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US 7,803,951 B2Granted
Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
AssigneeMerck Sharp & Dohme Corp.
InventorsRui Liang, Emma R. Parmee
Life of this patent
Estimating the term…
Abstract
Substituted aryl and heteroaryl derivatives are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
Claims19
A compound represented by formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- ring A is selected from the group consisting of:
- 6-10 membered aryl and 5-10 membered heteroaryl, said heteroaryl containing from 1-4 heteroatoms, 0-2 of which are O or S atoms, and 0-4 of which are N;
- Y is present or absent, and when present, represents O, S, NH or CH2;
- X is present or absent, and when present, represents O or CH2;
- each R1 is H or is selected from the group consisting of:
- (a) halo, OH, CO2R4, SOpR5, CN, NO2 C(O)NR6R7 or NR6R7;
- (b) C1-10alkyl, C(O)C1-6alkyl or OC1-6alkyl, the alkyl portions being optionally substituted with:
- (1) 1-5 halo groups, up to perhalo, and 1-2 groups selected from OH, CO2R4, SOpR5, CN, NO2 C(O)NR6R7, NR6R7 and phenyl optionally substituted with 1-3 halo groups and 1-2 groups selected from:
- OH, C1-3alkyl, haloC1-3alkyl, CN, OC1-3alkyl and OhaloC1-3alkyl;
- (c) a 6-10 membered aryl or aryloxy group, said groups being optionally substituted with 1-3 halo groups and 1-2 groups selected from:
- OH, C1-3alkyl, haloC1-3alkyl, CN, OC1-3alkyl and OhaloC1-3alkyl;
- R2 is C1-10alkyl or aryl optionally substituted with 1-3 groups selected from (a), (b) and (c) above;
- R3 represents CH2CH2CO2R4, CH2CH(OH)CO2R4, CH2CF2CO2R4 or 5-tetrazolyl;
- R4 is H or C1-6alkyl, and
- R5 represents a member selected from the group consisting of:
- C1-10alkyl, Aryl or Ar—C1-10alkyl, said C1-10alkyl, Aryl and Ar—C1-10alkyl being optionally substituted with 1-3 halo groups;
- R6 and R7 each independently represent H or C1-3alkyl,
- R8 is selected from the group consisting of:
- H, OH, C1-3alkyl, haloC1-3alkyl, CN, OC1-3alkyl and OhaloC1-3alkyl, and
- p is 0, 1 or 2.
18 more elements
Dependencies are inferred from the claim text.