775330-11-5Relevant articles and documents
DEUTERATED BENZOPYRAN COMPOUND AND APPLICATION THEREOF
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Paragraph 0078-0080, (2015/03/18)
features as shown in Formula (I), or pharmaceutically acceptable salts or stereoisomers thereof, or prodrug molecules thereof. With excellent anti-inflammatory and analgesic effects and the capability to inhibit growth of tumor cells, such compounds are novel COX-2 selective inhibitors. The compounds and pharmaceutically acceptable salts thereof disclosed by the present application can be applied in preparing anti-inflammatory and analgesic drugs and drugs for treating or preventing tumors.
BENZO-FUSED HETEROCYCLIC DERIVATIVES USEFUL AS AGONISTS OF GPR120
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, (2014/09/30)
The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
The novel benzopyran class of selective cyclooxygenase-2 inhibitors. Part III: The three microdose candidates
Wang, Jane L.,Aston, Karl,Limburg, David,Ludwig, Cindy,Hallinan, Ann E.,Koszyk, Francis,Hamper, Bruce,Brown, David,Graneto, Matthew,Talley, John,Maziasz, Timothy,Masferrer, Jaime,Carter, Jeffery
scheme or table, p. 7164 - 7168 (2011/01/03)
In this manuscript, we report the discovery of the substituted 2-trifluoromethyl-2H-benzopyran-3-carboxylic acids as a novel series of potent and selective cyclooxygenase-2 (COX-2) inhibitors. We provide the structure-activity relationships, optimization of design, testing criteria, and human half-life data. The challenge of a surprisingly long half-life (t 1/2 = 360 h) of the first clinical candidate 1 and human t 1/2 had been difficult to predict based on allometric scaling for this class of highly ppb compounds. We used a microdose strategy which led to the discovery of clinical agents 18c-(S), 29b-(S), and 34b-(S) with human half-life of 57, 13, and 11 h.
