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1. 发明申请

WO2012101261A1 IL17 AND IFN-GAMMA INHIBITION FOR THE TREATMENT OF AUTOIMMUNE INFLAMMATION 审中-公开
标题翻译： IL17和IFN-γ抑制剂治疗自身免疫性炎症
公开(公告)号：WO2012101261A1
公开(公告)日：2012-08-02
申请号：PCT/EP2012/051357
申请日：2012-01-27
申请人： 4SC DISCOVERY GMH , LEBAN, Johann , TASLER, Stefan , BAUMGARTNER, Roland , SAEB, Wael , CHEVRIER, Carine
发明人： LEBAN, Johann , BAUMGARTNER, Roland , SAEB, Wael , CHEVRIER, Carine
IPC分类号： C07D413/04 , A61K31/422 , A61P29/00
CPC分类号： C07D413/04
摘要： The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.
摘要翻译：本发明涉及通式（I）的化合物及其药学上可接受的盐或溶剂化物作为抗炎剂和免疫调节剂。

2. 发明申请

WO2004113302A1 N-SUBSTITUTED 6,8-DIALKOXY-1,2,3,4-TETRAHYDRO-1H-ISOQUINOLINE AS POTASSIUM CHANNELS MODULATORS 审中-公开
标题翻译： N-取代的6,8-二烷氧基-1,2,3,4-四氢-1H-异喹啉作为钾通道调节剂
公开(公告)号：WO2004113302A1
公开(公告)日：2004-12-29
申请号：PCT/EP2004/006552
申请日：2004-06-17
申请人： 4SC AG , GARCIA, Gabriel , SAEB, Wael , KRAMER, Bernd
发明人： GARCIA, Gabriel , SAEB, Wael , KRAMER, Bernd
IPC分类号： C07D217/06
CPC分类号： C07D217/06
摘要： The invention relates to compounds having the Formula (I) or a salt, or a physiologically functional derivative, or a prodrug thereof, (I) wherein Z is carbonyl or sulfonyl; R 1 is alkyl, alkenyl, alkynyl, aryl, H, halogen, haloalkyl, haloalkoxy, hydroxyalkyl, cycloalkyl or heteroaryl; R 2 is H, OH, -CH 2 -SO 2 -alkyl, -CH 2 -SO 2 -cycloalkyl, -CH 2 -SO 2 -aryl, -CH 2 -SO 2 -heteroaryl, alkylamine, alkenylamine, alkynylamine, cycloalkylamine, arylamine, heteroarylamine, aryl, haloalkyl, haloalkoxy, hydroxyalkyl, cycloalkyl, heteroaryl or a linear or branched alkyl, alkenyl, alkynyl, which can optionally be substituted by one or more substituentes R 3 ; R 3 is H, alkyl, alkenyl, alkynyl, cycloalkyl, -CO 2 R 4 , -CONHR 4 , -CONR 4 R 4 , - CR 4 O, SO 2 R 4 , -NR 4 -CO-R 4 , alkoxy, alkylthio, -OH, -SH, -O-aryl, -O-cycloalkyl, -S-aryl, -S-cycloalkyl, hydroxyalkyl, halogen, haloalkyl, haloalkoxy, CN, NO 2 , hydroxyalkylamine, aminoalkyl, alkylamine, aryl or heteroaryl; R 4 is H, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkylthio, -O-aryl, - O-cycloalkyl, OH, SH, -S-aryl, -S-cycloalkyl, hydroxyalkyl, haloalkyl, haloalkoxy, hydroxyalkyl-amine, aminoalkyl, alkylamine, aryl or heteroaryl; R 5 is alkyl, alkenyl or alkynyl.
摘要翻译：本发明涉及具有式（I）的化合物或其盐或其生理功能衍生物或其前药，其中Z为羰基或磺酰基; R 1是烷基，烯基，炔基，芳基，H，卤素，卤代烷基，卤代烷氧基，羟基烷基，环烷基或杂芳基; R 2是H，OH，-CH 2 -SO 2 - 烷基，-CH 2 -SO 2 - 环烷基，-CH 2 -SO 2 - 芳基，-CH 2 -SO 2 - 杂芳基，烷基胺，链烯基胺，炔基胺，环烷基胺，芳基胺，杂芳基胺，芳基卤代烷基，卤代烷氧基，羟基烷基，环烷基，杂芳基或直链或支链烷基，烯基，炔基，其可任选被一个或多个取代基R 3取代; R 3是H，烷基，烯基，炔基，环烷基，-CO 2 R 4，-CONHR 4，-CONR 4 R 4，-CR 4，SO 2 R 4， NR 4 -CO-R 4，烷氧基，烷硫基，-OH，-SH，-O-芳基，-O-环烷基，-S-芳基，-S-环烷基，羟烷基，卤素，卤代烷基，卤代烷氧基， CN，NO 2，羟烷基胺，氨基烷基，烷基胺，芳基或杂芳基; R 4是H，卤素，烷基，烯基，炔基，环烷基，烷氧基，烷硫基，-O-芳基，-O-环烷基，OH，SH，-S-芳基，-S-环烷基，羟基烷基，卤代烷基，卤代烷氧基，羟基烷基 - 胺，氨基烷基，烷基胺，芳基或杂芳基; R 5是烷基，烯基或炔基。

