公开(公告)号：US20070027193A1

公开(公告)日：2007-02-01

申请号：US10736739

申请日：2004-11-10

申请人： Johann Leban ,  Bernd Kramer ,  Roland Baugartner ,  Katharina Aulinger-Fuchs ,  Stefan Tasler

发明人： Johann Leban ,  Bernd Kramer ,  Roland Baugartner ,  Katharina Aulinger-Fuchs ,  Stefan Tasler

IPC分类号： A61K31/44 ,  A61K31/401

CPC分类号： A61K31/401 ,  A61K31/44 ,  C07C233/60 ,  C07C2601/10 ,  C07D333/24 ,  Y02A50/411

摘要： The present invention provides a compound capable of binding to the ubiquinone binding site of DHODH which contains a non-aromatic ring system as a core structure, a group capable of interacting with structural elements of subsite 2 or 3 of the ubiquinone binding site of DHODH and a group capable of interacting hydrophobically with structural elements of subsite 1 of the ubiquinone binding site of DHODH. Furthermore, the present invention provides a compound capable of binding to the ubiquinone binding site of DHODH which contains an aromatic ring system as a core structure, a group capable of interacting with residues His 56 and/or Tyr 356 of subsite 3 of the ubiquinone binding site of DHODH and a group capable of interacting hydrophobically with structural elements of subsite 1 of the ubiquinone binding site of DHODH.

公开(公告)号：US20070224672A1

公开(公告)日：2007-09-27

申请号：US11626140

申请日：2007-01-23

申请人： Johann Leban ,  Bernd Kramer ,  Roland Baumgartner ,  Katharina Aulinger-Fuchs ,  Stefan Tasler

发明人： Johann Leban ,  Bernd Kramer ,  Roland Baumgartner ,  Katharina Aulinger-Fuchs ,  Stefan Tasler

IPC分类号： C12N9/02 ,  G06F19/00

CPC分类号： A61K31/401 ,  A61K31/44 ,  C07C233/60 ,  C07C2601/10 ,  C07D333/24 ,  Y02A50/411

摘要： The present invention provides a compound capable of binding to the ubiquinone binding site of DHODH which contains a non-aromatic ring system as a core structure, a group capable of interacting with structural elements of subsite 2 or 3 of the ubiquinone binding site of DHODH and a group capable of interacting hydrophobically with structural elements of subsite 1 of the ubiquinone binding site of DHODH. Furthermore, the present invention provides a compound capable of binding to the ubiquinone binding site of DHODH which contains an aromatic ring system as a core structure, a group capable of interacting with residues His 56 and/or Tyr 356 of subsite 3 of the ubiquinone binding site of DHODH and a group capable of interacting hydrophobically with structural elements of subsite 1 of the ubiquinone binding site of DHODH.

摘要翻译： 本发明提供能够结合DHODH的泛素结合位点的化合物，其含有非芳香族环系统作为核心结构，能够与DHODH的泛素结合位点的亚位点2或3的结构元件相互作用的基团和 能够与DHODH的泛醌结合位点的亚位点1的结构元件疏水相互作用的基团。 此外，本发明提供能够结合含有芳环系统作为核心结构的DHODH的泛素结合位点的化合物，能够与泛醌结合的亚位点3的残基His 56和/或Tyr 356相互作用的基团 DHODH的位点和能够与DHODH的泛素结合位点的亚位点1的结构元件疏水相互作用的基团。

公开(公告)号：US07247736B2

公开(公告)日：2007-07-24

申请号：US10736739

申请日：2004-11-10

申请人： Johann Leban ,  Bernd Kramer ,  Roland Baumgartner ,  Katharina Aulinger-Fuchs ,  Stefan Tasler

发明人： Johann Leban ,  Bernd Kramer ,  Roland Baumgartner ,  Katharina Aulinger-Fuchs ,  Stefan Tasler

