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1. 发明专利

HU9904624A2 SACCHARIN DERIVATIVES, PROCESS FOR PRODUCING THEM, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATES 未知
公开(公告)号：HU9904624A2
公开(公告)日：2002-01-28
申请号：HU9904624
申请日：1999-12-17
申请人： SANOFI SYNTHELABO
发明人： DR KAPUI ZOLTAN , DR VARGA MARTON , DR BATORI SANDOR , DR MIKUS ENDRE , T NAGY LAJOS , URBAN SZABO KATALIN , DR LEVAI FERENC , DR ARANYI PETER , PASCAL MARC , VASVARINE DR DEBRECZY LELLE , DR HERMECZ ISTVAN
IPC分类号： A61K31/519 , A61K31/5377 , A61P1/04 , A61P1/16 , A61P1/18 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/10 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/06 , A61P25/00 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/10 , A61P33/02 , A61P33/12 , A61P35/00 , A61P37/02 , A61P43/00 , C07D471/04
摘要： Orally active compounds of general formula (I) wherein R1 is methyl, ethyl or 2-morpholino-ethyl group, R2 is piperidino, morpholino or 4-methyl-piperazinyl group, n is 2 or 3 and their salts, solvates and hydrates.

2. 发明专利

HU0105407D0 NOVEL COMPOUNDS 未知
公开(公告)号：HU0105407D0
公开(公告)日：2002-03-28
申请号：HU0105407
申请日：2001-12-21
申请人： SANOFI SYNTHELABO
发明人： BOER KINGA , TIMARI GEZA , DR BATORI SANDOR , BALAZS LASZLO , DR KAPUI ZOLTAN , DR MIKUS ENDRE , URBAN-SZABO KATALIN , T NAGY LAJOS , DR ARANYI PETER , DR BENCZE JUDIT , HAJDU FELIX , DR SZABO TIBOR , WALCZ ERZSEBET
IPC分类号： A61K31/437 , A61K31/444 , A61P9/00 , A61P11/00 , A61P13/12 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , C07B61/00 , C07D215/54 , C07D215/56 , C07D471/04
摘要： Triazolo-quinoline derivatives are new. Triazolo-quinoline derivatives of formula (I), their salts, solvates and optically active isomers and the salts or solvates are new. [Image] R 1> and R 2>H or straight or branched 1-4C alkyl; R 3>straight or branched 1-4C alkyl, phenyl, thienyl, furyl (optionally substituted by at least one straight or branched 1-4C alkyl, straight or branched 1-4C alkoxy or halo), H, 5 - 6 membered heteroaromatic ring containing 1 - 3 N atom or 5-membered heteroaromatic ring containing one nitrogen atom and one oxygen atom or one nitrogen atom and one sulfur atom (optionally substituted by at least one straight or branched 1-4C alkyl, straight or branched 1-4C alkoxy or halo); R 4> and R 5>H; R 4>+R 5>1,3-butadienyl (optionally substituted by methylenedioxy or at least one straight or branched 1-4C alkyl, straight or branched 1-4C alkoxy, OH or halo); R 6>H, cyano, aminocarbonyl, 1-4C alkoxycarbonyl or carboxy; R 7>phenyl, benzyl, thienyl, furyl (all 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 or 1-4C alkylene (optionally substituted by phenyl), amino, mono- or dialkylamino, 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 (optionally substituted by at least one straight or branched 1-4C alkyl, straight or branched 1-4C alkoxy or halo); X : -CH 2-, -NH-, -NR 1> 2>-, S, O, sulfo or sulfoxy; R 1> 2>a straight or branched 1-4C alkyl or 3-6C cycloalkyl; and n : 0 - 2. Independent claims are also included for: (1) Preparation of (I); and (2) New intermediate, 1,2-diamino-pyridium salt of formula (II). [Image] ACTIVITY : Cardiant; Nephrotropic; Antiallergic; Antiinflammatory; Dermatological; Antipsoriatic; Hypotensive; Ophthalmological; Antidiabetic; Antiasthmatic; Immunosuppressive; Antirheumatic; Cytostatic; Vasotropic; Antiarrhythmic. MECHANISM OF ACTION : Adenosine A 3 receptor antagonist. The compounds were tested for adenosine A 3 receptor antagonistic activity using HEK-293 cells. Test details are described but no results for the specific compounds given. In general compound (I) showed a K i of 3.5 and 0.78 nM.

3. 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.

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