公开(公告)号：US09914956B2

公开(公告)日：2018-03-13

申请号：US14422310

申请日：2013-08-16

Applicant: Academia Sinica

Inventor： Chi-Huey Wong ,  Jim-Min Fang ,  Yih-Shyun E. Cheng ,  Charng-Sheng Tsai

IPC: C12Q1/70 ,  C12Q1/40 ,  C12N9/96 ,  C08B37/00 ,  C12Q1/34 ,  C12Q1/04 ,  C07H13/04 ,  C07H13/12 ,  C07H5/00 ,  C12N9/24

CPC classification number: C12Q1/40 ,  C07H5/00 ,  C07H13/04 ,  C07H13/12 ,  C12N9/2402 ,  C12Q1/04 ,  C12Q1/34 ,  C12Q1/70 ,  C12Y302/01018 ,  G01N2333/11

Abstract: Provided herein are novel irreversible sialidase inhibitors. These compounds can be conjugated with a detectable tagging moiety such as azide-annexed biotin via CuAAC for isolation and identification of sialidases. The provided compounds and the corresponding detectable conjugates are useful for detecting sialidase-containing pathogens and imaging in situ sialidase activities under physiological conditions.

公开(公告)号：US09759726B2

公开(公告)日：2017-09-12

申请号：US14698660

申请日：2015-04-28

Applicant: Academia Sinica

Inventor： Chi-Huey Wong ,  Jim-Min Fang ,  Jiun-Jie Shie

IPC: C07D309/14 ,  G01N33/58 ,  C07K7/08 ,  G01N21/64 ,  C07D311/02 ,  C07F5/02

CPC classification number: G01N33/582 ,  C07D309/14 ,  C07D311/02 ,  C07F5/027 ,  C07K7/08 ,  G01N21/64 ,  G01N2333/924 ,  G01N2458/30

Abstract: Provided are azido-BODIPY compounds of formula (I), cyclooctyne-based fluorogenic probes of formula (IV), and activity-based probes of formula (VI). These compounds undergo azide-alkyne cycloadditions (AAC) with to form triazolyl products. The provided compounds are useful for detection and imaging of alkyne-, or azide-containing molecules. Methods for detection and imaging biomolecules using compounds of the present disclosure are disclosed.

公开(公告)号：US20150148360A1

公开(公告)日：2015-05-28

申请号：US14416051

申请日：2013-07-19

Applicant: Academia Sinica ,  National Taiwan University

Inventor： Jung-Hsin Lin ,  Jim-Min Fang ,  Ting-Rong Chen ,  Jhih-Bin Chen ,  Ching-Chow Chen ,  Tzu-Tang Wei

IPC: C07D215/14 ,  C07D209/24 ,  C07D213/56 ,  C07D207/34 ,  C07D239/42 ,  A61K45/06 ,  A61K31/4045 ,  A61K31/47 ,  A61K31/44 ,  A61K31/401 ,  A61K31/505 ,  C07C259/06 ,  A61K31/221

CPC classification number: C07D215/14 ,  A61K31/221 ,  A61K31/401 ,  A61K31/4045 ,  A61K31/44 ,  A61K31/47 ,  A61K31/505 ,  A61K45/06 ,  C07B2200/07 ,  C07C259/06 ,  C07C259/08 ,  C07C2602/28 ,  C07D207/34 ,  C07D209/24 ,  C07D213/56 ,  C07D239/42

Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds and pharmaceutical compositions for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g., cancer, hypercholesterolemia, an acute or chronic inflammatory disease, autoimmune disease, allergic disease, pathogen infection, neurodegenerative disease, and a disease associated with oxidative stress), or inhibiting drug resistance of cancer cells.