IPC分类号： C07D333/10 ,  C07C235/84

CPC分类号： A61K31/401 ,  A61K31/44 ,  C07C233/60 ,  C07C2601/10 ,  C07D333/24 ,  Y02A50/411

摘要： The present invention provides a compound capable of binding to the ubiquinone binding site of DHODH which contains a non-aromatic ring system as a core structure, a group capable of interacting with structural elements of subsite 2 or 3 of the ubiquinone binding site of DHODH and a group capable of interacting hydrophobically with structural elements of subsite 1 of the ubiquinone binding site of DHODH. Furthermore, the present invention provides a compound capable of binding to the ubiquinone binding site of DHODH which contains an aromatic ring system as a core structure, a group capable of interacting with residues His 56 and/or Tyr 356 of subsite 3 of the ubiquinone binding site of DHODH and a group capable of interacting hydrophobically with structural elements of subsite 1 of the ubiquinone binding site of DHODH.

摘要翻译： 本发明提供能够结合DHODH的泛素结合位点的化合物，其含有非芳香族环系统作为核心结构，能够与DHODH的泛素结合位点的亚位点2或3的结构元件相互作用的基团和 能够与DHODH的泛醌结合位点的亚位点1的结构元件疏水相互作用的基团。 此外，本发明提供能够结合含有芳环系统作为核心结构的DHODH的泛素结合位点的化合物，能够与泛醌结合的亚位点3的残基His 56和/或Tyr 356相互作用的基团 DHODH的位点和能够与DHODH的泛素结合位点的亚位点1的结构元件疏水相互作用的基团。

公开(公告)号：US20070208012A1

公开(公告)日：2007-09-06

申请号：US11561701

申请日：2006-11-20

申请人： Aldo Ammendola ,  Katharina Aulinger-Fuchs ,  Astrid Gotschlich ,  Bernd Kramer ,  Martin Lang ,  Wael Saeb ,  Udo Sinks ,  Andreas Wuzik

发明人： Aldo Ammendola ,  Katharina Aulinger-Fuchs ,  Astrid Gotschlich ,  Bernd Kramer ,  Martin Lang ,  Wael Saeb ,  Udo Sinks ,  Andreas Wuzik

IPC分类号： A01N43/58 ,  C07D409/00 ,  A01N43/54 ,  A01N43/60 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

CPC分类号： C07D231/40 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D209/08 ,  C07D209/42 ,  C07D209/86 ,  C07D211/16 ,  C07D211/22 ,  C07D211/34 ,  C07D211/60 ,  C07D231/12 ,  C07D261/14 ,  C07D263/48 ,  C07D277/36 ,  C07D277/46 ,  C07D307/66 ,  C07D307/68 ,  C07D333/36 ,  C07D333/38

摘要： The present invention relates to the use of compounds of the general Formula (XIII): In particular the invention refers to a family of compounds that block the quorum sensing system of Gram-negative bacteria, a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of microbial damages and diseases, in particular for diseases where there is an advantage in inhibiting quorum sensing regulated phenotypes of pathogens.

公开(公告)号：US20070093534A1

公开(公告)日：2007-04-26

申请号：US11560699

申请日：2006-11-16

申请人： Aldo Ammendola ,  Katharina Aulinger-Fuchs ,  Astrid Gotschlich ,  Bernd Kramer ,  Martin Lang ,  Wael Saeb ,  Udo Sinks ,  Andreas Wuzik

发明人： Aldo Ammendola ,  Katharina Aulinger-Fuchs ,  Astrid Gotschlich ,  Bernd Kramer ,  Martin Lang ,  Wael Saeb ,  Udo Sinks ,  Andreas Wuzik

IPC分类号： A61K31/4439 ,  A61K31/427 ,  A61K31/422 ,  A61K31/4192 ,  A61K31/416 ,  A61K31/4178 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

CPC分类号： C07D231/40 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D209/08 ,  C07D209/42 ,  C07D209/86 ,  C07D211/16 ,  C07D211/22 ,  C07D211/34 ,  C07D211/60 ,  C07D231/12 ,  C07D261/14 ,  C07D263/48 ,  C07D277/36 ,  C07D277/46 ,  C07D307/66 ,  C07D307/68 ,  C07D333/36 ,  C07D333/38

摘要： The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C═O, C═S, SO2, CH—OR13, C═NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C═O, C═S, SO2, CH—OR13, C═NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;

