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1. 发明授权

US06867207B2 IL-5 inhibiting 6-azauracil derivatives 失效
标题翻译： IL-5抑制6-氮尿嘧啶衍生物
公开(公告)号：US06867207B2
公开(公告)日：2005-03-15
申请号：US09891888
申请日：2001-06-26
申请人： Jean Fernand Armand Lacrampe , Eddy Jean Edgard Freyne , Marc Gaston Venet , Gustaaf Maria Boeckx
发明人： Jean Fernand Armand Lacrampe , Eddy Jean Edgard Freyne , Marc Gaston Venet , Gustaaf Maria Boeckx
IPC分类号： A61P37/08 , C07D401/10 , C07D403/10 , C07D403/12 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D253/065 , A61K31/53 , A61K17/00
CPC分类号： C07D401/10 , C07D403/10 , C07D403/12 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14
摘要： The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, p and q are 0, 1, 2, 3 or 4 and q is also 5; X is O, S, NR3 or a direct bond; R1 is hydrogen, hydroxy, halo, optionally substituted amino, optionally substituted C1-6alkyl, C1-6alkyloxy, C3-7cycloalkyl or aryl; R2 is aryl, Het1, C3-7cycloalkyl, optionally substituted C1-6alkyl; and if X is O, S or NR3, then R2 may also be a carbonyl or thiocarbonyl linked substituent; R3 is hydrogen or C1-4alkyl; R4 and R5 independently are optionally substituted C1-6alkyl, halo, hydroxy, mercapto, C1-6alkyloxy, C1-6akylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6 or NR7R8; R6 is substituted sulfonyl or sulfinyl; R7 and R8 are hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R9 and R10 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, carboxyl, C1-4alkyloxycarbonyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3 and C(═O)Het3; R12 and R13 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl and R6; aryl is optionally substituted phenyl; Het1, Het2 and Het3 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.
摘要翻译：本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐及其立体化学异构形式，p和q分别为0,1,2,3或4，q也为5; X是O，S，NR 3或直接键; R 1是氢，羟基，卤素，任选取代的氨基，任选取代的C 1-6烷基，C 1-6烷氧基，C 3-7环烷基或芳基; R 2是芳基，Het 1，C 3-7环烷基，任选取代的C 1-6烷基; 并且如果X是O，S或NR 3，则R 2也可以是羰基或硫代羰基连接的取代基; R 3是氢或C 1-4烷基; R 4和R 5独立地是任选取代的C 1-6烷基，卤素，羟基，巯基，C 1-6烷氧基，C 1-6烷硫基，C 1-6烷基羰基氧基，芳基，氰基，硝基，Het 3，或NR 7 R 8; R 6是取代的磺酰基或亚磺酰基; R 7和R 8是氢，任选取代的C 1-4烷基，芳基，羰基或硫代羰基连接的取代基，C 3-7环烷基，Het 3和R 6; R 9和R 10各自独立地选自氢，任选取代的C 1-4烷基，苯基，羰基或硫代羰基连接的取代基，C 3-7环烷基，Het 3和R 6; R 11是羟基，巯基，氰基，硝基，卤素，三卤代甲基，C 1-4烷氧基，羧基，C 1-4烷氧基羰基，三卤代C 1-4烷基磺酰氧基，R 6，NR 7 R 8，C（= O） NR 7 R 8，芳基，芳氧基，芳基羰基，C 3-7环烷基，C 3-7环烷氧基，邻苯二甲酰亚胺-2-基，Het 3和C（= O）Het 3; R 12和R 13各自独立地选自氢，任选取代的C 1-4烷基，苯基，羰基或硫代羰基连接的取代基，C 3-7环烷基和R 6; 芳基是任选取代的苯基; Het <1>，Het <

