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1. 发明授权

US6156757A 1,2,3,4-tetrahydro-benzofuro[3,2-C]pyridine derivatives 有权
标题翻译： 1,2,3,4-四氢 - 苯并呋喃并[3,2-C]吡啶衍生物
公开(公告)号：US6156757A
公开(公告)日：2000-12-05
申请号：US402593
申请日：1999-10-04
申请人： Ludo Edmond Josephine Kennis , Christopher John Love , Paul Fran.cedilla.ois Bischoff
发明人： Ludo Edmond Josephine Kennis , Christopher John Love , Paul Fran.cedilla.ois Bischoff
IPC分类号： A61K31/00 , A61K31/427 , A61K31/435 , A61K31/4353 , A61K31/4355 , A61K31/4375 , A61K31/445 , A61K31/5025 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/529 , A61P1/00 , A61P3/00 , A61P3/10 , A61P9/00 , A61P15/00 , A61P15/10 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/24 , A61P25/28 , C07D491/04 , C07D491/048 , C07D498/04 , C07D513/04 , C07D519/00
CPC分类号： C07D491/04 , C07D513/04
摘要： The present invention concerns the compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R.sup.1 is independently hydrogen, halogen, C.sub.1-6 alkyl, nitro, hydroxy or C.sub.1-4 alkyloxy; Alk is C.sub.1-6 alkanediyl; n is 1 or 2; D is an optionally substituted mono-, bi- or tricyclic nitrogen containing heterocycle having central .alpha..sub.2 -adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine.
摘要翻译： PCT No.PCT / EP98 / 02136 Sec。 371 1999年10月4日第 102（e）日期1999年10月4日PCT提交1998年4月2日PCT公布。第WO98 / 45297号公报日期：1998年10月15日本发明涉及式I化合物的N-氧化物，其药学上可接受的加成盐和立体化学异构形式，其中每个R 1独立地是氢，卤素，C 1-6烷基，硝基，羟基或C 1-4烷氧基 ; Alk是C1-6烷二基; n为1或2; D是具有中枢性α2-肾上腺素受体拮抗剂活性的任选取代的单环，双环或三环含氮杂环。它还涉及它们的制备，包含它们的组合物及其作为药物的用途。

2. 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。

3. 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。

4. 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。

5. 发明申请

US20120065216A1 QUINAZOLINEDIONE DERIVATIVES AS PARP INHIBITORS 有权
标题翻译：喹诺酮衍生物作为PARP抑制剂
公开(公告)号：US20120065216A1
公开(公告)日：2012-03-15
申请号：US13298934
申请日：2011-11-17
申请人： Ludo Edmond Josephine Kennis , Josephus Carolus Mertens , Jacobus Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
发明人： Ludo Edmond Josephine Kennis , Josephus Carolus Mertens , Jacobus Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
IPC分类号： A61K31/517 , C07D401/14 , C07D405/14 , A61P25/18 , A61P25/08 , A61P25/14 , A61P25/02 , A61P3/10 , A61P25/28 , A61P25/16 , A61P19/02 , A61P31/18 , A61P35/04 , A61P9/10 , A61P29/00 , C07D401/04
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所述式（I）化合物的药物组合物，其中R1，L1，L2，X，Y和Z具有定义的含义。

6. 发明申请

US20080227791A1 Piperidin-4-Yl-Pyridazin-3-Ylamine Derivatives as Fast Dissociating Dopamine 2 Receptor Antagonists 有权
标题翻译：哌啶-4-Y1-哒嗪-3-胺衍生物作为快速分离多巴胺2受体拮抗剂
公开(公告)号：US20080227791A1
公开(公告)日：2008-09-18
申请号：US12091219
申请日：2006-10-24
申请人： Marcel Frans Leopold De Bruyn , Gregor James Macdonald , Ludo Edmond Josephine Kennis , Xavier Jean Michel Langlois , Frans Alfons Maria Van Den Keybus , 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 Keybus , Yves Emiel Maria Van Roosbroeck
IPC分类号： A61K31/501 , C07D401/12
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。

7. 发明授权

US06774129B2 Benzothieno[3,2-c]pyridines as &agr;2 antagonists 有权
标题翻译：苯并噻吩并[3,2-c]吡啶作为α2拮抗剂
公开(公告)号：US06774129B2
公开(公告)日：2004-08-10
申请号：US10123338
申请日：2002-04-16
申请人： Ludo Edmond Josephine Kennis , Serge Maria Aloysius Pieters , François Paul Bischoff
发明人： Ludo Edmond Josephine Kennis , Serge Maria Aloysius Pieters , François Paul Bischoff
IPC分类号： C07D49504
CPC分类号： C07D495/04
摘要： The present invention concerns the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; Alk is C1-6alkanediyl; n is 1 or 2; p is 0, 1 or 2; D is an optionally substituted mono-, bi- or tricyclic nitrogen containing heterocycle having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and 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，其中每个R 1独立地是氢，卤素，C 1-6烷基，硝基，羟基或C 1-4烷氧基; Alk是C1-6烷二基; n为1或2; p为0,1或2; D是具有中枢性α2-肾上腺素受体拮抗剂活性的任选取代的单环，双环或三环含氮杂环。它还涉及它们的制备，包含它们的组合物及其作为药物的用途。

