http://rdf.ncbi.nlm.nih.gov/pubchem/patent/NZ-504528-A

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classificationCPCAdditional http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K38-00
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D207-16
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D207-16
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http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P7-02
filingDate 1998-12-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_944cc283c723f7bb049a308e2ab4daad
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1d3067f346c83724f94159a6262fd728
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_28565a11212acd61c79616ba11227ac3
publicationDate 2002-03-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber NZ-504528-A
titleOfInvention (4-amidinobenzylamino)- substituted proline derivatives and pharmaceuticals thereof, useful as thrombin inhibitors
abstract A compound of formula (I), wherein: R1 is H, C(O)R11, SiR12R13R14 or optionally substituted alkyl; R2 and R3 are independently H, alkyl, cyclohexyl or phenyl; Rx represents a structural fragment of formula IIa, IIb or IIc; Y is CH2, (CH2)2, CH=CH, (CH2)3, CH2CH=CH or CH=CHCH2, which latter three groups are optionally substituted by alkyl, methylene, oxo or hydroxy; n is 0, 1, 2, 3 or 4; and B is a structural fragment of formula IVa, IVb, IVc or IVd, wherein X1, X2, X3 and X4 are independently CH, N or N-O; X5 and X6 are independently a single bond or CH2; one of X7, X8 and X9 represents S, O or NH, and the other two independently represent -CH=, =CH-, -N=, =N-, -N(O)= or =N(O)-; R31 represents, in all cases one or more optional substituents selected from halo, alkyl, alkoxy or -O-(CH2)p-C(O)N(R32)(R33); p is 0, 1, 2, 3 or 4; and R32 and R33 are independently H, alkyl or cycloalkyl; with the proviso that when B represents a structural fragment of formula IVa (in which X1, X2, X3 and X4 all represent CH), a structural fragment of formula or IVb or a structural fragment of formula or IVc, R31 represents one or more substituents selected from halo, alkyl, alkoxy or -O-(CH2)p-C(O)N(R32)(R33). Also described is a pharmaceutical formulation including a compound of formula (I) in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier. The compounds of formula (I) are useful for the treatment of a condition where inhibition of thrombin (e.g. thrombosis) is required or desired. The compounds of formula (I) are useful as anticoagulants.
priorityDate 1997-12-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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