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1. 发明申请

WO2004105765A1 MACROCYCLIC QUINAZOLINE DERIVATIVES AS ANTIPROLIFERATIVE AGENTS 审中-公开
标题翻译：大环喹诺酮衍生物作为抗增生剂
公开(公告)号：WO2004105765A1
公开(公告)日：2004-12-09
申请号：PCT/EP2004/005621
申请日：2004-05-25
申请人： JANSSEN PHARMACEUTICA N.V. , 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
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
IPC分类号： A61K31/529
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, CH 2 , NH or S; in particular Z represents NH; Y represents -C 3-9 alkyl-, -C 3-9 alkenyl-, -C 3-9 alkynyl-, -C 3-7 alkyl-CO-NH- optionally substituted with amino, mono- or di(C 1-4 alkyl)amino or C 1-4 alkyloxycarbonylamino-, -C 3-7 alkenyl-CO-NH- optionally substituted with amino, mono- or di(C 1-4 alkyl)amino- or C 1-4 alkyloxycarbonylamino-, C 1-5 alkyl-oxy-C 1-5 alkyl-, -C 1-5 alkyl NR 13 -, -C 1-5 alkyl-, -C 1-5 alkyl-NR 14 -CO-C 1-5 alkyl-, -C 1-5 alkyl-CO NR 15 -C 1-5 alkyl-, -C 1-6 alkyl-CO-NH-, -C 1-6 alkyl-NH-CO-, -C 1-3 alkyl-NH-CS-Het 20 -, -C 1-3 alkyl-NH-CO-Het 20 -, -C 1-2 alkyl-CO-Het 21 -CO-, -Het 22 -CH 2 -CO-NH-C 1-3 alkyl-, -CO-NH-C 1-6 alkyl-, -NH-CO-C 1-6 alkyl-, -CO-C 1-7 alkyl-, -C 1-7 alkyl-CO-, -C 1-6 alkyl-CO-C 1-6 alkyl-, -C 1-2 alkyl-NH-CO-CR 16 R 17 -NH-, -C 1-2 alkyl-CO-NH-CR 18 R 19 -CO-, -C 1-2 alkyl-CO-NR 20 -C 1-3 alkyl-CO-, C 1-2 alkyl-NR 21 -CH 2 -CO-NH-C 1-3 alkyl-, or -NR 22 -CO-C 1-3 alkyl-NH-; X 1 represents a direct bond, O or -O-C 1-2 alkyl-, CO, -CO-C 1-2 alkyl-, NR 11 , -NR 11 -C 1-2 alkyl-, CH 2 -, -O-N=CH- or -C 1-2 alkyl-; X 2 represents a direct bond, O, -O-C 1-2 alkyl-, CO, -CO-C 1-2 alkyl-, NR 12 , -NR 12 -C 1-2 alkyl-, -CH 2 -, -O-N=CH- or -C 1-2 alkyl-. 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.
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Z代表O，CH2，NH或S; 特别是Z表示NH; 一个或多个（C 1-4烷基）氨基或C 1-4烷氧基羰基氨基 - 取代的C 1-3烷基 - ， - C 3-9烯基 - ， - C 3-9炔基 - ， - 一个或多个（C 1-4烷基）氨基 - 或C 1-4烷氧基羰基氨基 - ，C 1-5烷基 - 氧基-C 1-5烷基 - ， - C 1-5烷基NR 13取代的-C 3-7烯基-CO-NH- - ， - C 1-5烷基 - ， - C 1-5烷基-NR 14 -CO-C 1-5烷基 - ， - C 1-5烷基-CO NR 15 -C 1-6烷基 - ， - C 1-6烷基-CO-NH - ，-C 1-6烷基-NH-CO - ， - C 1-3烷基-NH-CS-Het 20 - ， - C 1-3烷基-NH-CO-Het 20 - ， - C 1-2烷基-CO-Het -CO-，-Het 22，-CH 2 -CO-NH-C 1-3烷基 - ， - CO-NH-C 1-6烷基 - ， - -NH-CO-C 1-6烷基 - ， - CO-C 1-7烷基 - ， - C 1-7烷基-CO - ， - C 1-6烷基-CO-C 1-6烷基 - ， - C 1-2烷基-NH-CO-CR 16 R 17 -NH-，-C 1-2烷基-CO- NH-CR 18 R 19 -CO - ， - C 1-2烷基-CO-NR 20 -C 1-3烷基-CO-，C 1-2烷基-NR 21 -CH 2 -CO-NH-C1- 3-烷基 - 或-NR 22 -CO-C 1-3烷基-NH-; X 1表示直接键，O或-O-C 1-2烷基 - ，CO，-CO-C 1-2烷基 - ，NR 11，-NR 11 -C 1-2烷基 - ，CH 2 - ，--ON = CH-或-C1-2烷基 - ; X 2表示直接键，O，-O-C 1-2烷基 - ，CO，-CO-C 1-2烷基 - ，NR 12，-NR 12 -C 1-2烷基 - ， - CH 2 - ON = CH-或-C1-2烷基。在体外，在受体酪氨酸激酶EGFR的酶学测定中已经证明了本发明化合物的生长抑制作用抗肿瘤活性。

