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41. 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。}}

42. 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。

43. 发明申请

WO2006066795A1 2,5- AND 2,6-DISUBSTITUTED BENZAZOLE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：用作蛋白激酶抑制剂的2,5-和2,6-取代苯扎唑衍生物
公开(公告)号：WO2006066795A1
公开(公告)日：2006-06-29
申请号：PCT/EP2005/013503
申请日：2005-12-15
申请人： 4SC AG , HERZ, Thomas , KRAUSS, Rolf , KUBBUTAT, Michael , LANG, Martin , SCHÄCHTELE, Christoph , TASLER, Stefan , TOTZKE, Frank
发明人： HERZ, Thomas , KRAUSS, Rolf , KUBBUTAT, Michael , LANG, Martin , SCHÄCHTELE, Christoph , TASLER, Stefan , TOTZKE, Frank
IPC分类号： C07D417/12 , C07D473/34 , A61K31/505 , A61K31/52 , A61P35/00
CPC分类号： C07D473/34 , C07D417/12
摘要： The present invention relates to N 2 -heteroaryl-benzazole-2,(5 or 6)-diamine derivatives and compositions thereof as protein kinase inhibitors for the treatment of e.g. cancer. (I)
摘要翻译：本发明涉及作为蛋白激酶抑制剂的N 2 - 杂芳基 - 苯并噻唑-2（5或6） - 二胺衍生物及其组合物。癌症。（一世）

44. 发明申请

WO2004056797A1 AROMATIC COMPOUNDS AS ANTI-INFLAMMATORY, IMMUNOMODULATORY AND ANTI-PROLIFERATORY AGENTS 审中-公开
标题翻译：芳香化合物作为抗炎剂，免疫调节剂和抗增生剂
公开(公告)号：WO2004056797A1
公开(公告)日：2004-07-08
申请号：PCT/EP2003/014433
申请日：2003-12-17
申请人： 4SC AG
发明人： LEBAN, Johann , TASLER, Stefan
IPC分类号： C07D333/38
CPC分类号： C07D221/04 , C07D237/26 , C07D239/70 , C07D307/68 , C07D333/38 , C07D491/04 , C07D495/04
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。

45. 发明申请

WO2004056746A1 CYCLOALKENE DICARBOXYLIC ACID COMPOUNDS AS ANTI-INFLAMMATORY, IMMUNOMODULATORY AND ANTI-PROLIFERATORY AGENTS 审中-公开
标题翻译：环丙基二羧酸化合物作为抗炎，免疫调节剂和抗增生剂
公开(公告)号：WO2004056746A1
公开(公告)日：2004-07-08
申请号：PCT/EP2003/014434
申请日：2003-12-17
申请人： 4SC AG
发明人： LEBAN, Johann , KRALIK, Martin
IPC分类号： C07C233/57
CPC分类号： C07D221/04 , C07C233/58 , C07C233/60 , C07C235/40 , C07C259/08 , C07C2601/10 , C07D237/26 , C07D239/70 , C07D307/68 , C07D333/38 , C07D491/04 , C07D495/04
摘要： The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, 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 replaced by a group X, wherein X is selected from the group consisting of S, O, N, NR 4 , SO, CO or SO 2 ; D is O, S, SO 2 , NR 4 or CH 2 ; Z 1 and Z 2 are independent from each other O, S, or NR 5 ; R 2 is H, OR 6 , or NHR 7 ; E is an alkyl or cycloalkyl group or 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, haloalkyl, haloalkyloxy, alkyl, cycloalkyl, a monocyclic or polycyclic substituted or unsubstituted ring system for the use as a medicament.
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A是含有4至8个碳原子的非芳族环系统，其中环系包含至少一个双键，其中一个或更多的碳原子可以被X基团取代，其中X选自S，O，N，NR 4，SO，CO或SO 2; D是O，S，SO 2，NR 4或CH 2; Z 1和Z 2彼此独立地为O，S或NR 5; R 2是H，OR 6或NHR 7; E是烷基或环烷基或单环或多环取代或未取代的环系，其可以含有一个或多个基团X并且含有至少一个芳环; Y是氢，卤素，卤代烷基，卤代烷氧基，烷基，环烷基，单环或多环取代或未取代的环系统，用作药物。

46. 发明申请

WO2021064188A1 COMBINATION COMPRISING HDAC INHIBITOR, CTLA-4 INHIBITOR AND A PD-1 INHIBITOR OR PD-L1 INHIBITOR FOR CANCER TREATMENT 审中-公开
公开(公告)号：WO2021064188A1
公开(公告)日：2021-04-08
申请号：PCT/EP2020/077686
申请日：2020-10-02
申请人： 4SC AG
发明人： HAMM, Svetlana , HERMANN, Frank
IPC分类号： A61P35/00 , A61K31/497 , A61K39/00 , A61K45/06
摘要： The invention relates to medical uses of an HDAC inhibitor of the below general formula I, wherein R1 to R7 are as described herein, or a salt or solvate thereof in combination with CTLA-4 inhibitor and a PD-1 inhibitor or PD-L1 inhibitor for the treatment of cancer. (Formula)

