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1. 发明授权

US07750013B2 N-oxides as prodrugs of piperazine and piperidine derivatives 有权
标题翻译： N-氧化物作为哌嗪和哌啶衍生物的前药
公开(公告)号：US07750013B2
公开(公告)日：2010-07-06
申请号：US11504050
申请日：2006-08-15
申请人： Theodorus S. M. Koopman , Hendrink J. Koster , Peter H. Van Amsterdam , Roelof W. Feenstra , Marinus Verhage , Andrew C. McCreary , Mayke B. Hesselink , Gustaaf J. M. Van Scharrenburg
发明人： Theodorus S. M. Koopman , Hendrink J. Koster , Peter H. Van Amsterdam , Roelof W. Feenstra , Marinus Verhage , Andrew C. McCreary , Mayke B. Hesselink , Gustaaf J. M. Van Scharrenburg
IPC分类号： C07D263/58 , A61K31/423 , A61K31/496
CPC分类号： C07D263/58 , C07D413/04
摘要： The present disclosure relates to N-oxides of certain piperazine and piperidine derivatives and to methods for the preparation of these compounds. The disclosure also relates to the use of the compounds for the manufacture of a medicament giving a beneficial effect. The disclosure also relates to the use of the compounds for the manufacture of a medicament for treating a disease or condition. The disclosure further relates to the treatment of CNS-disorders, in particular the treatment of anxiety disorders, including generalized anxiety disorder and panic disorder, obsessive compulsive disorder, aggression, addiction (including craving), depression, autism, vertigo, schizophrenia and other psychotic disorders, Parkinson's disease and disturbances of cognition and memory. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.
摘要翻译：本公开内容涉及某些哌嗪和哌啶衍生物的N-氧化物以及这些化合物的制备方法。本公开还涉及该化合物在制备产生有益效果的药物中的用途。本公开还涉及化合物在制备用于治疗疾病或病症的药物中的用途。本发明还涉及中枢神经系统疾病的治疗，特别是焦虑症的治疗，包括广泛性焦虑障碍和恐慌症，强迫症，侵略，成瘾（包括渴望），抑郁症，孤独症，眩晕，精神分裂症等精神病疾病，帕金森病和认知和记忆障碍。化合物具有通式（1），其中符号具有说明书中给出的含义。

2. 发明授权

US08101619B2 Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition 有权
标题翻译：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。

3. 发明授权

US06828325B2 Phenylpiperazines 失效
标题翻译：苯基哌嗪
公开(公告)号：US06828325B2
公开(公告)日：2004-12-07
申请号：US10343232
申请日：2003-01-30
申请人： Roelof W. Feenstra , Eric Ronken , Cornelis G. Kruse , Andrew C. McCreary , Gustaaf J. M. van Scharrenburg
发明人： Roelof W. Feenstra , Eric Ronken , Cornelis G. Kruse , Andrew C. McCreary , Gustaaf J. M. van Scharrenburg
IPC分类号： A61K31496
CPC分类号： C07D413/12 , C07D471/06
摘要： The invention relates to novel phenylpiperazine derivatives of the formula wherein: —R represents the group (a) or (b) as indicated in the description. These compounds are (partial) D2 receptor agonists and are usefull for treating CNS disorders, in particular Parkinson's disease.
摘要翻译：本发明涉及下式的新的苯基哌嗪衍生物其中：-R代表如说明书中所指出的（a）或（b）组。这些化合物是（部分）D2受体激动剂，并且可用于治疗CNS疾病，特别是帕金森病。

4. 发明授权

US07678789B2 [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
标题翻译： [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。

5. 发明授权

US07297699B2 Piperazine and piperidine compounds 有权
标题翻译：哌嗪和哌啶化合物
公开(公告)号：US07297699B2
公开(公告)日：2007-11-20
申请号：US11129465
申请日：2005-05-16
申请人： Roelof W. Feenstra , Johannes A. M. van der Heijden , Cornelis G. Kruse , Stephen K. Long , Gustaaf J. M. van Scharrenburg
发明人： Roelof W. Feenstra , Johannes A. M. van der Heijden , Cornelis G. Kruse , Stephen K. Long , Gustaaf J. M. van Scharrenburg
IPC分类号： A61K31/496 , C07D263/58 , C07D277/68
CPC分类号： C07D263/58 , C07D413/12
摘要： The invention relates to a group of novel piperazine and piperidine derivatives of the formula wherein Y is hydrogen, halogen, alkyl (1-3C), or CN, CF3, OCF3, SCF3, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or hydroxy, X is O, S, SO or SO2, —Z represents —C, ═C or —N, R1 and R2 independently represent hydrogen or alkyl (1-3C), Q is benzyl or 2-, 3- or 4-pyridylmethyl, wich groups may be substited with one or more more substituents from the group halogen, nitro, cyano, amino, mono- or di (1-3C)alkylamino, (1-3C) alkoxy, CF3, OCF3, SCF3, (1-4C)-alkyl, (1-3C)alkylsulfonyl or hydroxy, and salts and prodrugs thereof. It has been found that these compounds have interesting pharmacological properties due to a combination of (partial) agonism towards the members of the dopamine D2-receptor subfamily and affinity for relevant serotonin and/or noradrenergic receptors
摘要翻译：本发明涉及下式的一组新的哌嗪和哌啶衍生物其中Y是氢，卤素，烷基（1-3C）或CN，CF 3，OCF 3， >，SCF 3，烷氧基（1-3C），氨基或单或二烷基（1-3C）取代的氨基或羟基，X是O，S，SO或SO 2， SUB，-Z表示-C，-C或-N，R 1和R 2独立地表示氢或烷基（1-3C），Q是苄基或2 - ，3-或4-吡啶基甲基，其基团可以被一个或多个取代基取代，所述取代基可以是卤素，硝基，氰基，氨基，单或二（1-3C）烷基氨基，（1-3C）烷氧基，CF OCF 3，SCF 3，（1-4C） - 烷基，（1-3C）烷基磺酰基或羟基，及其盐和前体药物其中。已经发现，这些化合物由于（多）向多巴胺D 2受体亚家族的成员的组合以及对相关的5-羟色胺和/或去甲肾上腺素能受体的亲和力而具有令人感兴趣的药理学性质

