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1. 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。

2. 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。

3. 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.

4. 发明申请

WO2005058870A1 AMINO-BENZIMIDAZOLES DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 审中-公开
标题翻译：氨基苯并咪唑衍生物作为呼吸道同种病毒复制的抑制剂
公开(公告)号：WO2005058870A1
公开(公告)日：2005-06-30
申请号：PCT/EP2004/053617
申请日：2004-12-20
申请人： TIBOTEC PHARMACEUTICALS LTD. , BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , GUILLEMONT, Jerôme, Emile, Georges , LACRAMPE, Jean, Fernand, Armand
发明人： BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , GUILLEMONT, Jerôme, Emile, Georges , LACRAMPE, Jean, Fernand, Armand
IPC分类号： C07D401/06
CPC分类号： C07D405/14 , C07D401/06 , C07D401/14
摘要： The present invention concerns amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula (I) their prodrugs, N -oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is Ar 1 or C 1-6 alkyl substituted with one or more substituents selected from trifluoromethyl, C 3-7 cycloalkyl, Ar 2 , hydroxy, C 1-4 alkoxy, C 1-4 alkylthio, Ar 2 -oxy-, Ar 2 -thio-, Ar 2 (CH2)„oxy, Ar 2 (CH 2 ) n thio, hydroxycarbonyl, aminocarbonyl, C 1-4 alkylcarbonyl, Ar 2 carbonyl, C 1-4 alkoxycarbonyl, Ar 2 (CH 2 ) n carbonyl, aminocarbonyloxy, C 1-4 alkylcarbonyloxy, Ar 2 carbonyloxy, Ar 2 (CH 2 ) n carbonyloxy, hydroxy-C 2- 4 -alkyloxy, C 1-4 alkoxycarbonyl(CH 2 ) n oxy, monoor di(C 1-4 alkyl)-aminocarbonyl, mono- or di(C 1-4 alkyl)aminocarbonyloxy, aminosulfonyl, mono- or di(C 1-4 alkyl)aminosulfonyl, dioxolanyl optionally substituted with one or two C 1-6 alkyl radicals, and a heterocycle selected from pyrrolidinyl, pyrrolyl, dihydropyrrolyl, thiazolidinyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, pyridyl and tetrahydropyridyl, which each may optionally be substituted with oxo or C 1 - 6 alkyl; G is a direct bond or optionally substituted C 1-10 alkanediyl R 1 is Ar 1 or a monocyclic or bicyclic heterocycle; one of R 2a and R 3a is C 1-6 alkyl and the other one of R 2 a and R 3a is hydrogen; in case R 2 a is different from hydrogen then R 2b is hydrogen or C 1-6 alkyl, and R 3b is hydrogen; in case R 3a is different from hydrogen then R 3b is hydrogen or C 1-6 alkyl, and R 2b is hydrogen; Ar 1 is phenyl or substituted phenyl and Ar 2 is phenyl or substituted phenyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.
摘要翻译：本发明涉及对呼吸道合胞病毒复制具有抑制活性的氨基苯并咪唑，其具有式（I）的前药，N-氧化物，加成盐，季胺，金属络合物和立体化学异构形式，其中Q为Ar1或C1 被一个或多个选自三氟甲基，C 3-7环烷基，Ar 2，羟基，C 1-4烷氧基，C 1-4烷硫基，Ar 2 - 氧基 - ，Ar 2 - 硫基 - ，Ar 2 （CH2）“氧基，Ar2（CH2）nthio，羟基羰基，氨基羰基，C1-4烷基羰基，Ar2羰基，C1-4烷氧基羰基，Ar2（CH2）n羰基，氨基羰基氧基，C1-4 烷基羰基氧基，Ar 2羰基氧基，Ar 2（CH 2）n - 羰基氧基，羟基-C 2 - 4-烷氧基，C 1-4烷氧基羰基（CH 2）n羟基，一或二（C 1-4烷基） - 氨基羰基，单或二 1-4烷基）氨基羰基氧基，氨基磺酰基，一或二（C 1-4烷基）氨基磺酰基，任选被一个或两个C 1-6烷基取代的二氧戊环，以及选自吡咯烷基，吡咯基，二氢吡咯基，噻唑烷基，咪唑基，三唑基，哌啶基，高哌啶基，哌嗪基，吡啶基和四氢吡啶基，其各自可以任选被氧代或C 1-6烷基取代; G是直接键或任选取代的C 1-10烷二基R 1是Ar 1或单环或双环杂环; R 2a和R 3a之一是C 1-6烷基，R 2 a和R 3a中的另一个是氢; 在R 2不同于氢的情况下，R 2b是氢或C 1-6烷基，R 3b是氢; 在R 3a不同于氢的情况下，R 3b是氢或C 1-6烷基，R 2b是氢; Ar 1是苯基或取代的苯基，Ar 2是苯基或取代的苯基。它还涉及它们的制备方法和包含它们的组合物，以及它们作为药物的用途。

