- CCR2 MODULATORS
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Compounds are provided that are modulators of the CCR2 receptor. The compounds have the general formula (I) and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activtation of CCR2 receptors.
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Paragraph 0154; 0156
(2016/12/07)
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- Antiparasitic agents
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The invention provides novel compounds having the formula: STR1 wherein R when taken individually is H; R1 when taken individually is H or OH; R and R1 when taken together represent a double bond; R2 is an alpha-branched C3 -C8 alkyl, alkenyl, alkynyl, alkoxyalkyl or alkylthioalkyl group; a C3 -C8 cycloalkyl, C5 -C8 cycloalkenyl or C5 -C8 cycloalkylalkyl group, any of which may be substituted by methylene or one or more C1 -C4 alkyl groups or halo atoms; or a 3 to 6 membered oxygen or sulphur containing heterocyclic ring which may be substituted by one or more C1 -C4 alkyl groups or halo atoms; R3 is hydrogen or methyl; R4 is H or 4'-(alpha-L-oleandrosyl)-alpha-L-oleandrosyloxy with the proviso that when R2 is alkyl it is not isopropyl or sec-butyl; when R4 is H, each of R and R1 is H, and R2 is not methyl or ethyl; and when R4 is H, R is H, R1 is OH, and R2 is not 2-buten-2-yl, 2-penten-2-yl or 4-methyl-2-penten-2-yl. The compounds are broad spectrum antiparasitic agents having utility as anthelmintics, ectoparasiticides, insecticides and acaricides. The invention also provides a process for producing the novel avermectin and milbemycin derivatives by adding a carboxylic acid or derivative thereof to a fermentation of an avermectin or milbemycin producing organism.
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