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1. 发明专利

JP2011042653A Triazolo-quinoline derivative useful as adenosine receptor ligand 审中-公开
标题翻译：三唑醇衍生物作为腺苷受体配体有用
公开(公告)号：JP2011042653A
公开(公告)日：2011-03-03
申请号：JP2010200550
申请日：2010-09-08
申请人： Sanofi-Aventis , サノフィ−アベンティス
发明人： ARANYI PETER , BALAZS LASZLO , BATORI SANDOR , BENCE JUDIT , BOER KINGA , HAJDU FELIX , KAPUI ZOLTAN , MIKUS ENDRE , SZABO TIBOR , NAGY T LAJOS , TIMARI GEZA , URBAN-SZABO KATALIN , WALCZ ERZSEBET
IPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4738 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/28 , A61P27/06 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07B61/00 , C07D215/54 , C07D215/56
CPC分类号： C07D471/04 , C07D215/54 , C07D215/56
摘要： PROBLEM TO BE SOLVED: To provide a ligand having a triazolo-quinoline structure and showing a high selectivity to the A3 adenosine receptor.
SOLUTION: This specific triazolo-quinoline compound is expressed by formula (I).
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供具有三唑并喹啉结构并且对A3腺苷受体显示高选择性的配体。解决方案：该具体的三唑并喹啉化合物由式（I）表示。版权所有（C）2011，JPO＆INPIT

2. 发明申请

WO2008149168A1 TRIAZOLO [1, 5-A] QUINOLINES AS ADENOSINE A3 RECEPTOR LIGANDS 审中-公开
标题翻译：三唑醇[1，5-A]喹诺酮作为腺苷A3受体配体
公开(公告)号：WO2008149168A1
公开(公告)日：2008-12-11
申请号：PCT/HU2008000063
申请日：2008-06-02
申请人： SANOFI AVENTIS , SUSAN EDIT , BOER KINGA , KAPUI ZOLTAN , TIMARI GEZA , BATORI SANDOR , SZLAVIK ZOLTAN , MIKUS ENDRE , VARGANE SZEREDI JUDIT , FINET MICHEL , URBAN SZABO KATALIN , SZABO TIBOR
发明人： SUSAN EDIT , BOER KINGA , KAPUI ZOLTAN , TIMARI GEZA , BATORI SANDOR , SZLAVIK ZOLTAN , MIKUS ENDRE , VARGANE SZEREDI JUDIT , FINET MICHEL , URBAN SZABO KATALIN , SZABO TIBOR
IPC分类号： C07D215/58 , A61K31/4745 , A61P11/06 , A61P29/00 , C07D471/04 , C07F7/22
CPC分类号： C07D471/04
摘要： The present invention relates to the adenosine A3 receptor ligands of the general formula (I), within them favourably to the antagonists, to their salts, solvates, N-oxides and isomers, to the pharmaceutical compositions containing the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, to the use of the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, to the preparation of the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, as well as to the new intermediates of the general formula (II), (VI), (XI), (XII) and (XV), and to the preparation thereof.
摘要翻译：本发明涉及含有通式（I）的化合物的药物组合物，其通式（I）的腺苷A 3受体配体，其有利于拮抗剂，其盐，溶剂合物，N-氧化物和异构体，），它们的盐，溶剂合物，N-氧化物和异构体，通式（I）的化合物，其盐，溶剂合物，N-氧化物和异构体用于制备通式（I ），它们的盐，溶剂合物，N-氧化物和异构体，以及通式（II），（VI），（XI），（XII）和（XV）的新中间体及其制备。

