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1. 发明申请

WO2008149168A8 TRIAZOLO [1, 5-A] QUINOLINES AS ADENOSINE A3 RECEPTOR LIGANDS 审中-公开
公开(公告)号：WO2008149168A8
公开(公告)日：2008-12-11
申请号：PCT/HU2008/000063
申请日：2008-06-02
申请人： SANOFI-AVENTIS , SUSÁN, Edit , BOÉR, Kinga , KAPUI, Zoltán , TÍMÁRI, Géza , BÁTORI, Sándor , SZLÁVIK, Zoltán , MIKUS, Endre , VARGÁNÉ SZEREDI, Judit , FINET, Michel , URBÁN SZABÓ, Katalin , SZABÓ, Tibor
发明人： SUSÁN, Edit , BOÉR, Kinga , KAPUI, Zoltán , TÍMÁRI, Géza , BÁTORI, Sándor , SZLÁVIK, Zoltán , MIKUS, Endre , VARGÁNÉ SZEREDI, Judit , FINET, Michel , URBÁN SZABÓ, Katalin , SZABÓ, Tibor
IPC分类号： C07D215/58 , C07D471/04 , C07F7/22 , A61K31/4745 , A61P11/06 , A61P29/00
摘要： The present invention relates to the adenosine A3 receptor ligands of the general formula (I), within them favourably to the antagonists, to their salts, solvates, N -oxides and isomers, to the pharmaceutical compositions containing the compounds of the general formula (I), their salts, solvates, N -oxides and isomers, to the use of the compounds of the general formula (I), their salts, solvates, N -oxides and isomers, to the preparation of the compounds of the general formula (I), their salts, solvates, N -oxides and isomers, as well as to the new intermediates of the general formula (II), (VI), (XI), (XII) and (XV), and to the preparation thereof.

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

WO02096879A9 AMINOQUINOLINE AND AMINOPYRIDINE DERIVATIVES AND THEIR USE AS ADENOSINE A3 LIGANDS 审中-公开
标题翻译：氨基喹啉和氨基吡啶衍生物及其作为腺苷A3配体使用
公开(公告)号：WO02096879A9
公开(公告)日：2003-11-20
申请号：PCT/HU0200048
申请日：2002-05-29
申请人： SANOFI SYNTHELABO , ARANYI PETER , BALAZS LASZLO , BALOGH MARIA , BATA IMRE , BATORI SANDOR , T NAGY LAJOS , TIMARI GEZA , BOER KINGA , FINANCE OLIVIER , KAPUI ZOLTAN , MIKUS ENDRE , SZAMOSVOELGYI ZSUZSANNA , SZELECZKY GABOR , URBAN-SZABO KATALIN
发明人： ARANYI PETER , BALAZS LASZLO , BALOGH MARIA , BATA IMRE , BATORI SANDOR , T NAGY LAJOS , TIMARI GEZA , BOER KINGA , FINANCE OLIVIER , KAPUI ZOLTAN , MIKUS ENDRE , SZAMOSVOELGYI ZSUZSANNA , SZELECZKY GABOR , URBAN-SZABO KATALIN
IPC分类号： C07D215/54 , A61K20060101 , A61K31/4706 , A61K31/4709 , A61P20060101 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/06 , A61P25/00 , A61P25/16 , A61P25/24 , A61P27/06 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07D20060101 , C07D213/75 , C07D213/85 , C07D215/46 , C07D215/48 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
CPC分类号： C07D401/12 , C07D213/85 , C07D215/46 , C07D215/48 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： Compounds of general formula (I), wherein R and R stand for hydrogen atom or form together an 1,3-butadienyl group, optionally substituted by a methylenedioxy group or one or more straight or branched C1-4 alkyl group, straight or branched C1-4 alkoxy group, hydroxy group or halogen atom; are strong adenosine A3 receptor ligands preferably antagonists.
摘要翻译：通式（I）的化合物，其中R 4和R 5代表氢原子或一起形成1,3-丁二烯基，任选被亚甲二氧基或一个或多个直链或支链C 1-4烷基基团，直链或支链C 1-4烷氧基，羟基或卤素原子; 是强的腺苷A3受体配体优选拮抗剂。