2. 发明申请

WO2003037891A1 HETEROARYL AMINES AS GLYCOGEN SYNTHASE KINASE 3BETA INHIBITORS (GSK3 INHIBITORS) 审中-公开
标题翻译：杂多胺作为糖原合成酶激酶3β抑制剂（GSK3抑制剂）
公开(公告)号：WO2003037891A1
公开(公告)日：2003-05-08
申请号：PCT/EP2002/012077
申请日：2002-10-29
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , LOVE, Christopher, John , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , VINKERS, Hendrik, Maarten , VAN AKEN, Koen, Jeanne, Alfons , DIELS, Gaston, Stanislas, Marcella
发明人： FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , LOVE, Christopher, John , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , VINKERS, Hendrik, Maarten , VAN AKEN, Koen, Jeanne, Alfons , DIELS, Gaston, Stanislas, Marcella
IPC分类号： C07D403/12
CPC分类号： C07D213/74 , C07D239/42 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： This invention concerns a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A is a 6-membered heterocycle; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally substituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; optionally substituted C 1-6 alkyloxy C 1-6 alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R 2 is hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R 3 is hydrogen; hydroxy; halo; optionally substituted C 1-6 alkyl or C 1-6 alkenyl or C 2-6 alkynyl; C 1-6 alkyloxy; C 1-6 alkylthio; C 1-6 alkyloxycarbonyl; C 1-6 alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C 1-6 alkyl)amino; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; polyhaloC 1-6 alkylthio; R 21 ; R 21 -C 1-6 alkyl; R 21 -O-; R 21 -S-; R 21 -C(=0)-; R 21 -S(=0)p-; R 7 -S =O R 7 -S(=O)p-NH-; R 21 -S(=O)p-NH-; R 7 -C(=0)-; -NHC(=0)H; -C(=O)NHNH2; R 7 -C(=O)-NH-; R 21 -C(=O)-NH-; -C(=NH)R 7 ; -C(=NH)R 21 ; R° is an optionally substituted heterocycle provided that -X-R 2 and/or R 3 is other than hydrogen;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，其N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中环A为6-元杂环; R 1是氢; 芳基; 甲酰基; ç<子> 1-6 烷基羰基; 任选取代的C 1-6烷基; ç<子> 1-6 烷氧基羰基; 任选取代的C 1-6烷氧基C 1-6烷基羰基; X是直接键或连接基原子或基团; Z是直接键或连接基原子或基团; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，每个所述基团可以任选被取代; R 3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 1-6链烯基或C 2-6炔基; ç<子> 1-6 烷氧基; ç<子> 1-6 烷硫基; ç<子> 1-6 烷氧基羰基; ç<子> 1-6 烷基羰基氧基; 羧基; 氰基; 硝基; 氨基; 单 - 或二（C 1-6烷基）氨基; 多卤代<子> 1-6 烷基; 多卤代<子> 1-6 烷氧基; 多卤代<子> 1-6 烷硫基; [R ^{21 ; [R ^{21 -C <子> 1-6 烷基; [R ^{21 -O-; [R ^{21 -S-; [R ^{21 -C（= O） - ; [R ^{21 -S（= O）p - ; R 7 -S = O R 7 -S（= O）p -NH-; [R ^{21 -S（= O）P-NH-; [R ^{7 -C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; [R ^{7 C（= O）-NH-; [R ^{21 C（= O）-NH-; -C（= NH）R ^{7 ; -C（= NH）R ^{21 ; R＆度; 是任选取代的杂环，条件是-XR 2和/或R 3不为氢;它们的用途，包含它们的药物组合物及其制备方法。}}}}}}}}}}}}

