- NOVEL COMPOUNDS HAVING EFFECTS OF TREATING INFLAMMATORY DISEASE AS P38 MAP KINASE INHIBITOR
-
The present invention relates to novel compounds exhibiting anti-inflammatory activity. The compound of the present invention plays a critical role in the production of inflammatory prodrug (pro-inflammatory cytokines) and has an excellent inhibitory effe
- -
-
Paragraph 0053
(2021/10/27)
-
- Fine Tuning of MOF-505 Analogues To Reduce Low-Pressure Methane Uptake and Enhance Methane Working Capacity
-
We present a crystal engineering strategy to fine tune the pore chemistry and CH4-storage performance of a family of isomorphic MOFs based upon PCN-14. These MOFs exhibit similar pore size, pore surface, and surface area (around 3000 m2 g?1) and were prepared with the goal to enhance CH4 working capacity. [Cu2(L2)(H2O)2]n (NJU-Bai 41: NJU-Bai for Nanjing University Bai's group), [Cu2(L3)(H2O)2]n (NJU-Bai 42), and [Cu2(L4)(DMF)2]n (NJU-Bai 43) were prepared and we observed that the CH4 volumetric working capacity and volumetric uptake values are influenced by subtle changes in structure and chemistry. In particular, the CH4 working capacity of NJU-Bai 43 reaches 198 cm3 (STP: 273.15 K, 1 atm) cm?3 at 298 K and 65 bar, which is amongst the highest reported for MOFs under these conditions and is much higher than the corresponding value for PCN-14 (157 cm3 (STP) cm?3).
- Zhang, Mingxing,Zhou, Wei,Pham, Tony,Forrest, Katherine A.,Liu, Wenlong,He, Yabing,Wu, Hui,Yildirim, Taner,Chen, Banglin,Space, Brian,Pan, Yi,Zaworotko, Michael J.,Bai, Junfeng
-
supporting information
p. 11426 - 11430
(2017/09/11)
-
- SUBSTITUTED PYRIMIDINES
-
Disclosed are substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
- -
-
Page/Page column 45
(2013/04/10)
-
- Discovery of biphenylketones as dual modulators of inflammation and bone loss
-
Biphenylketones were identified as novel inhibitors of NFκB activation. Structure-activity studies led to the identification of compound 4c, which had good potency against osteoclasts (IC50 = 0.8 μM), showed oral activity, and was able to compl
- Greig, Iain R.,Coste, Emmanuel,Ralston, Stuart H.,Van'T Hof, Rob J.
-
scheme or table
p. 5548 - 5551
(2010/12/29)
-
- Structure-activity relationships comparing N-(6-methylpyridin-yl)- substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists
-
The metabotropic glutamate receptor subtype 5 (mGluR5) has been implicated in anxiety, depression, pain, mental retardation, and addiction. The potent and selective noncompetitive mGluR5 antagonist 2-methyl-6-(phenylethynyl)pyridine (MPEP, 1) has been a critically important tool used to further elucidate the role of mGluR5 in these CNS disorders. In an effort to provide novel and structurally diverse selective mGluR5 antagonists, we previously described a set of analogues with moderate activity wherein the alkyne bond was replaced with an amide group. In the present report, extended series of both amide and alkyne-based ligands were synthesized. MGluR5 binding and functional data were obtained that identified (1) several novel alkynes with comparable affinities to 1 at mGluR5 (e.g., 10 and 20-23), but (2) most structural variations to the amide template were not well tolerated, although a few potent amides were discovered (e.g., 55 and 56). Several of these novel analogues show drug-like physical properties (e.g., cLogP range = 2-5) that support their use for in vivo investigation into the role of mGluR5 in CNS disorders.
- Kulkarni, Santosh S.,Zou, Mu-Fa,Cao, Jianjing,Deschamps, Jeffrey R.,Rodriguez, Alice L.,Conn, P. Jeffrey,Newman, Amy Hauck
-
experimental part
p. 3563 - 3575
(2010/04/05)
-