3,6-ketal and enol ether macrolide antibiotics
    1.
    发明授权
    3,6-ketal and enol ether macrolide antibiotics 失效
    3,6-缩酮和烯醇醚大环内酯类抗生素

    公开(公告)号:US6043226A

    公开(公告)日:2000-03-28

    申请号:US257709

    申请日:1999-02-25

    CPC分类号: C07H17/08

    摘要: This invention relates to compounds of formulas 1 and 2 ##STR1## and to pharmaceutically acceptable salts and solvates thereof, wherein X, X.sup.1, R.sup.1, R.sup.2, R.sup.7, R.sup.17 and R.sup.19 are as defined herein. The compounds of formulas 1 and 2 may be useful in the treatment of bacterial, parasitic and protozoal infections, as well as disorders related to bacterial, parasitic and protozoal infections, in mammals, fish and birds. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and 2 and to methods of treating bacterial, parasitic and protozoal infections by administering the compounds of formula 1 and 2.

    摘要翻译: 本发明涉及式1和式2的化合物及其药学上可接受的盐和溶剂合物,其中X,X 1,R 1,R 2,R 7,R 17和R 19如本文所定义。 式1和2的化合物可用于治疗细菌,寄生虫和原生动物感染以及与哺乳动物,鱼和鸟类中的细菌,寄生虫和原生动物感染有关的疾病。 本发明还涉及含有式1和2化合物的药物组合物以及通过施用式1和式2化合物来治疗细菌,寄生虫和原生动物感染的方法。

    Efficient synthesis of 5-heteroatom-containing -pyrazoles
    4.
    发明授权
    Efficient synthesis of 5-heteroatom-containing -pyrazoles 失效
    有效合成含有5-杂原子的吡唑

    公开(公告)号:US06794512B2

    公开(公告)日:2004-09-21

    申请号:US10285836

    申请日:2002-11-01

    IPC分类号: C07D23124

    摘要: An efficient synthesis of sulfonyl pyrazoles of formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, R1 through R9 are as defined in the specification, comprising reacting a compound of formula II: wherein the ring of the formula (R5)-A-(SOmR4), m R1 through R9 are as defined above and wherein R10 is halo, (C1-C6)alkyl-SO3—, (C6-C10)aryl-SO3—, (C1-C6)alkyl-SO2—, or (C6-C10)aryl-SO2—; wherein each of said (C1-C6)alkyl component of said (C1-C6)alkyl-SO3— and (C1-C6)alkyl-SO2— radicals may optionally be substituted on any carbon atom by one to six fluoro substituents per (C1-C6)alkyl component; with a compound of formula R3—H, wherein R3 is as defined above, in the presence of a fluoride containing salt and in the presence of a solvent.

    摘要翻译: 式I的磺酰基吡唑的有效合成:其中式(R 5)-A-(SO m R 4),m,R 1至R 9的环如说明书中所定义, 包括使式II化合物反应:其中式(R 5)-A-(SO m R 4),m R 1至R 9的环如上所定义,其中R 10, 是(C 1 -C 6)烷基-SO 3 - ,(C 6 -C 10)芳基-SO 3 - ,(C 1 -C 6)烷基-SO 2 - 或(C 6 -C 10)芳基-SO 2 - 其中所述(C 1 -C 6)烷基-SO 3 - 和(C 1 -C 6)烷基-SO 2 - 基团的所述(C 1 -C 6)烷基组分中的每一个可任选地在任何碳原子上被1-6个氟取代基取代 -C 6)烷基组分; 与式R 3 -H的化合物,其中R 3如上所定义,在含氟化物盐的存在下和在溶剂存在下。

    5-heterocyclo-pyrazoles
    5.
    发明授权
    5-heterocyclo-pyrazoles 失效
    5-杂环 - 吡唑

    公开(公告)号:US06627626B2

    公开(公告)日:2003-09-30

    申请号:US10286674

    申请日:2002-11-01

    IPC分类号: A61K3155

    摘要: The present invention relates to 5-heterocyclo-pyrazoles of the formula I: wherein ring W, m, n, and R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.

    摘要翻译: 本发明涉及式I的5-杂环吡唑:其中环W,m,n和R 1至R 5如说明书中所定义,含有它们的药物组合物及其药物用途 。 本发明的化合物可用于治疗或缓解哺乳动物,优选人,狗,猫和家畜中的炎症和其它炎症相关疾病,例如关节炎,结肠癌和阿尔茨海默病。

    Heterocyclo-alkylsulfonyl pyrazoles
    7.
    发明授权
    Heterocyclo-alkylsulfonyl pyrazoles 失效
    杂环烷基磺酰基吡唑

    公开(公告)号:US07056933B2

    公开(公告)日:2006-06-06

    申请号:US10285745

    申请日:2002-11-01

    IPC分类号: C07D401/14 A61K31/439

    CPC分类号: C07D401/14

    摘要: The present invention relates to heterocyclo alkylsulfonyl pyrazoles of the formula I: wherein the ring of the formula (R5)—A—(SOmR4), m, X, R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.

    摘要翻译: 本发明涉及式I的杂环烷基磺酰基吡唑:其中式(R 5)5 - ((CH 3) SUP>),m,X,R 1至R 5如本说明书中所定义,含有它们的药物组合物及其药物用途。 本发明的化合物可用于治疗或缓解哺乳动物,优选人,狗,猫和家畜中的炎症和其它炎症相关疾病,例如关节炎,结肠癌和阿尔茨海默病。