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    Heterobifunctional pan-selectin inhibitors
    3.
    发明授权
    Heterobifunctional pan-selectin inhibitors 有权
    异双功能泛选择素抑制剂

    公开(公告)号：US07728117B2

    公开(公告)日：2010-06-01

    申请号：US11515343

    申请日：2006-09-01

    Applicant: John L. Magnani ,  John T. Patton, Jr. ,  Arun K. Sarkar ,  Sergei A. Svarovsky ,  Beat Ernst

    Inventor： John L. Magnani ,  John T. Patton, Jr. ,  Arun K. Sarkar ,  Sergei A. Svarovsky ,  Beat Ernst

    IPC: C07H17/04 ,  C07H15/22

    CPC classification number: A61K31/706 ,  A61K47/549 ,  C07H15/22 ,  C07H15/26 ,  C07H17/00

    Abstract: Compounds and methods are provided for modulating in vitro and in vivo processes mediated by selectin binding. More specifically, selectin modulators and their use are described, wherein the selectin modulators that modulate (e.g., inhibit or enhance) a selectin-mediated function comprise particular glycomimetics alone or linked to a member of a class of compounds termed BASAs (Benzyl Amino Sulfonic Acids) or a member of a class of compounds termed BACAs (Benzyl Amino Carboxylic Acids).

    Abstract translation: 提供化合物和方法用于调节由选择素结合介导的体外和体内过程。 更具体地，描述了选择素调节剂及其用途，其中调节（例如，抑制或增强）选择素介导的功能的选择素调节剂单独包含特定的糖模拟物或连接到称为BASAs的化合物类别（苄基氨基磺酸 ）或称为BACAs（苄基氨基羧酸）的一类化合物的成员。

    Pan-selectin inhibitor with enhanced pharmacokinetic activity
    4.
    发明授权
    Pan-selectin inhibitor with enhanced pharmacokinetic activity 有权
    Pan-selectin抑制剂具有增强的药代动力学活性

    公开(公告)号：US08895510B2

    公开(公告)日：2014-11-25

    申请号：US12418774

    申请日：2009-04-06

    Applicant: John L. Magnani

    Inventor： John L. Magnani

    IPC: A61K31/7064 ,  C07H15/22 ,  A61P9/10

    CPC classification number: C07H15/26 ,  A61K31/7034 ,  A61K31/7036 ,  A61K31/7064 ,  C07H15/22

    Abstract: Compounds, compositions and methods are provided for treatment of diseases or complications associated therewith, in which a selectin plays a role. More specifically, particular glycomimetics and uses thereof are described. For example, use of particular glycomimetics for treating sickle cell disease or a cancer involving a selectin, or complications associated with either, is described.

    Abstract translation: 提供化合物，组合物和方法用于治疗与其相关的疾病或并发症，其中选择素起作用。 更具体地，描述了特定的糖模拟物及其用途。 例如，描述了使用特定的糖模拟物来治疗镰状细胞病或涉及选择蛋白的癌症，或与之有关的并发症。

    GLYCOMIMETIC INHIBITORS OF SIGLEC-8
    6.
    发明申请
    GLYCOMIMETIC INHIBITORS OF SIGLEC-8 审中-公开
    SIGCOM-8的GLYCOMIMETIC INHIBITORS

    公开(公告)号：US20090175792A1

    公开(公告)日：2009-07-09

    申请号：US12304879

    申请日：2007-06-19

    Applicant: John L. Magnani ,  Arun K. Sarkar

    Inventor： John L. Magnani ,  Arun K. Sarkar

    IPC: A61K49/00 ,  C12N5/02 ,  A61K31/35

    CPC classification number: A61K31/7036 ,  A61K31/7012

    Abstract: Compounds, compositions and methods are provided for detecting or modulating in vitro and in vivo processes mediated by Siglec-8 binding. More specifically, Siglec-8 modulators and their use are described, wherein the Siglec-8 modulators that modulate a Siglec-8-mediated function comprise particular glycomimetics alone or linked to a diagnostic or therapeutic agent.

    Abstract translation: 提供化合物，组合物和方法用于检测或调节由Siglec-8结合介导的体外和体内过程。 更具体地，描述了Siglec-8调节剂及其用途，其中调节Siglec-8介导的功能的Siglec-8调节剂单独包含特定的糖模拟物或与诊断或治疗剂连接。

    Heterobifunctional compounds for selectin inhibition
    7.
    发明申请
    Heterobifunctional compounds for selectin inhibition 审中-公开
    用于选择素抑制的异双功能化合物

    公开(公告)号：US20090036386A1

    公开(公告)日：2009-02-05

    申请号：US11920499

    申请日：2006-05-24

    Applicant: John L. Magnani ,  Arun K. Sarkar ,  John T. Patton, JR.

    Inventor： John L. Magnani ,  Arun K. Sarkar ,  John T. Patton, JR.

    IPC: A61K31/7042 ,  C07H17/04

    CPC classification number: C07H17/04 ,  C07H19/056

    Abstract: Compounds and methods are provided for modulating in vitro and in vivo processes mediated by selectin binding. More specifically, selectin modulators and their use are described, wherein the selectin modulators that modulate (e.g., inhibit or enhance) a selectin-mediated function comprise glycomimetics linked to a compound, for example a member of a class of compounds termed BASAs (Benzyl Amino Sulfonic Acids) or a member of a class of compounds termed BACAs (Benzyl Amino Carboxylic Acids).