2. 发明授权

US06894046B2 IL-5 inhibiting 6-azauracil derivatives 失效
公开(公告)号：US06894046B2
公开(公告)日：2005-05-17
申请号：US09812731
申请日：2001-03-19
申请人： Eddy Jean Edgard Freyne , Jean Fernand Armand Lacrampe , Frederik Dirk Deroose , Marc Gaston Venet
发明人： Eddy Jean Edgard Freyne , Jean Fernand Armand Lacrampe , Frederik Dirk Deroose , Marc Gaston Venet
IPC分类号： C07D253/06 , A61K31/53 , A61K31/7028 , A61K31/706 , A61K51/00 , A61P17/00 , A61P27/02 , A61P27/16 , A61P29/00 , A61P37/00 , C07D253/075 , C07D401/10 , C07D403/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07H15/26 , C07D253/07
CPC分类号： C07D253/075 , C07D401/10 , C07D413/10 , C07D417/10 , C07D417/14
摘要： The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 4; X is O, S, NR5 or a direct bond; Y is O, S, NR5 or S(O)2; R1 independently is C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or substituted C1-4alkyl; R2 is Het1, C3-7cycloalkyl or optionally substituted C1-6alkyl and if X is O, S or NR5, then R2 may also represent aminocarbonyl, aminothiocarbonyl, C1-4alkylcarbonyl, C1-4alkylthiocarbonyl, arylcarbonyl, arylthiocarbonyl, Het1carbonyl or Het1thiocarbonyl; R3 and R4 independently are hydrogen, C1-6alkyl or C3-7cycloalkyl; R3 and R4 form a C2-6alkanediyl; R5 is hydrogen or C1-4alkyl; R6 is a sulfonyl or sulfinyl derivative; R7 and R8 are independently hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl containing moiety, C3-7cycloalkyl, —Y—C1-4alkanediyl-C(═O)—O—R14, Het3, Het4 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, formyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, C1-4alkanediyl-C(═O)—O—R14, —C(═O)—O—R14, —Y—C1-4alkanediyl-C(═O)—O—R14, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3 and C(═O)Het3; R14 is hydrogen, C1-4alkyl, C3-7cycloalkyl, aminocarbonylmethylene or mono- or di(C1-4alkyl)aminocarbonylmethylene; aryl is optionally substituted phenyl; Het1, Het2, Het3 and Het4 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

3. 发明授权

US07947694B2 Substituted pyrazolo[3,4-D]pyrimidines as cell cycle kinase inhibitors 有权
标题翻译：取代的吡唑并[3,4-D]嘧啶作为细胞周期激酶抑制剂
公开(公告)号：US07947694B2
公开(公告)日：2011-05-24
申请号：US11813654
申请日：2006-01-09
申请人： Eddy Jean Edgard Freyne , Jean Fernand Armand Lacrampe , Timothy Pietro Suren Perera , Peter Ten Holte , Yannick Aimé Eddy Ligny , Delphine Yvonne Raymonde Lardeau , Tom Lavrijssen
发明人： Eddy Jean Edgard Freyne , Jean Fernand Armand Lacrampe , Timothy Pietro Suren Perera , Peter Ten Holte , Yannick Aimé Eddy Ligny , Delphine Yvonne Raymonde Lardeau , Tom Lavrijssen
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。

