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    Motilide compounds
    1.
    发明授权
    Motilide compounds 有权
    化合物

    公开(公告)号：US06750205B2

    公开(公告)日：2004-06-15

    申请号：US10409429

    申请日：2003-04-07

    申请人： Gary Ashley ,  Mark Burlingame ,  Christopher Carreras ,  Daniel Santi

    发明人： Gary Ashley ,  Mark Burlingame ,  Christopher Carreras ,  Daniel Santi

    IPC分类号： A61K3170

    CPC分类号： C07H17/08

    摘要： The present invention provides novel macrolide compounds of the formulas wherein: R is hydroxyl or methoxy; R1 is selected from the group consisting of hydrogen, hydroxyl, halide, NH2, OR9, where R9 is C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or heteroaryl and R10 and R11 are each independently hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, or aryl; R2 and R3 are each independently selected from the group consisting of hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, alkylaryl, alkenylaryl alkynylaryl or R2 and R3 together form a cycloalkyl or a cycloaryl moiety; R4 is hydrogen or methyl; R5 is hydrogen, hydroxyl, oxo, or together with R6 and the carbons to which they are attached form a cyclic carbonate; R6 is hydrogen, hydroxyl, OR12 where R12 is C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, or together with R5 and the carbons to which they are attached form a cyclic carbonate; R7 is methyl, C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, alkylaryl, alkenylaryl, alkynylaryl, amidoalkylaryl, amidoalkenylaryl, or amidoalkynylaryl; R8 is C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, alkylaryl, alkenylaryl, alkynylaryl, amidoalkylaryl, amidoalkenylaryl, or amidoalkynylaryl; and, x is a single or a double bond.

    摘要翻译： 本发明提供下式的新型大环内酯化合物，其中R是羟基或甲氧基; R 1选自氢，羟基，卤素，NH 2，OR 9，其中R 9是C 1 -C 10 烷基，C 2 -C 10烯基，C 2 -C 10炔基，芳基或杂芳基，R 10和R 11各自独立地为氢，C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基或芳基; R 2和R 3各自独立地选自氢，C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，芳基，烷基芳基，烯基芳基炔基芳基或R 2和R 3一起 形成环烷基或环芳基部分; R 4是氢或甲基; R 5是氢，羟基，氧代或与R 6一起，并且它们连接的碳形成环状碳酸酯; 其中R 12是C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，或与R 5一起形成的碳原子和它们所连接的碳原子形成环状 碳酸酯; R 7是甲基，C 3 -C 10烷基，C 2 -C 10烯基，C 2 -C 10 炔基，烷基芳基，烯基芳基，炔基芳基，酰氨基烷基芳基，酰氨基烯基芳基或酰胺基炔基芳基; R 8是C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，烷基芳基，链烯基芳基，炔基芳基，酰氨基烷基芳基，酰胺基烯基芳基或酰胺基炔基芳基; x是单键或双键。

    Motilide compounds
    2.
    发明授权
    Motilide compounds 有权
    化合物

    公开(公告)号：US06562795B2

    公开(公告)日：2003-05-13

    申请号：US09788314

    申请日：2001-02-15

    申请人： Gary Ashley ,  Mark Burlingame ,  Christopher Carreras ,  Daniel Santi

    发明人： Gary Ashley ,  Mark Burlingame ,  Christopher Carreras ,  Daniel Santi

    IPC分类号： A61K3170

    CPC分类号： C07H17/08

    摘要： The present invention provides novel macrolide compounds of the formulas wherein: R is hydroxyl or methoxy; R1 is selected from the group consisting of hydrogen, hydroxyl, halide, NH2, OR9,  where R9 is C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or heteroaryl and R10 and R11 are each independently hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, or aryl; R2 and R3 are each independently selected from the group consisting of hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, alkylaryl, alkenylaryl, alkynylaryl or R2 and R3 together form a cycloalkyl or a cycloaryl moiety; R4 is hydrogen or methyl; R5 is hydrogen, hydroxyl, oxo, or together with R6 and the carbons to which they are attached form a cyclic carbonate; R6 is hydrogen, hydroxyl, OR12 where R12 is C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, or together with R5 and the carbons to which they are attached form a cyclic carbonate; R7 is methyl, C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, alkylaryl, alkenylaryl, alkynylaryl, amidoalkylaryl, amidoalkenylaryl, or amidoalkynylaryl; R8 is C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, alkylaryl, alkenylaryl, alkynylaryl, amidoalkylaryl, amidoalkenylaryl, or amidoalkynylaryl; and, x is a single or a double bond.

