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    Protein tyrosine phosphatase-inhibiting compounds
    6.
    发明授权
    Protein tyrosine phosphatase-inhibiting compounds 失效
    蛋白酪氨酸磷酸酶抑制化合物

    公开(公告)号：US06388076B1

    公开(公告)日：2002-05-14

    申请号：US09645785

    申请日：2000-08-24

    Applicant: Adnan Mjalli ,  Sepehr Sarshar ,  Xiaodong Cao ,  Farid Bakir

    Inventor： Adnan Mjalli ,  Sepehr Sarshar ,  Xiaodong Cao ,  Farid Bakir

    IPC: C07D47104

    CPC classification number: C07D471/04

    Abstract: Y—X—C(R′)═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 wherein (*) indicates a potential point of attachment to X.

    Abstract translation: 本发明涉及具有式（A1）所示的一般结构的新型蛋白质酪氨酸磷酸酶调节化合物，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，用于其纯化 的蛋白质或糖蛋白，以及它们在诊断中的用途。 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。

    Peptidyl derivatives as inhibitors of interleukin-1.beta. converting enzyme
    7.
    发明授权
    Peptidyl derivatives as inhibitors of interleukin-1.beta. converting enzyme 失效
    肽基衍生物作为白细胞介素-1β转换酶的抑制剂

    公开(公告)号：US5430128A

    公开(公告)日：1995-07-04

    申请号：US342991

    申请日：1994-11-21

    Applicant: Kevin T. Chapman ,  Malcolm MacCoss ,  Adnan Mjalli

    Inventor： Kevin T. Chapman ,  Malcolm MacCoss ,  Adnan Mjalli

    IPC: A61K38/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/08 ,  C07K5/00 ,  C07K7/00 ,  C07K17/00

    CPC classification number: C07K5/0202 ,  A61K38/00

    Abstract: Novel peptidyl derivatives of formula I are found to be potent inhibitors of interleukin-1.beta. converting enzyme (ICE). Compounds of formula I may be useful in the treatment of inflammatory or immune-based diseases of the lung and airways; central nervous system and surrounding membranes; the eyes and ears; joints, bones, and connective tissues; cardiovascular system including the pericardium; the gastrointestinal and urogenital systems; the skin and mucosal membranes. Compounds of formula I are also useful in treating the complications of infection (e.g., gram negative shock) and tumors in which IL 1 functions as an autocrine growth factor or as a mediator of cachexia. ##STR1##

    Abstract translation: 发现式I的新型肽基衍生物是白细胞介素-1β转换酶（ICE）的有效抑制剂。 式I化合物可用于治疗肺和气道炎性或免疫性疾病; 中枢神经系统和周围膜; 眼睛和耳朵 关节，骨骼和结缔组织; 包括心包的心血管系统; 胃肠道和泌尿生殖系统; 皮肤和粘膜。 式I化合物也可用于治疗感染（例如，革兰氏阴性休克）的并发症和其中IL1作为自分泌生长因子或作为恶病质介质的肿瘤。

    Carboxamide Derivatives as Therapeutic Agents
    8.
    发明申请
    Carboxamide Derivatives as Therapeutic Agents 失效
    甲酰胺衍生物作为治疗剂

    公开(公告)号：US20080119512A1

    公开(公告)日：2008-05-22

    申请号：US12019045

    申请日：2008-01-24

    Applicant: Adnan Mjalli ,  Robert Andrews ,  Ramosh Gopalaswamy ,  Chris Wysong

    Inventor： Adnan Mjalli ,  Robert Andrews ,  Ramosh Gopalaswamy ,  Chris Wysong

    IPC: A61K31/4704 ,  A61K31/165 ,  A61K31/4462

    CPC classification number: C07D231/12 ,  C07C235/38 ,  C07C237/20 ,  C07C271/22 ,  C07C2601/08 ,  C07C2603/18 ,  C07D207/16 ,  C07D211/34 ,  C07D217/26 ,  C07D233/56 ,  C07D249/08 ,  C07D309/04

    Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

    Abstract translation: 本发明提供某些化合物，其制备方法，包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作晚期糖基化终产物（RAGE）的受体与其配体如晚期糖基化终产物（AGE），S100 /钙粒蛋白/ EN-RAGE，β-淀粉样蛋白和两性蛋白之间相互作用的调节剂 ，以及由RAGE引起的人类疾病的管理，治疗，控制或辅助治疗。 这些疾病或疾病状态包括急性和慢性炎症，糖尿病晚期并发症的发展，例如血管通透性增加，肾病，动脉粥样硬化和视网膜病变，阿尔茨海默病的发展，勃起功能障碍和肿瘤侵袭和转移。

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