专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20080139568A1 Phthalazine Derivatives as Parp Inhibitors 有权
标题翻译：酞嗪衍生物作为抑制剂
公开(公告)号：US20080139568A1
公开(公告)日：2008-06-12
申请号：US11569889
申请日：2005-06-28
申请人： Laurence Anne Mevellec , Ludo Edmond Josephine Kennis , Josephus Carolus Mertens , Jacobus Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
发明人： Laurence Anne Mevellec , Ludo Edmond Josephine Kennis , Josephus Carolus Mertens , Jacobus Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
IPC分类号： A61K31/502 , C07D403/02
CPC分类号： A61K31/55 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/542 , C07D237/34 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D417/14 , C07D451/04 , C07D471/04 , C07D513/04
摘要： The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2 L1, L2, X, Y, Q and Z have defined meanings.
摘要翻译：本发明提供式（I）化合物，它们作为PARP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R 1，R 2，L 2 L 2，L 2，X，Y，Q和Z具有定义的含义。

2. 发明授权

US5688799A 9-Hydroxy-pyrido�1,2-a!pyrimidin-4-one ether derivatives 失效
标题翻译： 9-羟基 - 吡啶并[1,2-a]嘧啶-4-酮醚衍生物
公开(公告)号：US5688799A
公开(公告)日：1997-11-18
申请号：US637754
申请日：1996-03-03
申请人： Jan Vandenberk , Ludo Edmond Josephine Kennis
发明人： Jan Vandenberk , Ludo Edmond Josephine Kennis
IPC分类号： A61K31/505 , A61K31/519 , A61P1/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D471/04 , C07D221/00 , C07D239/00
CPC分类号： C07D471/04
摘要： The present invention is concerned with novel compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof and the stereochemically isomeric forms thereof, wherein Alk represents C.sub.1-4 alkanediyl; D is a bicyclic heterocycle of formula ##STR2## wherein each R.sup.1 independently is C.sub.2-6 alkenyl; C.sub.2-6 alkynyl; C.sub.3-6 cycloalkyl optionally substituted with C.sub.1-4 alkyl; C.sub.1-19 alkyl optionally substituted with C.sub.3-6 cycloalkyl, halo, C.sub.1-6 alkyloxy or cyano; and each R.sup.2 independently is hydrogen or C.sub.1-4 alkyl. Novel compounds; compositions; processes for preparing novel compounds and intermediates are described.
摘要翻译： PCT No.PCT / EP94 / 03804 Sec。 371日期：1996年5月3日 102（e）日期1996年5月3日PCT 1994年11月16日PCT公布。 WO95 / 14691 PCT出版物日期：1995年6月1日本发明涉及具有式（I）的药学上可接受的酸加成盐和其立体化学异构形式的新化合物，其中Alk表示C1-4烷二基; D是式（a）或C 2-6烯基的双环杂环; C 2-6炔基; 任选被C 1-4烷基取代的C 3-6环烷基; 任选被C 3-6环烷基，卤素，C 1-6烷氧基或氰基取代的C 1-19烷基; 并且每个R 2独立地是氢或C 1-4烷基。新型化合物组成; 描述了制备新化合物和中间体的方法。

3. 发明申请

US20170022181A1 FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：快速分解多巴胺2受体拮抗剂
公开(公告)号：US20170022181A1
公开(公告)日：2017-01-26
申请号：US15264185
申请日：2016-09-13
申请人： Marcel Frans Leopold De Bruyn , Gregor James Macdonald , Ludo Edmond Josephine Kennis , Xavier Jean Michel Langlois , Frans Alfons Maria Van den Keytus , Yves Emiel Maria Van Roosbroeck
发明人： Marcel Frans Leopold De Bruyn , Gregor James Macdonald , Ludo Edmond Josephine Kennis , Xavier Jean Michel Langlois , Frans Alfons Maria Van den Keytus , Yves Emiel Maria Van Roosbroeck
IPC分类号： C07D401/12 , C07D409/14
CPC分类号： C07D401/12 , A61K31/501 , C07D409/14
摘要： The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
摘要翻译：本发明涉及快速解离多巴胺2受体拮抗剂，制备这些化合物的方法，包含这些化合物作为活性成分的药物组合物。该化合物可用作治疗或预防中枢神经系统疾病（例如精神分裂症）的药物，通过发挥抗精神病作用而没有运动副作用。

4. 发明授权

US08623872B2 Quinazolinone derivatives as PARP inhibitors 有权
标题翻译：喹唑啉酮衍生物作为PARP抑制剂
公开(公告)号：US08623872B2
公开(公告)日：2014-01-07
申请号：US11569892
申请日：2005-06-28
申请人： Jérôme Emile Georges Guillemont , Ludo Edmond Josephine Kennis , Josephus Carolus Mertens , Jacobus Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
发明人： Jérôme Emile Georges Guillemont , Ludo Edmond Josephine Kennis , Josephus Carolus Mertens , Jacobus Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
IPC分类号： A61K31/497 , C07D239/72
CPC分类号： C07D403/12 , A61K31/517 , A61K45/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, L, X, Y and Z have defined meanings.
摘要翻译：本发明提供式（I）化合物，它们作为PARP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R1，R2，R3，L，X，Y和Z具有定义的含义。

