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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)

Inactive Publication Date: 2007-03-15
TAKEDA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes a method for treating various diseases such as diabetes and inflammatory bowel disease using a compound called Compound I. The method involves administering a daily dose of between 1 mg and 250 mg of Compound I to a patient. The compound can be administered orally, through injection, or through other routes such as transdermal or nasal. The method can be performed for at least 30 days or more. The patent also provides combination therapy methods where Compound I can be combined with other antidiabetic or incretin compounds to enhance their therapeutic effects.

Problems solved by technology

Unfortunately, GLP-1 (7-36) is degraded rapidly in vivo and has been shown to have a short half-life in vivo (t1 / 2=1.5 minutes).

Method used

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  • Administration of dipeptidyl peptidase inhibitors
  • Administration of dipeptidyl peptidase inhibitors
  • Administration of dipeptidyl peptidase inhibitors

Examples

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Effect test

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

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K38/04A61K31/426
CPCA61K31/426A61K31/44A61K31/513A61K38/26A61K45/06Y10S514/866A61K2300/00A61K9/2018A61P3/00A61P31/18A61P35/00A61P43/00A61P5/50A61P3/10
Inventor CHRISTOPHER, RONALD J.COVINGTON, PAUL
Owner TAKEDA PHARMA CO LTD
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