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Title:
PEPTIDE BORONIC ACID INHIBITOR OF TRYPSIN-LIKE PROTEASE
Document Type and Number:
Japanese Patent JPS6463583
Kind Code:
A
Abstract:

NEW MATERIAL: The compd. of formula I [Y1, Y2 are each OH, F, together form a part derived from a dihydroxy compd. having 2 pieces of OH separated by ≥ two pieces of bond atoms in 1 to 20C, in some cases, in chain and ring including a heteroatom; R2 is -(CH2)2-X (X is NH2 etc.; (z) is 3 to 5) etc.; (n), (o), (p), (q) are 1, 0; A1 to A3 are amino acids of L, D configuration, such as Arg, Asn of Al; R1 is peptide including 1 to 20 pieces of amino acids, 1 to 20C acyl, sulfonyl, H, N-terminal protecting group].

EXAMPLE: The compd. of formula II.

USE: A trypsin-like protease inhibitor.

PROCESS: For example, the compd. of formula III is dissolved in DMF and is heated by adding sodium azide thereto. Ethyl acetate is added thereto and the compd. is washed with water, etc. An org. layer is subjected to drying, filtering and evaporating, then to processing with chromatography.


Inventors:
CHIYAARUZU EIDORIAN KETONAA
ASHIYOKUKUMARU BIIKUKATSUPA SH
Application Number:
JP13577088A
Publication Date:
March 09, 1989
Filing Date:
June 03, 1988
Export Citation:
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Assignee:
DU PONT
International Classes:
A61K38/00; A61K38/06; A61K38/55; A61P7/02; A61P29/00; C07K5/06; C07F5/00; C07F5/02; C07K5/00; C07K5/04; C07K5/065; C07K5/08; C07K5/097; C07K5/10; C07K5/103; C07K14/81; C12N9/99; A61K; C07F; C07K; (IPC1-7): A61K37/64; C07F5/02; C07K5/06; C07K5/08; C07K5/10; C12N9/99
Attorney, Agent or Firm:
Chika Takagi (2 outside)