    摘要翻译： 本发明提供下式的新型大环内酯化合物，其中R为羟基或甲氧基; R 1选自氢，羟基，卤素，NH 2，OR 9，其中R 9为C 1 -C 10烷基，C 2 -C 10烯基， C10炔基，芳基或杂芳基，R10和R11各自独立地为氢，C1-C10烷基，C2-C10烯基，C2-C10炔基或芳基; R2和R3各自独立地选自氢，C1-C10 烷基，C 2 -C 10烯基，C 2 -C 10炔基，芳基，烷基芳基，烯基芳基，炔基芳基或R 2和R 3一起形成环烷基或环芳基部分; R 4是氢或甲基; R 5是氢，羟基，氧代或与R 6一起 并且与它们相连的碳原子形成环状碳酸酯; R 6是氢，羟基，OR 12，其中R 12是C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，或与R 5和它们所连接的碳一起 形成环状碳酸酯; R 7是甲基，C 3 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，烷基芳基，链烯基芳基 ，芳基芳基，酰氨基烷基芳基，酰胺基烯基芳基或酰氨基炔基芳基; R8是C1-C10烷基，C2-C10烯基，C2-C10炔基，烷基芳基，烯基芳基，炔基芳基，酰氨基烷基芳基，酰氨基烯基芳基或酰胺基炔基芳基; x是单键或双键。

    Method for evaluating therapeutic efficacy
    5.
    发明授权
    Method for evaluating therapeutic efficacy 有权
    评估疗效的方法

    公开(公告)号：US06875576B2

    公开(公告)日：2005-04-05

    申请号：US10077461

    申请日：2002-02-15

    申请人： Christopher Carreras ,  Susan Dillon

    发明人： Christopher Carreras ,  Susan Dillon

    IPC分类号： A61K31/7048 ,  A61P1/00 ,  A61P1/04 ,  A61P1/08 ,  A61P1/10 ,  A61P1/14 ,  A61P43/00 ,  C07H17/00 ,  C07H17/08 ,  C07H21/04 ,  C07K14/72 ,  C12N5/08 ,  C12N5/10 ,  C12N15/09 ,  C12Q1/02 ,  G01N33/15 ,  G01N33/50 ,  G01N33/566 ,  G01N33/74 ,  G01N33/567

    CPC分类号： G01N33/5041 ,  C07H21/04 ,  C07K14/723 ,  G01N33/5008 ,  G01N33/566 ,  G01N33/74 ,  G01N2333/72 ,  G01N2333/726 ,  G01N2500/00

    摘要： The present invention relates to in vitro methods for evaluating compounds that better correlate with therapeutic efficiency than evaluating compounds based on potency alone. In general, the inventive method comprises: (i) determining a potency value for a compound against its target receptor; (ii) determining a desensitization value for the compound against its target receptor; and (iii) comparing the potency value with the desensitization value. If the desired action of a compound is as a receptor agonist, then the compound's desensitization value should be larger than the compound's potency value. This ensures that the concentration of a compound required for potency will not also cause the receptor to desensitize at the same time, thus in an essence nullifying the desired effect. The inventive methods are used to evaluate novel motilide compounds as well as ABT-229 and EM-574, two motilide compounds for which clinical trials have been initiated.

    摘要翻译： 本发明涉及用于评价与治疗效能更好相关的化合物的体外方法，而不仅仅是基于单独的效力来评价化合物。 通常，本发明的方法包括：（i）确定化合物对其靶受体的效价值; （ii）确定化合物对其靶受体的脱敏值; 和（iii）将效力值与脱敏值进行比较。 如果化合物的所需作用是受体激动剂，则化合物的脱敏值应大于化合物的效价值。 这确保了效力所需的化合物的浓度不会同时导致受体脱敏，因此在本质上无效期望的效果。 本发明的方法用于评价新型的动物酰胆碱化合物以及ABT-229和EM-574，这两种化合物已经开始临床试验。