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1. 发明申请

WO2012001151A1 NOVEL SALTS AS ANTI-INFLAMMATORY, IMMUNOMODULATORY AND ANTI-PROLIFERATORY AGENTS 审中-公开
标题翻译：作为抗炎剂，免疫调节剂和抗增生剂的新型盐
公开(公告)号：WO2012001151A1
公开(公告)日：2012-01-05
申请号：PCT/EP2011/061132
申请日：2011-07-01
申请人： 4SC AG , AMMENDOLA, Aldo , DIEDERICHS, Julia , LEBAN, Johann , VITT, Daniel
发明人： AMMENDOLA, Aldo , DIEDERICHS, Julia , LEBAN, Johann , VITT, Daniel
IPC分类号： C07C233/58 , C07C233/59 , C07C233/60 , C07D307/30 , C07D333/38 , C07D333/58 , A61K31/167
CPC分类号： C07D333/38 , C07C233/59 , C07C233/60 , C07C255/60 , C07C2601/10 , C07D307/30 , C07D333/58
摘要： The present invention relates to a salt selected from the group comprising the N-methyl-D- glucamine salt (NMG), the diethylamine salt (DEA) salt, the magnesium salt, the tromethamine salt, the choline salt, the L-arginine salt, the zinc salt, and the 4-(2- hydroxyethyl)niorpholine (HEM) salt of compounds of the general formula (I) wherein X is selected from the group consisting of CH 2 , S, or O; D is O or S; R 8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1; and q is 0 or 1; with the proviso that compounds wherein X = CH 2 , q = 0, Y = unsubstituted phenyl and E = unsubstituted phenylene are excluded; or a hydrate thereof.
摘要翻译：本发明涉及选自N-甲基-D-葡萄糖胺盐（NMG），二乙胺盐（DEA）盐，镁盐，氨基丁三醇盐，胆碱盐，L-精氨酸盐，锌盐和通式（I）化合物的4-（2-羟基乙基）二脯氨酸（HEM）盐，其中X选自CH 2，S或O; D为O或S; R8是氢或烷基; E是任选取代的亚苯基; Y是单环或双环取代或未取代的6-9元环系，其可含有一个或多个选自N或S的杂原子并且含有至少一个芳环; n为0或1; q为0或1; 条件是其中X = CH 2，q = 0，Y =未取代的苯基和E =未取代的亚苯基的化合物被排除; 或其水合物。

2. 发明申请

WO2012001148A1 NOVEL CALCIUM SALTS OF COMPOUND AS ANTI-INFLAMMATORY, IMMUNOMODULATORY AND ANTI-PROLIFERATORY AGENTS 审中-公开
标题翻译：作为抗炎剂，免疫调节剂和抗增生剂的化合物的新型钙盐
公开(公告)号：WO2012001148A1
公开(公告)日：2012-01-05
申请号：PCT/EP2011/061128
申请日：2011-07-01
申请人： 4SC AG , AMMENDOLA, Aldo , DIEDERICHS, Julia , LEBAN, Johann , VITT, Daniel
发明人： AMMENDOLA, Aldo , DIEDERICHS, Julia , LEBAN, Johann , VITT, Daniel
IPC分类号： C07C233/58 , C07C233/59 , C07C233/60 , C07D307/30 , C07D333/38 , C07D333/58 , A61K31/167
CPC分类号： C07D333/38 , C07C233/59 , C07C233/60 , C07C255/60 , C07C2601/10 , C07D307/30 , C07D333/58
摘要： The present invention relates to calcium salts of compounds of the general formula (I) wherein X is selected from the group consisting of CH 2 , S, or O; D is O or S; R 8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1, and q is 0 or 1; with the proviso that compounds wherein X = CH 2 , q =0, Y- unsubstituted phenyl and E = unsubstituted phenylene are excluded; or a hydrate thereof.
摘要翻译：本发明涉及通式（I）化合物的盐，其中X选自CH 2，S或O; D为O或S; R8是氢或烷基; E是任选取代的亚苯基; Y是单环或双环取代或未取代的6-9元环系，其可含有一个或多个选自N或S的杂原子并且含有至少一个芳环; n为0或1，q为0或1; 条件是排除其中X = CH 2，q = 0，Y-未取代的苯基和E =未取代的亚苯基的化合物; 或其水合物。

3. 发明申请

WO9622305A3 Modified peptides 审中-公开
标题翻译：修饰肽
公开(公告)号：WO9622305A3
公开(公告)日：1996-09-06
申请号：PCT/GB9600057
申请日：1996-01-12
申请人： WELLCOME FOUND , DANIELS ALEJANDRO JOSE , HEYER DENNIS , LEBAN JOHANN JAKOB
发明人： DANIELS ALEJANDRO JOSE , HEYER DENNIS , LEBAN JOHANN JAKOB
IPC分类号： A61K38/00 , C07C279/14 , C07K5/06 , C07K5/072 , A61K38/05
CPC分类号： C07K5/06095 , A61K38/00 , C07C279/14 , C07K5/06191
摘要： The present invention relates to compounds of formula (I), to the use of such compounds in medicine especially in the treatment or prophylaxis of conditions associated with eating disorders and to pharmaceutical compositions containing such compounds.

