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1.发明申请Compositions, Kits and Methods for a Titration Schedule for Pardoprunox Compounds 审中-公开Pardoprunox化合物滴定计划的组成，试剂盒和方法公开(公告)号：US20090215796A1
公开(公告)日：2009-08-27
申请号：US12391393
申请日：2009-02-24
申请人： Juliana B. Bronzova , Gustaaf J. M. Van Scharrenburg , Serge V. Van De Witte , Hendrik Teunissen
发明人： Juliana B. Bronzova , Gustaaf J. M. Van Scharrenburg , Serge V. Van De Witte , Hendrik Teunissen
IPC分类号： A61K31/496 , A61P25/16 , A61P25/00
CPC分类号： A61K31/496
摘要： The present invention is directed to compositions, kits, and methods for a titration schedule to facilitate the treatment of a central nervous system condition or disorder by administering a plurality of dosage units of a composition comprising a compound 7-(4-methyl)-1-piperazinyl-2(3H)-benzoxazolone (INN pardoprunox).
摘要翻译： 本发明涉及用于滴定方案的组合物，试剂盒和方法，以便于通过施用包含化合物7-（4-甲基）-1的组合物的多个剂量单位来治疗中枢神经系统病症或病症 - 哌嗪基-2（3H） - 苯并恶唑酮（INN pardoprunox）。
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![[1,2,4]-dithiazoli(di)ne derivatives, inducers of gluthathione-S-transferase and NADPH quinone oxido-reductase, for prophylaxis and treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular](/abs-image/US/2010/03/16/US07678789B2/abs.jpg.150x150.jpg)
2.发明授权[1,2,4]-dithiazoli(di)ne derivatives, inducers of gluthathione-S-transferase and NADPH quinone oxido-reductase, for prophylaxis and treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular 有权[1,2,4] - 二噻唑（di）ne衍生物，谷胱甘肽-S-转移酶和NADPH醌氧化还原酶的诱导剂，用于预防和治疗与一般细胞毒性有关的不利条件和特别是细胞凋亡公开(公告)号：US07678789B2
公开(公告)日：2010-03-16
申请号：US11349910
申请日：2006-02-09
申请人： Roelof W. Feenstra , Hiskias G. Keizer , Maria L. Pras-Raves , Bernard J Van Vliet , Gustaaf J. M. Van Scharrenburg
发明人： Roelof W. Feenstra , Hiskias G. Keizer , Maria L. Pras-Raves , Bernard J Van Vliet , Gustaaf J. M. Van Scharrenburg
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4535 , A61K31/4436 , A61K31/41 , C07D417/04 , C07D413/04 , C07D285/01
CPC分类号： C07D285/01 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to 5-imino-5H-[1,2,4]-dithiazol-3-yl-amine and [1,2,4]-dithiazolidine-3,5-diylidene-diamine derivatives as inducers of gluthathione-S-transferase (GST) and NADPH quinone oxidoreductase (NQO), to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said [1,2,4]-dithiazoli(di)ne derivatives. The invention also relates to the use of a compound disclosed herein for the treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular. The invention relates to compounds of the general formula (I): wherein wherein the symbols have the meanings given in the specification.
摘要翻译： 本发明涉及5-亚氨基-5H- [1,2,4] - 二噻唑-3-基 - 胺和[1,2,4] - 二噻唑烷-3,5-二亚胺基二胺衍生物作为谷胱甘肽 - S-转移酶（GST）和NADPH醌氧化还原酶（NQO），用于制备这些化合物的方法和用于合成所述[1,2,4] - 二噻唑（di）ne衍生物的新中间体。 本发明还涉及本文公开的化合物用于治疗与一般细胞毒性和特别是细胞凋亡相关的不利条件的用途。 本发明涉及通式（I）的化合物：其中符号具有说明书中给出的含义。
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公开(公告)号：US08106056B2
公开(公告)日：2012-01-31
申请号：US11762239
申请日：2007-06-13
IPC分类号： A61K31/497 , A61K31/195 , A61K31/16 , A61K31/135
CPC分类号： A61K31/137 , A61K31/198 , A61K31/496 , A61K2300/00
摘要： The present invention relates to a composition containing bifeprunox or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function, including Parkinson's disease and restless leg syndrome.
摘要翻译： 本发明涉及含有双岐杆菌或其N-氧化物或其至少一种药理学可接受的盐的组合物：和L-DOPA或其至少一种药理学上可接受的盐，用于同时，分开或顺序地用于治疗所需疾病 恢复多巴胺能功能，包括帕金森病和不宁腿综合征。
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公开(公告)号：US07786126B2
公开(公告)日：2010-08-31
申请号：US11762206
申请日：2007-06-13
IPC分类号： A61K31/497 , A61K31/195 , A61K31/135
CPC分类号： A61K31/137 , A61K31/198 , A61K31/496 , A61K2300/00
摘要： A composition containing SLV308 or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function using this composition, including Parkinson's disease and restless leg syndrome.
