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1. 发明专利

JP2006052181A New quinoline derivative 审中-公开
标题翻译：新的喹啉衍生物
公开(公告)号：JP2006052181A
公开(公告)日：2006-02-23
申请号：JP2004235924
申请日：2004-08-13
申请人： Actelion Pharmaceuticals Ltd , アクテリオンファマシューティカルズリミテッドActelion Pharmaceuticals Ltd
发明人： AISSAOUI HAMED , BINKERT CHRISTOPH , MARTIN CLAUZEL , MATHYS BORIS , MUELLER KLAUS , NAYLER OLIVER , SCHERZ MICHAEL , VELKER JOERG , WELLER THOMAS
IPC分类号： C07D401/12 , A61K31/4709 , A61P1/16 , A61P3/10 , A61P5/14 , A61P7/06 , A61P7/08 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/08 , A61P13/12 , A61P15/08 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/16 , A61P29/00 , A61P31/04 , A61P35/00 , A61P43/00 , C07D409/14 , C07D417/14
摘要： PROBLEM TO BE SOLVED: To provide a new 4-(piperidinyl- and pyrrolidinyl-alkyl-ureido)-quinoline derivative, and to provide a medicinal composition thereof. SOLUTION: A 4-(piperidinyl- and pyrrolidinyl-alkyl-ureido)-quinoline derivative of general formula 1 [Py is a substituted pyridine or the like; X is an aryl, an aryl-O- or the like; Y is -C(R 4 )(R 5 )(CH 2 ) m -, or the like; Z is H, or the like; R 1 is H or an alkyl; R 4 and R 5 are H, an alkyl or the like], and the use of the derivative as an active ingredient for preparing a medicinal composition. The above-mentioned compound can inhibit the action of urotensin II, and can thereby be used for treating various diseases such as hypertension and cardiac failures related to the increases in the constriction and proliferation of blood vessels by the actions of urotensin II, and for other disease states. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供新的4-（哌啶基和吡咯烷基 - 烷基 - 脲基） - 喹啉衍生物，并提供其药物组合物。解决方案：通式1的4-（哌啶基 - 和吡咯烷基 - 烷基 - 脲基） - 喹啉衍生物[Py是取代的吡啶等; X是芳基，芳基-O-等; Y是-C（R 4 SP 3）（R 2 SP 3）（CH 2 SB 2），或者类似物 ; Z是H等; R 1是H或烷基; R 4 和R 5 是H，烷基等]，以及使用该衍生物作为制备药物组合物的活性成分。上述化合物可以抑制尿素转运蛋白II的作用，因此可以用于治疗各种疾病如高血压和与血管紧张素和增殖的增加有关的心脏衰竭，这些作用是通过尿激肽素II的作用，以及其他疾病状态。版权所有（C）2006，JPO＆NCIPI

