http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-070410-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0a9e6421e9257148abad101e1ce6c162 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5025 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 |
| filingDate | 2009-02-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2010-04-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-070410-A1 |
| titleOfInvention | TRIAZOLOPIRIDAZINAS AS PAR1 INHIBITORS THEIR PREPARATION AND ITS USE AS MEDICINES |
| abstract | Compounds with antithrombotic activity, which especially inhibit the protease activated receptor 1, to methods for its preparation and its use as medications, for the treatment of thrombosis, embolism, hypercoagulability and inflammatory disorders. Claim 1: A compound of the formula 1 and / or any stereoisomeric or tautomeric form of the compound of the formula 1 and / or mixtures of these forms in any proportion, and / or a physiologically compatible salt of the compound of the formula (1), wherein Q1 is a hydrogen atom, -C1-6 alkyl, -C3-6 cycloalkyl, -OH, -O-C1-6 alkyl or -O-C3-6 cycloalkyl, where each of alkyl and cycloalkyl is without substitute or mono-, di- or trisubstituted independently with -C 1-4 alkyl, -C 3-6 cycloalkyl, OH, -O-C 1-6 alkyl or -O-C 3-6 cycloalkyl, where some or all of the hydrogen atoms in the alkyl or cycloalkyl can be replaced by fluorine, Q2 and Q3 are the same or different and each is independently a hydrogen atom, -C1-6 alkyl or -C3-6cycloalkyl, where some or all of the hydrogen atoms in the alkyl or cycloalkyl can be replaced by fluorine, R1, R2 and R3 are the same or different and each is independently a hydrogen atom , -C 1-6 alkyl, -C3-6 cycloalkyl, -O-C 1-8 alkyl, -O-C3-6 cycloalkyl, -C0-4 -C (alkylene) -N (R11) -R12, -C0 alkylene -4-C (O) -O-R11, -C0-4-C alkylene (O) -R11, -C0-4-N alkylene (R11) -R12, -C0-4-N alkylene (R11) -C (O) -R12, halogen, OH, -CN, -NO2, -SO2CH3, -SO2CF3, -SF5, -Si [C1-4 alkyl] 3, -C 1-6 alkylene-O-C1-6 alkyl, -O -C 1-6 alkylene-C 1-6 alkyl, -O-C 0-4 alkylene-C 6-14 aryl where the aryl is unsubstituted or mono-, di- or trisubstituted independently with -O-C 1-6 alkyl, - C1-4 alkyl, OH, -C3-6cycloalkyl or -O-C3-6 cycloalkyl, -O-C1-4 alkylene-C3-6 cycloalkyl, - C4-15 Het, where Het is unsubstituted or mono-, di - or trisubstituted independently with -C 1-4 alkyl, -C 3-6 cycloalkyl, OH-O-C 1-6 alkyl or -O-C 3-6 cycloalkyl or -O-C 1-6 alkylene-C 1-6 alkylene -C1-6 alkyl, where each of the alkyl, alkylene and cycloalkyl is unsubstituted or mono-, di- or trisubstituted independently with -C1-4 alkyl, -C3-6 cycloalkyl, OH, -O-C1-6 alkyl, -to C6-14 ryl where the aryl is unsubstituted or mono-, di-, tri-, tetra- or pentas independently substituted with halogen, -C1-4 alkyl, -C3-6 cycloalkyl, OH, -O-C1-6 alkyl or -O C3-6 cycloalkyl, -Het C4-15 where Het is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted independently with halogen, -C1-4 alkyl, -C3-6 cycloalkyl, OH, -O-C1-6 alkyl or -O-C3-6 cycloalkyl, or -O-C3-6 cycloalkyl, or where some or all of the hydrogen atoms in the alkyl, alkylene or cycloalkyl can be replaced by fluorine, or R1 and R2 or R2 and R3, together with the ring atoms to which each one is attached, form a 5 to 8 member ring, where the ring consists only of carbon atoms or 1, 2 or 3 of these atoms are replaced by nitrogen, oxygen or sulfur atoms, where the ring is unsubstituted or mono- or disubstituted independently with -C 1-4 alkyl, -C 3-6 cycloalkyl, OH, -O-C 1-6 alkyl or -O-C 3- cycloalkyl. 