Macrocyclic beta-secretase inhibitors
    1.
    发明授权
    Macrocyclic beta-secretase inhibitors 有权
    大环β-分泌酶抑制剂

    公开(公告)号:US08012953B2

    公开(公告)日:2011-09-06

    申请号:US12571840

    申请日:2009-10-01

    IPC分类号: A61K31/33 C07D513/00

    CPC分类号: C07D498/04 C07D413/06

    摘要: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.

    摘要翻译: 公开了下式的新化合物或其药学上可接受的盐或溶剂化物,其中R1,R2,R3,n和X如说明书中所定义。 还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。 还公开了治疗认知或神经退行性疾病的方法,包括向需要这种治疗的患者施用至少一种式I化合物和至少一种选自除了那些的那些之外的其他化合物 式I,HMG-CoA还原酶抑制剂,γ-分泌酶抑制剂,非甾体抗炎剂,N-甲基-D-天冬氨酸受体拮抗剂,胆碱酯酶抑制剂和抗淀粉样蛋白抗体。

    MACROCYCLIC BETA-SECRETASE INHIBITORS
    2.
    发明申请
    MACROCYCLIC BETA-SECRETASE INHIBITORS 有权
    大分子β-分泌酶抑制剂

    公开(公告)号:US20100178294A1

    公开(公告)日:2010-07-15

    申请号:US12571840

    申请日:2009-10-01

    CPC分类号: C07D498/04 C07D413/06

    摘要: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease.Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.

    摘要翻译: 公开了下式的新化合物或其药学上可接受的盐或溶剂化物,其中R1,R2,R3,n和X如说明书中所定义。 还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。 还公开了治疗认知或神经退行性疾病的方法,包括向需要这种治疗的患者施用至少一种式I化合物和至少一种选自除了那些的那些之外的其他化合物 式I,HMG-CoA还原酶抑制剂,γ-分泌酶抑制剂,非甾体抗炎剂,N-甲基-D-天冬氨酸受体拮抗剂,胆碱酯酶抑制剂和抗淀粉样蛋白抗体。

    SUBSTITUTED AMIDE BETA SECRETASE INHIBITORS
    7.
    发明申请
    SUBSTITUTED AMIDE BETA SECRETASE INHIBITORS 有权
    取代分子式的分泌酶抑制剂

    公开(公告)号:US20110003825A1

    公开(公告)日:2011-01-06

    申请号:US12861347

    申请日:2010-08-23

    摘要: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease.Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.

    摘要翻译: 公开了下式的新化合物或其药学上可接受的盐或溶剂化物,其中R1,R2,R3,R4和X如说明书中所定义。 还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。 还公开了治疗认知或神经退行性疾病的方法,包括向需要这种治疗的患者施用至少一种式I化合物和至少一种选自除了那些的那些之外的其他化合物 式I,HMG-CoA还原酶抑制剂,γ-分泌酶抑制剂,非甾体抗炎剂,N-甲基-D-天冬氨酸受体拮抗剂,胆碱酯酶抑制剂和抗淀粉样蛋白抗体。

    Neuropeptide Y Y5 receptor antagonists
    8.
    发明授权
    Neuropeptide Y Y5 receptor antagonists 失效
    神经肽Y Y5受体拮抗剂

    公开(公告)号:US06667319B2

    公开(公告)日:2003-12-23

    申请号:US10202239

    申请日:2002-07-24

    IPC分类号: A61K314468

    摘要: The present invention discloses compounds which, are novel receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

    摘要翻译: 本发明公开了作为NPY Y5的新型受体拮抗剂的化合物及其制备方法。 在另一个实施方案中,本发明公开了包含这种NPY Y5受体拮抗剂的药物组合物以及使用它们治疗肥胖,代谢紊乱,进食障碍如食欲过盛和糖尿病的方法。

    PREPARATION AND USE OF COMPOUNDS AS PROTEASE INHIBITORS
    9.
    发明申请
    PREPARATION AND USE OF COMPOUNDS AS PROTEASE INHIBITORS 审中-公开
    化合物作为蛋白酶抑制剂的制备和使用

    公开(公告)号:US20140206715A1

    公开(公告)日:2014-07-24

    申请号:US14226338

    申请日:2014-03-26

    IPC分类号: C07D471/04

    摘要: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6′R7′); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7′ are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.

    摘要翻译: 公开了式I化合物或其立体异构体,互变异构体或其药学上可接受的盐或溶剂合物,其中Q是键或-N(R 5) - ; T是键,-O - , - C(O) - ; S,-N(R 5) - 或-C(R 6'R 7'); U是键或-C(R6)(R7)-Y是C或N; Z是C或N; 环A包括变量Y和Z是具有0至4个,优选0至2个杂原子的3至9元环烷基,环烯基,杂环基,杂环烯基,芳基和杂芳基环,其独立地选自O,S, N和-N(R) - ,其中当环A是环烷基,环烯基,杂环基或杂环烯基时,环A是未取代的或被1至5个独立选择的R 1部分和/或氧代取代。 并且R,R 1,R 2,R 3,R 4,R 5,R 6,R 6,R 7和R 7'如本说明书中所定义; 包含式I化合物的药物组合物和抑制天冬氨酰蛋白酶的方法,特别是治疗心血管疾病,认知和神经变性疾病的方法。

    Substituted amide beta secretase inhibitors
    10.
    发明授权
    Substituted amide beta secretase inhibitors 有权
    取代的酰胺β分泌酶抑制剂

    公开(公告)号:US08367712B2

    公开(公告)日:2013-02-05

    申请号:US12861347

    申请日:2010-08-23

    IPC分类号: A01N43/50 A61K31/415

    摘要: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease.Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.

    摘要翻译: 公开了下式的新化合物或其药学上可接受的盐或溶剂化物,其中R1,R2,R3,R4和X如说明书中所定义。 还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。 还公开了治疗认知或神经退行性疾病的方法,包括向需要这种治疗的患者施用至少一种式I化合物和至少一种选自除了那些的那些之外的其他化合物 式I,HMG-CoA还原酶抑制剂,γ-分泌酶抑制剂,非甾体抗炎剂,N-甲基-D-天冬氨酸受体拮抗剂,胆碱酯酶抑制剂和抗淀粉样蛋白抗体。