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1. 发明申请

US20110237569A1 SPIRO AZEPANE-OXAZOLIDINONES AS Kv1.3 POTASSIUM CHANNEL BLOCKERS 有权
标题翻译： SPIRO AZEPANE-OXAZOLIDINONES作为Kv1.3钾通道阻断剂
公开(公告)号：US20110237569A1
公开(公告)日：2011-09-29
申请号：US13133042
申请日：2009-12-10
申请人： Pieter Smid , Michael Mlinaric , Konrad F. Koehler , Sara Nunez Garcia , Elmar Wegener , Josephus H.M. Lange
发明人： Pieter Smid , Michael Mlinaric , Konrad F. Koehler , Sara Nunez Garcia , Elmar Wegener , Josephus H.M. Lange
IPC分类号： A61K31/55 , C07D498/10 , A61P3/10 , A61P37/02 , A61P3/04
CPC分类号： C07D498/10
摘要： This invention concerns Spiro azepane-ox-azolidinones as voltage gated Kv1.3 potassium channel blockers, pharmaceutical compositions containing these compounds, methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in the treatment of diabetes, psoriasis, obesity, transplant rejection and inflammatory neuropathies, including T-cell mediated autoimmune diseases such as rheumatoid arthritis and multiple sclerosis. The compounds have formula (1): wherein R1, R2, (R3)n, and (R4)m have the meanings given in the specification.
摘要翻译：本发明涉及作为电压门控的Kv1.3钾通道阻滞剂的螺氮氮杂环庚烷 - 恶唑烷酮，含有这些化合物的药物组合物，制备化合物的方法，制备用于其合成的新中间体的方法和制备组合物的方法。本发明还涉及这些化合物和组合物的用途，特别是它们在将它们施用于患者以在治疗糖尿病，银屑病，肥胖症，移植排斥和炎性神经病中的治疗效果方面的用途，包括T细胞介导的自身免疫性疾病作为类风湿性关节炎和多发性硬化。化合物具有式（1）：其中R1，R2，（R3）n和（R4）m具有本说明书中给出的含义。

2. 发明授权

US08575148B2 Spiro azepane-oxazolidinones as Kv1.3 potassium channel blockers 有权
标题翻译：螺氮氮杂环恶唑烷酮作为Kv1.3钾通道阻滞剂
公开(公告)号：US08575148B2
公开(公告)日：2013-11-05
申请号：US13133042
申请日：2009-12-10
申请人： Pieter Smid , Michael Mlinaric , Konrad F. Koehler , Sara Nuñez Garcia , Elmar Wegener , Josephus H. M. Lange
发明人： Pieter Smid , Michael Mlinaric , Konrad F. Koehler , Sara Nuñez Garcia , Elmar Wegener , Josephus H. M. Lange
IPC分类号： A61P3/10 , A61P29/00 , A61K31/55 , C07D498/10
CPC分类号： C07D498/10
摘要： This invention concerns spiro azepane-ox-azolidinones as voltage gated Kv1.3 potassium channel blockers, pharmaceutical compositions containing these compounds, methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in the treatment of diabetes, psoriasis, obesity, transplant rejection and inflammatory neuropathies, including T-cell mediated autoimmune diseases such as rheumatoid arthritis and multiple sclerosis. The compounds have formula (1): wherein R1, R2, (R3)n, and (R4)m have the meanings given in the specification.
摘要翻译：本发明涉及作为电压门控Kv1.3钾通道阻断剂的螺氮氮杂环庚烷 - 恶唑烷酮，含有这些化合物的药物组合物，制备化合物的方法，制备用于其合成的新中间体的方法和制备组合物的方法。本发明还涉及这些化合物和组合物的用途，特别是它们在将它们施用于患者以在治疗糖尿病，银屑病，肥胖症，移植排斥和炎性神经病中的治疗效果方面的用途，包括T细胞介导的自身免疫性疾病作为类风湿性关节炎和多发性硬化。化合物具有式（1）：其中R1，R2，（R3）n和（R4）m具有本说明书中给出的含义。

3. 发明申请

US20060122177A1 Phenylpiperazines with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites 审中-公开
标题翻译：具有与多巴胺-D2受体的亲合力和5-羟色胺再摄取位点的组合的苯基哌嗪
公开(公告)号：US20060122177A1
公开(公告)日：2006-06-08
申请号：US11294611
申请日：2005-12-06
申请人： Roelof Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
发明人： Roelof Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
IPC分类号： A61K31/538 , A61K31/496 , C07D413/02 , C07D405/02 , C07D403/02
CPC分类号： C07D263/58 , C07D307/79 , C07D319/18
摘要： The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors and to methods for the preparation of these compounds. 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.
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受体的亲和性以及制备这些化合物的方法。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。化合物具有通式（1），其中符号具有说明书中给出的含义。

