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1. 发明授权

US07138403B2 2,4,5-trisubstituted thiazolyl derivatives and their antiinflammatory activity 有权
标题翻译： 2,4,5-三取代噻唑衍生物及其抗炎活性
公开(公告)号：US07138403B2
公开(公告)日：2006-11-21
申请号：US10486820
申请日：2002-08-09
申请人： Christopher John Love , Jean Pierre Frans Van Wauwe , Marc J. De Brabander , Roger Clive Moses , Mykhalyo Goncharenko , Ludwig Paul Cooymans , Nele Vandermaesen , Gaston Stanislas Marcella Diels , Anthony William Sibley , Caterina Noula
发明人： Christopher John Love , Jean Pierre Frans Van Wauwe , Marc J. De Brabander , Roger Clive Moses , Mykhalyo Goncharenko , Ludwig Paul Cooymans , Nele Vandermaesen , Gaston Stanislas Marcella Diels , Anthony William Sibley , Caterina Noula
IPC分类号： C07D239/24 , A61K31/495
CPC分类号： C07D417/04 , C07D277/28 , C07D417/14
摘要： This invention concerns the use of a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl or C1-6alkyloxy; polyhaloC1-4alkyl; C1-4alkyloxy; cyano; amino; aminocarbonyl; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; H2N—S(═O)2—; mono- or di(C1-6alkyl)amino-S(═O)2; —C(═N—Rx)NRyRz; Q is an optionally substituted carbocycle or an optionally substituted heterocycle; L is substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through TNF-α and/or IL-12.
摘要翻译：本发明涉及式（I）化合物的N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构体形式的用途，其中Z为卤素; C 1-6烷基; 被羟基，羧基，氰基，氨基，一或二（C 1-6烷基）氨基，氨基羰基，一或二（C（C 1-6）烷基）氨基取代的C 1-6烷基 C 1-6烷基）氨基羰基，C 1-6烷氧基羰基或C 1-6烷基氧基; 多卤代1-4烷基; C 1-4烷氧基; 氰基; 氨基; 氨基羰基; 单或二（C 1-6烷基）氨基羰基; C 1-6烷氧基羰基; C 1-6烷基羰基氧基; H 2 -N-S（-O）2 - ; 单或二（C 1-6烷基）氨基-S（-O）2; -C（-N-R x X）NR z R z Z; Q是任选取代的碳环或任选取代的杂环; L是取代的苯基或任选取代的单环5或6元部分饱和或芳族杂环或双环部分饱和或芳族杂环; 芳基是任选取代的苯基; 用于制备用于预防或治疗通过TNF-α和/或IL-12介导的疾病的药物。

2. 发明授权

US06951857B2 6-Azauracil derivatives as IL-5 inhibitors 失效
公开(公告)号：US06951857B2
公开(公告)日：2005-10-04
申请号：US10434896
申请日：2003-05-09
申请人： Eddy Jean Edgard Freyne , Gustaaf Maria Boeckx , Jean Pierre Frans Van Wauwe , Gaston Stanislas Marcella Diels
发明人： Eddy Jean Edgard Freyne , Gustaaf Maria Boeckx , Jean Pierre Frans Van Wauwe , Gaston Stanislas Marcella Diels
IPC分类号： C07D253/06 , A61K31/53 , A61K51/00 , A61K51/04 , A61P11/06 , A61P17/00 , A61P27/02 , A61P27/14 , A61P37/08 , A61P43/00 , C07D253/075 , C07D403/10 , C07D417/10
CPC分类号： A61K51/0491 , A61K31/53 , A61K51/04 , A61K51/0461 , C07D253/075 , C07D403/10 , C07D417/10
摘要： The present invention is concerned with the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p represents 0, 1, 2 or 3; q represents 0, 1, 2, 3 or 4; R1 represents hydrogen, C1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, mercapto, C1-6alkylthio, C3-7cycloalkyl, aryl or C1-6alkyl substituted with mono- or di(C1-6alkyl)amino, C1-6alkyloxy, aryl or Het; R2 represents cyano or a radical of formula —C(═X)—Y—R5; wherein X represents O or S; Y represents O, S, NR6 or a direct bond; R5 represents hydrogen; C3-7cycloalkyl; aryl or optionally substituted C1-6alkyl; and where Y is a direct bond, R5 may also be halo or Het; R3 and R4 each independently represents halo, haloC1-6alkyl, C1-6alkyl, hydroxy, C1-6alkyloxy, C1-6alkylcarbonyloxy, mercapto, C1-6alkylthio, C1-6alkylsulfonyl, C1-6alkylsulfinyl, haloC1-6alkylsulfonyl, aryl, cyano, nitro, amino, mono- and di(C1-6alkyl)amino or (C1-6alkylcarbonyl)amino; aryl represents phenyl or substituted phenyl; and Het represents an optionally substituted heterocycle; in the manufacture of a medicament useful for treating eosinophil-dependent inflammatory diseases. The invention also relates to novel compounds, their preparation and compositions comprising them.

