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1. 发明申请

WO2005075458A8 PYRIMIDINE DERIVATIVES AS OREXIN RECEPTORS ANTAGONISTS 审中-公开
标题翻译：作为OREXIN受体拮抗剂的吡嗪衍生物
公开(公告)号：WO2005075458A8
公开(公告)日：2006-01-19
申请号：PCT/HU2005000010
申请日：2005-02-08
申请人： SANOFI AVENTIS , ARANYI PETER , BALOGH MARIA , BATORI SANDOR , BENCE JUDIT , FINET MICHEL , KAPUI ZOLTAN , PHILIPPO CHRISTOPHE , SZABO TIBOR , SZLAVIK ZOLTAN , TOEMOESKOEZI ZSUZSANNA , URBAN-SZABO KATALIN , VENIER OLIVIER
发明人： ARANYI PETER , BALOGH MARIA , BATORI SANDOR , BENCE JUDIT , FINET MICHEL , KAPUI ZOLTAN , PHILIPPO CHRISTOPHE , SZABO TIBOR , SZLAVIK ZOLTAN , TOEMOESKOEZI ZSUZSANNA , URBAN-SZABO KATALIN , VENIER OLIVIER
IPC分类号： C07D239/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/06 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P3/00
CPC分类号： C07D401/14 , C07D239/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/06
摘要： The present invention relates to the orexin receptor antagonists of the general formula (I), which are selective to orexin I receptors. (I)
摘要翻译：本发明涉及对食欲肽I受体有选择性的通式（I）的食欲素受体拮抗剂。（I）<子/

2. 发明申请

WO2005060959A8 PYRAZOLE DERIVATIVES AND USE THEREOF AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡唑衍生物及其作为OREXIN受体拮抗剂的用途
公开(公告)号：WO2005060959A8
公开(公告)日：2006-01-12
申请号：PCT/HU2004000117
申请日：2004-12-15
申请人： SANOFI AVENTIS , ALETRU MICHEL , ARANYI PETER , BALOGH MARIA , BATORI SANDOR , BENCE JUDIT , BOVY PHILIPPE , KAPUI ZOLTAN , MIKUS ENDRE , NAMANE CLAUDIE , PHILIPPO CHRISTOPHE , SZABO TIBOR , TOEMOESKOEZI ZSUZSANNA , URBAN-SZABO KATALIN
发明人： ALETRU MICHEL , ARANYI PETER , BALOGH MARIA , BATORI SANDOR , BENCE JUDIT , BOVY PHILIPPE , KAPUI ZOLTAN , MIKUS ENDRE , NAMANE CLAUDIE , PHILIPPO CHRISTOPHE , SZABO TIBOR , TOEMOESKOEZI ZSUZSANNA , URBAN-SZABO KATALIN
IPC分类号： C07D231/16 , C07D231/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , A61K31/415 , A61K31/4155 , A61P1/14 , A61P25/00
CPC分类号： C07D409/04 , C07D231/16 , C07D231/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.
摘要翻译：本发明涉及食欲素受体拮抗剂通式（I）化合物及其异构体，盐和溶剂合物，其含有它们的药物组合物及其治疗应用。

3. 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

4. 发明专利

AT429427T 未知
公开(公告)号：AT429427T
公开(公告)日：2009-05-15
申请号：AT05708501
申请日：2005-02-08
申请人： SANOFI AVENTIS
发明人： ARANYI PETER , BALOGH MARIA , BATORI SANDOR , BENCE JUDIT , FINET MICHEL , KAPUI ZOLTAN , PHILIPPO CHRISTOPHE , SZAB TIBOR , SZLAVIK ZOLTAN , TOEMOESKOEZI ZSUZSANNA , URBAN-SZABO KATALIN , VENIER OLIVIER
IPC分类号： C07D401/04 , C07D239/42 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/06
摘要： The present invention relates to substituted pyrimidine compounds of formula I useful as orexin receptor antagonists. The invention also relates to pharmaceutical compositions containing said compounds.

5. 发明专利

NO20043119L 未知
公开(公告)号：NO20043119L
公开(公告)日：2004-07-20
申请号：NO20043119
申请日：2004-07-20
申请人： SANOFI AVENTIS
发明人： BATORI SANDOR , KAPUI ZOLTAN , MIKUS ENDRE , SZABO TIBOR , NAGY LAJOS T , BALAZS LASZLO , BOER KINGA , URBAN-SZABO KATALIN , ARANYI PETER , BENCE JUDIT , HAJDU FELIX , TIMARI GEZA , 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 , A61K31/505
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.

