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11. 发明申请

WO2006061415A1 2,4 (4,6) PYRIMIDINE DERIVATIVES 审中-公开
标题翻译： 2,4（4,6）吡嗪衍生物
公开(公告)号：WO2006061415A1
公开(公告)日：2006-06-15
申请号：PCT/EP2005/056606
申请日：2005-12-08
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , WILLEMS, Marc , EMBRECHTS, Werner, Constant , Johan , VAN EMELEN, Kristof , VAN BRANDT, Sven, Franciscus, Anna , ROMBOUTS, Frederik, Jan, Rita
发明人： FREYNE, Eddy, Jean, Edgard , WILLEMS, Marc , EMBRECHTS, Werner, Constant , Johan , VAN EMELEN, Kristof , VAN BRANDT, Sven, Franciscus, Anna , ROMBOUTS, Frederik, Jan, Rita
IPC分类号： C07D487/08 , C07D487/22 , C07D498/18 , A61K31/505 , A61P35/00 , C07D259/00 , C07D239/00 , C07D241/00 , C07D209/00 , C07D273/00 , C07D221/00
CPC分类号： C07D487/18 , C07D487/08 , C07D487/22 , C07D498/08 , C07D498/18
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 1 and Z 2 represent NH; Y represents -C 3-9 alkyl-, -C 3-9 alkenyl-, -C 1-5 alkyl-NR 6 -C 1-5 alkyl-, -C 1-5 alkyl-NR 7 -CO-C 1 -5 alkyl-, -C 1-6 alkyl-CO-NH-, -C 1-6 alkyl-NH-CO-, -C 1-2 alkyl-CO-Het 10 -CO-, -C 1-3 alkyl-NH-CO-Het 3 -, -Het 4 -C 1-3 alkyl-CO-NH-C 1-3 alkyl-, -C 1-2 alkyl-NH-CO-L 1 -NH-, -NH-CO-L 2 -NH-, -C 1-2 alkyl-CO-NH-L 3 -CO-, -C 1-2 alkyl-NH-CO-L 1 -NH-CO-C 1-3 alkyl-, -C 1-2 alkyl-CO-NH-L 3 -CO-NH-C 1-3 alkyl-, -C 1-2 alkyl-NR 11 -CH 2 -CO-NH-C 1-3 alkyl-, Het 5 -CO-C 1-2 alkyl-, -C 1-5 alkyl-CO-NH-C 1-3 alkyl-CO-NH-, -C 1-5 alkyl-NR 13 -CO-C 1-3 alkyl-NH-, -C 1-3 alkyl-NH-CO-Het 27 -CO-, or -C 1-3 alkyl-CO-Het 28 -CO-NH-; X 1 represents a direct bond, O, -O-C 1-2 alkyl-, -CO-C 1-2 alkyl-, -NR 16 -C 1-2 alkyl-, -CO-NR 17 -, Het 23 -C 1-2 alkyl- or C 1-2 alkyl; X 2 represents a direct bond, O, -O-C 1-2 alkyl-, -CO-C 1-2 alkyl-, -NR 18 -C 1-2 alkyl-, -CO-NR 19 -, Het 24 -C 1-2 alkyl- or C 1-2 alkyl; R 1 and R 5 each independently represent hydrogen, halo, C 1-6 alkyloxy- or C 1-6 alkyloxy- substituted with Het 1 or C 1-4 alkyloxy-; R 2 and R 4 each independently represent hydrogen or halo; R 3 represents hydrogen or cyano; R 6 , R 7 , R 13 , R 17 and R 19 represent hydrogen; R 11 represents hydrogen or C 1-4 alkyl; R 16 and R 18 represent hydrogen, C 1-4 alkyl or Het 17 -C 1-4 alkyl-; L 1 , L 2 and L 3 each independently represents C 1-8 alkyl optionally substituted with one or where possible two or more