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1. 发明申请

WO02096879A9 AMINOQUINOLINE AND AMINOPYRIDINE DERIVATIVES AND THEIR USE AS ADENOSINE A3 LIGANDS 审中-公开
标题翻译：氨基喹啉和氨基吡啶衍生物及其作为腺苷A3配体使用
公开(公告)号：WO02096879A9
公开(公告)日：2003-11-20
申请号：PCT/HU0200048
申请日：2002-05-29
申请人： SANOFI SYNTHELABO , ARANYI PETER , BALAZS LASZLO , BALOGH MARIA , BATA IMRE , BATORI SANDOR , T NAGY LAJOS , TIMARI GEZA , BOER KINGA , FINANCE OLIVIER , KAPUI ZOLTAN , MIKUS ENDRE , SZAMOSVOELGYI ZSUZSANNA , SZELECZKY GABOR , URBAN-SZABO KATALIN
发明人： ARANYI PETER , BALAZS LASZLO , BALOGH MARIA , BATA IMRE , BATORI SANDOR , T NAGY LAJOS , TIMARI GEZA , BOER KINGA , FINANCE OLIVIER , KAPUI ZOLTAN , MIKUS ENDRE , SZAMOSVOELGYI ZSUZSANNA , SZELECZKY GABOR , URBAN-SZABO KATALIN
IPC分类号： C07D215/54 , A61K20060101 , A61K31/4706 , A61K31/4709 , A61P20060101 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/06 , A61P25/00 , A61P25/16 , A61P25/24 , A61P27/06 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07D20060101 , C07D213/75 , C07D213/85 , C07D215/46 , C07D215/48 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
CPC分类号： C07D401/12 , C07D213/85 , C07D215/46 , C07D215/48 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： Compounds of general formula (I), wherein R and R stand for hydrogen atom or form together an 1,3-butadienyl group, optionally substituted by a methylenedioxy group or one or more straight or branched C1-4 alkyl group, straight or branched C1-4 alkoxy group, hydroxy group or halogen atom; are strong adenosine A3 receptor ligands preferably antagonists.
摘要翻译：通式（I）的化合物，其中R 4和R 5代表氢原子或一起形成1,3-丁二烯基，任选被亚甲二氧基或一个或多个直链或支链C 1-4烷基基团，直链或支链C 1-4烷氧基，羟基或卤素原子; 是强的腺苷A3受体配体优选拮抗剂。

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

CA2448561C AMINOQUINOLINE DERIVATIVES AND THEIR USE AS ADENOSINE A3 LIGANDS 未知
公开(公告)号：CA2448561C
公开(公告)日：2011-07-19
申请号：CA2448561
申请日：2002-05-29
申请人： SANOFI SYNTHELABO
发明人： ARANYI PETER , BALAZS LASZLO , BALOGH MARIA , BATA IMRE , BATORI SANDOR , T NAGY LAJOS , TIMARI GEZA , BOER KINGA , FINANCE OLIVIER , KAPUI ZOLTAN , MIKUS ENDRE , SZAMOSVOELGYI ZSUZSANNA , SZELECZKY GABOR , URBAN-SZABO KATALIN
IPC分类号： C07D215/48 , C07D215/54 , A61K20060101 , A61K31/4706 , A61K31/4709 , A61P20060101 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/06 , A61P25/00 , A61P25/16 , A61P25/24 , A61P27/06 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07D20060101 , C07D213/75 , C07D213/85 , C07D215/46 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： The invention provides compounds of general formula (I), (see formula I) wherein R4 and R5 form together an 1,3-butadienyl group, optionally substituted by a methylenedioxy group or one or more straight or branched C1-4 alkyl group, straight or branched C1-4 alkoxy group, hydroxy group or halogen atom. The compounds of the invention are strong adenosine A3 receptor ligands preferably antagonists.

