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filingDate 2002-02-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_314b67bf53269592ef6568d132e59492
publicationDate 2004-11-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-037487-A1
titleOfInvention COMPOUNDS DERIVED FROM PYRIMIDINE, PROCESS TO PREPARE THEM, PHARMACEUTICAL COMPOSITION AND THE USE OF THEM IN THE MANUFACTURE OF MEDICINES THAT PRODUCE AN INHIBITING EFFECT OF THE CELL CYCLE (ANTI-PROLIFERATION CELL)
abstract Compounds derived from pyrimidine characterized in that it has the formula (1), where: ring A is a group of formula (2) or (3), where one or more of X1, X2, X3 and X4 are nitrogen and the others are CR5 where the values of R5 can be the same or different; R1 is halo, nitro, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, amino, carboxy, carbamoyl, mercapto, sulfamoyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C1-6 alkanoyl, N - (C1-6 alkyl) amino, N, N- (C1-6 alkyl) 2amino, C1-6 alkanoylamino, N- (C1-6 alkyl) carbamoyl, N, N- (C1-6 alkyl) 2carbamoyl, (alkyl C1-6) S (O) where a is between 1 and 2, N- (C1-6 alkyl) sulfamoyl or N, N- (C1-6 alkyl) 2sulfamoyl; where R1 can be optionally substituted on one carbon by one or more R6, R2 and R5 are independently selected from each other from hydrogen, halo, nitro, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, amino, carboxy, carbamoyl, mercapto, sulfamoyl, C1 alkyl -6, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C1-6 alkanoyl, C1-6 alkanoyloxy, N- (C1-6 alkyl) amino, N, N- (C1-6 alkyl) 2amino, C1-6 alkanoylamino, N- (C1-6 alkyl) carbamoyl, N, N- (C1-6 alkyl) 2carbamoyl, (C1-6 alkyl) S (O) where a is between 1 and 2, C1-6 alkoxycarbonyl , N- (C1-6 alkyl) sulfamoyl, N, N- (C1-6 alkyl) 2sulfamoyl, phenyl, heterocyclic group, phenylthio or (heterocyclic group) thio; where any R2 or R5 can be optionally substituted on a carbon by one or more R7; and where if said heterocyclic group contains a portion -NH- that nitrogen may be optionally substituted by a group selected from R8, n is between 1 and 2, where the values of R1 may be the same or different; R3 is halo, nitro, cyano, hydroxy, amino, carboxy, carbamoyl, mercapto, sulfamoyl, C2-6 alkenyl, or C2-6 alkynyl; p is 0-4; where the values of R3 can be the same or different; R4 is an A-E- group; where A is selected from C1-6 alkyl, phenyl, a heterocyclic group, C3-8 cycloalkyl, phenyl C1-6 alkyl, (heterocyclic group) C1-6 alkyl or C3-8 cycloalkyl C1-6 alkyl; where A can be optionally substituted on a carbon by one or more R9; and where if said heterocyclic group contains a portion -NH- that nitrogen may be optionally substituted by a group selected from R10; E is a direct link or -O-, -C (O) -, -OC (O) -, -C (O) O-, -N (Ra) C (O) -, -C (O) N ( Ra) -, -N (Ra) -, -S (O) a-, -SO2N (Ra) - or -N (Ra) SO2-; where Ra is hydrogen or C1-6 alkyl optionally substituted by one or more R11 is already 0-2, R9 is independently selected from oxo, halo, nitro, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, amino, carboxy, carbamoyl, mercapto, sulfamoyl , C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C1-6 alkanoyl, C1-6 alkanoyloxy, N- (C1-6 alkyl) amino, N, N- (C1-6 alkyl ) 2amino, C1-6 alkanoylamino, N- (C1-6 alkyl) carbamoyl, N, N- (C1-6 alkyl) 2carbamoyl, (C1-6 alkyl) S (O) where a is between 1 and 2, alkoxycarbonyl C1-6, C1-6 alkoxycarbonylamino, benzyloxycarbonylamino, N- (C1-6 alkyl) sulfamoyl and N, N- (C1-6 alkyl) 2sulfamoyl; where R9 can be optionally substituted on a carbon by one or more R12; q is 0-2; where the values of R4 can be the same or different; and where p + q L 5; R6, R7, R11 and R12 are independently selected from halo, nitro, cyano, hydroxy, trifluoromethoxy, trifluoromethyl, amino, carboxy, carbamoyl, mercapto, sulfamoyl, methyl, ethyl, methoxy, ethoxy, acetyl, acetoxy, methylamino, ethylamino, dimethylamino , diethylamino, N-methyl-N-ethyalmino, acetylamino, N-methylcarbamoyl, N-ethylcarbamoyl, N, N-dimethylcarbamoyl, N, N-diethylcarbamoyl, N-methyl-N-ethylcarbamoyl, methylthio, ethylthio, methyl sulfinyl, mesylsulfinyl , ethylsulfonyl, methoxycarbonyl, ethoxycarbonyl, N-methylsulfamoyl, N-ethylsulfamoyl, N, N-dimethylsulfamoyl, N, N-diethylsulfamoyl or N-methyl-N-ethylsulfamoyl; and R8 and R10 are independently selected from C1-4 alkyl, C1-4 alkanoyl, C1-4 alkylsulfonyl, C1-4 alkoxycarbonyl, carbamoyl N- (C1-4 alkyl) carbamoyl, N, N- (C1-4 alkyl) carbamoyl , benzyl, benzyloxycarbonyl, benzoyl and phenylsulfonyl, or a salt acceptable for pharmaceutical use or a live hydrolysable ester thereof. Also described are pharmaceutical compositions that comprise them, processes for their preparation and the use thereof in the manufacture of medicaments that produce an inhibitory effect of the cell cycle and are useful for the treatment of different types of cancers, fibroproliferative and differentiation disorders, psoriasis, arthritis, rheumatoid, Kaposi's sarcoma, hemangioma, acute and chronic kidney disease, atheroma, atherosclerosis, arterial restenosis, autoimmune diseases, acute and chronic inflammation, bone diseases and ocular diseases with proliferation of the retinal vessels.
priorityDate 2001-02-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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Total number of triples: 59.