substituents selected from phenyl, methylsulfide, cyano, polyhaloC 1-4 alkyl-phenyl-, C 1-4 alkyloxy, pyridinyl, mono- or di(C 1-4 alkyl)-amino- or C 3-6 cycloalkyl; Het 1 , Het 2 , Het 17 each independently represent morpholinyl, oxazolyl, isoxazolyl, or piperazinyl; Het 3 , Het 4 , Het 5 each independently represent morpholinyl, piperazinyl, piperidinyl or pyrrolidinyl; Het 10 represents piperazinyl, piperidinyl, pyrrolidinyl or azetidinyl; Het 22 represents morpholinyl, oxazolyl, isoxazolyl or piperazinyl wherein said Het 22 is optionally substituted with C 1-4 alkyl; Het 23 and Het 24 each independently represent a heterocycle selected from pyrrolidinyl, piperazinyl or piperidinyl wherein said Het 23 or Het 24 are optionally substituted with Het 22 -carbonyl; Het 27 and Het 28 each independently represent a heterocycle selected from morpholinyl, piperazinyl, piperidinyl or pyrrolidinyl.
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 1和Z 2，代表NH; Y表示-C 3-9 - 烷基 - ， - C 3-9 - 烯基 - ， - C 1-5烷基-NH- C 1-6烷基 - ， - C 1-5 - 烷基-NR 7 -CO-C 1 -C 6 - 1〜5个烷基 - ， - C 1-6 - 烷基-CO-NH - ， - C 1-6烷基-NH- CO - ， - C 烷基-CO-Het 10 -CO-，-C 1-3烷基-NH-CO-Het 3 H-4-C 1-3烷基-CO-NH-C 1-3烷基 - ， - C 烷基-NH-CO-L 1 -NH-，-NH-CO-L 2 -NH-，-C 烷基-CO-NH-L 3 -CO-，-C 1-12烷基-NH-CO-L， 1-NH-CO-C 1-3烷基 - ， - C 1-12烷基-CO-NH-L 3 -CO-NH-C 1-3烷基 - ， - C 1-12烷基-NR 11 -CH 2 - -CO-NH-C 1-3烷基 - ，Het 5 -CO-C 1-2烷基 - ， - C 烷基-CO-NH-C 1-3烷基-CO-NH - ， - C 1-5烷基-NH- 叔-C 1-3烷基-NH-，-C 1-3烷基-NH-CO-Het 27， -CO-或-C 1-3烷基-CO-Het 28 -CO-NH-; X 1表示直接键合，O，-OC 1-2烷基 - ， - CO-C 1-12 - 烷基 - ， - NR C 1-12烷基 - ， - CO-NR 17 - ，Het 23 -C _{1-2个烷基 - 或C 1-12烷基; O 2代表直接键合，O，-OC 1-2烷基 - ， - CO-C 1-2烷基 - ， - NR C 1-12烷基 - ， - CO-NR 19 - ，Het 24 -C _{1-2个烷基 - 或C 1-12烷基; R 1和R 2各自独立地表示氢，卤素，C 1-6烷氧基或C 1-6 >由Het 1或C 1-4烷氧基取代的烷氧基取代; R 2和R 4各自独立地表示氢或卤素; R 3表示氢或氰基; R 6，R 7，R 13，R 17和R 19代表氢; R 11表示氢或C 1-4烷基; R 16和R 18代表氢，C 1-4烷基或Het 17 -C 1 -4 烷基 - ; L 1，L 2和L 3各自独立地表示任选被一个或多个取代基取代的C 1-8烷基可能的两个或更多个选自苯基，甲基硫基，氰基，多卤代1-4烷基 - 苯基 - ，C 1-4烷基氧基，吡啶基，单 - 或二（C C 1-4烷基） - 氨基 - 或C 3-6环烷基; Het 2，Het 2，Het 17各自独立地表示吗啉基，恶唑基，异恶唑基或哌嗪基; Het 4，Het 4，Het 5 H 3各自独立地表示吗啉基，哌嗪基，哌啶基或吡咯烷基; Het 10表示哌嗪基，哌啶基，吡咯烷基或氮杂环丁烷基; Het 22代表吗啉基，恶唑基，异恶唑基或哌嗪基，其中所述Het 22任选被C 1-4烷基取代; Het 23和Het 24各自独立地表示选自吡咯烷基，哌嗪基或哌啶基的杂环，其中所述Het 23或Het 24， SUP>任选被Het 22-羰基取代; Het 27和Het 28各自独立地表示选自吗啉基，哌嗪基，哌啶基或吡咯烷基的杂环。}}

