- Targeting Acidic Mammalian chitinase Is Effective in Animal Model of Asthma
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This article highlights our work toward the identification of a potent, selective, and efficacious acidic mammalian chitinase (AMCase) inhibitor. Rational design, guided by X-ray analysis of several inhibitors bound to human chitotriosidase (hCHIT1), led
- Mazur, Marzena,Olczak, Jacek,Olejniczak, Sylwia,Koralewski, Robert,Czestkowski, Wojciech,Jedrzejczak, Anna,Golab, Jakub,Dzwonek, Karolina,Dymek, Barbara,Sklepkiewicz, Piotr L.,Zagozdzon, Agnieszka,Noonan, Tom,Mahboubi, Keyvan,Conway, Bruce,Sheeler, Ryan,Beckett, Paul,Hungerford, William M.,Podjarny, Alberto,Mitschler, Andre,Cousido-Siah, Alexandra,Fadel, Firas,Golebiowski, Adam
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p. 695 - 710
(2018/02/17)
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- SUBSTITUTED AMINO TRIAZOLES, AND METHODS USING SAME
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Disclosed are novel substituted amino triazoles of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of Formula (I) are inhibitors of Acidic mammalian chitinase (AMCase) and are useful, in a non-limiting example, for treating asthma. Also provided are pharmaceutical compositions containing at least one compound of the present invention, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and at least one pharmaceutically acceptable carrier, solvent, adjuvant or diluent, and methods of using such compounds and/or compositions to treat asthma and/or to monitor asthma treatment.
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Page/Page column 77; 78
(2015/07/07)
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- Design and synthesis of a novel series of histamine H3 receptor antagonists through a scaffold hopping strategy
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Lead compounds 5-fluoro-2-methyl-N-[2-methyl-4-(2-methyl-[1,3′]bipyrrolidinyl-1′-yl)-phenyl]-benzamide (1), tetrahydro-pyran-4-carboxylic acid [((2S,3′S)-2-methyl-[1,3′]bipyrrolidinyl-1′-yl)-phenyl]-amide (2), and 3,5-dimethyl-isoxazole-4-carboxylic acid
- Gao, Zhongli,Hurst, William J.,Hall, Daniel,Hartung, Ryan,Reynolds, William,Kang, Jiesheng,Nagorny, Raisa,Hendrix, James A.,George, Pascal G.
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p. 429 - 438
(2015/01/30)
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- SUBSTITUTED N-HETEROCYCLOALKYL BIPYRROLIDINYLPHENYL AMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
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The present invention discloses and claims a series of substituted N- heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I). (Formula (I)) Wherein R, R1, R2, R3, R4, X, m, n and p are as describ
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Page/Page column 31
(2011/12/02)
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