Takeda Pharmaceutical Company Limited

Takeda Chemical Industries, Inc.

Hiroshima University

Masayuki Ii

Norikazu Tamura

Takashi Ichikawa

Katsumi Itoh

Yuzo Ichimori

Junji Yamada

Tomoyuki Kitazaki

Naoko Matsunaga

Osamu Hazeki

Kaoru Hazeki

The present invention provides a method of screening for a drug for the prophylaxis or treatment of at least one disease selected from the group consisting of cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, severe sepsis and septic shock, which includes selecting a substance that binds to an intracellular region of TLR4, and inhibits signal transduction from said molecule, and a kit for this method, which contains (1) a cell that expresses wild-type TLR4 and (2) a cell that expresses a mutant TLR4, and which can detect a signal from TLR4 with expression of a reporter gene as an index.

Screening method for a substance that binds to an intracellular region of TLR4

The present invention is directed to a class of cyclohexene derivatives bearing sulfamoyl and ester groups which have an inhibitory activity on nitric oxide (NO) production and cytokine production, and are useful as an agent for the prophylaxis and/or treatment of diseases such as, cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, and septic shock.

Substituted aromatic-ring compounds, process for producing the same and use

A compound of the formula: wherein Ris an aliphatic hydrocarbon group optionally having substituent(s), an aromatic hydrocarbon group optionally having substituent(s), a heterocyclic group optionally having substituent(s), a group of the formula: ORwherein Ris a hydrogen atom or an aliphatic hydrocarbon group optionally having substituent(s), or a group of the formula: wherein Rand Rare the same or different and each is a hydrogen atom or an aliphatic hydrocarbon group optionally having substituent(s), X is a methylene group, a nitrogen atom, a sulfur atom or an oxygen atom, Y is an optionally substituted methylene group or an optionally substituted nitrogen atom, ring A is a 5 to 8-membered ring optionally substituted further by 1 to 4 substituent(s) selected from (1) an aliphatic hydrocarbon group optionally having substituent(s), (2) an aromatic hydrocarbon group optionally having substituent(s), (3) a group of the formula: ORwherein Ris a hydrogen atom, or an aliphatic hydrocarbon group optionally having substituent(s) and (4) a halogen atom, Ar is an aromatic hydrocarbon group optionally having substituent(s), a group of the formula: is a group of the formula: or the formula: m is an integer of 0 to 2, n is an integer of 1 to 3, and the sum of m and n is not more than 4, provided that when X is a methylene group, Y is an optionally substituted methylene group, and a salt thereof have an inhibitory activity on nitric oxide (NO) production and cytokine production, and are useful as an agent for the prophylaxis and/or treatment of diseases, such as cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, septic shock and the like.

Substituted aromatic-ring compounds, process for producing the same, and use

Cycloalkene derivatives, process for producing the same, and use

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Minoo, Japan

Masayuki Ii