5. 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。

6. 发明申请

WO2007107543A1 INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 审中-公开
标题翻译： MDM2和P53之间相互作用的抑制剂
公开(公告)号：WO2007107543A1
公开(公告)日：2007-09-27
申请号：PCT/EP2007/052579
申请日：2007-03-19
申请人： JANSSEN PHARMACEUTICA N.V. , LACRAMPE, Jean, Fernand, Armand , MEYER, Christophe , SCHOENTJES, Bruno , LARDEAU, Delphine, Yvonne, Raymonde , PONCELET, Alain, Philippe , VAN HIJFTE, Luc
发明人： LACRAMPE, Jean, Fernand, Armand , MEYER, Christophe , SCHOENTJES, Bruno , LARDEAU, Delphine, Yvonne, Raymonde , PONCELET, Alain, Philippe , VAN HIJFTE, Luc
IPC分类号： C07D401/12 , C07D405/12 , C07D471/04 , A61K31/4409 , A61P35/00
CPC分类号： C07D405/12 , C07D401/12 , C07D471/04
摘要： The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R 1 , R 2 , A and Z have defined meanings.
摘要翻译：本发明提供式（I）化合物，其作为p53-MDM2相互作用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n，m，p，s，t， 1，R 2，A和Z具有定义的含义。

7. 发明申请

WO2006032631A1 INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 审中-公开
标题翻译： MDM2和P53之间相互作用的抑制剂
公开(公告)号：WO2006032631A1
公开(公告)日：2006-03-30
申请号：PCT/EP2005/054604
申请日：2005-09-16
申请人： JANSSEN PHARMACEUTICA N.V. , LACRAMPE, Jean, Fernand, Armand , MEYER, Christophe , LIGNY, Yannick, Aimé, Eddy , CSOKA, Imre, Christian, Francis , VAN HIJFTE, Luc , ARTS, Janine , SCHOENTJES, Bruno , WERMUTH, Camille, Georges , GIETHLEN, Bruno , CONTRERAS, Jean-Marie , JOUBERT, Muriel
发明人： LACRAMPE, Jean, Fernand, Armand , MEYER, Christophe , LIGNY, Yannick, Aimé, Eddy , CSOKA, Imre, Christian, Francis , VAN HIJFTE, Luc , ARTS, Janine , SCHOENTJES, Bruno , WERMUTH, Camille, Georges , GIETHLEN, Bruno , CONTRERAS, Jean-Marie , JOUBERT, Muriel
IPC分类号： C07D401/12 , A61K31/4709 , A61P35/00 , A61K31/4439 , C07D401/14 , C07D403/12 , C07D487/04 , C07D413/14 , A61K31/519 , A61K31/501
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X, Y, Q and Z have defined meanings.
摘要翻译：本发明提供式（I）化合物，其作为p53-MDM2相互作用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n，m，p，s，t，R