3. 发明申请

WO03039549A2 SELECTIVE ANTIBACTERIAL AGENTS 审中-公开
标题翻译：选择性抗菌剂
公开(公告)号：WO03039549A2
公开(公告)日：2003-05-15
申请号：PCT/EP0211760
申请日：2002-10-21
申请人： 4SC AG , KRAMER BERND , AMMENDOLA ALDO , SAEB WAEL
发明人： KRAMER BERND , AMMENDOLA ALDO , SAEB WAEL
IPC分类号： C07D239/30 , A01N43/08 , A01N43/10 , A01N43/12 , A01N43/40 , A01N43/54 , A01N43/56 , A01N43/60 , A01N43/80 , A01N43/90 , A01N47/02 , A61B17/00 , A61F2/20 , A61F2/24 , A61F2/30 , A61J1/05 , A61K8/49 , A61K31/175 , A61K31/38 , A61K31/381 , A61K31/415 , A61K31/4155 , A61K31/42 , A61K31/435 , A61K31/437 , A61K31/44 , A61K31/4436 , A61K31/444 , A61K31/445 , A61K31/498 , A61K31/505 , A61K31/506 , A61M1/00 , A61M5/14 , A61M25/00 , A61M39/02 , A61P31/04 , A61P43/00 , A61Q17/00 , A61Q19/00 , C02F1/00 , C07D213/81 , C07D213/82 , C07D231/16 , C07D231/40 , C07D261/18 , C07D307/68 , C07D333/34 , C07D333/38 , C07D333/70 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04 , C09K3/00 , C11D3/48
CPC分类号： A01N43/54 , A01N43/56 , A61K8/49 , A61K8/4973 , A61K8/4986 , A61K31/175 , A61K31/38 , A61K31/415 , A61K31/42 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/505 , A61Q17/005 , A61Q19/00 , C07D231/16 , C07D231/40 , C07D307/68 , C07D333/38 , C07D333/70 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04
摘要： The present invention relates to the use of compounds of the general Formula (I), for the regulation of the quorum sensing system of microorganisms wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R is H, alkyl, cycloalkyl, aryl or heteroaryl; R is H, alkyl, cycloalkyl, aryl or heteroaryl; A and A each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR , CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR , SO or SO2; said substituted ring system carries a substituent R on one or more of the carbon atoms of said ring system;said substituted C1-C20-alkyl group carries a substituent R on one or more of the carbon atoms of said alkyl group; R is independently H, OR , SR , hydroxyalkyl, hydroxyalkylamino, cycloalkyl, halogen, haloalkyl, haloalkyloxy, NO2, CN, SO2NR R , CO2NR R , COR , CO2R , SO2R , SO3R , NR R , alkyl, aryl or heteroaryl; R is H, alkyl, cycloalkyl, aryl or heteroaryl; R is H, O-alkyl, O-aryl, alkyl, heteroaryl or aryl; Y and Y are independent from each other C=O, C=S, SO or C=NR ; p is 0, m is 0, n is 0; or p is 0, m is 0, n is 1;or p is 0, m is 1, n is 1; or p is 1, m is 0, n is 0; or p is 1, m is 0, n is 1; or p is 1, m is 1, n is 1.
摘要翻译：本发明涉及通式（I）化合物在调节微生物群体感应体系中的应用，其中式（I）中R为H，烷基，环烷基，芳基或杂芳基; R 1是H，烷基，环烷基，芳基或杂芳基; R 2是H，烷基，环烷基，芳基或杂芳基; A 1和A 2各自独立地表示可以含有一个或多个Z基团的任选取代的C 1 -C 20 - 烷基或可以包含以下的单环或多环任选取代的芳族或非芳族环系统一个或多个基团X，并且在多环系统的情况下，所述体系含有至少一个芳环; Z选自S，O，N，NR 4，CO，CO 2，CS，SO或SO 2 X选自S，O，N，NR 4，SO或SO 2 ; 所述取代的环系统在所述环系统的一个或多个碳原子上带有取代基R 3;所述取代的C 1 -C 20烷基在所述烷基的一个或多个碳原子上带有取代基R 3 组; R 3独立地是H，OR 4，SR 4，羟烷基，羟基烷基氨基，环烷基，卤素，卤代烷基，卤代烷氧基，NO 2，CN，SO 2 NR 4 R 5，CO 2 NR 4 R 5 ，COR 4，CO 2 R 4，SO 2 R 4，SO 3 R 4，NR 4 R 5，烷基，芳基或杂芳基; R 4是H，烷基，环烷基，芳基或杂芳基; R 5是H，O-烷基，O-芳基，烷基，杂芳基或芳基; Y 1和Y 2彼此独立地为C = O，C = S，SO 2或C = NR 5; p为0，m为0，n为0; 或p为0，m为0，n为1;或p为0，m为1，n为1; 或p为1，m为0，n为0; 或p为1，m为0，n为1; 或p为1，m为1，n为1。