4. 发明专利

CA2470067C IMIDAZOQUINOLINE DERIVATIVES 未知
公开(公告)号：CA2470067C
公开(公告)日：2011-02-15
申请号：CA2470067
申请日：2002-12-17
申请人： SANOFI SYNTHELABO
发明人： ARANYI PETER , BALAZS LASZLO , BALOGH MARIA , BATORI SANDOR , BOER KINGA , GERBER KATALIN , KAPUI ZOLTAN , MIKUS ENDRE , TIMARI GEZA , T NAGY LAJOS , URBAN-SZABO KATALIN , VARGANE SZEREDI JUDIT
IPC分类号： C07D215/54 , C07D471/04 , A61K31/437 , A61K31/4545 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61P1/04 , A61P3/04 , A61P3/10 , A61P7/00 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/16 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D215/56 , C07D405/12 , C07D409/12 , C07D487/04
摘要： The present invention relates to adenosine A3 receptor ligands of the general formula (I), whithin those preferably antagonists, as well as their salts, solvates and isomers, and the pharmaceutical compositions containings them, to the use of the compounds of the general formula (I), as well as their salts, solvates and isomers, to the preparation of the compounds of the general formula (I) and their salts, solvates and isomers, furthermore to the new intermediates of the general formulae (II) and (III) and to the preparation thereof.

5. 发明专利

EA007066B1 ПРОИЗВОДНЫЕ ТРИАЗОЛОХИНОЛИНА, ПРИМЕНИМЫЕ В КАЧЕСТВЕ ЛИГАНДОВ АДЕНОЗИНОВЫХ РЕЦЕПТОРОВ 未知
公开(公告)号：EA007066B1
公开(公告)日：2006-06-30
申请号：EA200400848
申请日：2002-12-17
申请人： SANOFI SYNTHELABO
发明人： ARANYI PETER , BALAZS LASLO , BATORI SANDOR , BENCE JUDIT , BOER KINGA , HAJDU FELIX , KAPUI ZOLTAN , MIKUS ENDRE , SZABO TIBOR , T NAGY LAJOS , TIMARI GEZA , URBAN-SZABO RANALIN , WALCZ ERZEBET
IPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/505 , A61P9/00 , A61P11/00 , A61P13/12 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , C07B61/00 , C07D213/89 , C07D215/54 , C07D215/56 , C07D405/12
摘要： Данноеизобретениеотноситсяк лигандамаденозиновыхАрецепторовобщейформулы (I), которыепредпочтительноявляютсяантагонистами, атакжек ихсолям, сольватами изомерам, ик содержащимихфармацевтическимкомпозициям, кприменениюсоединенийобщейформулы (I) , атакжеихсолей, сольватови изомеров, кполучениюсоединенийобщейформулы (I) иихсолей, сольватови изомеров, крометого, кновымпромежуточнымсоединениямобщейформулы (II) иихполучению.

6. 发明专利

CA2470067A1 IMIDAZOQUINOLINE DERIVATIVES 未知
公开(公告)号：CA2470067A1
公开(公告)日：2003-07-03
申请号：CA2470067
申请日：2002-12-17
申请人： SANOFI SYNTHELABO
发明人： URBAN-SZABO KATALIN , TIMARI GEZA , MIKUS ENDRE , T NAGY LAJOS , KAPUI ZOLTAN , BATORI SANDOR , BALOGH MARIA , VARGANE SZEREDI JUDIT , BOER KINGA , BALAZS LASZLO , GERBER KATALIN , ARANYI PETER
IPC分类号： C07D215/54 , A61K31/437 , A61K31/4545 , A61K31/4706 , A61K31/4709 , A61P1/04 , A61P3/04 , A61P3/10 , A61P7/00 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/16 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D215/56 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , A61K31/47
摘要： The present invention relates to adenosine A3 receptor ligands of the genera l formula (I), whithin those preferably antagonists, as well as their salts, solvates and isomers, and the pharmaceutical compositions containings them, to the use of the compounds of the general formula (I), as well as their salts, solvates and isomers, to the preparation of the compounds of the general formula (I) and their salts, solvates and isomers, furthermore to the new intermediates of the general formulae (II) and (III) and to the preparation thereof.

