Heterocyclic Derivatives and Their Use as Stearoyl-Coa Desaturase Inhibitors
    51.
    发明申请
    Heterocyclic Derivatives and Their Use as Stearoyl-Coa Desaturase Inhibitors 失效
    杂环衍生物及其作为硬脂酰辅酶A去饱和酶抑制剂的用途

    公开(公告)号:US20080096895A1

    公开(公告)日:2008-04-24

    申请号:US11575640

    申请日:2005-09-20

    CPC分类号: A61K31/496 A61K31/501

    摘要: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, G, J, K, L, M, V R2, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

    摘要翻译: 公开了在哺乳动物,优选人中治疗SCD介导的疾病或病症的方法,其中所述方法包括向有需要的哺乳动物施用式(I)化合物:其中x,y,G,J,K ,L,M,VR 2,R 3,R 4,R 5,R 5a R 6,R 6,R 6,R 7,R 7a,R 8, < 8a>和< 8a>在本文中定义。 还公开了包含式(I)化合物的药物组合物。

    Heteropolycyclic inhibitors of protein kinases
    53.
    发明授权
    Heteropolycyclic inhibitors of protein kinases 失效
    蛋白激酶的杂多环抑制剂

    公开(公告)号:US07196083B2

    公开(公告)日:2007-03-27

    申请号:US10310600

    申请日:2002-12-04

    IPC分类号: A61K31/53

    CPC分类号: C07D487/04 C07D513/04

    摘要: A method of inhibiting tumor growth is provided, comprising administering an effective dose of a compound of the formula wherein, independently at each occurrence, w is C or N, v and x are N with H substitution as needed to fulfill open valence sites; y and z are selected from N and C, with H substitution as needed to fulfill open valence sites, with the proviso that each of w, v, x, y and z is not simultaneously C; the ring formed from v, w, x, y and z may be saturated or unsaturated; and R1, R2, R3 and R4 are selected from hydrogen, alkyl, aryl, alkaryl, aralkyl, heteroalkyl, and heteroaryl; wherein any adjacent two of R1, R2, R3 and R4 may join together to form a 5, 6 or 7-membered carbocyclic ring or a 5, 6 or 7-membered heterocyclic ring containing at least one atom selected from nitrogen, oxygen and sulfur.

    摘要翻译: 提供了一种抑制肿瘤生长的方法,包括施用有效剂量的下式的化合物

    Heteropolycyclic inhibitors of protein kinases
    55.
    发明授权
    Heteropolycyclic inhibitors of protein kinases 失效
    蛋白激酶的杂多环抑制剂

    公开(公告)号:US06514972B2

    公开(公告)日:2003-02-04

    申请号:US09900073

    申请日:2001-07-06

    IPC分类号: C07D48704

    CPC分类号: C07D487/04 C07D513/04

    摘要: A compound of the formula wherein, independently at each occurrence, v, w, and x are selected from C, N, O, and S, with H substitution as needed to fulfill open valence sites; y and z are selected from N and C, with H substitution as needed to fulfill open valence sites, with the proviso that each of w, v, x, y and z is not simultaneously C; the ring formed from v, w, x, y and z may be saturated or unsaturated; and R1, R2, R3 and R4 are selected from hydrogen, alkyl, aryl, alkaryl, aralkyl, heteroalkyl, and heteroaryl; wherein any adjacent two of R1, R2, R3 and R4 may join together to form a 5, 6 or 7-membered carbocyclic or heterocyclic ring, with the proviso that each of R1, R2, R3 and R4 is not simultaneously hydrogen. Pharmaceutical compositions of said compounds, and methods of use in the treatment of biological conditions including cellular hyperproliferation, are disclosed.

    摘要翻译: 在每次出现时,v,w和x独立地选自C,N,O和S的化合物,根据需要进行H取代以实现开价值位点; y和z选自N和C,根据需要进行H取代以满足开价值位置,条件是w,v,x,y和z中的每一个不同时为C; 由v,w,x,y和z形成的环可以是饱和或不饱和的; 并且R 1,R 2,R 3和R 4选自氢,烷基,芳基,烷芳基,芳烷基,杂烷基和杂芳基; 其中R 1,R 2,R 3和R 4中的任何相邻的两个可以连接在一起以形成5,6或7-元碳环或杂环,条件是R 1,R 2,R 3和R 4中的每一个不是同时氢。 公开了所述化合物的药物组合物,以及用于治疗包括细胞过度增殖的生物学条件的方法。

    Vanadium complexes and derivatives thereof and methods related thereto
    58.
    发明授权
    Vanadium complexes and derivatives thereof and methods related thereto 失效
    钒络合物及其衍生物及其相关方法

    公开(公告)号:US06232340B1

    公开(公告)日:2001-05-15

    申请号:US09064707

    申请日:1998-04-22

    IPC分类号: A61K3128

    摘要: Organovanadium complexes, and more specifically hydroxyoxovanadium(V), &mgr;-oxo dimeric oxovanadium(V) and cis-dioxovanadium(V) complexes, are provided. The complexes may be formulated into a pharmaceutical composition. The complexes and/or compositions may be used in the treatment of a variety of disease states, including use as anti-proliferative and/or anti-metastatic agents and/or to treat drug resistant tumors and/or to methods of reducing the ability of tumors to metastasize and/or for the treatment of diabetes, arthritis, multiple sclerosis, diseases involving passageways of the body, and autoimmune diseases including but not limited to psoriasis and lupus.

    摘要翻译: 有机复合物,更具体地是羟基氧钒(V),多氧代二氧代钒(V)和顺式二氧代钒(V)络合物)。 配合物可以配制成药物组合物。 复合物和/或组合物可用于治疗各种疾病状态,包括用作抗增殖和/或抗转移剂和/或治疗药物抗性肿瘤和/或降低其抗性的方法 肿瘤转移和/或用于治疗糖尿病,关节炎,多发性硬化,涉及身体通道的疾病和自身免疫性疾病,包括但不限于牛皮癣和狼疮。