Santen Pharmaceutical Co., Ltd.

Hiroshi Enomoto

Kenji Kawashima

Hiroyuki Inoue

Minoru Yamamoto

Hiroshi Suhara

Masakazu Ban

Masato Horiuchi

Noriyoshi Yamamoto

Masaaki Murai

Kazuhiro Kudou

Takaaki Inaba

Noriko Ishizaka

Takahiro Honda

Mamoru Matsuda

Kazuyoshi Okamoto

Shin-ichiro Hirai

Shinji Takaoka

Hiroaki Kurashima

Yukie Fujita

Noriko Kawashima

Koji Ohashi

Yasutaka Fujioka

A compound represented by the following general formula (1) or a salt thereof. Rrepresents a halogen atom and so on; Rand Reach represent a hydrogen atom and so on; Rand Reach represent a hydrogen atom and so on, or Rand Rmay form an oxo group; Rand Reach represent a lower alkyl group optionally having a substituent and so on, or they may bind to each other to form a nitrogen-containing heterocyclic ring which may be substituted by one or plural R; Rrepresents an aryl group optionally having a substituent and so on; ring A represents a benzene ring and so on; and m represents 0, 1 or 2. 

Compound having PARP inhibitory activity

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

A compound having the following formula wherein A is &#x2014;O&#x2014;; B is alkylene or alkenylene optionally containing &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;(NR)&#x2014;, &#x2014;CO&#x2014; or &#x2014;N&#x2550;; Rand Rare alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, wherein the alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl is unsubstituted or substituted by halogen, cycloalkyl, aryl, adamantyl or amino; Ris a substituted or unsubstituted pyridine ring; Rand Rare hydrogen or alkyl; Ris hydrogen or alkyl; X is O or S; and each hydrogen of the said amino is unsubstituted or substituted by alkyl, alkoxycarbonyl, cycloalkyloxycarbonyl, arylalkoxycarbonyl or halogenoalkyloxycarbonyl. The compound is a TNF-&#x3b1; production inhibitor that is useful for treating autoimmune diseases such as rheumatoid arthritis.

TNF-&#x3b1; production inhibitors

A purpose of the present invention is to provide TNF-&#x3b1; production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts thereof according to the present invention have excellent TNF-&#x3b1; production inhibitory activities, 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, adamantyl or the like, Ris aryl or an unsaturated heterocycle, and &#x201c;X&#x201d; is oxygen or sulfer respectively.

A purpose of the present invention is to provide TNF-&#x3b1; production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts thereof according to the present invention have excellent TNF-&#x3b1; production inhibitory activities, 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, adamantyl or the like, Ris aryl or an unsaturated heterocycle, and X is oxygen or sulfer respectively.

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Ikoma, Japan

Hiroshi Enomoto