Institute of Medicinal Molecular Design, Inc.

Shionogi Company Limited

Susumu Muto

Akiko Itai

Takeshi Yanase

Youichi Yamaguchi

Tatsuo Nagano

Hiroshi Fukasawa

Tomomi Sotome

Ryuko Tokuyama

Masayuki Komukai

Terukazu Kato

Takafumi Ohara

Ryukou Tokuyama

Toshifumi Wakamatsu

Tatsurou Ichige

A Inst Of Medicinal Molecular Design Inc Itai

Tomomi Saotome

The compound represented by the following formula (I) and the like have PAI-1 inhibition activity; wherein: Rrepresents a Caryl group which may be substituted or the like; T represents a single bond or the like; m represents 0 or 1; when m is 0, G represents &#x2014;N&#x2014;C(&#x2550;O)&#x2014;COH or the like; when m is 1, G represents an oxygen atom or the like; Rrepresents a Caryl group which may be substituted or the like; E represents the following formula (II) wherein one of R, R, Rand Rrepresents the formula R-T-, each of the other three independently represents a hydrogen atom or the like, and Rrepresents the formula &#x2014;X&#x2014;Y', a hydrogen atom or the like; X represents &#x2014;CH&#x2014; or the like; Y&#x2032; represents a carboxy group or the like; M represents a single bond or the like. 

PAI-1 inhibitor

A medicament having inhibitory activity against NF-&#x3ba;B activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient: wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.

Inhibitors against the production and release of inflammatory cytokines

A compound of the formula (I): or a pharmaceutically acceptable salt thereof.

Derivative having PPAR agonistic activity

Inflammatory cytokine release inhibitor

A compound represented by the following general formula (I) or a salt thereof, or a hydrate thereof or a solvate thereof having an inhibitory action against plasminogen activator inhibitor-1 (PAI-1): wherein Rrepresents a Caryl group; or a substituted Caryl group, Rrepresents a Caryl group; or a Caryl group substituted with a group or groups selected from the group consisting of a halogen atom, nitro group, a Calkyl group, a halogenated Calkyl group, a Calkoxy group, a halogenated Calkoxy group, a phenyl group and carboxy group, X represents &#x2014;CH&#x2014;, &#x2014;CHCH&#x2014;, &#x2014;CH&#x2550;CH&#x2014; or &#x2014;N(R)&#x2014;C(&#x2550;O)&#x2014;, Y represents carboxy group or a bioisostere of carboxy group, Rrepresents hydrogen atom, a Calkyl group or a Caralkyl group, m represents 0 or 1.

Carboxilic acid derivatives

Disclosed is a compound which is useful as an 11&#x3b2;-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: 

Oxazolidinone derivative having inhibitory activity on 11&#x3b2;-hydroxysteroid dehydrogenase type 1

A compound represented by the following general formula (I) or a salt thereof, or a hydrate thereof or a solvate thereof having an inhibitory action against plasminogen activator inhibitor-1 (PAI-1): wherein Rrepresents a Caryl group; or a Caryl group substituted with a group or groups selected from the group consisting of a halogen atom, cyano group, nitro group, a Calkyl group, a halogenated Calkyl group, a Calkoxy group, a halogenated Calkoxy group and a Calkylsulfanyl group, Rrepresents a Caryl group; or a Caryl group substituted with a group or groups selected from the group consisting of a halogen atom, hydroxy group, a Calkyl group, a halogenated Calkyl group, a Calkoxy group, a halogenated Calkoxy group, a Calkylsulfanyl group and phenyl group, X represents a single bond or oxygen atom, Z represents a phenylene group or a substituted phenylene group, m represents 0 or 1.

N-phenyloxamide derivatives

A medicament for the preventive and/or therapeutic treatment of allergic diseases and/or endometriosis and/or hysteromyoma which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substitutents in addition to the group represented by formula &#x2014;O-A wherein A has the same meaning as that defined above and the group represented by formula &#x2014;X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substitutents in addition to the group represented by formula &#x2014;O-A wherein A has the same meaning as that defined above and the group represented by formula &#x2014;X-E wherein each of X and E has the same meaning as that defined above.

Antiallergic agents

A compound represented by the following formula (I) or a salt thereof: wherein R, R, Rand Rrepresent hydrogen atom, a halogen atom, cyano group, nitro group, a Calkyl group, a halogenated Calkyl group or a Calkoxy group, Rrepresents a halogen atom, cyano group, a Calkyl group, a halogenated Calkyl group or a Calkoxy group, Rrepresents a Ccycloalkyl group, a substituted Ccycloalkyl group, a 5 to 7-membered completely saturated heterocyclic group or a substituted 5 to 7-membered completely saturated heterocyclic group, X represents a single bond, oxygen atom, sulfur atom, NR, &#x2014;O&#x2014;CH&#x2014; or &#x2014;N(R)&#x2014;CH&#x2014;, Rrepresents hydrogen atom or a Calkyl group, or Rmay combine with a substituent of Rto represent a single bond, methylene group or ethylene group, Rrepresents hydrogen atom, a Calkyl group or a Caralkyl group, which is useful as an active ingredient of a medicament for prophylactic and/or therapeutic treatment of diseases caused by an activation of STAT6 and/or NF-&#x3ba;B.

N-(3,4-disubstituted phenyl) salicylamide derivatives

A medicament having inhibitory activity against NF-&#x3ba;B activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: 

O-substituted hydroxyaryl derivatives

A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the following general formula (I) or a salt thereof: wherein one of Rand Rrepresents hydrogen atom and the other represents the formula &#x2014;X-A wherein A represents hydrogen atom or an acyl group, X represents oxgen atom or NH; one of Rand Rrepresents hydrogen atom and the other represents the following formula: wherein Y represents a sulfonyl group or a carbonyl group, Rrepresents a cyclic group, Z represents a single bond or a Cto Calkylene group, Rrepresents hydrogen atom or a Cto Calkyl group.

Amide derivatives

A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the general formula (I) or a physiologically acceptable salt thereof: 

Sulfonamide derivatives

A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the following general formula (I): wherein X represents a single bond or a Cto Calkylene group which may be substituted; A represents a Cto Calkyl group which may be substituted, a Cto Caryl group which may be substituted, or a 4 to 10-membered monocyclic or bicyclic and unsaturated, partly saturated, or completely saturated heterocyclic group which may be substituted, wherein said heterocyclic group comprises as ring-constituting atoms 1 to 4 hetero atoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom.

Growing community of inventors

Tokyo, Japan

Susumu Muto