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1. 发明申请

WO2007034254A8 AMINO-ALKYL-AMIDE DERIVATIVES AS CCR3 RECEPTOR LIGANDS 审中-公开
标题翻译：氨基酸 - 酰胺衍生物作为CCR3受体配体
公开(公告)号：WO2007034254A8
公开(公告)日：2008-05-15
申请号：PCT/HU2006000080
申请日：2006-09-21
申请人： SANOFI AVENTIS , SANTA MIHALYNE , PAPPNE BEHR AGNES , KAPUI ZOLTAN , ARANYI PETER , BATORI SANDOR , BARTANE BODOR VERONIKA , VARGA MARTON , MIKUS ENDRE , URBAN-SZABO KATALIN , VARGANE SZEREDI JUDIT , SZABO TIBOR , SUSAN EDIT , KOVACS MARIANNA
发明人： PAPPNE BEHR AGNES , KAPUI ZOLTAN , ARANYI PETER , BATORI SANDOR , BARTANE BODOR VERONIKA , VARGA MARTON , MIKUS ENDRE , URBAN-SZABO KATALIN , VARGANE SZEREDI JUDIT , SZABO TIBOR , SUSAN EDIT , KOVACS MARIANNA , T NAGY LAJOS
IPC分类号： C07C233/35 , A61K31/4965 , C07C233/40 , C07C233/78 , C07C323/63 , C07D235/28 , C07D263/58
CPC分类号： C07C233/78 , C07C233/40 , C07D235/28 , C07D263/58
摘要： The present invention relates to the CCR3 receptor ligands of the general formula (I), within them favourably to antagonists and to the salts, solvates and isomers thereof, to the pharmaceutical compositions containing them, to the use of the compounds of the general formula (I) and their salts, solvates and isomers and to the preparation of the compounds of the general formula (I) and their salts, solvates and isomers.
摘要翻译：本发明涉及通式（I）的CCR3受体配体，其中有利于拮抗剂及其盐，溶剂化物和异构体，含有它们的药物组合物，涉及使用通式（ I）及其盐，溶剂合物和异构体以及通式（I）化合物及其盐，溶剂合物和异构体的制备。

2. 发明申请

WO2007034254A2 AMINO-ALKYL-AMIDE DERIVATIVES AS CCR3 RECEPTOR LIGANDS 审中-公开
标题翻译：氨基酸 - 酰胺衍生物作为CCR3受体配体
公开(公告)号：WO2007034254A2
公开(公告)日：2007-03-29
申请号：PCT/HU2006000080
申请日：2006-09-21
申请人： SANOFI AVENTIS , SANTA MIHALYNE , PAPPNE BEHR AGNES , KAPUI ZOLTAN , ARANYI PETER , BATORI SANDOR , BARTANE BODOR VERONIKA , VARGA MARTON , MIKUS ENDRE , URBAN-SZABO KATALIN , VARGANE SZEREDI JUDIT , SZABO TIBOR , SUSAN EDIT , KOVACS MARIANNA
发明人： PAPPNE BEHR AGNES , KAPUI ZOLTAN , ARANYI PETER , BATORI SANDOR , BARTANE BODOR VERONIKA , VARGA MARTON , MIKUS ENDRE , URBAN-SZABO KATALIN , VARGANE SZEREDI JUDIT , SZABO TIBOR , SUSAN EDIT , KOVACS MARIANNA , T NAGY LAJOS
IPC分类号： C07C233/35 , A61K31/4965 , C07C233/40 , C07C233/78 , C07C323/63 , C07D235/28 , C07D263/58
CPC分类号： C07C233/78 , C07C233/40 , C07D235/28 , C07D263/58
摘要： The present invention relates to the CCR3 receptor ligands of the general formula (I), within them favourably to antagonists and to the salts, solvates and isomers thereof, to the pharmaceutical compositions containing them, to the use of the compounds of the general formula (I) and their salts, solvates and isomers and to the preparation of the compounds of the general formula (I) and their salts, solvates and isomers.
摘要翻译：本发明涉及通式（I）的CCR3受体配体，其有利于拮抗剂及其盐，溶剂化物和异构体，含有它们的药物组合物，涉及使用通式（ I）及其盐，溶剂合物和异构体以及通式（I）化合物及其盐，溶剂合物和异构体的制备。