4. 发明申请

US20060122175A1 Benzdioxane piperazine derivatives with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites 审中-公开
标题翻译：具有对多巴胺-D2受体的亲合力和5-羟色胺再摄取位点的组合的二恶烷哌嗪衍生物
公开(公告)号：US20060122175A1
公开(公告)日：2006-06-08
申请号：US11294610
申请日：2005-12-06
申请人： Roelof Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
发明人： Roelof Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
IPC分类号： A61K31/5415 , A61K31/538 , A61K31/498 , A61K31/496 , C07D417/14 , C07D413/14 , C07D405/14 , C07D403/14
CPC分类号： C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to a group of novel 3-(2-piperidin-4-yl-ethyl)-1H-indole derivatives with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors and to methods for the preparation of these compounds. 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.
摘要翻译：本发明涉及一种具有双重作用方式的新型3-（2-哌啶-4-基 - 乙基）-1H-吲哚衍生物：5-羟色胺再摄取抑制和对多巴胺-D2- / >受体和制备这些化合物的方法。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。化合物具有通式（1），其中符号具有说明书中给出的含义。

5. 发明授权

US08796262B2 Fused heterocyclic derivatives as S1P modulators 有权
标题翻译：稠合杂环衍生物作为S1P调节剂
公开(公告)号：US08796262B2
公开(公告)日：2014-08-05
申请号：US13808908
申请日：2011-07-08
申请人： Pieter Smid , Wouter I. Iwema Bakker , Hein K. A. C. Coolen , Leonardus A. J. M. Sliedregt , Maria J. P. van Dongen , Jacobus A. J. den Hartog , Adrian Hobson
发明人： Pieter Smid , Wouter I. Iwema Bakker , Hein K. A. C. Coolen , Leonardus A. J. M. Sliedregt , Maria J. P. van Dongen , Jacobus A. J. den Hartog , Adrian Hobson
IPC分类号： A01N43/00 , A01N43/46 , A61K31/55 , C07D495/04 , C07D513/04 , C07D491/048 , C07D487/04 , C07D471/04 , C07D491/04 , C07D498/04
CPC分类号： C07D491/048 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： This invention relates to new fused heterocyclic derivatives having affinity to S1P receptors, a pharmaceutical composition containing said compounds, as well as the use of said compounds for the preparation of a medicament for treating, alleviating or preventing diseases and conditions in which any S1P receptor is involved or in which modulation of the endogenous S1P signaling system via any S1P receptor is involved.
摘要翻译：本发明涉及对S1P受体具有亲和性的新的稠合杂环衍生物，含有所述化合物的药物组合物，以及所述化合物在制备用于治疗，缓解或预防任何S1P受体是涉及或参与通过任何S1P受体调节内源性S1P信号传导系统。

6. 发明申请

US20060122206A1 Tetrahydropyridin-4-yl indoles with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites 有权
标题翻译：具有对多巴胺-D2受体和5-羟色胺再摄取位点的亲和力的组合的四氢吡啶-4-基吲哚
公开(公告)号：US20060122206A1
公开(公告)日：2006-06-08
申请号：US11294657
申请日：2005-12-06
申请人： Roelof Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
发明人： Roelof Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
IPC分类号： A61K31/513 , C07D403/14
CPC分类号： C07D401/14
摘要： The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin-4-yl indoles of the formula. and tautomers, stereoisomers, prodrugs, N-oxides, pharmacologically acceptable salts, hydrates and solvates thereof, wherein: R1 is hydrogen, halogen, alkyl(C1-3) or alkoxy(C1-3), CN or CF3, R2 is hydrogen or alkyl(C1-3), R3 is hydrogen or alkyl(C1-3), Z is hydrogen or alkyl(C1-3), alkoxy(C1-3) or alkylthio(C1-3), A is hydrogen or alkyl(C1-3), or A and Z together form a saturated or (partly) unsaturated 5- or 6-membered ring which may be substituted with halogen, alkyl (C1-3) or phenyl, in which ring Z represents carbon, sulfur of nitrogen.
摘要翻译：本发明涉及一组具有双重作用方式的新的四氢吡啶-4-基吲哚：5-羟色胺再摄取抑制和对多巴胺-D 2受体的亲和性，制备这些化合物的方法和涉及可用于合成所述四氢吡啶-4-基吲哚的新型中间体。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。本发明涉及下式的新的四氢吡啶-4-基吲哚。和其互变异构体，立体异构体，前药，N-氧化物，其药理学上可接受的盐，水合物和溶剂化物，其中：R 1是氢，卤素，烷基（C 1-3 - 或烷氧基（C 1-3 - ），CN或CF 3 R 2，R 2是氢或烷基（C 1-3 - R 3是氢或烷基（C 1-3），Z是氢或烷基（C 1-3），烷氧基（C 1-3-3）或烷硫基（C 1-3-3），A是氢或烷基（C 1-3-3），或A和Z一起形成饱和或（部分）不饱和的5或6元环，其可被卤素，烷基（C 1-3-3）或苯基取代，其中环Z表示碳，硫氮。

