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    • 2. 发明专利
      NO20060702L  未知
    • NO20060702L
    • 2006-02-28
    • NO20060702
    • 2006-02-14
    • SANOFI AVENTIS
    • SZEREDI JUDIT , BATORI SANDOR , KAPUI ZOLTAN , MIKUS ENDRE , TIMARI GEZA , URBAN-SZABO KATALIN , ARANYL PETER , BOER KINGA , GERBER KATALIN , FINET MICHEL
    • C07D215/48 , A61P11/00 , C07C229/50 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D491/04
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 4. 发明专利
      HU0302440A2 AMINOQUINOLINE DERIVATIVES, PROCESS FOR PRODUCING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
    • AMINOQUINOLINE DERIVATIVES, PROCESS FOR PRODUCING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    • HU0302440A2
    • 2005-05-30
    • HU0302440
    • 2003-07-31
    • SANOFI AVENTIS
    • ARANYI PETER DR , BATORI SANDOR DR , TIMARI GEZA DR , BOER KINGA , KAPUI ZOLTAN DR , MIKUS ENDRE DR , URBAN-SZABO KATALIN , GERBER KATALIN , SZEREDI JUDIT , FINET MICHEL
    • C07D215/54
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 5. 发明专利
      NO329743B1  未知
    • NO329743B1
    • 2010-12-13
    • NO20043117
    • 2004-07-20
    • SANOFI AVENTIS
    • SZEREDI JUDIT , BALOGH MARIA , BATORI SANDOR , KAPUI ZOLTAN , MIKUS ENDRE , NAGY LAJOS T , BALAZS LASZLO , TIMARI GEZA , BOER KINGA , URBAN-SZABO KATALIN , ARANYI PETER , GERBER KATALIN
    • C07D215/54 , C07D471/04 , 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 , C07D487/04
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 8. 发明专利
      NO20043117L  未知
    • NO20043117L
    • 2004-07-20
    • NO20043117
    • 2004-07-20
    • SANOFI AVENTIS
    • SZEREDI JUDIT , BALOGH MARIA , BATORI SANDOR , KAPUI ZOLTAN , MIKUS ENDRE , NAGY LAJOS T , BALAZS LASZLO , TIMARI GEZA , BOER KINGA , URBAN-SZABO KATALIN , ARANYI PETER , GERBER KATALIN
    • 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
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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