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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.

3. 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.

4. 发明专利

HU0500878A2 AMIDE DERIVATIVES AS CCR3 RECEPTOR LIGANDS, PROCESS FOR PRODUCING THEM, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE AND INTERMEDIATES 未知
公开(公告)号：HU0500878A2
公开(公告)日：2007-05-29
申请号：HU0500878
申请日：2005-09-22
申请人： SANOFI AVENTIS
发明人： PAPPNE BEHR AGNES , KAPUI ZOLTAN , ARANYI PETER DR , BATORI SANDOR , BARTANE BODOR VERONIKA , T NAGY LAJOS , VARGA MARTON , FERENCZY GYOERGY , MIKUS ENDRE DR , URBAN-SZABO KATALIN , VARGANE SZEREDI JUDIT , WALCZ ERZSEBET , SUSAN EDIT
IPC分类号： C07C237/00 , A61K31/16 , A61P11/06 , A61P31/16 , A61P37/00 , C07D235/04 , C07D239/72 , C07D263/54 , C07D277/62 , C07D487/04 , C07D513/04
摘要： Amino alkyl amide derivatives and their salts, solvates and their isomers are new. Amino alkyl amide derivatives of formula Ar 1-X-N(R 1)-Y-N(R 2)-C(=O)-Z'-Ar 2 and their salts, solvates and their isomers are new. Ar 1phenyl (optionally substituted by halogen); X,Y : straight 1-4C alkylene (optionally substituted by straight or branched 1-4C alkyl); Z' : straight 2-4C alkylene or alkenylene (both optionally substituted by straight or branched 1-4C alkyl) or valence bond; R 1,R 2hydrogen atom or straight or branched 1-4C alkyl; Ar 2phenyl-, thienyl- or furyl (all optionally substituted by straight or branched 1-4C alkyl or alkoxy, hydroxyl, amino (optionally mono- or di-substituted by straight or branched 1-4C alkyl), trifluoromethyl, cyano, 1-2C alkylenedioxy or halogen atom), 5- or 6-membered heterocyclic ring (containing 1 - 3 nitrogen atoms, or 2 nitrogen atoms and 1 oxygen atom, or 1 nitrogen atom and 1 oxygen atom, or 1 nitrogen atom and 1 sulfur atom and optionally substituted by straight or branched 1-4C alkyl or alkoxy, halogen atom, nitro, cyano, carboxyl, phenyl (optionally substituted by straight or branched 1-4C alkyl, halogen atom or benzyloxy), oxo, NR 1 0R 1 1, CONR 1 0R 1 1 or SO 2NR 1 0R 1 1), the benzologs of these 5- or 6-membered heterocycle (in which the benzene ring is optionally substituted by T 1, trifluoromethyl, nitro, 1-2C alkylenedioxy or sulfonyl) or 5- or 6-membered heterocyclic ring (containing 1 - 3 nitrogen atoms, or 1 nitrogen atom and 1 oxygen atom, or 1 nitrogen atom and 1 sulfur atom and condensed with 6-membered heteroaromatic rings (containing 1 or 2 nitrogen atoms) and optionally substituted by T 1); T 1halogen atom, straight or branched 1-4C alkyl or alkoxy, cyano, carboxyl, hydroxyl, NR 1 0R 1 1, CONR 1 0R 1 1 or SO 2NR 1 0R 1 1; R 1 0,R 1 1,R 1 4hydrogen atom, straight or branched 1-4C alkyl, 3-6C cycloalkyl or benzyl; NR 1 0+R 1 1a group of formula (i); R 1 2,R 1 3hydrogen atom or straight or branched 1-4C alkyl; A : methylene group, oxygen atom, sulfur atom or NR 1 4; q : 0 - 3; r : 1 or 2; o,s : 0 or 1. Independent claims are included for the following: (1) preparation of the amino-alkyl-amide derivatives (I); and (2) a pyridine compound of formula Ar' 2-Z 1-C(=O)-W' forming a narrower group of a ketone compound of formula Ar 2-Z'-C(=O)-W' (II). Ar' 21,2,4-triazolo[1,5-a]pyridine- or triazolo[5,4-b]pyridine group (both optionally substituted by straight or branched 1-4C alkyl or alkoxy, hydroxyl, NR 1 0R 1 1, CONR 1 0R 1 1 or SO 2NR 1 0R 1 1); Z 11,3-propylene group; W' : halogen atom, hydroxyl, O(1-4C alkyl) or OCO-Z'-Ar 2. ACTIVITY : Antiasthmatic; Dermatological; Antiinflammatory; Gastrointestinal-Gen.; Antiulcer; Antiallergic; Ophthalmological; Neuroprotective; Virucide; Anti-HIV. MECHANISM OF ACTION : CC chemokine receptor 3 (CCR3) receptor antagonist. The CCR3 receptor antagonist effect of the amino-alkyl-amide derivatives (I) was examined on eotaxin binding test on human CCR3 (hCCR3) receptor expressing recombinant K562 and RBL2H3 cells and using Eotaxin labeled with radioactive iodine ( 1> 2> 3>I). The compound (I) showed IC 5 0 value of 0.5 - 500 (preferably 0.5 - 15) nM. No results for specific compounds are given.