4. 发明申请

WO2010128050A3 DIHYDROOROTATE - DEHYDROGENASEE INHIBITORS AS VIROSTATIC COMPOUNDS 审中-公开
标题翻译： DIHYDROOROTETE - DEHYDROGENASEE抑制剂作为VIROSTATIC化合物
公开(公告)号：WO2010128050A3
公开(公告)日：2011-05-05
申请号：PCT/EP2010056042
申请日：2010-05-04
申请人： 4SC AG , VITT DANIEL , GROEPPEL MANFRED , BAUMGARTNER ROLAND , LEBAN JOHANN
发明人： VITT DANIEL , GROEPPEL MANFRED , BAUMGARTNER ROLAND , LEBAN JOHANN
IPC分类号： A61K31/196 , A61K31/341 , A61K31/381 , A61K31/44 , A61P31/12
CPC分类号： A61K31/196 , A61K31/341 , A61K31/381 , A61K31/44 , C07D213/78 , C07D307/68 , C07D333/38
摘要： The present invention relates to compounds of the general formula (I) 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（I）的化合物及其盐和生理功能衍生物。

5. 发明申请

WO2006032322A1 NOVEL HETEROCYCLIC NF-κB INHIBITORS 审中-公开
标题翻译：新型杂环NF-κB抑制剂
公开(公告)号：WO2006032322A1
公开(公告)日：2006-03-30
申请号：PCT/EP2005/008261
申请日：2005-07-29
申请人： 4SC AG , LEBAN, Johann , SCHMITT, Harald , WOLF, Kristina , PEGORARO, Stefano , WUZIK, Andreas
发明人： LEBAN, Johann , SCHMITT, Harald , WOLF, Kristina , PEGORARO, Stefano , WUZIK, Andreas
IPC分类号： C07D417/14
CPC分类号： C07D263/48 , C07D277/56 , C07D401/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/04 , C07D491/04 , C07D495/04
摘要： The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, (I) wherein R 1 is independently hydrogen, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R 2 is independently -NR 3 R 4 , (II) or (III) R 3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, -OH, -SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R 4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R 5 is independently H, COR 6 , C0 2 R 6 , SOR 6 , SO 2 R 6 , SO 3 R 6 , alkyl, cycloalkyl, alkoxy, -NH 2 , alkylamine, -NR 7 COR 6 , halogen, -OH, -SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R 6 is independently H, alkyl, cycloalkyl, -NH 2 , alkylamine, aryl or heteroaryl; R 7 is independently H, alkyl, cycloalkyl, alkoxy, -OH, -SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; p is 0, or l; q is 0, or 1; X is CO, or SO 2 .
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，（I）其中R

6. 发明申请

WO2003006424A1 NOVEL COMPOUNDS AS ANTI-INFLAMMATORY, IMMUNOMODULATORY AND ANTI-PROLIFERATORY AGENTS 审中-公开
标题翻译：新型化合物作为抗炎药，免疫调节剂和抗增生剂
公开(公告)号：WO2003006424A1
公开(公告)日：2003-01-23
申请号：PCT/EP2001/007948
申请日：2001-07-10
申请人： 4SC AG , KRAMER, Bernd , LEBAN, Johann
发明人： KRAMER, Bernd , LEBAN, Johann
IPC分类号： C07C233/60
CPC分类号： 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
摘要： 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.
摘要翻译：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

