October 29, 2012

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The following patent record is from the CAplusSM database.

CAPLUS COPYRIGHT 2012 ACS

Patent Number: WO 201298217
Title: Preparation of fused dihydrofurans as GPR119 modulators for the treatment of diabetes, obesity and related disorders
Inventor(s): Himmelsbach, Frank; Langkopf, Elke; Nosse, Bernd
Patent Assignee(s): Boehringer Ingelheim International GmbH, Germany
Source: PCT Int. Appl., 149pp. CODEN: PIXXD2
Language: Japanese

Abstract:
The present invention relates to compds. I [R1 = (un)substituted 5-6 membered heteroaryl containing 1-3 heteroatoms selected from N, O and S, and wherein optionally a second ring may be condensed to said heteroaryl (wherein said second ring is (un)substituted unsatd. or aromatic and 5-6 membered and may contain 1-3 heteroatoms selected from N, O and S, and wherein in said second ring 1-2 CH2 groups may be optionally replaced by C(O), S(O), SO2 or (un)substituted NH); A = 1,2,3,6-tetrahydropyridin-4-yl ring substituted at the N atom with alkylSO2, (un)substituted Ph, and 5-6 membered heteroaryl containing 1-3 heteroatoms selected from N, O and S; and wherein optionally a second ring may be condensed to said Ph or heteroaryl (wherein said second ring is unsatd. or aromatic and 5-6 membered and may contain 1-3 heteroatoms selected from N, O and S, and wherein in said second ring 1-2 CH2 groups may be optionally replaced by C(O), S(O), SO2 or (un)substituted NH); L1, L2 = F, alkyl (may be substituted with 1 or more F atoms); X1-X3 = CR2, N (such that 0-2 membered of the group consisting of X1-X3 have the meaning N); R2 = H, F, Cl, CN, etc.; n = 0-4; m = 0-2], which have valuable pharmacol. properties, and in particular  bind to the GPR119 receptor and modulate its activity. Over ninety compds. I were prepared  E.g., a multi-step synthesis of II, starting from 4-(benzofuran-2-yl)piperidine hydrochloride, was described. The effect of compds. I on the activation of GPR119 and on the stimulation of intracellular cAMP concentration was determined using the AlphaScreen cAMP assay kit (EC50 values were given). Pharmaceutical compns. comprising compound I, alone or in combination with other therapeutic agents, were disclosed.

Please note:  Abstracts for patent records in CAplus are routinely enhanced to better describe the claimed invention. In this example, CAS enhanced the abstract using information from the publication.

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