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    Modulators of proteins with phosphotryrosine recognition units
    2.
    发明授权
    Modulators of proteins with phosphotryrosine recognition units 失效
    具有磷酸基酪氨酸识别单元的蛋白质调节剂

    公开(公告)号：US5753687A

    公开(公告)日：1998-05-19

    申请号：US766114

    申请日：1996-12-16

    申请人： Adnan Mjalli ,  Sepehr Sarshar ,  Xiaodong Cao ,  Farid Bakir

    发明人： Adnan Mjalli ,  Sepehr Sarshar ,  Xiaodong Cao ,  Farid Bakir

    IPC分类号： A61K31/415 ,  C07D233/54 ,  C07D233/56 ,  C07D233/66

    CPC分类号： A61K31/415 ,  C07D233/54 ,  C07D233/56 ,  C07D233/66

    摘要： Y--X--C(R').dbd.C(R")COOR'" (A1) The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryoic cells, whole animals and human beings. R' and R" are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R'" is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or ##STR1## wherein (*) indicates a potential point of attachment to X.

    摘要翻译： YXC（R'）= C（R“）COOR”'（A1）本发明涉及具有式（A1）所示的一般结构的新的蛋白质酪氨酸磷酸酶调节化合物及其制备方法， 该化合物用于治疗人和动物疾病，用于蛋白质或糖蛋白的纯化及其在诊断中的应用。 本发明涉及在体外系统，微生物，真核细胞，整个动物和人类中调节具有磷酸酪氨酸识别单元的分子的活性，包括蛋白酪氨酸磷酸酶（PTP酶）和具有Src同源性-2结构域的蛋白质。 R'和R“独立地选自氢，卤素，氰基，硝基，三卤代甲基，烷基，芳基烷基。 R“选自氢，烷基，取代的烷基，芳基，芳基烷基。 X是芳基。 Y选自氢或 其中（*）表示与X的连接点。

    Modulators of proteins with phosphotyrosine recognition units
    3.
    发明申请
    Modulators of proteins with phosphotyrosine recognition units 审中-公开
    具有磷酸酪氨酸识别单元的蛋白质的调节剂

    公开(公告)号：US20020183518A1

    公开(公告)日：2002-12-05

    申请号：US09995550

    申请日：2001-11-27

    申请人： ONTOGEN CORPORATION

    发明人： Adnan M. M. Mjalli ,  Xiaodong Cao ,  Edmund J. Moran

    IPC分类号： C07D265/32 ,  C07D211/60 ,  C07D295/08

    CPC分类号： C07D471/04

    摘要： YnullXnullC(Rnull)nullC(Rnull)COORnullnullnullnull(A1) The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryoic cells, whole animals and human beings. Rnull and Rnull are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. Rnullnull is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or 1 wherein (*) indicates a potential point of attachment to X.

    摘要翻译： 在线公式中YXC（R'）= C（R“'）COOR”'（A1）本发明涉及新蛋白酪氨酸 具有式（A1）所示的一般结构的磷酸酶调节化合物，其制备方法，包含该化合物的组合物，其用于治疗人和动物病症的用途，其用于蛋白质或糖蛋白的纯化及其用途 用于诊断。 本发明涉及在体外系统，微生物，真核细胞，整个动物和人类中调节具有磷酸酪氨酸识别单元的分子的活性，包括蛋白酪氨酸磷酸酶（PTP酶）和具有Src同源性-2结构域的蛋白质。 R'和R“独立地选自氢，卤素，氰基，硝基，三卤代甲基，烷基，芳基烷基。 R“选自氢，烷基，取代的烷基，芳基，芳基烷基。 X是芳基。 Y选自氢或其中（*）表示与X连接的潜在点。

    Naphthalenedione nitric oxide synthase (NOS) inhibitors
    4.
    发明授权
    Naphthalenedione nitric oxide synthase (NOS) inhibitors 失效