3. 发明申请

WO2005058913A1 PYRIDO- AND PYRIMIDOPYRIMIDINE DERIVATIVES AS ANTI- PROLIFERATIVE AGENTS 审中-公开
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：WO2005058913A1
公开(公告)日：2005-06-30
申请号：PCT/EP2004/053501
申请日：2004-12-15
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , WILLEMS, Marc , STORCK, Pierre, Henri , PONCELET, Virginie, Sophie , VAN EMELEN, Kristof , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , EMBRECHTS, Werner, Constant, Johan , PERERA, Timothy, Pietro, Suren
发明人： FREYNE, Eddy, Jean, Edgard , WILLEMS, Marc , STORCK, Pierre, Henri , PONCELET, Virginie, Sophie , VAN EMELEN, Kristof , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , EMBRECHTS, Werner, Constant, Johan , PERERA, Timothy, Pietro, Suren
IPC分类号： C07D498/18
CPC分类号： C07D498/16 , C07D471/04 , C07D487/04 , C07D487/16 , C07D487/22
摘要： The present invention concerns the compounds of formula (I) the N -oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein a 1 -a 2 =a 3 -a 4 represents a divalent radical selected from N-CH=CH-CH, N-CH N-CH or CH-CH=N-CH; Z represents NH; Y represents -C 3-9 alkyl-, -C l-5 alkyl-NR 13 -C l-5 alkyl-,-C 1 - 6 alkyl-NH-CO- or -CO-NH -C 1-6 alkyl- ; X 1 represents -O- or -NR 11 -; X 2 represents -C 1-2 alkyl-, -O-C 1-2 alkyl, -O- or -O-CH 2 -;R 1 represents hydrogen or halo; R 2 represents hydrogen, cyano, halo, hydroxycarbonyl-C l-4 alkyloxycarbonyl-, Het 16 -carbonyl- or Ar 5 ; R 3 represents hydrogen; R 4 represents hydroxy, C 1-4 alkyloxy-, Ar 4 -C 1-4 alkyloxy or R 4 represents C l-4 alkyloxy substituted with one or where possible two or more substituents selected from C 1-4 alkyloxy- or Het 2 -; R 11 represents hydrogen; R 12 represents hydrogen, C l-4 alkyl- or C l-4 alkyl-oxy-carbonyl-; R 13 represents Het 14 -C l-4 alkyl, in particular morpholinyl-C l-4 alkyl; Het 2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C 1-4 alkyl-, preferably methyl; Het 14 represents morpholinyl; Het 16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar 4 represents phenyl; Ar 5 represents phenyl optionally substituted with cyano.
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a 1 -a 2 = a 3 -a 4表示选自N-CH = CH-CH，N-CHN-CH或CH-CH = N-CH的二价基团; 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-C 1-6烷基 - ; X 1表示-O-或-NR 11 - ; X 2表示-C 1-2烷基 - ， - O-C 1-2烷基，-O-或-O-CH 2 - ; R 1表示氢或卤素; R 2代表氢，氰基，卤素，羟基羰基-C 1-4烷基氧基羰基，Het 16 - 羰基 - 或Ar 5。 R 3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。 - ; R 11表示氢; R 12表示氢，C 1-4烷基 - 或C 1-4烷基 - 氧 - 羰基 - ; R 13代表Het 14 -Cl-4烷基，特别是吗啉基-C 1-4烷基; Het 2表示选自被C 1-4烷基，优选甲基取代的吗啉基或哌啶基的杂环; Het <14>代表吗啉基; Het 16表示选自吗啉基或吡咯烷基的杂环; Ar 4表示苯基; Ar 5表示任选被氰基取代的苯基。

