Title:
NOVEL DIPEPTIDE OR ITS PHARMACOLOGICALLY PERMISSIBLE SALT AND ITS MEDICAL USE
Document Type and Number:
Japanese Patent JP3408379
Kind Code:
B2
Abstract:
PROBLEM TO BE SOLVED: To obtain a novel dipeptide which has specific and high inhibitory activity against HIV protease, is readily absorbable in digestive tracts, can be largely reduced its oral dose with much increased in vivo stability.
SOLUTION: This dipeptide is represented by formula I (R1 is a five- or six-membered monocyclic hydrocarbon; X is methylene, chloromethylene, O, S, SO2; R21 and R22 are each H, a 1-6C aliphatic hydrocarbon; R3 is an aliphatic hydrocarbon, an aromatic monocyclic hydrocarbon) or its pharmacologically permissible salt, typically (R)-N-t-butyl-3-[(2S,3S)-2-hydroxy-3-[benzoyl]amino-4- phenylbutanoyl]-1,3-thiazolidine-4-carboxamide. The compound of formula I is prepared by leading a compound of formula II to an N-acylated derivative as an intermediate. In addition, the compounds of formula III (R11 is H, amino; R12 is H, a hydrocarbon), formula IV, formula V (R31-R33 are each H, a halogen, an aliphatic hydrocarbon) also are novel.
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Inventors:
Ryohei Kato
Tsutomu Mitsumoto
Fukasawa Tominaga
Naoko Morohashi
Yoshiaki Kiso
Tsutomu Mitsumoto
Fukasawa Tominaga
Naoko Morohashi
Yoshiaki Kiso
Application Number:
JP18563196A
Publication Date:
May 19, 2003
Filing Date:
June 26, 1996
Export Citation:
Assignee:
Japan Energy Co., Ltd.
International Classes:
C07D277/06; A61K31/40; A61K31/401; A61K31/421; A61K31/425; A61K31/426; A61P31/12; A61P31/18; A61P37/04; C07D207/16; C07D263/06; (IPC1-7): A61K31/401; A61K31/421; A61K31/426; A61P31/18; A61P37/04; C07D207/16; C07D263/06; C07D277/06
Domestic Patent References:
| JP8311024A | ||||
| JP9194355A | ||||
| JP6100533A |
Attorney, Agent or Firm:
Seiya Fujino
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