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Modulators of the gpr119 receptor and the treatment of disorders related thereto

A kind of solvate, C1-C6 technology, applied in the field of solvate and hydrate, formula compound and its medicinal salt

Inactive Publication Date: 2013-02-06
ARENA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0050] Parenteral administration of PYY has been reported 3-36 Significantly reduced food intake and weight gain in rats, decreased appetite and reduced food intake in humans and reduced food intake in mice (but not in Y2R-null mice, presumably requiring Y2R for food intake effects )

Method used

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  • Modulators of the gpr119 receptor and the treatment of disorders related thereto
  • Modulators of the gpr119 receptor and the treatment of disorders related thereto
  • Modulators of the gpr119 receptor and the treatment of disorders related thereto

Examples

Experimental program
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preparation example Construction

[1291] for the active level of 125 The synthetic method that I is combined in the target molecule comprises:

[1292] A. Sandmeyer and similar reactions: This method converts aryl or heteroaryl amines into diazonium salts, such as diazonium tetrafluoroborate, and the subsequent use of Na 125 I convert to 125 I labeled compound. A representative method is reported by Zhu, G-D and colleagues in J. Org. Chem., 2002, 67, 943-948.

[1293] B. The ortho iodine of phenol ( 125 I)ization: This method allows 125 I was bound in the ortho position to the phenol as reported by Collier, T.L and co-workers in J. Labelled Compd. Radiopharm., 1999, 42, S264-S266.

[1294] C. For aryl bromide and heteroaryl bromide 125 I Exchange: This method is usually a two-step process. The first step is to convert the aryl or heteroaryl bromide to the corresponding trialkyltin intermediate using, for example, the following method: 3 ) 3 SnSn(CH 3 ) 3 ] in the presence of Pd-catalyzed reactions [...

Embodiment 1

[1300] Embodiment 1: the synthesis of compound of the present invention.

[1301] Exemplary syntheses for compounds of the invention are shown in Figures 8 to 15 , where the variables have the same definitions as used throughout this specification.

[1302] The compounds of the present invention and their synthesis are further illustrated by the following examples. The following examples are provided to further define the invention without, however, limiting the invention to the specifics of these examples. Compounds described before and after this paper were named according to AutoNom version 2.2, AutoNom 2000, CS ChemDraw Ultra version 7.0.1 or CS ChemDraw Ultra version 9.0.7. In some instances, common names are used, and it is understood that such common names will be known to those skilled in the art.

[1303] Chemistry: Proton NMR ( 1 H NMR) spectra were recorded on a Bruker Avance-400 equipped with QNP (Quad Nucleus Probe) or BBI (Broad Band Inverse) and z-gradient....

Embodiment 11

[1305] Example 1.1: Preparation of tert-butyl 4-((1s,4s)-4-hydroxycyclohexyloxy)piperidine-1-carboxylate (intermediate 1) and 4-((1r,4r)-4-hydroxy Cyclohexyloxy)piperidine-1-carboxylate tert-butyl ester (Intermediate 2).

[1306] Step A: Preparation of 4-(pyridin-4-yloxy)cyclohexanol.

[1307]To a solution of sodium hydride (13.77 g, 344 mmol) in DMSO (250 mL) was added cyclohexane-1,4-diol (20 g, 172 mmol) portionwise at room temperature. The mixture was stirred at room temperature for 1 hour, then 4-chloropyridine hydrochloride (25.8 g, 172 mmol) was added portionwise. The mixture was stirred at room temperature for 2 hours until hydrogen evolution ceased, then heated at 80° C. for 8 hours. The mixture was diluted with ice water and extracted with DCM (6 times). The organic layers were combined and washed with water and brine, with MgSO 4 dry. The solvent was removed and the resulting solid was dried under high vacuum at 80° C. for 2 hours to further remove any remainin...

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Abstract

The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more additional pharmacetical agents, such as, an inhibitor of DPP-IV, a biguanide, an SGLT2 inhibitor, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.

Description

technical field [0001] The present invention relates to compounds of formula (Ia) and pharmaceutically acceptable salts, solvates and hydrates thereof, for use as a single agent or in combination with one or more other pharmaceutical agents for the treatment of, for example, disorders selected from: GPR119- Receptor-related disorders; conditions alleviated by increasing blood incretin levels; metabolism-related disorders; type II diabetes; obesity; and complications associated with them, such as DPP-IV inhibitors agents, biguanides, SGLT2 inhibitors, or alpha-glucosidase inhibitors. Background technique [0002] A) diabetes [0003] Diabetes is a serious disease that affects more than 100 million people worldwide. In the United States, there are 12 million people with diabetes, with 600,000 new cases diagnosed each year. [0004] Diabetes mellitus is a diagnostic term denoting a group of disorders characterized by abnormal glucose homeostasis leading to hyperglycemia. Th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/46C07D401/04C07D401/12C07D401/14C07D405/12C07D405/14C07D413/04C07D413/06C07D413/14C07D417/14A61K31/445A61K31/454A61K31/495A61P3/10
CPCC07D401/14C07D401/12C07D417/14C07D413/04C07D413/14C07D405/14C07D405/12C07D211/46C07D401/04C07D413/06A61P3/00A61P3/04A61P3/10A61P19/00A61P19/08A61P19/10A61P25/00A61P43/00
Inventor R.M.琼斯韩相敦D.J.布扎德J.莱曼S.纳拉亚南岳大伟
Owner ARENA PHARMA
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