4. 发明授权

US06911444B2 Non-steroidal IL-5 inhibitors, processes and intermediates for their preparation and pharmaceutical compositions comprising said inhibitors 失效
标题翻译：非甾体IL-5抑制剂，其制备方法和中间体以及包含所述抑制剂的药物组合物
公开(公告)号：US06911444B2
公开(公告)日：2005-06-28
申请号：US10075876
申请日：2002-02-14
申请人： Jean Fernand Armand Lacrampe , Eddy Jean Edgard Freyne , Frederik Dirk Deroose , Jérôme Michel Claude Fortin , Erwin Coesemans
发明人： Jean Fernand Armand Lacrampe , Eddy Jean Edgard Freyne , Frederik Dirk Deroose , Jérôme Michel Claude Fortin , Erwin Coesemans
IPC分类号： C07D413/10 , A61K31/53 , A61K31/5377 , A61K51/04 , A61P1/02 , A61P1/04 , A61P11/06 , A61P11/08 , A61P15/02 , A61P17/06 , A61P27/02 , A61P27/16 , A61P37/08 , A61P43/00 , C07D417/10 , C07D417/14 , C07D253/075
CPC分类号： A61K51/0491 , A61K51/0461 , A61K51/0463 , A61K51/0468 , C07D417/10 , C07D417/14
摘要： The present invention relates to IL-5 inhibiting 6-azauracil derivatives useful for treating eosinophil-dependent inflammatory diseases, to processes and intermediates for their preparation as well as to pharmaceutical compositions comprising the said derivatives. It further relates to the use of such derivatives as a medicine, and to processes for marking a receptor or imaging an organ using the said derivatives.
摘要翻译：本发明涉及用于治疗嗜酸性粒细胞依赖性炎性疾病的IL-5抑制性6-氮尿嘧啶衍生物，其制备方法和中间体以及包含所述衍生物的药物组合物。它还涉及这样的衍生物作为药物的使用，以及使用所述衍生物标记受体或成像器官的方法。

7. 发明授权

US07241763B2 3-furanyl analogs of toxoflavine as kinase inhibitors 失效
标题翻译：毒素黄嘌呤的3-呋喃基类似物作为激酶抑制剂
公开(公告)号：US07241763B2
公开(公告)日：2007-07-10
申请号：US10520641
申请日：2003-07-08
申请人： Jean Fernand Armand LaCrampe , Richard William Connors , Chih Yung Ho , Alan Richardson , Eddy Jean Edgard Freyne , Peter Jacobus Johannes Buijnsters , Annette Cornelia Bakker
发明人： Jean Fernand Armand LaCrampe , Richard William Connors , Chih Yung Ho , Alan Richardson , Eddy Jean Edgard Freyne , Peter Jacobus Johannes Buijnsters , Annette Cornelia Bakker
IPC分类号： C07D407/04 , C07D487/04 , A61K31/53 , A61P35/00 , A61P19/02
CPC分类号： C07D487/04
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m, n, R1, R2, R3, R4 and R5 are as defined herein, the use of such compounds as inhibitors of cyclin-dependent serine/threonine kinases (Cdks), as well as kinases and phosphatases involved in cell cycle regulation such as the tyrosine kinases Wee1, Mik1 and Myt1 or the tyrosine dephosphatases such as Cdc25 and Pyp3. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating cell proliferative disorders such as atherosclerosis, restenosis and cancer.
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，n，R 1，R 2， R 3，R 4和R 5如本文所定义，使用这些化合物作为细胞周期蛋白依赖性丝氨酸/苏氨酸激酶的抑制剂（Cdks），以及参与细胞周期调节的激酶和磷酸酶，例如酪氨酸激酶Wee1，Mik1和Myt1或酪氨酸脱磷酶如Cdc25和Pyp3。本发明进一步涉及包含本发明化合物的药物组合物和治疗细胞增殖性疾病如动脉粥样硬化，再狭窄和癌症的方法。

