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filingDate 2006-06-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_feb29b1d69ea0d4b4344c137083a4bf4
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publicationDate 2007-07-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-054770-A1
titleOfInvention OXOINDOLES AS INHIBITORS OF KINASES, A METHOD FOR THEIR DEVELOPMENT, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THEIR PREPARATION, A GAME OF ELEMENTS THAT USE THEM AND THEIR USE IN THE MANUFACTURE OF MEDICINES FOR THE PROCESSING OF MEDIAIN QUASINES BY MEK.
abstract Oxindoles of the formula (1), its use as activators or inhibitors of protein kinases, a method for its preparation, its use in the preparation of a medicament for the treatment of diseases and its use in the elaboration of a pharmaceutical composition. Claim 1: A compound of the formula (1) wherein X is Ar or Het; R2 is H, A, Ar, (CH2) mCON (R8) 2, (CH2) mCONHAr, S (O) mA, S (O) mAr, NHCOA, NHCOAr, NHSO2A, NHSO2Ar, SO2N (R8) 2, N ( CH2) nC (CH3) 2 (CH2) nN (R8) 2, (CH2) nN (R8) SOmA, (CH2) nN (R8) SOmAr, (CH2) nSOmA, (CH2) nSOmAr or (CH2) nSOmN (R8 )TO; R3, R4, R5, R6, R7 are, independently of each other, H, A, Ar, OR8, SR8, OAr, SAr, N (R8) 2, NHAr, NAr2, Hal, NO2, CN, COR8, COAr , S (O) mA, S (O) mAr, NHCOA, NHCOAr, NHSO2A, NHSO2Ar, SO2N (R8) 2, O (CH2) nN (R8) 2, O (CH2) nNHR8, O (CH2) n-morpholine , O (CH2) n-piperazine, O (CH2) n-pyrrolidine, O (CH2) n-piperidine, O-piperidine, O (CH2) n-oxopiperazine, O (CH2) n-oxomorpholine, O (CH2) n -oxopyrrolidine, O (CH2) nC (CH3) 2 (CH2) nN (R8) 2, N (CH2) nC (CH3) 2 (CH2) nN (R8) 2, O (CH2) nN (R8) SOmA, O (CH2) nN (R8) SOmAr, O (CH2) nN (R8) SOmN (R8) 2A, (CH2) nN (R8) SOmA, (CH2) nN (R8) SOmAr, (CH2) nN (R8) SOmN ( R8) 2A, O (CH2) nSOmA, O (CH2) nSOmAr, O (CH2) nSOmN (R8) A, (CH2) nSOmA, (CH2) nSOmAr or (CH2) nSOmN (R8) A, R8 is H, A or A-Ar; A is a linear or branched alkyl or cycloalkyl that is optionally substituted by Hal, Ar is aryl; Het is heteroaryl; Hal is Cl, Br, I or F; n, p are, independently of each other, 0-5; m is 0-2; with the proviso that one of the residues R2, R3, R4, R5, R6 or R7 is different from H and that the compound 3- (1-amino-2-phenyl-ethylidene) -1-methyl-1,3 is excluded -dihydro-indole-2-one, and the salts, derivatives, prodrugs, solvates and stereoisomers acceptable for physiological use thereof, including all the proportions of mixtures thereof. Claim 12: A method of making a compound according to formula (1), characterized in that, a) an aromatic or heteroaromatic nitrile is reacted according to formula (2) Ns-X-R1-R7 wherein R1 , R7 and X are as defined in claim 1, with a straight or branched chain alcohol according to formula (3) HO-R9 wherein R9 is (CH2) q and q is 1-10; and that the product according to formula (4) wherein R1, R7, R9 and X are as defined in claim 1, is then reacted with a compound according to formula (5), wherein R2, R3, R4, R5 and R6 are as defined in claim 1, or b) a compound of formula (1) is isolated or treated with an acid or a base, to obtain the salt thereof. Claim 27: A set (set of elements), consisting of separate packages of: a) an amount effective for therapeutic use of one or more compounds according to one of claims 1 to 11 and b) an amount effective for therapeutic use of one or more additional pharmaceutically active agents other than the compounds according to one of claims 1 to 11. Claim 28: A process of making a pharmaceutical composition, characterized in that one or more compounds are converted according to one of the claims 1 to 11 and one or more compounds selected from the group consisting of excipients, auxiliaries, adjuvants, diluents, vehicles and pharmaceutically active agents, solids, liquids or semi-liquids, other than the compounds according to one of claims 1 to 11, in a proper dosage form.
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Total number of triples: 59.