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Anti -malarial agents

A solvate, aminopyrazine technology, applied in the direction of anti-infective drugs, resistance to vector-borne diseases, drug combinations, etc., can solve the problems of high price, human toxicity and side effects, etc.

Inactive Publication Date: 2014-11-05
UNIVERSITY OF CAPE TOWN +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, many of these drugs are expensive, and some show extreme toxicity and undesired side effects in humans

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0193] In one embodiment, the present invention provides aminopyrazine derivatives according to formula (I), and pharmaceutically acceptable salts, complexes, hydrates, solvates thereof, or polymorphs and tautomers thereof Use of isomers, geometric isomers, optically active forms and pharmaceutically active derivatives for the preparation of pharmaceutical compositions for the treatment or prevention of malaria:

[0194]

[0195] Among them, X is CR 1 or N; Y is selected from CF 3 , -C(O)-NR 3 R 4 , O-R 6 , SO 2 -R 6 ; 1 selected from H and halogen; R 2 from SO 2 -R 5 and -C(O)-R 10 ; 3 and R 4 independently selected from H and optionally substituted C 1 -C 6 the alkyl group; R 5 from-NR 7 R 8 and R 9 ; 6 is optionally substituted C1 -C 6 the alkyl group; R 7 and R 8 independently selected from H and optionally substituted C 1 -C 6 the alkyl group; R 9 is optionally substituted C 1 -C 6 Alkyl and optionally substituted C 3 -C 8 Cycloalkyl; R 10...

Embodiment 1

[0237] Example 1: Synthesis of compounds according to the invention

[0238] The aminopyrazine derivatives can be prepared from readily available starting materials using methods and procedures well known to those skilled in the art. It is to be understood that where typical or preferred experimental conditions (ie, reaction temperatures, times, moles of reagents, solvents, etc.) have been given, other experimental conditions can also be used unless otherwise stated. Preferred reaction conditions may vary with the particular reactants or solvent employed, but such conditions can be determined by one skilled in the art using routine optimization procedures.

[0239] A general synthetic method for obtaining compounds of formula (I) is shown in Scheme 1 below. Aminopyrazine derivatives according to formula (I), wherein the substituents are as defined above, can be prepared using four steps: from custom-made or commercially available aminopyrazines according to formula (i), acco...

Embodiment 2

[0298] Example 2: Synthesis of additional compounds of the invention

[0299] The following compounds listed in Table 1 below were prepared using a procedure similar to that described in Example 1.

[0300] Table 1

[0301]

[0302]

[0303]

[0304]

[0305] Compounds 13-19 and compounds 20-32 were synthesized according to Scheme 1 and Scheme 5, respectively. Compound 33 and compound 34 were synthesized according to Scheme 1. Chiral HPLC of individual enantiomers Compound 35 and Compound 36 in a mixture [using Chiral Pak IA (250X4.6) mm5u; 0.1% DEA in hexane: ethanol (40:60) as mobile phase, flow rate 1.0 mL / min] obtained after isolation, and compound 21 was synthesized according to scheme 3.

[0306] Starting materials generally described in the reaction schemes used to synthesize the compounds of the examples are listed in Table 2 below.

[0307] Table 2

[0308]

[0309]

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Abstract

The present invention is related to a use of aminopyrazine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyrazine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.

Description

technical field [0001] The present invention relates to novel antimalarial agents. Specifically, the present invention relates to a reagent for preparing a pharmaceutical preparation for preventing or treating malaria, its application and preparation method. Background technique [0002] Malaria is caused by a parasitic protozoan disease of the genus Plasmodium that infects and destroys red blood cells, causing fever, severe anemia, cerebral malaria, and, if left untreated, death. In sub-Saharan Africa, Plasmodium falciparum is the dominant species and is responsible for almost 1 million deaths per year. In Africa, the disease burden is highest among children under five and pregnant women. Plasmodium vivax causes 25-40% of the global malaria burden, especially in South and Southeast Asia and Central and South America. The other two major species known to infect humans are P. ovale and P. malariae. [0003] Malaria is a common disease in many developing countries. Approx...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04C07D401/10C07D401/14C07D413/10C07D241/26A61K31/444A61K31/497A61P33/06
CPCC07D241/20A61K31/497A61K31/551C07D401/10C07D403/10C07D401/04C07D401/14A61K31/4965A61K31/5377A61P33/00A61P33/06Y02A50/30A61K45/06
Inventor Y·尤尼斯K·奇贝勒M·J·韦提D·沃特森
Owner UNIVERSITY OF CAPE TOWN
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