Back to results
US 2010/0075987 A1Published application
Acyl bipiperidinyl compounds, compositions containing such compounds and methods of treatment
AssigneeMerck Sharp & Dohme Corp.
InventorsHarold B. Wood, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang, Ralph T. Mosley
Life of this patent
Estimating the term…
Abstract
Bipiperidyl compounds of the formula: (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
Claims21
1-35. (canceled)
A compound represented by formula I
- or a pharmaceutically acceptable salt thereof wherein:
- R1 represents a 6-10 membered Aryl group or a 5-10 membered Heteroaryl group containing one or two rings, at least one nitrogen atom, 0-2 additional nitrogen atoms, and 0-1 oxygen or sulfur atom, said Aryl or Heteroaryl group being optionally substituted with 1-3 halo groups and 1-2 members selected from the group consisting of:
- (1) CN or OH;
- (2) C1-6alkyl, OC1-6alkyl or C3-6cycloalkyl, said members being optionally substituted with 1-3 halo groups and 1-2 members selected from the group consisting of:
- i) S(O)xC1-3alkyl, wherein x is 0, 1 or 2 and the alkyl portion is optionally substituted with 1-3 halo atoms;
- ii) a 5-10 membered Heteroaryl moiety optionally substituted with 1-3 halo atoms or C1-3alkyl groups;
- iii) C1-3alkoxy or haloC1-3alkoxy;
- iv) CN;
- v) NHz, NHC1-3alkyl and N(C1-3alkyl)2 the alkyl portions being optionally substituted with 1-3 halo groups;
- vi) OH;
- vii) C(O)C1-6alkyl the alkyl portion being optionally substituted with 1-3 halo atoms;
- viii) phenyl optionally substituted with 1-2 halo atoms or C1-3alkyl groups;
- ix) C(O)NRdRe or NRdC(O)Re, wherein Rd is selected from H and C1-3alkyl and Re is selected from H, C1-6alkyl, C3-6cycloalkyl, a 5-6 membered Heteroaryl group and phenyl;
- x) C(O)2Re, wherein Re is as defined above;
- xi) Heteroaryl optionally substituted with 1-2 halo or C1-3alkyl groups;
- (3) S(O)xC1-6alkyl, and SO2NRdRe wherein the C1-6alkyl group is optionally substituted with 1-3 halo groups and x, Rd and Re are as defined above;
- (4) NH2, NH(C1-6alkyl) or N(C1-6alkyl)2, wherein the alkyl portions are optionally substituted with 1-3 halo groups and 1 group selected from i) through xi) above;
- (5) C(O)NRdRe or NRdC(O)Re wherein Rd and Re are as defined above;
- (6) C(O)C1-6alkyl optionally substituted with 1-3 halo atoms;
- (7) CO2Re, wherein Re is as defined above;
- (8) Phenyl, a 5-10 membered Heteroaryl or a 5-10 membered Heterocyclic moiety, each being optionally substituted with 1-3 halo atoms and 1-2 C1-3 alkyl groups;
- and
- R2 is selected from the group consisting of C1-8alkyl, C3-6cycloalkyl, OC1-8alkyl and O-Phenyl, the phenyl portion of which being optionally substituted with 1-3 halo groups and 0-1 C1-3alkyl, haloalkyl, alkoxy or haloalkoxy groups, and each of said C1-8alkyl, C3-6cycloalkyl and OC1-6alkyl being optionally substituted with 1-3 halo groups, and 0-1 members selected from the group consisting of OH, oxo, CN, OC1-6alkyl, haloC1-6alkoxy, pyridyl, C(O)C1-3alkyl, phenyl, and C(O)phenyl,
- said phenyl, pyridyl and the phenyl portion of C(O)phenyl being optionally substituted with 1-3 halo atoms, and 1-2 C1-6alkyl or OC1-6alkyl groups.
21 more elements
Dependencies are inferred from the claim text.