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    INHIBITION OF FATTY ACID SYNTHASE AS A MEANS TO REDUCE ADIPOCYTE MASS
    5.
    发明申请
    INHIBITION OF FATTY ACID SYNTHASE AS A MEANS TO REDUCE ADIPOCYTE MASS 审中-公开
    脂肪酸合成酶的抑制作为减少ADIPOCYTE质量的手段

    公开(公告)号：WO1997018806A1

    公开(公告)日：1997-05-29

    申请号：PCT/US1996017678

    申请日：1996-11-15

    Applicant: THE JOHNS HOPKINS UNIVERSITY ,  KUHAJDA, Francis, P. ,  PASTERNACK, Gary, R. ,  TOWNSEND, Craig, A. ,  MANI, Neelakandha, S.

    Inventor： THE JOHNS HOPKINS UNIVERSITY

    IPC: A61K31/365

    CPC classification number: A61K31/365

    Abstract: Weight loss was noted in nude mice treated with cerulenin, a non-competitive inhibitor of FAS. Sustained reduction of adipocyte mass in humans without toxicity would significantly impact disease prevention worldwide. Aside from psychological and self-esteem improvement, weight loss via reduction of adipocyte mass may: (1) ameliorate hyperglycemia associated with non-insulin-dependent diabetes mellitus thereby reducing diabetic complications such as arterial disease, blindness, cataracts, etc., (2) reduce hypertension, (3) reduce risk of coronary artery vascular disease and stroke, and (4) reduce the risk of other complications of massive obesity such as osteoarthritis, surgical complications, etc. There is also potential use in livestock and poultry to reduce the saturated fat content of meat products. Therefore FAS inhibitors are disclosed herein as novel agents for weight reduction. A family of compounds ( gamma -substituted- alpha -methylene- beta -carboxy- gamma -butyrolactones) whose synthesis was based on the cerulenin motif is shown herein to inhibit fatty acid synthesis, inhibit growth in certain susceptible tumor cells, and induce weight loss.

    Abstract translation: 在使用非竞争性FAS抑制剂的木瓜素处理的裸小鼠中注意到体重减轻。 持续减少人体脂肪细胞质量无毒性将严重影响全球疾病预防。 除了心理和自尊心的改善之外，通过减少脂肪细胞质量可以减轻体重：（1）改善与非胰岛素依赖性糖尿病相关的高血糖，从而减少糖尿病并发症，如动脉疾病，失明，白内障等（2 ）降低高血压，（3）降低冠状动脉血管疾病和卒中的风险，（4）降低骨质疏松，手术并发症等巨大肥胖的其他并发症的风险。畜禽养殖也有潜在的用途 肉制品的饱和脂肪含量。 因此，本文公开了FAS抑制剂作为减轻体重的新型药剂。 本文显示了其合成基于苏氨酸基序的化合物（γ-取代-α-亚甲基-β-羧基-γ-丁内酯）家族，以抑制脂肪酸合成，抑制某些易感的肿瘤细胞中的生长并诱导体重减轻 。

    PROCESSES FOR THE PREPARATION OF CARBON-LINKED TETRAHYDRO-PYRAZOLO-PYRIDINE MODULATORS OF CATHEPSIN S
    9.
    发明申请
    PROCESSES FOR THE PREPARATION OF CARBON-LINKED TETRAHYDRO-PYRAZOLO-PYRIDINE MODULATORS OF CATHEPSIN S 审中-公开
    制备CATHEPSIN的碳链烷基四氢吡喃 - 吡啶调节剂的方法

    公开(公告)号：WO2009102937A1

    公开(公告)日：2009-08-20

    申请号：PCT/US2009/034031

    申请日：2009-02-13

    Applicant: SUNESIS PHARMACEUTICALS, INC. ,  MANI, Neelakandha, S. ,  LIANG, Jimmy, T. ,  DENG, Xiaohu

    Inventor： MANI, Neelakandha, S. ,  LIANG, Jimmy, T. ,  DENG, Xiaohu

    IPC: C07D471/04

    CPC classification number: C07D471/04

    Abstract: Method of making carbon-linked tetrahydro-pyrazolo-pyridine compounds of the following Formula (I) and pharmaceutically acceptable salts thereof: comprising reacting a compound of formula (IX): with a compound of formula (X): to form a compound of Formula (I); wherein: R 1 and R 7 taken together with the nitrogen to which they are attached form a morpholine ring, unsubstituted or substituted with one or two methyl substituents; R 3 is H or OH; R 4 is -SO 2 CH 3 , -CONH 2 , or -COCONH 2 ; R 5 is H or methyl; R 6 is a benzyl group, unsubstituted or substituted with one or two substituents independently selected from the group consisting of C 1-4 alkyl, CF 3 , halo, OH, -OC 1-4 alkyl, -OCF 3 , -OCHF 2 , NR dd R ee , -CO 2 C 1-4 alkyl, -SC 1-4 alkyl, and -SO 2 C 1-4 alkyl; where R dd and R ee are each independently H or C 1-4 alkyl; R 7 is H, fluoro, or chloro; and LG 1 is iodide, bromide, or trifluoromethanesulfonate. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis.

    Abstract translation: 制备下式（I）的碳 - 连四氢 - 吡唑并 - 吡啶化合物及其药学上可接受的盐的方法：包括使式（Ⅸ）化合物与式（Ⅹ）化合物反应：使式 （一世）; 其中：R 1和R 7与它们所连接的氮一起形成吗啉环，未被取代或被一个或两个甲基取代基取代; R3是H或OH; R4是-SO2CH3，-CONH2或-COCONH2; R5是H或甲基; R6是未取代的或被一个或两个取代基取代的苄基，所述取代基独立地选自C 1-4烷基，CF 3，卤素，OH，-OC 1-4烷基，-OCF 3，-OCHF 2，NR d R e，-CO 2 C 1-4烷基， SC1-4烷基和-SO2C1-4烷基; 其中Rdd和Ree各自独立地为H或C 1-4烷基; R7是H，氟或氯; 和LG1是碘化物，溴化物或三氟甲磺酸盐。 这些化合物可用于治疗由组织蛋白酶S活性介导的疾病状态，病症和病症的药物组合物和方法，例如银屑病，疼痛，多发性硬化，动脉粥样硬化和类风湿性关节炎。

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