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    Compounds useful as alkaline phosphatase inhibitors and therapeutic agents
    1.
    发明授权
    Compounds useful as alkaline phosphatase inhibitors and therapeutic agents 失效
    可用作碱性磷酸酶抑制剂和治疗剂的化合物

    公开(公告)号：US5516647A

    公开(公告)日：1996-05-14

    申请号：US148142

    申请日：1993-11-05

    申请人： Mazhar Husain ,  Dominique Bridon ,  Mark Bures ,  James D. Ratajczyk ,  Fortuna Haviv ,  Christopher Bieniarz

    发明人： Mazhar Husain ,  Dominique Bridon ,  Mark Bures ,  James D. Ratajczyk ,  Fortuna Haviv ,  Christopher Bieniarz

    IPC分类号： C07D513/04 ,  C12Q1/42 ,  C07D513/02

    CPC分类号： C07D513/04 ,  C12Q1/42 ,  Y10S435/81

    摘要： The present invention discloses novel compounds useful as alkaline phosphatase inhibitors and therapeutic agents. Preferably, the novel compounds are useful as selective inhibitors of human alkaline phosphatases as opposed to Escherichia coli alkaline phosphatases. The novel compounds can also be used as cancer therapeutic agents, anti-depressive agents, anti-anergic agents, and antihelminthic agents. The novel compounds have the following general formula: ##STR1## wherein R' is an aryl, aryl ether, aryl thioether, aromatic heterocyclic, aromatic heterocyclic thioether, or aromatic heterocyclic ether group. More preferably, R' is a phenyl or a pyridine. Most preferably, R' is of the following formula: ##STR2## 2-thiopyridine, or ##STR3## 2-oxypyridine. R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.1 ', R.sub.2 ', R.sub.3 ', R.sub.4 ', and R.sub.5 ' can be the same or different, and at least one of which is selected from the group consisting of: H, C.sub.1 -C.sub.6 alkyl, halo C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, nitro, amino, carboxy, and halo groups with the proviso that each novel compound has no more than three substituents. Hydrogen is not considered a substituent.

    摘要翻译： 本发明公开了可用作碱性磷酸酶抑制剂和治疗剂的新化合物。 优选地，新化合物可用作人碱性磷酸酶的选择性抑制剂，与大肠杆菌碱性磷酸酶相反。 新化合物也可以用作癌症治疗剂，抗抑郁剂，抗过敏剂和抗栓剂。 新化合物具有以下通式：其中R'为芳基，芳基醚，芳基硫醚，芳族杂环，芳族杂环硫醚或芳族杂环醚基团。 更优选地，R'是苯基或吡啶。 最优选地，R'具有下列结构式：2-甲基吡啶或2-氧代吡啶。 R1，R2，R3，R4，R1'，R2'，R3'，R4'和R5'可以相同或不同，其中至少一个选自：H，C 1 -C 6烷基 ，卤素C 1 -C 6烷基，苯基，C 1 -C 6烷氧基，苯氧基，三氟甲基，硝基，氨基，羧基和卤素基团，条件是每个新化合物不超过三个取代基。 氢不被认为是取代基。

    Method of treatment of diabetes and/or obesity with reduced nausea side effect
    2.
    发明申请
    Method of treatment of diabetes and/or obesity with reduced nausea side effect 失效
    减少恶心副作用的糖尿病和/或肥胖症的治疗方法

    公开(公告)号：US20070207958A1

    公开(公告)日：2007-09-06

    申请号：US11595576

    申请日：2006-11-09

    申请人： Dominique Bridon ,  Jean-Paul Castaigne ,  Karen Thibaudeau

    发明人： Dominique Bridon ,  Jean-Paul Castaigne ,  Karen Thibaudeau

    IPC分类号： A61K38/22

    CPC分类号： A61K38/26 ,  A61K47/643

    摘要： The present invention provides methods of administering an insulinotropic peptide in an amount effective to treat a disorder or condition while reducing nausea side effect by administering to a subject in need thereof an insulinotropic peptide conjugated to albumin. The present invention also provides methods of selecting a subject for administration of a conjugated insulinotropic peptide. Exemplary disorders or conditions treatable with an insulinotropic peptide include obesity and type II diabetes.