12. 发明申请

WO2008049904A2 USE OF MTKI 1 FOR TREATING OR PREVENTING BONE CANCER 审中-公开
标题翻译：使用MTKI 1治疗或预防骨癌
公开(公告)号：WO2008049904A2
公开(公告)日：2008-05-02
申请号：PCT/EP2007/061501
申请日：2007-10-25
申请人： JANSSEN PHARMACEUTICA NV , PERERA, Timothy, Pietro, Suren , JANICOT, Michel, Marie, François , MEERT, Theo, Frans , FREYNE, Eddy, Jean, Edgard
发明人： PERERA, Timothy, Pietro, Suren , JANICOT, Michel, Marie, François , MEERT, Theo, Frans , FREYNE, Eddy, Jean, Edgard
IPC分类号： A61K31/529 , A61P35/00 , A61P35/04
CPC分类号： A61K31/529
摘要： The present invention is concerned with the finding that 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 bone cancers and methods for killing bone cancer cells, including osteosarcomas, chondrosarcomas, myeloma bone disease and osteolytic bone metastases from other primary sites. It accordingly provides methods for treating, preventing, delaying or mitigating bone cancer, or for preventing and treating of bone loss associated with cancer metastases.
摘要翻译：本发明涉及大环喹唑啉衍生物4,6-乙二亚甲基嘧啶并[4,5-b] [6,1,12]苯并恶二氮杂环十五碳烯，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骨癌的药物和用于杀死骨癌的方法细胞，包括骨肉瘤，软骨肉瘤，骨髓瘤骨病和其他原发部位的骨溶解性骨转移。因此，它提供了治疗，预防，延缓或减轻骨癌或预防和治疗与癌症转移相关的骨丢失的方法。

13. 发明申请

WO2004007499A1 3-FURANYL ANALOGS OF TOXOFLAVINE AS KINASE INHIBITORS 审中-公开
标题翻译：托吡醇作为激酶抑制剂的3-FURANYL模拟物
公开(公告)号：WO2004007499A1
公开(公告)日：2004-01-22
申请号：PCT/EP2003/050293
申请日：2003-07-08
申请人： JANSSEN PHARMACEUTICA N.V. , LACRAMPE, Jean, Fernand, Armand , CONNORS, Richard, William , HO, Chih, Yung , RICHARDSON, Alan , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes , BAKKER, Annette, Cornelia
发明人： LACRAMPE, Jean, Fernand, Armand , CONNORS, Richard, William , HO, Chih, Yung , RICHARDSON, Alan , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes , BAKKER, Annette, Cornelia
IPC分类号： C07D487/04
CPC分类号： C07D487/04
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 m represents an integer being 0 or 1; n represents an integer being 0, 1 or 2; R 1 represents C 1-4 alkyl, C 1-4 alkyl substituted with pyridinyl, phenyl, piperidinyl or piperidinyl substituted with C 1-4- alkyloxycarbonyl; R 2 represents hydrogen or C 1-4 alkyl; R 3 represents hydrogen or C 1-4 alkyl; or R 2 and R 3 taken together with the carbon atom to which they are attached form cyclopentyl or piperidinyl wherein said cyclopentyl or piperidinyl each independently may optionally be substituted with one, or where possible, two or three substituents each independently selected from C 1-4 alkyloxycarbonyl, phenylcarbonyl or -C(=NH)-NH 2 ; R 4 represents halo or C 1-4 alkyloxy; R 5 represents Het 2 , C 1-4 alkyl substituted with one or where possible more substituents being selected from hydroxy, halo, Het 3 or NR 6 R 7 , or C 1-4 alkyloxy substituted with one or where possible more substituents being selected from Het 4 or -C(=O)-Het 4 ; R 6 and R 7 are each independently selected from hydrogen, C 1-4 alkyl, Het 5 or C 1-4 alkyl substituted with one or where possible more substituents being selected from hydroxy or Het 5 ; Het 2 represents piperazinyl; Het 3 represents a heterocycle selected from morpholinyl, pyrrolidinyl, piperidinyl, or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from C 1-4 alkyl preferably methyl, aminosulfonyl, mono- or di(C 1-4 alkyl)aminosulfonyl, hydroxyC 1 -4 alkyloxyC 1-4 alkyl, C 1-4 alkyloxyC 1-4 alkyl or C 1-4 alkyloxy; Het 4 represents a heterocycle selected from morpholinyl or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three C 1-4 alkyl substituents, preferably methyl; Het 5 represents a heterocycle selected from pyridinyl, pyrrolidinyl or piperidinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from aminosulfonyl, C 1-4 alkyloxycarbonyl or mono- or di(C 1-4 alkyl)aminosulfonyl.
摘要翻译：本发明涉及式（I）化合物的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m表示0或1的整数; n表示0或1或2的整数; R 1表示C 1-4烷基，被吡啶基取代的C 1-4烷基，苯基，哌啶基或被C 1-4 - 烷氧基羰基取代的哌啶基; R 2表示氢或C 1-4烷基; R 3表示氢或C 1-4烷基; 或R 2和R 3与它们所连接的碳原子一起形成环戊基或哌啶基，其中所述环戊基或哌啶基各自独立地可以任选被一个或可能的两个或三个取代基各自独立地选择 C 1-4烷氧基羰基，苯基羰基或-C（= NH）-NH 2; R 4表示卤素或C 1-4烷氧基; R 5表示Het 2，被一个或多个可能的更多选自羟基，卤素，Het 3或NR 6 R 7的取代基取代的C 1-4烷基，或被一个或多个在可能的情况下更多的取代基选自Het 4或-C（= O）-Het 4; R 6和R 7各自独立地选自氢，C 1-4烷基，Het 5或被一个或多个可能的更多取代基选自羟基或Het 5取代的C 1-4烷基; Het 2表示哌嗪基; Het 3表示选自吗啉基，吡咯烷基，哌啶基或哌嗪基的杂环，其中所述单环杂环各自独立地可以任选地被一个取代，或者如果可能的话，两个或三个取代基各自独立地选自C 1-4烷基，优选甲基，氨基磺酰基，单 - 或二（C 1-4烷基）氨基磺酰基，羟基C 1-4烷氧基C 1-4烷基，C 1-4烷氧基C 1-4烷基或C 1-4烷氧基; Het 4表示选自吗啉基或哌嗪基的杂环，其中所述单环杂环各自独立地可以任选地被一个取代，或在可能的情况下被两个或三个C 1-4烷基取代基，优选甲基取代; Het 5表示选自吡啶基，吡咯烷基或哌啶基的杂环，其中所述单环杂环各自独立地可以任选地被一个或两个或三个取代基独立地选自氨基磺酰基，C 1-4烷氧基羰基或单或二（C1 1-4烷基）氨基磺酰基。

