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1. 发明申请

WO2017222881A1 TREATMENT OF FABRY DISEASE 审中-公开
标题翻译：治疗FABRY疾病
公开(公告)号：WO2017222881A1
公开(公告)日：2017-12-28
申请号：PCT/US2017/037381
申请日：2017-06-14
申请人： ACADEMIA SINICA , SHIH, Ming-Che
发明人： CHENG, Wei-Chieh
IPC分类号： A61K31/7028 , C07D207/02
CPC分类号： C07D207/02 , A61K31/40 , A61K31/7028 , A61K38/47 , A61K45/06 , A61P3/00 , C07D207/12 , C12Y302/01022 , A61K2300/00
摘要： Disclosed herein are novel uses of a polyhydroxylated pyrrolidine for the manufacture of a medicament for treating Fabry disease (FD). Accordingly, the present disclosure provides a method of treating a subject having or suspected of having FD. The method includes the step of, administering to the subject a therapeutically effective amount of a compound of formula (I), a salt, an ester or a solvate thereof, wherein: R 1 is H, or C 1-3 amine optionally substituted with -COR 2 ; R 2 is alkyl or alkene optionally substituted with cycloalkyl or phenyl having at least one substituent selected from the group consisting of, halo, alkyl, haloalkyl, and alkoxyl; so as to ameliorate, alleviate mitigate and/or prevent symptoms associated with the FD. According to preferred embodiments of the present disclosure, the compound of formula (I) is a chaperon of a mutated human lysosomal α-galactosidase A (α-Gal A).
摘要翻译：本文公开了多羟基化吡咯烷用于制造用于治疗法布里病（FD）的药物的新用途。因此，本公开提供了治疗患有或怀疑患有FD的受试者的方法。该方法包括向受试者施用治疗有效量的式（I）化合物，其盐，酯或溶剂化物的步骤，其中：R 1是H或C 任选被-COR 2 2取代的胺; R 2是任选被环烷基或具有至少一个选自卤素，烷基，卤代烷基和烷氧基的取代基的苯基取代的烷基或烯基; 以改善，减轻缓解和/或预防与FD有关的症状。根据本公开的优选实施方案，式（I）的化合物是突变的人溶酶体α-半乳糖苷酶A（α-Gal A）的伴侣。

2. 发明申请

WO2022197564A1 POLYHYDROXYLATED INDOLIZIDINE AND PYRROLIZIDINE DERIVATIVES AND USES THEREOF 审中-公开
公开(公告)号：WO2022197564A1
公开(公告)日：2022-09-22
申请号：PCT/US2022/020074
申请日：2022-03-11
申请人： ACADEMIA SINICA , LIU, Fu-Tong
发明人： CHENG, Wei-Chieh , CHEN, Wei-An , CHEN, Yu-Hsin , CHENG, Ting-Jen , SHEN, Chia-Ning , HSIEH, Chiao-Yun , HUNG, Pi-Fang
IPC分类号： A61K31/395 , A61K31/40 , A61K31/407 , C07D403/02 , C07D487/00 , C07D487/04
摘要： Disclosed herein are novel polyhydroxylated indolizidine and pyrrolizidine derivates and methods for using the same in the treatment of cancer. The present poly hydroxylated indolizidine and pyrrolizidine derivates has the structure of formula (I), wherein: X is 0 or S; a, b and c are independently an integral of 0 or 1; and R is selected from the group consisting of H, C1-6 alkyl, alkenyl, alkynyl, and, heteroawl, cycloalkyl. cycloalkenyl, aralkyl, aralkenyl, aralkynyl, heteroaralkyl, heteroaralkenyl, heteroaralkynyl. heterocyclyl, alkoxy, aryloxy, and sulfonyl.

3. 发明申请

WO2021067324A1 METHODS OF TREATING POMPE DISEASE 审中-公开
公开(公告)号：WO2021067324A1
公开(公告)日：2021-04-08
申请号：PCT/US2020/053352
申请日：2020-09-30
申请人： ACADEMIA SINICA , SHIH, Ming-Che
发明人： CHENG, Wei-Chieh , LI, Huang-Yi , HWU, Wuh-Liang , CHIEN, Yin-Hsiu , LEE, Ni-Chung
IPC分类号： A61K31/435 , A61K31/445 , C07D207/12 , C07D211/40
摘要： Disclosed herein are novel uses of ADMDP stereoisomers or their derivatives for the manufacture of a medicament for treating Pompe disease. Accordingly, the present disclosure provides a method of treating Pompe disease in a subject. The method includes the step of, administering to the subject a therapeutically effective amount of a compound of formula (I), or a salt, an ester or a solvate thereof, wherein R1 and R2 are independently H or alkyl optionally substituted by -NH2 or -OH, so as to ameliorate, alleviate mitigate and/or prevent symptoms associated with the Pompe disease. According to certain embodiments of the present disclosure, the compound of formula (I) may serve a stabilizer of α-glucosidase via preventing its denaturalization of deactivation.

