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filingDate 2003-10-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2005-07-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-043055-A1
titleOfInvention DERIVATIVES OF 1- (4-BENZIL-PIPERAZIN-1-IL) -3- FENIL-PROPENONA
abstract Compound that is a CCR-1 antagonist, and that finds use pharmaceutically for the treatment of diseases and conditions where CCR-1 is involved, for example inflammatory diseases. Claim 1: A compound of the formula (1), or a pharmaceutically acceptable salt or ester thereof, wherein R, is -X-R10, -X- (R10) 2 or -NR11R12; wherein X is a linker comprising an atom or a chain comprising 2, 3 or 4 atoms selected from N, C, O or S, and where, when this linker comprises two or more carbon atoms, the linker It can comprise one or more links C = C or C ::: C; wherein, any of these atoms has up to two optional substituents selected from hydrogen, oxo, cyano, halo, nitro or optionally substituted oxyl, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino sulfur; R10 is a substituent independently selected from the group consisting of hydrogen, cyano, halo, nitro or optionally substituted oxyl, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino, cycloalkyl, heterocycloalkyl, aryl, heteroaryl; R11 and R12 each represent a lower alkyl group connected to each other, such that R1 is an optionally substituted heterocycloalkyl or heteroaryl group; R2 and R7 represent one or more substituents attached to the phenyl ring selected from the group consisting of hydrogen, cyano, halogen, nitro or oxyl optionally substituted, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino, sulfur, cycloalkyl, heterocycloalkyl , aryl, heteroaryl or a substituent that forms a bicyclic ring system of which the phenyl ring with which it is attached is part of the bicyclo, for example butadiene-forming naphthyl, or heterobutadiene, quinoxalinyl or isoquinolinyl-forming quinolinyl; R3 and R4 are independently selected from the group consisting of hydrogen, cyano, halogen, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, cycloalkyl, heterocycloalkyl, aryl; R5 and R6 are selected from the group consisting of hydrogen, cyano, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, cycloalkyl, heterocycloalkyl, aryl; optional substituents on X are one or more substituents independently selected from the group consisting of hydrogen, oxo, cyano, halo, nitro or optionally substituted oxyl, lower alkyl, lower alkenyl, lower alkynyl, amino, sulfur, sulfinyl, sulfonyl; wherein the optionally substituted substituents are optionally substituted one or more times by a substituent independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro, oxyl, lower alkyl, lower alkenyl, lower alkynyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; optional substituents on R10 are one or more substituents independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro or optionally substituted oxyl, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; wherein the optionally substituted substituents are optionally substituted one or more times by a substituent independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro or optionally substituted oxyl, lower alkyl, lower alkenyl, lower alkynyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; wherein the optionally substituted substituents are optionally substituted one or more times by a substituent independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro or optionally substituted oxyl, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; wherein the optionally substituted substituents are optionally substituted one or more times by a substituent independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro, oxyl, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; the optional substituents on R11 and R12 are one or more substituents independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro, optionally substituted oxyl, lower alkyl, lower alkenyl, lower alkynyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; the optional substituents on R2 and R7 are one or more substituents independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro, optionally substituted oxyl, lower alkyl, lower alkenyl, lower alkynyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; wherein the optionally substituted substituents are optionally substituted one or more times by a substituent independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro or optionally substituted oxyl, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; wherein the optionally substituted substituents are optionally substituted one or more times by a substituent independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro or optionally substituted oxyl, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; wherein the optionally substituted substituents are optionally substituted one or more times by a substituent independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro or optionally substituted oxyl, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; wherein the optionally substituted substituents are optionally substituted one or more times by a substituent independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro, oxyl, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; the optional substituents on R3 and R4 are one or more substituents independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro or oxyl optionally substituted, lower alkyl, lower alkenyl, lower alkynyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; wherein the optionally substituted substituents are optionally substituted one or more times by a substituent independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro or optionally substituted oxyl, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; wherein the optionally substituted substituents are optionally substituted one or more times by a substituent independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro or oxyl, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; the optional substituents on R5 and R6 are one or more substituents independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro or oxyl optionally substituted, lower alkyl, lower alkenyl, lower alkynyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl, imino, oxime; wherein the optionally substituted substituents are optionally substituted one or more times by a substituent independently selected from the group consisting of hydrogen, oxo, hydroxyl, cyano, halogen, nitro or optionally substituted oxyl, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; wherein the optionally substituted substituents are optionally substituted one or more times by a substituent independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro or optionally substituted oxyl, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; wherein the optionally substituted substituents are optionally substituted one or more times by a substituent independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro or optionally substituted oxyl, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl; wherein the optionally substituted substituents are optionally substituted one or more times by a substituent independently selected from the group consisting of hydrogen, oxo, cyano, halogen, nitro or oxyl, lower alkyl, lower alkenyl, lower alkynyl, carbonyl, amino, sulfur, cycloalkyl, heterocycloalkyl, aryl.
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Total number of triples: 48.