2. 发明专利

JP2008081504A New thiazolidin-4-one derivative 有权
标题翻译：新的噻唑烷-4-酮衍生物
公开(公告)号：JP2008081504A
公开(公告)日：2008-04-10
申请号：JP2007279142
申请日：2007-10-26
申请人： Actelion Pharmaceuticals Ltd , アクテリオンファーマシューティカルズリミテッドActelion Pharmaceuticals Ltd
发明人： BINKERT CHRISTOPH , BOLLI MARTIN , MATHYS BORIS , MUELLER KLAUS , SCHERZ MICHAEL , NAYLER OLIVER
IPC分类号： A61K31/426 , A61K31/427 , A61P1/04 , A61P3/10 , A61P13/12 , A61P17/06 , A61P19/02 , A61P21/04 , A61P25/00 , A61P29/00 , A61P35/04 , A61P37/00 , A61P37/08 , C07D277/20 , C07D277/54 , C07D417/06
CPC分类号： C07D277/54 , A61K31/426 , C07D277/20 , C07D277/42 , C07D417/06
摘要： PROBLEM TO BE SOLVED: To provide a pharmaceutical composition containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system, and to provide a new thiazolidin-4-one derivative excellent in use as a pharmacologically active compound. SOLUTION: The invention relates to the new thiazolidin-4-one derivatives of general formula (I) and their use as an active ingredient in preparation of a pharmaceutical composition, a method for preparing the compound of the general formula (I), the pharmaceutical composition containing at least one of the derivatives, and to the use of them as an immunosuppressive agent containing the compositions alone or with other immunosuppressive agents. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供含有至少一种噻唑烷-4-酮衍生物的药物组合物，以预防或治疗与活化的免疫系统相关的病症，并提供使用优异的新的噻唑烷-4-酮衍生物作为药理活性化合物。解决方案：本发明涉及通式（I）的新噻唑烷-4-酮衍生物及其作为药物组合物制备中的活性成分的用途，制备通式（I）化合物的方法，，含有至少一种衍生物的药物组合物，以及它们作为单独使用组合物或与其它免疫抑制剂一起使用的免疫抑制剂。版权所有（C）2008，JPO＆INPIT

3. 发明申请

WO2004026836A8 1-PYRIDIN-4-YL-UREA DERIVATIVES 审中-公开
标题翻译： 1-吡啶-4-基尿素衍生物
公开(公告)号：WO2004026836A8
公开(公告)日：2005-05-12
申请号：PCT/EP0310154
申请日：2003-09-12
申请人： ACTELION PHARMACEUTICALS LTD , AISSAOUI HAMED , BINKERT CHRISTOPH , MATHYS BORIS , MUELLER CLAUS , NAYLER OLIVER , SCHERZ MICHAEL , WELLER THOMAS , VELKER JOERG , CLOZEL MARTINE
发明人： AISSAOUI HAMED , BINKERT CHRISTOPH , MATHYS BORIS , MUELLER CLAUS , NAYLER OLIVER , SCHERZ MICHAEL , WELLER THOMAS , VELKER JOERG , CLOZEL MARTINE
IPC分类号： C07D215/00 , C07D401/12
CPC分类号： C07D401/12
摘要： The invention relates to novel 1-pyridyn-4-yl urea derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as neurohormonal antagonists.
摘要翻译：本发明涉及新的1-吡啶-4-基脲衍生物和相关化合物及其在制备药物组合物中作为活性成分的用途。本发明还涉及相关方面，包括制备化合物的方法，含有一种或多种这些化合物的药物组合物，特别是它们作为神经激素拮抗剂的用途。

4. 发明申请

WO02076979A8 1,2,3,4-TETRAHYDROISOQUINOLINES DERIVATIVES AS UROTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为UROTENSIN II受体拮抗剂的1,2,3,4-四氢喹啉衍生物
公开(公告)号：WO02076979A8
公开(公告)日：2003-11-06
申请号：PCT/EP0203131
申请日：2002-03-20
申请人： ACTELION PHARMACEUTICALS LTD , AISSAOUI HAMED , BINKERT CHRISTOPH , CLOZEL MARTINE , MATHYS BORIS , MUELLER CLAUS , NAYLER OLIVER , SCHERZ MICHAEL , VELKER JOERG , WELLER THOMAS
发明人： AISSAOUI HAMED , BINKERT CHRISTOPH , CLOZEL MARTINE , MATHYS BORIS , MUELLER CLAUS , NAYLER OLIVER , SCHERZ MICHAEL , VELKER JOERG , WELLER THOMAS
IPC分类号： C07D491/056 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/4741 , A61K31/4745 , A61K31/55 , A61K45/00 , A61P3/10 , A61P5/14 , A61P7/00 , A61P7/06 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/08 , A61P13/12 , A61P15/10 , A61P21/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/02 , A61P27/06 , A61P27/16 , A61P29/02 , A61P31/04 , A61P35/00 , A61P43/00 , C07D401/12 , C07D403/12 , C07D405/14 , C07D407/14 , C07D471/02 , C07D471/04 , C07D491/04
CPC分类号： C07D401/12 , C07D405/14 , C07D471/04 , C07D491/04
摘要： The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as neurohormonal antagonists especially urotensin II antagonists.
摘要翻译：本发明涉及式（I）的新型1,2,3,4-四氢异喹啉衍生物及其相关化合物及其在制备药物组合物中作为活性成分的用途。本发明还涉及包括制备化合物的方法，包含这些化合物中的一种或多种的药物组合物，特别是其作为神经激素拮抗剂尤其是尿素保护素II拮抗剂的用途的相关方面。

