| 2024-01-23 |
Decrypting orphan GPCR drug discovery via multitask learning |
Journal of Cheminformatics. 2024 Jan 23;16:Article number 10. |
 |
| 2023-07-20 |
Natural fucoidans inhibit coronaviruses by targeting viral spike protein and host cell furin |
Biochemical Pharmacology. 2023 Jul 20;215:Article number 115688. |
|
| 2023-01 |
Modulating the affinity and signaling bias of cannabinoid receptor 1 antagonists |
Bioorganic Chemistry. 2023 Jan;130:Article number 106236. |
|
| 2022-02-05 |
Discovery and development of a novel N-(3-bromophenyl)-{[(phenylcarbamoyl)amino]methyl}-N-hydroxythiophene-2-carboximidamide indoleamine 2,3-dioxygenase inhibitor using knowledge-based drug design |
European Journal of Medicinal Chemistry. 2022 Feb 5;229:Article number 114043. |
|
| 2020-02-10 |
Unique sulfur-aromatic interactions contribute to the binding of potent imidazothiazole indoleamine 2,3-Dioxygenase inhibitors |
Journal of Medicinal Chemistry. 2020 Feb 10;63(4):1642-1659. |
|
| 2019-10 |
In vivo efficacy of cannabinoid receptor 1 antagonist, CPD1, in treating non-alcoholic fatty liver disease |
Hepatology. 2019 Oct;70:1333A. |
|
| 2019-08 |
A structure-function approach identifies L-PGDS as a mediator responsible for glucocorticoid-induced leptin expression in adipocytes |
Biochemical Pharmacology. 2019 Aug;166:203-211. |
|
| 2019-01-01 |
Fluorine-18 isotope labeling for positron emission tomography imaging. Direct evidence for DBPR211 as a peripherally restricted CB1 inverse agonist |
Bioorganic and Medicinal Chemistry. 2019 Jan 1;27(1):216-223. |
|
| 2018-10-06 |
Median nerve stimulation induces analgesia via orexin-initiated endocannabinoid disinhibition in the periaqueductal gray |
Proceedings of the National Academy of Sciences of the United States of America. 2018 Nov;115(45):E10720-E10729. |
|
| 2018-08-21 |
DUSP6 mediates T cell receptor-engaged glycolysis and restrains TFH cell differentiation |
Proceedings of the National Academy of Sciences of the United States of America. 2018 Aug 21;115(34):E8027-E8036. |
|
| 2018-07 |
4-Bromophenylhydrazinyl benzenesulfonylphenylureas inhibit indoleamine 2,3-dioxygenase in vitro and in vivo |
Cancer Research. 2018 Jul;78(13, Suppl.):Meeting Abstract 1664. |
|
| 2018-04 |
4-Bromophenylhydrazinyl benzenesulfonylphenylureas as indoleamine 2,3-dioxygenase inhibitors with in vivo target inhibition and anti-tumor efficacy |
Bioorganic Chemistry. 2018 Apr;77:600-607. |
|
| 2017-11 |
Caveolin-1 secreted from adipose tissues and adipocytes functions as an adipogenesis enhancer |
Obesity. 2017 Nov;25(11):1932-1940. |
|
| 2016-12 |
Phenyl benzenesulfonylhydrazides: Selective indoleamine 2,3-dioxygenase inhibitors with potent in vivo pharmacodynamic activity and antitumor efficacy |
European Journal of Cancer. 2016 Dec;68(Suppl. 1):S83-S84. |
|
| 2016-07-22 |
Orexins contribute to restraint stress-induced cocaine relapse by endocannabinoid-mediated disinhibition of dopaminergic neurons |
Nature Communications. 2016 Jul 22;7:Article number 12199. |
|
| 2016-01 |
Important hydrogen bond networks in Indoleamine 2,3-Dioxygenase 1 (IDO1) inhibitor design revealed by crystal structures of imidazoleisoindole derivatives with IDO1 |
Journal of Medicinal Chemistry. 2016 Jan;59 (1):282-293. |
|
| 2016-01 |
Phenyl benzenesulfonylhydrazides exhibit selective Indoleamine 2,3-Dioxygenase inhibition with potent in vivo pharmacodynamic activity and antitumor efficacy |
Journal of Medicinal Chemistry. 2016 Jan;59(1):419-430. |
|
| 2015-10 |
Identification of substituted naphthotriazolediones as novel tryptophan 2,3-dioxygenase (TDO) inhibitors through structure-based virtual screening |
Journal of Medicinal Chemistry. 2015 Oct;58 (19):7807-7819. |
|
| 2015-05 |