8. 发明申请

WO2004007498A9 3-PHENYL ANALOGS OF TOXOFLAVINE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的TOXOFLAVINE的3-苯基类似物
公开(公告)号：WO2004007498A9
公开(公告)日：2004-08-12
申请号：PCT/EP0350292
申请日：2003-07-08
申请人： JANSSEN PHARMACEUTICA NV , LACRAMPE JEAN FERNAND ARMAND , CONNORS RICHARD WILLIAM , HO CHIH YUNG , RICHARDSON ALAN , FREYNE EDDY JEAN EDGARD , BUIJNSTERS PETER JACOBUS JOHAN , 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 JOHAN , BAKKER ANNETTE CORNELIA
IPC分类号： A61K31/53 , A61K31/5377 , A61P9/10 , A61P35/00 , A61P43/00 , C07D487/04 , C07D519/00
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 stereo-chemically isomeric forms thereof, wherein n represents an integer being 0, 1 or 2; m represents an integer being 0 or 1; R represents C1-4alkyl; R represents C1-4alkyl; R represents C1-4alkyl; or R and R taken together with the carbon atom to which they are attached form a C3-8cycloalkyl or Het wherein said C3-8cycloalkyl or Het each independently may optionally be substituted with C1-4alkyloxycarbonyl; R represents halo or C1-4alkyloxy; R represents C1-4alkyloxycarbonyl, -O-(mono- or di(C1-4alkyl)aminosulfonyl), C1-4alkyl substituted with one or where possible more substituent being selected from Het or NR R , C1-4alkyloxy substituted with one or where possible more substituents being selected from amino, Het or NR R ; R and R are each independently selected from hydrogen, C1-4alkyl, C1-4alkyloxyC1-4alkyl, -Het or C1-4alkyl substituted with one or where possible more substituents being selected from hydroxy, or Het ; R and R are each independently selected from hydrogen, C1-4alkyl, -Het or mono- or di(C1-4alkyl)aminosulphonyl; Het 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(C1-4 alkyl)aminosulfonyl, hydroxyC1-4alkyloxyC1-4alkyl or C1-4alkyloxy; Het 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 C1-4alkyl, C1-4alkyloxycarbonyl or mono- or di(C1-4alkyl)aminosulfonyl; Het 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(Cl4alkyl)aminosulfonyl; Het represents piperidinyl.
摘要翻译：本发明涉及式（I）的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形式，其中n表示0,1或2的整数; m表示0或1的整数; R 1表示C 1-4烷基; R 2表示C 1-4烷基; R 3代表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C 3-8环烷基或Het 1，其中所述C 3-8环烷基或Het 1各自独立地可任选被C 1 -C 8 - 4alkyloxycarbonyl; R 4代表卤素或C 1-4烷氧基; R 5表示C 1-4烷氧基羰基，-O-（一或二（C 1-4烷基）氨基磺酰基），被一个或可能的更多取代基取代的C 1-4烷基，所述取代基选自Het 3或NR 6 R 6; 被一个或在可能的情况下被选自氨基，Het 4或NR 8 R 9的更多取代基取代的C 1-4烷氧基; R 6和R 7各自独立地选自氢，C 1-4烷基，C 1-4烷氧基C 1-4烷基，-Het 5或被一个或可能的更多取代基取代的C 1-4烷基，所述取代基选自羟基或Het <5>; R 8和R 9各自独立地选自氢，C 1-4烷基，-Het 7或单 - 或二（C 1-4烷基）氨基磺酰基; Het 3代表选自哌啶基或哌嗪基的杂环，其中所述单环杂环各自独立地可任选被一个或任选地两个或三个取代基取代，所述取代基各自独立地选自羟基，氨基磺酰基，氨基，单或二（C1- 4烷基）氨基磺酰基，羟基C1-4烷氧基C1-4烷基或C1-4烷氧基; Het 4代表选自吗啉基，哌啶基或哌嗪基的杂环，其中所述单环杂环各自独立地可任选被一个或在可能的情况下被两个或三个取代基取代，所述取代基各自独立地选自C 1-4烷基，C 1-4烷氧基羰基或一或二（C 1-4烷基）氨基磺酰基; Het 5代表选自吡啶基或哌啶基的杂环，其中所述单环杂环各自独立地可任选地被一个或任选地两个或三个取代基取代，所述取代基各自独立地选自氨基磺酰基或单或二（C 1-4烷基）氨基磺酰基; Het 7代表哌啶基。

