Fujisawa Pharmaceutical Company, Ltd.

Other

Daijiro Hagiwara

Masaaki Matsuo

Hiroshi Miyake

Masashi Hashimoto

Keiji Hemmi

Hiroshi Matsuda

Hidekazu Takeno

Matsuhiko Aratani

Shinji Shigenaga

Nobukiyo Konishi

Takashi Manabe

Kenji Murano

Takashi Kamiya

Masumi Itoh

Hiroaki Nishimura

Kozo Sawada

Kazuo Okumura

Tadashi Terasaka

Matsuhiko Aratari

Misashi Hashimoto

Tetsuo Onami

Thiazolylbenzofuran derivatives and pharmaceutical compositions

Piperazine derivatives

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

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.

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

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

Peptide compounds and pharmaceutical compositions thereof

The present invention relates to DTrp-Phe containing tripeptides and pharmaceuticals, which possess tachykinin antagonism activity as well as processes of making such peptides.

Peptide compounds, processes for preparation thereof and pharmaceutical

Peptide compounds having Substance P antagonism of the formula: ##STR1## wherein R.sup.1 is lower alkyl, aryl, arylamino, pyridyl, pyrrolyl, pyrazolopyridyl, quinolyl, or a group of the formula: ##STR2## wherein the symbol of a line and dotted line is a single bond or a double bond; X is CH or N; Z is O, S or NH; R.sup.2 is hydrogen or lower alkyl; R.sup.3 is hydrogen or hydroxy; R.sup.4 is lower alkyl which may have suitable substituent(s); R.sup.5 is ar(lower)alkyl which may have suitable substituent(s) or pyridyl(lower)alkyl, or R.sup.4 and R.sup.5 are linked together to form benzene-condensed lower alkylene; A is an amino acid residue excepting D-Trp, which may have suitable substituent(s); and Y is bond, lower alkylene or lower alkenylene; and their pharmaceutically acceptable salts are disclosed.

Peptide compounds having substance P antagonism, processes for

New peptides, process for preparation thereof and use thereof

This invention relates to a novel method of producing oxo-containing azetidinone compounds, or salts thereof, or hydrates thereof, said compounds having utility as antimicrobial agents and as intermediates for the synthesis of other azetidinone compounds having antimicrobial activity.

Method of producing oxo-containing azetidinone compounds

This invention relates to cephalosporin analogues and pharmaceutically acceptable salts thereof, of high antimicrobial activity.

Cephalosporin analogues and antimicrobial compositions

The invention deals with Cephalosporin Analogues of the formula: ##STR1## wherein R.sup.1 is amino or amino substituted with a pharmaceutically acceptable carboxylic acyl protective group for the amino substituents in cephalosporin compounds or with benzyl, phenethyl or trityl, and

Growing community of inventors

Moriguchi, Japan

Daijiro Hagiwara