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1. 发明授权

US10793601B2 Therapeutic spalt-like transcription factor 4 (SALL4) peptide 有权
公开(公告)号：US10793601B2
公开(公告)日：2020-10-06
申请号：US16095603
申请日：2017-04-28
申请人： National University of Singapore , The Brigham and Women's Hospital, Inc. , Agency for Science, Technology and Research
发明人： Bee Hui Liu , Daniel Geoffrey Tenen , Li Chai , Cheng San Brian Chia , Anders Poulsen
IPC分类号： A61K38/00 , A61K38/08 , C07K7/06 , C07K7/08
摘要： Isolated peptides and pharmaceutical compositions comprising isolated peptides that bind to retinoblastoma binding protein 4 (RBBp4) and block the Spalt-Like Transcription Factor 4 (SALL4)-RBBp4 interaction are described. Methods of inhibiting binding of SALL4 to RBBp4 and methods of treating a subject having a disorder mediated by a dysregulation of SALL4 are also described.

2. 发明申请

US20190218253A1 Therapeutic SALL4 Peptide 审中-公开
公开(公告)号：US20190218253A1
公开(公告)日：2019-07-18
申请号：US16095603
申请日：2017-04-28
申请人： National University of Singapore , The Brigham and Women's Hospital, Inc. , Agency for Science, Technology and Research
发明人： Bee Hui Liu , Daniel Geoffrey Tenen , Li Chai , Cheng San Brian Chia , Anders Poulsen
IPC分类号： C07K7/06 , C07K7/08
摘要： The present invention provides, in certain embodiments, isolated peptides and pharmaceutical compositions comprising isolated peptides that bind to retinoblastoma binding protein 4 RBBp4 such that, the binding blocks the SALL4-RBBp4 interaction. Methods of inhibiting binding of SALL4 with RBBp4 and methods for treating a subject having a disorder mediated by a dysregulation of SALL4 are also provided.

3. 发明申请

US20190071416A1 COMPOUNDS FOR TREATMENT OF CANCER AND EPIGENETICS 审中-公开
公开(公告)号：US20190071416A1
公开(公告)日：2019-03-07
申请号：US15767129
申请日：2016-10-10
申请人： Agency For Science, Technology and Research
发明人： Klement Jihao Foo , Anders Poulsen , Thomas Hugo Keller , Si Si Liew , Cheng San Brian Chia , Jin Yan Melgious Ang , Chuhul Huang
IPC分类号： C07D401/06 , A61P35/00 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/08 , C07D405/14
摘要： Compounds For Inhibition Of Cancer and Epigenesis. The present invention relates to quinolines and 5,6,7,8-tetrahydroacridines of the formula (I) wherein Z1, Z2, X, R1 to R8 and Y are defined as described in the specification, or a pharmaceutically acceptable form or prodrug thereof, that are inhibitors of methyl transferases such as protein lysine methyltransferases and more particularly SMYD3. The present invention also relates to the methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of disorders/conditions/diseases involving, relating to or associated with enzymes having methyl transferase activities/functions and/or via unspecified/multi-targeted mechanisms.

4. 发明授权

US09981964B2 Maleimide derivatives as modulators of wnt pathway 有权
公开(公告)号：US09981964B2
公开(公告)日：2018-05-29
申请号：US15105312
申请日：2014-12-17
申请人： Agency for Science, Technology and Research
发明人： Jenefer Alam , Anders Poulsen , Soo Yei Ho , Wei Ling Wang , Athisayamani Jeyaraj Duraiswamy
IPC分类号： C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy); optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or -alkylaryl; R2 represents H; or alkyl; R3 represents H; or alkyl; U, V and W represent —(CH2)—; or U and V together represent —CH═CH— and W represents C═O; Y represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6 alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); and Z represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6 alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl).