9. 发明申请

WO1997049704A1 N-[4-(HETEROARYLMETHYL)PHENYL]-HETEROARYLAMINES 审中-公开
标题翻译： N- [4-（杂芳基）苯基] -HETEROARYLAMINES
公开(公告)号：WO1997049704A1
公开(公告)日：1997-12-31
申请号：PCT/EP1997003248
申请日：1997-06-19
申请人： JANSSEN PHARMACEUTICA N.V. , VENET, Marc, Gaston , MABIRE, Dominique, Jean-Pierre , LACRAMPE, Jean, Fernand, Armand , SANZ, Gérard, Charles
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D417/12
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/04 , C07D513/04
摘要： The present invention is concerned with compounds of formula (I), the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R is hydrogen, hydroxy, C1-6alkyl or aryl; R is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; formula (1) is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.
摘要翻译：本发明涉及式（I）化合物，N-氧化物，其药学上可接受的加成盐和立体化学异构形式，其中R 1是氢，羟基，C 1-6烷基或芳基; R 2是氢; 任选取代的C 1-12烷基; 3-7环烷基; C 2-8烯基，任选取代的吡咯烷基或芳基; R 3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环; 式（1）是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。

10. 发明申请

WO1994013681A1 ANTIALLERGIC TRIAZOLO(PYRROLO, THIENO OR FURANO)AZEPINE DERIVATIVES 审中-公开
标题翻译：抗坏血酸（PYRROLO，THIENO或FURANO）亚胺衍生物
公开(公告)号：WO1994013681A1
公开(公告)日：1994-06-23
申请号：PCT/EP1993003322
申请日：1993-11-25
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , LACRAMPE, Jean, Fernand, Armand , PILATTE, Isabelle, Noelle, Constance
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D495/14
CPC分类号： C07D487/14 , C07D491/14 , C07D495/14
摘要： Antiallergic triazolo(pyrrolo, thieno or furano)azepines of formula (I), the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; -E-G- is a bivalent radical of formula -X-C(R ) CH- (a-1); or -CH C(R )-X- (a-2); X represents O, S or NR ; R represents hydrogen, C1-6alkyl or C1-4alkylcarbonyl; -B D- is a bivalent radical of formula -C(R ) N- (b-1); or -N C(R )- (b-2); L represents hydrogen; C1-6alkyl; substituted C1-6alkyl; C3-6alkenyl; C3-6alkenyl substituted with aryl; or, L represents a radical of formula -Alk-Y-Het (c-1), -Alk-NH-CO-Het (c-2) or -Alk-Het (c-3). Compositions comprising said compounds, processes of preparing the same and intermediates in the preparation thereof.
摘要翻译：式（I）的抗过敏三唑（吡咯，噻吩或呋喃）吖庚因，其药学上可接受的加成盐和立体化学异构形式，其中每个虚线独立地表示任选的键; -E-G-是式-X-C（R 1）符号CH-（a-1）的二价基团。或-CH = C（R 2）-X-（a-2）; X表示O，S或NR 3; R 3表示氢，C 1-6烷基或C 1-4烷基羰基; -B-D是式-C（R 4）符号N-（b-1）的二价基团。或-N-C（R 5） - （b-2）; L表示氢; C1-6烷基; 取代的C 1-6烷基; C3-6alkenyl; 被芳基取代的C 3-6烯基; 或者，L表示式-Alk-Y-Het1（c-1），-Alk-NH-CO-Het2（c-2）或-Alk-Het3（c- 3）。包含所述化合物的组合物，其制备方法及其制备中的中间体。

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