Santen Pharmaceutical Co., Ltd.

Masaaki Murai

Minoru Yamamoto

Kenji Kawashima

Hiroshi Enomoto

Kazuhiro Kudou

Takaaki Inaba

Noriko Ishizaka

Kazuo Nishimura

Kazuyoshi Okamoto

Hiroyuki Aono

Kenji Oki

Hisayuki Seike

Hidehito Matsuoka

Fumio Tsuji

Chikako Setoguchi

Iwao Seki

Minoru Sasano

Noriko Kawashima

A method for treating a TRPV1-mediated disease by administering to a patient a therapeutically effective amount of a compound or a salt thereof having the following formula [I]: wherein A represents a lower alkylene group or a lower alkenylene group; Rrepresents a hydrogen atom, an unsubstituted or substituted alkyl group or an unsubstituted or substituted alkenyl group; and Rand Rare the same or different and represent a hydrogen atom, an unsubstituted lower alkyl group or a lower alkyl group substituted by a monocyclic cycloalkyl group, a polycyclic cycloalkyl group or an aryl group.

Method for treating a TRPV1-mediated disease

An indole compound having a carbamoyl group, a ureido group and a substituted oxy group having the following formula (1) or a salt thereof: In the formula (1), Rrepresents a hydrogen atom, an alkyl group, a hydroxy group, or an alkoxy group; Rrepresents a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; Rrepresents a halogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group, a heterocyclic group an alkoxy group, an alkenyloxy group, an alkynyloxy group, a cycloalkyloxy group, an aryloxy group or a heterocyclic oxy group; m represents 0, 1, 2, or 3.

Indole derivative having, carbamoyl group, ureido group and substituted oxy group

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

A compound represented by the following formula (1) or a salt thereof: The compound has an inhibitory activity on the production of interleukin-6, and is therefore useful as a therapeutic agent for a disease associated with interleukin-6, ocular inflammatory diseases and the like. In the formula, Rrepresents a halogen atom, a hydrogen atom, a lower alkyl group which may have a substituent, a formyl group, or a lower alkylcarbonyl group which may have a substituent, Rrepresents a bicyclic hydrocarbon group which may have a substituent or a bicyclic heterocyclic group which may have a substituent, Rrepresents a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, or an acyl group.

Pyrrole derivative having, as substituents, ureido group, aminocarbonly group and bicyclic group which may have substituent

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

An object of the present invention is to find new pharmacological actions of urea compounds having structure represented by the general formula [1]. The urea compounds having the structure represented by the general formula [1] have excellent angiogenesis inhibitory actions. [wherein 'A' is &#x2014;(NR)&#x2014;, &#x2014;(CRR)&#x2014; or &#x2014;O&#x2014;, 'B' is alkylene or alkenylene, R, R, R, Rand Rare hydrogen, alkyl, alkenyl, adamantylalkyl or the like, Ris aryl or an unsaturated heterocycle, and X is oxygen or sulfur].

Angiogenesis inhibitor

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Ikoma, Japan

Masaaki Murai