5. 发明申请

US20160318926A1 MALEIMIDE DERIVATIVES AS MODULATORS OF WNT PATHWAY 有权
标题翻译：作为WNT PATHWAY的调节剂的马来酰亚胺衍生物
公开(公告)号：US20160318926A1
公开(公告)日：2016-11-03
申请号：US15105312
申请日：2014-12-17
申请人： AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
发明人： Jenefer Alam , Anders Poulsen , Soo Yei Ho , Wei Ling Wang , Athisayamani Jeyaraj Duraiswamy
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy); optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or -alkylaryl; R2 represents H; or alkyl; R3 represents H; or alkyl; U, V and W represent —(CH2)—; or U and V together represent —CH═CH— and W represents C═O; Y represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6 alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); and Z represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6 alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl).
摘要翻译：本发明涉及式（I）化合物，其用于疾病治疗的组合和用途，或其药学上可接受的盐，溶剂化物或多晶型物，包括所有互变异构体和立体异构体，其中R 1表示任选取代的烷基（其中任选的取代基包括一个或多个取代基，各自独立地选自C 1-6烷氧基）; 任选取代的碳环基（其中任选的取代基包括一个或多个取代基，各自独立地选自C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基，C 1-6卤代烷氧基和卤素）; 或 - 烷基芳基; R2表示H; 或烷基; R3表示H; 或烷基; U，V和W表示 - （CH 2） - ; 或U和V一起表示-CH = CH-，W表示C = O; Y表示芳基; 杂芳基; 任选取代的碳环基（其中任选的取代基包括一个或多个各自独立地选自C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基，C 1-6卤代烷氧基和卤素的取代基）。或任选取代的杂环基（其中任选的取代基包括一个或多个各自独立地选自C 1-6烷基，C 1-6烷氧基，-C（O）OC 1-6烷基，-C（O）C 1-6烷基和-C（O）NHCl -6-烷基）; Z表示芳基; 杂芳基; 任选取代的碳环基（其中任选的取代基包括一个或多个各自独立地选自C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基，C 1-6卤代烷氧基和卤素的取代基）。或任选取代的杂环基（其中任选的取代基包括一个或多个各自独立地选自C 1-6烷基，C 1-6烷氧基，-C（O）OC 1-6烷基，-C（O）C 1-6烷基和-C（O） NHC 1-6烷基）。

6. 发明授权

US11834430B2 Compounds useful as inhibitors of isoprenylcysteine carboxyl methyltransferase 有权
公开(公告)号：US11834430B2
公开(公告)日：2023-12-05
申请号：US16646693
申请日：2018-09-12
申请人： AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
发明人： Soo Yei Ho , Anders Poulsen , Sum Wai Eldwin Tan , Shi Hua Ang , Thomas Hugo Keller
IPC分类号： C07D401/04 , C07D231/12 , C07D233/12 , C07D249/08 , C07D401/12 , C07D401/14 , A61P35/00 , C07D233/06 , C07D233/60 , C07D261/08 , C07D277/24 , C07D403/12
CPC分类号： C07D401/04 , A61P35/00 , C07D231/12 , C07D233/06 , C07D233/60 , C07D249/08 , C07D261/08 , C07D277/24 , C07D401/12 , C07D401/14 , C07D403/12
摘要： The present invention relates to compounds of general Formula (I), and/or tautomers, enantiomers, solvates, hydrates, and pharmaceutically acceptable salts thereof. The present invention also relates to compounds of Formula (I) for use in therapy, methods of treating isoprenylcysteine carboxyl methyltransferase (ICMT) related disorders or uses of compounds of Formula (I) in the manufacture of a medicament for the treatment of ICMT-related disorders, wherein the disorder is cancer and/or progeria. The present invention further relates to processes for synthesizing compounds of Formula (I).

7. 发明申请

US20210130317A1 Compounds Useful as Inhibitors of Isoprenylcysteine Carboxyl Methyltransferase 有权
公开(公告)号：US20210130317A1
公开(公告)日：2021-05-06
申请号：US16646693
申请日：2018-09-12
申请人： AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
发明人： Soo Yei Ho , Anders Poulsen , Sum Wai Eldwin Tan , Shi Hua Ang , Thomas Hugo Keller
IPC分类号： C07D401/04 , C07D249/08 , C07D233/60 , C07D277/24 , C07D401/12 , C07D231/12 , C07D233/06 , C07D261/08 , C07D401/14 , C07D403/12 , A61P35/00
摘要： The present invention relates to compounds of general Formula (I), and/or tautomers, enantiomers, solvates, hydrates, and pharmaceutically acceptable salts thereof. The present invention also relates to compounds of Formula (I) for use in therapy, methods of treating isoprenylcysteine carboxyl methyltransferase (ICMT) related disorders or uses of compounds of Formula (I) in the manufacture of a medicament for the treatment of ICMT-related disorders, wherein the disorder is cancer and/or progeria. The present invention further relates to processes for synthesizing compounds of Formula (I).

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