Abstract translation: 本发明提供新的式（I）化合物及其药物组合物。 式（I）化合物是组蛋白脱乙酰酶（HDAC）和3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶（HMGR）的抑制剂。 还提供了使用化合物和药物组合物来抑制HDAC和HMGR的活性，治疗与HDAC或HMGR相关的疾病（例如癌症，高胆固醇血症，急性或慢性炎性疾病，自身免疫性疾病，过敏性疾病，病原体感染， 神经变性疾病和与氧化应激相关的疾病），或抑制癌细胞的耐药性。

公开(公告)号：US20150038445A1

公开(公告)日：2015-02-05

申请号：US14378013

申请日：2013-02-11

Applicant: Academia Sinica

Inventor： Chih-Cheng Chen ,  Yun-Lian Lin ,  Jim-Min Fang ,  Yijuang Chern ,  Chia-Ching John Lin ,  Wei-Nan Chen ,  Chun-Jung Lin

IPC: A61K31/7076 ,  A61K36/8988

CPC classification number: A61K31/7076 ,  A61K36/8988 ,  A61K45/06 ,  A61K2300/00

Abstract: The disclosure provides a new use of adenosine analogs for the treatment of pain through activation of neurokinin 1 (NK1) receptor signaling pathway, thereby inducing the activation of M-type potassium channel to induce outward currents. A method and pharmaceutical composition for treating pain comprising an adenonsine analog that activates NK1 receptor signaling, thereby inducing outward current are also provided.

Abstract translation: 本公开提供了腺苷类似物用于通过激活神经激肽1（NK1）受体信号传导途径治疗疼痛的新用途，从而诱导M型钾通道的活化以诱导外向电流。 还提供了一种用于治疗疼痛的方法和药物组合物，其包含激活NK1受体信号传导的腺苷类似物，从而诱导外向电流。

公开(公告)号：US10765681B2

公开(公告)日：2020-09-08

申请号：US16075202

申请日：2017-02-03

Applicant: Academia Sinica ,  National Taiwan University

Inventor： Chi-Huey Wong ,  Pan-Chyr Yang ,  Jim-Min Fang ,  Szu-Hua Pan ,  Ting-Jen R. Cheng ,  Ling-Wei Li

IPC: C07D473/00 ,  A61K31/522 ,  A61K45/06 ,  A61K31/337 ,  A61K31/52 ,  A61K31/506 ,  A61K31/502 ,  A61K31/167 ,  A61K31/454 ,  A61K38/05 ,  A61K31/517 ,  A61K31/4025 ,  A61K31/5377 ,  A61K31/69 ,  A61K31/44 ,  A61K35/00

Abstract: The present disclosure provides compounds of Formulas (I′) and (I), and pharmaceutically acceptable salts thereof. The compounds described herein may be useful in treating and/or preventing proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, and uses thereof for treating proliferative diseases.

公开(公告)号：US10342818B2

公开(公告)日：2019-07-09

申请号：US14849782

申请日：2015-09-10

Applicant: Academia Sinica

Inventor： Yun-Lian Lin ,  Yijuang Chern ,  Jim-Min Fang ,  Jung-Hsing Lin ,  Nai-Kuei Huang

IPC: A01N43/04 ,  A61K31/70 ,  A61K31/7076 ,  C07H19/167 ,  A61K31/706 ,  A61K31/7064

Abstract: The present invention provides therapeutic agents for preventing and treating neurodegenerative diseases. These agents synergistically target both the adenosine A2A receptor (A2AR) and the equilibrative nucleoside transporter 1 (ENT1).

公开(公告)号：US10117890B2

公开(公告)日：2018-11-06

申请号：US15376281

申请日：2016-12-12

Applicant: Academia Sinica

Inventor： Chih-Cheng Chen ,  Yun-Lian Lin ,  Jim-Min Fang ,  Yijuang Chern ,  Chia-Ching John Lin ,  Wei-Nan Chen ,  Chun-Jung Lin

IPC: A01N43/04 ,  A61K31/70 ,  A61K31/7076 ,  A61K36/8988 ,  A61K45/06

Abstract: Methods for treating pain such as fibromyalgia, comprising administering to a subject in need thereof an effective amount of an adenosine analog, wherein the adenosine analog may be a compound of Formula (I): (I), or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions comprising the adenosine analog for use in treating pain (e.g., fibromyalgia), optionally further comprising Substance P (SP), are also provided.

