Other

Showa Denko Kabushiki Kaisha

The United States of America, As Represented by the Secretary, Department of Health and Human Services

Teikoku Seiyaku Co., Ltd.

Shosuke Okamoto

Kobe Gakuin University

Watanabe Chemical Industries, Ltd.

Yoshio Okada

Taketoshi Naito

Yoshio Kimura

Lawrence H Lazarus

Morihiko Yamada

Norio Ohno

Akiko Okunomiya

Yasuhiro Katsuura

Koichi Kawasaki

Hiroshi Nojima

Yuko Tsuda

Toshio Yokoi

Takashi Shishikura

Yumi Seki

Shin Iguchi

Sharon D Bryant

Tingyou Li

The present invention relates to symmetric and asymmetric dimeric Dmt (2',6&#x2032;-ditnethyl) compounds and Dmt derivative compounds with dual &#x3b4; and &#x3bc; opioid receptor antagonist activity. Also, the present invention provides compositions comprising these compounds and it provides methods of using these compounds.

Dmt-derivative compounds and related compositions and methods of use

1. A peptide derivative represented by the following formula (1) or a salt thereof;wherein Ris hydrogen atom or methyl group, Ris hydrogen atom or hydroxy group and n is an integer of 1-8, provided that Ris hydrogen atom when Ris hydrogen atom, which has specific and high binding affinity with the &#x3bc;-opioid receptor.

Opioid derivative

New compounds N-.alpha.-9-fluorenylmethoxycarbonyl-aspartic acid-.beta.-1-adamantyl esters are stable under the basic condition of the normal peptide condensation process and do not form succinimide. Peptides containing aspartic acid can be synthesized with high purity and at high yields by using N-.alpha.-9-fluorenylmethoxycarbonyl-aspartic acid-.beta.-1-adamantyl ester.

Aspartic acid derivatives

New aspartic acid derivatives include N-.alpha.-t-butoxycarbonyl-aspartic acid-.beta.-2-adamantyl ester-.alpha.-benzyl ester, N-.alpha.-t-butoxycarbonyl-aspartic acid-.beta.-2-adamantyl ester and benzyloxycarbonyl-aspartic acid-.beta.-2-adamantyl ester-.alpha.-benzyl ester.

A phenylalanine derivative having the formula (I): ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen provided that both R.sup.1 and R.sup.2 are not hydrogen at the same time;

Phenylalanine derivative and proteinase inhibitor

A phenylalanine derivative having the formula (I): ##STR1## wherein A represents ##STR2## B represents ##STR3## wherein m is 0, 1, or 2 and n is 3, 4, or 5; X represents (a) hydroxy, (b) nitro, (c) amino, (d) phenoxy which may be substituted with (i) halogen or (ii) nitro, (e) c.sub.1 -C.sub.4 alkyloxy which may be substituted wit (i) phenyl or (ii) benzoyl, (f) benzoyl, (g) pyridyloxy which may be substituted with (i) halogen or (ii) nitro, or (h) c.sub.1 -C.sub.4 alkyl which may by substituted with halogen;

Growing community of inventors

Akashi, Japan

Yoshio Okada