公开(公告)号：AU2013305827A1

公开(公告)日：2015-03-05

申请号：AU2013305827

申请日：2013-08-21

Applicant: SHIE JIUN-JIE ,  ACADEMIA SINICA ,  WONG CHI-HUEY ,  FANG JIM-MIN

Inventor： WONG CHI-HUEY ,  FANG JIM-MIN ,  SHIE JIUN-JIE

IPC: C07D311/06 ,  A61K31/37 ,  A61P29/00 ,  C07D491/04 ,  C07D493/04

Abstract: Provided are benzocyclooctyne compounds of formula (I). These compounds undergo strain-promoted azide-alkyne cyclo additions (SPAAC) without presence of toxic metal catalysts. The provided compounds are useful for diagnosis and imaging of azide-containing molecules. Methods for detection and imaging biomolecules using compounds of the present disclosure are disclosed.

公开(公告)号：CA2697837A1

公开(公告)日：2009-03-05

申请号：CA2697837

申请日：2008-08-29

Applicant: ACADEMIA SINICA

Inventor： WONG CHI-HUEY ,  FANG JIM-MIN ,  SHIE JIUN-JIE ,  CHENG YIH-SHYUN EDMOND ,  JAN JIA-TSRONG

IPC: A61K31/7076 ,  A61K9/16 ,  A61K31/70 ,  A61K31/7052 ,  C07C233/52 ,  C07C247/14 ,  C07H19/04

Abstract: Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and > 20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5- cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio- and stereoselective bromoamidation of a bromoarene cis- dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation.

公开(公告)号：EP2841066A4

公开(公告)日：2015-11-25

申请号：EP13775664

申请日：2013-04-12

Applicant: ACADEMIA SINICA ,  WONG CHI HEUY ,  FANG JIM-MIN ,  LIU KUNG-CHENG ,  JAN JIA-TSRONG ,  CHENG YIH SHYUN E ,  CHENG TING JEN R

Inventor： WONG CHI-HUEY ,  FANG JIM-MIN ,  LIU KUNG-CHENG ,  JAN JIA-TSRONG ,  CHENG YIH-SHYUN E ,  CHENG TING-JEN R

IPC: A61K31/35 ,  A61K31/36 ,  A61K47/48 ,  A61P29/00 ,  A61P31/16

CPC classification number: A61K47/481 ,  A61K47/55

Abstract: Novel dual-targeted, bifunctional anti-influenza drugs formed by conjugation with anti-inflammatory agents are disclosed. Exemplary drugs according to the invention include caffeic acid (CA)-bearing zanamivir (ZA) conjugates ZA-7-CA (1), ZA-7-CA-amide (7) and ZA-7-Nap (43) for simultaneous inhibition of influenza virus neuraminidase and suppression of proinflammatory cytokines. Synthetic methods for preparation of these enhanced anti-influenza conjugate drugs are provided. The synthetic bifunctional ZA conjugates act synergistically towards protection of mice lethally infected by H1N1 or H5N1 influenza viruses. The efficacy of ZA-7-CA, ZA-7-CA-amide and ZA-7-Nap conjugates is much greater than the combination therapy of ZA with anti-inflammatory agents.

公开(公告)号：EP2849566A4

公开(公告)日：2015-08-19

申请号：EP13746079

申请日：2013-02-11

Applicant: ACADEMIA SINICA

Inventor： CHEN CHIH-CHENG ,  LIN YUN-LIAN ,  FANG JIM-MIN ,  CHERN YIJUANG ,  LIN CHIA-CHING JOHN ,  CHEN WEI-NAN ,  LIN CHUN-JUNG

IPC: A01N43/04 ,  A61K31/70 ,  A61P25/04 ,  A61P29/02

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.

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向外的电流。 还提供了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：EP2190439A4

公开(公告)日：2013-02-20

申请号：EP08828468

申请日：2008-08-29

Applicant: ACADEMIA SINICA

Inventor： FANG JIM-MIN ,  SHIE JIUN-JIE ,  WONG CHI-HUEY ,  CHENG YIH-SHYUN EDMOND ,  JAN JIA-TSRONG

IPC: A61K31/7076 ,  A61K9/16 ,  A61K31/7052 ,  C07C233/52 ,  C07C247/14 ,  C07H19/04

CPC classification number: A61K31/70 ,  A61K31/7076

公开(公告)号：EP2885311A4

公开(公告)日：2016-04-13

申请号：EP13831440

申请日：2013-08-16

Applicant: ACADEMIA SINICA

Inventor： WONG CHI-HUEY ,  FANG JIM-MIN ,  CHENG YIH-SHYUN E ,  TSAI CHARNG-SHENG

IPC: C07H13/04 ,  C07H13/12 ,  C12N9/24 ,  C12Q1/04 ,  C12Q1/34 ,  C12Q1/40 ,  C12Q1/70

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.

Abstract translation: 本文提供了新的不可逆唾液酸酶抑制剂。 这些化合物可以通过CuAAC与可检测的标记部分如叠氮化物附着的生物素缀合，用于分离和鉴定唾液酸酶。 提供的化合物和相应的可检测的缀合物可用于检测含唾液酸酶的病原体并在生理条件下成像原位唾液酸酶活性。

公开(公告)号：EP2888238A4

公开(公告)日：2016-01-27

申请号：EP13830785

申请日：2013-08-21

Applicant: ACADEMIA SINICA

Inventor： WONG CHI-HUEY ,  FANG JIM-MIN ,  SHIE JIUN-JIE

IPC: C07D311/06 ,  A61K31/37 ,  A61P29/00 ,  C07D491/04 ,  C07D493/04

CPC classification number: G01N33/582 ,  A61K49/0032 ,  C07D311/78 ,  C07D311/94 ,  C07D405/06 ,  C07D405/14 ,  C07D413/06 ,  C07D491/04 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04

Abstract: Provided are benzocyclooctyne compounds of formula (I). These compounds undergo strain-promoted azide-alkyne cyclo additions (SPAAC) without presence of toxic metal catalysts. The provided compounds are useful for diagnosis and imaging of azide-containing molecules. Methods for detection and imaging biomolecules using compounds of the present disclosure are disclosed.

Abstract translation: 提供式（I）的苯并环辛烯化合物。 这些化合物经历应变促进的叠氮炔环加成（SPAAC），而不存在有毒金属催化剂。 所提供的化合物可用于含叠氮化物分子的诊断和成像。 公开了使用本公开的化合物检测和成像生物分子的方法。

公开(公告)号：EP2498774A4

公开(公告)日：2013-04-17

申请号：EP10859431

申请日：2010-11-12

Applicant: ACADEMIA SINICA

Inventor： LIN YUN-LIAN ,  CHERN YIJUANG ,  FANG JIM-MIN ,  LIN JUNG-HSING ,  HUANG NAI-KUEI

IPC: C07H19/167 ,  A61K31/426 ,  A61K31/56 ,  A61P11/06

CPC classification number: A61K31/7076 ,  C07H19/167

公开(公告)号：EP2874994A4

公开(公告)日：2016-04-27

申请号：EP13819542

申请日：2013-07-19

Applicant: ACADEMIA SINICA ,  UNIV NAT TAIWAN

Inventor： CHEN CHING-CHOW ,  CHEN JHIH-BIN ,  WEI TZU-TANG ,  LIN JUNG-HSIN ,  FANG JIM-MIN ,  CHERN TING-RONG

IPC: C07C235/26 ,  A61K31/44 ,  A61K31/47 ,  A61P35/00

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.