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    Furanopyridine derivatives and methods of use
    23.
    发明授权
    Furanopyridine derivatives and methods of use 有权
    呋喃并吡啶衍生物和使用方法

    公开(公告)号：US07674907B2

    公开(公告)日：2010-03-09

    申请号：US11184237

    申请日：2005-07-18

    Applicant: Joseph J. Nunes ,  Matthew W. Martin ,  Ryan White ,  David McGowan ,  Jean E. Bemis ,  Frank Kayser ,  Jiasheng Fu ,  Jinqian Liu ,  XianYun Jiao

    Inventor： Joseph J. Nunes ,  Matthew W. Martin ,  Ryan White ,  David McGowan ,  Jean E. Bemis ,  Frank Kayser ,  Jiasheng Fu ,  Jinqian Liu ,  XianYun Jiao

    IPC: C07D491/048 ,  A61K31/4355

    CPC classification number: C07D491/04 ,  C07D491/14

    Abstract: The present invention relates to furanopyridine compounds having the general Formula I: and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of modulating Lck and ACK-1 enzymes and of treating various related diseases and conditions, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, comprising administering to the mammal a therapeutically effective amount a compound of Formula I, as described above, and methods of manufacturing medicaments comprising the compound of Formula I.

    Abstract translation: 本发明涉及具有通式I的呋喃并吡啶化合物及其立体异构体，互变异构体，溶剂合物，药用盐和衍生物及其前药。 本发明还包括药物组合物，其包含式I化合物，调节Lck和ACK-1酶的方法以及治疗各种相关疾病和病症，包括炎症，T细胞活化抑制，增殖，关节炎，器官移植，缺血或再灌注 损伤，心肌梗塞，中风，多发性硬化，炎性肠病，克罗恩病，狼疮，超敏反应，1型糖尿病，牛皮癣，皮炎，桥本氏甲状腺炎，干燥综合征，自身免疫性甲状腺功能亢进，艾迪生病，自身免疫性疾病，肾小球肾炎，过敏性疾病，哮喘 ，干草组织，湿疹，癌症，结肠癌，胸腺瘤，仅举几个例子，在哺乳动物中，包括向哺乳动物施用治疗有效量的如上所述的式I化合物和制备包含以下化合物的药物的方法： 一级方程式

    FXR modulators
    25.
    发明授权
    FXR modulators 失效

    公开(公告)号：US06777446B2

    公开(公告)日：2004-08-17

    申请号：US09945293

    申请日：2001-08-31

    Applicant: Jonathan Houze ,  Sharon McKendry ,  Joshua P. Gergely ,  Yi Xia ,  Bei Shan ,  Frank Kayser

    Inventor： Jonathan Houze ,  Sharon McKendry ,  Joshua P. Gergely ,  Yi Xia ,  Bei Shan ,  Frank Kayser

    IPC: A61K31166

    CPC classification number: C07D209/48 ,  C07C233/75 ,  C07C237/22 ,  C07C311/19 ,  C07C311/29 ,  C07C2601/14 ,  C07D241/44 ,  C07D279/02

    Abstract: The present invention provides compounds, pharmaceutical compositions and methods that are useful in modulating the farnesoid X receptor (FXR). As FXR is involved in negatively controlling the expression level of cholesterol 7&agr;-hydroxylase (cyp7a), the rate-limiting enzyme involved in the oxidative metabolism of cholesterol into bile acids, the compounds described herein find utility in treating diseases associated with abnormally high or low cholesterol levels. In certain aspects, the FXR modulators (e.g., antagonists) described herein block the negative feed-back downregulation of cyp7a expression produced by certain cholic acids, the endogenous ligands for FXR. Moreover, as FXR forms heterodimers with the retinoid X receptor (RXR) in some cell types, modulation of the level of FXR activity in cells has a wide range of effects on a variety of biological processes which are mediated by RXR or other RXR-interacting proteins such as PPAR&ggr; and PPAR&agr;. Thus, compounds described herein are useful in treating other biological activities such as obesity, diabetes, lipid associated disorders, cancer, inflammatory disorders, disorders involving a disrupted or dysfunctional epidermal barrier, and various other metabolic disorders.

    Method and device for producing a coke coal cake for carrying out a coking process in a furnace chamber
    26.
    发明授权
    Method and device for producing a coke coal cake for carrying out a coking process in a furnace chamber 失效
    生产用于在炉室中进行焦化工艺的焦煤饼的方法和装置

    公开(公告)号：US06332957B1

    公开(公告)日：2001-12-25

    申请号：US09402167

    申请日：1999-09-30

    Applicant: Peter Gross ,  Frank Kayser

    Inventor： Peter Gross ,  Frank Kayser

    IPC: C10B4502

    CPC classification number: C10B31/10 ,  C10B45/02

    Abstract: The aim of the invention is to provide a method and a stamping device which is affiliated with said method. Using known economical stamping techniques, the stamping device permits coke coal cakes which are produced in an edgewise manner to be inserted into a coking furnace in a manner suited for positioning, i.e. in a flat-lying manner. To this end, a coke coal cake (1) having a small cake height and a large cake base surface is stamped inside a stamp die in an edgewise arrangement while using known techniques. Afterwards, the coke coal cake (1) remains in the stamp die and is placed in a position by a tipping and holding device (3) which is placed on the stamp die and which is suited for carrying out functions. In said position, the coke coal cake (1) which has not yet been removed from the die is inserted into the furnace chamber, is removed from the die therein, and is placed on the furnace base. This is especially achieved by using an inventive stamping device which is characterized in that a tipping and holding device (3) is connected to the stamp die of a stamping machine. A setting base (2) is arranged in the tipping and holding device such that the base is both a part of the stamp die and a part of the setting base.

    Abstract translation: 本发明的目的是提供一种与所述方法相关联的方法和冲压装置。 使用已知的经济冲压技术，冲压装置允许以沿边方式生产的焦煤饼以适于定位的方式即平坦的方式插入焦化炉中。 为此，使用已知技术，沿着边缘排列将具有小饼块高度和大饼状基面的焦煤饼（1）冲压在印模模具内。 此后，焦煤饼（1）保留在印模中，并通过放置在印模上的适合于执行功能的倾翻保持装置（3）放置在位置。 在该位置上，将尚未从模具中取出的焦煤饼（1）插入炉室，从其中的模具中取出，并放置在炉底上。 这通过使用本发明的冲压装置特别实现，其特征在于，倾翻和保持装置（3）连接到冲压机的冲压模具。 设置基座（2）设置在倾翻保持装置中，使得基座既是冲压模具的一部分又是设置基座的一部分。

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