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filingDate 1999-10-19-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bff559247bcce518ca8fe2c6e55f9b64
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e94f4292af38f3dc971799f82b5df9d5
publicationDate 2003-03-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber NZ-511067-A
titleOfInvention Serine protease inhibiting isoquinoline derivatives and their use for treating or preventing thrombin-mediated or thrombin-associated diseases
abstract A serine protease inhibitor of formula (I), wherein: J is H, R1, R1-SO2, R3OOC-(CHR2)p-, (R2a, R2b)N-CO-(CHR2)p- or Het-CO-(CHR2)p-; D 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-1,2,3,4- tetrahydroisoquinoline-1-carboxylic acid, D-1,2,3,4- tetrahydroisoquinoline-3-carboxylic acid, D-2- aminotetraline-2-carboxylic acid, 2-aminoindan-2-carboxylic acid, D-perhydroisoquinolyl 1-carboxylic acid or D- perhydroisoquinolyl 3-carboxylic acid; E is -N(3-6C)cycloalkyl-CH2- or the fragment of formula (a), optionally substituted with (1-6C)alkyl or (1- 6C)alkoxy; R1 is selected from (1-12C)alkyl, (3-12C)cycloalkyl and (3- 12C)cycloalkyl(1-6C)alkylene, which groups may optionally be substituted with (3-12C)cycloalkyl, (1-6C)alkoxy, oxo, and from (6-14C)aryl, (7-15C)aralkyl and (14- 20C)(bisaryl)alkyl, whereby the aryl group may optionally be substituted with (1-6C)alkyl, (3-12C)cycloalkyl, (1- 6C)alkoxy, OH, CF3 or halogen; R2 is H; R2a and R2b are each independently selected from H, (1- 8C)alkyl, (3-8C)cycloalkyl and (3-6C)cycloalkyl(1- 4C)alkylene, which can each be optionally substituted with (3-6C)cycloalkyl, (1-6C)alkoxy, and from (6-14C)aryl and (7- 15C)aralkyl whereby the aryl group may optionally be substituted with (1-6C)alkyl, (3-6C)cycloalkyl, (1- 6C)alkoxy, CF3 or halogen; R3 is H, (1-8C)alkyl, (3-8C)cycloalkyl or (3- 6C)cycloalkyl(1-4C)alkylene, which can each be optionally substituted with (3-6C)cycloalkyl, (1-6C)alkoxy, and from (7-15C)aralkyl whereby the aryl group may optionally be substituted with (1-6C)alkyl, (3-6C)cycloalkyl, (1- 6C)alkoxy, CF3 or halogen and form Het-(1-6C)alkyl; R4 is 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 N-alkoxycarbonyl protected derivative thereof; and/or a pharmaceutically acceptable addition salt and/or solvate thereof and its use in therapy and manufacture of a medicament for treating or preventing thrombin-mediated and thrombin-associated diseases is disclosed.
priorityDate 1998-10-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 47.