3. 发明授权

US06743792B2 6-azauracil derivatives as IL-5 inhibitors 失效
标题翻译： 6-氮尿嘧啶衍生物作为IL-5抑制剂
公开(公告)号：US06743792B2
公开(公告)日：2004-06-01
申请号：US09855068
申请日：2001-05-14
申请人： Eddy Jean Edgard Freyne , Gustaaf Maria Boeckx , Jean Pierre Frans Van Wauwe , Gaston Stanislas Marcella Diels
发明人： Eddy Jean Edgard Freyne , Gustaaf Maria Boeckx , Jean Pierre Frans Van Wauwe , Gaston Stanislas Marcella Diels
IPC分类号： C07D253075
CPC分类号： A61K51/0491 , A61K31/53 , A61K51/04 , A61K51/0461 , C07D253/075 , C07D403/10 , C07D417/10
摘要： The present invention is concerned with the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p represents 0, 1, 2 or 3; q represents 0, 1, 2, 3 or 4; R1 represents hydrogen, C1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, mercapto, C1-6alkylthio, C3-7cycloalkyl, aryl or C1-6alkyl substituted with mono- or di(C1-6alkyl)-amino, C1-6alkyloxy, aryl or Het; R2 represents cyano or a radical of formula —C(═X)—Y—R5; wherein X represents O or S; Y represents O, S, NR6 or a direct bond; R5 represents hydrogen; C3-7cycloalkyl; aryl or optionally substituted C1-6alkyl; and where Y is a direct bond, R5 may also be halo or Het; R3 and R4 each independently represents halo, haloC1-6alkyl, C1-6alkyl, hydroxy, C1-6alkyloxy, C1-6alkylcarbonyloxy, mercapto, C1-6alkylthio, C1-6alkylsulfonyl, C1-6alkylsulfinyl, haloC1-6alkylsulfonyl, aryl, cyano, nitro, amino, mono- and di(C1-6alkyl)amino or (C1-6alkylcarbonyl)amino; aryl represents phenyl or substituted phenyl; and Het represents an optionally substituted heterocycle; in the manufacture of a medicament useful for treating eosinophil-dependent inflammatory diseases. The invention also relates to novel compounds, their preparation and compositions comprising them.
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，其中p代表0,1,2或3; q表示0,1,2,3或4; R 1表示氢，C 1-6烷基，一或二（C 1-6烷基）氨基C 1-6烷氧基，巯基，C 1-6烷硫基，C 3-7环烷基，芳基或被单或二（C 1-6烷基）氨基，C 1-6烷氧基，芳基或Het; R 2表示氰基或式-C（= X）-Y-R 5的基团; 其中X表示O或S; Y表示O，S，NR 6或直接键; R 5表示氢; C 3-7环烷基; 芳基或任选取代的C 1-6烷基; 并且其中Y是直接键，R 5也可以是卤素或Het; R 3和R 4各自独立地表示卤素，卤代C 1-6烷基，C 1-6烷基，羟基，C 1-6烷氧基，C 1-6烷基羰氧基，巯基，C 1-6烷硫基，C 1-6烷基磺酰基，C 1-6烷基亚磺酰基，卤代C 1-6烷基磺酰基，芳基，氰基，硝基，氨基，单和二（C 1-6烷基）氨基或（C 1-6烷基羰基）氨基; 芳基表示苯基或取代的苯基; 并且Het表示任选取代的杂环; 在制备可用于治疗嗜酸性粒细胞依赖性炎性疾病的药物中。本发明还涉及新化合物，其制备方法和包含它们的组合物。

