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1. 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.

2. 发明专利

HU0202001A2 AZABICYCLO-OCTANE AND NONANE DERIVATIVES WITH DDP-IV INHIBITING ACTIVITY 未知
公开(公告)号：HU0202001A2
公开(公告)日：2005-08-29
申请号：HU0202001
申请日：2002-06-14
申请人： SANOFI AVENTIS
发明人： ARANYI PETER DR , BALAZS LASZLO , BATA IMRE DR , BATORI SANDOR DR , BORONKAY EVA , KAPUI ZOLTAN DR , SUSAN EDIT , SZABO TIBOR , URBAN-SZABO KATALIN , T NAGY LAJOS , VARGA MARTON DR
IPC分类号： A61K31/439 , A61K31/444 , A61K31/496 , A61K31/506 , A61P3/00 , A61P3/10 , A61P13/12 , A61P17/00 , A61P25/18 , A61P25/22 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D207/06 , C07D207/16 , C07D263/06 , C07D277/06 , C07D451/04 , C07D451/14
摘要： Heterocyclic amides useful as inhibitors of dipeptylpeptidase-IV (DPP-IV) enzyme, process for the preparation thereof and intermediates therefore.

3. 发明专利

HU0500879A2 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：HU0500879A2
公开(公告)日：2007-05-29
申请号：HU0500879
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 DR , MIKUS ENDRE DR , URBAN-SZABO KATALIN , VARGANE SZEREDI JUDIT , SZABO TIBOR , SUSAN EDIT , KOVACS MARIANNA
IPC分类号： C07C237/00 , A61K31/16 , A61P11/06 , A61P31/16 , A61P37/00 , C07D263/54 , C07D277/62
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.

4. 发明专利

HU0500877A2 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：HU0500877A2
公开(公告)日：2007-05-29
申请号：HU0500877
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 DR , FERENCZY GYOERGY , MIKUS ENDRE DR , URBAN-SZABO KATALIN , VARGANE SZEREDI JUDIT , SZABO TIBOR , WALCZ ERZSEBET
IPC分类号： C07C237/00 , A61K31/16 , A61P11/06 , A61P31/16 , A61P37/00 , C07C323/60 , C07D209/30 , C07D233/84 , C07D235/04 , C07D235/28 , C07D239/34 , C07D239/38 , C07D239/72 , C07D241/44 , C07D257/04 , C07D263/54 , C07D263/58 , C07D271/10 , C07D271/113 , C07D277/16 , C07D277/62 , C07D277/70 , C07D401/04 , C07D405/04 , C07D413/04 , C07D471/04 , C07D498/04 , C07D513/04
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.

5. 发明专利

HU227684B1 ADAMANTANE AND AZABICYCLO-OCTANE AND NONANE DERIVATIVES AND THEIR USE AS DPP-IV INHIBITORS 未知
公开(公告)号：HU227684B1
公开(公告)日：2011-11-28
申请号：HU0302788
申请日：2003-08-29
申请人： SANOFI AVENTIS
发明人： ARANYI PETER DR , BATA IMRE , BATORI SANDOR , BORONKAY EVA , BOVY PHILLIPE , KAPUI ZOLTAN , SUSAN EDIT , SZABO TIBOR , URBAN-SZABO KATALIN , VARGA MARTON
IPC分类号： C07D401/12 , A61K31/506 , A61P3/10 , C07D207/16 , C07D213/74 , C07D215/38 , C07D221/22 , C07D231/38 , C07D241/20 , C07D253/06 , C07D261/14 , C07D277/42 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D451/02 , C07D471/04
摘要： The present invention relates to the novel compounds of the general formula (I) possessing dipeptidyl peptidase IV enzyme inhibitory activity, pharmaceutical compositions thereof, methods of using said compounds, processes for their preparation and intermediates of the general formulae (II), (IV), (V), (VII), (VIII) and (IX).

6. 发明专利

HU0302788A2 ADAMANTANE AND AZABICYCLO-OCTANE AND NONANE DERIVATIVES, PROCESS OF THEIR PREPARATION AND THEIR USE AS DPP-IV INHIBITORS 未知
公开(公告)号：HU0302788A2
公开(公告)日：2007-09-28
申请号：HU0302788
申请日：2003-08-29
申请人： SANOFI AVENTIS
发明人： ARANYI PETER DR , BATA IMRE , BATORI SANDOR , BORONKAY EVA , BOVY PHILLIPE , KAPUI ZOLTAN , SUSAN EDIT , SZABO TIBOR , URBAN-SZABO KATALIN , VARGA MARTON
IPC分类号： C07D401/12 , A61K31/506 , C07D207/16 , C07D213/74 , C07D215/38 , C07D221/22 , C07D231/38 , C07D241/20 , C07D253/06 , C07D261/14 , C07D277/42 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D451/02 , C07D471/04
摘要： The present invention relates to the novel compounds of the general formula (I) possessing dipeptidyl peptidase IV enzyme inhibitory activity, pharmaceutical compositions thereof, methods of using said compounds, processes for their preparation and intermediates of the general formulae (II), (IV), (V), (VII), (VIII) and (IX).

7. 发明专利

HU0500886A2 AMIDE DERIVATIVES AS CCR3 RECEPTOR LIGANDS, PROCESS FOR PRODUCING THEM, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE 未知
公开(公告)号：HU0500886A2
公开(公告)日：2007-05-29
申请号：HU0500886
申请日：2005-09-23
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 , MIKUS ENDRE DR , URBAN-SZABO KATALIN , VARGANE SZEREDI JUDIT , SZABO TIBOR , SUSAN EDIT , KOVACS MARIANNA
IPC分类号： C07D263/54 , A61K31/16 , A61P11/06 , A61P31/16 , A61P37/00 , C07C233/40 , C07C233/78 , C07C237/00 , C07D235/04 , C07D235/28 , C07D263/58
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.

8. 发明专利

HU0302440A2 AMINOQUINOLINE DERIVATIVES, PROCESS FOR PRODUCING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：HU0302440A2
公开(公告)日：2005-05-30
申请号：HU0302440
申请日：2003-07-31
申请人： SANOFI AVENTIS
发明人： 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
IPC分类号： C07D215/54
摘要： 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.

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