47. 发明申请

WO2019200238A1 COMBINATIONS INCLUDING A CPG-C TYPE OLIGONUCLEOTIDE AND A HISTONE DEACETYLASE INHIBITOR FOR TREATING CANCER 审中-公开
公开(公告)号：WO2019200238A1
公开(公告)日：2019-10-17
申请号：PCT/US2019/027187
申请日：2019-04-12
申请人： DYNAVAX TECHNOLOGIES CORPORATION , 4SC AG
发明人： GUIDUCCI, Cristiana , COFFMAN, Robert L , DEGAGNE, Emilie , HAMM, Svetlana , HERMANN, Frank , BARTZ, René
IPC分类号： A61K31/7115 , A61K31/4155 , A61P35/00
摘要： The present disclosure describes combination therapies comprising a histone deacetylase inhibitor and a toll-like receptor 9 agonist. In particular, the present disclosure describes combinations of an inhibitor of a zinc-dependent histone deacetylase and a CpG-C type oligonucleotide for the treatment of cancer.

48. 发明申请

WO2019197682A1 PHARMACEUTICAL COMBINATION PRODUCTS COMPRISING A HISTONE DEACETYLASE (HDAC) INHIBITOR AND A TLR7 AGONIST AND/OR TLR8 AGONIST FOR THE TREATMENT OF CANCER 审中-公开
公开(公告)号：WO2019197682A1
公开(公告)日：2019-10-17
申请号：PCT/EP2019/059651
申请日：2019-04-15
申请人： 4SC AG
发明人： HAMM, Svetlana
IPC分类号： C07D403/12 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/4155 , A61K31/4439 , A61K31/5377 , C07D231/12 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/14 , C07D207/48 , A61P35/00 , A61P37/00
摘要： The invention relates to pharmaceutical combination products comprising an HDAC inhibitor, e.g. (E)-N-(2-amino-phenyl)-3-{1-[4-(1-methyl-1H-pyrazol-4-yl)-benzenesulfonyl]-1H-pyrrol-3-yl}- acrylamide as well as salts and or solvents thereof and TLR7 agonist and/or TLR8 agonist for the treatment of cancer. The present invention also relates to methods of treatment of patients suffering from cancer with these pharmaceutical combination products.

49. 发明申请

WO2017060524A1 (E)-N-(2-AMINOPHENYL)-3-(1-((4-(1-METHYL-1H-PYRAZOL-4-YL)PHENYL)SULFONYL)-1H-PYRROL-3-YL)ACRYLAMIDE FOR THE TREATMENT OF LATENT VIRAL INFECTIONS 审中-公开
标题翻译：（E）-N-（2-氨基苯基）-3-（1 - （（4-（1-甲基-1H-吡唑-4-基）苯基）磺酰基）-1H-吡咯-3-基）丙烯酰胺治疗病毒性感染
公开(公告)号：WO2017060524A1
公开(公告)日：2017-04-13
申请号：PCT/EP2016/074197
申请日：2016-10-10
申请人： 4SC AG
发明人： KOHLHOF, Hella , GRÖPPEL, Manfred , VITT, Daniel
IPC分类号： A61K31/4155 , A61K45/06 , A61P31/12 , A61P31/18 , A61P31/22
CPC分类号： A61K31/4155 , A61K45/06 , Y02A50/467
摘要： The present invention relates to the medical application of (E)-N-(2-arninophenyl)-3-(1-((4- (1-methyl-1H-pyrazoi-4-yl)phenyl)suifonyl)-1H-pyrrol-3-yl)acrylamide or a salt, prodrug or solvate thereof in the treatment of latent viral infections, such as latent viral infections with HIV.
摘要翻译：本发明涉及（E）-N-（2-氨基苯基）-3-（1 - （（4-（1-甲基-1H-吡唑-4-基）苯基）磺酰基）-1H- 吡咯-3-基）丙烯酰胺或其盐，前药或溶剂合物在治疗潜伏性病毒感染，例如HIV的潜伏性病毒感染。

50. 发明申请

WO2010128050A2 ANTI-INFLAMMATORY AGENTS AS VIROSTATIC COMPOUNDS 审中-公开
标题翻译：抗炎药物作为维生素A化合物
公开(公告)号：WO2010128050A2
公开(公告)日：2010-11-11
申请号：PCT/EP2010/056042
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： A61K31/381
CPC分类号： A61K31/196 , A61K31/341 , A61K31/381 , A61K31/44 , C07D213/78 , C07D307/68 , C07D333/38 , Y02A50/385 , Y02A50/387 , Y02A50/393 , Y02A50/397 , Y02A50/467
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。

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