    公开(公告)号：US5866569A

    公开(公告)日：1999-02-02

    申请号：US928183

    申请日：1997-09-12

    申请人： Adnan M. M. Mjalli ,  Sepehar Sarshar ,  Chengzhi Zhang

    发明人： Adnan M. M. Mjalli ,  Sepehar Sarshar ,  Chengzhi Zhang

    IPC分类号： A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/12 ,  A61K31/415

    CPC分类号： A61K31/495 ,  A61K31/496

    摘要： There are disclosed methods useful for the inhibition of inducible nitric oxide synthase by the adminstration of a compound of the formula I:. when R.sub.2 is H then R.sub.1 is selected from the group consisting of:1) aryl,--NH--C.sub.0 -C.sub.10 alkyl -aryl, N-(C.sub.0 -C.sub.10 alkyl substituted aryl).sub.2, --C.sub.0 -C.sub.10 alkyl substituted aryl, --N(C.sub.0 -C.sub.10 alkyl substituted aryl)(C.sub.0 -C.sub.10 alkyl), wherein "Aryl" is optionally attached to Compound I through C or N and is selected from the group consisting of isoindanolyl, isoindolinyl, tetrahydroquinolyl, phenyl, naphthyl, pyridyl, furyl, pyrryl, thienyl, isothiazolyl, imidazolyl, benzimidazolyl, triazolyl, tetrazolyl, pyrazinyl,pyrimidyl, quinolyl, isoquinolyl, benzofuryl, benzothienyl, pyrazolyl, indolyl, isoindolyl, purinyl, carbazolyl, isoxazolyl, thiazolyl, oxazolyl, benzthiazolyl, and benzoxazolyl; and the term "substituted aryl" denotes mono-, di- and/or tri-substituted aryl wherein aryl is as defined above and in which the substituents are independently selected from the group consistng of H, trifluoromethyl, amino, hydroxy, halo, nitro, --O--C.sub.1 -C.sub.6 alkyl, --S--C.sub.1 -C.sub.6 alkyl, --NH--C.sub.1 -C.sub.6 alkyl, --N (C.sub.1 -C.sub.6 allyl).sub.2, --C(O) --C.sub.1 -C.sub.6 alkyl, --NHC(O) C.sub.1 -C.sub.6 alkyl, --C.sub.1 -C.sub.11 COO.sub.2 R wherein R.dbd.C.sub.1 -C.sub.11 alkyl, or --C.sub.1 -C.sub.11 alkylphenyl, --C.sub.1 -C.sub.11 CONHR wherein R.dbd.C.sub.1 -C.sub.11 alkyl or C.sub.1 -C.sub.11 alkylphenyl, carboxy, --C(O) O C.sub.1 -C.sub.6 alkyl; trans-CH.dbd.CHCO.sub.2 R; wherein R.dbd.C.sub.1 -C.sub.11 alkyl or C.sub.1 -C.sub.6 alkylphenyl, trans CH.dbd.CHCONHR; wherein R.dbd.C.sub.1 -C.sub.11 alkyl or C.sub.1 -C.sub.11 alkylphenyl;2) cyclic --N(CH.sub.2 CH.sub.2).sub.2 Y, cyclic NCHA(CH.sub.2).sub.3, or --NH C.sub.2 -C.sub.11 alkyl-Y wherein A=i) C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkylaryl or,ii) COZR.sub.3 wherein Z=oxygen, NH and R.sub.3 =H, or C.sub.1 -C.sub.10 alkyl, or C.sub.0 -C.sub.10 alkylaryl wherein aryl group is as defined in (1) above, and Y=i) oxygen,or S, or NH orii) NC.sub.0 -C.sub.10 alkyl oriii) NC.sub.1 -C.sub.10 alkylsubstituted aryl,iv) NC=ZMR.sub.3 or COZR.sub.3 wherein Z=oxygen, or NH; M=C, oxygen, N, and R.sub.3 is C.sub.0 -C.sub.10 alkyl substituted aryl; wherein Z is as defined in (2iv) above and R.sub.3 is C.sub.0 -C.sub.10 alkylsubstituted aryl wherein "substituted aryl" is as defined above.; R.sub.2 is hydrogen; or R.sub.1 and R.sub.2 taken together forming another aryl group; and X is hydrogen, halo, alkyl, alkoxy, hydroxy, nitro, amino, trifluoromethyl and aryl, to a patient in need of such inhibition such as hypotension, inflammtion, autoimmune diseases, and septic shock and the like.

    Sample wash station assembly
    8.
    发明授权
    Sample wash station assembly 失效

    公开(公告)号：US5976470A

    公开(公告)日：1999-11-02

    申请号：US87376

    申请日：1998-05-29

    申请人： Romaine Maiefski ,  Don Wendell

    发明人： Romaine Maiefski ,  Don Wendell

    IPC分类号： G01N1/14 ,  B01J19/00 ,  C40B60/14 ,  G01N1/34 ,  G01N35/10

    CPC分类号： G01N35/1067 ,  B01J19/0046 ,  B01J2219/00313 ,  B01J2219/00351 ,  B01J2219/00373 ,  B01J2219/00376 ,  B01J2219/00389 ,  B01J2219/00391 ,  B01J2219/00416 ,  B01J2219/00418 ,  B01J2219/00484 ,  C40B60/14 ,  G01N35/1065 ,  Y10T436/11 ,  Y10T436/25 ,  Y10T436/2575

    摘要： A wash station assembly and method for washing selected samples in a sample containing assembly. The wash station assembly includes a wash station having a frame and a fluid dispensing assembly connected to the frame. The fluid dispensing assembly has a selector valve that is connectable to a plurality of fluid lines and is adjustable to allow only one of the fluids to pass through the selector valve at a time. An array of syringes is coupled to the selector valve and positioned to receive the fluid passing through the selector valve. Each syringe includes a check valve that prevents backflow of fluid or air into the syringe through the pipetting needles. A distribution manifold is connected to the selector valve and receives the fluid passing through the selector valve. The manifold has a plurality of distribution channels coupled to the syringes, to direct the fluid into the syringes. Each distribution channel has a manifold valve therein that prevents backflow of fluid into the manifold from the syringes. An array of pipetting needles is connected to the syringes and is positioned to direct the fluid into the sample containing assembly for washing the samples. The pipetting needles have a radially directed opening in the distal end to direct the fluid radially away from the needle during the dispensing process. A waste management system is connected to the wash station to automatically separate halogenated waste fluids from non-halogenated waste fluids.