http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-038366-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a7f82940e47ba7a1188f8e2ffca55e0f |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-18 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K45-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-00 |
| filingDate | 2002-11-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-01-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-038366-A1 |
| titleOfInvention | 1,2,4-TRIAZOLO COMPOUNDS [1,5-C] SUBSTITUTED PYRIMIDINS, ANTAGONISTS OF THE ADENOSINE A2A RECEPTOR, PHARMACEUTICAL COMPOSITIONS, THE USE OF SUCH COMPOUNDS FOR THE MANUFACTURE OF A MEDICINAL PRODUCT FOR THE PROCESSING OF DISEASE SYSTEMS AND CENTRAL SYSTEMS A KIT THAT INCLUDES COMBINATION |
| abstract | A substituted 1,2,4-triazolo [1,5-c] pyrimidine compound having the structural formula (1) or one of its salts or solvates acceptable for pharmaceutical use, in which R is selected from the group consisting of R4- heteroaryl, R5-phenyl, (C4-6) cycloalkenyl, as shown in structure (2), C (= CH2) CH3, -CsC-CH3, -CH = C (CH3) 2, and -CH = CH-CH3 , R2 is selected from the group consisting of -WX-, -NR19 (CH2) mWX-, and NR19CH (CH3) -WX, or R2 is selected from the group consisting of alkyl, alkenyl, and -NR18R19, wherein said alkyl, alkenyl and NR18R19, is optionally substituted by -WX; R3 is selected from the group consisting of H, halo, alkyl, trifluoromethyl, alkoxy, alkoxyalkyl, hydroxyalkyl, alkylamino, alkylaminoalkyl, dialkylamino, dialkylaminoalkyl, aminoalkyl, aryl, heteroaryl, and CN; R4 is 1 to 3 substituents, which may be the same or different and are independently selected from the group consisting of H, C1-6 alkyl, -CF3, halogen, -NO2, NR15R16, C1-6 alkoxy, C1-6 alkylthio , C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, -COOR17 and -C (O) NR6R7; R5 is 1 to 5 substituents, which may be the same or different and are independently selected from the group consisting of H, halogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, -CN, -NH2 C1-6 alkylamino, di - ((C1-6) alkyl) amino, -CF3, -OCF3, -S (O) 0-2 (C1-6) alkyl and -CH2-SO2-phenyl; R6 and R7, which may be the same or different, are each independently selected from the group consisting of H, and C1-6 alkyl; R8 is 1 to 5 substituents that may be the same or different and are independently selected from the group consisting of H, halogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, -CN, amino, di - ((C1- 6) alkyl) amino, -CF3, -OCF3, acetyl, -NO2, hydroxy (C1-6) alkoxy, (C1-6) -alkoxy (C1-6) alkoxy, di - ((C1-6) -alkoxy) (C1-6) alkoxy, (C1-6) -alkoxy (C1-6) alkoxy- (C1-6) -alkoxy, carboxy (C1-6) -alkoxy, (C1-6) -alkoxycarbonyl (C1-6) alkoxy, (C3-6) cycloalkyl (C1-6) alkoxy, di - ((C1-6) alkyl) amino (C1-6) alkoxy, morpholinyl, (C1-6) alkyl-SO2-, (C1-6) alkyl-SO2- (C1-6) alkoxy, tetrahydropyranyloxy, (C1-6) alkylcarbonyl (C1-6) -alkoxy, (C1-6) alkoxycarbonyl, (C1-6) alkylcarbonyloxy (C1-6) -alkoxy, -SO2NH2 , phenoxy, structures (3), -O-CH2-P (O) (OR6) 2- and -P (O) (OR6) 2; or the adjacent R8 substituents together are -O-CH2-O; -O-CH2CH2-O-, -O-CF2-O- or -O-CF2CF2-O- and form a ring with the C atoms to which they are attached; R9 is selected from the group consisting of (C1-6) alkyl, R8-aryl, R8-aryl (C1-6) alkyl-, thienyl, pyridyl, cycloalkyl (C3-6), (C1-6) alkyl-OC (O ) -NH- (C1-6) alkyl-, di - ((C1-6) alkyl) aminomethyl, cycloheteroaryl (C1-6) alkyl, aryloxy (C1-6) alkyl, alkoxy (C1-6) alkyl, and as It is shown in structures (4); R10 is 1-2 substituents, which may be the same or different, and are independently selected from the group consisting of H, C1-6 alkyl, R5-aryl, and R4-heteroaryl, or two R10 substituents on the same C may form = O; R11 is H or C1-6 alkyl, -C (O) alkyl, or R17 and R11 taken together are - (CH2) pA- (CH2) q, where p and q are, each independently, 2 or 3 and A is select from the group formed by a bond -CH2-, -S-, and -O-, and form a ring