5. 发明授权

US08080557B2 Quinazolinedione derivatives as PARP inhibitors 有权
标题翻译：喹唑啉二酮衍生物作为PARP抑制剂
公开(公告)号：US08080557B2
公开(公告)日：2011-12-20
申请号：US11569948
申请日：2005-06-28
申请人： Ludo Edmond Josephine Kennis , Josephus Carolus Mertens , Jacbous Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
发明人： Ludo Edmond Josephine Kennis , Josephus Carolus Mertens , Jacbous Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
IPC分类号： A61K31/517 , A61K31/519 , C07D239/72
CPC分类号： C07D401/04 , A61K31/517 , A61K45/06 , C07D401/06 , C07D401/14 , C07D403/12 , C07D405/14
摘要： The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, L1, L2, X, Y and Z have defined meanings.
摘要翻译：本发明提供式（I）化合物，它们作为PARP抑制剂的用途以及包含其中R1，L1，L2，X，Y和Z具有定义含义的式（I）化合物的药物组合物。

6. 发明授权

US07893280B2 2,4-disubstituted thiazolyl derivatives 有权
标题翻译： 2,4-二取代噻唑衍生物
公开(公告)号：US07893280B2
公开(公告)日：2011-02-22
申请号：US11435335
申请日：2006-05-16
申请人： Christopher Love , Jean Pierre Frans Van Wauwe , Marc De Brabander , Ludwig Cooymans , Nele Vandermaesen , Ludo Edmond Josephine Kennis
发明人： Christopher Love , Jean Pierre Frans Van Wauwe , Marc De Brabander , Ludwig Cooymans , Nele Vandermaesen , Ludo Edmond Josephine Kennis
IPC分类号： A61K31/425 , C07D207/00
CPC分类号： C07D417/04 , C07D277/42 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： This invention concerns the use of a compound of formula (I′) a N-oxide, pharmaceutically acceptable addition salt, quaternary amine and stereochemically isomeric form thereof, wherein Q is optionally substituted C3-6cycloalkyl, phenyl, naphthyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl; or Q is a radical of formula wherein X and Y each independently are O, NR3, CH2 or S, with R3 being hydrogen or C1-4alkyl; q is 1 to 4; Z is O or NR4 with R4 being hydrogen or C1-4alkyl; r is 1 to 3; L is optionally substituted phenyl or L is Het with Het being an optionally substituted five- or six-membered heterocyclic ring or an optionally substituted bicyclic heterocyclic ring; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through cytokines.
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形式的用途，其中Q是任选取代的C 3-6环烷基，苯基，萘基，吡啶基，嘧啶基，吡嗪基，哒嗪基，苯并噻唑基，苯并恶唑基，苯并咪唑基，吲唑基或咪唑并吡啶基; 或Q是下式的基团，其中X和Y各自独立地是O，NR 3，CH 2或S，其中R 3是氢或C 1-4烷基; q为1〜4; Z是O或NR4，其中R4是氢或C1-4烷基; r为1〜3; L是任选取代的苯基或L是Het，Het是任选取代的五元或六元杂环或任选取代的双环杂环; 用于制备用于预防或治疗通过细胞因子介导的疾病的药物。

7. 发明授权

US07803795B2 Phthalazine derivatives as parp inhibitors 有权
标题翻译：酞嗪衍生物作为抑制剂
公开(公告)号：US07803795B2
公开(公告)日：2010-09-28
申请号：US11569889
申请日：2005-06-28
申请人： Laurence Anne Mevellec , Ludo Edmond Josephine Kennis , Josephus Carolus Mertens , Jacobus Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
发明人： Laurence Anne Mevellec , Ludo Edmond Josephine Kennis , Josephus Carolus Mertens , Jacobus Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
IPC分类号： C07D237/32 , A61K31/498 , A61K31/55 , C07D403/12 , C07D405/04 , C07D211/58 , A61P9/10 , A61P29/00 , A61P35/00 , A61P3/10 , A61P3/14
CPC分类号： A61K31/55 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/542 , C07D237/34 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D417/14 , C07D451/04 , C07D471/04 , C07D513/04
摘要： The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2 L1, L2, X, Y, Q and Z have defined meanings.
摘要翻译：本发明提供式（I）化合物，它们作为PARP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R 1，R 2，L 1，L 2，X，Y，Q和Z具有定义的含义。