5. 发明申请

WO02083641A3 AMINO-AZA-CYCLOHEXANES FOR THE TREATMENT OF MALARIA 审中-公开
标题翻译：用于治疗疟疾的氨基 - 氨基环己烷
公开(公告)号：WO02083641A3
公开(公告)日：2003-02-27
申请号：PCT/EP0203948
申请日：2002-04-09
申请人： ACTELION PHARMACEUTICALS LTD , BOSS CHRISTOPH , BINKERT CHRISTOPH , FISCHLI WALTER , MEYER SOLANGE , RICHARD-BILDSTEIN SYLVIA , STRICKNER PANJA , WELLER THOMAS
发明人： BOSS CHRISTOPH , BINKERT CHRISTOPH , FISCHLI WALTER , MEYER SOLANGE , RICHARD-BILDSTEIN SYLVIA , STRICKNER PANJA , WELLER THOMAS
IPC分类号： A61P33/06 , C07D211/58 , C07D401/12 , A61K31/506
CPC分类号： C07D401/12 , C07D211/58
摘要： The invention relates to novel compounds which are substituted amino-aza-cyclohexane derivatives of the general formula (I). The invention also concerns related aspects including pharmaceutical compositions containing one or more compounds of the general formula I and their use as medicaments for the treatment of protozoal infections, especially malaria.
摘要翻译：本发明涉及通式（I）的取代氨基 - 氮杂 - 环己烷衍生物的新化合物。本发明还涉及包含一种或多种通式I化合物的药物组合物及其作为用于治疗原生动物感染，特别是疟疾的药物的用途的相关方面。

6. 发明申请

WO2004105738A3 USE OF TETRAHYDROPYRIDINE DERIVATIVES 审中-公开
标题翻译：四氢吡啶衍生物的使用
公开(公告)号：WO2004105738A3
公开(公告)日：2005-03-03
申请号：PCT/EP2004005064
申请日：2004-05-12
申请人： ACTELION PHARMACEUTICALS LTD , BUR DANIEL , FISCHLI WALTER , REMEN LUBOS , RICHARD-BILDSTEIN SYLVIA , WELLER THOMAS , BOSS CHRISTOPH , BINKERT CHRISTOPH , MEYER SOLANGE
发明人： BUR DANIEL , FISCHLI WALTER , REMEN LUBOS , RICHARD-BILDSTEIN SYLVIA , WELLER THOMAS , BOSS CHRISTOPH , BINKERT CHRISTOPH , MEYER SOLANGE
IPC分类号： A61K31/4418 , A61P33/06 , A61K31/415
CPC分类号： A61K31/4418
摘要： The invention relates to tetrahydropyridine derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of plasmepsin II.
摘要翻译：本发明涉及四氢吡啶衍生物及其相关化合物及其在制备药物组合物中作为活性成分的用途。本发明还涉及包括制备化合物的方法，含有一种或多种这些化合物的药物组合物，特别是其作为浆细胞素II抑制剂的用途的相关方面。