with the N to which they are attached; R12 is 1-2 substituents, which may be the same or different, and are independently selected from the group consisting of H, C1-6 alkyl, hydroxy, C1-6 alkoxy, halogen, and -CF3, R13 is selected from the group formed by H, C 1-6 alkyl, phenyl, benzyl, C 2-6 alkenyl, C 1-6 alkoxy (C 1-6) alkyl, di - ((C 1-6) alkyl) amino (C 1-6) alkyl, pyrrolidinyl (C1-6) alkyl and piperidino (C1-6) alkyl; R14 is selected from the group consisting of H, halogen, (C1-6) alkyl, or (C1-6) alkoxy; R15 is selected from the group consisting of H and (C1-6) alkyl; R16 is selected from the group consisting of H, (C1-6) C-alkyl (O) - and (C1-6) alkyl-SO2-, R17 is selected from the group consisting of (C1-6) alkyl, (C1-6 ) hydroxyalkyl, - (C3-6) cycloalkyl, (C1-6) alkoxy (C1-6) alkoxy, (C1-6) alkoxy, (C1-6) alkoxy (C1-6) alkyl, allyl, propargyl, R8- heteroaryl-, R8-aryl-, and R8-aryl (C1-6) alkyl-; R18 is selected from the group consisting of a bond of -CH2-, -CH (OH) -, -CH (CH3) - -C (CH3) n-, - (CH2) n- and -O (CH2) n-, R19 is selected from the group consisting of H, (C1-6) alkyl, (C1-6) alkyl (C1-6) cycloalkyl, (C1-6) cycloalkyl (C1-6) alkyl and (C1-6) alkoxy (C1 -6) alkyl; Q and Q1 can be the same or different and are selected, each independently, from the group consisting of structures (5) and structures (6) m and n, each independently, 1-3, p and q, each in independently, 0-2; s is 0-4; W is aryl or heteroaryl having 1-3 heteroatoms, which may be the same or different, and are selected, each independently from the group consisting of N, O and S, and where said aryl or heteroaryl is optionally substituted with 1-3 substituents, which may be the same or different, and are independently selected from the group consisting of alkyl, aryl, alkylcycloalkyl, halo, hydroxy, hydroxyalkyl, alkoxy, alkylalkoxy, alkoxyalkoxy, -NR6R7-, (C2-6) alkene , and -CN, or X is selected from the group consisting of H, NH2, -N (R6) (CH2) s-aryl, N (R6) (CH2) s-heteroaryl, -N (R6) (CH2) m + 1-OH, and -N (CH3) 2, or X is -R18 -YZ; Y is selected from the group consisting of -N (R6) CH2CH2N (R7) -, -N (R6) (CH2) naryl, -OCH2CH2N (R6) -, -O-, -S-, -CH2S-, - (CH2 ) 2-3-N (R6) -, R8-divalent heteroaryl, structures (7) and (8) and Z is selected from the group consisting of H, alkyl, alkoxyalkyl, R8-aryl, R8-aryl (C1-6) alkyl-, R8-heteroaryl, R8-bicyclic alkyl-, aminoalkyl, alkylamino, NH2, -N (R6) (CH2) s-aryl, -N (R6) (CH2) s-heteroaryl, -N (R6) C ( O) OR17, alkylcycloheteroaryl, cycloheteroalkyl, cycloheteroalkylalkyl, alkoxycycloheteroalkyl, heteroaryl, -heteroarylR8-benzofused-, diphenylmethyl and R9-C (O) -; or when Y is like in structures (9); Z may also be -OH, R9-SO2-, R17-N (R11 (CH2) sC (O) -, R17-OC (O) -, R17-O (CH2) nC (O) -, (CH2) nC (O) -benzofused heteroaryl, (CH2) benzofused n-heteroaryl- or R17-N (R11) -C (S) -; or when Q is as in structure (10), Z may also be R17R11N-, phenylamino or pyridylamino; or Z and Y together are selected from the group consisting of structures (11) or one of their N-oxides, as shown in structures (12) and as shown in structures (13), their pharmaceutical compositions, and the use of said antagonists of the adenosine A2a receptor for the manufacture of a medicament for the treatment of heart attack or diseases of the central nervous system to a patient in need of such treatment.A kit comprising in separate containers in a single package, pharmaceutical compositions for use combined for the treatment of Parkinson's disease, where a container contains a pharmaceutical composition comprising one or more compounds of formula (1) in one or more vehicles acceptable for pharmaceutical use, and where, in separate containers, one or more pharmaceutical compositions comprise, each, one or more agents useful for the treatment of Parkinson's disease in one or more vehicles acceptable for pharmaceutical use. |
| priorityDate | 2001-11-30-04:00^^<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: 49.