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    Method of identifying inhibitors of DHODH
    2.
    发明授权
    Method of identifying inhibitors of DHODH 有权
    鉴定DHODH抑制剂的方法

    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。

    Method of Identifying Inhibitors of DHODH
    3.
    发明申请
    Method of Identifying Inhibitors of DHODH 审中-公开
    鉴定DHODH抑制剂的方法

    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。

    Inhibitors of cancer cell, T-cell and keratinocyte proliferation
    7.
    发明申请
    Inhibitors of cancer cell, T-cell and keratinocyte proliferation 失效
    癌细胞抑制剂，T细胞和角化细胞增殖

    公开(公告)号：US20070037753A1

    公开(公告)日：2007-02-15

    申请号：US11501722

    申请日：2006-08-10

    申请人： Johann Leban ,  Martin Kralik

    发明人： Johann Leban ,  Martin Kralik

    IPC分类号： A61K38/05 ,  A61K38/04 ,  C07K5/04 ,  C07D403/02

    CPC分类号： C07D233/72 ,  A61K38/00 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/14 ,  C07K5/0205 ,  C07K5/06078 ,  C07K5/06191 ,  Y02A50/409

    摘要： The invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Y is —NRaRb, —NRcC═ONRaRb, —NRcC═SNRaRb, —NRcC═NRdNaRb, heterocycle, —C═ONRaRb, heterocycle, or aryl; n is 0 to 8; m is 0, or 1; r is 0 to 3; t is 0 to 3; X is O or N; Z is CH2, C═O, C═S or a single bond; Z1 is CO—R2, CS—R2, (CH2)t—R2 or the side-chain of a naturally occuring amino acid;, Z2 is CO—R2, CS—R2 or (CH2)t—R3 or the side-chain of a naturally occuring amino acid; Z3 is CO—R2, CS—R2 or (CH2)t—R4 or the side-chain of a naturally occuring amino acid; Z4 is H, alkyl, alkoxy, or cycloalkyl; R1, R2, R3, and R4 are independently from each other H, OH, SH, NH2, CN, NO2, alkyl, cycloalkyl, heterocycloalkyl, haloalkyl, alkylthio, haloalkyloxy, hydroxyalkyl, hydroxyalkylamino, alkylamino, alkylaryl, alkylsulfinyl, alkylsulfonyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxyalkyl, alkoxy, aryloxy, heteroaryl, aryl, or halogen.

    摘要翻译： 本发明涉及通式（I）的化合物及其盐和生理功能衍生物，其中Y是-NR a，R b， C-ON＆lt; b＆gt; b＆lt;＆lt;＆lt; C＆gt; C-SNR＆lt; b＆gt; b C 1 -C 6卤代烷基，杂环基，C 1 -C 6 - 杂环或芳基;杂环或芳基; n为0〜8; m为0或1; r为0〜3; t为0〜3; X是O或N; Z是CH 2，C-O，C-S或单键; Z 1是CO-R 2，CS-R 2，（CH 2）2， / SUB> -R 2或天然存在的氨基酸的侧链; Z 2是CO-R 2，CS- R 2或（CH 2）2 -TH 3或天然存在的氨基酸的侧链 ; Z 3是CO-R 2，CS-R 2或（CH 2 CH 2） / SUB→4或天然存在的氨基酸的侧链; Z 4是H，烷基，烷氧基或环烷基; R 1，R 2，R 3和R 4彼此独立地为H，OH，SH ，NH 2，CN，NO 2，烷基，环烷基，杂环烷基，卤代烷基，烷硫基，卤代烷氧基，羟烷基，羟烷基氨基，烷基氨基，烷基芳基，烷基亚磺酰基，烷基磺酰基，烷硫基烷基，烷基亚磺酰基烷基 烷基磺酰基烷基，烷氧基烷基，烷氧基，芳氧基，杂芳基，芳基或卤素。

    Novel heterocyclic NF-kB inhibitors
    8.
    发明申请
    Novel heterocyclic NF-kB inhibitors 失效
    新型杂环NF-kB抑制剂

    公开(公告)号：US20060069102A1

    公开(公告)日：2006-03-30

    申请号：US11192009

    申请日：2005-07-29

    申请人： Johann Leban ,  Harald Schmitt ,  Kristina Wolf ,  Stefano Pegoraro ,  Andreas Wuzik

    发明人： Johann Leban ,  Harald Schmitt ,  Kristina Wolf ,  Stefano Pegoraro ,  Andreas Wuzik

    IPC分类号： A61K31/496 ,  A61K31/4545 ,  C07D417/14

    CPC分类号： C07D401/14 ,  C07D263/48 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04

    摘要： The present invention relates to compounds of the general formula (1) and salts and physiologically functional derivatives thereof, wherein R1 is independently hydrogen; alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, R3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 is independently H, COR6, CO2R6, SOR6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 is independently H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; p is 0, or 1; q is 0, or 1; X is CO, or SO2.