3. 发明申请

WO2010013078A3 PYRROLIDINYL-ALKYL-AMIDE DERIVATIVES THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION AS CCR3 RECEPTOR LIGANDS 审中-公开
标题翻译：吡咯烷基 - 烷基 - 酰胺衍生物的制备及其作为CCR3受体配体的治疗应用
公开(公告)号：WO2010013078A3
公开(公告)日：2010-03-25
申请号：PCT/HU2009000067
申请日：2009-07-29
申请人： SANOFI AVENTIS , PAPPNE BEHR AGNES , BATORI SANDOR , BARTANE BODOR VERONIKA , SZLAVIK ZSOLT , BATA IMRE , URBAN SZABO KATALIN , KAPUI ZOLTAN , MIKUS ENDRE
发明人： PAPPNE BEHR AGNES , BATORI SANDOR , BARTANE BODOR VERONIKA , SZLAVIK ZSOLT , BATA IMRE , URBAN SZABO KATALIN , KAPUI ZOLTAN , MIKUS ENDRE
IPC分类号： C07D417/12 , A61K31/428 , A61K31/429 , A61K31/4353 , A61P1/04 , A61P11/02 , A61P11/06 , A61P17/00 , C07D513/04
CPC分类号： C07D513/04 , C07D417/12
摘要： The present invention relates to the CCR3 receptor ligands of the general formula (I) or (IA) -within them favourably to the antagonists-, and to the salts and isomers thereof, to the pharmaceutical compositions containing them, to the use of the compounds of the general formula (I) and (IA), and their salts and isomers and to the preparation of the compounds of the general formula (I) and (IA), and their salts and isomers.
摘要翻译：本发明涉及通式（I）或（IA）的CCR3受体配体 - 有利地包括拮抗剂 - 及其盐和异构体，含有它们的药物组合物，涉及化合物（I）和（IA）化合物及其盐和异构体以及制备通式（I）和（IA）化合物及其盐和异构体的方法。

4. 发明申请

WO2010013078A8 PYRROLIDINYL-ALKYL-AMIDE DERIVATIVES THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION AS CCR3 RECEPTOR LIGANDS 审中-公开
标题翻译：吡咯烷基-L-酰胺衍生物他们的制备及其治疗应用作为CCR3受体配体
公开(公告)号：WO2010013078A8
公开(公告)日：2010-05-20
申请号：PCT/HU2009000067
申请日：2009-07-29
申请人： SANOFI AVENTIS , PAPPNE BEHR AGNES , BATORI SANDOR , BARTANE BODOR VERONIKA , SZLAVIK ZOLTAN , BATA IMRE , URBAN SZABO KATALIN , KAPUI ZOLTAN , MIKUS ENDRE
发明人： PAPPNE BEHR AGNES , BATORI SANDOR , BARTANE BODOR VERONIKA , SZLAVIK ZOLTAN , BATA IMRE , URBAN SZABO KATALIN , KAPUI ZOLTAN , MIKUS ENDRE
IPC分类号： C07D417/12 , A61K31/428 , A61K31/429 , A61K31/4353 , A61P1/04 , A61P11/02 , A61P11/06 , A61P17/00 , C07D513/04
CPC分类号： C07D513/04 , C07D417/12
摘要： The present invention relates to the CCR3 receptor ligands of the general formula (I) or (IA) -within them favourably to the antagonists-, and to the salts and isomers thereof, to the pharmaceutical compositions containing them, to the use of the compounds of the general formula (I) and (IA), and their salts and isomers and to the preparation of the compounds of the general formula (I) and (IA), and their salts and isomers.
摘要翻译：本发明涉及通式（I）或（IA）的CCR3受体配体，其有利于拮抗剂及其盐和异构体与含有它们的药物组合物，使用化合物的通式（I）和（IA）及其盐和异构体以及通式（I）和（IA）的化合物及其盐和异构体的制备。

5. 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.

6. 发明专利

CA2623312A1 AMINO-ALKYL-AMIDE DERIVATIVES AS CCR3 RECEPTOR LIGANDS 未知
公开(公告)号：CA2623312A1
公开(公告)日：2007-03-29
申请号：CA2623312
申请日：2006-09-19
申请人： SANOFI AVENTIS
发明人： T NAGY LAJOS , SZABO TIBOR , MIKUS ENDRE , FERENCZY GYORGY , URBAN-SZABO KATALIN , BATORI SANDOR , ARANYI PETER , KAPUI ZOLTAN , PAPPNE BEHR AGNES , BARTANE BODOR VERONIKA , VARGANE SZEREDI JUDIT , WALCZ ERSZEBET , VARGA MARTON
IPC分类号： C07C323/63 , A61K31/4965 , C07C233/35 , C07C323/60 , C07D209/30 , C07D233/84 , C07D235/28 , C07D239/34 , C07D239/38 , C07D241/44 , C07D257/04 , C07D263/58 , C07D271/10 , C07D271/113 , C07D277/16 , C07D277/70 , C07D401/04 , C07D405/04 , C07D413/04 , C07D471/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to the CCR3 receptor ligands of the general formula (I), within them favourably to antagonists and to the salts, solvates and isomers thereof, to the pharmaceutical compositions containing them, to the use of the compounds of the general formula (I) and their salts, solvates and isomers, to the preparation of the compounds of the general formula (I) and their salts, solvates and isomers and to the new intermediates of the general formula (III).

