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    • 3. 发明授权
    • Retinoid antagonists and use thereof
    • 类视黄醇拮抗剂及其用途
    • US06326397B1
    • 2001-12-04
    • US09307009
    • 1999-05-07
    • Werner BollagMichael KlausPeter MohrPaola Panina-BordignonMichael RosenbergerFrancesco Sinigaglia
    • Werner BollagMichael KlausPeter MohrPaola Panina-BordignonMichael RosenbergerFrancesco Sinigaglia
    • A01N5300
    • C07C57/48C07C57/42
    • The present invention relates to novel retinoid antagonists of the formula I wherein the dotted bond can be either hydrogenated or form a double bond; and, when the dotted bond forms a double bond, R1 is lower alkyl and R2 is hydrogen; and, when the dotted bond is hydrogenated, R1 and R2 taken together are methylene to form a cis-substituted cyclopropyl ring; R3 is hydroxy or lower alkoxy; R4 is alkyl or alkoxy; and R5 and R6 are, independently, a C4-12 alkyl or a 5-12 cycloalkyl substituent containing from 1-3 rings which are either unsubstituted or substituted with from 1-3 lower alkyl groups, with the carbon atom of R5 and R6 being linked to the remainder of the molecule to form a quaternary carbon atom pharmaceutically acceptable salts of carbocylic acids of the formula I; as well as method for the treatment of osteoporosis and preneoplastic and neoplastic diseases, and a method for reducing or abolishing adverse events in subjects receiving retinoid agonist treatment by administering a retinoid antagonist.
    • 本发明涉及式I的新型类视黄醇拮抗剂,其中虚线键可以被氢化或形成双键; 并且当虚线键形成双键时,R 1为低级烷基且R 2为氢; 并且当点键被氢化时,R 1和R 2一起为亚甲基以形成顺式取代的环丙基环; R3是羟基或低级烷氧基; R4是烷基或烷氧基; 并且R 5和R 6独立地是C 1-4烷基或含有1-3个环的5-12个环烷基取代基,它们是未取代的或被1-3个低级烷基取代,R5和R6的碳原子是 与分子的其余部分连接以形成式I的碳酸的药学上可接受的盐的季碳原子; 以及用于治疗骨质疏松症和肿瘤前和肿瘤性疾病的方法,以及通过施用类视黄醇拮抗剂减少或消除接受类视黄醇激动剂治疗的受试者的不良事件的方法。
    • 5. 发明授权
    • Article for insert control by passive evaporation of an active ingredient
    • 用于通过被动蒸发活性成分进行插入控制的物品
    • US06582714B1
    • 2003-06-24
    • US08419219
    • 1995-04-10
    • Robert R. EmmrichJohn W. MikkonenThomas A. Lajiness
    • Robert R. EmmrichJohn W. MikkonenThomas A. Lajiness
    • A01N5300
    • A01N53/00A01N57/12A01N25/34A01N25/18A01N25/00A01N2300/00
    • An insect control article to control flying insects. The insect control article has a substrate that is impregnated with an active insect control ingredient that is available for passive evaporation. The active insect control ingredient is selected from the group consisting of transfluthrin, prallethrin, tefluthrin, esbiothrin, and combinations thereof. The method of the invention for controlling flying insects includes providing an insect control article having a substrate that is impregnated with an active insect control ingredient available for passive evaporation, wherein the active insect control ingredient is selected from the group consisting of transfluthrin, prallethrin, vaporthrin, teflurthrin, esbiothrin, DDVP, and combinations thereof. The insect control article is then placed in an environment with air movement in such a manner that the substrate of the insect control article is exposed to the air movement, and the active insect control ingredient impregnated within the substrate is allowed to evaporate passively into the air.
    • 控制飞虫的防虫物品。 昆虫控制制品具有浸渍有可用于被动蒸发的活性昆虫控制成分的底物。 活性昆虫控制成分选自氟氯氰菊酯,丙烯菊酯,三氟氯氰菊酯,异烟草蛋白及其组合。 用于控制飞虫的本发明的方法包括提供具有浸渍有可用于被动蒸发的活性昆虫控制成分的底物的昆虫控制制品,其中所述活性昆虫控制成分选自氟氯氰菊酯,丙醚菊酯,vaporthrin ,特氟菊酯,嗜铬蛋白,DDVP及其组合。 然后将昆虫控制制品置于具有空气运动的环境中,使得昆虫控制制品的基底暴露于空气运动,并且将浸渍在基材内的活性昆虫控制成分被动地蒸发到空气中 。