7. 发明申请

WO2004026836A3 1-PYRIDIN-4-YL-UREA DERIVATIVES 审中-公开
标题翻译： 1-吡啶-4-YL-UREA衍生物
公开(公告)号：WO2004026836A3
公开(公告)日：2005-01-20
申请号：PCT/EP0310154
申请日：2003-09-12
申请人： ACTELION PHARMACEUTICALS LTD , AISSAOUI HAMED , BINKERT CHRISTOPH , MATHYS BORIS , MUELLER CLAUS , NAYLER OLIVER , SCHERZ MICHAEL , WELLER THOMAS , VELKER JOERG , CLOZEL MARTINE
发明人： AISSAOUI HAMED , BINKERT CHRISTOPH , MATHYS BORIS , MUELLER CLAUS , NAYLER OLIVER , SCHERZ MICHAEL , WELLER THOMAS , VELKER JOERG , CLOZEL MARTINE
IPC分类号： C07D215/00 , C07D401/12
CPC分类号： C07D401/12
摘要： The invention relates to novel 1-pyridyn-4-yl urea derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as neurohormonal antagonists.
摘要翻译：本发明涉及新颖的1-吡啶-4-基脲衍生物及其相关化合物及其在制备药物组合物中作为活性成分的用途。本发明还涉及包括制备化合物的方法，含有一种或多种这些化合物的药物组合物，特别是其作为神经激素拮抗剂的用途的相关方面。

8. 发明专利

ES2421448T3 Derivados de piperazina como agentes contra la malaria 未知
公开(公告)号：ES2421448T3
公开(公告)日：2013-09-02
申请号：ES06809659
申请日：2006-10-20
申请人： ACTELION PHARMACEUTICALS LTD
发明人： BINKERT CHRISTOPH , BOSS CHRISTOPH , CORMINBOEUF OLIVIER , GRISOSTOMI CORINNA , MEYER SOLANGE
IPC分类号： C07D295/18 , C07D209/04 , C07D209/16 , C07D213/26 , C07D213/38 , C07D213/40 , C07D213/60 , C07D213/74 , C07D217/04 , C07D217/14 , C07D233/54 , C07D239/42 , C07D277/28 , C07D307/14 , C07D317/58
摘要： Un compuesto seleccionado del grupo que consiste en compuestos de piperazina de Fórmula I: en la que X representa -CH2- o un enlace; n representa el número entero 1; R1 representa alquilo; cicloalquilo; hidroxi-etilo; benzo[1,3]dioxolilo; fenilo que puede estar mono-sustituido conhalógeno, alquilo, alcoxi, -CF3, o alquil-carbonilo, o fenilo que está di- o tri-sustituido, en el que los sustituyentesestán seleccionados independientemente entre alquilo y halógeno; piridilo que puede estar mono-sustituido conhalógeno, alquilo, o -CF3; furanilo que puede estar mono-sustituido con metilo, hidroxi-metilo, o bromo, o furanilo queestá di-sustituido con alquilo; tienilo que puede estar mono-sustituido con metilo o cloro; pirimidinilo; isoquinolinilo;benzhidrilo; imidazolilo opcionalmente mono-sustituido con alquilo; o tiazolilo; o X representa -C(>=O)- y R1representa hidrógeno; R2 representa indolilo; imidazolilo opcionalmente mono-sustituido con alquilo; fenilo que puede estar mono-sustituidocon halógeno, alquilo, hidroxi, o ciano, o fenilo que está di-sustituido con halógeno; piridilo; benzotienilo; tiazolilo; otienilo; R3 representa indolilo; piridilo que puede estar mono-sustituido con alcoxi, alcoxi-alcoxi, -NR31R32, morfolino,piperidino, oxo-piperidinilo, oxo-pirrolidinilo, piridilo, o fenilo; o fenilo que está mono-sustituido con fenilo, piridilo,alquilo, alcoxi, dialquil-amino, morfolino, N-bencil-N-alquil-amino, (dialquil-amino)-alcoxi, fenil-alcoxi, o tetrahidroisoquinolinilo;o R3 representa el siguiente grupo:**Fórmula**