14. 发明申请

WO2004007498A3 3-PHENYL ANALOGS OF TOXOFLAVINE AS KINASE INHIBITORS 审中-公开
公开(公告)号：WO2004007498A3
公开(公告)日：2004-01-22
申请号：PCT/EP2003/050292
申请日：2003-07-08
申请人： JANSSEN PHARMACEUTICA N.V. , LACRAMPE, Jean, Fernand, Armand , CONNORS, Richard, William , HO, Chih, Yung , RICHARDSON, Alan , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes , BAKKER, Annette, Cornelia
发明人： LACRAMPE, Jean, Fernand, Armand , CONNORS, Richard, William , HO, Chih, Yung , RICHARDSON, Alan , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes , BAKKER, Annette, Cornelia
IPC分类号： C07D487/04
摘要： The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereo-chemically isomeric forms thereof, wherein n represents an integer being 0, 1 or 2; m represents an integer being 0 or 1; R 1 represents C 1-4 alkyl; R 2 represents C 1 - 4 alkyl; R 3 represents C 1-4 alkyl; or R 2 and R 3 taken together with the carbon atom to which they are attached form a C 3-8 cycloalkyl or Het 1 wherein said C 3-8 cycloalkyl or Het 1 each independently may optionally be substituted with C 1-4 alkyloxycarbonyl; R 4 represents halo or C 1-4 alkyloxy; R 5 represents C 1-4 alkyloxycarbonyl, -O-(mono- or di(C 1-4 alkyl)aminosulfonyl), C 1 - 4 alkyl substituted with one or where possible more substituent being selected from Het 3 or NR 6 R 7 , C 1-4 alkyloxy substituted with one or where possible more substituents being selected from amino, Het 4 or NR 8 R 9 ; R 6 and R 7 are each independently selected from hydrogen, C 1-4 alkyl, C 1-4 alkyloxyC 1-4 alkyl, -Het 5 or C 1-4 alkyl substituted with one or where possible more substituents being selected from hydroxy, or Het 5 ; R 8 and R 9 are each independently selected from hydrogen, C 1-4 alkyl, -Het 7 or mono- or di(C 1-4 alkyl)aminosulphonyl; Het 3 represents a heterocycle selected from piperidinyl, or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from hydroxy, aminosulfonyl, amino, mono-or di(C 1-4 alkyl)aminosulfonyl, hydroxyC 1-4 alkyloxyC 1-4 alkyl or C 1-4 alkyloxy; Het 4 represents a heterocycle selected from morpholinyl, piperidinyl or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from C 1-4 alkyl, C 1-4 alkyloxycarbonyl or mono- or di(C 1-4 alkyl)aminosulfonyl; Het 5 represents a heterocycle selected from pyridinyl or piperidinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from aminosulfonyl, or mono- or di(C l4 alkyl)aminosulfonyl; Het 7 represents piperidinyl.

