Fujisawa Pharmaceutical Company, Ltd.

Ujisawa Pharmaceutical Co., Ltd.

Masahiro Neya

Keiji Hemmi

Natsuko Kayakiri

Masashi Hashimoto

Hirokazu Tanaka

Naoki Fukami

Hiroshi Marusawa

Keisuke Imai

Hitoshi Yamazaki

Teruo Kyoto Oku

Kentaro Sato

Masayoshi Murata

Yuki Sawada

Tsuyoshi Mizutani

Chiyoshi Kasahara

Hitoshi Sawada

Kazuhiko Ohne

Shinya Watanabe

Tatsuya Zenkoh

Yoshimasa Imamura

Keiji Hemmi, Deceased

Hatsuko Kayakiri

Noriko Mukai

A compound of formula (I) in which Ris halo, lower alkoxy, optionally substituted aryl, optionally substituted aryloxy, optionally substituted heterecyclic group or optionally substituted lower alkynyl, Ris amidated carboxy, Ris hydrogen or acyl, Ar is aryl or heterocyclic group, X is thia, sulfinyl or sulfonyl, Y and Z are each lower alkylene, m and n are each an integer of 0 to 2, and a salt thereof, useful as inhibitors of matrix metalloproteinases (MMP) or the production of tumor necrosis factor &#x3b1; (TNF &#x3b1;)

Thiazepinyl hydroxamic acid derivatives as matrix metalloproteinase inhibitors

A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; R is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R is an optionally substituted lower alkyl, an optionally substituted lower alkoxy, an optionally substituted aryloxy, an optionally substituted lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substituted amino; R is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R5 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; and R is a hydroxy or a protected hydroxy, and a pharmaceutically acceptable salt thereof. The compound of the present invention is useful as a medicament for prophylactic and therapeutic treatment of MMP-or TNF&agr;-medicated diseases.

Piperazine compounds as inhibitors of MMP or TNF

A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R,is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; R,is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R,is an optionally substituted lower alkyl, an optionally substituted lower alkoxy, an optionally substituted aryloxy, an optionally substitued lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substitued amino; R,is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R,is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; and R,is a hydroxy or a protected hydroxy, and a pharmaceutically acceptable salt thereof. The compound of the present invention is useful as a medicament for prophylactic and therapeutic treatment of MMP- or TNF&agr;-mediated diseases.

Endothelin antagonists

Peptide compounds, their preparation and uses

Peptide compounds of the formula (I') ##STR1## in which R.sup.1 is acyl,

Peptide compound and its preparation

Endothelin antagonists and their preparation

This invention relates to new amino acid derivatives and pharmaceutically acceptable salts thereof, wherein the amino acid derivatives are useful in the treatment and/or prevention of hypertension, heart failure, renal diseases or glaucoma.

Amino acid derivatives, a process for the preparation thereof and

Novel peptides of the formula (I') ##STR1## in which R.sup.1 is hydrogen or acyl,

A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl optionally substituted aryl; or amino optionally substituted; and

Amino acid derivatives, processes for the preparation thereof and

The invention relates to novel intermediate compounds for preparation of novel amino acid derivatives having renin inhibiting activity.

Intermediate for preparation of amino acid derivatives

A compound of the formula: ##STR1## wherein R.sup.1 is aryl optionally substituted with a substituent selected from the group consisting of halogen and halo(lower)alkyl; lower alkyl or cyclo(lower)alkyl; and

Renin inhibitor peptide compounds, a process for the preparation thereof

A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl optionally substituted with a substituent selected from the group consisting of acyl, hydroxy, lower alkoxy, aryl, lower alkylthio and a group of the formula: ##STR2## in which R.sup.5 is hydrogen or acyl and R.sup.6 is hydrogen or lower alkyl; aryl; or amino optionally substituted with substituent(s) selected from the group consisting of lower alkyl and acyl; and

Growing community of inventors

Tsuchiura, Japan

Masahiro Neya