4. 发明申请

WO2007009524A1 2-ARYLBENZOTHIAZOLES AND USES THEREOF 审中-公开
标题翻译： 2-ARYLBENZOTHIAZOLES及其用途
公开(公告)号：WO2007009524A1
公开(公告)日：2007-01-25
申请号：PCT/EP2006/004620
申请日：2006-05-16
申请人： 4SC AG , EHLERT, Jan , HERZ, Thomas , KRAUSS, Rolf , KUBBUTAT, Michael , LANG, Martin , SAEB, Wael , SCHÄCHTELE, Christoph , TASLER, Stefan , TOTZKE, Frank , ZIRRGABEL, Ute
发明人： EHLERT, Jan , HERZ, Thomas , KRAUSS, Rolf , KUBBUTAT, Michael , LANG, Martin , SAEB, Wael , SCHÄCHTELE, Christoph , TASLER, Stefan , TOTZKE, Frank , ZIRRGABEL, Ute
IPC分类号： C07D417/12 , A61K31/426
CPC分类号： C07D417/12 , C07D417/14 , C07D473/34 , C07D487/04 , C07D495/04
摘要： The present invention relates to compounds of the general formula (I) and salts, prodrugs, and stereoisomers thereof, formula (I),wherein Y independently represents S, O, NR 2 , SO, SO 2 ; A independently represents a fife- or six-membered aromatic carbocycle or heterocycle and wherein R 1 to R 20 in formula (I) represent independently of each other a variety of different substituents comprising alkyl, aryl, aralkyl, alkylaryl, heteroaryl groups and monofunctional moieties.
摘要翻译：本发明涉及通式（I）的化合物及其盐，前体药物和立体异构体，式（I），其中Y独立地表示S，O，NR 2，SO，SO， > 2 ; A独立地表示芳族或六元芳族碳环或杂环，并且其中式（I）中的R 1至R 20彼此独立地表示各种不同的取代基包括烷基，芳基，芳烷基，烷基芳基，杂芳基和单官能部分。

