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23 条记录 (耗时 0.021 秒)

    Inhibition of matrix metalloproteases by substitued biaryl oxobutyric acids
    4.
    发明授权
    Inhibition of matrix metalloproteases by substitued biaryl oxobutyric acids 失效
    通过取代的联芳基氧代丁酸抑制基质金属蛋白酶

    公开(公告)号：US06500847B2

    公开(公告)日：2002-12-31

    申请号：US09845392

    申请日：2001-04-30

    申请人： Michael C. VanZandt ,  David R. Brittelli ,  Brian R. Dixon

    发明人： Michael C. VanZandt ,  David R. Brittelli ,  Brian R. Dixon

    IPC分类号： A61K3144

    CPC分类号： C07D253/08 ,  A61K31/425 ,  A61K31/426 ,  A61K31/4706 ,  A61K31/502 ,  A61K31/513 ,  A61K31/517 ,  A61K31/53 ,  A61K31/5513 ,  C07C62/38 ,  C07D237/32

    摘要： Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: wherein r is 0-2, T is selected from and R40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.

    摘要翻译： 提出了基质金属蛋白酶抑制化合物，其药物组合物和使用这些化合物的疾病治疗方法。 本发明的化合物具有以下通式：其中r为0-2，选自T，R 40为单或双杂环结构。这些化合物可用于抑制基质金属蛋白酶，因此可用于抑制MMP的贡献 ，如骨关节炎，类风湿关节炎，脓毒性关节炎，牙周病，角膜溃疡，蛋白尿，动脉瘤主动脉疾病，疏水性表皮松解症，大疱疹，导致炎症反应的病症，MMP活性介导的骨质减少，下颌关节病，神经系统脱髓鞘疾病 系统，肿瘤转移或创伤性关节损伤后的退行性软骨损失，以及来自动脉粥样硬化斑块破裂的冠状动脉血栓形成。 本发明还提供了用于治疗这些病症的药物组合物和方法。

    Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids
    5.
    发明授权
    Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids 失效
    通过取代的联芳基氧代丁酸抑制基质金属蛋白酶

    公开(公告)号：US06225314B1

    公开(公告)日：2001-05-01

    申请号：US09343142

    申请日：1999-06-29

    申请人： Michael C. VanZandt ,  David R. Brittelli ,  Brian R. Dixon

    发明人： Michael C. VanZandt ,  David R. Brittelli ,  Brian R. Dixon

    IPC分类号： A61K31495

    CPC分类号： C07D253/08 ,  A61K31/425 ,  A61K31/426 ,  A61K31/4706 ,  A61K31/502 ,  A61K31/513 ,  A61K31/517 ,  A61K31/53 ,  A61K31/5513 ,  C07C62/38 ,  C07D237/32

    摘要： Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: wherein r is 0-2, T is selected from and R40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from arteriosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.

    摘要翻译： 提出了基质金属蛋白酶抑制化合物，其药物组合物和使用这些化合物的疾病治疗方法。 本发明的化合物具有以下通式：其中r为0-2，选自T，R 40为单或双杂环结构。这些化合物可用于抑制基质金属蛋白酶，因此可用于抑制MMP的贡献 ，如骨关节炎，类风湿关节炎，脓毒性关节炎，牙周病，角膜溃疡，蛋白尿，动脉瘤主动脉疾病，疏水性表皮松解症，大疱疹，导致炎症反应的病症，MMP活性介导的骨质减少，下颌关节病，神经系统脱髓鞘疾病 系统，肿瘤转移或创伤性关节损伤后的退行性软骨损失，以及动脉硬化斑块破裂引起的冠状动脉血栓形成。 本发明还提供了用于治疗这些病症的药物组合物和方法。

    Certain substituted ureas, as modulators of kinase activity
    7.
    发明授权
    Certain substituted ureas, as modulators of kinase activity 有权
    某些取代的脲，作为激酶活性的调节剂

    公开(公告)号：US08222421B2

    公开(公告)日：2012-07-17

    申请号：US12840246

    申请日：2010-07-20

    申请人： Scott A. Mitchell ,  Mihaela Diana Danca ,  Peter A. Blomgren ,  David R. Brittelli ,  Pavel Zhichkin ,  Matthew E. Voss

    发明人： Scott A. Mitchell ,  Mihaela Diana Danca ,  Peter A. Blomgren ,  David R. Brittelli ,  Pavel Zhichkin ,  Matthew E. Voss

    IPC分类号： C07D215/38

    CPC分类号： C07D471/04 ,  C07D401/06

    摘要： Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, and prodrugs thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicles chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.

