http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-076363-A1

Outgoing Links

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filingDate 2010-04-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2011-06-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-076363-A1
titleOfInvention ARILSULFONAMIDE CCR3 ANTAGONISTS
abstract Pharmaceutical composition and uses for the treatment, prevention or improvement of one or more symptoms of a disorder, disease or condition mediated by CCR3. Claim 1: A compound of the formula (1) or an enantiomer, a mixture of enantiomers, a mixture of two or more diastereomers, a tautomer or a mixture of two or more tautomers thereof, or a salt, solvate, hydrate or prodrug pharmaceutically acceptable thereof; wherein: R1, R2, R3, R4, R5 and R6 are each independently (a) hydrogen, halo, cyano, nitro or guanidine; (b) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl or heterocyclyl; or (c) -C (O) R1a, -C (O) OR1a, -C (O) NR1bR1c, -C (NR1a) NR1bR1c, -OR1a, -OC (O) R1a, -OC (O) OR1a, - OC (O) NR1bR1c, -OC (= NR1a) NR1bR1c, -OS (O) R1a, -OS (O) 2R1a, -OS (O) NR1bR1c, -OS (O) 2NR1bR1c, -NR1bR1c, -NR1aC (O) R1d, -NR1aC (O) OR1d, -NR1aC (O) NR1bR1c, -NR1aC (= NR1d) NR1bR1c, -NR1aS (O) R1d, -NR1aS (O) 2R1d, -NR1aS (O) NR1bR1c, -NN) 2NR1bR1c, -SR1a, -S (O) R1a, -S (O) 2R1a, -S (O) NR1bR1c or -S (O) 2NR1bR1c; R7 is (a) halo, cyano, nitro, oxo or guanidine; (b) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl or heterocyclyl; or (c) -C (O) R1a, -C (O) OR1a, -C (O) NR1bR1c, -C (NR1a) NR1bR1c, -OR1a, -OC (O) R1a, -OC (O) OR1a, - OC (O) NR1bR1c, -OC (= NR1a) NR1bR1c, -OS (O) R1a, -OS (O) 2R1a, -OS (O) NR1bR1c, -OS (O) 2NR1bR1c, -NR1bR1c, -NR1aC (O) R1d, -NR1aC (O) OR1d, -NR1aC (O) NR1bR1c, -NR1aC (= NR1d) NR1bR1c, -NR1aS (O) R1d, -NR1aS (O) 2R1d, -NR1aS (O) NR1bR1c, -NN) 2NR1bR1c, -SR1a, -S (O) R1a, -S (O) 2R1a, -S (O) NR1bR1c or -S (O) 2NR1bR1c; X is O or S; RYa is -C (O) R1a, -C (O) OR1a, -C (O) NR1bR1c, -C (S) NR1bR1c, -C (S) NR1aC (O) NR1bR1c, -C (NR1a) NR1bR1c, -C (NNO2) NR1bR1c, -S (O) R1a, -S (O) 2R1a, -S (O) NR1bR1c or -S (O) 2NR1bR1c; provided that RYa is not -C (O) O-t-butyl; m is an integer from 0 to 3; n is an integer from 1 to 3; p is an integer from 0 to 4; and each R1a, R1b, R1c and R1d is independently hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-14 aryl, heteroaryl or heterocyclyl; or each pair of R1b and R1c, together with the N atom to which they are linked, independently form heteroaryl or heterocyclyl; provided that the compound is not 4- (2- (3,5-dimethylphenoxy) -5-nitrophenylsulfonyl) piperazin-1-carbaldehyde; wherein each alkyl, alkenyl, alkynyl, cycloalkyl, aryl, aralkyl, heterocyclyl and heteroaryl optionally is substituted with one or more groups selected, independently, from (a) cyano, halo and nitro; (b) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl and heterocyclyl; wherein each is optionally substituted with one or more, in one embodiment, one, two, three or four substituents Q; and (c) -C (O) Ra, -C (O) ORa, -C (O) NRbRc, -C (NRa) NRbRc, -ORa, -OC (O) Ra, -OC (O) ORa, - OC (O) NRbRc, -OC (= NRa) NRbRc, -OS (O) Ra, -OS (O) 2Ra, -OS (O) NRbRc, -OS (O) 2NRbRc, -NRbRc, -NRaC (O) Rd, -NRaC (O) ORd, -NRaC (O) NRbRc, -NRaC (= NRd) NRbRc, -NRaS (O) Rd, -NRaS (O) 2Rd, -NRaS (O) NRbRc, -NRaS (O) 2NRbRc, -SRa, -S (O) Ra, -S (O) 2Ra, -S (O) NRbRc or -S (O) 2NRbRc; wherein each Ra, Rb, Rc and Rd is, independently, (i) hydrogen; (ii) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl or heterocyclyl, wherein each is optionally substituted with one or more , in one embodiment, one, two, three or four substituents Q; or (iii) Rb and Rc, together with the N atom to which they are attached, form heterocyclyl, optionally substituted with one or more, in one embodiment, one, two, three or four substituents Q; wherein each Q is independently selected from the group consisting of (a) cyano, halo and nitro; (b) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl and heterocyclyl; and (c) -C (O) Re, -C (O) ORe, -C (O) NRfRg, -C (NRe) NRfRg, -ORe, -OC (O) Re, -OC (O) ORe, - OC (O) NRfRg, -OC (= NRe) NRfRg, -OS (O) Re, -OS (O) 2Re, -OS (O) NRfRg, -OS (O) 2NRfRg, -NRfRg, -NReC (O) Rh, -NReC (O) ORh, -NReC (O) NRfRg, -NReC (= NRh) NRfRg, -NReS (O) Rh, -NReS (O) 2Rh, -NReS (O) NRfRg, -NReS (O) 2NRfRg, -SRe, S (O) Re, -S (O) 2Re, -S (O) NRfRg or -S (O) 2NRfRg; wherein each Re, Rf, Rg and Rh is, independently, (i) hydrogen; (ii) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl or heterocyclyl; or (iii) Rf and Rg, together with the N atom to which they are attached, form heterocyclyl.
priorityDate 2009-04-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

Incoming Links

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Total number of triples: 51.