTERS, Peter Jacobus Johannes Antonius , WILLEMS, Marc , EMBRECHTS, Werner Constant Johan
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： This invention concerns a compound of formula (I), a N -oxide, a pharmaceutically acceptable addition salt, a quaternary arnine and a stereochernic ally isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R 1 represents hydrogen; aryl; formyI; C l . 6 alkylcarbonyl, C 1-6 alkyl; C 1-6 alkyloxycarbonyl; C 1-6 alkyl substituted with formyl, C 1-6 alkylearbonyl, C 1-6 alkyloxycarbonyl, C 1 - 6 alkylcarbonyloxy; or C 1 - 6 alkyloxyC 1-6 alkylcarbonyl optionally substituted with C 1-6 alkyloxycarbonyl; X represents a direct bond; -(CH 2 ) n3 or -(CH 2 ) m4 -X 1a -X 1b -; R 2 represents C 3-7 cycloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one heteroatom. selected from 0, S or N; benzoxazolyl or a radical of formula (a-1), wherein said R 2 substituent may optionally be substituted; R 3 represents halo; hydroxy; optionally substituted C 1-.6 alkyl; C 2-6 a]kenyl or C 2-6 alkynyl, each optionally substituted; optionally substituted polyhaloC 1-6 alkyl; optionally substituted C 1-6 alkyloxy; optionally substituted polyhaloC 1-6 alkyloxy; C 1-6 alkylthio; polyhaloC 1-6 a]kylthio; C 1-6 a]kyloxycarbonyl; C 1-6 alkylcarbonyloxy; C 1-6 alkylearbonyl; polyhaloC 1-6 alkylcarbonyl; cyano; carboxyl; aryloxy; arylthio; arylcarbonyl; NR 6b R 7b ; C(=O)-NR 6b R 7b ; -NR 5 -C(=O)R 5 ;'-S(=O) nl -R 8a ; -NR 5 S(=O) nl -R 8a ;-NR 5 -S(=O) nl -R 8a ; -S-CN; -NR 5 -CN;R 4 represents hydrogen; halo; hydroxy; optionally substituted C 1-4 alkyl; C 2-4 alkenyl or C 2-4 alkynyl, each optionally substituted; polyha]oC 1-3 alkyl; optionally substituted C 1-4 alkyloxy; polyhalo-C 1-3 alkyloxy; C 1-4 alkylthio; polyhaloC 1-3 alkylthio C 1-4 alkyloxycarbonyl; C 1-4 alkylcarbonyloxy; C 1-4 alkylcarbonyl; polyhatoC 1-4 alkylcarbonyl; nitro; cyano; carboxyl; NR 10 R 11 ; C(=O)NR 10 -R 11 ;NR 5 -C(=O)-NR 10 R 11 ;-NR 5 -C(=O)-R 5 ; -S(=O) nl ,-R 12 -NR 5 -S(=O) nI -R 12 ; -S-CN; -NR 5 -CN; their use, pharmaceutical compositions comprising them and processes for their preparation.
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，季铵和其立体异构体异构体形式，其中环A表示苯基，吡啶基，嘧啶基，哒嗪基或吡嗪基; R 1表示氢; 芳基; 甲酰基; C 1-6烷基羰基，C 1-6烷基; C1-6alkyloxycarbonyl; 被甲酰基，C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6烷基羰氧基取代的C 1-6烷基; 或任选被C 1-6烷氧基羰基取代的C 1-6烷氧基C 1-6烷基羰基; X表示直接键; - （CH2）n3or - （CH2）m4-X1a-X1b-; R 2表示C 3-7环烷基; 苯基; 含有至少一个杂原子的4,5,6-或7-元单环杂环。选自0，S或N; 苯并恶唑基或式（a-1）的基团，其中所述R 2取代基可任选被取代; R 3表示卤素; 羟基; 任选取代的C 1-6烷基; C 2-6烯基或C 2-6炔基，各自任选取代; 任选取代的多卤代C 1-6烷基; 任选取代的C 1-6烷氧基; 任选取代的多卤代C 1-6烷氧基; C 1-6烷; polyhaloC1-6a]烷硫基; C1-6a] kyloxycarbonyl; C1-6alkylcarbonyloxy; C1-6alkylearbonyl; polyhaloC1-6alkylcarbonyl; 氰基; 羧基; 芳; 芳; 基羰基; NR 6b; R 7b; C（= O）-NR 6b R 7b; -NR <5> -C（= O）R <5>;' - S（= O）NL-R <8A>; -NR 5 S（= O）n -R 8 8a; -NR 5 -S（= O）n -R 8 8a; -S-CN; -NR 5 -CN; R 4表示氢; 光环; 羟基; 任选取代的C 1-4烷基; C2-4烯基或C2-4炔基，各自任选取代; polyha] OC 1-3烷基; 任选取代的C 1-4烷氧基; 多卤代C1-3alkyloxy; C1-4alkylthio; 多卤代C 1-3烷硫基C 1-4烷氧基羰基; C1-4alkylcarbonyloxy; C1-4alkylcarbonyl; polyhatoC1-4alkylcarbonyl; 硝基; 氰基; 羧基; NR 10 R 11; C（= O）NR 10 -R 11; NR 5 -C（= O）-NR 10 R 11; -NR 5 -C（= O）-R 5 >; -S（= O）n1，-R 12 -NR 5 -S（= O）n I -R 12; -S-CN; -NR 5 -CN; 其用途，包含它们的药物组合物及其制备方法。