3. 发明专利

HN2009003357A NUEVOS COMPUESTO LIGANDOS DEL RECEPTOR DE LA ADENOSINA A3 未知
公开(公告)号：HN2009003357A
公开(公告)日：2013-08-12
申请号：HN2009003357
申请日：2009-12-04
申请人： SANOFI AVENTIS
发明人： SUSAN EDIT , BOER KINGA , KAPUI ZOLTAN , TIMARI GEZA , BATORI SANDOR , SZLAVIK ZOLTAN , MIKUS ENDRE , VARGANE SZEREDI JUDIT , FINET MICHEL , URBAN SZABO KATALIN , SZABO TIBOR
IPC分类号： C07D215/58 , A61K31/4745 , A61P11/06
摘要： LA PRESENTE INVENCION SE REFIERE A LOS LIGANDOS DEL RECEPTOR DE ADENOSIMA A3, DE FORMULA GENERAL I) DENTRO DE ELLOS LOS FAVORABLES A LOS ANTAGONISTAS, SUS SALES, SOLVATOS, N-OXIDOS E ISOMERICOS, A LAS COMPOSICIONES FARMACEUTICAS QUE CONTIENEN GENERAL I) SUS SALES, SOLVATOS, N- OXIDOS E ISOMEROS, A LA PREPARACION DE LOS COMPUESTOS DE FORMULA GENERAL I) SUS SALES, SOLVATOS, N- OXIDOS E ISOMEROS , ASI COMO A LOS NUEVOS INTERMEDIARIOS DE FORMULA GENERAL. (II), (VI), (XI), (XII), Y (XV) Y A LA PREPARACION DE ELLOS.

4. 发明专利

RU2489432C2 ТРИАЗОЛО[1,5-a]ХИНОЛИНЫ В КАЧЕСТВЕ ЛИГАНДОВ РЕЦЕПТОРА АДЕНОЗИНА А3 未知
公开(公告)号：RU2489432C2
公开(公告)日：2013-08-10
申请号：RU2009149518
申请日：2008-06-02
申请人： SANOFI AVENTIS
发明人： SHUSHAN EHDIT , BOER KINGA , KAPUI ZOL TAN , TIMARI GEZA , BATORI SHANDOR , SLAVIK ZOL TAN , MIKUSH EHNDRE , VARGANE SEREDI JUDIT , FINE MISHEL , URBAN SABO KATALIN , SABO TIBOR
IPC分类号： C07D471/04 , A61K31/4745 , A61P11/06 , A61P29/00 , C07D215/58 , C07F7/22
摘要： Описываютсяновыепроизводныетриазоло[1,5-а]хинолинаобщейформулы (I)гдеХ означает -NH-; R-циано;Rи RозначаютН илиметил; R- фенил, возможнозамещенный, или 5- или 6-членныйгетероциклил;Rозначаетфенилилиодинатомазота, содержащий 6-членныйгетероциклил;R- одинатомазотасодержащий 6-членныйгетероциклилилигруппуформулы (а),где Rи RнезависимоозначаютС-циклоалкилилиСалкил; илигруппуформулы (b)где Rи RозначаютСалкил;Z - кислородилигруппа -NR-, где R- водород. Салкил, Сциклоалкил, бензил, -СН-ацетил, -СН-СН-О-СН-СНилиацетил;W обозначаетатомазотаилигруппу -СН-;m ио означают 2; p и r означаютнольили 1; t означаетноль; способыихполучения, новыепромежуточныесоединенияописываемыхспособовполучения, фармацевтическаякомпозиция, содержащаяданныесоединения, иприменениесоединенийобщейформулы (I) иихфармацевтическиприемлемыхсолейв качествелигандоврецепторааденозина A3 прилеченииразличныхзаболеваний. 2 табл., 4 ил.

5. 发明专利

UA99463C2 未知
公开(公告)号：UA99463C2
公开(公告)日：2012-08-27
申请号：UAA200913976
申请日：2008-06-02
申请人： SANOFI AVENTIS
发明人： SUSAN EDIT , BOER KINGA , KAPUI ZOLTAN , TIMARI GEZA , BATORI SANDOR , SZLAVIK ZOLTAN , MIKUS ENDRE , VARGANE SZEREDI JUDIT , FINET MICHEL , URBAN SZABO KATALIN , SZABO TIBOR
IPC分类号： C07D215/58 , A61K31/4745 , A61P11/06 , A61P29/00 , C07D471/04 , C07F7/22
摘要： ДанноеизобретениекасаетсялигандовАрецептороваденозинаобщейформулы(I),срединихпреимущественноантагонистов, ихсолей, сольватов, N-оксидови изомеров, фармацевтическихкомпозиций, которыесодержатсоединенияобщейформулы (I), ихсоли, сольваты, N-оксидыи изомеры, применениясоединенийобщейформулы (I), ихсолей, сольватов, N-оксидови изомеров, получениясоединенийобщейформулы (I), ихсолей, сольватов, N-оксидови изомеров, атакженовыхпромежуточныхсоединенийобщихформул (II), (VI), (XI), (XII) и (XV) иихполучения.