A novel peripheral cannabinoid receptor 1 antagonist, BPR0912, reduces weight independently of food intake and modulates thermogenesis |
Diabetes, Obesity and Metabolism. 2015 May;17(5):495-504. |
|
| 2014-08 |
Discovery and structure-activity relationships of phenyl benzenesulfonylhydrazides as novel indoleamine 2,3-dioxygenase inhibitors |
Bioorganic and Medicinal Chemistry Letters. 2014 Aug;24(15):3403-3406. |
|
| 2014-08 |
A novel mechanism for acupuncture-induced analgesia: involvement of orexins and endocannabinoids |
Journal of Neurochemistry. 2014 Aug;130(Suppl. s1):38. |
|
| 2013-11-13 |
Discovery of 1-(2,4-Dichlorophenyl)-N-(piperidin-1-yl)-4-((pyrrolidine-1-sulfonamido)methyl)-5 -(5-((4-(trifluoromethyl)phenyl)ethynyl)thiophene-2-yl)-1H-pyrazole-3-carboxamide as a novel peripherally restricted cannabinoid-1 receptor antagonist with significant weight-loss efficacy in diet-induced obese mice |
Journal of Medicinal Chemistry. 2013 Nov 13;56(24):9920-9933. |
|
| 2013-09-11 |
噻吩化合物及其醫藥組成物 |
I408136/2013-09-11 |
|
| 2013-05 |
Mesenchymal stem cells tune the development of monocyte-derived dendritic cells toward a myeloid-derived suppressive phenotype through growth-regulated oncogene chemokines |
Journal of Immunology. 2013 May;190(10):5065-5077. |
|
| 2013-03-27 |
Thiophene compounds |
EP2068870/2013-03-27 |
|
| 2012-07-04 |
噻吩化合物 |
ZL200780036897.1/2012-07-04 |
|
| 2012-07 |
Induction of fatty acid oxidation resists weight gain, ameliorates hepatic steatosis and reduces cardiometabolic risk factors |
International Journal of Obesity. 2012 Jul;36(7):999-1006. |
|
| 2011-10-01 |
硒吩化合物及其醫藥組成物 |
I349668/2011-10-01 |
|
| 2011-06 |
A new perspective of cannabinoid 1 receptor antagonists: Approaches toward peripheral CB1R blockers without crossing the blood-brain barrier |
Current Topics In Medicinal Chemistry. 2011 Jun;11(12):1421-1429. |
|
| 2011-03-21 |
吡唑化合物及其醫藥組成物 |
I339205/2011-03-21 |
|
| 2011-01-13 |
Discovery of novel N -Beta- d -Xylosylindole derivatives as sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the management of hyperglycemia in diabetes |
Journal of Medicinal Chemistry. 2011 Jan 13;54(1):166-178. |
|
| 2010-11-16 |
Thiophene compounds |
US7834046B2/2010-11-16 |
|
| 2010-10 |
Biphasic suppression of appetite by cannabinoid CB1 receptor antagonists with distinct functional activities |
Pharmacological Research. 2010 Oct;62(4):337-343. |
|
| 2010-09-28 |
Selenophene compounds |
US7803799B2/2010-09-28 |
|
| 2010-09 |
Discovery of 1-(2,4-Dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophe n-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist |
ChemMedChem. 2010 Sep;5(9):1439-1443. |
|
| 2009-07-23 |
Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H-pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobesity efficacy in DIO mice |
Journal of Medicinal Chemistry. 2009 Jul 23;52(14):4496-4510. |
|
| 2009-02-01 |
1,2,3-Triazole derivatives as new cannabinoid CB1 receptor antagonists |
Bioorganic and Medicinal Chemistry Letters. 2009 Feb 1;19(3):1022-1025. |
|
| 2008-09-21 |
Bioisosteric replacement of the pyrazole 3-carboxamide moiety of rimonabant. A novel series of oxadiazoles as CB1 cannabinoid receptor antagonists |
Organic and Biomolecular Chemistry. 2008 Sep 21;6(18):3399-3407. |
|
| 2008-09-11 |
Bioisosteric replacement of the pyrazole 5-aryl moiety of N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A). A novel series of alkynylthiophenes as potent and selective cannabinoid-1 receptor antagonists |
Journal of Medicinal Chemistry. 2008 Sep 11;51(17):5397-5412. |
|
| 2008-02-07 |
Design, synthesis, and biological evaluation of novel alkenylthiophenes as potent and selective CB1 cannabinoid receptor antagonists |
Organic and Biomolecular Chemistry. 2008 Feb;6(3):447-450. |
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