8. 发明授权

US06320048B1 3-piperidinyl-1,2-benzisoxazoles 失效
标题翻译： 3-哌啶基-1,2-苯并异恶唑
公开(公告)号：US06320048B1
公开(公告)日：2001-11-20
申请号：US08100907
申请日：1993-08-03
申请人： Cornelus Gerardus Maria Janssen , Alfonsus Guilielmus Knaeps , Ludo Edmond Josephine Kennis , Jan Vandenberk
发明人： Cornelus Gerardus Maria Janssen , Alfonsus Guilielmus Knaeps , Ludo Edmond Josephine Kennis , Jan Vandenberk
IPC分类号： C07B5700
CPC分类号： C07D471/04
摘要： There is disclosed a process for preparing an enantiomeric form of the compound having the formula: or a pharmaceutically acceptable acid addition salt thereof, wherein said process comprises the steps of: (a) reacting a racemic mixture of said compound with a chiral acid or acid chloride selected from the group consisting of tartaric acid, malic acid, mandelic acid, camphor sulfonic acid, 4,5-dihydro-1H-2-benzopyran-2-carboxylic acid, and the acid chlorides thereof, to form a mixture of diastereomeric salts or esters; (b) physically separating said mixture of diastereomeric salts or esters by selective crystallization or chromatography; and (c) converting said separated diastereomeric salts or esters into the corresponding enantiomeric forms of said compound by hydrolysis in an acidic or basic aqueous medium.
摘要翻译：公开了具有下式的化合物或其药学上可接受的酸加成盐的对映体形式的方法，其中所述方法包括以下步骤：（a）使所述化合物的外消旋混合物与手性酸或酸反应选自酒石酸，苹果酸，扁桃酸，樟脑磺酸，4,5-二氢-1H-2-苯并吡喃-2-羧酸及其酰氯的氯化物，以形成非对映体盐的混合物或酯;（b）通过选择性结晶或色谱法物理分离所述非对映体盐或酯的混合物; 和（c）通过在酸性或碱性水性介质中水解将所述分离的非对映体盐或酯转化成所述化合物的相应对映体形式。

9. 发明授权

US6057325A Hexahydro-pyrido(4,3-b)indole derivatives as antipsychotic drugs 失效
标题翻译：六氢吡啶并（4,3-b）吲哚衍生物作为抗精神病药
公开(公告)号：US6057325A
公开(公告)日：2000-05-02
申请号：US180366
申请日：1998-11-09
申请人： Ludo Edmond Josephine Kennis , Josephus Carolus Mertens
发明人： Ludo Edmond Josephine Kennis , Josephus Carolus Mertens
IPC分类号： A61K31/00 , A61K31/505 , A61K31/513 , A61K31/519 , A61K31/529 , A61K31/54 , A61K31/542 , A61P25/00 , A61P43/00 , C07D471/04 , C07D498/04 , C07D513/04 , C07D519/00
CPC分类号： C07D471/04
摘要： This invention concerns the compounds of formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C.sub.1-6 alkanediyl; R.sup.1 is hydrogen, C.sub.1-6 alkyl, aryl or aryl C.sub.1-6 alkyl; R.sup.2, R.sup.3 and R.sup.4 are each independently selected from hydrogen, halo, hydroxy, nitro, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, trifluoromethyl, C.sub.1-6 alkylthio, mercapto, amino, mono- and di(C.sub.1-6 alkyl)amino, carboxyl, C.sub.1-6 alkyloxycarbonyl or C.sub.1-6 alkylcarbonyl; R.sup.5 is hydrogen, C.sub.1-6 alkyl, phenyl or phenylC.sub.1-6 alkyl; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, or a radical of formula --NR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 are each independently selected from hydrogen, C.sub.1-6 alkyl, phenyl or phenylC.sub.1-6 alkyl; R.sup.7 is hydrogen or C.sub.1-6 alkyl; or R.sup.6 and R.sup.7 taken together may form a bivalent radical of formula --R.sup.6 --R.sup.7 --; having central dopamine and serotonin antogonistic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译： PCT No.PCT / EP97 / 02710 Sec。 371日期：1998年11月9日 102（e）1998年11月9日PCT PCT 1997年5月15日PCT公布。公开号WO97 / 44040 PCT 日期1997年11月27日本发明涉及药学上可接受的加成盐及其立体化学异构形式的化合物，其中Alk是C 1-6烷二基; R1是氢，C1-6烷基，芳基或芳基C1-6烷基; R2，R3和R4各自独立地选自氢，卤素，羟基，硝基，氰基，C1-6烷基，C1-6烷氧基，三氟甲基，C1-6烷硫基，巯基，氨基，单和二（C1-6烷基），C 1-6烷氧基羰基或C 1-6烷基羰基; R5是氢，C1-6烷基，苯基或苯基C1-6烷基; R 6是氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基或式-NR 8 R 9基团，其中R 8和R 9各自独立地选自氢，C 1-6烷基，苯基或苯基C 1-6烷基; R7是氢或C1-6烷基; 或R6和R7一起可以形成式-R6-R7-的二价基团; 具有中枢多巴胺和血清素神经活性; 其制剂，含有它们的组合物及其作为药物的用途。

10. 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。

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