7. 发明专利

CA2732631A1 PYRROLIDINYL-ALKYL-AMIDE DERIVATIVES THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION AS CCR3 RECEPTOR LIGANDS 未知
公开(公告)号：CA2732631A1
公开(公告)日：2010-02-04
申请号：CA2732631
申请日：2009-07-29
申请人： SANOFI AVENTIS
发明人： PAPPNE BEHR AGNES , BATORI SANDOR , BARTANE BODOR VERONIKA , BATA IMRE , URBAN SZABO KATALIN , KAPUI ZOLTAN , MIKUS ENDRE , SZLAVIK ZOLTAN
IPC分类号： C07D417/12 , A61K31/428 , A61K31/429 , A61K31/4353 , A61P1/04 , A61P11/02 , A61P11/06 , A61P17/00 , C07D513/04
摘要： The present invention relates to the CCR3 receptor ligands of the general formula (I) or (IA) -within them favourably to the antagonists-, and to the salts and isomers thereof, to the pharmaceutical compositions containing them, to the use of the compounds of the general formula (I) and (IA), and their salts and isomers and to the preparation of the compounds of the general formula (I) and (IA), and their salts and isomers.

8. 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.

9. 发明专利

AU2009275626B2 Pyrrolidinyl-alkyl-amide derivatives their preparation and their therapeutic application as CCR3 receptor ligands 未知
公开(公告)号：AU2009275626B2
公开(公告)日：2013-11-07
申请号：AU2009275626
申请日：2009-07-29
申请人： SANOFI AVENTIS
发明人： PAPPNE BEHR AGNES , BATORI SANDOR , BARTANE BODOR VERONIKA , SZLAVIK ZSOLT , BATA IMRE , URBAN SZABO KATALIN , KAPUI ZOLTAN , MIKUS ENDRE
IPC分类号： C07D417/12 , A61K31/428 , A61K31/429 , A61K31/4353 , A61P1/04 , A61P11/02 , A61P11/06 , A61P17/00 , C07D513/04
摘要： The present invention relates to the CCR3 receptor ligands of the general formula (I) or (IA) -within them favourably to the antagonists-, and to the salts and isomers thereof, to the pharmaceutical compositions containing them, to the use of the compounds of the general formula (I) and (IA), and their salts and isomers and to the preparation of the compounds of the general formula (I) and (IA), and their salts and isomers.