5. 发明申请

WO03039549A8 SELECTIVE ANTIBACTERIAL AGENTS 审中-公开
标题翻译：选择性抗菌剂
公开(公告)号：WO03039549A8
公开(公告)日：2004-02-26
申请号：PCT/EP0211760
申请日：2002-10-21
申请人： 4SC AG , KRAMER BERND , AMMENDOLA ALDO , SAEB WAEL
发明人： KRAMER BERND , AMMENDOLA ALDO , SAEB WAEL
IPC分类号： C07D239/30 , A01N43/08 , A01N43/10 , A01N43/12 , A01N43/40 , A01N43/54 , A01N43/56 , A01N43/60 , A01N43/80 , A01N43/90 , A01N47/02 , A61B17/00 , A61F2/20 , A61F2/24 , A61F2/30 , A61J1/05 , A61K8/49 , A61K31/175 , A61K31/38 , A61K31/381 , A61K31/415 , A61K31/4155 , A61K31/42 , A61K31/435 , A61K31/437 , A61K31/44 , A61K31/4436 , A61K31/444 , A61K31/445 , A61K31/498 , A61K31/505 , A61K31/506 , A61M1/00 , A61M5/14 , A61M25/00 , A61M39/02 , A61P31/04 , A61P43/00 , A61Q17/00 , A61Q19/00 , C02F1/00 , C07D213/81 , C07D213/82 , C07D231/16 , C07D231/40 , C07D261/18 , C07D307/68 , C07D333/34 , C07D333/38 , C07D333/70 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04 , C09K3/00 , C11D3/48
CPC分类号： A01N43/54 , A01N43/56 , A61K8/49 , A61K8/4973 , A61K8/4986 , A61K31/175 , A61K31/38 , A61K31/415 , A61K31/42 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/505 , A61Q17/005 , A61Q19/00 , C07D231/16 , C07D231/40 , C07D307/68 , C07D333/38 , C07D333/70 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04
摘要： The present invention relates to the use of compounds of the general Formula (I), for the regulation of the quorum sensing system of microorganisms wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R is H, alkyl, cycloalkyl, aryl or heteroaryl; R is H, alkyl, cycloalkyl, aryl or heteroaryl; A and A each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR , CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR , SO or SO2; said substituted ring system carries a substituent R on one or more of the carbon atoms of said ring system;said substituted C1-C20-alkyl group carries a substituent R on one or more of the carbon atoms of said alkyl group; R is independently H, OR , SR , hydroxyalkyl, hydroxyalkylamino, cycloalkyl, halogen, haloalkyl, haloalkyloxy, NO2, CN, SO2NR R , CO2NR R , COR , CO2R , SO2R , SO3R , NR R , alkyl, aryl or heteroaryl; R is H, alkyl, cycloalkyl, aryl or heteroaryl; R is H, O-alkyl, O-aryl, alkyl, heteroaryl or aryl; Y and Y are independent from each other C=O, C=S, SO or C=NR ; p is 0, m is 0, n is 0; or p is 0, m is 0, n is 1;or p is 0, m is 1, n is 1; or p is 1, m is 0, n is 0; or p is 1, m is 0, n is 1; or p is 1, m is 1, n is 1.
摘要翻译：本发明涉及通式（I）化合物用于调节微生物的群体感应系统的用途，其中在式（I）中，R是H，烷基，环烷基，芳基或杂芳基; R 1是H，烷基，环烷基，芳基或杂芳基; R 2是H，烷基，环烷基，芳基或杂芳基; A 1和A 2各自独立地表示可含有一个或多个Z基团的任选取代的C 1 -C 20烷基，或单环或多环任选取代的芳族或非芳族环系，其可含有一个或多个基团X，并且在多环系统的情况下，所述系统含有至少一个芳环; Z选自S，O，N，NR 4，CO，CO 2，CS，SO或SO 2 X选自S，O，N，NR 4，SO或SO 2 ; 所述取代的环体系在所述环体系的一个或多个碳原子上带有取代基R 3;所述取代的C 1 -C 20烷基在所述烷基的一个或多个碳原子上带有取代基R 3 组; R 3独立地为H，OR 4，SR 4，羟烷基，羟烷基氨基，环烷基，卤素，卤代烷基，卤代烷氧基，NO 2，CN，SO 2 NR 4 R 5，CO 2 NR 4 R 5 COR 4，CO 2 R 4，SO 2 R 4，SO 3 R 4，NR 4 R 5，烷基，芳基或杂芳基; R 4是H，烷基，环烷基，芳基或杂芳基; R 5是H，O-烷基，O-芳基，烷基，杂芳基或芳基; Y 1和Y 2彼此独立地为C = O，C = S，SO 2或C = NR 5; p是0，m是0，n是0; 或者p是0，m是0，n是1;或者p是0，m是1，n是1; 或者p是1，m是0，n是0; 或者p是1，m是0，n是1; 或者p是1，m是1，n是1。

