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    Novel compounds
    3.
    发明申请
    Novel compounds 审中-公开
    新型化合物

    公开(公告)号：US20040209822A1

    公开(公告)日：2004-10-21

    申请号：US10844699

    申请日：2004-05-13

    Applicant: SmithKline Beecham p.l.c.

    Inventor： Andrew Faller ,  Anne-Geraldine Rousseau ,  David Timothy MacPherson ,  Peter Henry Milner

    IPC: A61K038/04 ,  C07F005/00

    CPC classification number: C07C311/13 ,  C07C259/06 ,  C07D307/52

    Abstract: Compounds of the formula (I): 1 wherein: X1 is alkyl, sulphonyl or carboxy; X2 is hydrogen or alkyl; R1 is arylmethyl or heterocycylmethyl; R2 is alkyl, alkenyl, cycloalkyl or cycloalkenyl; and R3 is hydrogen, alkyl, alkenyl, alkynyl or aryl; are useful in the treatment of disorders mediated by s-CD23.

    Abstract translation: 式（I）的化合物：其中：X 1是烷基，磺酰基或羧基; X 2是氢或烷基; R 1是芳基甲基或杂环基甲基; R 2是烷基，烯基，环烷基或环烯基; 和R 3是氢，烷基，烯基，炔基或芳基; 可用于治疗由s-CD23介导的疾病。

    Oxadiazole derivative compounds and drugs containing these compounds as the active ingredient
    4.
    发明申请
    Oxadiazole derivative compounds and drugs containing these compounds as the active ingredient 审中-公开
    恶二唑衍生物化合物和含有这些化合物作为活性成分的药物

    公开(公告)号：US20040204368A1

    公开(公告)日：2004-10-14

    申请号：US10479254

    申请日：2003-12-01

    Inventor： Kazuyuki Ohmoto ,  Kazuhito Kawabata

    IPC: A61K038/04 ,  C07K005/04

    CPC classification number: C07D271/113 ,  A61K38/00 ,  C07K5/06139

    Abstract: An oxadiazole derivative of formula (I) and a non-toxic salt thereof, 1 wherein all symbols have the same meaning as described in the specification. The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of inflammatory diseases, diseases induced by apoptosis, diseases induced by disorders of immune responses, autoimmune diseases, diseases induced by decomposition of proteins which compose organism, shock, circulatory system disorders, blood coagulation system(s) disorders, malignant tumors, acquired immune deficiency syndrome (AIDS) and AIDS-related complex (ARC), parasitic diseases, nerve degeneration diseases, pulmonary disorders, bone resorption diseases, endocrinesthenia, etc.

    Abstract translation: 式（I）的恶二唑衍生物及其无毒盐，其中所有符号具有与说明书中所述相同的含义。 式（I）化合物对半胱氨酸蛋白酶具有抑制活性，因此可用作预防和/或治疗炎性疾病，由凋亡诱导的疾病，由免疫应答障碍引起的疾病，自身免疫性疾病，疾病 由构成生物的蛋白质，休克，循环系统疾病，凝血系统疾病，恶性肿瘤，获得性免疫缺陷综合征（AIDS）和AIDS相关综合征（ARC），寄生虫病，神经变性疾病，肺部 疾病，骨吸收疾病，内分泌等。

    PH-dependent polypeptide aggregation and its use
    5.
    发明申请
    PH-dependent polypeptide aggregation and its use 审中-公开
    PH依赖多肽聚集及其应用

    公开(公告)号：US20040192887A1

    公开(公告)日：2004-09-30

    申请号：US10397059

    申请日：2003-03-25

    Inventor： Ralph Zahn

    IPC: C07K016/00 ,  C12Q001/70 ,  G01N033/53 ,  C07K007/00 ,  C07K017/00 ,  A61K038/04 ,  C07K001/00 ,  C07K014/00 ,  C07K005/00

    CPC classification number: C07K14/47

    Abstract: The invention provides an alternative method of reversible aggregation and/or dissociation of polypeptides. Proteins or polypeptides according to the invention have an inherent aggregation capability, wherein the aggregation is an oligomerization of the polypeptide that is based on the presence and the strucuture of peptide repeats localized in a flexibly disordered domain of this polypeptide. The flexibly disordered domain comprising the peptide repeats preferrably is located in close proximity with the N-terminus of the protein amino acid sequence. Preferably, each of the peptide repeats has a sequence that comprises one to four identical octapeptides with the amino acid sequence: PHGGGWGQ. Preferred proteins are selected from the group comprising cellular prion proteins (PrPC) and engineered polypeptides or fusion proteins with a respective inherent reversible aggregation and dissociation capability. Because of the new mechanism of aggregation, the oligomerization reaction of the protein is reversible in a fluidic environment depending on the pH of this fluidic environment. Oligomerization occurs at a pH of 6.2 to 7.8, and the dissociation into monomers is reported to be at a pH range of 4.5 to 5.5. 1