6. 发明专利

HK1138581A1 TRIAZOLO [1, 5-A] QUINOLINES AS ADENOSINE A3 RECEPTOR LIGANDS 未知
公开(公告)号：HK1138581A1
公开(公告)日：2010-08-27
申请号：HK10104249
申请日：2010-04-29
申请人： SANOFI AVENTIS
发明人： SUSAN EDIT , BOER KINGA , KAPUI ZOLTAN , TIMARI GEZA , BATORI SANDOR , SZLAVIK ZOLTAN , MIKUS ENDRE , VARGANE SZEREDI JUDIT , FINET MICHEL , URBAN SZABO KATALIN , SZABO TIBOR
IPC分类号： A61K20060101 , A61P20060101 , C07D20060101 , C07F20060101

7. 发明专利

CA2505910C IMIDAZOQUINOLINE DERIVATIVES AS ADENOSINE A3 RECEPTOR LIGANDS 未知
公开(公告)号：CA2505910C
公开(公告)日：2010-07-13
申请号：CA2505910
申请日：2003-11-11
申请人： SANOFI AVENTIS
发明人： ARANYI PETER , BALAZS LASZLO , BALOGH MARIA , BATORI SANDOR , T NAGY LAJOS , TIMARI GEZA , BOER KINGA , KAPUI ZOLTAN , MIKUS ENDRE , GERBER KATALIN , VARGANE SZEREDI JUDIT , URBAN-SZABO KATALIN , WALCZ ERZSEBET
IPC分类号： C07D471/04 , A61K31/415 , A61P3/00 , A61P9/00 , A61P11/00 , A61P13/12 , A61P17/00 , A61P25/00 , A61P29/00 , A61P35/00 , C07D221/00 , C07D235/00
摘要： Compounds of general formula (I), wherein X, Z, R1-R10, m, n, o, p, r as described in the description are strong adenosine A3 receptor ligands preferably antagonists.