7. 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。

8. 发明申请

US20070066634A2 TETRAHYDROPYRIDIN-4-YL INDOLES WITH A COMBINATION OF AFFINITY FOR DOPAMINE-D2 RECEPTORS AND SEROTONIN REUPTAKE SITES 有权
标题翻译：具有多巴胺D2受体和丝氨酸蛋白酶重复位点的亲和力组合的四氢吡啶并[4-YL]吲哚
公开(公告)号：US20070066634A2
公开(公告)日：2007-03-22
申请号：US11294657
申请日：2005-12-06
申请人： Roelof van Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
发明人： Roelof van Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
IPC分类号： A61K31/513 , C07D403/14
CPC分类号： C07D401/14
摘要： The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin-4-yl indoles of the formula. and tautomers, stereoisomers, prodrugs, N-oxides, pharmacologically acceptable salts, hydrates and solvates thereof, wherein: R1 is hydrogen, halogen, alkyl(C1-3) or alkoxy(C1-3), CN or CF3, R2 is hydrogen or alkyl(C1-3), R3 is hydrogen or alkyl(C1-3), Z is hydrogen or alkyl(C1-3), alkoxy(C1-3) or alkylthio(C1-3), A is hydrogen or alkyl(C1-3), or A and Z together form a saturated or (partly) unsaturated 5- or 6- membered ring which may be substituted with halogen, alkyl (C1-3) or phenyl, in which ring Z represents carbon, sulfur of nitrogen.
摘要翻译：本发明涉及一组具有双重作用方式的新的四氢吡啶-4-基吲哚：5-羟色胺再摄取抑制和对多巴胺-D 2受体的亲和性，制备这些化合物的方法和涉及可用于合成所述四氢吡啶-4-基吲哚的新型中间体。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。本发明涉及下式的新的四氢吡啶-4-基吲哚。和其互变异构体，立体异构体，前药，N-氧化物，其药理学上可接受的盐，水合物和溶剂化物，其中：R 1是氢，卤素，烷基（C 1-3 - 或烷氧基（C 1-3 - ），CN或CF 3 R 2，R 2是氢或烷基（C 1-3 - R 3是氢或烷基（C 1-3），Z是氢或烷基（C 1-3），烷氧基（C 1-3-3）或烷硫基（C 1-3-3），A是氢或烷基（C 1-3-3），或A和Z一起形成饱和或（部分）不饱和的5-或6-元环，其可以被卤素，烷基（C 1-3-3）或苯基取代，其中环Z表示碳，硫氮。

