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US 11,884,654 B2Granted
Substituted anilines as CCR(4) antagonists
AssigneeChemoCentryx, Inc.
InventorsTrevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. McMahon, Jay Powers, Sreenivas Punna, Ju Yang
Life of this patent
Estimating the term…
Abstract
Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
Claims15
A pharmaceutical composition comprising a compound of formula (Ic)
- or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient,
- wherein
- X and Y are each N;
- Z is CH;
- Q is CH or N;
- R1 is selected from hydrogen, C1-8 alkyl, C1-8 haloalkyl, and halogen;
- each R2 is a member selected from the group consisting of C1-8 alkyl, C1-8 haloalkyl, halogen and —CN;
- R4 is hydrogen or methyl;
- R6 is absent or is a member selected from the group consisting of H, —OH, C1-8 alkyl, C1-8 hydroxyalkyl, C1-4 alkoxy-C1-4 alkyl, —C(O)NRaRb, —CO2H, —C(O)ORa, —C(O)Ra, and —SO2Ra;
- R7 is absent or is selected from the group consisting of H, C1-8 alkyl and C1-8 haloalkyl;
- each Ra and Rb are independently selected from the group consisting of hydrogen, C1-8 alkyl, C1-8 hydroxyalkyl, C1-8 haloalkyl, and C1-8 alkoxy;
- and
- the subscript n is 1.
10 more elements
A method of assaying a small organic molecule for CCR(4) antagonistic activity, said method comprising
- (a) contacting the small organic molecule with cells expressing CCR(4) and a radioactive CCR(4) ligand to form a reaction mixture;
- (b) aspirating the reaction mixture onto a polyethyleneimine-treated GF/B glass filter;
- (c) measuring the amount radioactivity remaining on the GF/B glass filter,
- wherein said method comprises performing steps (a)-(c) with a positive control sample having a formula selected from the group consisting of formula (Ie):
- or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient, wherein
- the bond represented by in the ring comprising Y is a single bond or a double bond;
- R1 is a member selected from the group consisting of hydrogen, C1-8 alkyl, C1-8 haloalkyl, C1-8 hydroxyalkyl, C3-8 cycloalkyl, halogen, —CN, —SO2Me and —C(O)NH2;
- each R2 is a member selected from the group consisting of C1-8 alkyl, C1-8 haloalkyl, halogen, —CN and C1-8 alkoxy;
- R4 is a member selected from the group consisting of hydrogen, C1-8 alkyl, C1-8 haloalkyl and C1-8 hydroxyalkyl;
- the subscripts n is independently an integer from 0 to 3;
- Q is a member selected from the group consisting of C and N;
- Y and Z are independently selected from the group consisting of CH and N;
- R6 is selected from the group consisting of H, —OH, C1-8 alkyl, C1-8 hydroxyalkyl, C1-4 alkoxy-C1-4 alkyl, —C(O)NRaRb, C1-8 alkylene-C(O)NRaRb, —NH—C1-4 alkylene-C(O)NRaRb, —C(O)—C1-4 alkylene-NRaRb, —CO2H, C1-8 alkylene-CO2H, —N(Ra)C(O)NRaRb, C1-8 alkylene N(Ra)C(O)NRaRb, —NRaRb, C1-8 alkylene-NRaRb, C1-8 alkoxy, —C(O)ORa, C1-8 alkylene-C(O)ORa, —CN, —C(O)Ra, —SO2Ra and —N(Ra)C(O)Rb;
- wherein
- each Ra and Rb are independently selected from the group consisting of hydrogen, C1-8 alkyl, C1-8 hydroxyalkyl, C1-8 haloalkyl, and C1-8 alkoxy;
- and
- R7 is absent or is selected from the group consisting of H, C1-8 alkyl and C1-8 haloalkyl.
14 more elements
Dependencies are inferred from the claim text.