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    Fused indazole compounds
    4.
    发明授权
    Fused indazole compounds 失效
    稠合吲唑化合物

    公开(公告)号：US07390797B2

    公开(公告)日：2008-06-24

    申请号：US10503216

    申请日：2003-02-21

    申请人： Norihito Ohi ,  Nobuaki Sato ,  Naohiro Kohmura

    发明人： Norihito Ohi ,  Nobuaki Sato ,  Naohiro Kohmura

    IPC分类号： A61K31/416 ,  A61K31/4162 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/554 ,  C07D231/54 ,  C07D245/04 ,  C07D243/10 ,  C07D225/04 ,  C07D223/14 ,  C07D267/04

    CPC分类号： A61K31/55 ,  A61K31/416 ,  A61K31/4439 ,  C07D231/54 ,  C07D401/12 ,  C07D405/12 ,  C07D487/06

    摘要： The present invention provides a novel fused indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein Z11 and Z12 each independently represent a carbonyl group, a methylene group, etc.; represents a double bond or a single bond; R1a represents a hydrogen atom, etc.; the ring A represents a benzene ring, a naphthalene ring or a 5- to 10-membered aromatic heterocyclic ring, etc.; and R2a, R2b and R2c each independently represent (1) a hydrogen atom, (2) a halogen atom, (3) a nitro group, etc.

    摘要翻译： 本发明提供了具有优异JNK抑制作用的新的稠合吲唑化合物。 更具体地，它提供由下式表示的化合物，其盐或它们的水合物。 其中Z 11和Z 12各自独立地表示羰基，亚甲基等; “img id =”CUSTOM-CHARACTER-00001“he =”2.79mm“wi =”6.35mm“file =”US07390797-20080624-P00001.TIF“alt =”custom character“img-content =”character“img-format =“tif”/>表示双键或单键; R 1a表示氢原子等; 环A表示苯环，萘环或5至10元芳族杂环等; 和R 2a，R 2b和R 2c各自独立地表示（1）氢原子，（2）卤素原子，（3） 硝基等

    Oxaza heterocycles and pharmaceutical compositions containing same
    5.
    发明授权
    Oxaza heterocycles and pharmaceutical compositions containing same 失效
    含氮杂环和含有它们的药物组合物

    公开(公告)号：US4892870A

    公开(公告)日：1990-01-09

    申请号：US227572

    申请日：1988-08-01

    申请人： Sung J. Lee

    发明人： Sung J. Lee

    IPC分类号： A61K31/42 ,  A61K31/535 ,  A61K31/5377 ,  A61K31/55 ,  A61P25/04 ,  A61P29/00 ,  A61P37/00 ,  C07D261/04 ,  C07D261/12 ,  C07D265/02 ,  C07D267/04

    CPC分类号： C07D265/02 ,  C07D261/04 ,  C07D261/12 ,  C07D267/04

    摘要： A novel class of 5, 6 or 7 member heterocycles which belong to the 3-isoxazolidinone, 2H-1,2-oxazin-3 (4H)-one and 3-isoxazepinone series of compounds and which are substituted at the 4-carbon by a benzylidene radical. The compounds have utility as analgesic agents, immunomodulating agents, anti-inflammatory agents and anti-pyretic agents and they may be combined with excipients to provide formuations which are useful in treating arthritis and conditions generally associated with that disease.

    摘要翻译： 属于3-异恶唑烷酮，2H-1,2-恶嗪-3（4H） - 酮和3-异恶唑酮系列化合物的5,6或7元杂环的新类，其在4-碳被 亚苄基。 这些化合物可用作镇痛剂，免疫调节剂，抗炎剂和抗热解剂，并且它们可与赋形剂组合以提供可用于治疗关节炎和通常与该疾病相关的病症的制剂。

    C-nitroso compounds and use thereof
    7.
    发明申请
    C-nitroso compounds and use thereof 失效
    C-亚硝基化合物及其用途

    公开(公告)号：US20050203295A1

    公开(公告)日：2005-09-15

    申请号：US11052777

    申请日：2005-02-09

    申请人： Jonathan Stamler ,  Eric Toone

    发明人： Jonathan Stamler ,  Eric Toone

    IPC分类号： A61K31/00 ,  A61K31/194 ,  A61K31/195 ,  A61K31/222 ,  A61K31/553 ,  A61K31/635 ,  A61K38/00 ,  A61L27/00 ,  A61L31/00 ,  A61P7/02 ,  A61P9/10 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  C07C207/00 ,  C07C291/08 ,  C07D231/12 ,  C07D267/04 ,  C07D279/02 ,  C07D267/02

    CPC分类号： C07C207/00 ,  A61K31/00 ,  A61K31/195 ,  A61K2300/00

    摘要： A C-nitroso compound having a molecular weight ranging from about 225 to about 1,000 (from about 225 to about 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. The compound is preferably water-soluble and preferably contains a carbon alpha to the nitrosylated carbon which is part of a ketone group. In one embodiment, the C-nitroso compound is obtained by nitrosylation of a conventional drug or such drug modified to modify the carbon acid pKa thereof When such drug is a nonsteroidal anti-inflammatory drug, the resulting C-nitroso compound functions as a COX-1 and COX-2 inhibitor without the deleterious effects associated with COX-1 inhibition but with the advantageous effects associated with COX-1 and COX-2 inhibition. One such C-nitroso compound is a nitrosoketoibuprofen. A specific example of this kind of compound is isolated as dimeric 2-[4′-(α-nitroso)isobutyrylphenyl]propionic acid. In another case, the C-nitroso compound contains the moiety where X is S, O or NR. One embodiment is directed to COX-2 inhibitors where a tertiary carbon atom and/or an oxygen atom and/or a sulfur atom is nitrosylated.

    摘要翻译： 单体基团的分子量范围为约225至约1,000（约225至约600）的C-亚硝基化合物，其中亚硝基连接到叔碳上，其通过碳的亚硝基化获得 pKa小于约25的酸可用作NO供体。 当化合物从pKa小于约10的碳酸获得时，当以微摩尔浓度使用时，其提供血管松弛效果，并且该活性由以纳摩尔浓度获得的谷胱甘肽加强。 当化合物由pKa为约15至约20的碳酸获得时，在没有谷胱甘肽的纳摩尔浓度下获得血管松弛效果。 该化合物优选是水溶性的并且优选地含有作为酮基的一部分的亚硝基化碳的碳α。 在一个实施方案中，C-亚硝基化合物通过常规药物的亚硝基化或经修饰以改变其碳酸pKα的药物而获得。当这种药物是非甾体抗炎药物时，所得的C-亚硝基化合物起COX- 1和COX-2抑制剂，没有与COX-1抑制相关的有害作用，但具有与COX-1和COX-2抑制相关的有利效果。 一种这样的C-亚硝基化合物是亚硝基基布洛芬。 这种化合物的具体实例被分离为二聚2- [4' - （α-亚硝基）异丁酰苯基]丙酸。 在另一种情况下，C-亚硝基化合物包含其中X是S，O或NR的部分。 一个实施方案涉及其中叔碳原子和/或氧原子和/或硫原子被亚硝酰化的COX-2抑制剂。