8. 发明专利

MEP19108A AMINOQUINOLINE DERIVATIVES AND THEIR USE AS ADENOSINE A3 LIGANDS 未知
公开(公告)号：MEP19108A
公开(公告)日：2010-06-10
申请号：MEP19108
申请日：2004-07-23
申请人： SANOFI AVENTIS
发明人： ARANYI PETER , BATORI SANDOR , TIMARI GEZA , BOER KINGA , KAPUI ZOLTAN , MIKUS ENDRE , URBAN-SZABO KATALIN , GERBER KATALIN , VARGANE SZEREDI JUDIT , FINET MICHEL
IPC分类号： A61K31/47 , A61P11/00 , C07C229/50 , C07C229/60 , C07D215/48 , C07D215/54 , C07D265/26 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D491/04
摘要： Aminoquinoline derivatives (I) and their salts, solvates, isomers (tautomers, desmotrops, optically active isomers) and their salts or solvates are new. Aminoquinoline derivatives of formula (I) and their salts, solvates, isomers (tautomers, desmotrops, optically active isomers) and their salts or solvates are new. [Image] R 1>H or 1-4C alkyl; R 2>H or 1-4C alkyl; R 3>H, 1-4C alkyl, 3-6C cycloalkyl, phenyl, thienyl or furyl (optionally substituted by 1-4C alkyl, 1-4C alkoxy or halo), 5-6 membered heteroaromatic ring containing 1-3N, 5 membered heteroaromatic ring containing O, N or S (optionally substituted with 1-4C alkyl, 1-4C alkoxy or halo); R 4>, R 5>H, 3-6C cycloalkyl or 1-4C alkyl (optionally containing amino group substituted by 1-2 1-4C alkyl, OH, carboxy or alkyl group substituted with 1-4C alkyl), benzyl, -SO 2OH or 1-4C acyl; NR 4>R 5>a group of formula (a); R 7>, R 8>H, 1-4C alkyl or 3-6C cycloalkyl; R 6>H, 1-4C alkyl, phenyl, benzyl, thienyl or furyl (optionally substituted by methylenedioxy or 1 or more 1-4C alkyl, 1-4C alkoxy, hydroxy, trifluoromethyl, cyano or halo), or 5 or 6 membered heteroaromatic ring (containing either 1-3 N, 1 N and 1 O or 1 N and 1 S, and optionally substituted by 1 or more 1-4C alkyl, 1-4C alkoxy or halo); X : CH 2, NH, NR 9>, S, O, sulfo or sulfoxy; R 9>1-4C alkyl or 3-6C cycloalkyl; Z : O, S, CHR 1> 0> or NR 1>; R 1> 0>H, 1-4C alkyl or 3-6C cycloalkyl; R 1> 1>H, 1-4C alkyl, 3-6C cycloalkyl, SO 2OH or 1-4C acyl; n : 0-2; m, o : 1-3; and p, r : 0-1. Provided that either: (1) R 4> and R 5> are H, 3-6C cycloalkyl or 1-4C alkyl optionally contains amino group substituted 1-2 1-4C alkyl, OH, carboxy or alkyl group substituted with 1-4C alkyl; (2) R 4> is H, 1-4C alkyl or benzyl and R 5> is H, -SO 2OH or 1-4C acyl; or (3) NR 4>R 5> is (a). [Image] Independent claims are also included for the following: (1) preparation of (I); and (2) new compounds of formulae (II''), (III''), (IV''), (V''), (VI''), (VII''), (VIII'') and (XIII''). [Image] ACTIVITY : Cardiant; Nephrotropic; Respiratory-Gen.; CNS-Gen.; Cytostatic; Ophthalmological; Antiinflammatory; Antiasthmatic; Vasotropic; Antidepressant; Antiarrhythmic; Antiparkinsonian; Nootropic; Antiallergic; Dermatological; Antiarthritic; Immunosuppressive; Gastrointestinal-Gen.; Anabolic; Hypertensive; Antipsoriatic; Antirheumatic; Neuroprotective; Antidiabetic. MECHANISM OF ACTION : Adenosine A3 ligands. (I) were tested for adenosine A3 ligand activity in HEK-293 cells. The inhibitory constant value of (I) was 0.5-15 nM.

9. 发明专利

DOP2009000276A TRIAZOL [1,5-A] QUINOLINAS COMO LIGANDOS DEL RECEPTOR DE LA ADENOSINA A3 未知
公开(公告)号：DOP2009000276A
公开(公告)日：2010-01-31
申请号：DO2009000276
申请日：2009-12-04
申请人： SANOFI AVENTIS
发明人： SUSAN EDIT , BOER KINGA , KAPUL ZOLTAN , TIMARI GEZA , BATORI SANDOR , SZLAVIK ZOLTAN , MIKUS ENDRE , VARGABE SZEREDI JUDIT , FINET MICHAEL , SZABO KATALIN URBAN , SZABO TIBOR
IPC分类号： C07D215/58
摘要： La presente invencion se refiere a los ligandos del receptor de adenosina A3 de formula general (I), dentro de ellos los favorables a los antagonistas, a sus sales, solvatos, N-oxidos e isomeros, a las composiciones farmaceuticas que contienen los compuestos de formula general (I), sus sales, solvatos, N-oxidos e isomeros, al use de los compuestos de formula general (I), sus sales, solvatos, N-oxidos e isomeros, a la preparación de los compuestos de formula general (I), sus sales, solvatos, N-oxidos e isomeros, asi como a los nuevos intermediarios de formula general (II), (VI), (XI), (XII) y (XV) y a la preparacion de ellos.

