Santen Pharmaceutical Co., Ltd.

Yumi Hagiwara

Toshiyuki Mori

Masatomo Kato

Mamoru Matsuda

Miwa Takai

Takahiro Matsuyama

Tatsuji Kurose

Kenji Oki

Atsuyoshi Dota

Kenji Imoto

The object aims to find a novel pharmacological activity of a novel 1,2,3,4-tetrahydroquinoxaline derivative which contains, as a substituent, a phenyl group having a sulfonic acid ester structure introduced therein. A compound represented by general formula (1) or a salt thereof is useful as a glucocorticoid receptor agonist, particularly as a therapeutic agent for diseases against which a glucocorticoid receptor agonist (e.g., a steroid) is believed to be effective, such as inflammatory bone/joint diseases, inflammatory ophthalmic diseases (inflammatory ophthalmic diseases in the anterior or posterior segment of an eye). Rrepresents a group represented by general formula (2a), (3a), (4a) or (5a); Rrepresents a lower alkyl group which may have a substituent, a lower cycloalkyl group which may have a substituent, or the like; Rrepresents a lower alkyl group; R, R, Ror Rrepresent a halogen atom, a lower alkyl group which may have a substituent, a hydroxy group, a lower alkoxy group which may have a substituent, or the like; and m, n, p or q represents a number of 0, 1 or 2. 

Method for treating an inflammatory disease by administering a 1,2,3,4- tetrahydroquinoxaline compound containing a phenyl group having a sulfonic acid ester structure introduced therein as a substituent

The present invention is related to glucocorticoid receptor agonists comprised of a compound represented by formula (1) which is 2,2,4-trimethyl-6-phenyl-1,2-dihydroquinoline derivative or a salt thereof and novel pharmacological effects of the glucocorticoid receptor agonists. In the formula (1), Rrepresents formula (2a), (3a), (4a) or (5a); R2 represents &#x2014;(CO)&#x2014;R8, &#x2014;(CO)O&#x2014;R9, or the like; R&#x2014;O&#x2014; is substituted at the 4- or -5-position of benzene ring A; Rrepresents a lower alkyl group; R, R, Ror Rrepresents a halogen atom, a lower alkyl group which may have a substituent, or the like; m, n, p or q represents 0, 1 or the like; R, Ror the like represents a lower alkyl group which may have a substituent, a lower alkenyl group, or the like. 

Glucocorticoid receptor agonist comprising 2,2,4-trimethyl-6-phenyl-1,2-dihydroquinoline derivatives having substituted oxy group

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Ikoma, Japan

Yumi Hagiwara