【発明の名称】改良トロンビン阻害剤

Japanese Patent JPH05506252

A

This invention relates to coating invasive devies with novel biologically active molecules which bind to and inhibit thrombin. These molecules comprise a catalytic site directed moiety (CSDM) of the formula: wherein X is hydrogen or is characterized by a backbone chain consisting of from 1 to 100 atoms; R1 is selected from the group consisting of unsubstituted, mono-substituted, di-substituted and tri-substituted saturated ring structures; R2 is a bond or is characterized by a backbone chain consisting of from 1 to 5 atoms; R3 is a bond or is characterized by a backbone chain consisting of from 1 to 3 atoms; R4 is any amino acid; R5 is any L-amino acid which comprises a guanidinium- or amino-containing side chain group; R6 is a non-amide bond; and Y is characterized by a backbone chain consisting of from 1 to 9 atoms; or the formula: wherein R1' is selected from the group consisting of unsubstituted, mono-substituted, di-substituted and tri-substituted ring structures; R4' is any amino acid comprising a side chain group characterized by the capacity to accept a hydrogen bond at a pH of between about 5.5 and 9.5; and X, R2, R3, R5, R6 and Y are defined as above. Preferred thrombin inhibitors are further characterized by a anion binding exosite associating domain (ABEAM) and a linker portion of between 18 ANGSTROM and 42 ANGSTROM in length which connects the Y to the ABEAM.

Malaganore, John M.
Jablonsky, Joe-An-M.
Bourdon, Paul Earl.

JP50574592A

September 16, 1993

February 03, 1992

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Biogen, Inc.

A61K51/00; A61L33/00; A61P7/02; C07K5/00; C07K5/107; C07K7/00; C07K7/02; A61K38/55; C07K7/06; C07K7/08; C07K14/815; C12N9/99; C12N15/15; A61K38/00; (IPC1-7): A61K37/64; A61K49/02; A61L33/00; C12N9/99

JP4507253Y

Hidesaku Yamamoto

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