8. 发明授权

US06469001B1 IL-5 inhibiting 6-azauracil derivatives 失效
标题翻译： IL-5抑制6-氮尿嘧啶衍生物
公开(公告)号：US06469001B1
公开(公告)日：2002-10-22
申请号：US09856625
申请日：2001-05-22
申请人： Eddy Jean Edgard Freyne , Frederik Dirk Deroose , Davy Petrus Franciscus Maria Petit , Jean Fernand Armand Lacrampe
发明人： Eddy Jean Edgard Freyne , Frederik Dirk Deroose , Davy Petrus Franciscus Maria Petit , Jean Fernand Armand Lacrampe
IPC分类号： C07D253075
CPC分类号： C07D253/075 , C07D417/10
摘要： The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 3; q is 0 to 5; —A—B— is —(CH2)r—, —(CH2)t—O—, —(CH2)t—S(═O)u— or —(CH2)t—NR3—; r is 2 to 4; t is 1 to 3; u is 0 to 2; X1 is O, S, NR3 or a direct bond; R1 and R4 are C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or C1-4alkyl substituted with Het3, R6 or NR7R8; R2 represents aryl, Het1, C3-7cycloalkyl, cyano, C1-6alkyl, —C(═Q)—X2—R15 or C1-6alkyl substituted with one or two substituents selected from hydroxy, cyano, amino, mono- or di(C1-4alkyl)amino, C1-6alkyloxy, C1-6alkylsulfonyloxy, C1-6alkyloxycarbonyl, C3-7cycloalkyl, aryl, aryloxy, arylthio, Het1, Het1 oxy, Het1 thio and —C(═Q)—X2—R15; R3 is hydrogen or C1-4alkyl; R15 is hydrogen, optionally substituted C1-6alkyl, C3-7cycloallcyl, aryl; where X2 is a direct bond, R15 is also halo or Het1; where X2 is NR5, R15 is also hydroxy; where X2 is C(═O)—NH—NH or NH—NH—C(═O), R15 is replaced by R11; R5 is hydrogen, C1-6alkyl, C1-6alkyloxy or arylC1-6alkyl; Q is O, S or NR3; X2 is O, S, NR5, C(═O)—NH—NH, NH—NH—C(═O) or a direct bond; R6 is a sulfonyl or sulfinyl derivative; R7 and R8 are independently hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl containing moiety, C3-7cycloalkyl, —Y—C1-4alkanediyl—C(═O)—O—R14, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, formyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, C1-4alkanediyl—C(═O)—O—R14, —C(═O)—O—R14,. —Y—C1-4alkanediyl—C(═O)—O—R14, aryl, aryloxy, arcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3, Het4 and C(═O)Het3; aryl is optionally substituted phenyl; Het1, Het2, Het3 and Het4 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.
摘要翻译：本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐和立体化学异构形式，其中p为0-3; q为0〜5; -A-B-是 - （CH 2）r - ， - （CH 2）t -O-， - （CH 2）t -S（= O）u - 或 - （CH 2）t -NR 3 - ; r为2〜4; t为1〜3; 你是0到2; X1是O，S，NR3或直接键; R 1和R 4是C 1-6烷基，卤素，多卤代C 1-6烷基，羟基，巯基，C 1-6烷氧基，C 1-6烷硫基，C 1-6烷基羰基氧基，芳基，氰基，硝基，Het 3，R 6，NR 7 R 8或被Het 3，或NR7R8; R 2表示芳基，Het 1，C 3-7环烷基，氰基，C 1-6烷基，-C（= Q）-X 2 -R 15或被一个或两个选自羟基，氰基，氨基，单 - 或二 1-4烷基）氨基，C 1-6烷氧基，C 1-6烷基磺酰氧基，C 1-6烷氧基羰基，C 3-7环烷基，芳基，芳氧基，芳硫基，Het 1，Het 1氧基，Het 1硫基和-C（= Q）-X 2 -R 15; R3是氢或C1-4烷基; R 15是氢，任选取代的C 1-6烷基，C 3-7环烷基，芳基; 其中X2是直接键，R15也是卤素或Het1; 其中X2是NR5，R15也是羟基; 其中X2是C（= O）-NH-NH或NH-NH-C（= O），R15被R11代替; R5是氢，C1-6烷基，