4. 发明授权

US07514445B2 Heteroaryl amines as glycogen synthase kinase 3β inhibitors (GSK3 inhibitors) 有权
标题翻译：杂芳基胺作为糖原合酶激酶3β抑制剂（GSK3抑制剂）
公开(公告)号：US07514445B2
公开(公告)日：2009-04-07
申请号：US10493452
申请日：2002-10-29
申请人： Eddy Jean Edgard Freyne , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Werner Constant Johan Embrechts , Christopher John Love , Paul Adriaan Jan Janssen , Paulus Joannes Lewi , Jan Heeres , Marc René de Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Koen Jeanne Alfons Van Aken , Gaston Stanislas Marcella Diels
发明人： Eddy Jean Edgard Freyne , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Werner Constant Johan Embrechts , Christopher John Love , Paul Adriaan Jan Janssen , Paulus Joannes Lewi , Jan Heeres , Marc René de Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Koen Jeanne Alfons Van Aken , Gaston Stanislas Marcella Diels
IPC分类号： A61K31/506 , A61P3/10 , A61P25/28 , A61P25/02 , C07D403/06 , C07D403/12 , C07D403/14
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 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; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21—C1-6alkyl; R21—O—; R21—S—; R21—C(═O)—; R21—S(═O)p—; R7—S(═O)p—; R7—S(═O)p—NH—; R21—S(═O)p—NH—; R7—C(═O)—; —NHC(═O)H; —C(═O)NHNH2; R7—C(═O)—NH—; R21—C(═O)—NH—; —C(═NH)R7—C(═NH)R21; R4 is an optionally substituted heterocycle provided that —X—R2 and/or R3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.
摘要翻译：本发明涉及式的化合物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是6-元杂环; R1是氢; 芳基; 甲酰基 C 1-6烷基羰基; 任选取代的C 1-6烷基; C 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是直接键或连接原子或基团; Z是直接键或连接原子或基团; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，所述基团中的每一个可任选被取代; R3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; C 1-6烷氧基; C 1-6烷硫基; C 1-6烷氧基羰基; C 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C 1-6烷基; 多卤代C 1-6烷氧基; 多卤代C 1-6烷硫基; R21; R21-C1-6烷基; R21-O-; R21-S-; R21-C（-O） - ; R21-S（-O）p-; R7-S（-O）p-; R7-S（-O）p-NH-; R21-S（-O）p-NH-; R7-C（-O） - ; -NHC（-O）H; -C（-O）NHNH 2; R7-C（-O）-NH-; R 21 -C（-O）-NH-; -C（ - NH）R 7 -C（-NH）R 21; R4是任选取代的杂环，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。