    摘要翻译： 本发明涉及通式（1）的化合物及其盐和生理功能衍生物，

    Heterocyclic NF-kB inhibitors
    9.
    发明授权
    Heterocyclic NF-kB inhibitors 失效
    杂环NF-kB抑制剂

    公开(公告)号：US07601745B2

    公开(公告)日：2009-10-13

    申请号：US11375259

    申请日：2006-03-15

    申请人： Johann Leban ,  Harald Schmitt ,  Kristina Wolf ,  Stefano Pegoraro ,  Andreas Wuzik

    发明人： Johann Leban ,  Harald Schmitt ,  Kristina Wolf ,  Stefano Pegoraro ,  Andreas Wuzik

    IPC分类号： A01N43/52 ,  A01N43/78 ,  A61K31/415 ,  A61K31/425 ,  C07D235/04 ,  C07D263/58 ,  C07D263/60 ,  C07D277/82 ,  C07D403/02 ,  C07D413/00 ,  C07D498/00

    CPC分类号： C07D277/56 ,  C07D263/48 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

    摘要： The present invention relates to compounds of the general formula (III) or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof, wherein R3 is H, —C(O)NRaRb, halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR4′OR5′, NH2, amine, alkylamine, alkoxy, cycloalkyl, heterocycloalkyl, hydroxyalkyl, or haloalkyloxy; R4 is H, halogen, alkyl, —C(NR7)NR7R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N═CR7R8, —NR7C(O)R8, cycloalkyl, heterocycloalkyl, haloalkyl, hydroxyalkyl, hyodroxyalkylamino, alkylamino, heteroaryl, or aryl; R5 is halogen, alkyl, —C(NR7)NR7R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N═CR7R8, —NR7C(O)R8, cycloalkyl, heterocycloalkyl, haloalkyl, hydroxyalkyl, hydroxyalkylamino, alkylamino, heteroaryl, or aryl.

    摘要翻译： 本发明涉及通式（III）的化合物或其药学上可接受的盐与酸或碱或其药学上可接受的前药或立体异构体，其中R 3是H，-C（O）NR a R b，卤素，烷基， 卤代烷基，芳基，杂芳基，OH，SH，NR4'OR5'，NH2，胺，烷基胺，烷氧基，环烷基，杂环烷基，羟基烷基或卤代烷氧基。 R 4是H，卤素，烷基，-C（NR 7）NR 7 R 8， - （CH 2）paryl， - （CH 2）p NR 17 R 8，-C（O）NR 7 R 8，-N-CR 7 R 8，-NR 7 C（O）R 8，环烷基，杂环烷基， 卤代烷基，羟基烷基，羟基烷基氨基，烷基氨基，杂芳基或芳基; R5是卤素，烷基，-C（NR7）NR7R8， - （CH2）paryl， - （CH2）pNR7R8，-C（O）NR7R8，-N-CR7R8，-NR7C（O）R8，环烷基，杂环烷基，卤代烷基， 羟基烷基，羟基烷基氨基，烷基氨基，杂芳基或芳基。

    Inhibitors of cancer cell, T-cell and keratinocyte proliferation
    10.
    发明授权
    Inhibitors of cancer cell, T-cell and keratinocyte proliferation 失效
    癌细胞抑制剂，T细胞和角化细胞增殖

    公开(公告)号：US07531517B2

    公开(公告)日：2009-05-12

    申请号：US11501722

    申请日：2006-08-10

    申请人： Johann Leban ,  Martin Kralik

    发明人： Johann Leban ,  Martin Kralik

    IPC分类号： A61K38/05

    CPC分类号： C07D233/72 ,  A61K38/00 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/14 ,  C07K5/0205 ,  C07K5/06078 ,  C07K5/06191 ,  Y02A50/409

    摘要： The invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Y is —NRaRb, —NRcC═ONRaRb, —NRcC═SNRaRb, —NRcC═NRdNaRb, heterocycle, —C═ONRaRb, heterocycle, or aryl; n is 0 to 8; m is 0, or 1; r is 0 to 3; t is 0 to 3; X is O or N; Z is CH2, C═O, C═S or a single bond; Z1 is CO—R2, CS—R2, (CH2)t—R2 or the side-chain of a naturally occuring amino acid;, Z2 is CO—R2, CS—R2 or (CH2)t—R3 or the side-chain of a naturally occuring amino acid; Z3 is CO—R2, CS—R2 or (CH2)t—R4 or the side-chain of a naturally occuring amino acid; Z4 is H, alkyl, alkoxy, or cycloalkyl; R1, R2, R3, and R4 are independently from each other H, OH, SH, NH2, CN, NO2, alkyl, cycloalkyl, heterocycloalkyl, haloalkyl, alkylthio, haloalkyloxy, hydroxyalkyl, hydroxyalkylamino, alkylamino, alkylaryl, alkylsulfinyl, alkylsulfonyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxyalkyl, alkoxy, aryloxy, heteroaryl, aryl, or halogen.

    摘要翻译： 本发明涉及通式（I）的化合物及其盐和生理功能衍生物，其中Y为-NR a R b，-NR c C -ONR a R b，-NR c C -R SNR a R b，-NR c C-NR d N a R b，杂环，-C-ONR a R b，杂环， 或芳基; n为0〜8; m为0或1; r为0〜3; t为0〜3; X是O或N; Z是CH 2，C-O，C-S或单键; Z1是CO-R2，CS-R2，（CH2）t-R2或天然存在的氨基酸的侧链; Z2是CO-R2，CS-R2或（CH2）t-R3或侧链 的天然存在的氨基酸; Z3是CO-R2，CS-R2或（CH2）t-R4或天然存在的氨基酸的侧链; Z4是H，烷基，烷氧基或环烷基; R 1，R 2，R 3和R 4彼此独立地是H，OH，SH，NH 2，CN，NO 2，烷基，环烷基，杂环烷基，卤代烷基，烷硫基，卤代烷氧基，羟烷基，羟烷基氨基，烷基氨基，烷基芳基，烷基亚磺酰基，烷基磺酰基， 烷基亚磺酰基烷基，烷基磺酰基烷基，烷氧基烷基，烷氧基，芳氧基，杂芳基，芳基或卤素。