    Abstract translation: 本发明提供了多肽的可逆聚集和/或解离的替代方法。 根据本发明的蛋白质或多肽具有固有的聚集能力，其中聚集是多肽的寡聚化，其基于定位于该多肽的柔性无序结构域中的肽重复序列的存在和结构。 优选地，包含肽重复序列的柔性无序结构域位于蛋白质氨基酸序列的N-末端附近。 优选地，每个肽重复序列具有包含1-4个与氨基酸序列PHGGGWGQ相同的八肽的序列。 优选的蛋白质选自包含细胞朊蛋白（PrP））和具有相应固有的可逆聚集和解离能力的工程改造的多肽或融合蛋白。 由于聚合的新机制，蛋白质的低聚反应在流体环境中是可逆的，这取决于该流体环境的pH。 低聚发生在6.2至7.8的pH下，据报导单体的解离在4.5至5.5的pH范围内。

    Novel heteroaryl peptidomimetics as thrombin receptor antagonists
    7.
    发明申请
    Novel heteroaryl peptidomimetics as thrombin receptor antagonists 失效
    新型杂芳基肽模拟物作为凝血酶受体拮抗剂

    公开(公告)号：US20040138141A1

    公开(公告)日：2004-07-15

    申请号：US10732701

    申请日：2003-12-10

    Inventor： Han-Cheng Zhang ,  Bruce E. Maryanoff ,  William J. Hoekstra ,  Kimberly White

    IPC: A61K038/06 ,  A61K038/05 ,  A61K038/04

    CPC classification number: C07K5/06191 ,  C07K5/06095

    Abstract: The invention is directed to novel heteroaryl peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, angiogenesis and related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted heteroaryl peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.

    Abstract translation: 本发明涉及可用作凝血酶受体拮抗剂用于治疗与血栓形成，再狭窄，高血压，心力衰竭，心律失常，炎症，心绞痛，中风，动脉粥样硬化，缺血性疾病，血管生成和相关疾病相关的疾病的新型杂肽体模拟化合物， 癌症和神经变性疾病。 还公开了包含本发明的取代的杂芳基肽模拟物的药物组合物和治疗由凝血酶受体介导的病症的方法。

    Ketoamide inhibitors in chronic nerve disease
    8.
    发明申请
    Ketoamide inhibitors in chronic nerve disease 失效
    酮酰胺抑制剂在慢性神经疾病中的应用

    公开(公告)号：US20040127427A1

    公开(公告)日：2004-07-01

    申请号：US10671360

    申请日：2003-09-25

    Inventor： James C. Powers ,  Jonathan D. Glass

    IPC: A61K038/04

    CPC classification number: A61K45/06 ,  A61K38/04 ,  A61K2300/00

    Abstract: Compositions and methods for treating neural pathologies are provided. In particular, compositions and methods for treating neural pathologies including axonal degeneration are provided. The compositions include peptide null-ketomides optionally in combination with a second therapeutic agent. Another aspect of the invention provides compositions and methods for treating hyperproliferative disorders. Exemplary compositions for treating hyperproliferative disorders include an anti-proliferative agent such as paclitaxel, in combination with a calpain inhibitor such as AK295.

    Abstract translation: 提供了治疗神经病变的组合物和方法。 特别地，提供了用于治疗包括轴索变性的神经病变的组合物和方法。 组合物包括任选与第二治疗剂组合的肽α-酮基转移酶。 本发明的另一方面提供了用于治疗过度增殖性疾病的组合物和方法。 用于治疗过度增殖性疾病的示例性组合物包括与钙蛋白酶抑制剂如AK295组合的抗增殖剂如紫杉醇。

    Peptidic compounds as cysteine protease inhibitors
    9.
    发明申请
    Peptidic compounds as cysteine protease inhibitors 有权
    肽类化合物作为半胱氨酸蛋白酶抑制剂

    公开(公告)号：US20040127426A1

    公开(公告)日：2004-07-01

    申请号：US10603437

    申请日：2003-06-24

    Applicant: AXYS PHARMACEUTICALS, INC.

    Inventor： Michael Graupe ,  John O. Link

    IPC: A61K038/04 ,  A61K031/445 ,  A61K031/401 ,  A61K031/663

    CPC classification number: C07D263/56 ,  A61K38/00 ,  C07D413/12 ,  C07D417/12

    Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

    Abstract translation: 本发明涉及半胱氨酸蛋白酶，特别是组织蛋白酶B，K，L，F和S的抑制剂的化合物，因此可用于治疗由这些蛋白酶介导的疾病。 本发明涉及包含这些化合物的药物组合物及其制备方法。

    Prodrugs of excitatory amino acids
    10.
    发明申请
    Prodrugs of excitatory amino acids 失效
    兴奋性氨基酸的前药

    公开(公告)号：US20040121962A1

    公开(公告)日：2004-06-24

    申请号：US10250448

    申请日：2003-11-12

    Inventor： David Scott Coffey ,  James Allen Monn ,  Concepcion Pedregal-Tercero

    IPC: A61K038/04 ,  C07K005/04

    CPC classification number: C07C237/12 ,  C07C271/22 ,  C07C2602/18 ,  Y02P20/55

    Abstract: This invention relates to synthetic excitatory amino acid prodrugs according to formula (I) and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders. 1

    Abstract translation: 本发明涉及式（I）的合成兴奋性氨基酸前药及其制备方法。 本发明进一步涉及使用和药物组合物的方法，其包含用于治疗神经障碍和精神障碍的化合物。

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