Melanocortin receptor ligands
    1.
    发明授权
    Melanocortin receptor ligands 失效
    黑皮质素受体配体

    公开(公告)号:US07026335B2

    公开(公告)日:2006-04-11

    申请号:US10410775

    申请日:2003-04-09

    IPC分类号: A61K31/445 C07D401/04

    CPC分类号: C07D401/06 C07D211/26

    摘要: The present invention relates to compounds which comprise a 4-substituted piperidine ring linked to a substituted or unsubstituted hydrocarbyl ring. The compounds, including all enatiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein preferably R is substituted aryl, W is a pendant unit having the formula: -L-Q L is a linking unit, Q is preferably a cyclic hydrocarbyl unit; W1 is preferably a carbocyclic unit and W2 is a heteroatom comprising unit.

    摘要翻译: 本发明涉及包含与取代或未取代的烃基环连接的4-取代的哌啶环的化合物。 化合物,包括所有对映异构体和非对映体形式及其药学上可接受的盐,具有下式:其中优选R是取代的芳基,W是具有下式的侧链单元:<?in-line-formula description =“In-line Formulas” - =“lead”?> - LQ <?in-line-formula description =“In-line Formulas”end =“tail”?> L是连接单元,Q优选为环状烃基单元; W 1优选是碳环单元,W 2是含杂原子的单元。

    Heterocyclic compounds useful as malonyl-CoA decarboxylase inhibitors
    5.
    发明授权
    Heterocyclic compounds useful as malonyl-CoA decarboxylase inhibitors 失效
    可用作丙二酰辅酶A脱羧酶抑制剂的杂环化合物

    公开(公告)号:US07696365B2

    公开(公告)日:2010-04-13

    申请号:US10900958

    申请日:2004-07-28

    IPC分类号: C07D307/00

    摘要: The present invention provides methods for the use of compounds as depicted by structure I, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity.

    摘要翻译: 本发明提供了使用结构I所示化合物的方法,含有该化合物的药物组合物,以及预防,治疗和治疗由MCD抑制调节的代谢疾病和疾病的方法。 本发明公开的化合物可用于预防,管理和治疗涉及丙二酰辅酶A调节的葡萄糖/脂肪酸代谢途径的疾病。 特别地,这些化合物和含有它们的药物组合物在心血管疾病,糖尿病,癌症和肥胖症的预防,治疗和治疗中被指出。

    Method of forming oseltamivir and derivatives thereof
    6.
    发明授权
    Method of forming oseltamivir and derivatives thereof 有权
    奥司他韦及其衍生物的形成方法

    公开(公告)号:US08304553B2

    公开(公告)日:2012-11-06

    申请号:US12809521

    申请日:2008-12-10

    申请人: Xuewei Liu Jimei Ma

    发明人: Xuewei Liu Jimei Ma

    摘要: A process is provided for the synthesis of 4,5-diamino cyclohexene carboxylate ester (1): or a pharmaceutically acceptable salt thereof. R1-R3 are a silyl-, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. R4, R11 and R12 are H, a silyl-group, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. 3,4-Dihydropyran compound (9): with R5 and R6 being suitable protecting groups, is reacted to form aldehyde (4): which is oxidized and converted to N-substituted carbamate (3): with R7 being a suitable protecting group. (3) is, via oxazolinidone (13): converted to azido carboxylate ester (2): and then to 4,5-diamino cyclohexene carboxylate ester (1).

    摘要翻译: 提供了用于合成4,5-二氨基环己烯羧酸酯(1)的方法:或其药学上可接受的盐。 R 1 -R 3是甲硅烷基,脂族,脂环族,芳族,芳基脂族基或芳基脂环基。 R4,R11和R12是H,甲硅烷基,脂族,脂环族,芳族,芳基脂族或芳基脂环族基团。 3,4-二氢吡喃化合物(9):其中R 5和R 6是合适的保护基,反应形成醛(4):其被氧化并转化成N-取代的氨基甲酸酯(3):其中R 7是合适的保护基。 (3)通过恶唑啉酮(13):转化为叠氮基羧酸酯(2):然后转化为4,5-二氨基环己烯羧酸酯(1)。

    METHOD OF FORMING OSELTAMIVIR AND DERIVATIVES THEREOF
    7.
    发明申请
    METHOD OF FORMING OSELTAMIVIR AND DERIVATIVES THEREOF 有权
    形成奥司他韦及其衍生物的方法

    公开(公告)号:US20110021762A1

    公开(公告)日:2011-01-27

    申请号:US12809521

    申请日:2008-12-10

    申请人: Xuewei Liu Jimei Ma

    发明人: Xuewei Liu Jimei Ma

    摘要: A process is provided for the synthesis of 4,5-diamino cyclohexene carboxylate ester (1): or a pharmaceutically acceptable salt thereof. R1-R3 are a silyl-, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. R4, R11 and R12 are H, a silyl-group, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. 3,4-Dihydropyran compound (9): with R5 and R6 being suitable protecting groups, is reacted to form aldehyde (4): which is oxidized and converted to N-substituted carbamate (3): with R7 being a suitable protecting group. (3) is, via oxazolinidone (13): converted to azido carboxylate ester (2): and then to 4,5-diamino cyclohexene carboxylate ester (1).

    摘要翻译: 提供了用于合成4,5-二氨基环己烯羧酸酯(1)的方法:或其药学上可接受的盐。 R 1 -R 3是甲硅烷基,脂族,脂环族,芳族,芳基脂族基或芳基脂环基。 R4,R11和R12是H,甲硅烷基,脂族,脂环族,芳族,芳基脂族或芳基脂环族基团。 3,4-二氢吡喃化合物(9):其中R 5和R 6是合适的保护基,反应形成醛(4):其被氧化并转化成N-取代的氨基甲酸酯(3):其中R 7是合适的保护基。 (3)通过恶唑啉酮(13):转化为叠氮基羧酸酯(2):然后转化为4,5-二氨基环己烯羧酸酯(1)。