7. 发明申请

WO2010119284A1 BICYCLIC HETEROCYCLYL DERIVATIVES AS FGFR KINASE INHIBITORS FOR THERAPEUTIC USE 审中-公开
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：WO2010119284A1
公开(公告)日：2010-10-21
申请号：PCT/GB2010/050617
申请日：2010-04-15
申请人： ASTEX THERAPEUTICS LIMITED , SAXTY, Gordon , BERDINI, Valerio , FREYNE, Eddy Jean Edgard , PAPANIKOS, Alexandra , BENDERITTER, Pascal , EMBRECHTS, Werner Constant Johan , WROBLOWSKI, Berthold , AKKARI, Rhalid
发明人： SAXTY, Gordon , BERDINI, Valerio , FREYNE, Eddy Jean Edgard , PAPANIKOS, Alexandra , BENDERITTER, Pascal , EMBRECHTS, Werner Constant Johan , WROBLOWSKI, Berthold , AKKARI, Rhalid
IPC分类号： C07D471/04 , A61P35/00 , 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. 发明申请

WO2010119285A1 IMIDAZO [1,2-A]PYRIDINE DERIVATIVES AS FGFR KINASE INHIBITORS FOR USE IN THERAPY 审中-公开
标题翻译：作为用于治疗的FGFR激酶抑制剂的咪唑并[1,2-A]吡啶衍生物
公开(公告)号：WO2010119285A1
公开(公告)日：2010-10-21
申请号：PCT/GB2010/050618
申请日：2010-04-15
申请人： ASTEX THERAPEUTICS LIMITED , SAXTY, Gordon , BERDINI, Valerio , MURRAY, Christopher William , FREYNE, Eddy Jean Edgard , LIGNY, Yannick Aimé Eddy , BONNET, Pascal Ghislain André , WROBLOWSKI, Berthold , PAPANIKOS, Alexandra
发明人： SAXTY, Gordon , BERDINI, Valerio , MURRAY, Christopher William , FREYNE, Eddy Jean Edgard , LIGNY, Yannick Aimé Eddy , BONNET, Pascal Ghislain André , WROBLOWSKI, Berthold , PAPANIKOS, Alexandra
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
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。