5. 发明授权

US08318731B2 Pyrrolopyrimidines 有权
标题翻译：吡咯并嘧啶
公开(公告)号：US08318731B2
公开(公告)日：2012-11-27
申请号：US12670670
申请日：2008-07-25
申请人： Gaston Stanislas Marcella Diels , Peter Ten Holte , Eddy Jean Edgard Freyne , Thierry Andre Regis Grand-Perret , Kristof Van Emelen , Werner Constant Johan Embrechts , Pascal Ghislain André Bonnet
发明人： Gaston Stanislas Marcella Diels , Peter Ten Holte , Eddy Jean Edgard Freyne , Thierry Andre Regis Grand-Perret , Kristof Van Emelen , Werner Constant Johan Embrechts , Pascal Ghislain André Bonnet
IPC分类号： C07D487/08 , C07D498/08 , A61K31/529 , A61P35/02
CPC分类号： C07D498/08 , C07D487/08
摘要： The present invention relates to compounds or pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to compounds that are polo-like kinase (PLKs) inhibitors useful for the treatment of disease states mediated by PLK, especially PLK4, in particular such compounds that are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.
摘要翻译：本发明涉及其化合物或药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途。本发明特别涉及可用于治疗由PLK，特别是PLK4介导的疾病状态的polo样激酶（PLK）抑制剂的化合物，特别是可用于治疗涉及异常细胞增殖的病理过程的此类化合物，如肿瘤生长，类风湿关节炎，再狭窄和动脉粥样硬化。

6. 发明申请

US20100190786A1 INDOLIN-2-ONES AND AZA-INDOLIN-2-ONES 有权
标题翻译：吲哚-2-ONES和AZA-INDOLIN-2-ONES
公开(公告)号：US20100190786A1
公开(公告)日：2010-07-29
申请号：US12663158
申请日：2008-06-20
申请人： Gaston Stanislas Marcella Diels , Marc Gustaaf Celine Verdonck , Peter Jacobus Johannes Antonius Buijnsters , Kristof Van Emelen
发明人： Gaston Stanislas Marcella Diels , Marc Gustaaf Celine Verdonck , Peter Jacobus Johannes Antonius Buijnsters , Kristof Van Emelen
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/529 , C07D498/18 , A61P19/02 , A61P35/04
CPC分类号： C07D209/34 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds or pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to certain indolin-2-ones and aza-indolin-2-ones which possess anti-tumour activity and are accordingly useful in methods of treatment of the human or animal body, in particular such compounds are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.
摘要翻译：本发明涉及其化合物或药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途。本发明特别涉及具有抗肿瘤活性的某些二氢吲哚-2-酮和氮杂 - 二氢吲哚-2-酮，因此可用于人或动物体的治疗方法，特别是这些化合物可用于治疗涉及异常细胞增殖的病理过程，例如肿瘤生长，类风湿性关节炎，再狭窄和动脉粥样硬化。

7. 发明授权

US07410970B2 Substituted 1,4,-di-piperidin-4-yl-piperazine derivatives and their use as neurokinin antagonists 失效
标题翻译：取代的1,4-二 - 哌啶-4-基 - 哌嗪衍生物及其作为神经激肽拮抗剂的用途
公开(公告)号：US07410970B2
公开(公告)日：2008-08-12
申请号：US10527821
申请日：2003-10-07
申请人： Frans Eduard Janssens , François Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts , Yves Emiel Maria Van Roosbroeck , Gaston Stanislas Marcella Diels
发明人： Frans Eduard Janssens , François Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts , Yves Emiel Maria Van Roosbroeck , Gaston Stanislas Marcella Diels
IPC分类号： A61K31/496 , A61K31/497 , C07D401/00 , C07D403/00 , C07D403/14 , C07D405/00 , C07D409/00
CPC分类号： C07D401/14 , C07D211/58 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The invention concerns substituted 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of emesis, anxiety, depression, pain, pancreatitis and IBS.
摘要翻译：本发明涉及具有神经激肽拮抗活性的取代的1,4-二哌啶-4-基 - 哌嗪衍生物，特别是NK 1拮抗活性，其制备方法，包含它们的组合物及其作为药物的用途，特别是用于治疗呕吐，焦虑，抑郁，疼痛，胰腺炎和IBS。