4. 发明申请

WO2005058318A1 3-CYANO-QUINOLINE DERIVATIVES WITH ANTIPROLIFERATIVE ACTIVITY 审中-公开
标题翻译：具有抗增殖活性的3-氰基喹啉衍生物
公开(公告)号：WO2005058318A1
公开(公告)日：2005-06-30
申请号：PCT/EP2004/053497
申请日：2004-12-15
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , VAN EMELEN, Kristof , EMBRECHTS, Werner, Constant, Johan , PERERA, Timothy, Pietro, Suren
发明人： FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , VAN EMELEN, Kristof , EMBRECHTS, Werner, Constant, Johan , PERERA, Timothy, Pietro, Suren
IPC分类号： A61K31/439
CPC分类号： C07D215/54 , A61K31/4748 , C07D498/06
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. Compounds of formula (I) inhibit tyrosine kinase enzymes.
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。式（I）化合物抑制酪氨酸激酶。

5. 发明申请

WO2005012304A2 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：WO2005012304A2
公开(公告)日：2005-02-10
申请号：PCT/EP2004/051457
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： C07D487/00
CPC分类号： C07D487/04
摘要： This invention concerns compounds of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochernically isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R 1 represents hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; C 1-6 a]kyl; C 1-6 alkyloxycarbonyl; C 1-6 alkyl substituted with formyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonytoxy; or optionally substituted C 1-6 alkyloxyCl-6alkylcarbonyl; X 1 represents a direct bond; -(CH 2 ) n3 - or -(CH 2 ) n4 -X 1a -X 1b -; R 2 represents optionally substituted C 3-7 CYCloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one heteroatorn selected from 0, S or N; benzoxazolyl or a radical of formula (a-1); X 2 represents a direct bond; -NR 1 -NR 1 -(CH 2 ) N3 -; -0-; -0-(CH 2 ) n3 -; -C(=O)-; -C(=O)- (CH 2 ) n3 -; -C(=O)-NR 5 -(CH 2 ) n3 -; -C(=S)-; -S-; -S(=O) n1 -; -(CH 2 ) n3 -; -(CH 2 ) n4 -X 1a -X 1b -; -X 1a .-X 1b -(CH 2 ) n4 -; -S(=O) n1 -NR 5 -(CH 2 ) n3 -NR 5 _ or -S(=O) n1 ,-NR 5 -(CH 2 ) n3 -; R 3 represents an optionally substituted 5-or 6-membered monocyclic heterocycle containing at least one heteroatom selected from 0, S or N, or a 9-or 10-membered bicyclic heterocycle containing at least one heteroatom selected from 0, S or N; R 4 represents hydrogen; halo; hydroxy; optionally substituted C 1-4 alkyl; optionally substituted C 2-4 alkenyl or C 2-4 alkynyl; polyhaloC 1-3 alkyl; optionally substituted C 1-4 alkyloxy; polyhaloC 1-3 alkyloxy; C 1-4 alkylthio; polyhaloC 1-3 alkylthio; C 1-4 alkyloxycarbonyl; C 1-4 alkylcarbonyloxy; C 1-4 alkylcarbonyl; polyhaloC 1-4 alkylcarbonyl; nitro; cyano; carboxyl; NR 9 R 10 ; C(=O)NR 9 R 10 ;-NR 5_ C(=O)-NR 9 R 10 ; -NR 5 -C(=O)-R 5 ; -S(=O) n1 ,-R 11 -NR 5 -S(=O) n1 ,-R 11 -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）的化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体异构体形式，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 a] kyl; C 1-6烷氧基羰基; 被甲酰基，C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基氧基取代的C 1-6烷基; 或任选取代的C 1-6烷氧基C 1-6烷基羰基; X1表示直接键; - （CH 2）n3-或 - （CH 2）n4-X1a-X1b-; R 2表示任选取代的C 3-7C环烷基; 苯基; 含有至少一个选自0，S或N的杂化剂的4,5,6-或7-元单环杂环; 苯并恶唑基或式（a-1）基团; X2表示直接键; -NR 1 -NR 1 - （CH 2）N 3 - ; -0-; -O-（CH 2）N 3 - ; -C（= O） - ; -C（= O） - （CH 2）n3-; -C（= O）-NR <5> - （CH2）N3-; -C（= S） - ; -S-; -S（= O）N 1 - ; - （CH2）N3-; - （CH 2）N 4 - X1A-X1b-; -X1a.-X1b-（CH2）N4-; -S（= O）n1-NR5 - （CH2）n3-NR5或-S（= O）n1，-NR5 - （CH2）n3-; R 3表示含有至少一个选自O，S或N的杂原子或含有至少一个选自O，S或S的杂原子的9元或10元双环杂环的任选取代的5元或6元单环杂环， N; R 4表示氢; 光环; 羟基; 任选取代的C 1-4烷基; 任选取代的C 2-4烯基或C 2-4炔基; polyhaloC1-3alkyl; 任选取代的C 1-4烷氧基; polyhaloC1-3alkyloxy; C1-4alkylthio; polyhaloC1-3alkylthio; C1-4alkyloxycarbonyl; C1-4alkylcarbonyloxy; C1-4alkylcarbonyl; polyhaloC1-4alkylcarbonyl; 硝基; 氰基; 羧基; NR <9> - [R <10>; C（= O）NR <9> - [R <10>; - NR <5_> C（= O）-NR <9> - [R <10>; -NR <5> C（= O）-R <5>; -S（= O）n1，-R 11 -NR 5 -S（= O）n1，-R 11 -S-CN; -NR 5 -CN; 其用途，包含它们的药物组合物及其制备方法。

