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29 条记录 (耗时 0.045 秒)

    Three dimensional structure of a ZAP tyrosine protein kinase fragment and modeling methods
    1.
    发明授权
    Three dimensional structure of a ZAP tyrosine protein kinase fragment and modeling methods 失效
    ZAP酪氨酸蛋白激酶片段的三维结构和建模方法

    公开(公告)号：US06251620B1

    公开(公告)日：2001-06-26

    申请号：US08975040

    申请日：1997-11-18

    申请人： Marcos H. Hatada ,  Xiaode Lu ,  Ellen R. Laird ,  Jennifer L. Karas ,  Mark J. Zoller ,  Dennis A. Holt

    发明人： Marcos H. Hatada ,  Xiaode Lu ,  Ellen R. Laird ,  Jennifer L. Karas ,  Mark J. Zoller ,  Dennis A. Holt

    IPC分类号： C12Q148

    CPC分类号： C12N9/1205

    摘要： The invention relates to human ZAP-70, and in particular, to the region of ZAP-70 containing the tandem Src homology-2 (“SH2”) domains, to crystalline forms thereof, liganded or unliganded, which are particularly useful for the determination of the three-dimensional structure of the protein. The three dimensional structure of the tandem SH2 region of ZAP provides information useful for the design of pharmaceutical compositions which inhibit the biological function of ZAP and other members of the ZAP family of SH2 domain-containing proteins, particularly those biological functions mediated by molecular interactions involving one or both SH2 domains.

    摘要翻译： 本发明涉及人ZAP-70，特别涉及含有串联Src同源性-2（“SH2”）结构域的ZAP-70区域，其结构形式为配体或非配体，其特别可用于测定 的蛋白质的三维结构。 ZAP的串联SH2区域的三维结构提供了有用的药物组合物的设计信息，该药物组合物抑制ZAP和包含SH2结构域的蛋白质的ZAP家族的其他成员的生物学功能，特别是那些通过分子相互作用介导的那些生物学功能 一个或两个SH2结构域。

    17.alpha. and 17.beta.-substituted estra-1,3,5(10)-triene-3-carbboxlic acid
    9.
    发明授权
    17.alpha. and 17.beta.-substituted estra-1,3,5(10)-triene-3-carbboxlic acid 失效

    公开(公告)号：US5618806A

    公开(公告)日：1997-04-08

    申请号：US325462

    申请日：1994-10-28

    申请人： Dennis A. Holt ,  Mark A. Levy

    发明人： Dennis A. Holt ,  Mark A. Levy

    IPC分类号： A61K8/00 ,  A61K8/49 ,  A61K31/56 ,  A61K31/57 ,  A61Q5/00 ,  A61Q9/04 ,  C07C69/00 ,  C07J1/00 ,  C07J3/00 ,  C07J5/00 ,  C07J7/00 ,  C07J9/00 ,  C07J17/00 ,  C07J31/00 ,  C07J33/00 ,  C07J41/00 ,  C07J43/00 ,  C07J63/00 ,  C07J75/00

    CPC分类号： C07J9/00 ,  C07J1/0014 ,  C07J17/00 ,  C07J3/00 ,  C07J3/005 ,  C07J31/006 ,  C07J33/002 ,  C07J41/0094 ,  C07J43/003

    摘要： Invented are 17.alpha. and 17.beta.-substituted acyl-3-carboxy aromatic A ring analogues of steroidal synthetic compounds. Representative of such compounds include the following ##STR1## wherein Z is .alpha. or .beta. ##STR2## in which A is absent or present as a linear or branched, saturated or unsaturated hydrocarbon chain containing from 1-6 carbon atoms and R isa) a linear or branched, saturated or unsaturated hydrocarbon chain containing 1-12 carbon atoms substituted with one or more substituents selected from the group consisting of: --OC.sub.6 -C.sub.12 aryl, --OC.sub.1 -C.sub.4 alkyl, halogen, carboxy and --S(O).sub.n .sup.R.sup.7, where n is 0-2 and R.sup.7 is hydrogen or C.sub.1-4 alkyl;b) C.sub.3 -C.sub.8 nonaromatic, unsaturated or saturated, cycloalkyl, optionally substituted with one or more substituents selected from the group consisting of:--OC.sub.6 -C.sub.12 aryl, --(CH.sub.2).sub.m OH, --OC.sub.1 -C.sub.4 alkyl, C.sub.6 -C.sub.12 aryl, C.sub.1 -C.sub.4 alkyl, trifluoromethyl, halogen, --(CH.sub.2).sub.p COOH, --S(O).sub.n R.sup.7 and protected --OH, where m is 0-4, p is 0-3, n is 0-2 and R.sup.7 is hydrogen or C.sub.1-4 alkyl; orc) C.sub.4 -C.sub.12 aryl, optionally containing one or more heteroatoms, provided that when C is 4 the aromatic ring contains at least one heteroatom, and optionally substituted with one or more substituents selected from the group consisting of:--OC.sub.6 -C.sub.12 aryl, --(CH.sub.2).sub.m OH, C.sub.6 -C.sub.12 aryl, C.sub.1 -C.sub.4 alkyl, --OC.sub.1 -C.sub.4 alkyl, trifluoromethyl, halogen, --(CH.sub.2).sub.p COOH, --S(O).sub.n R.sup.7 and protected --OH, where m is 0-4, p is 0-3, n is 0-2 and R.sup.7 is hydrogen or C.sub.1-4 alkyl. Also invented are pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5.alpha.-reductase. Also invented are intermediates and processes used in preparing these compounds.