8. 发明授权

US5952510A 1,3-dihydro-1-(phenylalkenyl)-2H-imidazol-2-one derivatives having PDE IV and cytokine inhibiting activity 失效
标题翻译：具有PDE IV和细胞因子抑制活性的1,3-二氢-1-（苯基烯基）-2H-咪唑-2-酮衍生物
公开(公告)号：US5952510A
公开(公告)日：1999-09-14
申请号：US945849
申请日：1997-09-30
申请人： Eddy Jean Edgard Freyne , Gaston Stanislas Marcella Diels , Jose Ignacio Andres-Gil , Francisco Javier Fernandez-Gadea
发明人： Eddy Jean Edgard Freyne , Gaston Stanislas Marcella Diels , Jose Ignacio Andres-Gil , Francisco Javier Fernandez-Gadea
IPC分类号： A61K31/415 , A61K31/4166 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07D233/32 , C07D233/38 , C07D233/70
CPC分类号： C07D233/32 , C07D233/70
摘要： The present invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; difluoromethyl; trifluoromethyl; C.sub.3-6 cycloalkyl; a saturated 5-, 6 or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo�2.2.1!-2-heptenyl; bicyclo�2.2.1!heptanyl; C.sub.1-6 alkylsulfonyl; arylsulfonyl; or substituted C.sub.1-10 alkyl; R.sup.3 is hydrogen, halo or C.sub.1-6 alkyloxy; R.sup.4 is hydrogen; cyano; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkyloxycarbonyl or aryl; R.sup.5 is hydrogen; cyano; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkyloxycarbonyl or aryl; Y is a direct bond or C.sub.1-3 alkanediyl; --A--B-- is a bivalent radical of formula --CR.sup.6 .dbd.CR.sup.7 -- or --CHR.sup.6 --CHR.sup.7 --; L is hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; C.sub.1-6 alkyloxycarbonyl; C.sub.1-6 alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het is morpholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl;, -furanyl or -thienyl; having PDE IV and cytokine inhibiting activity. Further, pharmaceutical compositions, preparations and use as a medicine are described.
摘要翻译： PCT No.PCT / EP96 / 01395 Sec。 371日期：1997年9月30日 102（e）1997年9月30日PCT PCT 1996年3月28日PCT公布。 WO96 / 31486 PCT公开号日期：1996年10月10日本发明涉及N-氧化物形式的化合物，其药学上可接受的酸或碱加成盐及其立体化学异构形式，其中R 1和R 2各自独立地为氢; C 1-6烷基; 二氟甲基三氟甲基 C 3-6环烷基; 含有一个或两个选自氧，硫或氮的杂原子的饱和的5-，6-或7-元杂环; 茚满基双环[2.2.1] -2-庚烯基; 双环[2.2.1]庚基; C 1-6烷基磺酰基; 芳基磺酰基; 或取代的C 1-10烷基; R3是氢，卤素或C1-6烷氧基; R4是氢; 氰基; 任选取代的C 1-6烷基; C 1-6烷氧基羰基或芳基; R5是氢; 氰基; 任选取代的C 1-6烷基; C 1-6烷氧基羰基或芳基; Y是直接键或C1-3烷二基; -A-B-是式-CR6 = CR7-或-CHR6-CHR7-的二价基团; L是氢; 任选取代的C 1-6烷基; C 1-6烷基羰基; C 1-6烷氧基羰基; C 1-6烷基磺酰基或芳基磺酰基; 芳基是任选取代的苯基; 哌嗪基，呋喃基或噻吩基;吗啉基或任选取代的哌啶基，哌嗪基，具有PDE IV和细胞因子抑制活性。此外，描述了作为药物的药物组合物，制剂和用途。