8. 发明授权

US06506768B2 Tetrahydro &ggr;-carbolines 失效
标题翻译：四氢γ-咔啉
公开(公告)号：US06506768B2
公开(公告)日：2003-01-14
申请号：US09930005
申请日：2001-08-15
申请人： Ludo Edmond Josephine Kennis , Josephus Carolus Mertens
发明人： Ludo Edmond Josephine Kennis , Josephus Carolus Mertens
IPC分类号： C07D47104
CPC分类号： C07D471/04
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 R1 is hydrogen, optionally substituted C1-6alkyl, aryl; R2 is each independently a halogen, hydroxy, C1-6alkyl, C1-6alkyloxy or nitro; n is 0, 1, 2 or 3; Alk is C1-6alkanediyl; D is an optionally substituted saturated or unsaturated nitrogen containing heterocycle; and aryl is optionally substituted phenyl; having a great therapeutic breadth. It further relates to their use as a medicine, their preparation as well as compositions containing them.
摘要翻译：本发明涉及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R 1是氢，任选取代的C 1-6烷基，芳基; R2各自独立地为卤素，羟基，C 1-6烷基，C 1-6烷氧基或硝基; n为0,1,2或3; Alk是C1-6烷二基; D是任选取代的饱和或不饱和的含氮杂环; 芳基是任选取代的苯基; 具有很大的治疗广度。它还涉及它们作为药物的用途，它们的制备以及含有它们的组合物。

9. 发明授权

US06224849B1 Alkylaminobenzothiazole and-benzoxazole derivatives 有权
标题翻译：烷基氨基苯并噻唑和苯并恶唑衍生物
公开(公告)号：US06224849B1
公开(公告)日：2001-05-01
申请号：US09604427
申请日：2000-06-27
申请人： Ludo Edmond Josephine Kennis , Josephus Carolus Mertens , Serge Maria Aloysius Pieters
发明人： Ludo Edmond Josephine Kennis , Josephus Carolus Mertens , Serge Maria Aloysius Pieters
IPC分类号： A61K5100
CPC分类号： C07D263/58 , C07B59/002 , C07D277/82
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is O or S; n is 2, 3, 4 or 5; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy or halo; R2 is hydrogen, C1-6alkyl, phenyl, phenylC1-6alkyl or phenylcarbonyl; R3 and R4 each independently are selected from hydrogen, halo, nitro, C1-6alkyl, C1-6alkyloxy, haloC1-6alkyl, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl; or R3 and R4 may also be taken together to form a bivalent radical of formula —CH═CH—CH═CH—; it further relates to processes for their preparation, compositions comprising them as well as their use as a medicine; compounds of formula (I) containing a radioactive isotope; a process of marking dopamine D4 receptor sites; and a process for imaging an organ are disclosed.
摘要翻译：本发明涉及N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中X是O或S; n为2,3,4或5; R1是氢，C1-6烷基，C1-6烷氧基或卤素; R2是氢，C1-6烷基，苯基，苯基C1-6烷基或苯基羰基; R 3和R 4各自独立地选自氢，卤素，硝基，C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷基，氨基磺酰基，单或二（C 1-4烷基）氨基磺酰基; 或者R 3和R 4也可以一起形成式-CH = CH-CH = CH-的二价基团; 它还涉及它们的制备方法，包含它们的组合物以及它们作为药物的用途; 含有放射性同位素的式（I）化合物; 标记多巴胺D4受体位点的过程; 并且公开了用于成像器官的方法。

10. 发明授权

US07105550B2 2,4-disubstituted thiazolyl derivatives 有权
标题翻译： 2,4-二取代噻唑衍生物
公开(公告)号：US07105550B2
公开(公告)日：2006-09-12
申请号：US10220350
申请日：2001-02-20
申请人： Christopher Love , Jean Pierre Frans Van Wauwe , Marc De Brabander , Ludwig Cooymans , Nele Vandermaesen , Ludo Edmond Josephine Kennis
发明人： Christopher Love , Jean Pierre Frans Van Wauwe , Marc De Brabander , Ludwig Cooymans , Nele Vandermaesen , Ludo Edmond Josephine Kennis
IPC分类号： A61K31/41 , A61K31/425 , A61K31/415
CPC分类号： C07D417/04 , C07D277/42 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： This invention concerns the use of a compound of formula (I′) a N-oxide, pharmaceutically acceptable addition salt, quaternary amine and stereochemically isomeric form thereof, wherein Q is optionally substituted C3-6cycloalkyl, phenyl, naphthyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl; or Q is a radical of formula wherein X and Y each independently are O, NR3, CH2 or S, with R3 being hydrogen or C1-4alkyl; q is 1 to 4; Z is O or NR4 with R4 being hydrogen or C1-4alkyl; r is 1 to 3; L is optionally substituted phenyl or L is Het with Het being an optionally substituted five- or six-membered heterocyclic ring or an optionally substituted bicyclic heterocyclic ring; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through cytokines.
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形式的用途，其中Q是任选取代的C 3-6环烷基，苯基，萘基，吡啶基，嘧啶基，吡嗪基，哒嗪基，苯并噻唑基，苯并恶唑基，苯并咪唑基，吲唑基或咪唑并吡啶基。或Q是下式的基团，其中X和Y各自独立地为O，NR 3，CH 2或S，其中R 3为氢或C 1-4烷基; q为1〜4; Z为O或NR 4，其中R 4为氢或C 1-4烷基; r为1〜3; L是任选取代的苯基或L是Het，Het是任选取代的五元或六元杂环或任选取代的双环杂环; 用于制备用于预防或治疗通过细胞因子介导的疾病的药物。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式