摘要翻译： 含有SLV308或其N-氧化物或其至少一种药学上可接受的盐的组合物：和L-DOPA或其至少一种药理学上可接受的盐，用于同时，分别或顺序地用于治疗需要恢复多巴胺能功能的疾病，其使用 这种组合物，包括帕金森病和不宁腿综合征。
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![Hexa- and octahydro-pyrido[1,2-a]pyrazine derivatives with NK1 antagonistic activity](/abs-image/US/2007/07/17/US07244734B2/abs.jpg.150x150.jpg)
5.发明授权Hexa- and octahydro-pyrido[1,2-a]pyrazine derivatives with NK1 antagonistic activity 失效具有NK1拮抗活性的六氢和八氢吡啶并[1,2-a]吡嗪衍生物公开(公告)号：US07244734B2
公开(公告)日：2007-07-17
申请号：US10946176
申请日：2004-09-22
申请人： Wouter I. Iwema Bakker , Gustaaf J. M. Van Scharrenburg , Adrianus Van Den Hoogenband , Andrew C. McCreary
发明人： Wouter I. Iwema Bakker , Gustaaf J. M. Van Scharrenburg , Adrianus Van Den Hoogenband , Andrew C. McCreary
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D401/00
CPC分类号： C07D471/04
摘要： The invention relates to hexahydro-pyrido[1,2-a]pyrazine derivatives having interesting neurokinin-NK1 receptor antagonistic activity. The invention also relates to methods for the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these compounds as an active ingredient, as well as to the use of these compositions for the treatment of disorders in which neurokinin receptors are involved. The invention relates to compounds represented by the general formula (1) wherein the symbols have the meanings as given in the description.
摘要翻译： 本发明涉及具有感兴趣的神经激肽-NN1受体拮抗活性的六氢 - 吡啶并[1,2-a]吡嗪衍生物。 本发明还涉及制备这些化合物的方法，含有药理学活性量的这些化合物中的至少一种作为活性成分的药物组合物，以及这些组合物用于治疗神经激肽 受体参与。 本发明涉及由通式（1）表示的化合物，其中符号具有说明书中给出的含义。
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公开(公告)号：US06780864B1
公开(公告)日：2004-08-24
申请号：US09831149
申请日：2001-08-14
申请人： Roelof Feenstra , Johannes A. M. Van Der Heijden , Cornelis G. Kruse , Stephen K. Long , Johannes Mos , Gerben M. Visser , Gustaaf J. M. Van Scharrenburg , Gerrit P. Toorop
发明人： Roelof Feenstra , Johannes A. M. Van Der Heijden , Cornelis G. Kruse , Stephen K. Long , Johannes Mos , Gerben M. Visser , Gustaaf J. M. Van Scharrenburg , Gerrit P. Toorop
IPC分类号： C07D26358
CPC分类号： C07D263/58 , C07D209/34 , C07D235/26 , C07D277/68 , C07D401/04 , C07D413/04 , C07D417/04 , Y02P20/55
摘要： The invention relates to a group of novel piperazine and piperidine derivatives of formula (I), wherein: S1 is hydrogen, halogen, alkyl (1-3C), CN, CF3, OCF3, SCF3, alkoxy (1-3C), amino or mono- or dialkyl (1-3C) substituted amino, or hydroxy; X represents NR3, S, CH2, O, SO or SO2, wherein R3 is H or alkyl (1-3C); . . . Z represents ═C or —N; —R1 independently represent H or alkyl (1-3C), or R1 and R2 together can form a bridge 2 or 3 C-atoms; R4 is hydrogen or alkyl (1-3C); Q is methyl, ethyl, ethyl substituted with one or more fluorine atoms, cyclopropyl—methyl, optionally substituted with one or more fluorine atoms, and salts and prodrugs thereof. It has been found that these compounds have both partial dopamine D2-receptor agonism and partial serotonin 5-HT1A-receptor agonism mediated activities.
摘要翻译： 本发明涉及一组式（I）的新的哌嗪和哌啶衍生物，其中：S1为氢，卤素，烷基（1-3C），CN，CF3，OCF3，SCF3，烷氧基（1-3C），氨基或 单或二烷基（1-3C）取代的氨基或羟基; X表示NR 3，S，CH 2，O，SO或SO 2，其中R 3是H或烷基（1-3C）; 。 。 。 Z表示= C或-N; -R1独立地表示H或烷基（1-3C），或者R1和R2一起可以形成桥2或3个C原子; R4是氢或烷基（1-3C）; Q是甲基，乙基，被一个或多个氟原子取代的乙基，任选被一个或多个氟原子取代的环丙基甲基，及其盐和前药。 已经发现这些化合物具有部分多巴胺D2受体激动和部分5-羟色胺5-HT 1A受体激动介导的活性。
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7.发明授权Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition 有权具有部分多巴胺-D2受体激动剂和5-羟色胺再摄取抑制组合的苯基哌嗪衍生物公开(公告)号：US08101619B2
公开(公告)日：2012-01-24
申请号：US11294603
申请日：2005-12-06
申请人： Roelof W. Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria L. Pras-Raves , Andrew C. McCreary , Bernard J. Van Vliet , Mayke B. Hesselink , Cornelis G. Kruse , Gustaaf J. M. Van Scharrenburg
发明人： Roelof W. Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria L. Pras-Raves , Andrew C. McCreary , Bernard J. Van Vliet , Mayke B. Hesselink , Cornelis G. Kruse , Gustaaf J. M. Van Scharrenburg
IPC分类号： A61K31/496 , C07D263/58
CPC分类号： C07D263/58 , C07D413/12
摘要： The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect.The compounds have the general formula (1): wherein the symbols have the meanings given in the specification, and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.