9. 发明授权

US06803364B1 Il-5 inhibiting 6-azauracil derivatives 失效
标题翻译： Il-5抑制6-氮尿嘧啶衍生物
公开(公告)号：US06803364B1
公开(公告)日：2004-10-12
申请号：US09868384
申请日：2001-08-29
申请人： Eddy Jean Edgard Freyne , Frederik Dirk Deroose , Jean Fernand Armand Lacrampe , Werner Constant Johan Embrechts , Jerome Michel Claude Fortin
发明人： Eddy Jean Edgard Freyne , Frederik Dirk Deroose , Jean Fernand Armand Lacrampe , Werner Constant Johan Embrechts , Jerome Michel Claude Fortin
IPC分类号： C07D25306
CPC分类号： C07D253/075 , C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention is concerned with the compounds of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein p is 0 to 4; q is 0 to 5; X is O, S, NR3 or a direct bond; or —X—R2 is CN; R1 is H, OH, halo, NH2, mono- or di(C1-4alkyl)NH2, C1-6alkyl, C1-6alkylO, C3-7cycloalkyl, aryl, arylC1-6alkyl, NH2C1-4akyl, mono- or di(C1-4alkyl)NH2C1-4akyl or mono- or di(C1-4alkyl)NH2C1-4alkylNH2; R2 is aryl, Het1, optionally substituted C3-7cycloalkyl, optionally substituted C1-6alkyl; R3 is H or C1-4alkyl; R4 and R5 are —C(═O)—Z—R14, C1-6alkyl, halo, polyhaloC1-6alkyl, OH, mercapto, C1-6alkylO, C1-6alkylthio, C1-6alkylC(═O)O, aryl, cyano, nitro, Het3, R6, NR7R8 or C1-4alkyl substituted with —C(═O)—Z—R14, Het3, R6 or NR7R8; Z is O, S, NH, —CH2O or —CH2—S—; R14 is H, C1-20acyl, optionally substituted C1-20alkyl, optionally substituted C3-20alkenyl, C3-20alkynyl, C3-7cycloalkyl, polyhaloC1-20alkyl, Het5, phenyl; or R14 is an oxygen containing radical; aryl is optionally substituted phenyl; Het1, Het2, Het3 and Het5 are optionally substituted heterocycles; Het4 is a monocyclic heterocycle; provided however that R2 is other than NH2C(═O), C1-6alkylOC(═O)C1-6alkyl; and R11 is other than COOH, C1-4alkylOC(═O), NH2C(═O), C1-4alkylNH2C(═O), OHC1-4alkylNH2C(═O), C1-4alkylC(═O)NH2C(═O), C3-7cycloalkylNH2C(═O); and R7, R8, R9, R10, R12, R13, R15 and R16 are other than C1-4alkylC(═O)OC1-4alkylC(═O), OHC1-4alkylC(═O); and Het3 is other than a monocyclic heterocycle substituted with COOH or C1-4alkylOC(═O); and the compounds of formula (I) contain at least one —C(═O)—Z—R14 moiety: to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.
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，季胺或其立体化学异构形式，其中p为0至4; q为0〜5; X是O，S，NR 3或直接键; 或-X-R 2为CN; R 1是H，OH，卤素，NH 2，单或二（C 1-4烷基）NH 2，C 1-6烷基，C 1-6烷基O，C 3-7环烷基，芳基，芳基C 1-6烷基，NH 2 C 1-4烷基，单或二（C 1-4烷基）NH 2 C 1-4芳基或单或二（C 1-4烷基）NH 2 C 1-4烷基NH 2; R 2是芳基，Het 1，任选取代的C 3-7环烷基，任选取代的C 1-6烷基; R 3是H或C 1-4烷基; R 4和R 5是-C（= O）-ZR 14，C 1-6烷基，卤素，多卤代C 1-6烷基，OH，巯基，C 1-6烷基O，C 1-6烷硫基，C 1-6烷基C（= O ）O，芳基，氰基，硝基，Het 3，R 6，NR 7 R 8或被-C（= O）-ZR 14，Het 3取代的C 1-4烷基， R 6或NR 7 R 8; Z是O，S，NH，-CH 2 O或-CH 2 -S-; R 14是H，C 1-20酰基，任选取代的C 1-20烷基，任选取代的C 3-20烯基，C 3-20炔基，C 3-7环烷基，多卤代C 1-20烷基，Het 5，苯基; 或R 14是含氧基团; 芳基是任选取代的苯基; Het 1，Het 2，Het 3和Het 5是任选取代的杂环; Het 4是单环杂环; 但是R 2不是NH