公开(公告)号：US09353061B2

公开(公告)日：2016-05-31

申请号：US14416051

申请日：2013-07-19

Applicant: Academia Sinica ,  National Taiwan University

Inventor： Jung-Hsin Lin ,  Jim-Min Fang ,  Ting-Rong Chern ,  Jhih-Bin Chen ,  Ching-Chow Chen ,  Tzu-Tang Wei

IPC: A61K31/221 ,  C07D215/14 ,  C07C259/08 ,  A61K31/401 ,  A61K31/4045 ,  A61K31/44 ,  A61K31/47 ,  A61K31/505 ,  A61K45/06 ,  C07C259/06 ,  C07D207/34 ,  C07D209/24 ,  C07D213/56 ,  C07D239/42

CPC classification number: C07D215/14 ,  A61K31/221 ,  A61K31/401 ,  A61K31/4045 ,  A61K31/44 ,  A61K31/47 ,  A61K31/505 ,  A61K45/06 ,  C07B2200/07 ,  C07C259/06 ,  C07C259/08 ,  C07C2602/28 ,  C07D207/34 ,  C07D209/24 ,  C07D213/56 ,  C07D239/42

Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds and pharmaceutical compositions for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g., cancer, hypercholesterolemia, an acute or chronic inflammatory disease, autoimmune disease, allergic disease, pathogen infection, neurodegenerative disease, and a disease associated with oxidative stress), or inhibiting drug resistance of cancer cells.

Abstract translation: 本发明提供新的式（I）化合物及其药物组合物。 式（I）化合物是组蛋白脱乙酰酶（HDAC）和3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶（HMGR）的抑制剂。 还提供了使用化合物和药物组合物来抑制HDAC和HMGR的活性，治疗与HDAC或HMGR相关的疾病（例如癌症，高胆固醇血症，急性或慢性炎性疾病，自身免疫性疾病，过敏性疾病，病原体感染， 神经变性疾病和与氧化应激相关的疾病），或抑制癌细胞的耐药性。

公开(公告)号：US09874562B2

公开(公告)日：2018-01-23

申请号：US15210565

申请日：2016-07-14

Applicant: Academia Sinica

Inventor： Chi-Huey Wong ,  Jim-Min Fang ,  Yih-Shyun Edmund Cheng ,  Jiun-Jie Shie

IPC: G01N33/569

CPC classification number: G01N33/56983 ,  A61K31/665 ,  A61K31/683 ,  C07F9/6552 ,  G01N2333/11

Abstract: Methods and compositions for detection of drug resistant pathogens and treatment against infections thereof are provided. Methods for detection of oseltamivir-resistant influenza viruses by competitive binding assays utilizing non-oseltamivir influenza virus neuraminidase inhibitors and oseltamivir carboxylate are provided. Influenza virus neuraminidase inhibitors coupled to sensors and useful for employment in the methods of the invention are disclosed. Novel phosphonate compounds active as neuraminidase inhibitors against wild-type and oseltamivir-resistant influenza strains of H1N1, H5N1 and H3N2 viruses are disclosed. An enantioselective synthetic route to preparation of these phosphonate compounds via sialic acid is provided.

公开(公告)号：US20170224716A1

公开(公告)日：2017-08-10

申请号：US15376281

申请日：2016-12-12

Applicant: Academia Sinica

Inventor： Chih-Cheng Chen ,  Yun-Lian Lin ,  Jim-Min Fang ,  Yijuang Chern ,  Chia-Ching John Lin ,  Wei-Nan Chen ,  Chun-Jung Lin

IPC: A61K31/7076 ,  A61K45/06 ,  A61K36/8988

CPC classification number: A61K31/7076 ,  A61K36/8988 ,  A61K45/06 ,  A61K2300/00

Abstract: The invention provides a new use of adenosine analogs for the treatment of pain through activation of neurokinin 1 (NK1) receptor signaling pathway, thereby inducing the activation of activation of M-type potassium channel to induce outward currents. A method and pharmaceutical composition for treating pain comprising an adenonsine analog that activates NK1 receptor signaling, thereby inducing outward current are also provided.