Santen Pharmaceutical Co., Ltd.

Takahiro Matsuyama

Kenji Kawashima

Toshiyuki Mori

Masatomo Kato

Miwa Takai

Mamoru Matsuda

Tomoko Oda

Yusuke Yamazaki

Daisuke Shii

Tatsuji Kurose

Shinji Takaoka

Yumi Hagiwara

Kenji Oki

Atsuyoshi Dota

Kenji Imoto

The present invention relates to defined quinoxalin-2-one compounds or a pharmaceutically acceptable salt or a hydrate or a solvate thereof. The compounds, salts or hydrates have a glucocorticoid receptor agonist activity, and are useful as a medicine, in particular as a prophylactic or therapeutic agent for a glucocorticoid receptor related disease.

[4-(1,3,3-trimethyl-2-OXO-3,4-dihydro-1H-quinoxalin-7-yl)phenoxy]ethyloxy compound or salt thereof

The present invention relates to a novel [4-(1,3,3-trimethyl-2-oxo-3,4-dihydro-1H-quinoxalin-7-yl)phenoxy]ethyloxy compound or a salt thereof. The compound or a salt thereof of the present invention has a glucocorticoid receptor agonist activity, and is useful as a medicine, in particular as a prophylactic or therapeutic agent for the glucocorticoid receptor related disease.

[4-(1,3,3-trimethyl-2-oxo-3,4-dihydro-1H-quinoxalin-7-yl)phenoxy]ethyloxy compound or salt thereof

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

Growing community of inventors

Ikoma, Japan

Takahiro Matsuyama