10. 发明授权

US06498158B1 Il-5 inhibiting 6-azauracil derivatives 失效
标题翻译： Il-5抑制6-氮尿嘧啶衍生物
公开(公告)号：US06498158B1
公开(公告)日：2002-12-24
申请号：US09856626
申请日：2001-05-22
申请人： Jean Fernand Armand Lacrampe , Yannick Ligny , Eddy Jean Edgard Freyne , Frederik Dirk Deroose
发明人： Jean Fernand Armand Lacrampe , Yannick Ligny , Eddy Jean Edgard Freyne , Frederik Dirk Deroose
IPC分类号： C07D253075
CPC分类号： C07D253/075 , C07D405/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14
摘要： The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 3; q is 0 to 4; —A—B— represents —(CH2)r—, —(CH2)t—O—, —(CH2)t—S(═O)u— or —(CH2)t—NR3—; r is 2 to 4; t is 1 to 3; u is 0 to 2; X1 is O, S, NR3 or a direct bond; R1 and R4 are C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or substituted C1-4alkyl; R2 is aryl, Het1, C3-7cycloalkyl, cyano, optionally substituted C1-6alkyl, —C(═Q)—X2—R15; R3 is hydrogen or C1-4alkyl; R15 is hydrogen, optionally substituted C1-6alkyl, C3-7cycloalkyl, aryl; where X2 is a direct bond, R15 may also be halo or Het1; where X2 is NR5, R15 may also be hydroxy; where X2 is C(═O)—NH—NH or NH—NH—C(═O), R15 may be replaced by R11; Q is O, S or NR3; X2 is O, S, NR5, C(═O)—NH—NH, NH—NH—C(═O) or a direct bond; R5 is hydrogen, C1-6alkyl, C1-6alkyloxy or arylC1-6alkyl; R6 is a sulfonyl or sulfinyl derivative; R7 and R8 are independently hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl containing moiety, C3-7cycloalkyl, —Y-C1-4alkanediyl-C(═O)—O—R14, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, formyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, C1-4alkanediyl-C(═O)—O—R14, —C(═O)—O—R14, —Y-C1-4alkanediyl-C(═0)—O—R14, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3, Het4 and C(═O)Het3; aryl is optionally substituted phenyl; Het1, Het2, Het3 and Het4 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.
摘要翻译：本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐和立体化学异构形式，其中p为0-3; q为0〜4; -A-B-表示 - （CH 2）r - ， - （CH 2）t -O-， - （CH 2）t -S（= O）u - 或 - （CH 2）t -NR 3 - ; r为2〜4; t为1〜3; 你是0到2; X1是O，S，NR3或直接键; R 1和R 4是C 1-6烷基，卤素，多卤代C 1-6烷基，羟基，巯基，C 1-6烷氧基，C 1-6烷硫基，C 1-6烷基羰氧基，芳基，氰基，硝基，Het 3，R 6，NR 7 R 8或取代的C 1-4烷基; R 2是芳基，Het 1，C 3-7环烷基，氰基，任选取代的C 1-6烷基，-C（= Q）-X 2 -R 15; R3是氢或C1-4烷基; R 15是氢，任选取代的C 1-6烷基，C 3-7环烷基，芳基; 其中X2是直接键，R15也可以是卤素或Het1; 其中X2是NR5，R15也可以是羟基; 其中X 2是C（= O）-NH-NH或NH-NH-C（= O），R 15可以被R 11取代; Q是O，S或NR 3; X2是O，S，NR5，C（= O）-NH-NH，NH-NH-C（= O）或直接键; R5是氢，C1-6烷基，C1-6烷氧基或芳基C1-6烷基; R6是磺酰基或亚磺酰基衍生物; R 7和R 8独立地为氢，任选取代的C 1-4烷基，芳基，含羰基部分，C 3-7环烷基，-Y-C 1-4烷二基-C（= O）-O-R 14，Het 3

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