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1. 发明授权

US07247736B2 Method of identifying inhibitors of DHODH 有权
标题翻译：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。

2. 发明申请

US20070224672A1 Method of Identifying Inhibitors of DHODH 审中-公开
标题翻译：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。

3. 发明申请

US20070027193A1 Method of identifying inhibitors of DHODH 有权
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.

4. 发明授权

US08592456B2 IL17 and IFN-gamma inhibition for the treatment of autoimmune inflammation 有权
公开(公告)号：US08592456B2
公开(公告)日：2013-11-26
申请号：US13360050
申请日：2012-01-27
申请人： Johann Leban , Stefan Tasler , Roland Baumgartner , Wael Saeb , Carine Chevrier
发明人： Johann Leban , Stefan Tasler , Roland Baumgartner , Wael Saeb , Carine Chevrier
IPC分类号： A61K31/454 , A61K31/444 , A61K31/4439 , A61K31/422 , C07D401/14 , C07D405/14 , C07D405/04
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.

5. 发明授权

US07365094B2 Compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents 有权
标题翻译：化合物作为抗炎，免疫调节和抗增殖剂
公开(公告)号：US07365094B2
公开(公告)日：2008-04-29
申请号：US10736742
申请日：2003-12-17
申请人： Johann Leban , Stefan Tasler
发明人： Johann Leban , Stefan Tasler
IPC分类号： A61K31/341 , A61K31/381 , A61K31/4025 , C07D207/333 , C07D307/40 , C07D333/26
CPC分类号： C07D333/38 , C07D307/68
摘要： The present invention relates to compounds of the general formula (II) and salts and physiologically functional derivatives thereof, for the use as a medicament.
摘要翻译：本发明涉及用作药物的通式（II）的化合物及其盐和生理功能衍生物。

6. 发明授权

US08354436B2 IL17 and IFN-gamma inhibition for the treatment of autoimmune inflammation 有权
标题翻译： IL17和IFN-γ抑制用于治疗自身免疫性炎症
公开(公告)号：US08354436B2
公开(公告)日：2013-01-15
申请号：US13360063
申请日：2012-01-27
申请人： Johann Leban , Stefan Tasler , Wael Saeb , Carine Chevrier
发明人： Johann Leban , Stefan Tasler , Wael Saeb , Carine Chevrier
IPC分类号： A61K31/4406 , A61K31/4402 , A61K31/4409 , A61K31/4155 , C07D413/14 , C07D285/12 , C07D271/10 , C07D263/10 , C07D261/10
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

US20070037753A1 Inhibitors of cancer cell, T-cell and keratinocyte proliferation 失效
标题翻译：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。

8. 发明申请

US20060069102A1 Novel heterocyclic NF-kB inhibitors 失效
标题翻译：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，

9. 发明授权

US07601745B2 Heterocyclic NF-kB inhibitors 失效
标题翻译：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。

10. 发明授权

US07531517B2 Inhibitors of cancer cell, T-cell and keratinocyte proliferation 失效
标题翻译：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。

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