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1. 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。}}

2. 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。

3. 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。

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

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。

6. 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 - 。}

7. 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。

8. 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。

9. 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。

10. 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。}}}}

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