Kowa Company Limited

Kyoko Yasuoka

Tomoyuki Koshi

Seiichi Sato

Yoshinori Kyotani

Takahiro Kitamura

Hiromichi Shigyo

Hideo Yoshizaki

Junko Totsuka

Shunji Takemura

Masao Ohkuchi

Masahiro Tamura

Hiroyuki Ishiwata

Takayuki Matsuda

Mototsugu Kabeya

Toshimi Mizoguchi

Toru Kanke

Junya Tagashira

Natsuyo Kumai

Tomoko Furuyama

Compounds represented by the general formula (1) or salts thereof or solvates of both; PAR-2 antagonists containing the compounds; and preventive or therapeutic agents for PAR-2 related diseases containing the antagonists as the active ingredient: (1) wherein Ris hydrogen, halogeno, or a group represented by the general formula (2): (wherein Ris straight-chain or branched Calkylene or the like; and Rand Rtogether with the nitrogen atom adjacent to them form a 5- to 7-membered ring); Ris straight-chain or branched Calkyl or the like; Rand Rare each independently hydrogen, one to three halogen atoms, or the like; and A-A-Ais a tripeptide residue composed of &#x3b1;-amino acids each independently selected from the group consisting of glycine, alanine, cyclohexylalanine, and so on.

PAR-2 antagonists

The present invention is directed to a compound represented by formula (1): (wherein Rrepresents an alkyl group which may have a substituent or an alkenyl group which may have a substituent; and each of Rand Rrepresents a hydrogen atom, an alkyl group, a hydroxyalkyl group, a dihydroxyalkyl group, or an alkynyl group, or Rand Rform, together with the nitrogen atom adjacent thereto, a nitrogen-containing saturated heterocyclic group which may have a substituent) and a drug composition containing the compound. The compound exhibits tumor necrosis factor (TNF-&#x3b1;) production inhibitory effect and improved absorption upon oral administration.

Benzofuran derivative

A phenylpyridazine derivative represented by the formula (1): Wherein, R1, R2, R3, X, Y, Z and n have the same meaning as defined in the specification; or a salt thereof, or a medicine containing the compound. The present invention provides water-soluble phenylpyridazine derivatives and medicines containing them, which have excellent inhibitory activity against interleukin-&#x3b2; production, high water solubility and high oral absorbability.

Water-soluble phenylpyridazine derivative and medicine containing the same

Compounds having the formula (1): wherein Rrepresents an alkyl or alkenyl group, Rand Reach independently represent a hydrogen atom or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl group, or Rand Rmay be fused together with the adjacent nitrogen atom to form a substituted or unsubstituted, nitrogen-containing, saturated heterocyclic group, X, Y and Z each independently represent a hydrogen atom, an alkyl group, a halogen atom or the like, and n stands for an integer of from 1 to 5; and also to medicinal compositions containing them. These compounds have inhibitory activity against IL-1&#x3b2; production, high water solubility and good oral absorbability.

Water-soluble phenylpyridazine compounds and compositions containing the same

Compounds having the formula (1):wherein Rrepresents an alkyl or alkenyl group, Rand Reach independently represent a hydrogen atom or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl group, or Rand Rmay be fused together with the adjacent nitrogen atom to form a substituted or unsubstituted, nitrogen-containing, saturated heterocyclic group, X, Y and Z each independently represent a hydrogen atom, an alkyl group, a halogen atom or the like, and n stands for an integer of from 1 to 5; and also to medicinal compositions containing them. These compounds have inhibitory activity against IL-1&#x3b2; production, high water solubility and good oral absorbability.

Compounds having the formula (1):wherein Rrepresents an alkyl or alkenyl group, Rand Reach independently represents a hydrogen atom or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl group, or Rand Rmay be fused together with the adjacent nitrogen atom to form a substituted or unsubstituted, nitrogen-containing, saturated heterocyclic group, X, Y and Z each independently represents a hydrogen atom, an alkyl group, a halogen atom or the like, and n stands for an integer of from 1 to 5; and also to pharmaceutical compositions containing them. These compounds have inhibitory activity against IL-1&#x3b2; production, high water solubility and good oral absorbability.

Pyridazin-3-one derivatives and medicines containing the same

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Higashiyamato, Japan

Kyoko Yasuoka