    摘要翻译： 本发明提供以有效治疗病症或病症的量施用促胰岛素肽的方法，同时通过向有需要的受试者施用与白蛋白缀合的促胰岛素肽来减轻恶心副作用。 本发明还提供了选择用于给予共轭促胰岛素肽的受试者的方法。 用促胰岛素肽治疗的示例性疾病或病症包括肥胖症和II型糖尿病。

    Long lasting natriuretic peptide derivatives
    4.
    发明申请
    Long lasting natriuretic peptide derivatives 审中-公开
    持久的利钠肽衍生物

    公开(公告)号：US20050176641A1

    公开(公告)日：2005-08-11

    申请号：US11040810

    申请日：2005-01-21

    申请人： Peter Bakis ,  Dominique Bridon ,  Julie Carette ,  France Leclaire ,  Roger Leger ,  Martin Robitaille

    发明人： Peter Bakis ,  Dominique Bridon ,  Julie Carette ,  France Leclaire ,  Roger Leger ,  Martin Robitaille

    IPC分类号： A61K38/17 ,  C07K7/08 ,  C07K14/47

    CPC分类号： A61K38/2242 ,  A61K47/62

    摘要： This invention relates to long lasting natriuretic peptide (NP) derivatives. The NP derivative has a NP peptide and a reactive entity coupled to the NP peptide. The reactive entity is able to covalently bond with a functionality on a blood component. In particular, this invention relates to NP derivatives having an extended in vivo half-life, and method for the treatment of cardiovascular diseases and disorders such as acute decompensated congestive heart failure (CHF) and chronic CHF.

    摘要翻译： 本发明涉及长效利钠肽（NP）衍生物。 NP衍生物具有NP肽和与NP肽偶联的反应性实体。 反应性实体能够与血液成分上的官能团共价键合。 特别地，本发明涉及具有延长的体内半衰期的NP衍生物，以及用于治疗心血管疾病和疾病如急性失代偿性充血性心力衰竭（CHF）和慢性CHF的方法。

    Affinity markers for human serum albumin
    5.
    发明申请
    Affinity markers for human serum albumin 失效
    人血清白蛋白的亲和标记

    公开(公告)号：US20050037974A1

    公开(公告)日：2005-02-17

    申请号：US10934841

    申请日：2004-09-02

    申请人： Alexander Krantz ,  Wolin Huang ,  Arthur Hanel ,  Darren Holmes ,  Dominique Bridon

    发明人： Alexander Krantz ,  Wolin Huang ,  Arthur Hanel ,  Darren Holmes ,  Dominique Bridon

    IPC分类号： A61K38/00 ,  A61K47/48 ,  A61K49/00 ,  C07K14/665 ,  A61K38/08 ,  C07K7/06

    CPC分类号： A61K49/0021 ,  A61K38/00 ,  A61K47/62 ,  A61K47/6901 ,  A61K49/0043 ,  A61K49/0056 ,  C07K14/665

    摘要： Methods and compositions are provided for identifying compounds having affinity or complementarity to a target molecule. Compounds according to the invention may be described by the formula E-Ca—R—Cb-A, wherein E is a therapeutic or diagnostic agent, R is a reactive group, Ca and Cb are connector groups between E and R and between R and A, respectively, and A is a group having an affinity for human serum albumin, wherein affinity group A comprises a sequence of amino acid residues —O1—O2—X1—X2—B in which the amino acid residues are independently selected from the group of all twenty naturally occurring amino acids. Compounds according to the invention may be used for labeling the target molecule, particularly where the target molecule is naturally found in a complex mixture, such as a physiological fluid, like blood. By affinity labeling in vivo, the lifetime of physiologically active entities can be greatly enhanced by becoming bound to long-lived blood components. The covalently bound entity may also serve as an antagonist or agonist of a particular binding protein or as an enzyme inhibitor.

    摘要翻译： 提供了用于鉴定与靶分子具有亲和力或互补性的化合物的方法和组合物。 根据本发明的化合物可以由式E-Ca-R-Cb-A描述，其中E是治疗或诊断剂，R是反应性基团，Ca和Cb是E和R之间的连接基团，R和 A，A是对人血清白蛋白具有亲和性的基团，其中亲和基团A包含氨基酸残基-O1-O2-X1-X2-B的序列，其中氨基酸残基独立地选自 的二十种天然存在的氨基酸。 根据本发明的化合物可以用于标记靶分子，特别是当目标分子天然存在于复杂混合物如生理液体如血液中时。 通过体内亲和标记，生理活性实体的寿命可以通过与长寿命的血液成分结合而大大增强。 共价结合的实体也可以用作特异性结合蛋白的拮抗剂或激动剂或作为酶抑制剂。