http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-061647-A1
Outgoing Links
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| filingDate | 2007-06-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2008-09-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-061647-A1 |
| titleOfInvention | INHIBITORS OF CXCR2 AND ITS PHARMACEUTICAL COMPOSITIONS |
| abstract | Due to their properties as chemokine receptor inhibitors, especially as CXCR2 inhibitors, the compounds of formula 1 and pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine-mediated diseases. Claim 1: A compound of the formula (1) wherein X is -CR3 = CR4-, -CR5 = N-, -N = CR6-, -NR7- or -S-; R3, R4, R5 and R6 are, independently of each other, hydrogen, F, CI, Br, I, C1-6 alkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 , 12 or 13 hydrogen atoms may be substituted with fluorine atoms, C3-6 cycloalkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or 11 hydrogen atoms may be substituted with atoms of fluorine, C4-8 cycloalkylalkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 or 15 hydrogen atoms may be substituted with fluorine atoms, alkoxy C1-6, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 or 13 hydrogen atoms can be substituted with fluorine atoms, C3-6 cycloalkoxy, where 1, 2 , 3, 4, 5, 6, 7, 8, 9, 10 or 11 hydrogen atoms may be substituted with fluorine atoms, C4-8 cycloalkylalkoxy, where 1, 2, 3, 4, 5, 6, 7, 8 , 9, 10, 11, 12, 13, 14 or 15 hydrogen atoms may be substituted with fluorine atoms, -S-C1-6 alkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 or 13 hydrogen atoms may be substituted two with fluorine atoms, OH, CN, NO2, NR27R28, C (O) R29, C (O) NR30R31, S (O) oR32, S (O) pNR33R34, aryl, heteroaryl, arylalkyl with C1-4alkyl or heteroarylalkyl C1-4; R27 is hydrogen or C1-4 alkyl; R28 is hydrogen, C1-4 alkyl, aryl, C (O) H, C (O) C1-4 alkyl or C (O) aryl; R29 is hydrogen, OH, C1-4 alkyl, C1-4 alkoxy or aryl; R30, R31, R33 and R34 are, independently of one another, hydrogen, C1-4 alkyl or aryl; R32 is OH, C1-4 alkyl, C1-4 alkoxy or aryl; o and p are, independently of one another, 1 or 2; R7 is hydrogen, C1-4 alkyl or C (O) R35; R35 is hydrogen, C1-4 alkyl or aryl; Y1, Y2, Y3 and Y4 are, independently of each other, -CR8- or nitrogen, with the proviso that at least two of Y1, Y2, Y3 and Y4 are defined as -CR8-; R8 is hydrogen, F, CI, Br, I, C1-6 alkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 or 13 hydrogen atoms may be substituted with fluorine atoms, C3-6 cycloalkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or 11 hydrogen atoms may be substituted with fluorine atoms, C4-8 cycloalkylalkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 or 15 hydrogen atoms may be substituted with fluorine atoms, C1-6 alkoxy, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 or 13 hydrogen atoms may be substituted with fluorine atoms, C3-6 cycloalkoxy, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or 11 hydrogen atoms may be substituted with fluorine atoms, C4-8 cycloalkylalkoxy, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 or 15 hydrogen atoms may be substituted with fluorine atoms, -S-C1-6 alkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 or 13 atoms of hydrogen can be substituted with fluorine atoms, OH, CN, NO2, NR36R37 , C (O) R38, C (O) NR39R40, S (O) qR41, S (O) rNR42R43, aryl, heteroaryl, arylalkyl with C1-4 alkyl or heteroarylalkyl with C1-4 alkyl; R36 is hydrogen or C1-4 alkyl; R37 is hydrogen, C1-4 alkyl, aryl, C (O) H, C (O) C1-4 alkyl or C (O) aryl; R38 is hydrogen, OH, C1-4 alkyl, C1-4 alkoxy or aryl; R39, R40, R42 and R43 are, independently of one another, hydrogen, C1-4 alkyl or aryl; R41 is OH, C1-4 alkyl, C1-4 alkoxy or aryl; q and r are, independently of each other, 1 or 2; Z is -C (O) -, -S (O) - or -S (O) 2-; A is C3-8 cycloalkyl, heterocyclyl having 5, 6, 7 or 8 atoms, phenyl or heteroaryl having 5 or 6 atoms; wherein said cycloalkyl, heterocyclyl, phenyl or heteroaryl may be fused to a C3-8 cycloalkyl radical, a heterocyclyl radical having 5, 6, 7 or 8 atoms, a phenyl radical or a heteroaryl radical having 5 or 6 atoms, and where said cycloalkyl, heterocyclyl, phenyl or heteroaryl and the cycloalkyl radical, heterocyclyl radical, phenyl radical or heteroaryl radical optionally fused is unsubstituted or substituted with 1, 2, 3, 4 or 5 radicals selected from the group consisting of F, CI, Br, I, OH, CN, NO2, SF5, C1-6 alkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 or 13 hydrogen atoms may be substituted with fluorine atoms, C3-6 cycloalkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or 11 hydrogen atoms may be substituted with fluorine atoms, C4-8 cycloalkylalkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 or 15 hydrogen atoms may be substituted with fluorine atoms, C1-6 alkoxy, where 1, 2, 3, Four. Five , 6, 7, 8, 9, 10, 11, 12 or 13 hydrogen atoms may be substituted with fluorine atoms, C3-6 