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filingDate 2001-09-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2004-05-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-035205-A1
titleOfInvention USEFUL COMPOUNDS IN THE TREATMENT OF INFLAMMATORY DISEASES, PROCESS FOR PREPARATION, INTERMEDIARIES AND PHARMACEUTICAL COMPOSITIONS
abstract Compounds of the formula (1) wherein: R 1 represents C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, (C 2-6 alkynyl) -Y1-, aryl-Y1-, heteroaryl-Y1-, aryl- ( O) t-aryl-Y1-, aryl- (O) t-heteroaryl-Y1-, heteroaryl- (O) t-aryl-Y1-, heteroaryl- (O) t-heteroaryl-Y1-, (C2-6 alkenyl ) -Y1-, aryl-O-Y1-, heteroaryl-O-Y1-, (C1-6 alkyl) -SO2-Y1-, M-Y1-, J2-Y1-, -CN or (C3-8 cycloalkyl) -Y1- or (C3-8 cycloalkenyl) -Y1-, wherein cycloalkyl or cycloalkenyl may be optionally substituted by one or more hydroxyl or C1-6 alkyl groups; R2 represents hydrogen or C1-6 alkyl; X represents ethylene or a group of the formula CReRf wherein Re and Rf independently represent hydrogen or C1-4 alkyl or Re and Rf can together with the C atom to which they are attached, form a C3-8 cycloalkyl group; R3 and R4 independently represent hydrogen or C1-4 alkyl; Z represents a bond, CO, SO2, CR9R6 (CH2) n, (CH2) n, (CH2) nCR9R6, CHR6 (CH2) nO, CHR6 (CH2) nS, CHR6 (CH2) nOCO, CHR6 (CH2) nCO, COCHR6 (CH2) not SO2CHR6 (CH2) n; R5 represents C1-6 alkyl, C2-6 alkenyl, aryl, heteroaryl, aryl- (C2-6 alkenyl) or a group of formula -Y2-J1; R6 represents hydrogen, C1-4 alkyl, CONR7R8 or COOC- (C1-6 alkyl); a and b represent 1 or 2, such that a + b represents 2 or 3; n represents an integer from 0 to 4; J1 and J2 independently represent a portion of the formula (2) wherein X1 represents oxygen, NR13 or sulfur; X2 represents CH2, oxygen, NR10 or sulfur; m1 represents an integer from 1 to 3; and m2 represents an integer from 1 to 3, with the condition that m1 + m2 is in the range of 3 to 5, also with the condition that when X1 and X2 represents oxygen, NR13, NR10 or sulfur, m1 and m2 they must not be equal to less than 2, wherein the portion of formula (2) is optionally substituted with one or more -Y3-aryl, -Y3-heteroaryl, -Y3-CO-aryl, -CO (C3-8 cycloalkyl) , -Y3-CO-heteroaryl, C1-6 alkyl, -Y3-COO (C1-6 alkyl), -Y3-CO (C1-6 alkyl), -Y3-W-, -Y3-CO-W, -Y3 -NR11R12, -Y3-CONR11R12, hydroxyl, oxo, -Y3-SO2NR11R12, -Y3-SO2 (C1-6 alkyl), -Y3-SO2aryl, -Y3-SO2heteroaryl, -Y3-NR14 (C1-6 alkyl), - Y3-NR14SO2 (C1-6 alkyl), -Y3-NR14CONR11R12, -Y3-NR14COOR15, or -Y3-OCONR11R12, and is optionally fused to an aryl or monocyclic heteroaryl ring; R7, R8, R9, R10, R13, R14 and R15 independently represent hydrogen or C1-6 alkyl; R11 and R12 independently represent hydrogen or C1-6 alkyl, or R11 and R12 together with the nitrogen atom to which they are attached can form a morpholine, piperidine or pyrrolidine ring; M represents a C3-8 cycloalkyl or C3-8 cycloalkenyl group fused to a monocyclic aryl or monocyclic heteroaryl group; W represents a 5-7 membered ring, non-aromatic, saturated or unsaturated, containing between 1 and 3 heteroatoms selected from nitrogen, oxygen or sulfur, optionally substituted with one or more C1-6 alkyl, halogen or hydroxyl groups; t represents 0 or 1; Y1, Y2 and Y3 independently represent a bond or a group of the formula - (CH2) pCRcRd (CH2) q- where Rc and Rd independently represent hydrogen or C1-4 alkyl, or Rc and Rd can, together with the atom of C to which they are attached, form a C3-8 cycloalkyl group, and p and q independently represent an integer from 0 to 5, where p + q is an integer from 0 to 5; and the salts and solvates thereof. Processes for its preparation, intermediates and pharmaceutical compositions containing them are also described. These compounds are useful in the treatment of inflammatory diseases.
priorityDate 2000-09-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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