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11 条记录 (耗时 0.021 秒)

    Substituted cyclic amine metalloprotease inhibitors
    1.
    发明申请
    Substituted cyclic amine metalloprotease inhibitors 审中-公开
    取代的环状胺金属蛋白酶抑制剂

    公开(公告)号：US20020072517A1

    公开(公告)日：2002-06-13

    申请号：US09888759

    申请日：2001-06-25

    申请人： The Procter & Gamble Company

    发明人： Michael George Natchus ,  Biswanath De ,  Stanislaw Pikul ,  Neil Gregory Almstead ,  Roger Gunnard Bookland ,  Yetunde Olabisi Taiwo ,  Menyan Cheng

    IPC分类号： A61K031/55 ,  A61K031/445 ,  C07D223/08 ,  C07D211/30

    CPC分类号： C07D207/42

    摘要： The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I). 1 Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

    摘要翻译： 本发明提供了可用作金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。 特别地，本发明涉及具有式（I）结构的化合物。 还公开了使用这些化合物或含有它们的药物组合物治疗以金属蛋白酶活性为特征的疾病的化合物，药物组合物和方法。

    Isoxazolone compounds useful in treating diseases associated with unwanted cytokine activity
    3.
    发明申请
    Isoxazolone compounds useful in treating diseases associated with unwanted cytokine activity 失效
    可用于治疗与不想要的细胞因子活性相关的疾病的异恶唑酮化合物

    公开(公告)号：US20040122025A1

    公开(公告)日：2004-06-24

    申请号：US10726111

    申请日：2003-12-02

    申请人： The Procter & Gamble Company

    发明人： Michael Philip Clark ,  Jane Far-Jine Djung ,  Steven Karl Laughlin ,  Joshua Spector Tullis ,  Michael George Natchus ,  Biswanath De

    IPC分类号： A61K031/513 ,  C07D413/02

    CPC分类号： C07D413/04 ,  A61K31/44 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  C07D413/14

    摘要： Isoxazolone compounds having the generic structure: 1 are used to treat disease associated with unwanted cytokine activity, including rheumatoid arthritis, osteoarthritis, diabetes, HIV/AIDS, inflammatory bowel disease, Crohn's disease, ulcerative colitis, congestive heart, hypertension, chronic obstructive pulmonary disease, septic shock syndrome, tuberculosis, adult respiratory distress, asthma, atherosclerosis, muscle degeneration, periodontal disease, cachexia, Reiter's syndrome, gout, acute synovitis, anorexia and bulimia nervosa fever, malaise, myalgia and headaches.

    摘要翻译： 具有通用结构的异恶唑酮化合物用于治疗与不想要的细胞因子活性相关的疾病，包括类风湿性关节炎，骨关节炎，糖尿病，艾滋病毒/艾滋病，炎性肠病，克罗恩病，溃疡性结肠炎，充血性心脏病，高血压，慢性阻塞性肺病， 败血性休克综合征，结核病，成人呼吸窘迫，哮喘，动脉粥样硬化，肌肉退化，牙周病，恶病质，莱特综合征，痛风，急性滑膜炎，厌食症和神经性贪食症，不适，肌痛和头痛。

    Heterocyclic side chain containing, n-substituted metalloprotease inhibitors
    8.
    发明申请
    Heterocyclic side chain containing, n-substituted metalloprotease inhibitors 审中-公开
    杂环侧链含有取代的金属蛋白酶抑制剂

    公开(公告)号：US20040127498A1

    公开(公告)日：2004-07-01

    申请号：US10758791

    申请日：2004-01-16

    申请人： The Procter & Gamble Company

    发明人： Stanislaw Pikul ,  Norman Eugene Ohler ,  Neil Gregory Almstead ,  Steyen Karl Laughlin ,  Michael George Natchus ,  Biswanath De ,  Paul Mitchell Hershberger

    IPC分类号： A61K031/53 ,  A61K031/454 ,  C07D43/14

    CPC分类号： C07D401/12 ,  C07D211/34 ,  C07D211/66 ,  C07D211/96 ,  C07D309/06 ,  C07D309/08 ,  C07D309/14 ,  C07D407/12

    摘要： Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): 1 where R1, R2, R3, n, A, E, X, G, Gnull, M and Z have the meanings described in the specification and the claims, as well as optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.

    摘要翻译： 公开了作为金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。 特别地，化合物具有下式（I）的结构：其中R 1，R 2，R 3，n，A，E，X，G，G'，M和Z具有 说明书和权利要求书中描述的含义，以及式I的光学异构体，非对映异构体和对映异构体及其药学上可接受的盐，可生物水解的酰胺，酯和酰亚胺。 还描述了包含这些化合物的药物组合物，以及使用该化合物或药物组合物治疗金属蛋白酶相关疾病的方法。

    6,7-Dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines
    9.
    发明申请
    6,7-Dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines 失效
    6,7-二氢-5H-吡唑并[1,2-a]吡唑-1-酮，其控制炎性细胞因子

    公开(公告)号：US20030134867A1

    公开(公告)日：2003-07-17

    申请号：US10246214

    申请日：2002-09-18

    申请人： The Procter & Gamble Company

    发明人： Michael Philip Clark ,  Matthew John Laufersweiler ,  Jane Far-Jine Djung ,  Michael George Natchus ,  Biswanath De

    IPC分类号： A61K031/506 ,  C07D43/04

    CPC分类号： C07D487/04

    摘要： The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: 1 wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; each R2 unit is independently selected from the group consisting of: a) hydrogen; b) null(CH2)jO(CH2)nR8; c) null(CH2)jNR9aR9b; d) null(CH2)jCO2R10; e) null(CH2)jOCO2R10 f) null(CH2)jCON(R10)2; g) null(CH2)jOCON(R10)2; h) two R2 units can be taken together to form a carbonyl unit; i) and mixtures thereof; R8, R9a, R9b, and R10 are each independently hydrogen, C1-C4 alkyl, and mixtures thereof; R9a and R9b can be taken together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; two R10 units can be take together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; j is an index from 0 to 5, n is an index from 0 to 5; Z is O, S, NR11, or NOR11; R11 is hydrogen or C1-C4 alkyl.

    摘要翻译： 本发明涉及能够防止炎性细胞因子细胞外释放的化合物，所述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R包括醚或胺; R1是：a）取代或未取代的芳基; 或b）取代或未取代的杂芳基; 每个R 2单元独立地选自：a）氢; b） - （CH 2）j O（CH 2）n R 8; c） - （CH2）jNR9aR9b; d） - （CH 2）j CO 2 R 10; e） - （CH 2）j CO 2 R 10 f） - （CH 2）j CON（R 10）2; g） - （CH 2）jOCON（R 10）2; h）两个R2单元可以一起取代形成羰基单元; i）及其混合物; R8，R9a，R9b和R10各自独立地为氢，C1-C4烷基及其混合物; R9a和R9b可以一起形成包含3至7个原子的碳环或杂环; 两个R 10单元可以一起形成包含3至7个原子的碳环或杂环; j是从0到5的索引，n是从0到5的索引; Z是O，S，NR11或NOR11; R 11是氢或C 1 -C 4烷基。