6. 发明专利

DE602005014086D1 未知
公开(公告)号：DE602005014086D1
公开(公告)日：2009-06-04
申请号：DE602005014086
申请日：2005-02-08
申请人： SANOFI AVENTIS
发明人： ARANYI PETER , BALOGH MARIA , BATORI SANDOR , BENCE JUDIT , FINET MICHEL , KAPUI ZOLTAN , PHILIPPO CHRISTOPHE , SZAB TIBOR , SZLAVIK ZOLTAN , TOEMOESKOEZI ZSUZSANNA , URBAN-SZABO KATALIN , VENIER OLIVIER
IPC分类号： C07D401/04 , A61K31/505 , C07D239/42 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/06
摘要： The present invention relates to substituted pyrimidine compounds of formula I useful as orexin receptor antagonists. The invention also relates to pharmaceutical compositions containing said compounds.

7. 发明专利

AU2002353240B2 Triazolo-quinolin derivatives useful as adenosine receptor ligands 未知
公开(公告)号：AU2002353240B2
公开(公告)日：2008-06-19
申请号：AU2002353240
申请日：2002-12-17
申请人： SANOFI AVENTIS
发明人： SZABO TIBOR , WALCZ ERZSEBET , HAJDU FELIX , MIKUS ENDRE , BATORI SANDOR , URBAN-SZABO KATALIN , KAPUI ZOLTAN , BENCE JUDIT , ARANYI PETER , TIMARI GEZA , NAGY LAJOS T , BALAZS LASZLO , BOER KINGA
IPC分类号： C07D471/04 , 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
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.

8. 发明专利

RS56004A DERIVATI TRIAZOLO-KVINOLINA KORISNI KAO VEZNICI RECEPTORA ADENOZINA 未知
公开(公告)号：RS56004A
公开(公告)日：2006-10-27
申请号：YUP56004
申请日：2002-12-17
申请人： SANOFI AVENTIS
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： 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 , C07D213/89 , C07D405/12 , A61K31/505 , A61N25/00
摘要： Predmetni pronalazak odnosi se na veznike A3 receptora adenozina opšte formule (I), među njima poželjno na antagoniste, kao i na njihove soli, solvate i izomere i farmaceutske preparate koji ih sadrže, na upotrebu jedinjenja opšte formule (I), kao i njihovih soli, solvata i izomera, na pripremanje jedinjenja opšte formule (I) i njihovih soli, solvata i izomera, dalje na nove intermedijere opšte formule (II) i na njihovo prirpemanje.

9. 发明专利

TNSN04106A1 TRIAZOLO-QUINOLIN DERIVATIVES USEFUL AS ADENOSINE RECEPTOR LIGANDS 未知
公开(公告)号：TNSN04106A1
公开(公告)日：2006-06-01
申请号：TNSN04106
申请日：2004-06-08
申请人： SANOFI-AVENTIS
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： C07D215/54 , A61K31/437 , A61K31/444 , A61P9/00 , A61P11/00 , A61P13/12 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , C07B61/00 , C07D215/56 , C07D471/04
摘要： THE PRESENT INVENTION RELATES TO ADENOSINE A? 3 ? RECEPTOR LIGANDS OF THE GENERAL FORMULA (1); WHITHIN 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 (1); AS WELL AS THEIR SALTS; SOLVATES AND ISOMERS; TO THE PREPARATION OF THE COMPOUNDS OF THE GENERAL FORMULA (1) 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

ZA200404802B Triazolo-quinolin derivatives useful as adenosine receptor ligands. 未知
公开(公告)号：ZA200404802B
公开(公告)日：2005-08-29
申请号：ZA200404802
申请日：2004-06-17
申请人： SANOFI AVENTIS
发明人： ARANYI PETER , BATORI SANDOR , BOER KINGA , KAPUI ZOLTAN , SZABO TIBOR , TIMARI GEZA , WALCZ ERZSEBET , BALAZS LASZLO , BENCE JUDIT , HAJDU FELIX , MIKUS ENDRE , NAGY LAJOS T , URBAN-SZABO KATALIN
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 , C07D , A61K , A61N
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.

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