9. 发明授权

US08338422B2 Indolin-2-ones and aza-indolin-2-ones 有权
标题翻译：二氢吲哚-2-酮和氮杂 - 二氢吲哚-2-酮
公开(公告)号：US08338422B2
公开(公告)日：2012-12-25
申请号：US12663158
申请日：2008-06-20
申请人： Gaston Stanislas Marcella Diels , Marc Gustaaf Celine Verdonck , Peter Jacobus Johannes Antonius Buijnsters , Kristof Van Emelen
发明人： Gaston Stanislas Marcella Diels , Marc Gustaaf Celine Verdonck , Peter Jacobus Johannes Antonius Buijnsters , Kristof Van Emelen
IPC分类号： C07D209/34 , C07D471/04 , C07D487/04 , A61K31/404 , A61K31/407 , A61P35/00
CPC分类号： C07D209/34 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds or pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to certain indolin-2-ones and aza-indolin-2-ones which possess anti-tumor activity and are accordingly useful in methods of treatment of the human or animal body, in particular such compounds are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.
摘要翻译：本发明涉及其化合物或药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途。本发明特别涉及具有抗肿瘤活性的某些二氢吲哚-2-酮和氮杂 - 二氢吲哚-2-酮，因此可用于人或动物体的治疗方法，特别是这些化合物可用于治疗涉及异常细胞增殖的病理过程，例如肿瘤生长，类风湿性关节炎，再狭窄和动脉粥样硬化。

10. 发明申请

US20100105668A1 Quinazoline derivatives 有权
标题翻译：喹唑啉衍生物
公开(公告)号：US20100105668A1
公开(公告)日：2010-04-29
申请号：US12624637
申请日：2009-11-24
申请人： Eddy Jean Edgard Freyne , Timothy Pietro Suren Perera , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Gaston Stanislas Marcella Diels , Werner Constant Johan Embrechts , Peter ten Holte , Frederik Jan Rita Rombouts , Carsten Schultz-Fademrecht
发明人： Eddy Jean Edgard Freyne , Timothy Pietro Suren Perera , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Gaston Stanislas Marcella Diels , Werner Constant Johan Embrechts , Peter ten Holte , Frederik Jan Rita Rombouts , Carsten Schultz-Fademrecht
IPC分类号： A61K31/541 , C07D239/70 , A61K31/517 , C07D413/02 , A61K31/5377 , C07D417/02 , C07C211/00 , C07D239/72
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 wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl-, —O—N═CH— or —C1-2alkyl-; R1 and R2 are hydrogen or halo; R3 are hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 are hydrogen or C1-4alkyl; R14 and R15 are hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 are hydrogen or C1-4alkyl optionally substituted with phenyl or hydroxy; R20 and R21 are hydrogen or C1-4alkyl optionally substituted with C1-4alkyloxy; Het20, Het21 and Het22 are a heterocycle selected from the group consisting pyrrolidinyl, 2-pyrrolidinonyl or piperidinyl optionally substituted with hydroxy.
摘要翻译：本发明涉及下式的化合物其中Z代表NH; Y代表任选被氨基，一或二（C 1-4烷基）氨基或C 1-4烷氧基羰基氨基 - ， - C 3-7烯基-CO-的氨基取代的-C 3-9烷基 - ， - C 2-9烯基 - ， - 氨基，一或二（C 1-4烷基）氨基 - 或C 1-4烷氧基羰基氨基 - ，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 1-6烷基-CO-NH - ， - C 1-5烷基-CO NR 15 -C 1-5烷基 - ， - C 1-3烷基-NH-CO-Het 20 - ， - C 1-2烷基-CO-Het 21 -CO-， - C 1-2烷基 -NH-CO-CR16R17-NH-，-C1-2烷基-CO-NH-CR18R19-CO-，-C1-2烷基-CO-NR20-C1-3烷基-CO-或-NR22-CO-C1-3烷基 - NH-; X1表示直接键，O或-O-C 1-2烷基 - ; -X 2表示直接键，-CO-C 1-2烷基 - ，NR 12，-NR 12 -C 1-2烷基 - ， - O-N = CH-或-C 1-2烷基 - ; R1和R2是氢或卤素; R3是氢; R4代表氢或C1-4烷氧基; R 12和R 13是氢或C 1-4烷基; R14和R15是氢; R 16和R 17各自独立地表示氢或C 1-4烷基; R 18和R 19是氢或任选被苯基或羟基取代的C 1-4烷基; R 20和R 21是氢或任选被C 1-4烷氧基取代的C 1-4烷基; Het20，Het21和Het22是选自吡咯烷基，2-吡咯烷基或任选被羟基取代的哌啶基的杂环。

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