Original document(29 pages) Authorized document(26 pages) 中文版
    The invention provides novel compounds having the formula: (I) 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.
Application Number
申请号
86105218 Application Date
申请日
1986.07.25
Title 名称 Method for making medication of resistance to parositic disease
Publication Number
公开号
1009133 Publication Date
公开日
1987.03.04
Approval Pub. Date 1990.12.12 Granted Pub. Date 1990.12.12
International Classification 分类号 C07D493/22;C07H17/08;C12P17/08;C12P19/62
Applicant(s) Name
申请人
Pfizer Inc.
Address 地址
Inventor(s) Name 发明人 Paul Steffan Jeppesen
Attorney & Agent 代理人 CAO HENGXING
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