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    Modified macrophage migration inhibitory factor inhibitors
    2.
    发明授权
    Modified macrophage migration inhibitory factor inhibitors 有权

    公开(公告)号：US08618147B2

    公开(公告)日：2013-12-31

    申请号：US13751530

    申请日：2013-01-28

    Applicant: Yousef Al-Abed

    Inventor： Yousef Al-Abed

    IPC: C07D261/04

    CPC classification number: C07D261/04 ,  A61K31/42 ,  A61K31/421 ,  A61K45/06 ,  Y02A50/385 ,  Y02A50/411 ,  A61K2300/00

    Abstract: Provided are various compounds of Formula I (I). Also provided are various compounds of Formula II (II). Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.

    METHOD FOR TREATING PATHOLOGIES ASSOCIATED WITH HYPOXIA USING MIF INHIBITORS
    4.
    发明申请
    METHOD FOR TREATING PATHOLOGIES ASSOCIATED WITH HYPOXIA USING MIF INHIBITORS 有权
    使用MIF抑制剂治疗与HYPOXIA相关的病理学的方法

    公开(公告)号：US20130004506A1

    公开(公告)日：2013-01-03

    申请号：US13528350

    申请日：2012-06-20

    Applicant: Edmund Miller ,  Yousef Al-Abed ,  Yinzhong Zhang ,  Kai Fan Cheng

    Inventor： Edmund Miller ,  Yousef Al-Abed ,  Yinzhong Zhang ,  Kai Fan Cheng

    IPC: A61K31/42 ,  A61P9/12 ,  A61P25/00 ,  A61P25/28 ,  A61P9/00 ,  A61P25/22 ,  A61P25/24 ,  A61K39/395 ,  A61P11/00

    CPC classification number: A61K31/42 ,  A61K2039/505 ,  C07K16/24 ,  C07K2317/70

    Abstract: Methods are provided for treating pathologies associated with hypoxia with an MIF inhibitor. Methods are also provided for treating a subject having, or at risk for pulmonary hypertension, with an MIF inhibitor. Methods are also provided for treating a subject having, or at risk from, a CNS disorder associated with hypoxia, with an MIF inhibitor. Methods are also provided of treating severe chronic lung disease, hypoxia-induced right ventricular hypertrophy or hypoxia-induced pulmonary vascular remodeling with an MIF inhibitor. Methods of diagnosing a subject with pulmonary hypertension are also provided.

    Abstract translation: 提供了用MIF抑制剂治疗与缺氧相关的病症的方法。 还提供了用MIF抑制剂治疗患有或具有肺动脉高压风险的受试者的方法。 还提供了用MIF抑制剂治疗具有或与其相关的CNS紊乱或具有风险的受试者的方法。 还提供治疗严重慢性肺部疾病，缺氧诱导的右心室肥大或缺氧诱导的肺血管重塑与MIF抑制剂的方法。 还提供了诊断患有肺动脉高压的受试者的方法。

    Compounds having MIF antagonist activity
    5.
    发明授权
    Compounds having MIF antagonist activity 有权
    具有MIF拮抗剂活性的化合物

    公开(公告)号：US06599938B1

    公开(公告)日：2003-07-29

    申请号：US09699258

    申请日：2000-10-27

    Applicant: Yousef Al-Abed ,  Richard J. Bucala

    Inventor： Yousef Al-Abed ,  Richard J. Bucala

    IPC: A61K3124

    CPC classification number: C07D209/20 ,  C07C251/24 ,  C07C323/58

    Abstract: There is disclosed a genus of optionally substituted Schiff base condensation products (and the carba analogs thereof) comprising an amino acid component and a benzaldehyde component, that have MIF (macrophage migration inhibitory factor) antagonist activity. The compounds are useful for treating a variety of diseases involving inflammatory activity or pro-inflammatory cytokine responses, such as autoimmune diseases, asthma, arthritis, EAE, ARDS and various forms of sepsis and septic shock, and other conditions characterized by underlying MIF responses including, for instance, tumor growth and neovascularization.

    Abstract translation: 公开了包含具有MIF（巨噬细胞迁移抑制因子）拮抗剂活性的氨基酸组分和苯甲醛组分的任选取代的席夫碱缩合产物（及其咔唑类似物）。 这些化合物可用于治疗涉及炎症活性或促炎细胞因子应答的各种疾病，例如自身免疫性疾病，哮喘，关节炎，EAE，ARDS和各种形式的败血症和败血性休克，以及以下MIF反应为特征的其他病症，包括 ，例如肿瘤生长和新血管形成。

    Phenolic hydrazone macrophage migration inhibitory factor inhibitors
    7.
    发明授权
    Phenolic hydrazone macrophage migration inhibitory factor inhibitors 失效
    酚腙巨噬细胞迁移抑制因子抑制剂

    公开(公告)号：US08742173B2

    公开(公告)日：2014-06-03

    申请号：US13418877

    申请日：2012-03-13

    Applicant: Yousef Al-Abed

    Inventor： Yousef Al-Abed

    IPC: C07C251/86

    CPC classification number: C07C251/86 ,  C07C281/02 ,  C07C311/49

    Abstract: Provided are various compounds of Formula (I): Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.