10. 发明专利

AU2004259127B2 Aminoquinoline derivatives and their use as adenosine A3 ligands 未知
公开(公告)号：AU2004259127B2
公开(公告)日：2009-05-28
申请号：AU2004259127
申请日：2004-07-23
申请人： SANOFI AVENTIS
发明人： BATORI SANDOR , URBAN-SZABO KATALIN , SZEREDI JUDIT VARGANE , TIMARI GEZA , GERBER KATALIN , MIKUS ENDRE , BOER KINGA , KAPUI ZOLTAN , FINET MICHEL , ARANYI PETER
IPC分类号： A61P11/00 , C07C229/50 , C07D215/48 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D491/04
摘要： Aminoquinoline derivatives (I) and their salts, solvates, isomers (tautomers, desmotrops, optically active isomers) and their salts or solvates are new. Aminoquinoline derivatives of formula (I) and their salts, solvates, isomers (tautomers, desmotrops, optically active isomers) and their salts or solvates are new. [Image] R 1>H or 1-4C alkyl; R 2>H or 1-4C alkyl; R 3>H, 1-4C alkyl, 3-6C cycloalkyl, phenyl, thienyl or furyl (optionally substituted by 1-4C alkyl, 1-4C alkoxy or halo), 5-6 membered heteroaromatic ring containing 1-3N, 5 membered heteroaromatic ring containing O, N or S (optionally substituted with 1-4C alkyl, 1-4C alkoxy or halo); R 4>, R 5>H, 3-6C cycloalkyl or 1-4C alkyl (optionally containing amino group substituted by 1-2 1-4C alkyl, OH, carboxy or alkyl group substituted with 1-4C alkyl), benzyl, -SO 2OH or 1-4C acyl; NR 4>R 5>a group of formula (a); R 7>, R 8>H, 1-4C alkyl or 3-6C cycloalkyl; R 6>H, 1-4C alkyl, phenyl, benzyl, thienyl or furyl (optionally substituted by methylenedioxy or 1 or more 1-4C alkyl, 1-4C alkoxy, hydroxy, trifluoromethyl, cyano or halo), or 5 or 6 membered heteroaromatic ring (containing either 1-3 N, 1 N and 1 O or 1 N and 1 S, and optionally substituted by 1 or more 1-4C alkyl, 1-4C alkoxy or halo); X : CH 2, NH, NR 9>, S, O, sulfo or sulfoxy; R 9>1-4C alkyl or 3-6C cycloalkyl; Z : O, S, CHR 1> 0> or NR 1>; R 1> 0>H, 1-4C alkyl or 3-6C cycloalkyl; R 1> 1>H, 1-4C alkyl, 3-6C cycloalkyl, SO 2OH or 1-4C acyl; n : 0-2; m, o : 1-3; and p, r : 0-1. Provided that either: (1) R 4> and R 5> are H, 3-6C cycloalkyl or 1-4C alkyl optionally contains amino group substituted 1-2 1-4C alkyl, OH, carboxy or alkyl group substituted with 1-4C alkyl; (2) R 4> is H, 1-4C alkyl or benzyl and R 5> is H, -SO 2OH or 1-4C acyl; or (3) NR 4>R 5> is (a). [Image] Independent claims are also included for the following: (1) preparation of (I); and (2) new compounds of formulae (II''), (III''), (IV''), (V''), (VI''), (VII''), (VIII'') and (XIII''). [Image] ACTIVITY : Cardiant; Nephrotropic; Respiratory-Gen.; CNS-Gen.; Cytostatic; Ophthalmological; Antiinflammatory; Antiasthmatic; Vasotropic; Antidepressant; Antiarrhythmic; Antiparkinsonian; Nootropic; Antiallergic; Dermatological; Antiarthritic; Immunosuppressive; Gastrointestinal-Gen.; Anabolic; Hypertensive; Antipsoriatic; Antirheumatic; Neuroprotective; Antidiabetic. MECHANISM OF ACTION : Adenosine A3 ligands. (I) were tested for adenosine A3 ligand activity in HEK-293 cells. The inhibitory constant value of (I) was 0.5-15 nM.

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