6. 发明申请

WO2003037877A1 AMINOBENZAMIDE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3β INHIBITORS 审中-公开
标题翻译：氨基苯甲酸衍生物作为GLYCOGEN SYNTHASE KINASE 3β抑制剂
公开(公告)号：WO2003037877A1
公开(公告)日：2003-05-08
申请号：PCT/EP2002/012079
申请日：2002-10-29
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , DAEYAERT, Frederik, Frans, Desire , KUKLA, Michael, Joseph , GEERTS, Hugo, Alfons, Gabriel , NUYDENS, Rony, Maria , MERCKEN, Marc, Hubert , LUDOVICI, Donald, William
发明人： FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , DAEYAERT, Frederik, Frans, Desire , KUKLA, Michael, Joseph , GEERTS, Hugo, Alfons, Gabriel , NUYDENS, Rony, Maria , MERCKEN, Marc, Hubert , LUDOVICI, Donald, William
IPC分类号： C07D239/30
CPC分类号： C07D239/42 , A61K31/506 , C07D239/47 , C07D239/48 , C07D239/50 , C07D403/12
摘要： This invention concerns a compound of formula (I),a N -oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally substituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; optionally substituted C 1-6 alkyloxyC 1-6 alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R 2 is hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R 3 is hydrogen; hydroxy; halo; optionally substituted C 1-6 alkyl or C 2-6 alkenyl or C 2-6 alkynyl; C 1-6 alkyloxy; C 1-6 alkylthio; C 1-6 alkyloxycarbonyl; C 1-6 alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C 1-6 alkyl)amino; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; polyhaloC 1-6 alkylthio; R 21 ; R 21 -C 1-6 alkyl; R 21 -O-; R 21 -S-; R 21 -C(=O)-; R 21 -S(=O) p -; R 7 -S(=O) p -; R 7 -S(=O) p -NH-; R 21 -S(=O) p -NH-; R 7 -C(=O)-; -NHC(=O)H; -C(=O)NHNH 2 ; R 7 -C(=O)-NH-; R 21 -C(=O)-NH-; -C(=NH)R 7 ; -C(=NH)R 21 ; R 4a or R 4b each independently represent hydrogen, R 8 , -Y 1 -NR 9 -Y 2 -NR 10 R 11 , -Y 1 -NR 9 -Y 1 -R 8 , -Y 1 -NR 9 R 10 ; provided that -X-R 2 and/or R 3 is other than hydrogen;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，其中N为氧化物，其药学上可接受的加成盐，季胺及其立体化学异构形式，其中环A为6-元杂环; R 1是氢; 芳基; 甲酰基; C1-6烷基; 任选取代的C 1-6烷基; C1-6alkyloxycarbonyl; 任选取代的C 1-6烷氧基C 1-6烷基羰基; X是直接键或连接原子或基团; Z是O或S; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，所述基团中的每一个可任选被取代; R 3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 2-6烯基或C 2-6炔基; C1-6烷; C 1-6烷; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; 羧基; 氰基; 硝基; 氨基; 单或二（C 1-6烷基）氨基; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; [R <21>; [R <21> -C 1-6烷基; [R <21> -O-; [R <21> -S-; [R <21> C（= O） - ; [R <21> -S（= O）p - ; [R <7> -S（= O）p - ; [R <7> -S（= O）P-NH-; [R <21> S（= O）P-NH-; [R <7> C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; [R <7> C（= O）-NH-; [R <21> C（= O）-NH-; -C（= NH）R <7>; -C（= NH）R 21; R 4a或R 4b各自独立地表示氢，R 8，-Y 1 -NR 9 -Y 2 -NR 10 R 11，-Y 1 -NR 9 -Y 1 -R 8，-Y1-NR 9 R 10; 条件是-X-R 2和/或R 3不是氢;它们的用途，包含它们的药物组合物及其制备方法。