7. 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。

8. 发明申请

WO2007017284A3 INHIBITORS OF CANCER CELL, T-CELL AND KERATINOCYTE PROLIFERATION 审中-公开
标题翻译：癌细胞，T细胞和角质细胞增殖抑制剂
公开(公告)号：WO2007017284A3
公开(公告)日：2007-07-26
申请号：PCT/EP2006007933
申请日：2006-08-10
申请人： 4SC AG , LEBAN JOHANN , KRALIK MARTIN
发明人： LEBAN JOHANN , KRALIK MARTIN
IPC分类号： C07K5/04 , A61K38/04 , C07D233/00 , C07K5/06 , C07K5/08 , C07K5/10
CPC分类号： C07D403/12 , A61K38/00 , C07D401/12 , C07D401/14 , C07D495/04 , C07K5/06078 , C07K5/06156 , C07K5/06191
摘要： The invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Y is -NR a R b , -NR c C=ONR a R b' -NR c C=SNR a R b , -NR c C=NR d N a R b , heterocycle, - C=ONR a R b , heterocycle, or aryl; n is O to 8; m is 0, or 1 ; r is 0 to 3; t is O to 3; X is O or N; Z is CH 2 , C=O, C=S or a single bond; Z 1 is CO-R 2 , CS-R 2 , (CH 2 ) t -R 2 or the side-chain of a naturally occuring amino acid; , Z 2 is CO-R 2 , CS-R 2 or (CH 2 ) t -R 3 or the side-chain of a naturally occuring amino acid; Z 3 is CO-R 2 , CS-R 2 or (CH 2 ) t -R 4 or the side-chain of a naturally occuring amino acid; Z 4 is H, alkyl, alkoxy, or cycloalkyl; R 1 , R 2 , R 3 , and R 4 are independently from each other H, OH, SH, NH 2 , CN, NO 2 , alkyl, cycloalkyl, heterocycloalkyl, haloalkyl, alkylthio, haloalkyloxy, hydroxyalkyl, hydroxyalkylarnino, 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'R'R'B''， / SUP> C = ONR R ^{b' -NR C C = SNR R ^{b -NR c C = NR d R a N b R c，杂环，-C = C 1 -C 4烷基，芳基，杂芳基或芳基; R 1，R 2，R 3，R 4， n是0至8; m是0或1; r是0至3; t是0到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，SUB），T 2， / 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 SUB）t R 3或天然存在的氨基酸的侧链; Z 3是CO-R 2，CS-R 2或者（CH 2，SUB 2）t，或者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，R 4和R 4相互独立地为H，OH，SH 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，羟基烷基氨基，烷基氨基，烷基芳基，烷基亚磺酰基，烷基磺酰基，烷基硫代烷基，，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。}}

9. 发明申请

WO2007016979A2 NOVEL HETEROCYCLIC NF-κB INHIBITORS 审中-公开
标题翻译：新型杂环NF-κB抑制剂
公开(公告)号：WO2007016979A2
公开(公告)日：2007-02-15
申请号：PCT/EP2006/002396
申请日：2006-03-15
申请人： 4SC AG , LEBAN, Johann , SCHMITT, Harald , WOLF, Kristina , PEGORARO, Stefano , WUZIK, Andreas
发明人： LEBAN, Johann , SCHMITT, Harald , WOLF, Kristina , PEGORARO, Stefano , WUZIK, Andreas
IPC分类号： C07D417/14 , C07D417/12 , C07D417/06 , C07D413/12 , C07D413/14 , C07D413/06 , C07D277/56 , C07D263/48 , C07D491/04 , A61K31/427 , A61P35/00
CPC分类号： C07D487/04 , C07D263/48 , C07D277/56 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D491/04
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, Formula (III) wherein R 3 is H, -C(O)NR a R b , halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR 4’ OR 5’ , NH 2 , amine, alkylamine, alkoxy, cycloalkyl, heterocyclo-alkyl,hydroxyalkyl, or haloalkyloxy; R 4 is H, halogen, alkyl, -C(NR 7 )NR 7’ R 8 , -(CH 2 ) p aryl, -(CH 2 ) P NR 7 R 8 , -C(O)NR 7 R 8 , -N=CR 7 R 8 , -NR 7 C(O)R 8 , cycloalkyl, heterocycloalkyl, haloalkyl, hydroxyalkyl, hydroxyalkylamino, alkylamino, heteroaryl, or aryl; R 5 is halogen, alkyl, -C(NR 7 )NR 7’ R 8 , -(CH 2 ) p aryl, -(CH 2 ) P NR 7 R 8 , -C(O)NR 7 R 8 , -N=CR 7 R 8 , -NR 7 C(O)R 8 , 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，式（III）其中R 3为H ，-C（O）NR a R b，卤素，烷基，卤代烷基，芳基，杂芳基，OH，SH，NR 4'或 NH 2，NH 2，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）2芳基， - （CH 2 CH 2）n NR 7 R 8，-C（O）NR 7 R 8，-N = CR 7 R 10， 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; R 5是卤素，烷基，-C（NR 7）NR 7 R 8， - （CH 芳基， - （CH 2）2 NR 7 R 7， R 8，C（O）NR 7 R 8，-N = CR 7 R 8， C 1 -C 10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. 发明申请

WO1996022305A2 MODIFIED PEPTIDES 审中-公开
标题翻译：改性肽
公开(公告)号：WO1996022305A2
公开(公告)日：1996-07-25
申请号：PCT/GB1996000057
申请日：1996-01-12
申请人： THE WELLCOME FOUNDATION LIMITED , DANIELS, Alejandro, Jose , HEYER, Dennis , LEBAN, Johann, Jakob
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07K05/06
CPC分类号： C07K5/06095 , A61K38/00 , C07C279/14 , C07K5/06191
摘要： The present invention relates to compounds of formula (I), to the use of such compounds in medicine especially in the treatment or prophylaxis of conditions associated with eating disorders and to pharmaceutical compositions containing such compounds.
摘要翻译：本发明涉及式（I）化合物，其用于医药领域，特别是用于治疗或预防与进食障碍有关的病症以及含有这些化合物的药物组合物。

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