10. 发明专利

AR072623A1 DERIVADOS DE PIRROLIDINIL-ALQUIL-AMIDA SU PREPARACION Y SU APLICACION TERAPEUTICA COMOLIGANDOS DE LOS RECEPTORES DE CCR3 未知
公开(公告)号：AR072623A1
公开(公告)日：2010-09-08
申请号：ARP090102883
申请日：2009-07-29
申请人： SANOFI AVENTIS
发明人： BATA IMRE , SZLAVIK ZOLTAN , MIKUS ENDRE , BATORI SANDOR , KAPUI ZOLTAN , BARTANE BODOR VERONIKA , PAPPNE BEHR AGNES , URBAN SZABO KATALIN
IPC分类号： C07D417/12 , C07D513/04 , A61K31/4353 , A61K31/4453 , A61K31/5377 , A61K31/4985 , A61P11/06 , A61P17/00 , A61P31/18 , A61P27/02
摘要： Composiciones farmacéuticas que los contienen, al uso de los compuestos de la formula general (1) y (1A), y a sus sales e isomeros y a la preparacion de los compuestos de la formula general (1) y (1A), y sus sales e isomeros. Reivindicacion 1: Compuestos de la formula general (1) o (1A): en donde: Ar1 representa un grupo fenilo o naftilo, opcionalmente sustituido con uno o más de: un grupo alquilo C1-4 recto o ramificado, identico o no idéntico, un grupo alcoxi C1-4 recto o ramificado, un átomo de halogeno, un grupo trifluorometilo, un grupo ciano, un grupo nitro, un grupo hidroxilo, un grupo alquilenodioxi C1-2, un grupo amino o un grupo amino sustituido con uno o dos grupos alquilo C1-4 rectos o ramificados, idénticos o no idénticos; R1 representa un átomo de hidrogeno, o un grupo alquilo C1-4, recto o ramificado; R4, R5, R6a, R6b representan un átomo de hidrogeno, o R4 representa un grupo alquilo C1-4 recto o ramificado, y R5, R6a y R6b representan un átomo de hidrogeno, o R5 representa un grupo alquilo C1-4 recto o ramificado, y R4, R6a y R6b representan un átomo de hidrogeno, o R6a representa un grupo alquilo C1-4 recto o ramificado, y R6b representa un grupo alquilo C1-4 recto o ramificado o un átomo de hidrogeno, y R4, R5, representan un átomo de hidrogeno; Y, Z representan independientemente un grupo alquileno C1-4, recto, opcionalmente sustituido con uno o más grupos alquilo C1-4 rectos o ramificados, idénticos o no idénticos; Ar2 representa un grupo fenilo, tienilo o furilo, opcionalmente sustituido con uno o más de: un grupo alquilo C1-4 recto o ramificado, idéntico o no idéntico, un grupo alcoxi C1-4 recto o ramificado, un átomo de halogeno, un grupo hidroxilo, un grupo ciano, un grupo nitro, un grupo trifluorometilo, un grupo alquilenodioxi C1-2, un grupo amino, un grupo amino sustituido con uno o dos grupos alquilo C1-4 rectos o ramificados, idénticos o no idénticos; o un anillo heterocíclico de 5 o 6 miembros que contiene uno, dos o tres átomos de nitrogeno, o un átomo de nitrogeno y un átomo de oxígeno, o un átomo de nitrogeno y un átomo de azufre, opcionalmente substituido con uno o más grupos de un grupo alquilo C1-4 recto o ramificado, idéntico o no idéntico, y un grupo alcoxi C1-4 recto o ramificado, un grupo hidroxilo, un átomo de halogeno, un grupo nitro, un grupo ciano, un grupo trifluorometilo, un grupo alquilenodioxi C1-2, un grupo -NR7R8, -CONR7R8 o -SO2NR7R8, en donde R7 y R8 representan independientemente un átomo de hidrogeno, un grupo alquilo C1-4 recto o ramificado, o R7 y R8 junto con el átomo de nitrogeno forman un grupo de la formula general (2): en donde: R2, R3 representan un grupo alquilo C1-4 recto o ramificado o un grupo cicloalquilo C3-6, A representa un grupo -CHR12, un átomo de oxígeno, un átomo de azufre o un grupo -NR9 - en donde R12 y R9 representan un átomo de hidrogeno, un grupo alquilo C1-4 recto o ramificado o un grupo cicloalquilo C3-6 -, m tiene el valor de 1, 2 o 3, n tiene el valor de 1 o 2, o tiene el valor de 0 o 1, p tiene el valor de 0 o 1; o el benzologo de un anillo heterocíclico de 5 o 6 miembros que contiene uno, dos o tres átomos de nitrogeno, o un átomo de nitrogeno y un átomo de oxígeno, o un átomo de nitrogeno y un átomo de azufre - opcionalmente sustituido con uno o más de un grupo alquilo C1-4 recto o raificado, idéntico o no idéntico, un grupo alcoxi C1-4, recto o ramificado, un grupo hidroxilo, un átomo de halogeno, un grupo trifluorometilo, un grupo nitro, un grupo ciano, un grupo alquilenodioxi C1-2, un grupo -NR7R8, -CONR7R8 o -SO2NR7R8 - en donde los significados de R7 y R8 son como se definieron más arriba; o el derivado de un anillo heterocíclico de 5 o 6 miembros que contiene uno, dos o tres átomos de nitrogeno, o un átomo de nitrogeno y un átomo de oxígeno, o un átomo de nitrogeno y un átomo de azufre, condensado con anillos heteroaromáticos de 6 miembros que contienen uno o dos átomos de nitrogeno - opcionalmente sustituidos con uno o más de un grupo alquilo C1-4, recto o ramificado, idéntico o no idéntico, un grupo alcoxi C1-4 recto o ramificado, un grupo hidroxilo, un átomo de halogeno, un grupo nitro, un grupo ciano, un grupo trifluorometilo, un grupo alquilenodioxi C1-2, un grupo -NR7R8, -CONR7R8 o -SO2NR7R8 - en donde los significados de R7 y R8 son como se definieron más arriba; Q representa un grupo -O-, un grupo -N- -H o -N- -CO-R10- en donde R10 representa un átomo de hidrogeno, un grupo alquilo C1-4 recto o ramificado, un grupo cicloalquilo C3-6, un gurpo fenilo, bencilo o -NH-R11 - en donde R11 representa un grupo alquilo C1-4 recto o ramificado, un grupo cicloalquilo C3-6, un grupo fenilo o bencilo -; y sus sales e isomeros y las sales de los mismos.

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