7. 发明申请

WO2003037869A1 AMIDE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3-BETA INHIBITORS 审中-公开
标题翻译：作为GLYCOGEN SYNTHASE KINASE 3-BETA抑制剂的酰胺衍生物
公开(公告)号：WO2003037869A1
公开(公告)日：2003-05-08
申请号：PCT/EP2002/012067
申请日：2002-10-29
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , LACRAMPE, Jean, Fernand, Armand , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , DAEYAERT, Frederik, Frans, Desire , KUKLA, Michael, Joseph , GEERTS, Hugo, Alfons, Gabriel , NUYDENS, Rony, Maria , MERCKEN, Marc, Hubert , LUDOVICI, Donald, William
发明人： FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , LACRAMPE, Jean, Fernand, Armand , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , DAEYAERT, Frederik, Frans, Desire , KUKLA, Michael, Joseph , GEERTS, Hugo, Alfons, Gabriel , NUYDENS, Rony, Maria , MERCKEN, Marc, Hubert , LUDOVICI, Donald, William
IPC分类号： C07D213/82
CPC分类号： C07D213/81 , C07D213/82 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： This invention concerns a compound of formula (I' ),a N -oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally substituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; optionally substituted C 1-6 alkyloxyC 1-6 alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R 2 is hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R 3 is hydrogen; hydroxy; halo; optionally substituted C 1-6 alkyl or C 2-6 alkenyl or C 2-6 alkynyl; C 1-6 alkyloxy; C 1-6 alkylthio; C 1-6 alkyloxycarbonyl; C 1-6 alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C 1-6 alkyl)amino; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; polyhaloC 1-6 alkylthio; R 21 ; R 21 -C 1-6 alkyl; R 21 -O-; R 21 -S-; R 21 -C(=O)-; R 21 -S(=O) p -; R 7 -S(=O) p -; R 7 -S(=O) p -NH-; R 21 -S(=O) p -NH-; R 7 -C(=O)-; -NHC(=O)H;-C(=O)NHNH 2 ; R 7 -C(=O)-NH-; R 21 -C(=O)-NH-; -C(=NH)R 7 ; -C(=NH)R 21 ; R 4a or R 4b each independently represent hydrogen, R 8 , -Y 1 -NR 9 -Y 2 -NR 10 R 11 , -Y 1 -NR 9 -Y 1 -R 8 , -Y 1 -NR 9 R 10 ; provided that -X-R 2 and/or R 3 is other than hydrogen; 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，季胺及其立体化学异构形式，其中环A表示6-元杂环; R 1是氢; 芳基; 甲酰基; C1-6烷基; 任选取代的C 1-6烷基; C1-6alkyloxycarbonyl; 任选取代的C 1-6烷氧基C 1-6烷基羰基; X是直接键或连接原子或基团; Z是O或S; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，所述基团中的每一个可任选被取代; R 3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 2-6烯基或C 2-6炔基; C1-6烷; C 1-6烷; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; 羧基; 氰基; 硝基; 氨基; 单或二（C 1-6烷基）氨基; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; [R <21>; [R <21> -C 1-6烷基; [R <21> -O-; [R <21> -S-; [R <21> C（= O） - ; [R <21> -S（= O）p - ; [R <7> -S（= O）p - ; [R <7> -S（= O）P-NH-; [R <21> S（= O）P-NH-; [R <7> C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; [R <7> C（= O）-NH-; [R <21> C（= O）-NH-; -C（= NH）R <7>; -C（= NH）R 21; R 4a或R 4b各自独立地表示氢，R 8，-Y 1 -NR 9 -Y 2 -NR 10 R 11，-Y 1 -NR 9 -Y 1 -R 8，-Y1-NR 9 R 10; 条件是-X-R 2和/或R 3不是氢; 其用途，包含它们的药物组合物及其制备方法。