摘要翻译： 本发明涉及一组具有双重作用方式的新型苯基哌嗪衍生物：5-羟色胺再摄取抑制和对多巴胺D2受体的部分激动作用。 本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。 所述化合物具有通式（1）：其中符号具有说明书中给出的含义及其互变异构体，立体异构体和N-氧化物，以及所述式（1）化合物的药理学上可接受的盐，水合物和溶剂化物， 其互变异构体，立体异构体和N-氧化物。
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8.发明授权Benzimidazolone and quinazolinone derivatives as agonists on human ORL1 receptors 有权苯并咪唑酮和喹唑啉酮衍生物作为人类ORL1受体的激动剂公开(公告)号：US08067603B2
公开(公告)日：2011-11-29
申请号：US10946177
申请日：2004-09-22
申请人： Jacobus A. J. Den Hartog , Gustaaf J. M. Van Scharrenburg , Herman H. Van Stuivenberg , Tinka Tuinstra , Jan-Willem Terpstra
发明人： Jacobus A. J. Den Hartog , Gustaaf J. M. Van Scharrenburg , Herman H. Van Stuivenberg , Tinka Tuinstra , Jan-Willem Terpstra
IPC分类号： C07D211/58 , A61K31/454
CPC分类号： C07C251/20 , C07C2603/28 , C07D401/04 , C07D451/04
摘要： The invention relates to a group of novel benzimidazolone and quinazolinone derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these imidazolone and quinazolinone derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1): wherein the symbols have the meanings as given in the description.
摘要翻译： 本发明涉及一组新的苯并咪唑酮和喹唑啉酮衍生物，它们是人类ORL1（伤害感受素）受体的激动剂。 本发明还涉及这些化合物的制备，含有药理活性量的这些咪唑啉酮和喹唑啉酮衍生物中的至少一种作为活性成分的药物组合物，以及这些药物组合物在治疗疾病中的用途 哪个ORL1受体参与。 本发明涉及通式（1）的化合物：其中符号具有说明书中给出的含义。
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公开(公告)号：US07915262B2
公开(公告)日：2011-03-29
申请号：US12843967
申请日：2010-07-27
IPC分类号： A61K31/497 , A61K31/195 , A61K31/135
CPC分类号： A61K31/137 , A61K31/198 , A61K31/496 , A61K2300/00
摘要： A composition containing SLV308 or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function using this composition, including Parkinson's disease and restless leg syndrome.
摘要翻译： 含有SLV308或其N-氧化物或其至少一种药学上可接受的盐的组合物：和L-DOPA或其至少一种药理学上可接受的盐，用于同时，分别或顺序地用于治疗需要恢复多巴胺能功能的疾病，其使用 这种组合物，包括帕金森病和不宁腿综合征。
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10.发明授权Hydronopol substituted benzimidazolone and quinazolinone derivatives as agonists on human ORL1 receptors 有权水诺酮取代的苯并咪唑酮和喹唑啉酮衍生物作为人类ORL1受体的激动剂公开(公告)号：US07851630B2
公开(公告)日：2010-12-14
申请号：US10952180
申请日：2004-09-29
申请人： Jacobus A. J. Den Hartog , Samuel David , Daniel Jasserand , Gustaaf J. M. Van Scharrenburg , Herman H. Van Stuivenberg , Tinka Tuinstra
发明人： Jacobus A. J. Den Hartog , Samuel David , Daniel Jasserand , Gustaaf J. M. Van Scharrenburg , Herman H. Van Stuivenberg , Tinka Tuinstra
IPC分类号： C07D211/58 , A61K31/454
CPC分类号： A61K31/397 , A61K31/4025 , A61K31/4184 , A61K31/4523 , A61K31/517 , C07D401/04 , C07D403/04
摘要： The invention relates to a group of hydronopol substituted benzimidazolone and quinazolinone derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these novel benzimidazolone and quinazolinone derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved.The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the description.
摘要翻译： 本发明涉及作为人类ORL1（伤害感受素）受体的激动剂的一组水诺酮取代的苯并咪唑酮和喹唑啉酮衍生物。 本发明还涉及这些化合物的制备，含有药理活性量的这些新的苯并咪唑酮和喹唑啉酮衍生物中的至少一种作为活性成分的药物组合物，以及这些药物组合物用于治疗疾病的用途 其中涉及ORL1受体。 本发明涉及通式（1）的化合物，其中符号具有说明书中给出的含义。
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