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    • 1. 发明申请
      WO2003039549A3 SELECTIVE ANTIBACTERIAL AGENTS 审中-公开
    • SELECTIVE ANTIBACTERIAL AGENTS
    • WO2003039549A3
    • 2003-05-15
    • PCT/EP2002/011760
    • 2002-10-21
    • 4SC AG , KRAMER, Bernd , AMMENDOLA, Aldo , SAEB, Wael
    • KRAMER, Bernd , AMMENDOLA, Aldo , SAEB, Wael
    • A61K31/505
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 2. 发明申请
      WO2003039529A1 SELECTIVE ANTIBACTERIAL AGENTS 审中-公开
    • SELECTIVE ANTIBACTERIAL AGENTS
    • 选择性抗菌剂
    • WO2003039529A1
    • 2003-05-15
    • PCT/EP2001/012875
    • 2001-11-07
    • 4SC A.G. , AMMENDOLA, Aldo , KRAMER, Bernd , SAEB, Wael
    • AMMENDOLA, Aldo , KRAMER, Bernd , SAEB, Wael
    • A61K31/175
    • 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
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 3. 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
    • N-SUBSTITUTED 6,8-DIALKOXY-1,2,3,4-TETRAHYDRO-1H-ISOQUINOLINE AS POTASSIUM CHANNELS MODULATORS
    • 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
    • WO2004113302A1
    • 2004-12-29
    • PCT/EP2004/006552
    • 2004-06-17
    • 4SC AG , GARCIA, Gabriel , SAEB, Wael , KRAMER, Bernd
    • GARCIA, Gabriel , SAEB, Wael , KRAMER, Bernd
    • C07D217/06
    • C07D217/06
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明申请
      WO2003006424A1 NOVEL COMPOUNDS AS ANTI-INFLAMMATORY, IMMUNOMODULATORY AND ANTI-PROLIFERATORY AGENTS 审中-公开
    • NOVEL COMPOUNDS AS ANTI-INFLAMMATORY, IMMUNOMODULATORY AND ANTI-PROLIFERATORY AGENTS
    • 新型化合物作为抗炎药，免疫调节剂和抗增生剂
    • WO2003006424A1
    • 2003-01-23
    • PCT/EP2001/007948
    • 2001-07-10
    • 4SC AG , KRAMER, Bernd , LEBAN, Johann
    • KRAMER, Bernd , LEBAN, Johann
    • C07C233/60
    • C07C233/58 , C07C233/59 , C07C233/60 , C07C233/62 , C07C255/60 , C07C323/40 , C07C2601/02 , C07C2601/10 , C07C2601/16 , C07D307/30 , C07D333/38 , C07D333/58 , C07D335/12
    • The present invention relates to compounds of the general formula (I), wherein A is a non-aromatic ring system containing 4 to 8 carbon atoms, wherein the ring system comprises at least one double bond and wherein one or more of the carbon atoms in the ring can be substituted by a group X, wherein X is selected from the group consisting of S, O, N, NH, NHR 4 , SO or SO 2 , and wherein one or more of the carbon atoms of the ring can carry a substituent R 1 ; D is O, S, SO 2 , NH, NHR 4 , or CH 2 ; R 1 is independently H, halogen, CF 3 , OCF 3 , or C 1 -C 5 -alkyl; R 2 is H, OH, OR 6 , NH 2 , NHR 7 ; R 6 is