6. 发明申请

WO2012101263A1 IL17 AND IFN-GAMMA INHIBITION FOR THE TREATMENT OF AUTOIMMUNE INFLAMMATION 审中-公开
标题翻译： IL17和IFN-GAMMA抑制自身免疫炎症的治疗
公开(公告)号：WO2012101263A1
公开(公告)日：2012-08-02
申请号：PCT/EP2012/051360
申请日：2012-01-27
申请人： 4SC DISCOVERY GMBH , LEBAN, Johann , TASLER, Stefan , SAEB, Wael , CHEVRIER, Carine
发明人： LEBAN, Johann , TASLER, Stefan , SAEB, Wael , CHEVRIER, Carine
IPC分类号： C07D413/04 , C07D413/14 , C07D417/14 , A61K31/4155 , A61P19/00 , A61P29/00
CPC分类号： C07D413/04 , C07D413/14 , C07D417/14
摘要： The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.
摘要翻译：本发明涉及作为抗炎和免疫调节剂的通式（I）化合物及其药学上可接受的盐或溶剂合物。

7. 发明申请

WO03039529A8 SELECTIVE ANTIBACTERIAL AGENTS 审中-公开
标题翻译：选择性抗菌剂
公开(公告)号：WO03039529A8
公开(公告)日：2003-10-02
申请号：PCT/EP0112875
申请日：2001-11-07
申请人： 4SC A G , AMMENDOLA ALDO , KRAMER BERND , SAEB WAEL
发明人： AMMENDOLA ALDO , KRAMER BERND , SAEB WAEL
IPC分类号： A01N43/54 , A01N43/56 , A61K8/49 , A61K31/175 , A61K31/38 , A61K31/415 , A61K31/42 , A61K31/435 , A61K31/44 , A61K31/445 , A61P31/00 , A61Q17/00 , A61Q19/00 , C07D231/16 , C07D231/40 , C07D307/68 , C07D333/38 , C07D333/70 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04 , A61K6/00 , A61K7/00 , A61K31/381 , A61K31/4178 , A61K31/4436 , A61K31/444 , A61K31/4535
CPC分类号： A61K8/49 , A01N43/54 , A01N43/56 , A61K8/4973 , A61K8/4986 , A61K31/175 , A61K31/38 , A61K31/415 , A61K31/42 , A61K31/435 , A61K31/44 , A61K31/445 , A61Q17/005 , A61Q19/00 , C07D231/16 , C07D231/40 , C07D307/68 , C07D333/38 , C07D333/70 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04
摘要： The present invention relates to the use of compounds of the general Formula (I) for regulation of the quorum sensing system of microorganisms, wherein in Formula (I) R is H, C1-C5-alkyl or an unsaturated or saturated carbocycle selected from the group consisting of cyclopentyl, cyclohexyl, aryl and heteroaryl; R is H, C1-C5-alkyl or an unsaturated or saturated carbocycle selected from the group consisting of cyclopentyl, cyclohexyl, aryl and heteroaryl; A and A are independently from each other an unsubstituted or substituted C1-C20-alkyl group or a monocyclic or polycyclic substituted or unsubstituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; X is selected from the group consisting of S, O, NH, NHR ,SO or SO2; said substituted ring system carries a substituent R on one or more of the carbon atoms of said ring system; said substituted C1-C20-alkyl group carries a substituent R on one or more of the carbon atoms of said alkyl group; R is independently H, OR , SR , halogen, haloalkyl, haloalkyloxy, NO2, CN, SO2NR R , CO2NR R , COR , CO2R , SO2R , SO3R , NR R , C1-C5-alkyl, aryl, or heteroaryl; R is H, C1-C5-alkyl or unsaturated or saturated carbocycle selected from the group consisting of cyclopentyl, cyclohexyl, aryl, heteroaryl; R is H, O-alkyl, O-aryl, alkyl or aryl; Z and Z are independent from each other O, S or NR , n is 0 or 1.
摘要翻译：本发明涉及通式（I）化合物用于调节微生物群体感应系统的用途，其中在式（I）中，R 1是H，C 1 -C 5 - 烷基或不饱和或饱和碳环选自环戊基，环己基，芳基和杂芳基; R 2是H，C 1 -C 5烷基或选自环戊基，环己基，芳基和杂芳基的不饱和或饱和碳环; A 1和A 2彼此独立地为未取代或取代的C 1 -C 20 - 烷基或单环或多环取代或未取代的芳族或非芳族环系，其可以含有一个或多个基团X 并且在多环系统的情况下，所述体系含有至少一个芳香环; X选自S，O，NH，NHR 4，SO或SO 2; 所述取代的环系在所述环系的一个或多个碳原子上带有取代基R 3; 所述取代的C 1 -C 20烷基在所述烷基的一个或多个碳原子上带有取代基R 3; R 3独立地是H，OR 4，SR 4，卤素，卤代烷基，卤代烷氧基，NO 2，CN，SO 2 NR 4 R 5，CO 2 NR 4 R 5，COR 4，，CO 2 R 4，SO 2 R 4，SO 3 R 4，NR 4 R 5，C 1 -C 5 - 烷基，芳基或杂芳基; R 4是选自环戊基，环己基，芳基，杂芳基的H，C 1 -C 5 - 烷基或不饱和或饱和碳环; R 5是H，O-烷基，O-芳基，烷基或芳基; Z 1和Z 2彼此独立地为O，S或NR 5，n为0或1。

