Santen Pharmaceutical Co., Ltd.

Kazuhiro Kudou

Minoru Yamamoto

Kenji Kawashima

Masakazu Ban

Hiroshi Enomoto

Noriyoshi Yamamoto

Masaaki Murai

Takaaki Inaba

Atsushi Ohno

Noriko Ishizaka

Masato Nagatsuka

Kazuyoshi Okamoto

An object is to provide a novel production method suitable for industrial production of a 3,3-dimethyl-3,4-dihydro-1H-quinoxalin-2-one derivative and a synthetic intermediate for the method. Provided is a method for producing a compound represented by formula (1): wherein Rrepresents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aryl group, Rrepresents a hydrogen atom, an optionally substituted alkyl group, a hydroxy group, or nitrogen atom-protecting group, Rrepresents a hydrogen atom, an optionally substituted alkyl group, a hydroxy group, or a nitrogen atom-protecting group, and X represents a hydroxy group or a leaving group,or a salt thereof, the method comprising the steps of: wherein R, R, and X are the same as defined in formula (1), Rrepresents an optionally substituted alkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aryl group, wherein R, R, R, and X are the same as defined in formulae (1) and (2),or a salt thereof, and

Production method for 3,3-dimethyl-3,4-dihydro-1H-quinoxalin-2-one derivative and intermediate for said production method

A method of manufacturing a compound or a salt thereof expressed with a formula (III) below, characterized by causing a compound or a salt thereof expressed with a formula (I) below and a compound or a salt thereof expressed with a formula (II) below to react in the presence of carbonate and copper salt or in the presence of hydroxide salt, carbonate, and copper salt. 

3-hydroxy-6H-benzo [C] chromene-6-one derivative and manufacturing method thereof

3-hydroxy-6H-benzo [c] chromene-6-one derivative and manufacturing method thereof

Disclosed is a compound represented by the general formula (1) or a salt thereof. The compound or a salt thereof has an inhibitory activity on IKK&#x3b2; and is therefore useful as preventive and/or therapeutic agent for a disease associated with IKK&#x3b2;. In the formula, Rrepresents a hydrogen atom, a lower alkyl group, an aryl group, a hydroxy group, or the like; Rrepresents a halogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, or the like; and m represents 0, 1, 2, or the like. 

Indole derivative having I&#x3ba;B kinase &#x3b2; inhibitory activity

Objects of the present invention are to study on the synthesis of a novel pyrrole derivative having a ureido group and an aminocarbonyl group as substituents or a salt thereof, to find a pharmacological effect of the derivative or a salt thereof, and to find a medicinal agent which has a prophylactic and/or therapeutic effect on a retinal disease or the like through oral administration. A compound represented by the general formula (1) or a salt thereof has an inhibitory activity against the production of interleukin-6 and/or an inhibitory effect on choroidal neovascularization, and is therefore useful as a prophylactic and/or therapeutic agent for a disease associated with interleukin-6, an ocular inflammatory disease and/or a retinal disease. In the formula, the ring A represents a benzene ring or the like; Rrepresents a halogen atom, a hydrogen atom, a lower alkyl group or the like; Rrepresents a halogen atom, a lower alkyl group which may have a substituent, a lower alkenyl group, a lower alkynyl group which may have a substituent, a lower cycloalkyl group, an aryl group, a hydroxy group, a lower alkoxy group which may have a substituent or the like; and n represents 0, 1, 2, 3 or the like. 

Pyrrole derivative having ureido group and aminocarbonyl group as substituents

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Ikoma, Japan

Kazuhiro Kudou