7. 发明专利

HU0105406D0 OVEL COMPOUNDS 未知
公开(公告)号：HU0105406D0
公开(公告)日：2002-03-28
申请号：HU0105406
申请日：2001-12-21
申请人： SANOFI SYNTHELABO
发明人： BOER KINGA , TIMARI GEZA , DR BALOGH MARIA , DR KAPUI ZOLTAN , DR MIKUS ENDRE , URBAN-SZABO KATALIN , DR ARANYI PETER , DR BATORI SANDOR , BALAZS LASZLO , T NAGY LAJOS , GERBER KATALIN , SZEREDI JUDIT
IPC分类号： C07D215/54 , A61K31/437 , A61K31/4545 , A61K31/4706 , A61K31/4709 , A61P1/04 , A61P3/04 , A61P3/10 , A61P7/00 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/16 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D215/56 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04
摘要： Imidazoquinoline derivatives (I), their salts, solvates and optically active isomers and salts or solvates, are new. Imidazoquinoline derivatives of formula (I), their salts, solvates and optically active isomers and salts or solvates, are new. [Image] R 1>, R 2>H or 1-4C alkyl; R 3>1-4C alkyl, 3-6C cycloalkyl, phenyl, thienyl, furyl (optionally substituted by at least one 1-4C alkyl, 1-4C alkoxy or halo), H, 5 - 6 membered heteroaromatic ring containing 1 - 3 N atoms or 5-membered heteroaromatic ring (containing one nitrogen atom and one oxygen atom or one nitrogen atom and one sulfur atom and optionally substituted by at least one 1-4C alkyl, 1-4C alkoxy or halo); R 4> - R 7>H, 1-4C alkyl, 1-4C alkoxy, OH or halo; or R 5>+R 6>methylenedioxy; R 8>H, cyano, aminocarbonyl, 1-4C alkoxycarbonyl or carboxy; R 9>, R 1> 0>T 1> or (CH 2) p-NR 1> 2>R 1> 3>; T 1>phenyl, phenyl-(1-4C)alkyl, thienyl-(1-4C)alkyl, furyl-(1-4C)alkyl (optionally substituted by methylenedioxy or at least one straight or branched 1-4C alkyl, straight or branched 1-4C alkoxy, OH, trifluoromethyl, cyano or halo), H, straight or branched 1-4C alkyl, 3-6C cycloalkyl, -(CH 2) m-OH, 5 - 6 membered heteroaromatic ring containing 1 - 3 N atoms or 5-membered heteroaromatic ring (containing one nitrogen atom and one oxygen atom or one nitrogen atom and one sulfur atom and optionally substituted by at least one straight or branched 1-4C alkyl, 1-4C alkoxy or halo); R 1> 2>, R 1> 3>T 1>; or NR 9>R 1> 0>, NR 1> 2>R 1> 3>3 - 7-membered heterocyclic group (optionally substituted by straight or branched 1-4C alkyl; X : -CH 2-, -NH-, -NR 1> 1>-, S, O, sulfo or sulfoxy; R 1> 1>1-4C alkyl or 3-6C cycloalkyl; n : 0 - 2; m : 1 - 4; p : 0 - 4; and provided that R 5>+R 6> is only methylenedioxy when R 4> and R 7> are H. Independent claims are also included for the following: (a) preparation of (I); and (b) new intermediates, imidazoquinoline acid compound of formula (II) and imidazoquinoline ester compound of formula (III). [Image] [Image] R 1> 4>1-4C alkyl. ACTIVITY : Cardiant; Nephrotropic; CNS Gen.; Respiratory Gen.; Antiallergic; Antiinflammatory; Dermatological; Antipsoriatic; Hypotensive; Ophthalmological; Antidiabetic; Antiasthmatic; Immunosuppressive; Antirheumatic; Cytostatic; Vasotropic; Antiarrhythmic; Antiparkinsonian; Antiarthritic; Antidepressant; Nootropic. MECHANISM OF ACTION : Adenosine A 3 Receptor Antagonist; Cytokine Production Inhibitor; TNF-alpha Release Inhibitor; Eosinophil, Neutrophil and Immune Cell Migration Inhibitor; Bronchoconstriction and Plasma Extravasation Inhibitor. The compounds were tested for adenosine A 3 receptor antagonistic activity using HEK293 cells. The general compound (I) showed a K i of 1.6 and 0.38 nM. No results for specific compounds given.

