Fujisawa Pharmaceutical Company, Ltd.

Masaaki Matsuo

Ikuo Ueda

Kiyoshi Tsuji

Hiroshi Matsuda

Daijiro Hagiwara

Nobukiyo Konishi

Hiroshi Miyake

Shinji Shigenaga

Takashi Manabe

Yoshinari Sato

Takashi Ogino

Katsuya Nakamura

Suminori Umio

Hiroyuki Okumura

Kazuo Okumura

Kenji Murano

Shizuo Maeno

Norihiro Igari

Masayuki Kato

Susumu Satoh

Tadashi Terasaka

Kyoichi Shimomura

Hachiro Seno

Glen W Spears

Takao Watanabe

Masakazu Kobayashi

Osamu Nakaguti

Hiroaki Nishimura

Yoshihiko Kitaura

Osamu Nakaguchi

Kiyoshi Taniguchi

Kazuhiko Take

Takatomo Ogahara

Daizo Morino

Naoaki Fujii

Piperazine derivatives as tachykinin antagonists

Thiazolylbenzofuran derivatives and pharmaceutical compositions

Piperazine derivatives

A piperazine compound of the formula: ##STR1## wherein: X is carbonyl or sulfonyl;

Heterotricyclic derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, nitro, amino or protected amino,

Heterotricyclic derivatives, process for their preparation and

A piperazine compound of the formula: ##STR1## wherein: X is carbonyl or sulfonyl; Y is a direct bond or lower alkylene; and R.sub.1, R.sub.2, R.sub.3, R.sub.4 are as defined herein. The compounds are advantageously used as Tachykinin antagonists in the treatment of respiratory diseases, ophthalmic diseases and inflammatory diseases, for example.

The present invention relates to new pyrazole derivatives represented by the following general formula (I) ##STR1## wherein R.sup.1 is aryl which is substituted with substituent(s) selected from the group consisting of lower alkylthio, cyclo(lower)alkyl, hydroxy, hydroxy(lower) alkyl, cyano, lower alkylenedioxy, acyl, acyloxy, aryloxy and lower alkoxy optionally substituted with acyl or lower alkoxy,

Pyrazole derivatives, processes for preparation thereof and

Quinolylbenzofuran derivatives as leukotriene antagonists

A method of making a peptide compound of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl,

Process for making peptide compounds having tachykinin antagonistic

Disclosed herein are compounds of the following formula: ##STR1## wherein R.sup.1 is a group of the formula ##STR2## 'X' is CH.sub.2 or N, 'Z' is O, S, or N--R.sup.6, 'A' is an amino acid residue, and Y, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are substituent variables as defined herein. The compounds are antagonists of tachykinin, and as such are useful for alleviation of pain and for treatment of disorders including asthma, bronchitis, rhinitis, conjunctivitis, dermatitis, arthritis, and urticaria.

Tachykinin antagonist dipeptides

This invention relates to new thiophene derivatives having antiinflammatory and analgesic activities and represented by the general formula [I]: ##STR1## wherein R.sup.1 is hydrogen, halogen, cyano, substituted lower alkyl, substituted or unsubstituted lower alkenyl, acyl, nitro, substituted or unsubstituted amino, sulfo, substituted or unsubstituted sulfamoyl, N-containing heterocyclicsulfonyl, hydoxy, substituted or unsubstituted heterocyclic group,

Thiophene derivatives

The present invention relates to new pyrazole derivatives represented by the following general formula (I) ##STR1## wherein R.sup.1 is aryl which is substituted with substituent(s) selected from the group consisting of lower alkylthio, cyclo(lower)alkyl, hydroxy, hydroxy(lower)alkyl, cyano, lower alkylenedioxy, acyl, acyloxy, aryloxy and lower alkoxy optionally substituted with acyl or lower alkoxy, R.sup.2 is halogen, halo(lower)alkyl, cyano or acyl, and R.sup.3 is aryl substituted with nitro, hydroxy, lower alkoxy, lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl, provided that when R.sup.3 is aryl substituted with nitro, hydroxy or lower alkoxy, then R.sup.1 is aryl substituted with lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl, and pharmaceutically acceptable salts thereof.

A compound of the formula: ##STR1## wherein R.sup.1 is aryl, or a group of the formula: ##STR2## wherein X is CH or N, and Z is O or N--R.sup.5,

Peptide compounds, a process for preparation thereof and pharmaceutical

A substance P antagonistic peptide of the following formula is disclosed: ##STR1##

Peptides having substance P antagonistic activity

Growing community of inventors

Toyonaka, Japan

Masaaki Matsuo