    Abstract translation: 提供式（I）的各种化合物：还提供包含上述化合物的药物组合物。 此外，提供了哺乳动物抑制巨噬细胞迁移抑制因子（MIF）活性的方法，以及治疗或预防哺乳动物炎症的方法。 还提供了治疗具有败血症，败血病和/或内毒素性休克的哺乳动物的方法。 还提供了治疗具有自身免疫疾病的哺乳动物的方法以及治疗具有肿瘤的哺乳动物的方法。

    Antitumor properties of NO modified protease inhibitors
    8.
    发明授权
    Antitumor properties of NO modified protease inhibitors 有权
    NO修饰蛋白酶抑制剂的抗肿瘤特性

    公开(公告)号：US08563578B2

    公开(公告)日：2013-10-22

    申请号：US13056696

    申请日：2009-07-30

    Applicant: Ferdinando Nicoletti ,  Yousef Al-Abed ,  Gianni Garotta

    Inventor： Ferdinando Nicoletti ,  Yousef Al-Abed ,  Gianni Garotta

    IPC: A61K31/47 ,  C07D217/00

    CPC classification number: A61K31/00 ,  A61K31/4725 ,  C07D401/12

    Abstract: HIV-protease inhibitors, particularly saquinavir, showed strong anticancer activity but numerous side effects limited its application. In order to overcome its toxicity original compounds were modified by covalent attachment of NO. The efficacy of parental and NO-modified drug was compared in vitro and in vivo. Anticancer activities of NO-modified saquinavir (Saq-NO) was monitored in vitro using assay for cell viability, proliferation, necrotic, autophagic and apoptotic cell death, differentiation, expression of intracellular molecules such as cyclin D3, p53 and Akt. Antitumor properties and toxicity of the compound was estimated in vivo. Saq-NO abrogated the viability of large spectrum of human and rodent tumor cell lines with IC50 significantly lower than parental drug and expressed strong antimelanoma action in vivo. In contrast to saquinavir, there was no detectable toxicity against primary cells in vitro and in vivo. Saq-NO permanently diminished cell proliferation by induction of cell cycle block accompanied with minor presence of tumor cell death. Repressed proliferation was coordinated with strong activation of p53 and differentiation of C6 and B16 cells into oligodendrocytes or “Schwan” like cells, respectively. Oppositely to general characteristic of saquinavir to inhibit Akt signalling, Saq-NO treatment resulted in transient and intensive upregulation of Akt. This antagonism between parental and modified compound could be the crucial for switch of saquinavir from toxic to completely untoxic drug.

    Abstract translation: HIV-蛋白酶抑制剂，特别是沙奎那韦，表现出很强的抗癌活性，但许多副作用限制了其应用。 为了克服其毒性，原始化合物通过NO的共价连接进行修饰。 在体外和体内比较了亲本和NO-修饰药物的功效。 通过测定细胞活力，增殖，坏死，自噬和凋亡细胞死亡，分化，细胞周期蛋白D3，p53和Akt等细胞内分子的表达，体外监测NO-修饰的沙奎那韦（Saq-NO）的抗癌活性。 在体内估计化合物的抗肿瘤性质和毒性。 Saq-NO消除了大量人和啮齿类动物肿瘤细胞系的活力，其IC50明显低于亲本药物，并在体内表达强烈的抗血管瘤作用。 与沙奎那韦相比，在体外和体内对原代细胞没有可检测的毒性。 Saq-NO通过诱导细胞周期阻滞而持续减少细胞增殖，伴随肿瘤细胞死亡的轻微存在。 抑制增殖与p53的强活化和C6和B16细胞分化为少突胶质细胞或“Schwan”样细胞分别协调。 与沙奎那韦抑制Akt信号的一般特征相反，Saq-NO处理导致Akt的瞬时和强化上调。 父母和修饰化合物之间的这种拮抗作用可能是将沙奎那韦从毒性转变为完全无毒的药物至关重要的。

    Phenolic Hydrazone Macrophage Migration Inhibitory Factor Inhibitors
    9.
    发明申请
    Phenolic Hydrazone Macrophage Migration Inhibitory Factor Inhibitors 有权
    酚腙巨噬细胞迁移抑制因子抑制剂

    公开(公告)号：US20090170951A1

    公开(公告)日：2009-07-02

    申请号：US12225572

    申请日：2007-03-23

    Applicant: Yousef Al-Abed

    Inventor： Yousef Al-Abed

    IPC: A61K31/13 ,  C07C249/00 ,  A61P29/00

    CPC classification number: C07C251/86 ,  C07C281/02 ,  C07C311/49

    Abstract: Provided are various compounds of Formula (I): Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.

    Abstract translation: 提供式（I）的各种化合物：还提供包含上述化合物的药物组合物。 此外，提供了哺乳动物抑制巨噬细胞迁移抑制因子（MIF）活性的方法，以及治疗或预防哺乳动物炎症的方法。 还提供了治疗具有败血症，败血病和/或内毒素性休克的哺乳动物的方法。 还提供了治疗具有自身免疫疾病的哺乳动物的方法以及治疗具有肿瘤的哺乳动物的方法。

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