Serine protease inhibitor

Details Serine protease inhibitor Serine protease inhibitor

2005-06-07

2005-06-07

Raymond, Richard L. (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C514S248000, C514S310000, C514S313000, C544S235000, C544S293000, C546S143000, C546S159000

Reexamination Certificate

active

06903107

ABSTRACT:
A serine protease inhibitor having the formula (I),in whichJ is H, R1, R1—O—C(O)—, R1—C(O—, R1—SO2—, R3OOC—(CHR2)p—, (R2a,R2b)N—CO—(CHR2)p— or Het-CO—(CHR2)p—;W is an amino-acid of the formula —NH—CHR1—C(O)—, —NR4—CH((CH2)qC(O)OR1)—C(O)—, —NR4—CH((CH2)qC(O)N(R2a,R2b))—C(O)—, —NR4—CH((CH2)qC(O)Het)-C(O)—, D-1-Tiq, D-3-Tiq, D-Atc, Aic, D-1-Piq, D-3 Piq, glutanyl or a (C1-C6) alkylester thereof;E is —NR2—CH2— or the fragment which is unsubstituted or substituted with (1-6C)alkyl, (1-6C)alkoxy or benzyloxy;R1is selected form (1-12C)alkyl, (2-12C)alkenyl, (2-12C)alkynyl, (3-12C)cycloalkyl and (3-12C)cycloalkyl(1-6C)alkylene, which groups are unsubstituted or substituted with (3-12C)cycloalkyl, (1-6C)alkoxy, oxo, OH, CF3or halogen, and from (6-14C)aryl, (7-15C)aralkyl, (8-16C)aralkenyl and (14-20C)(bisary)alkyl, wherein the aryl groups are unsubstituted or substituted with (1-6C)alkyl, (3-12C)cycloalkyl, (1-6C)alkoxy, OH, CF3or halogen;R2, R2aand R2bare each independently selected from H, (1-C)alkyl, (3-8C)alkenyl, (3-8C)alkynyl, (3-8C)cycloalkyl and (3-6C)cycloalkyl(1-4C)alkylene, which are unsubstituted or substituted with (3-6C)cycloalkyl, (1-6C)alkoxy, CF3or halogen, and from (6-14C)aryl and (7-15C)aralkyl, wherein the aryl groups are unsubstituted or substituted with (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)alkoxy, CF3or halogen;R3is the same as R2or is Het-(1-6C)alkyl;R4is H or (1-3C)alkyl;X and Y are CH or N, with the proviso that they are not both N;Het is a 4-, 5- or 6-membered heterocycle containing one or more heteroatoms selected from O, N and S;m is 1 or 2;p is 1, 2 or 3;q is 1, 2 or 3;t is 2, 3 or 4;or a pharmaceutically acceptable addition salt or solvate thereof.

REFERENCES:
patent: 0 064 294 (1982-11-01), None
patent: 0 393 926 (1990-10-01), None
patent: WO 97 38977 (1997-10-01), None
patent: WO 98 47876 (1998-10-01), None
patent: 99/47503 (1999-09-01), None

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