Dipeptidyl peptidase IV inhibitors, process for their preparation and compositions containing them
AssigneeGlenmark Pharmaceuticals S.A.
InventorsAbraham Thomas, Gopalan Balasubramanian, V. S. Prasadarao Lingam, Daisy Manish Shah
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Abstract
The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: wherein X, Y, a, R1, and R2 are as defined herein.
Claims47
A method of inhibiting DPP-IV in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a compound of formula (I)
- wherein:
- Y is —S(O)m, —CH2—, CHF, or —CF2;
- m is 0, 1, or 2;
- X is a bond, C1-C5 alkyl, or —C(═O)—;
- the dotted line [----] in the carbocyclic ring represents an optional double bond;
- R1 is CN, or a substituted or unsubstituted heteroaryl ring or substituted or unsubstituted heterocyclic ring, wherein the ring is a five-membered ring having at least one nitrogen atom;
- R2 is hydrogen, nitrile (—CN), or COOH;
- or
- a tautomeric form, stereoisomer, enantiomer, diastereomer, N-oxide, or pharmaceutically acceptable salt thereof.
A method of treatment is of a disease selected from impaired glucose homeostasis, impaired glucose tolerance, arthritis, allograft rejection in transplantation, inflammatory bowel disease, obesity, hyperglycemia, and hyperinsulinemia in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a compound of formula (I)
- wherein:
- Y is —S(O)m, —CH2—, CHF, or —CF2;
- m is 0, 1, or 2;
- X is a bond, C1-C5 alkyl, or —C(═O)—;
- the dotted line [----] in the carbocyclic ring represents an optional double bond;
- R1 is CN, or a substituted or unsubstituted heteroaryl ring or substituted or unsubstituted heterocyclic ring, wherein the ring is a five-membered ring having at least one nitrogen atom;
- R2 is hydrogen, nitrile (—CN), or COOH,
- or a tautomeric form, stereoisomer, enantiomer, diastereomer, N-oxide, or pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.