9. 发明申请

WO2006061417A2 MTKI QUINAZOLINE DERIVATIVES 审中-公开
标题翻译： MTKI喹诺酮衍生物
公开(公告)号：WO2006061417A2
公开(公告)日：2006-06-15
申请号：PCT/EP2005/056609
申请日：2005-12-08
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy Jean Edgard , WILLEMS, Marc , TEN HOLTE, Peter , PAPANIKOS, Alexandra , EMBRECHTS, Werner Constant Johan , STORCK, Pierre Henri , PONCELET, Virginie Sophie
发明人： FREYNE, Eddy Jean Edgard , WILLEMS, Marc , TEN HOLTE, Peter , PAPANIKOS, Alexandra , EMBRECHTS, Werner Constant Johan , STORCK, Pierre Henri , PONCELET, Virginie Sophie
IPC分类号： C07D498/08 , A61K31/529 , A61P35/00 , C07D273/00 , C07D239/00
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 -C 3-9 alkyl-,-C 1-5 alkyl-NR 13 -C 1-5 alkyl-, -C 1-5 alkyl-NR 14 -CO-C 1-5 alkyl-, -C 1-2 alkyl-NR 21 -H 2 -CO-NH-C 1-3 alkyl- or -C 1-2 alkyl-NR 23 -CO-CR 16 R 17 -NH-; X 1 represents O or -O-C 1-2 alkyl-; X 2 represents a direct bond, C 1-2 alkyl, -CO-C 1-2 alkyl or NR 12 -C 1-2 alkyl; R 1 represents hydrogen or halo; R 2 represents halo, acetylene or Het 1 ; R 3 represents hydrogen or cyano; R 4 represents Ar 4 -C 1-4 alkyloxy-, C 1-4 alkyloxy- or C 1-4 alkyloxy substituted with one or where possible two or more substituents selected from Het 2 , NR 7 R 8 , hydroxy and C 1-4 alkyloxy-C 1-4 alkyloxy-; R 7 represents hydrogen or C 1-4 alkyl; R 8 represents C 1-4 alkyl substituted with NR 25 R 26 or C 1-4 alkylsulfonyl ; R 12 represents hydrogen or C 1-4 alkyl-; R 13 represents Ar 6 -sulfonyl or C 1-6 alkyloxycarbonyl optionally substituted with phenyl; R 16 and R 17 represents hydrogen, C 1-4 alkyl or R 16 and R 17 taken together with the carbon atom to which they are attached from a C 3-6 cycloalkyl; R 23 represents C 1-4 alkyl and R 23 represents hydrogen when R 16 and R 17 taken together with the carbon atom to which they are attached from a C 3-6 cycloalkyl; R 25 , R 26 , R 27 and R 28 each independently represent hydrogen or C 1-4 alkylcarbonyl; Het 1 represents 2-bora-l,3-dioxolanyl; Het 2 represents piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl or 1,1-dioxothiomorpholinyl wherein said Het 2 is optionally substituted with C 1-4 alkyloxycarbonyl or NR 27 R 28 -C 1-4 alkyl; Ar 4 and Ar 5 represents phenyl; Ar 6 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-C 3-9 - 烷基 - ， - 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 1-2个碳原子的烷基-NR 21 -CO-NH-C 1-3烷基 - 或-C- SUB> 1-2 烷基 - NR ^{23 -CO-CR ^{16 - [R ^{17 -NH-; X 1表示O或-O-C 1-12烷基 - ; X 2表示直接键，C 1-12烷基，-CO-C 1-2烷基或NR 12， SUP> -C _{1-2 烷基; R 1表示氢或卤素; R 2表示卤素，乙炔或Het 1; R 3表示氢或氰基; R 4表示Ar 4 -C 1-4烷氧基 - ，C 1-4烷氧基或C 1 -C 4烷氧基 - 被一个或多个可能的两个或更多个选自Het 2，R 7，R 8，R 8和R 8的取代基取代的C 1-4烷氧基，，羟基和C 1-4烷氧基-C 1-4烷氧基 - ; R 7表示氢或C 1-4烷基; R 8表示被NR 25 R 26取代的C 1-4烷基或C 1-4烷基烷基磺酰基; R 12表示氢或C 1-4烷基 - ; R 13表示任选被苯基取代的Ar 6 - 磺酰基或C 1-6烷氧基羰基; R 16和R 17代表氢，C 1-4烷基或R 16和R 17 与其连接的碳原子一起与C 3-6环烷基一起取代; R 25表示C 1-4烷基，R 23表示氢，当R 16和R 17 与其连接的碳原子一起与C 3-6环烷基一起取代; 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; Het 代表2-硼-1,3-二氧戊环基; Het 2是哌啶基，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Het 2任选被C 1-4烷氧基羰基或NR 27 R 28，-C 1-4烷基; Ar 4和Ar 5代表苯基; Ar 6表示任选被硝基取代的苯基。}}}}