6. 发明授权

US06911448B2 Piperazine and piperidine compounds 失效
标题翻译：哌嗪和哌啶化合物
公开(公告)号：US06911448B2
公开(公告)日：2005-06-28
申请号：US10257677
申请日：2001-05-10
申请人： Roelof W. Feenstra , Johannes A. M. van der Heijden , Cornelis G. Kruse , Stephen K. Long , Gustaaf J. M. van Scharrenburg
发明人： Roelof W. Feenstra , Johannes A. M. van der Heijden , Cornelis G. Kruse , Stephen K. Long , Gustaaf J. M. van Scharrenburg
IPC分类号： C07D413/10 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/445 , A61K31/4523 , A61K31/496 , A61P25/00 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/30 , A61P43/00 , C07D263/54 , C07D263/58 , C07D277/62 , C07D413/04 , C07D413/12 , C07D413/14 , A61K31/454
CPC分类号： C07D263/58 , C07D413/12
摘要： The invention relates to a group of novel piperazine and piperidine derivatives of the formula wherein Y is hydrogen, halogen, alkyl (1-3C), or CN, CF3, OCF3, SCF3, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or hydroxy, X is O, S, SO or SO2, ---Z represents —C, ═C or —N, R1 and R2 independently represent hydrogen or alkyl (1-3C), Q is benzyl or 2-, 3- or 4-pyridylmethyl, wich groups may be substited with one or more more substituents from the group halogen, nitro, cyano, amino, mono- or di (1-3C)alkylamino, (1-3C) alkoxy, CF3, OCF3, SCF3, (1-4C)-alkyl, (1-3C)alkylsulfonyl or hydroxy, and salts and prodrugs thereof. It has been found that these compounds have interesting pharmacological properties due to a combination of (partial) agonism towards the members of the dopamine D2-receptor subfamily and affinity for relevant serotonin and/or noradrenergic receptors
摘要翻译：本发明涉及下式的一组新的哌嗪和哌啶衍生物其中Y是氢，卤素，烷基（1-3C）或CN，CF 3，OCF 3， >，SCF 3，烷氧基（1-3C），氨基或单或二烷基（1-3C）取代的氨基或羟基，X是O，S，SO或SO 2， Z表示-C，-C或-N，R 1和R 2独立地表示氢或烷基（1-3C），Q表示苄基或2-，3-或4-吡啶基甲基，其可以被一个或多个取代基取代为卤素，硝基，氰基，氨基，单或二（1-3C）烷基氨基，（1-3C）烷氧基，CF 3 3，OCF 3，SCF 3，（1-4C） - 烷基，（1-3C）烷基磺酰基或羟基，和盐及其前体药物。已经发现，这些化合物由于（多）向多巴胺D 2受体亚家族的成员的组合以及对相关的5-羟色胺和/或去甲肾上腺素能受体的亲和力而具有令人感兴趣的药理学性质

7. 发明授权

US07371737B2 2-substituted-6-trifluoromethyl purine derivatives with adenosine-A3 antagonistic activity 有权
标题翻译：具有腺苷-3A拮抗活性的2-取代-6-三氟甲基嘌呤衍生物
公开(公告)号：US07371737B2
公开(公告)日：2008-05-13
申请号：US11219818
申请日：2005-09-07
申请人： Melle Koch , Jacobus A. J. den Hartog , Gerrit-Jan Koomen , Martinus J. Wanner , Roelof W. Feenstra
发明人： Melle Koch , Jacobus A. J. den Hartog , Gerrit-Jan Koomen , Martinus J. Wanner , Roelof W. Feenstra
IPC分类号： A01N43/04 , A01N43/90 , A61K31/70 , C07H19/00 , C07D473/00
CPC分类号： C07D473/40 , C07H19/16
摘要： The present invention relates to 2-substituted-6-trifluoromethyl purine derivatives as selective adenosine antagonists, in particular adenosine-A3 receptor antagonists, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said purine derivatives.The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及2-取代-6-三氟甲基嘌呤衍生物作为选择性腺苷拮抗剂，特别是腺苷-A 3受体拮抗剂，用于制备这些化合物的方法和用于所述嘌呤衍生物的合成。化合物具有通式（1），其中符号具有说明书中给出的含义。