    Abstract translation: 提供化合物和方法用于调节由选择素结合介导的体外和体内过程。 更具体地，描述了选择素调节剂及其用途，其中调节（例如，抑制或增强）选择素介导的功能的选择素调节剂包括与化合物连接的糖模拟物，例如称为BASAs的化合物类别（苄基氨基 磺酸）或称为BACAs（苄基氨基羧酸）的一类化合物的成员。

    Specific antagonist for both E- and P-selectins
    8.
    发明授权
    Specific antagonist for both E- and P-selectins 有权
    E-和P-选择素的特异性拮抗剂

    公开(公告)号：US07361644B2

    公开(公告)日：2008-04-22

    申请号：US10992480

    申请日：2004-11-18

    Applicant: John L. Magnani ,  John T. Patton, Jr.

    Inventor： John L. Magnani ,  John T. Patton, Jr.

    IPC: A61K31/7072 ,  C08B37/00

    CPC classification number: C07H15/18

    Abstract: Compounds and methods are provided for modulating in vitro and in vivo processes mediated by selectin binding. More specifically, selectin modulators and their use are described, wherein the selectin modulators that modulate (e.g., inhibit or enhance) a selectin-mediated function comprise a particular glycomimetic linked to a particular BASA (Benzyl Amino Sulfonic Acid).

    Abstract translation: 提供化合物和方法用于调节由选择素结合介导的体外和体内过程。 更具体地，描述了选择素调节剂及其用途，其中调节（例如抑制或增强）选择素介导的功能的选择素调节剂包含与特定BASA（苄基氨基磺酸）连接的特定的糖模拟物。

    Methods and compositions for the inhibition of cancer metastasis mediated by endothelial adhesion molecules
    9.
    发明授权
    Methods and compositions for the inhibition of cancer metastasis mediated by endothelial adhesion molecules 失效
    用于抑制内皮粘附分子介导的癌转移的方法和组合物

    公开(公告)号：US06465434B1

    公开(公告)日：2002-10-15

    申请号：US09447532

    申请日：1999-11-23

    Applicant: John L. Magnani ,  Eugene C. Butcher ,  Ellen L. Berg

    Inventor： John L. Magnani ,  Eugene C. Butcher ,  Ellen L. Berg

    IPC: A01N4304

    CPC classification number: C07H13/04 ,  A61K38/47 ,  A61K47/56 ,  C07K14/70564 ,  C07K16/30

    Abstract: Methods and compositions are disclosed for the inhibition of cancer metastases mediated by endothelial adhesion molecules. The present invention discloses that sialyl Lea and di-sialyl Lea, which are expressed at the surface of cancer cells, function as a binding partner for LEC-CAMs, such as ELAM-1, which are expressed at the surface of endothelial cells. The present invention also discloses that LEC-CAMs, such as ELAM-1, involved in cancer metastasis share a carbohydrate domain common to both sialyl Lea and sialyl Lex. Antibodies, saccharides, glycoconjugates, enzyme inhibitors and other compounds may be used in the methods of the present invention to inhibit the binding of malignant cells to endothelial cells for a variety of purposes in vivo and in vitro.

    Abstract translation: 公开了用于抑制由内皮粘附分子介导的癌转移的方法和组合物。 本发明公开了在癌细胞表面表达的唾液酸Lea和二唾液酸Lea作为LEC-CAM的结合配偶体，如在内皮细胞表面表达的ELAM-1。 本发明还公开了涉及癌症转移的LEC-CAM，如ELAM-1，共享唾液酸Lea和唾液酸Lex共同的碳水化合物结构域。 抗体，糖，糖缀合物，酶抑制剂和其它化合物可用于本发明的方法中，以体内和体外抑制恶性细胞与内皮细胞的结合，用于多种目的。

    Methods and compositions for endothelial binding
    10.
    发明授权
    Methods and compositions for endothelial binding 失效
    用于内皮结合的方法和组合物

    公开(公告)号：US06391857B1

    公开(公告)日：2002-05-21

    申请号：US08336466

    申请日：1994-11-09

    Applicant: John L. Magnani ,  Eugene C. Butcher ,  Ellen L. Berg

    Inventor： John L. Magnani ,  Eugene C. Butcher ,  Ellen L. Berg

    IPC: A61K3170

    CPC classification number: C07H13/04 ,  A61K38/47 ,  A61K47/56 ,  C07K14/705 ,  C07K14/70564 ,  C07K16/30 ,  Y10S530/807

    Abstract: Novel methods and compositions are provided for modulating homing of leukocytes, particularly lympho-cytes, where the compounds are cross-reactive with Neu5Ac2-3Gal&bgr;1-X[Fuc&agr;1-y]GlcNAc, where one of x and y is three and the other is four. These compounds may be administered to a host associated with inflammation, to avoid the deleterious effects of leukocyte infiltration and for directing molecules to such sites.

    Abstract translation: 提供新的方法和组合物用于调节白细胞，特别是淋巴细胞的归巢，其中化合物与Neu5Ac2-3Galbeta1-X [Fucalpha1-y] GlcNAc交叉反应，其中x和y之一是三个，另一个是四个 。 这些化合物可以施用于与炎症相关的宿主，以避免白细胞浸润的有害作用并将分子引导到这些位点。

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