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Purine compounds as prodrugs of a2b adenosine receptor antagonists, their process and medicinal applications
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A compound and solvate technology, applied in the field of purine compounds as prodrugs of A2B adenosine receptor antagonists, their preparation and medical application, can solve problems such as difficulty in using conventional pharmaceutical excipients, high-dose preparation, etc.
Inactive Publication Date: 2013-08-21
ADVINUS THERAPEUTICS PVT LTD
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These compounds are known to be relatively insoluble in aqueous media and difficult to formulate at higher doses using conventional pharmaceutical excipients
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[0202] According to another embodiment of the present invention, B is substituted aryl;
[0203] In another embodiment of the present invention, R 1 For the alkyl.
[0204] According to another embodiment of the present invention, R 2 selected from the group consisting of hydrogen, halogen, cyano, unsubstituted or substituted cycloalkyl, and unsubstituted or substituted heteroaryl.
[0205] A particular embodiment of the present invention is a compound selected from the group consisting of the following compounds or tautomers, polymorphs, stereoisomers, solvates or pharmaceutically acceptable salts thereof:
[0304] 5,6-Diamino-3-propyl-1H-pyrimidine-2,4-dione (4.25 g, 0.023 mol), 1-( A mixture of 3-trifluoromethyl-benzyl)-1H-pyrazole-4-carboxylic acid (6.23g, 0.023mol) in methanol (50ml) was cooled to 0°C, and EDCI.HCl (8.82g, 0.046 mol). The reaction mixture was stirred at 25°C for 6 hours and the organic volatiles were evaporated. Water (50ml) was added to the residue and the precipitate was filtered off and washed with cold water (50ml) to give 1-(3-trifluoromethyl-benzyl)-1H-pyrazole-4-carboxy as a light yellow solid Acid (6-amino-2,4-dioxo-3-propyl-1,2,3,4-tetrahydro-pyrimidin-5-yl)-amide (7.2 g, 72%).
[0339] Examples 3 and 4 were prepared in a similar manner to Examples 1 and 2.
[0340]
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Abstract
The present disclosure relates to purine compounds of formula (I) or formula (II) or its tautomers, polymorphs, stereoisomers, solvates or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2B adenosinereceptor antagonists. {Formulas should be inserted here} The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2B receptor. Such conditions include, but are not limited to, asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders including inflammatory bowel disease, sickle celldisease, and / or autoimmune diseases. and to their use in treating mammals for various disease states, such as gastrointestinal disorders, immunological disorders, hypersensitivity disorders, neurological disorders, and cardiovascular diseases due to both cellular hyperproliferation and apoptosis, and the like. The present disclosure also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.
Description
technical field [0001] The present invention relates to as A 2B Purine compounds or tautomers, polymorphs, stereoisomers, solvates or pharmaceutically acceptable salts thereof as prodrugs of adenosinereceptor antagonists, and their use in the treatment of various Use in conditions such as gastrointestinal disorders, immune disorders, hypersensitivity disorders, neurological disorders, and cardiovascular diseases caused by both hyperproliferation and apoptosis of cells. The invention also relates to processes for the preparation of such compounds and pharmaceutical compositions containing them. Background technique [0002] Adenosine is known to be an endogenous regulator of various physiological functions mediated by different membrane-specific receptors belonging to the G protein-coupled receptor family. Adenosine plays a role in cardiovascular, central nervous system, respiratory system, kidney, fat and platelets. Advances in molecular biology in recent years, together...
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