Monthly Archives: June 2005

CCR5 antagonists useful for treating AIDS

Document Number: 20050143390

Abstract:

Compounds of the formula embedded image or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N;

    • R, R4-R7 and R13 are H or alkyl;
    • R1 is H, alkyl, fluoroalkyl, R9-arylalkyl, R9-heteroarylalkyl, alkyl-SO2—, cycloalkyl-SO2—, fluoroalkyl-SO2—, R9-aryl-SO2—, R9-heteroaryl-SO2—, N(R22)(R23)—SO2—, alkyl-C(O)—, cycloalkyl-C(O)—, fluoroalkyl-C(O)—, R9-aryl-C(O)—, NH-alkyl-C(O)— or R9-aryl-NH—C(O)—;
    • R2 is H and R3 is H, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, R9-aryl, R9-arylalkyl, R9-heteroaryl, or R9-heteroarylalkyl, and when X and Z are each CH, R3 is alkoxy, R9-aryloxy, R9-heteroaryloxy, alkylC(O)O—, alkylaminoC(O)O—, alkylC(O)NR13—, alkylOC(O)NR13— or alkylaminoC(O)NR13—;
    • or R2 and R3 together are ═O, ═NOR10, ═N—NR11R12 or ═CH-alkyl;
    • R8 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenymethyl, alpha-substituted benzyl or alpha-substituted heteroarylmethyl;
    • R9-R12 are as defined; are disclosed for the treatment of HIV, solid organ transplant rejection, graft v. host disease, inflammatory diseases, atopic dermatitis, asthma, allergies or multiple sclerosis, as well as pharmaceutical compositions and combinations with antiviral or anti-inflammatory agents.

Application Number: 11059785

Primary Class: 514252180

Sub-Classes: 544295000

Inventors: Michael Miller, Westfield, NJ, US

Attorney, Agent or Firm: SCHERING-PLOUGH CORPORATION;PATENT DEPARTMENT (K-6-1, 1990), 2000 GALLOPING HILL ROAD, KENILWORTH, NJ, 07033-0530, US

Provisional Application: US 60279938, 2001-03-29

Filing Date: 2005-02-17

Publication Date: 2005-06-30

PDF: 20050143390

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