4. 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。

5. 发明申请

WO2007034254A3 AMINO-ALKYL-AMIDE DERIVATIVES AS CCR3 RECEPTOR LIGANDS 审中-公开
公开(公告)号：WO2007034254A3
公开(公告)日：2007-03-29
申请号：PCT/HU2006/000080
申请日：2006-09-21
申请人： SANOFI-AVENTIS , SÁNTA, Mihályné , PAPPNÉ BEHR, Ágnes , KAPUI, Zoltán , ARÁNYI, Péter , BÁTORI, Sándor , BARTÁNÉ BODOR, Veronika , VARGA, Márton , MIKUS, Endre , URBÁN-SZABÓ, Katalin , VARGÁNE SZEREDI, Judit , SZABÓ, Tibor , SUSÁN, Edit , KOVÁCS, Marianna
发明人： PAPPNÉ BEHR, Ágnes , KAPUI, Zoltán , ARÁNYI, Péter , BÁTORI, Sándor , BARTÁNÉ BODOR, Veronika , VARGA, Márton , MIKUS, Endre , URBÁN-SZABÓ, Katalin , VARGÁNE SZEREDI, Judit , SZABÓ, Tibor , SUSÁN, Edit , KOVÁCS, Marianna
IPC分类号： C07C233/35 , C07C323/63 , A61K31/4965
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.

6. 发明申请

WO2007034252A1 AMINO-ALKYL-AMIDE DERIVATIVES AS CCR3 RECEPTOR LIQUIDS 审中-公开
标题翻译：氨基酸 - 酰胺衍生物作为CCR3受体液体
公开(公告)号：WO2007034252A1
公开(公告)日：2007-03-29
申请号：PCT/HU2006/000078
申请日：2006-09-19
申请人： SANOFI-AVENTIS , SÁNTA, Mihályné , PAPPNÉ BEHR, Ágnes , KAPUI, Zoltán , ARÁNYI, Péter , BÁTORI, Sándor , BARTÁNÉ BODOR, Veronika , VARGA, Márton , FERENCZY, György , MIKUS, Endre , URBÁN-SZABÓ, Katalin , VARGÁNÉ SZEREDI, Judit , WALCZ, Erzsébet , SUSÁN, Edit
发明人： PAPPNÉ BEHR, Ágnes , KAPUI, Zoltán , ARÁNYI, Péter , BÁTORI, Sándor , BARTÁNÉ BODOR, Veronika , VARGA, Márton , FERENCZY, György , MIKUS, Endre , URBÁN-SZABÓ, Katalin , VARGÁNÉ SZEREDI, Judit , WALCZ, Erzsébet , SUSÁN, Edit
IPC分类号： C07C233/35 , A61K31/4965
CPC分类号： C07C233/40 , C07D209/50 , C07D217/24 , C07D235/16 , C07D237/14 , C07D241/44 , C07D263/56 , C07D277/64 , C07D471/04 , 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 and 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 (IIa).
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，溶剂化物和异构体以及通式（I）化合物及其盐，溶剂合物和异构体以及通式（IIa）的新中间体的制备。