6, where some or all The hydrogen atoms of the 5 to 8-membered ring formed, and in the alkyl or cycloalkyl, can be replaced by fluorine, each of R11 and R12 is independently a hydrogen atom, -C1-6 alkyl, -C3-6 cycloalkyl , -C0-4 alkylene-C6-14 aryl where the aryl is unsubstituted or mono-, di- or trisubstituted independently with -O-C1-6 alkyl, -C1-4 alkyl, OH, -C3-6 cycloalkyl or - O-C3-6 cycloalkyl, -C0-4-C4-15 alkylene where Het is unsubstituted or mono-, di-, tri-, tetra- or pentas independently substituted with halogen, -C 1-4 alkyl, -C3 -cycloalkyl 6, OH, -O-C1-6 alkyl or -O-C3-6 cycloalkyl, -SO2CH3 or -SO2CF3, where some or all of the hydrogen atoms in the alkyl, alkylene or cycloalkyl can be replaced by fluorine, or R11 and R12 in the fragments ôN (R11) -R12ö and ôN (R11) -C (O) -R12ö represent a 5 to 8-membered ring that is formed together with the nitrogen atom ôNö or the group ôN-C (O) ö for form cyclic amines, imides or lact amas containing up to 2 additional heteroatoms of the group of N, O and S, where the ring is unsubstituted or mono- or independently substituted with -C 1-4 alkyl, -C 3-6 cycloalkyl, OH, -O-C 1-6 alkyl or -C3-6 cycloalkyl, where some or all of the hydrogen atoms of the 5 to 8-membered ring formed, and in the alkyl or cycloalkyl, can be replaced by fluorine, R4, R5, R6, R7 and R8 are the same or different and each is independently a hydrogen atom, -C1-6 alkyl, -C3-6 cycloalkyl, OH, -CN, -NO2, -O-C1-8 alkyl, -O-C3-6 cycloalkyl, -C0 alkylene -4- (CO) -N (R21) -R22, -SO2CH3, -SO2CF3, -C0-4-C alkylene (O) -O-R21, halogen, -SF5, -C0-4-C alkylene (O) -R21, -C0-4-N alkylene (R21) -R22, -C0-4-N alkylene (R21) -C (O) -R22, -C 1-6 alkylene-C-6-alkyl, -C0 alkylene -6-O-C1-6 alkylene-O-C1-6 alkyl, -Si [C1-4 alkyl] 3, -C0-6 alkylene-C4-6 alkylene-C3-6 cycloalkyl, -C0-6 alkylene -O-C0-6 alkylene-C6-14 aryl where the aryl is unsubstituted or mono-, di- or trisubstituted independently with -O-C1-6 alkyl, -C1-4 alkyl, OH, -C3-6 cycloalkyl or -O-C3-6 cycloalkyl, or -Het C4-15 where Het is unsubstituted or mono- , di- or trisubstituted independently with -O-C1-6 alkyl, -C 1-4 alkyl, OH, -C3-6 cycloalkyl or -O-C3-6 cycloalkyl, where each of alkyl, alkylene and cycloalkyl is unsubstituted or mono-, di- or trisubstituted independently with -C 1-4 alkyl, -C 3-6 cycloalkyl, OH, -O-C 1-6 alkyl, -C 6-14 aryl where the aryl is unsubstituted or mono-, di-, tri -, tetra- or pentas substituted independently with halogen, -C1-4 alkyl, -C3-6 cycloalkyl, OH, -O-C1-6 alkyl or -O-C3-6 cycloalkyl, -Het C4-15 where Het is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted independently with halogen, -C 1-4 alkyl, -C3-6 cycloalkyl, OH, -O-C 1-6 alkyl or -O-C 3-6 cycloalkyl, or - C3-6 O-cycloalkyl, where some or all of the hydrogen atoms in the alkyl, alkylene or cycloalkyl can ree Scroll by fluorine, or R4 and R5, R5 and R6, R6 and R7 or R7 and R8, together with the ring atoms to which each one is attached, form a 5 to 