H, alkyl, cycloalkyl, aryl, arylalkyl, alkylaryl, alkoxyalkyl, acylmethyl, (acyloxy)alkyl, non-symmetrical(acyloxy)alkyldiester, dialkylphosphate; R 7 is H, alkyl, aryl, O-alkyl, O-aryl, cycloalkyl or O-cycloalkyl; R 8 is hydrogen or alkyl; R 3 is H, cycloalkyl, aryl, O-alkyl, O-aryl or O-cycloalkyl; R 4 is C 1 -C 5 -alkyl or an unsaturated or saturated carbocycle selected from the group consisting of cyclopentyl, cyclohexyl or aryl; Z 1 and Z 2 are independent from each other O, S, NH or NR 5 ; R 5 is OH, O-alkyl, O-aryl, alkyl or aryl; Ar is a monocyclic or polycyclic substituted or unsubstituted ring system which may contain one or more groups X and which contains at least one aromatic ring; Y is hydrogen, halogen, CF 3 , OCF 3 , substituted or unsubstituted alkyl; substituted or unsubstituted cycloalkyl, Ar, O-substituted or unsubstituted Ar, O-substituted or unsubstituted alkylaryl, O-substituted or unsubstituted arylalkyl or (Formula); m is 0 or 1; and q is 0 to 10; with the proviso that when ring A is an unsubstituted carbocyclus containing five carbon atoms and one double bond between the CZ 1 and CZ 2- substituents with Z 1 = Z 2 = O and R 2 = OH, the following compounds are excluded: q = 0; Y = hydrogen; Ar = phenylene or naphthylene, phenylene substituted with one or two chlorine atoms or with 2-methyl, 4-methyl, 4-methoxy, 4-ethoxy, 2, 6-diethyl, 2-chloro-4-methyl, 4-bromo, 4-cyano, 2, 3-difluoro, 2, 6-difluoro, 2, 3, 4-trifluoro; q = 0; Y = phenyl; Ar = phenylene; Q = 1; m = 1; R 3 = H; Ar = phenylene; Y = 4-chloro-phenyl; D = O, S; q =1; m = 1; R 3 = H; Ar = phenylene; Y = 4-phenyl; D = O.
    • 本发明涉及通式（I）的化合物，其中A是含有4-8个碳原子的非芳族环系，其中该环系包括至少一个双键，并且其中一个或多个碳原子在 该环可以被X基团取代，其中X选自S，O，N，NH，NHR 4，SO或SO 2，并且其中一个或多个环的碳原子可以携带 取代基R 1; D是O，S，SO 2，NH，NHR 4或CH 2; R 1独立地是H，卤素，CF 3，OCF 3或C 1 -C 5 - 烷基; R 2是H，OH，OR 6，NH 2，NHR 7; R 6是H，烷基，环烷基，芳基，芳烷基，烷基芳基，烷氧基烷基，酰基甲基，（酰氧基）烷基，非对称（酰氧基）烷基二酯，磷酸二烷基酯; R 7是H，烷基，芳基，O-烷基，O-芳基，环烷基或O-环烷基; R 8是氢或烷基; R 3是H，环烷基，芳基，O-烷基，O-芳基或O-环烷基; R 4是C 1 -C 5烷基或选自环戊基，环己基或芳基的不饱和或饱和碳环; Z 1和Z 2彼此独立地为O，S，NH或NR 5; R 5是OH，O-烷基，O-芳基，烷基或芳基; Ar是可以含有一个或多个基团X并且含有至少一个芳环的单环或多环取代或未取代的环系; Y是氢，卤素，CF 3，OCF 3，取代或未取代的烷基; 取代或未取代的环烷基，Ar，O-取代或未取代的Ar，O-取代或未取代的烷基芳基，O-取代或未取代的芳烷基或（式）; m为0或1; q为0〜10; 条件是当环A是具有Z 1 = Z 2 = O且R 2 = 0的CZ 1和CZ 2 - 取代基之间具有5个碳原子和1个双键的未取代的碳环化合物时， OH，不包括以下化合物：q = 0; Y =氢; Ar =亚苯基或亚萘基，被一个或两个氯原子取代的亚苯基或与2-甲基，4-甲基，4-甲氧基，4-乙氧基，2,6-二乙基，2-氯-4-甲基，4-溴， 4-氰基，2,3-二氟，2,6-二氟，2,3,4-三氟; q = 0; Y =苯基; Ar =亚苯基; Q = 1; m = 1; R 3 = H; Ar =亚苯基; Y = 4-氯 - 苯基; D = O，S; q = 1; m = 1; R 3 = H; Ar =亚苯基; Y = 4-苯基; D = O
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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