5. 发明专利

AU2006293635A1 Amino-alkyl-amide derivatives as CCR3 receptor liquids 未知
公开(公告)号：AU2006293635A1
公开(公告)日：2007-03-29
申请号：AU2006293635
申请日：2006-09-19
申请人： SANOFI AVENTIS
发明人： NAGY LAJOS T , MIKUS ENDRE , FERENCZY GYORGY , KAPUI ZOLTAN , ARANYI PETER , SUSAN EDIT , URBAN-SZABO KATALIN , WALCZ ERZSEBET , BEHR AGNES PAPPNE , BODOR VERONIKA BARTANE , SZEREDI JUDIT VARGANE , BATORI SANDOR , VARGA MARTON
IPC分类号： C07C233/35 , A61K31/4965
摘要： The invention relates to a compound of the general formula (I), as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology, and pharmaceutical preparations containing such compound. The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.

6. 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.

7. 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.

8. 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.

9. 发明专利

MA27501A1 DERIVES D'IMIDAZOQUINOLINE EN TANT QUE LIGANDS RECEPTEURS DE L'ADENOSINE A3 未知
公开(公告)号：MA27501A1
公开(公告)日：2005-08-01
申请号：MA28334
申请日：2005-06-13
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： A61K31/415 , A61P3/00 , A61P9/00 , A61P11/00 , A61P13/12 , A61P17/00 , A61P25/00 , A61P29/00 , A61P35/00 , C07D471/04
摘要： L'invention concerne des composés de formule (I), dans laquelle X, Z, R1 -R10, m, n, o, p, r sont, comme dans la description, de préférence de forts antagonistes des ligands récepteurs de l'adénosine A3.

10. 发明专利

NO20052866D0 未知
公开(公告)号：NO20052866D0
公开(公告)日：2005-06-13
申请号：NO20052866
申请日：2005-06-13
申请人： SANOFI AVENTIS
发明人： SZEREDI JUDIT , BALOGH MARIA , BATORI SANDOR , KAPUI ZOLTAN , MIKUS ENDRE , NAGY LAJOS T , BALAZS LASZLO , BOER KINGA , URBAN-SZABO KATALIN , GERBER KATALIN , WALCZ ERZSEBET , ARANYI PETER , TIMARI GEZA
IPC分类号： A61K31/415 , A61P3/00 , A61P9/00 , A61P11/00 , A61P13/12 , A61P17/00 , A61P25/00 , A61P29/00 , A61P35/00 , C07D471/04 , C07D
摘要： This invention is directed to a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, Z, m, n, o, p and r are as defined herein, its preparation, pharmaceutical composition and use as an adenosine A3 receptor ligand preferably an antagonist.

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