8 member ring, where the ring consists only carbon atoms or 1, 2 or 3 of these atoms are replaced by nitrogen, oxygen or sulfur atoms, where the ring is unsubstituted or mono- or independently disubstituted with -C 1-4 alkyl, -C 3-6 cycloalkyl, OH, -O-C1-6 alkyl or -O-C3-6 cycloalkyl, where some or all of the hydrogen atoms of the 5 to 8-membered ring formed, and in the alkyl or cycloalkyl, can be replaced by fluorine, each of R21 and R22 is independently a hydrogen atom, -C 1-6 alkyl, -C3-6 cycloalkyl, -C0-4 alkylene-C6-14 aryl where the aryl is unsubstituted or mono-, di- or trisubstituted independently with -O -C1-6alkyl, -C1-4alkyl, OH, -C3-6cycloalkyl or -O-C3-6cycloalkyl, -C0-4 -alkylene C4-15 where Het is unsubstituted or mono-, di-, tri-, tet ra- or pentasubstituted independently with halogen, -C1-4 alkyl, -C3-6 cycloalkyl, OH, -O-C1-6 alkyl or -O-C3-6 cycloalkyl, -SO2CH3 or -SO2CF3, where some or all atoms of hydrogen in the alkyl, alkylene or cycloalkyl can be replaced by fluorine, or R21 and R22 in the fragments "N (R21) -R22" and "N (R21) -C (O) -R22" represent a 5 to 8-membered ring that is formed together with the nitrogen atom ôNö or the group ôN-C (O) ö to form cyclic amines, imides or lactams containing up to 2 additional heteroatoms of the group of N, O and S, where the ring is unsubstituted or mono- or independently substituted with -C 1-4 alkyl, -C 3-6 cycloalkyl, OH, -O-C 1-6 alkyl or -O-C 3-6 cycloalkyl, where some or all of the hydrogen atoms of the 5 to 8 membered ring formed, and in the alkyl or cycloalkyl, they can be replaced by fluorine. Claim 9: A process for preparing the compound of the formula (1), according to one or more of claims 1 to 5, comprising: a) reacting a compound of the formula (2) in which each of R4 to R8, Q2 and Q3 is as defined in formula (1) and W is chloride, bromide, mesylate or tosylate with a compound of formula (3) in which each of R1, R2, R3 and Q1 it is as defined in formula (1), with or without the addition of a base, in a solvent to give a compound of formula (1), or b) reacting a compound of formula (7) in which each of R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 is as defined in formula (1) with a compound QW 'in which W' is chloride, bromide, mesylate, tosylate, methylsulfate or a similar suitable leaving group, with or without the addition of a base, to give a compound of the formula (1), or c) isolate the compound of the formula (1) prepared by the method a) or ) in free form or release it of physiologically incompatible salts or, in the case of presence of acidic or basic groups, convert it into physiologically compatible salts, od) separate a compound from the formula (1) prepared by method a) or b), or a suitable precursor of the formula (1) which, due to its chemical structure, is given in enantiomeric or diastereomeric forms, in pure enantiomers or diastereomers by salt formation with enantiomerically pure acids or bases, chromatography on chiral stationary phases or derivatization by means of enantiomerically compounds pure chiral such as amino acids, separation of diastereomers obtained in this way and elimination of chiral auxiliary groups. |
| priorityDate | 2008-02-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 46.