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Dihydrogen phosphate salt of a prostaglandin d2 receptor antagonist

A pharmaceutical carrier and drug technology, which is applied in the field of dihydrogen phosphate, can solve problems that are not specifically disclosed

Inactive Publication Date: 2011-04-06
AVENTIS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the '732 publication does not specifically disclose that 2-(3-{6-[2-(2,4-dichlorophenyl)ethylamino]-2-methoxypyrimidin-4-yl}phenyl)- Dihydrogen Phosphate of 2-Methylpropionic Acid

Method used

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  • Dihydrogen phosphate salt of a prostaglandin d2 receptor antagonist
  • Dihydrogen phosphate salt of a prostaglandin d2 receptor antagonist
  • Dihydrogen phosphate salt of a prostaglandin d2 receptor antagonist

Examples

Experimental program
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Effect test

Embodiment approach

[0047] A particular embodiment of the invention is the compound of formula (III) in crystalline form.

[0048] The compounds of the present invention exhibit prostaglandin D2 receptor antagonist activity and are useful pharmacologically active agents. Therefore, it is incorporated into pharmaceutical compositions and used to treat patients suffering from certain medical disorders.

[0049]Compounds of the present invention are antagonists of the prostaglandin D2 receptor according to assays described in the literature and in the Pharmacological Assays section below, the results of which are believed to correlate with pharmacological activity in humans and other mammals. Accordingly, in another embodiment, the present invention provides compounds of the invention and pharmaceutical compositions containing the compounds of the invention for use in the treatment of patients suffering from or susceptible to a condition ameliorated by administration of a PGD2 antagonist. patient. ...

Embodiment

[0117] 2-(3-{6-[2-(2,4-Dichlorophenyl)ethylamino]-2-methoxypyrimidin-4-yl}phenyl)-2-methylpropanoic acid dihydrogen phosphate

[0118] Step 1: 4,6-dichloro-2-methoxypyrimidine (0.7g), 2,4-dichlorophenethylamine (0.82g) and sodium bicarbonate (0.88g) were dissolved in ethanol (25mL) The solution was heated at 80°C for 3 hours and poured into water (400 mL). The resulting solid was filtered and air dried to give (6-chloro-2-methoxypyrimidin-4-yl)-[2-(2,4-dichloro Phenyl)ethyl]-amine .

[0119] Step 2: To a solution of lithium diisopropylamide in tetrahydrofuran / n-heptane / ethylbenzene (1.8 M, 17 mL) at 0 °C was added dropwise 2-(3-bromo-phenyl)- A solution of propionic acid (3 g, 13.9 mmol) in tetrahydrofuran (5 mL). The mixture was stirred for 1 hour, then a solution of methyl iodide (4.93 g, 34.8 mmol) in tetrahydrofuran (5 mL) was added dropwise over 10 minutes. The reaction mixture was stirred for 15 hours, quenched with 2N HCl, concentrated in vacuo, and diluted w...

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Abstract

The present invention is directed to the dihydrogen phosphate salt of 2-(3-{6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl}-phenyl)-2-methyl-propionic acid of Formula (III), a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of Formula (III), and a pharmaceutically acceptable carrier; and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like.

Description

field of invention [0001] Large-scale production of pharmaceutical compositions can pose many challenges to chemists and chemical engineers. While many of these challenges involve the handling of large quantities of reagents and the control of large-scale reactions, handling of the final product presents special challenges related to the nature of the final active product itself. Such a product must not only be high yielding, stable and easy to isolate, but it must have properties suitable for the type of pharmaceutical formulation that may ultimately be used. The stability of active ingredients of pharmaceutical formulations must be considered at every step of the production process, including synthesis, isolation, bulk storage, drug formulation and long-term formulation. Each of these steps can be affected by various environmental conditions such as temperature and humidity. [0002] The pharmaceutically active substance used for the preparation of the pharmaceutical compo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D239/46C07D239/47A61K31/505
CPCC07D239/47A61P1/00A61P11/00A61P11/06A61P11/08A61P17/00A61P17/02A61P17/04A61P19/02A61P25/20A61P27/00A61P27/12A61P27/14A61P29/00A61P31/00A61P35/00A61P37/00A61P37/08A61P9/10C07D239/46A61K31/505
Inventor B·朗之万E·奥顿D·谢勒
Owner AVENTIS PHARMA INC
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