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1. 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。

2. 发明授权

US06576640B1 Benzisoxazoles and phenones as &agr;2-antagonists 有权
标题翻译：苯并恶唑和苯酚作为α2-拮抗剂
公开(公告)号：US06576640B1
公开(公告)日：2003-06-10
申请号：US09868756
申请日：2001-07-26
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： A61K31437
CPC分类号： C07D471/04 , C07D491/04 , C07D495/04
摘要： The present invention concerns compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C5-12alkanediyl; n is 1 or 2; p is 1 and q is 2; or p is 2 and q is 1; X is —O—, —S—, —S(═O)—, —S(═O)2— or NR2; each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; R2 is hydrogen, C1-6alkyl, aryl or C1-6alkyl substituted with aryl; aryl is phenyl or phenyl substituted with a halogen or C1-6alkyl; D is an optionally substituted benzophenone or 3-benzisoxazolyl; having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.
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Alk是C 5-12烷二基; n为1或2; p为1，q为2; 或p为2，q为1; X是-O - ， - S - ， - S（= O） - ， - S（= O）2 - 或NR 2; 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; R2是氢，C1-6烷基，芳基或被芳基取代的C1-6烷基; 芳基是苯基或被卤素或C 1-6烷基取代的苯基; D是任选取代的二苯甲酮或3-苯并异恶唑基; 具有中枢性α2肾上腺素受体拮抗剂活性。它还涉及它们的制备，药物用途和组合物。

3. 发明授权

US6103725A 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：US6103725A
公开(公告)日：2000-08-15
申请号：US180369
申请日：1998-11-09
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： A61K31/00 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/495 , A61K31/496 , A61K51/00 , A61P25/00 , A61P25/18 , A61P43/00 , C07B59/00 , C07D263/28 , C07D263/58 , C07D277/82 , C07D413/12 , C07D417/12
CPC分类号： C07D263/58 , C07B59/002 , C07D277/82
摘要： The present invention concerns the compounds of formula ##STR1## 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; R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or halo; R.sup.2 is hydrogen, C.sub.1-6 alkyl, phenyl, phenylC.sub.1-6 alkyl or phenylcarbonyl; R.sup.3 and R.sup.4 each independently are selected from hydrogen, halo, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, haloC.sub.1-6 alkyl, aminosulfonyl, mono- or di(C.sub.1-4 alkyl)aminosulfonyl; or R.sup.3 and R.sup.4 may also be taken together to form a bivalent radical of formula --CH.dbd.CH--CH.dbd.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 D.sub.4 receptor sites; and a process for imaging an organ are disclosed.
摘要翻译： PCT No.PCT / EP97 / 02505 Sec。 371日期：1998年11月9日 102（e）1998年11月9日PCT PCT 1997年5月2日PCT公布。公开号WO97 / 43271 日期：1997年11月20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加成盐和立体化学异构形式，其中X为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。

4. 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。

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。

7. 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。

8. 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。

9. 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。

10. 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。

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