8. 发明申请

US20080146524A1 Selective inhibitors of neurotensin degrading enzymes 审中-公开
标题翻译：神经降压素降解酶的选择性抑制剂
公开(公告)号：US20080146524A1
公开(公告)日：2008-06-19
申请号：US12000273
申请日：2007-12-11
申请人： Pieter Smid , Roelof W. Feenstra , Cornelis G. Kruse
发明人： Pieter Smid , Roelof W. Feenstra , Cornelis G. Kruse
IPC分类号： A61K31/675 , A61P1/00 , A61P25/18 , A61P25/24 , A61P25/28 , A61P9/12 , C07F9/572 , C12N9/99
CPC分类号： C07K5/06 , A61K38/00 , C07F9/301 , C07F9/306 , C07F9/572 , C07F9/6539 , C07K5/06008 , C07K5/06026 , C07K5/06034 , C07K5/06139 , C07K5/06165
摘要： Embodiments of this invention relate to compounds that are selective inhibitors of neurotensin degrading enzymes, to pharmaceutical compositions containing these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions containing these compounds. The invention also relates to the use of such compounds and compositions for regulating blood pressure or gastric emptying, or treating Parkinson's disease, anxiety, depression, or psychosis. The compounds have the formula (1) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明的实施方案涉及作为神经降压素降解酶的选择性抑制剂的化合物，含有这些化合物的药物组合物，制备这些化合物的方法，用于制备用于合成这些化合物的新中间体的方法，以及制备含有这些化合物的组合物的方法化合物。本发明还涉及这些化合物和组合物用于调节血压或胃排空或治疗帕金森病，焦虑，抑郁或精神病的用途。化合物具有式（1），其中符号具有说明书中给出的含义。

9. 发明授权

US07186741B2 Neurotensin active 2,3,diaryl-pyrazolidine derivatives 有权
标题翻译：神经降压素活性2,3，二芳基 - 吡唑烷衍生物
公开(公告)号：US07186741B2
公开(公告)日：2007-03-06
申请号：US10490549
申请日：2003-03-17
申请人： Roelof W. Feenstra , Josephus H. M. Lange , Maria L. Pras-Raves , Cornelis G. Kruse , Herman H. van Stuivenberg , Tinka Tuinstra , Hiskias Keizer
发明人： Roelof W. Feenstra , Josephus H. M. Lange , Maria L. Pras-Raves , Cornelis G. Kruse , Herman H. van Stuivenberg , Tinka Tuinstra , Hiskias Keizer
IPC分类号： A61K31/415 , C07D231/04 , C07D401/04
CPC分类号： C07D401/04 , C07D231/04
摘要： The invention relates to a group of novel 2,3 diaryl-pyparazolidine derivatives having formula (1). The symbols used in formula (1) have the meanings given in the specification. The compounds have inhibiting activity on enzymes which degrade the neuropeptide neurotensin and can be used for the treatment of affections and diseases caused by disturbances of the neurotensin mediated transmission.
摘要翻译：本发明涉及一组具有式（1）的2,3-二芳基 - 吡唑烷衍生物。式（1）中使用的符号具有说明书中给出的含义。这些化合物对降解神经肽神经丝氨酸的酶具有抑制活性，可用于治疗由神经降压素介导的传播紊乱引起的感染和疾病。

10. 发明授权

US06214829B1 Piperazine compounds, their preparation, and methods of using them 有权
标题翻译：哌嗪化合物，它们的制备方法和使用它们的方法
公开(公告)号：US06214829B1
公开(公告)日：2001-04-10
申请号：US09144076
申请日：1998-08-31
申请人： Roelof W. Feenstra , Gerben M. Visser , Cornelis G. Kruse , Martinus T. M. Tulp , Stephen K. Long
发明人： Roelof W. Feenstra , Gerben M. Visser , Cornelis G. Kruse , Martinus T. M. Tulp , Stephen K. Long
IPC分类号： A61K31496
CPC分类号： C07D263/58 , C07D215/38 , C07D265/36 , C07D401/12 , C07D409/12
摘要： Novel piperazine and piperidine derivative compounds having interesting and advantageous pharmacological properties. The disdosed compounds have the general formula (a) and salts thereof. These compounds have high affinity for both the dopamine D2 receptors and serotonine 5-HT1A receptors, rendering them useful for the treatment of CNS-disorders, in particular schizophrenia.
摘要翻译：新颖的哌嗪和哌啶衍生化合物具有有趣和有利的药理学性质。所述化合物具有通式（a）及其盐。这些化合物对多巴胺D2受体和5-羟色胺5-HT 1A受体具有高亲和力，使其可用于治疗中枢神经系统疾病，特别是精神分裂症。

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