7. 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。

8. 发明申请

WO2003053969A1 IMIDAZOQUINOLINE DERIVATIVES 审中-公开
标题翻译：咪唑啉衍生物
公开(公告)号：WO2003053969A1
公开(公告)日：2003-07-03
申请号：PCT/HU2002/000144
申请日：2002-12-17
申请人： SANOFI-SYNTHELABO , ARÁNYI, Péter , BALÁZS, László , BALOGH, Mária , BÁTORI, Sándor , BOÉR, Kinga , GERBER, Katalin , KAPUI, Zoltán , MIKUS, Endre , TÍMÁRI, Géza , T. NAGY, Lajos , URBÁN-SZABÓ, Katalin , VARGÁNÉ SZEREDI, Judit
发明人： ARÁNYI, Péter , BALÁZS, László , BALOGH, Mária , BÁTORI, Sándor , BOÉR, Kinga , GERBER, Katalin , KAPUI, Zoltán , MIKUS, Endre , TÍMÁRI, Géza , T. NAGY, Lajos , URBÁN-SZABÓ, Katalin , VARGÁNÉ SZEREDI, Judit
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to adenosine A 3 receptor ligands of the general formula (I), whithin those preferably antagonists, as well as their salts, solvates and isomers, and the pharmaceutical compositions containings them, to the use of the compounds of the general formula (I), as well as their salts, solvates and isomers, to the preparation of the compounds of the general formula (I) and their salts, solvates and isomers, furthermore to the new intermediates of the general formulae (II) and (III) and to the preparation thereof.
摘要翻译：咪唑并喹啉衍生物（I），其盐，溶剂合物和光学活性异构体和盐或溶剂化物是新的。式（I）的咪唑并喹啉衍生物，其盐，溶剂合物和光学活性异构体和盐或溶剂化物是新的。 R 1>，R 2> H或1-4C烷基; R 3> 1-4C烷基，3-6C环烷基，苯基，噻吩基，呋喃基（任选被至少一个1-4C烷基，1-4C烷氧基或卤素取代），H为5-6元杂芳环，其含有1-3 N原子或5元杂芳环（含有一个氮原子和一个氧原子或一个氮原子和一个硫原子，任选被至少一个1-4C烷基，1-4C烷氧基或卤素取代）; R 4> R 7 H，1-4C烷基，1-4C烷氧基，OH或卤素; 或R 5> R 6>亚甲二氧基; R 8> H，氰基，氨基羰基，1-4C烷氧基羰基或羧基; R 9> R 1> 0> T 1>或（CH 2）p -NR 1> 2> R 1> 3>; 苯基 - （1-4C）烷基，噻吩基 - （1-4C）烷基，呋喃基（1-4C）烷基（任选被亚甲二氧基或至少一个直链或支链的1-4C烷基取代，直链或支链1-4C烷氧基，OH，三氟甲基，氰基或卤素），H，直链或支链的1-4C烷基，3-6C环烷基， - （CH 2）m -OH，含有1-3N的5-6元杂芳环原子或5元杂芳环（含有一个氮原子和一个氧原子或一个氮原子和一个硫原子，并任选被至少一个直链或支链的1-4C烷基，1-4C烷氧基或卤素取代）; R 1> 2>，R 1> 3> T 1>; 或任选被直链或支链的1-4C烷基取代; X：-CH 2 - ， - NH-， -NR 1> - ，S，O，磺基或磺氧基; R 1> 1-4C烷基或3-6C环烷基; n：0-2; m：1-4; p：0-4;和条件是当R 4>和R 7>为H时，R 5> R 6>只是亚甲二氧基。独立权利要求也包括在下列中：（a）（I）的制备;和（b）新的中间体咪唑并喹啉式（II）化合物和式（III）的咪唑并喹啉酯化合物[图像] [图像] R 1> 4> 1-4C烷基活性：Cardiant; Nephrotropic; CNS Gen; Respiratory Gen; Antiallergic; Antiinflammatory; 皮肤病学，抗牛皮癣，低血压，眼科学，抗糖尿病，抗哮喘，免疫抑制，抗风湿，细胞静止，血管性，抗心律不齐，抗帕金森病，抗关节炎，抗抑郁药，神经营养因子，作用机制：腺苷A受体拮抗剂;细胞因子生成抑制剂; TNF-α释放 ibitor; 嗜酸性粒细胞，嗜中性粒细胞和免疫细胞迁移抑制剂; 支气管收缩和等离子体外渗抑制剂。使用HEK293细胞测试化合物的腺苷A 3受体拮抗活性。一般化合物（I）显示K i为1.6和0.38nM。没有给出具体化合物的结果。

9. 发明申请

WO9842322A3 ANTITUSSIVE COMPOSITIONS 审中-公开
标题翻译：抗菌组合物
公开(公告)号：WO9842322A3
公开(公告)日：1998-12-17
申请号：PCT/HU9800027
申请日：1998-03-20
申请人： KORBONITS DEZSO , ARANYI PETER , JELINEK ISTVAN , MIKUS ENDRE
发明人： KORBONITS DEZSO , ARANYI PETER , JELINEK ISTVAN , MIKUS ENDRE
IPC分类号： C07D473/10 , A61K31/52 , A61K31/522 , A61P11/14 , A61K31/00
CPC分类号： A61K31/522
摘要： The invention relates to the use of theobromine and/or its salts and/or its complexes optionally in admixture with other known active ingredients and inert, solid or liquid carriers, additives and auxiliary agents for the manufacture of a pharmaceutical composition suitable for relieving cough syndrome. Further subject of the invention is a method of treatment of a human or animal subject being in a condition where relieving of cough is desirable which comprises the step of administering in an effective amount theobromine and/or its salts and/or its complexes optionally in admixture with other known active ingredients and suitable inert, solid or liquid carriers, additives and auxiliary agents.

10. 发明申请

WO2010013078A2 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：WO2010013078A2
公开(公告)日：2010-02-04
申请号：PCT/HU2009/000067
申请日：2009-07-29
申请人： SANOFI-AVENTIS , PAPPNÉ BEHR, Ágnes , BÁTORI, Sándor , BARTÁNÉ BODOR, Veronika , SZLÁVIK, Zsolt , BATA, Imre , URBÁN SZABÓ, Katalin , KAPUI, Zoltán , MIKUS, Endre
发明人： PAPPNÉ BEHR, Ágnes , BÁTORI, Sándor , BARTÁNÉ BODOR, Veronika , SZLÁVIK, Zsolt , BATA, Imre , URBÁN SZABÓ, Katalin , KAPUI, Zoltán , MIKUS, Endre
IPC分类号： C07D417/12 , C07D513/04 , A61K31/428 , A61K31/429 , A61K31/4353 , A61P11/06 , A61P11/02 , A61P17/00 , A61P1/04
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 - 其在拮抗剂 - 及其盐和异构体中有利地包含含有它们涉及通式（I）和（IA）化合物及其盐和异构体的用途以及通式（I）和（IA）化合物及其盐和异构体的制备。

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