8. 发明申请

WO2003039549A3 SELECTIVE ANTIBACTERIAL AGENTS 审中-公开
公开(公告)号：WO2003039549A3
公开(公告)日：2003-05-15
申请号：PCT/EP2002/011760
申请日：2002-10-21
申请人： 4SC AG , KRAMER, Bernd , AMMENDOLA, Aldo , SAEB, Wael
发明人： KRAMER, Bernd , AMMENDOLA, Aldo , SAEB, Wael
IPC分类号： A61K31/505
摘要： The present invention relates to the use of compounds of the general Formula (I), for the regulation of the quorum sensing system of microorganisms wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R 1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R 2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A 1 and A 2 each independently represent an optionally substituted C 1 -C 20 -alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR 4 , CO, CO 2 , CS, SO or SO 2 X is selected from the group consisting of S, O, N, NR 4 , SO or SO 2 ; said substituted ring system carries a substituent R 3 on one or more of the carbon atoms of said ring system;said substituted C 1 -C 20 -alkyl group carries a substituent R 3 on one or more of the carbon atoms of said alkyl group; R 3 is independently H, OR 4 , SR 4 , hydroxyalkyl, hydroxyalkylamino, cycloalkyl, halogen, haloalkyl, haloalkyloxy, NO 2 , CN, SO 2 NR 4 R 5 , CO 2 NR 4 R 5 , COR 4 , CO 2 R 4 , SO 2 R 4 , SO 3 R 4 , NR 4 R 5 , alkyl, aryl or heteroaryl; R 4 is H, alkyl, cycloalkyl, aryl or heteroaryl; R 5 is H, O-alkyl, O-aryl, alkyl, heteroaryl or aryl; Y 1 and Y 2 are independent from each other C=O, C=S, SO 2 or C=NR 5 ; p is 0, m is 0, n is 0; or p is 0, m is 0, n is 1;or p is 0, m is 1, n is 1; or p is 1, m is 0, n is 0; or p is 1, m is 0, n is 1; or p is 1, m is 1, n is 1.