15. 发明申请

WO2009150240A1 IMIDAZOPYRIDINE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSINE KINASES 审中-公开
标题翻译：作为受体酪氨酸激酶抑制剂的咪唑吡啶衍生物
公开(公告)号：WO2009150240A1
公开(公告)日：2009-12-17
申请号：PCT/EP2009/057318
申请日：2009-06-12
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , CARR, Maria, Grazia , CONGREVE, Miles, Stuart , FREDERICKSON, Martyn , GRIFFITHS-JONES, Charlotte, Mary , HAMLETT, Christopher, Charles, Frederick , MADIN, Andrew , MURRAY, Christopher, William , BENNING, Rajdeep Kaur , SAXTY, Gordon , VICKERSTAFFE, Emma , WOODHEAD, Andrew, James , WOODHEAD, Steven, John , FREYNE, Eddy, Jean, Edgard , GOVAERTS, Tom, Cornelis, Hortense , ANGIBAUD, Patrick, René , ASTEX THERAPEUTICS LIMITED
发明人： BERDINI, Valerio , CARR, Maria, Grazia , CONGREVE, Miles, Stuart , FREDERICKSON, Martyn , GRIFFITHS-JONES, Charlotte, Mary , HAMLETT, Christopher, Charles, Frederick , MADIN, Andrew , MURRAY, Christopher, William , BENNING, Rajdeep Kaur , SAXTY, Gordon , VICKERSTAFFE, Emma , WOODHEAD, Andrew, James , WOODHEAD, Steven, John , FREYNE, Eddy, Jean, Edgard , GOVAERTS, Tom, Cornelis, Hortense , ANGIBAUD, Patrick, René
IPC分类号： C07D471/04 , C07D513/04 , A61P35/00 , A61K31/437 , A61K31/506 , A61K31/501 , A61K31/53 , A61K31/444 , A61K31/497 , A61K31/496 , A61K31/4545
CPC分类号： C07D471/04 , C07D513/04
摘要： The invention relates to new bicyclic heterocyclic derivative compounds, 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：本发明涉及新的双环杂环衍生物化合物，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。癌症。

16. 发明申请

WO2009118370A1 AZA-BICYCLOHEXYL SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译： AZA-BICYCLOHEXYL取代的吲哚基氨基酸衍生物作为HISTONE DEACETYLASE的新型抑制剂
公开(公告)号：WO2009118370A1
公开(公告)日：2009-10-01
申请号：PCT/EP2009/053566
申请日：2009-03-26
申请人： JANSSEN PHARMACEUTICA NV , FREYNE, Eddy, Jean, Edgard , PILATTE, Isabelle,Noëlle, Constance , ANGIBAUD, Patrick, René
发明人： FREYNE, Eddy, Jean, Edgard , PILATTE, Isabelle,Noëlle, Constance , ANGIBAUD, Patrick, René
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
CPC分类号： C07D403/14 , C07D401/14 , C07D405/14
摘要： This invention comprises the novel compounds of Formula (I), wherein R 1 , R 2 , R 3 , R 4 , A and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中R1，R2，R3，R4，A和X具有定义的含义，具有组蛋白脱乙酰酶抑制酶活性; 其制剂，含有它们的组合物及其作为药物的用途。

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