公开(公告)号：US20100280036A1

公开(公告)日：2010-11-04

申请号：US12005810

申请日：2007-12-28

申请人： Aldo Ammendola ,  Katharina Aulinger-Fuchs ,  Astrid Gotschlich ,  Bernd Kramer ,  Martin Lang ,  Wael Saeb ,  Udo Sinks ,  Andreas Wuzik

发明人： Aldo Ammendola ,  Katharina Aulinger-Fuchs ,  Astrid Gotschlich ,  Bernd Kramer ,  Martin Lang ,  Wael Saeb ,  Udo Sinks ,  Andreas Wuzik

IPC分类号： A61K31/498 ,  C12N1/20 ,  A61K31/506 ,  A61K31/444 ,  A61K31/4436 ,  A61K31/426 ,  A61K31/425 ,  A61K31/421 ,  A61K31/42 ,  A61K31/4155 ,  A61K31/381 ,  C07D403/12 ,  C07D409/12 ,  C07D401/12 ,  C07D277/54 ,  C07D275/03 ,  C07D263/48 ,  C07D261/18 ,  C07D333/38 ,  A61P31/04

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 ,  Y02A50/473

摘要： The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 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, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2;

摘要翻译： 本发明涉及通式（I）的化合物的用途：其中在式（I）中，R为H，烷基，环烷基，芳基或杂芳基; R1是H，烷基，环烷基，芳基或杂芳基; R2是H，烷基，环烷基，芳基或杂芳基; A1和A2各自独立地表示可以含有一个或多个Z基团或可以含有一个或多个基团的单环或多环任选取代的芳族或非芳族环系的任选取代的C 1 -C 20 - 烷基 ）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，NR4，CO，CO2，CS，SO或SO2 X选自S，O，N，NR4，SO或SO2;

公开(公告)号：US20080188536A1

公开(公告)日：2008-08-07

申请号：US12005763

申请日：2007-12-28

申请人： Aldo Ammendola ,  Katharina Aulinger-Fuchs ,  Astrid Gotschlich ,  Bernd Kramer ,  Martin Lang ,  Wael Saeb ,  Udo Sinks ,  Andreas Wuzik

发明人： Aldo Ammendola ,  Katharina Aulinger-Fuchs ,  Astrid Gotschlich ,  Bernd Kramer ,  Martin Lang ,  Wael Saeb ,  Udo Sinks ,  Andreas Wuzik

IPC分类号： A61K31/415 ,  C07D231/40 ,  A01N43/56 ,  A61P31/04 ,  A01P1/00

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 ,  Y02A50/473

摘要： The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 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, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2;

公开(公告)号：US20080188491A1

公开(公告)日：2008-08-07

申请号：US12005920

申请日：2007-12-28

申请人： Aldo Ammendola ,  Katharina Aulinger-Fuchs ,  Astrid Gotschlich ,  Bernd Kramer ,  Martin Lang ,  Wael Saeb ,  Udo Sinks ,  Andreas Wuzik

发明人： Aldo Ammendola ,  Katharina Aulinger-Fuchs ,  Astrid Gotschlich ,  Bernd Kramer ,  Martin Lang ,  Wael Saeb ,  Udo Sinks ,  Andreas Wuzik

IPC分类号： A61K31/495 ,  C07D401/02 ,  C07D401/12 ,  A61K31/437 ,  A61K31/444 ,  C07D239/24 ,  A61P31/04

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 ,  Y02A50/473

摘要： The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 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, NR4, CO, CO, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2.