9. 发明申请

US20130203737A1 FUSED HETEROCYCLIC DERIVATIVES AS S1P MODULATORS 有权
公开(公告)号：US20130203737A1
公开(公告)日：2013-08-08
申请号：US13808908
申请日：2011-07-08
申请人： Pieter Smid , Wouter I. Iwema Bakker , Hein K.A.C. Coolen , Leonardus A.J.M. Sliedregt , Maria J.P. van Dongen , Jacobus A.J. den Hartog
发明人： Pieter Smid , Wouter I. Iwema Bakker , Hein K.A.C. Coolen , Leonardus A.J.M. Sliedregt , Maria J.P. van Dongen , Jacobus A.J. den Hartog
IPC分类号： C07D513/04 , C07D495/04 , C07D487/04 , C07D471/04 , C07D491/048 , C07D498/04
CPC分类号： C07D491/048 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to a fused heterocyclic derivative of the formula (I) wherein R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl, each optionally substituted with CN or one or more fluoro atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl optionally substituted with one or more fluoro atoms, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, dimethylamino, and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen, and phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, Z is a linking group —W—(Cn-alkylene)-T- wherein W is attached to R1 and selected from a bond, —O—, —CO—, —S—, —SO—, —SO2—, —NH—, —CH═CH—, —C(CF3)═CH—, —C≡C—, —CH2—O—, —O—CO—, —CO—O—, —CO—NH—, —NH—CO— and trans-cyclopropylene; n is an integer from 0 to 10; and T is attached to the phenylene/pyridyl moiety and selected from a bond, —O—, —S—, —SO—, —SO2—, —NH—, —CO—, —C═C—, —C≡C—, and trans-cyclopropylene; R2 is H or one or more substituents independently selected from cyano, halogen, (1-4C)alkyl optionally substituted with one or more halogen atoms, or (1-4C)alkoxy optionally substituted with one or more halogen atoms; ring structure A may contain one nitrogen atom; X is selected from C or N; if X is C, R3 is selected from H and (1-4C)alkyl, otherwise R3 is not present; Y is selected from NH, O and S; structure Q is a 5-, 6- or 7-membered cyclic amine; and R4 is (1-4C)alkylene-R5 wherein one or more carbon atoms in the alkylene group may independently be substituted with one or more halogen atoms or with (CH2)2 to form a cyclopropyl moiety, or R4 is (3-6C)cycloalkylene-R5, —CH2-(3-6C)cycloalkylene-R5, (3-6C)cycloalkylene-CH2-R5 or —CO—CH2-R5, wherein R5 is —OH, —PO3H2, —OPO3H2, —COOH, —COO(1-4C)alkyl or tetrazol-5-yl; or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (any) S1P receptor(s) is (are) involved or in which modulation of the endogenous S1P signaling system via any S1P receptor is involved.

10. 发明授权

US07371769B2 Tetrahydropyridin-4-yl indoles with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites 有权
标题翻译：具有对多巴胺-D2受体和5-羟色胺再摄取位点的亲和力的组合的四氢吡啶-4-基吲哚
公开(公告)号：US07371769B2
公开(公告)日：2008-05-13
申请号：US11294657
申请日：2005-12-06
申请人： Roelof van Hes , Pieter Smid , Cornelis G. Kruse , Martinus Th. M. Tulp
发明人： Roelof van Hes , Pieter Smid , Cornelis G. Kruse , Martinus Th. M. Tulp
IPC分类号： A01N43/64 , A61K31/41 , C07D209/04
CPC分类号： C07D401/14
摘要： The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect.The invention relates to novel tetrahydropyridin-4-yl indoles of the formula. and tautomers, stereoisomers, prodrugs, N-oxides, pharmacologically acceptable salts, hydrates and solvates thereof, wherein: R1 is hydrogen, halogen, alkyl(C1-3) or alkoxy(C1-3), CN or CF3, R2 is hydrogen or alkyl(C1-3), R3 is hydrogen or alkyl(C1-3), Z is hydrogen or alkyl(C1-3), alkoxy(C1-3) or alkylthio(C1-3), A is hydrogen or alkyl(C1-3), or A and Z together form a saturated or (partly) unsaturated 5- or 6-membered ring which may be substituted with halogen, alkyl (C1-3) or phenyl, in which ring Z represents carbon, sulfur of nitrogen.
摘要翻译：本发明涉及一组具有双重作用方式的新的四氢吡啶-4-基吲哚：5-羟色胺再摄取抑制和对多巴胺-D 2受体的亲和性，制备这些化合物的方法和涉及可用于合成所述四氢吡啶-4-基吲哚的新型中间体。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。本发明涉及下式的新的四氢吡啶-4-基吲哚。和其互变异构体，立体异构体，前药，N-氧化物，其药理学上可接受的盐，水合物和溶剂化物，其中：R 1是氢，卤素，烷基（C 1-3 - 或烷氧基（C 1-3 - ），CN或CF 3 R 2，R 2是氢或烷基（C 1-3 - R 3是氢或烷基（C 1-3），Z是氢或烷基（C 1-3），烷氧基（C 1-3-3）或烷硫基（C 1-3-3），A是氢或烷基（C 1-3-3），或A和Z一起形成饱和或（部分）不饱和的5或6元环，其可被卤素，烷基（C 1-3-3）或苯基取代，其中环Z表示碳，硫氮。

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