8. 发明专利

HU0102279D0 NEW COMPOUNDS 未知
公开(公告)号：HU0102279D0
公开(公告)日：2001-08-28
申请号：HU0102279
申请日：2001-05-31
申请人： SANOFI SYNTHELABO
发明人： BOER KINGA , TIMARI GEZA , BATORI SANDOR , KAPUI ZOLTAN , MIKUS ENDRE DR , ARANYI PETER , BATA IMRE , T NAGY LAJOS , URBAN-SZABO KATALIN , BALAZS LASZLO , BALOGH MARIA , SZAMOSVOELGYI ZSUZSANNA , SZELECKY GABOR , FINANCE OLIVIER
IPC分类号： A61K20060101 , A61P20060101 , C07D20060101 , C07D213/75

9. 发明专利

CA2470064C TRIAZOLO-QUINOLIN DERIVATIVES USEFUL AS ADENOSINE RECEPTOR LIGANDS 未知
公开(公告)号：CA2470064C
公开(公告)日：2010-01-26
申请号：CA2470064
申请日：2002-12-17
申请人： SANOFI SYNTHELABO
发明人： ARANYI PETER , BALAZS LASZLO , BATORI SANDOR , BENCE JUDIT , BOER KINGA , HAJDU FELIX , KAPUI ZOLTAN , MIKUS ENDRE , SZABO TIBOR , T NAGY LAJOS , TIMARI GEZA , URBAN-SZABO KATALIN , WALCZ ERZSEBET
IPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/505 , A61P9/00 , A61P11/00 , A61P13/12 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , C07B61/00 , C07D213/89 , C07D215/54 , C07D215/56 , C07D405/12
摘要： The present invention relates to adenosine A3 receptor ligands of the general formula (I), within those preferably antagonists, as well as their salts, solvates and isomers, and the pharmaceutical compositions containing them, to the use of the compounds of the general formula (I), as well as their salts, solvates and isomers, to the preparation of the compounds of the general formula (I) and theirs salts, solvates and isomers, furthermore to the new intermediates of the general formulae (II) and to the preparation thereof.

10. 发明专利

TNSN03117A1 AMINOQUINOLINE AND AMINOPYRIDINE DERIVATIVES AND THEIR USE AS ADENOSINE A3 LIGANDS 未知
公开(公告)号：TNSN03117A1
公开(公告)日：2005-12-23
申请号：TNSN03117
申请日：2003-07-08
申请人： SANOFI SYNTHELABO
发明人： ARANYI PETER , BALAZS LASZLO , BALOGH MARIA , BATA IMRE , BATORI SANDOR , T NAGY LAJOS , TIMARI GEZA , BOER KINGA , FINANCE OLIVIER , KAPUI ZOLTAN , MIKUS ENDRE , SZAMOSVOLGYI ZSUZSANNA , SZELECZKY GABOR , URBAN-SZABO KATALIN
IPC分类号： A61K31/4706 , A61P43/00 , C07D213/85 , C07D215/46 , C07D215/48 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： COMPOUNDS OF GENERAL FORMULA (I) WHEREIN R4 AND R5 STAND : FOR HYDROGEN ATOM OR FORM TOGETHER AN 1,3-BUTADIENYL GROUP, OPTIONALLY SUBSTITUTED BY A METHYLENEDIOXY GROUP OR ONE OR MORE STRAIGHT OR BRANCHED C1-4 ALKYL GROUP, STRAIGHT OR BRANCHED C1-4 ALKOXY GROUP, HYDROXY GROUP OR HALOGEN ATOM; ARE STRONG ADENOSINE A3 RECEPTOR LIGANDS PREFERABLY ANTAGONISTS.

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