Administration of dipeptidyl peptidase inhibitors

a technology of dipeptidyl peptidase and inhibitor, which is applied in the direction of peptides, drug compositions, metabolic disorders, etc., can solve the problems of short half-life and rapid degradation of glp-1 (7-36)

a technology of dipeptidyl peptidase and inhibitor, which is applied in the direction of peptides, drug compositions, metabolic disorders, etc., can solve the problems of short half-life and rapid degradation of glp-1 (7-36)

US20070060530A1Inactive Publication Date: 2007-03-15TAKEDA PHARMA CO LTD
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  • Administration of dipeptidyl peptidase inhibitors
  • Administration of dipeptidyl peptidase inhibitors
  • Administration of dipeptidyl peptidase inhibitors

Examples

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examples

1. Preparation of 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and Pharmaceutically Acceptable Salts

[0168]

[0169] A mixture of 2-bromo-5fluorotoluene (2) (3.5 g, 18.5 mmol) and CuCN (2 g, 22 mmol) in DMF (100 mL) was refluxed for 24 hours. The reaction was diluted with water and extracted with hexane. The organics were dried over MgSO4 and the solvent removed to give product 3 (yield 60%). 1H-NMR (400 MHz, CDCl3): δ 7.60 (dd, J=5.6, 8.8 Hz, 1H), 6.93-7.06 (m, 2H), 2.55 (s, 3H).

2-Bromomethyl-4-fluorobenzonitrile (4)

[0170] A mixture of 4-fluoro-2-methylbenzonitrile (3) (2 g, 14.8 mmol), NBS (2.64 g, 15 mmol) and AIBN (100 mg) in CCl4 was refluxed under nitrogen for 2 hours. The reaction was cooled to room temperature. The solid was removed by filtration. The organic solution was concentrated to give crude product as an oil, which was used in the next step without further purification. 1H-NMR (400 MHz, CDCl3): δ 7.68 (dd,...

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Abstract

Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.

Description

RELATED APPLICATION [0001] This application claims the benefit of U.S. Provisional Application No. 60 / 717,560 filed Sep. 14, 2005 and U.S. Provisional Application No. 60 / 747,280 filed May 15, 2006, each of which is incorporated herein by reference.FIELD OF THE INVENTION [0002] The invention relates to the method of administering compounds used to inhibit dipeptidyl peptidase IV as well as treatment methods based on such administration. DESCRIPTION OF RELATED ART [0003] Dipeptidyl Peptidase IV (IUBMB Enzyme Nomenclature EC.3.4.14.5) is a type II membrane protein that has been referred to in the literature by a wide a variety of names including DPP4, DP4, DAP-IV, FAPβ, adenosine deaminase complexing protein 2, adenosine deaminase binding protein (ADAbp), dipeptidyl aminopeptidase IV; Xaa-Pro-dipeptidyl-aminopeptidase; Gly-Pro naphthylamidase; postproline dipeptidyl aminopeptidase IV; lymphocyte antigen CD26; glycoprotein GP110; dipeptidyl peptidase IV; glycylproline aminopeptidase; gl...

Claims

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Application Information

Patent Timeline
15 Mar 2007
Publication
US20070060530A1
IPC
A61K38/04; A61K31/426
CPC
A61K31/426; A61K31/44; A61K31/513; A61K38/26; A61K45/06; Y10S514/866; A61K2300/00; A61K9/2018
Inventors
CHRISTOPHER, RONALD J.; COVINGTON, PAUL