9. 发明专利

ES2352555T3 DERIVADOS DE 5-(BENC-(Z)-ILIDEN)TIAZOLIDIN-4-ONA COMO AGENTES INMUNOSUPRESORES. 未知
公开(公告)号：ES2352555T3
公开(公告)日：2011-02-21
申请号：ES04819591
申请日：2004-11-16
申请人： ACTELION PHARMACEUTICALS LTD
发明人： BOLLI MARTIN , MUELLER CLAUS , NAYLER OLIVER , SCHERZ MICHAEL , BINKERT CHRISTOPH , MATHYS BORIS
IPC分类号： C07D277/20 , A61K31/426 , A61K31/427 , A61P37/06 , C07D417/06
摘要： Composición farmacéutica que contiene por lo menos un derivado de tiazolidin-4-ona de Fórmula General (I) **(Ver fórmula)** en la cualR1 representa alquilo inferior; alquenilo inferior; cicloalquilo; 5,6,7,8-tetrahidronaft-1-ilo; 5,6,7,8-tetrahidronaft-2-ilo; un grupo fenilo; o un grupo fenilo independientemente mono-, di- o tri-sustituido con alquilo inferior, halógeno, alcoxi inferior o -CF3; R2 representa alquilo inferior; alilo; ciclopropilo; ciclobutilo; ciclopentilo; mono- o di-alquilamino inferior; R3 representa -O-CR7R8-CR9R10-(CR11R12)n-O-R13; R4 representa hidrógeno; hidroxi; alcoxi inferior; alquilo inferior o halógeno; R5 y R6 representa cada uno independientemente alquilo inferior; R7 representa hidrógeno, alquilo inferior o hidroximetilo; R8, R9, R11 y R12 representa cada uno independientemente hidrógeno o metilo; R10 representa hidrógeno o alquilo inferior; y en caso que n represente el número entero 1, R10 representa además alcoxi inferior, hidroxi, -NH2, -NHR5 o -NR5R6; R13 representa hidrógeno; alquilo inferior; hidroxicarbonil-alquilo inferior; 1-glicerilo; o 2-glicerilo; n representa el número entero 0 o 1; e isómeros configuracionales, enantiómeros ópticamente puros, mezclas de enantiómeros tales como racematos, diastereómeros, mezclas de diastereómeros, racematos diaesteroméricos, mezclas de racematos diastereoméricos y la forma meso, así como también sales farmacéuticamente aceptables, complejos con solventes y formas morfológicas, y material vehículo inerte; y en la cual los términos "alquilo inferior", "alcoxi inferior", "mono- o di-alquilamino inferior" y "alquenilo inferior" tienen los siguientes significados: "alquilo inferior", solo o en combinación con otros grupos, significa grupos saturados de cadena lineal o ramificada con uno a siete átomos de carbono; "alcoxi inferior" significa un grupo R-O, en el cual R es un alquilo inferior; "mono- o di alquilamino inferior" significa un grupo R'-NH- o R'-NR''-, en el cual R' y R'' son cada uno independientemente un alquilo inferior; y "alquenilo inferior", solo o en combinación con otros grupos, significa grupos de cadena lineal o ramificada que comprende una unión olefínica y tres a siete átomos de carbono.

10. 发明专利

DK1689726T3 5-(benz-(z)-yliden)-thiazolidin-4-on-derivater som immunsuppresserende midler 未知
公开(公告)号：DK1689726T3
公开(公告)日：2010-12-06
申请号：DK04819591
申请日：2004-11-16
申请人： ACTELION PHARMACEUTICALS LTD
发明人： BOLLI MARTIN , SCHERZ MICHAEL , MUELLER CLAUS , MATHYS BORIS , BINKERT CHRISTOPH , NAYLER OLIVER
IPC分类号： C07D277/20 , A61K31/426 , A61K31/427 , A61P37/06 , C07D417/06

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