cycloalkoxy, where 1, 2, 3, 4, 5, 6, 7, 8, 9 , 10 or 11 hydrogen atoms may be substituted with fluorine atoms, C4-8 cycloalkylalkoxy, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 or 15 hydrogen atoms may be substituted with fluorine atoms or -S-C1-6 alkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 or 13 hydrogen atoms may be substituted with fluorine atoms; B is a linear linker consisting of 3, 4 or 5 carbon atoms, where 1 or 2 carbon atoms can be replaced by a member of a group containing heteroatoms consisting of O, NR19 or S (O) and and said linker it may contain 0, 1 or 2 double or triple bonds between carbon atoms within the linker, with the proviso that 2 of said heteroatom-containing groups are separated by at least 2 carbon atoms, that the heteroatom-containing groups are not adjacent to a double or triple bond within the linker or to a non-aromatic double bond that may be part of A, that the double or triple bonds are not accumulated, and that, if A is connected to the linker by a nitrogen atom that forms part of A, the linker atom that is connected to A is a carbon atom; and where the saturated carbon atoms of the linker, which are not adjacent to the groups containing heteroatoms, which are not adjacent to double or triple bonds within the linker or that are not adjacent to a heteroatom, which may be part of A, may be substituted, independently of each other, with hydrogen, F, OH, C1-6 alkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 or 13 hydrogen atoms may be substituted with fluorine atoms, C3-6 cycloalkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or 11 hydrogen atoms may be substituted with fluorine atoms, C4-8 cycloalkylalkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 or 15 hydrogen atoms may be substituted with fluorine atoms, C1-6 alkoxy, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 or 13 hydrogen atoms may be substituted with fluorine atoms; C3-6 cycloalkoxy, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or 11 hydrogen atoms may be substituted with C4-8 fluorine or cycloalkylalkoxy atoms, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 or 15 hydrogen atoms may be substituted with fluorine atoms; and where the saturated carbon atoms of the linker, which are adjacent to the groups containing heteroatoms, which are adjacent to the double or triple bonds of the linker, or that are adjacent to a heteroatom, which may be part of A, or atoms of carbon that are part of a double bond, can be substituted, independently of each other, with hydrogen, F, C1-6 alkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 or 13 hydrogen atoms may be substituted with fluorine atoms, C3-6 cycloalkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or 11 hydrogen atoms may be substituted with atoms of C4-8 fluorine or cycloalkylalkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 or 15 hydrogen atoms may be substituted with fluorine atoms; R19 is hydrogen, C1-6 alkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 or 13 hydrogen atoms may be substituted with fluorine atoms, C3-6 cycloalkyl , where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or 11 hydrogen atoms may be substituted with fluorine atoms, C4-8 cycloalkylalkyl, where 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 or 15 hydrogen atoms be substituted with fluorine atoms; C (O) R44 or C (O) NR45R46; R44, R45 and R46 are, independently of each other, hydrogen, C1-4 alkyl, where 1, 2, 3, 4, 5, 6 or 7 hydrogen atoms may be substituted with C3-4 fluorine or cycloalkyl atoms, where 1 , 2, 3, 4, 5 or 6 hydrogen atoms may be substituted with fluorine atoms; y is 0, 1 or 2; R1 is C1-6 alkyl; which may be unsubstituted or substituted with 1, 2, 3, 4 or 5 radicals selected from the group consisting of F, CI, Br, I and -Om- (CH2) n-R26; m is 0 or 1; n is 0, 1, 2 or 3; R26 is hydrogen, phenyl, heteroaryl having 5 or 6 atoms, C3-6 cycloalkyl or heterocyclyl having 3, 4, 5, 6, 7 or 8 atoms, where the phenyl, heteroaryl, cycloalkyl or heterocyclyl is unsubstituted or substituted with 1, 2 or 3 radicals selected from F, CI, Br or I; and R2 is C1-6 alkyl, phenyl, heteroaryl having 5 or 6 atoms, C3-8 cycloalkyl or heterocyclyl having 3, 4, 5, 6, 7 or 8 atoms; where the alkyl is unsubstituted or substituted with 1, 2, 3, 4 or 5 radicals selected from the group consisting of F, CI, Br, I and -Om- (CH2) n-R26; m is 0 or 1; n is 0, 1, 2 or 3; R26 is hydrogen, phenyl, heteroaryl having 5 or 6 atoms, C3-6 cycloalkyl or heterocyclyl having 3, 4, 5, 6, 7 or 8 atoms, where the phenyl, heteroaryl, cycloalkyl or heterocyclyl is unsubstituted or substituted with 1, 2 or 3 radicals selected from F, CI, Br or I; and where the phenyl, heteroaryl having 5 or 6 atoms, C3-8 cycloalkyl or heterocyclyl having 3, 4, 5, 6, 7 or 8 atoms is unsubstituted or substituted with 1, 2, 3, 4 or 5 radicals selected |
| priorityDate | 2006-06-28-04:00^^<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: 82.