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Purinone derivatives as hm74a agonists

A technology of purines and compounds, applied in the field of agonists of HM74a receptors

Inactive Publication Date: 2011-11-30
INCYTE CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Niaspan, while exhibiting prolonged dissolution times, still had a flushing frequency of about 70%, even with the recommended regimen of taking Niaspan with aspirin after a low-fat snack

Method used

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  • Purinone derivatives as hm74a agonists
  • Purinone derivatives as hm74a agonists
  • Purinone derivatives as hm74a agonists

Examples

Experimental program
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preparation example Construction

[0308]Preparation of compounds may involve protection and deprotection of various chemical groups. The necessity of protection and deprotection and the selection of appropriate protecting groups can be readily determined by those skilled in the art. The chemistry of protecting groups can be found, for example, in Greene et al., Protective Groups in Organic Synthesis, 2nd Ed., Wiley & Sons, 1991, which is hereby incorporated by reference in its entirety.

[0309] The reactions of the methods described herein can be carried out in suitable solvents readily selected by those skilled in the art of organic synthesis. Suitable solvents can be substantially nonreactive with the starting materials (reactants), intermediates or products at temperatures at which the reaction is complete (ie, temperatures in the range from the solvent's freezing temperature to the solvent's boiling temperature). A particular reaction can be carried out in one solvent or a mixture of more than one solven...

Embodiment 1

[0380] Preparation of 6-pentyl-8-(trifluoromethyl)-6,9-dihydro-5H-[1,2,4]triazolo[3,4-i]purin-5-one

[0381]

[0382] Step A: N-Amylurea

[0383]

[0384] To a 7.0 M aqueous ammonia solution in methanol (32 mL), 1-isocyanatopentane (5.0 g, 0.044 mol) was added dropwise. After the addition, the mixture was stirred at room temperature for 1 h, and concentrated under reduced pressure to give a white solid, which was used in the next step without further purification. to C 6 h 15 N 2 LCMS calculated for O(M+H): 131.1; found 131.1.

[0385] Step B: 6-Amino-1-pentylpyrimidine-2,4(1H,3H)-dione

[0386]

[0387] A mixture of N-amylurea (5.8 g, 0.044 mol), acetic anhydride (20 mL, 0.2 mol) and cyanoacetic acid (4.21 g, 0.0495 mol) was stirred at 70° C. for 2 h. After cooling to room temperature, the precipitate was collected by suction filtration, washed with EtOH, and air dried to yield 6.0 g of solid. The solid was treated in 3.0 M aqueous sodium hydroxide solution (2...

Embodiment 2

[0410] Preparation of 6-butyl-8-(trifluoromethyl)-6,9-dihydro-5H-[1,2,4]triazolo[3,4-i]purin-5-one

[0411]

[0412] The title compound was prepared using a method similar to that described in Example 1. for C 11 h 12 f 3 N 6 LCMS calculated for O: (M+H) 301.1; found 301.1.

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Abstract

The present invention relates to purinone derivatives of formula I, which are agonists of the HM74A receptor. The present invention further provides compositions of the compounds of the present invention, methods of using the compounds, and pharmaceutically acceptable salts thereof for treating diseases.

Description

[0001] This application claims priority to US Provisional Patent Application Serial No. 60 / 815,935 (filed June 23, 2006) and US Provisional Patent Application Serial No. 60 / 922,924 (filed April 11, 2007) , each of which is fully introduced here. technical field [0002] The present invention relates to agonists of HM74a receptors, compositions thereof, and methods of use thereof. Background technique [0003] Coronary artery disease (or CAD) is the number one cause of death in the United States (Nature Med 2002, 8: 1209-1262). The initiation and development of CAD involves a complex interplay of multiple physiological processes including inflammation, lipid homeostasis, and insulin resistance / diabetes. A variety of clinical studies have shown that the three main components of blood lipids, low-density lipoprotein (or LDL), high-density lipoprotein (or HDL), and triglyceride (TG), are associated with the development of atherosclerosis and CAD Tendency to be causally related...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/14A61K31/522A61K31/519A61P3/10
Inventor 布莱恩·麦克卡夫张柯郑昌盛薛褚彪曹敢峰王安来
Owner INCYTE CORP
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