4. 发明申请

WO2010011304A2 CRYSTAL STRUCTURE OF BIFUNCTIONAL TRANSGLYCOSYLASE PBP1B FROM E.COLI AND INHIBITORS THEREOF 审中-公开
标题翻译：大肠杆菌双功能转酰基酶PBP1B及其抑制剂的晶体结构
公开(公告)号：WO2010011304A2
公开(公告)日：2010-01-28
申请号：PCT/US2009/004246
申请日：2009-07-21
申请人： ACADEMIA SINICA , WONG, Chi-Huey , MA, Che, Alex , CHENG, Ting-Jen, Rachel , CHENG, Wei-Chieh
发明人： WONG, Chi-Huey , MA, Che, Alex , CHENG, Ting-Jen, Rachel , CHENG, Wei-Chieh
IPC分类号： C12Q1/48 , C12Q1/00 , G01N33/50 , G01N33/53
CPC分类号： C07C235/64 , C07C235/84 , C07K2299/00 , C12Q1/18 , C12Q1/48 , G01N2333/91102 , G01N2500/00
摘要： The crystal structure at 2.16 A resolution of the full-length bacterial bifunctional transglycosylase penicillin-binding protein Ib (PBPIb) from Escherichia coli , in complex with its inhibitor moenomycin, is provided. The atomic coordinates of the complex as well as the moenomycin binding site are provided. Three dimensional structures of amino acid residues involved in moenomycin binding and transglycosylation activity are identified. Binding site for peptidoglycan synthesis inhibitors comprising inhibitor- binding site comprises amino acid residues from at least one of transglycosylase (TG), UvrB domain 2 homolog (UB2H) and transmembrane (TM) domains of PBPIb are identified at an atomic level of resolution. Methods for rational drug design based on the atomic coordinates are provided. Methods for screening for antibiotics based on anisotropic binding assay and transglycosylase inhibitor assays are provided. Novel antibiotics based on the screening assays of the invention are disclosed.
摘要翻译：来自大肠杆菌的与其抑制剂默诺霉素复合的全长细菌双功能转糖基酶青霉素结合蛋白Ib（PBPIb）的2.16解析度的晶体结构是提供。提供了复合物的原子坐标以及默诺霉素结合位点。鉴定了涉及默诺霉素结合和转糖基活性的氨基酸残基的三维结构。包含抑制剂结合位点的肽聚糖合成抑制剂的结合位点包含来自PBIPb的转糖基酶（TG），UvrB结构域2同系物（UB2H）和跨膜（TM）结构域中的至少一个的氨基酸残基，其以原子水平的分辨率鉴定。提供了基于原子坐标的合理药物设计方法。提供了基于各向异性结合测定法和转糖基酶抑制剂测定法筛选抗生素的方法。公开了基于本发明筛选测定的新型抗生素。

5. 发明公开

EP4037682A1 METHODS OF TREATING POMPE DISEASE 审中-实审
公开(公告)号：EP4037682A1
公开(公告)日：2022-08-10
申请号：EP20872000.3
申请日：2020-09-30
申请人： Academia Sinica
发明人： CHENG, Wei-Chieh , LI, Huang-Yi , HWU, Wuh-Liang , CHIEN, Yin-Hsiu , LEE, Ni-Chung
IPC分类号： A61K31/435 , A61K31/445 , C07D207/12 , C07D211/40

6. 发明公开

EP4308108A1 POLYHYDROXYLATED INDOLIZIDINE AND PYRROLIZIDINE DERIVATIVES AND USES THEREOF 审中-实审
公开(公告)号：EP4308108A1
公开(公告)日：2024-01-24
申请号：EP22771972.1
申请日：2022-03-11
申请人： Academia Sinica
发明人： CHENG, Wei-Chieh , CHEN, Wei-An , CHEN, Yu-Hsin , CHENG, Ting-Jen , SHEN, Chia-Ning , HSIEH, Chiao-Yun , HUNG, Pi-Fang
IPC分类号： A61K31/395 , A61K31/40 , A61K31/407 , C07D403/02 , C07D487/00 , C07D487/04

7. 发明公开

EP3471736A1 TREATMENT OF FABRY DISEASE 审中-公开
公开(公告)号：EP3471736A1
公开(公告)日：2019-04-24
申请号：EP17815947.1
申请日：2017-06-14
申请人： Academia Sinica
发明人： CHENG, Wei-Chieh
IPC分类号： A61K31/7028 , C07D207/02

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