8. 发明申请

WO2008006884A2 MTKI QUINAZOLINE DERIVATIVES 审中-公开
标题翻译： MTKI喹唑啉衍生物
公开(公告)号：WO2008006884A2
公开(公告)日：2008-01-17
申请号：PCT/EP2007/057200
申请日：2007-07-12
申请人： JANSSEN PHARMACEUTICA N.V. , PAPANIKOS, Alexandra , FREYNE, Eddy, Jean, Edgard , TEN HOLTE, Peter , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , MEVELLEC, Laurence, Anne , STORCK, Pierre, Henri
发明人： PAPANIKOS, Alexandra , FREYNE, Eddy, Jean, Edgard , TEN HOLTE, Peter , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , MEVELLEC, Laurence, Anne , STORCK, Pierre, Henri
CPC分类号： C07D498/14 , C08K5/544
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 Y represents -C 3-9 alkyl-, -C 1-5 alkyl-NR 6 -C 1-5 alkyl- or -C 1-5 alkyl-NR 7 -CO-C 1-5 alkyl-; X 1 represents -O-; X 2 represents NR 5 -C 1-2 alkyl-; R 1 represents hydrogen, halo or Het 3 -O-; R 2 represents hydrogen; R 3 represents hydroxy, C 1-4 alkyloxy- or C 1-4 alkyloxy subst ituted with one or two substituents each independently selected from Het 4 , hydroxy, C 1-4 alkyloxy-, C 1-4 alkyloxy-C 1-4 alkyloxy and NR 9 R 10 ; R 5 represents hydrogen or C 1-4 alkyl; R 6 represents hydrogen or C 1-4 alkyl; R 7 represents hydrogen; R 9 and R 10 each independently represent hydrogen; C 1-4 alkyl-S(=O) 2 -C 1-4 alkyl-C(=O)-; C 1-4 alkyl or C 1-4 alkyl substituted with hydroxy; Het 3 represents pyridinyl optionally substituted with C 1-4 alkyl; Het 4 represents morpholinyl, piperidinyl or piperazinyl wherein said Het 4 is optionally substituted with hydroxy-C 1-4 alkyl or C 1-4 alkyl-S(=O) 2 -C 1-4 alkyl-.
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Y代表-C C 3-5烷基 - ， - C 1-5烷基-NR 6 -C 1-5烷基 - 或 -C <子> 1-5 烷基 - NR ^{7 -CO-C <子> 1-5 烷基 - ; X 1表示-O-; X 2表示NR 5 -C 1-2烷基 - 。 R 1表示氢，卤素或Het 3 -O-; R 2代表氢; R 3代表羟基，C 1-4烷氧基或C 1-4烷氧基，其中各取代基各自独立地选自Het 4，羟基，C 1-4烷氧基，C 1-4烷氧基-C 1-4烷氧基和NR 9 R 10; R 5代表氢或C 1-4烷基; R 6代表氢或C 1-4烷基; R 7代表氢; R 9和R 10各自独立地代表氢; ç<子> 1-4 烷基-S（= O）<子> 2 -C <子> 1-4 烷基-C（= O） - ; 被羟基取代的C 1-4烷基或C 1-4烷基; Het 3 3代表任选被C 1-4烷基取代的吡啶基; Het 4表示吗啉基，哌啶基或哌嗪基，其中所述Het 4任选被羟基-C 1-4烷基或C 1-14 -4 烷基-S（= O）<子> 2 -C <子> 1-4 烷基 - 。}

