Santen Pharmaceutical Co., Ltd.

Order-Made Medical Research Inc.

Tatsuji Kurose

Toshiyuki Mori

Masatomo Kato

Miwa Takai

Mamoru Matsuda

Takahiro Matsuyama

Yumi Hagiwara

Yasufumi Murakami

Kenji Oki

Hirotada Akiyama

Hiroyuki Satofuka

Shigeki Mukoubata

Atsuyoshi Dota

Sae Akao

Kenji Imoto

An object of the present invention is to provide an antibody against VEGF that inhibits binding of a vascular endothelial growth factor (VEGF) to neuropilin-1 (NRP1). The present invention provides an antibody against VEGF that inhibits binding of VEGF to NRP1.

Antibody inhibiting binding of VEGF to NRP1

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

Tatsuji Kurose