摘要翻译： 本发明涉及通式（I）的化合物的用途：其中在式（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各自独立地表示任选取代的C 1 -C 20 -C 20 - 烷基，其可以含有 一个或多个Z基团或可以含有一个或多个基团X的单环或多环任选取代的芳族或非芳族环系统，并且在多环系统的情况下，所述体系包含至少一个 芳香环 Z选自S，O，N，NR 4，CO，CO，CS，SO或SO 2 X选自S ，O，N，NR 4，SO或SO 2。

公开(公告)号：US20080176938A1

公开(公告)日：2008-07-24

申请号：US12005983

申请日：2007-12-28

申请人： Aldo Ammendola ,  Katharina Aulinger-Fuchs ,  Astrid Gotschlich ,  Bernd Kramer ,  Martin Lang ,  Wael Saeb ,  Udo Sinks ,  Andreas Wuzik

发明人： Aldo Ammendola ,  Katharina Aulinger-Fuchs ,  Astrid Gotschlich ,  Bernd Kramer ,  Martin Lang ,  Wael Saeb ,  Udo Sinks ,  Andreas Wuzik

IPC分类号： A61K31/341 ,  C07D307/34 ,  A01N43/08 ,  A61P31/04 ,  A01P1/00

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 ,  Y02A50/473

摘要： The present invention relates to the use of compounds of the general Formula (1): wherein in Formula (1), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 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, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2.

摘要翻译： 本发明涉及通式（1）的化合物的用途：其中在式（1）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各自独立地表示任选取代的C 1 -C 20 -C 20 - 烷基，其可以含有 一个或多个Z基团或可以含有一个或多个基团X的单环或多环任选取代的芳族或非芳族环系统，并且在多环系统的情况下，所述体系包含至少一个 芳香环 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。

公开(公告)号：US20100280034A1

公开(公告)日：2010-11-04

申请号：US12005783

申请日：2007-12-28

申请人： Aldo Ammendola ,  Katharina Aulinger-Fuchs ,  Astrid Gotschlich ,  Bernd Kramer ,  Martin Lang ,  Wael Saeb ,  Udo Sinks ,  Andreas Wuzik

发明人： Aldo Ammendola ,  Katharina Aulinger-Fuchs ,  Astrid Gotschlich ,  Bernd Kramer ,  Martin Lang ,  Wael Saeb ,  Udo Sinks ,  Andreas Wuzik

IPC分类号： A61K31/5375 ,  C12N1/20 ,  A61K31/495 ,  A61K31/47 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/426 ,  A61K31/421 ,  A61K31/4168 ,  A61K31/415 ,  A61K31/403 ,  A61K31/404 ,  A61K31/4015 ,  A61K31/381 ,  A61K31/341 ,  A61K31/196 ,  A61K31/167 ,  C07D295/185 ,  C07D215/08 ,  C07D401/06 ,  C07D211/16 ,  C07D277/46 ,  C07D263/48 ,  C07D261/14 ,  C07D231/40 ,  C07D209/86 ,  C07D209/08 ,  C07D207/27 ,  C07D333/38 ,  C07D307/68 ,  C07C229/56 ,  C07C235/00 ,  A01N43/56 ,  A01P15/00 ,  A61P31/04 ,  A01N43/10 ,  A01N43/78 ,  A01N43/80 ,  A01N43/50 ,  A01N43/08 ,  A01N43/40 ,  A01N43/42 ,  A01N43/60 ,  A01N43/84 ,  A01N43/36 ,  A01N43/38 ,  A01N37/22 ,  A01N37/46

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 ,  C07D261/14 ,  C07D263/48 ,  C07D275/03 ,  C07D277/46 ,  C07D277/54 ,  C07D307/68 ,  C07D333/38 ,  C07D333/70 ,  C07D403/12 ,  C07D409/04 ,  C07D409/12 ,  C07D471/04 ,  Y02A50/473

摘要： The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C═O, C═S, SO2, CH—OR13, C═NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C═O, C═S, SO2, CH—OR13, C═NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;

摘要翻译： 本发明涉及通式（XIII）化合物的用途：其中A 7为C = O，C = S，SO 2，CH-OR 13，C = NR 12或CH 2 -CHOR 13; A8为C（R14）2，O，S或NR12; A9为C = O，C = S，SO2，CH-OR13，C = NR12或CH2-CHOR13; m为0或1 q为0或1 r为0，或1 R 12为H，CH 3，CH 2 -CH 3，C 6 H 5，OCH 3，OCH 2 -CH 3，OH或SH; R 13是H，CH 3或CH 2 -CH 3; R 14是H，烷基，烷氧基，OH或SH;