9. 发明申请

WO2003039529A1 SELECTIVE ANTIBACTERIAL AGENTS 审中-公开
标题翻译：选择性抗菌剂
公开(公告)号：WO2003039529A1
公开(公告)日：2003-05-15
申请号：PCT/EP2001/012875
申请日：2001-11-07
申请人： 4SC A.G. , AMMENDOLA, Aldo , KRAMER, Bernd , SAEB, Wael
发明人： AMMENDOLA, Aldo , KRAMER, Bernd , SAEB, Wael
IPC分类号： A61K31/175
CPC分类号： A61K8/49 , A01N43/54 , A01N43/56 , A61K8/4973 , A61K8/4986 , A61K31/175 , A61K31/38 , A61K31/415 , A61K31/42 , A61K31/435 , A61K31/44 , A61K31/445 , A61Q17/005 , A61Q19/00 , C07D231/16 , C07D231/40 , C07D307/68 , C07D333/38 , C07D333/70 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04
摘要： The present invention relates to the use of compounds of the general Formula (I) for regulation of the quorum sensing system of microorganisms, wherein in Formula (I) R 1 is H, C 1 -C 5 -alkyl or an unsaturated or saturated carbocycle selected from the group consisting of cyclopentyl, cyclohexyl, aryl and heteroaryl; R 2 is H, C 1 -C 5 -alkyl or an unsaturated or saturated carbocycle selected from the group consisting of cyclopentyl, cyclohexyl, aryl and heteroaryl; A 1 and A 2 are independently from each other an unsubstituted or substituted C 1 -C 20 -alkyl group or a monocyclic or polycyclic substituted or unsubstituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; X is selected from the group consisting of S, O, NH, NHR 4 ,SO or SO 2 ; said substituted ring system carries a substituent R 3 on one or more of the carbon atoms of said ring system; said substituted C 1 -C 20 -alkyl group carries a substituent R 3 on one or more of the carbon atoms of said alkyl group; R 3 is independently H, OR 4 , SR 4 , halogen, haloalkyl, haloalkyloxy, NO 2 , CN, SO 2 NR 4 R 5 , CO 2 NR 4 R 5 , COR 4 , CO 2 R 4 , SO 2 R 4 , SO 3 R 4 , NR 4 R 5 , C 1 -C 5 -alkyl, aryl, or heteroaryl; R 4 is H, C 1 -C 5 -alkyl or unsaturated or saturated carbocycle selected from the group consisting of cyclopentyl, cyclohexyl, aryl, heteroaryl; R 5 is H, O-alkyl, O-aryl, alkyl or aryl; Z 1 and Z 2 are independent from each other O, S or NR 5 , n is 0 or 1.
摘要翻译：本发明涉及通式（I）化合物用于调节微生物群体感应系统的用途，其中在式（I）中R1是H，C1-C5-烷基或不饱和或饱和碳环，其选自由环戊基，环己基，芳基和杂芳基组成的基团; R2是H，C1-C5-烷基或选自环戊基，环己基，芳基和杂芳基的不饱和或饱和碳环; A 1和A 2彼此独立地是未被取代或取代的C 1 -C 20 - 烷基或可以含有一个或多个X基团的单环或多环取代或未取代的芳族或非芳族环系统，并且在多环系统，所述系统含有至少一个芳环; X选自S，O，NH，NHR 4，SO或SO 2; 所述取代的环系统在所述环系统的一个或多个碳原子上携带取代基R3; 所述取代的C 1 -C 20烷基在所述烷基的一个或多个碳原子上带有取代基R 3; R3独立地为H，OR4，SR4，卤素，卤代烷基，卤代烷氧基，NO2，CN，SO2NR4R5，CO2NR4R5，COR4，CO2R4，SO2R4，SO3R4，NR4R5，C1-C5-烷基，芳基或杂芳基; R4是选自环戊基，环己基，芳基，杂芳基的H，C1-C5-烷基或不饱和或饱和碳环; R5是H，O-烷基，O-芳基，烷基或芳基; Z1和Z2彼此独立为O，S或NR5，n为0或1。

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