10. 发明授权

EP1633365B1 MACROCYCLIC QUINAZOLINE DERIVATIVES AS ANTIPROLIFERATIVE AGENTS 有权
标题翻译：大环喹唑啉衍生物ALS抗增殖剂
公开(公告)号：EP1633365B1
公开(公告)日：2012-02-08
申请号：EP04739341.8
申请日：2004-05-25
申请人： Janssen Pharmaceutica NV
发明人： FREYNE, Eddy Jean Edgard , PERERA, Timothy Pietro Suren , BUIJNSTERS, Peter Jacobus Johannes Antonius , WILLEMS, Marc , DIELS, Gaston Stanislas Marcella , EMBRECHTS, Werner Constant Johan , TEN HOLTE, Peter , ROMBOUTS, Frederk, Jan, Rita , SCHULZ-FADEMRECHT, Carsten
IPC分类号： A61K31/529 , C07D498/08 , A61P35/00 , C07D239/88 , C07D239/93 , C07D239/94
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 (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents O, CH2, NH or S; in particular Z represents NH; Y represents -C3-9alkyl-, -C3-9alkenyl-, -C3-9alkynyl-, -C3-7alkyl-CO-NH- optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4 alkyloxycarbonylamino-, -C3-7alkenyl-CO-NH- optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-oxy-C1-5alkyl-, -C1-5alkyl NR13-, -C1-5alkyl-, -C1-5alkyl-NR14-CO-C1-5alkyl-, -C1-5alkyl-CO NR15-C1-5alkyl-, -C1-6alkyl-CO-NH-, -C1-6alkyl-NH-CO-, -C1-3alkyl-NH-CS-Het20-, -C1-3alkyl-NH-CO-Het20-, -C1-2alkyl-CO-Het21-CO-, -Het22-CH2-CO-NH-C1-3alkyl-, -CO-NH-C1-6alkyl-, -NH-CO-C1-6alkyl-, -CO-C1-7alkyl-, -C1-7alkyl-CO-, -C1-6alkyl-CO-C1-6alkyl-, -C1-2alkyl-NH-CO-CR16R17-NH-, -C1-2alkyl-CO-NH-CR18R19-CO-, -C1-2alkyl-CO-NR20-C1-3alkyl-CO-, C1-2alkyl-NR21-CH2-CO-NH-C1-3alkyl-, or -NR22-CO-C1-3alkyl-NH-; X1 represents a direct bond, O or -O-C1-2alkyl-, CO, -CO-C1-2alkyl-, NR11, -NR11-C1-2alkyl-, CH2-, -O-N=CH- or -C1-2alkyl-; X2 represents a direct bond, O, -O-C1-2alkyl-, CO, -CO-C1-2alkyl-, NR12, -NR12-C1-2alkyl-, -CH2-, -O-N=CH- or -C1-2alkyl-. The growth inhibitory effect anti-tumour activity of the present compounds has been demonstrated in vitro, in enzymatic assays on the receptor tyrosine kinase EGFR.

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