9. 发明申请

WO2006074984A1 PYRAZOLOPYRIMIDINES AS CELL CYCLE KINASE INHIBITORS 审中-公开
标题翻译：作为细胞周期激酶抑制剂的吡唑并嘧啶
公开(公告)号：WO2006074984A1
公开(公告)日：2006-07-20
申请号：PCT/EP2006/050096
申请日：2006-01-09
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , LACRAMPE, Jean, Fernand, Armand , PERERA, Timothy, Pietro, Suren , TEN HOLTE, Peter , LIGNY, Yannick, Aimé, Eddy , LARDEAU, Delphine, Yvonne, Raymonde , LAVRIJSSEN, Tom
发明人： FREYNE, Eddy, Jean, Edgard , LACRAMPE, Jean, Fernand, Armand , PERERA, Timothy, Pietro, Suren , TEN HOLTE, Peter , LIGNY, Yannick, Aimé, Eddy , LARDEAU, Delphine, Yvonne, Raymonde , LAVRIJSSEN, Tom
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X1 and X2 have defined meanings, having cell cycle kinase 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R 1，R 2，R 3，R 4，R 5，R 6，X 1和X 2具有定义的含义，具有抑制细胞周期激酶的酶活性，其制备方法，含有它们的组合物及其作为医学。

10. 发明申请

WO2006074985A1 5-MEMBERED ANNELATED HETEROCYCLIC PYRIMIDINES AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的5-MEMBERED ANNELATED HEOCOCYCLIC PYRIMIDINES
公开(公告)号：WO2006074985A1
公开(公告)日：2006-07-20
申请号：PCT/EP2006/050097
申请日：2006-01-09
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , LACRAMPE, Jean, Fernand, Armand , PERERA, Timothy, Pietro, Suren , TEN HOLTE, Peter , LIGNY, Yannick, Aimé, Eddy , LARDEAU, Delphine, Yvonne, Raymonde , LAVRIJSSEN, Tom
发明人： FREYNE, Eddy, Jean, Edgard , LACRAMPE, Jean, Fernand, Armand , PERERA, Timothy, Pietro, Suren , TEN HOLTE, Peter , LIGNY, Yannick, Aimé, Eddy , LARDEAU, Delphine, Yvonne, Raymonde , LAVRIJSSEN, Tom
IPC分类号： C07D473/32 , C07D487/04 , A61K31/519 , A61K31/52 , A61P35/00
CPC分类号： C07D473/32 , C07D487/04
摘要： This invention comprises the novel compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , Q 1 , Q 2 , X 1 , X 2 , Y and Z have defined meanings, having cell cycle kinase 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R 1，R 2，R 3，R 4， >，R 5，R 6，Q 1，Q 2，X 1，...，SUP Y，Z定义含有细胞周期激酶抑制酶活性，其制备方法，含有它们的组合物及其作为药物的用途。

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