    摘要翻译： 本文提供了选自式1化合物的某些化学实体及其药学上可接受的盐，溶剂合物，螯合物，非共价复合物及其前体药物。 还提供了包含至少一种化学实体和一种或多种选自载体，佐剂和赋形剂的药学上可接受的载体的药物组合物。 公开了治疗患有对血管生成激酶调节反应的某些疾病和病症的患者的方法，其包括向这些患者施用一定量的至少一种有效减少疾病或病症体征或症状的化学实​​体。 这些疾病包括癌症，包括乳腺肿瘤，子宫内膜癌，结肠癌和颈部鳞状细胞癌。 治疗方法包括给予至少一种化学实体作为单一活性剂或者与一种或多种其它治疗剂组合施用这样的至少一种化学实体。 一种用于确定样品中存在或不存在血管生成激酶的方法，包括在允许检测血管生成激酶活性，检测血管生成激酶活性水平的条件下将样品与至少一种化学实体接触 确定样品中存在或不存在血管生成激酶。

    Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids
    8.
    发明授权
    Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids 失效
    通过取代的联芳基氧代丁酸抑制基质金属蛋白酶

    公开(公告)号：US06762184B2

    公开(公告)日：2004-07-13

    申请号：US09845379

    申请日：2001-04-30

    申请人： Michael C. VanZandt ,  David R. Brittelli ,  Brian R. Dixon

    发明人： Michael C. VanZandt ,  David R. Brittelli ,  Brian R. Dixon

    IPC分类号： A61K3153

    CPC分类号： C07D253/08 ,  A61K31/425 ,  A61K31/426 ,  A61K31/4706 ,  A61K31/502 ,  A61K31/513 ,  A61K31/517 ,  A61K31/53 ,  A61K31/5513 ,  C07C62/38 ,  C07D237/32

    摘要： This application relates to matrix metalloprotease inhibitors having the generalized formula in which r is 0-2, T is selected from and R40 is a mono-or bi-heterocyclic structure. More particularly, the present application claims the various stereoisomeric forms of 4-(4′-choloro-biphenyl-4-yl)-4-oxo-2-[2-(4-oxo-4H-benzo[d][1,2,3]triazin-3-yl)ethyl]butyric acid, as well as their pharmaceutically acceptable salts. Pharmaceutical compositions containing these compounds, and methods for inhibiting matrix metalloprotease activity in mammals such as humans and for treating various conditions by administering such compounds are also claimed.

    摘要翻译： 本申请涉及具有广义结构的基质金属蛋白酶抑制剂，其r为0-2，T选自并且R 40为单或双杂环结构。 更具体地说，本申请要求4-（4'-氯 - 联苯-4-基）-4-氧代-2- [2-（4-氧代-4H-苯并[d] [1,3] 2,3]三嗪-3-基）乙基]丁酸，以及它们的药学上可接受的盐。 还要求保护含有这些化合物的药物组合物，以及用于抑制哺乳动物如人类中的基质金属蛋白酶活性的方法以及通过施用这些化合物来治疗各种病症。

    Substituted 4-arylbutyric acid derivatives as matrix metalloprotease
    9.
    发明授权
    Substituted 4-arylbutyric acid derivatives as matrix metalloprotease 失效
    取代的4-芳基丁酸衍生物作为基质金属蛋白酶

    公开(公告)号：US5863915A

    公开(公告)日：1999-01-26

    申请号：US857004

    申请日：1997-05-15

    申请人： Harold C. E. Kluender ,  Brian R. Dixon ,  David R. Brittelli

    发明人： Harold C. E. Kluender ,  Brian R. Dixon ,  David R. Brittelli

    IPC分类号： C07C59/90 ,  C07C69/84 ,  C07D209/48 ,  A61K31/19 ,  C07C59/84

    CPC分类号： C07D209/48 ,  C07C59/90

    摘要： Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein R.sup.1 represents C.sub.6 -C.sub.12 alkyl; C.sub.5 -C.sub.12 alkoxy; C.sub.5 -C.sub.12 alkylthio; a polyether of formula R.sup.2 O(C.sub.2 H.sub.4 O).sub.a -- in which a is 1 or 2 and R.sup.2 is C.sub.1 -C.sub.5 alkyl, phenyl, or benzyl; and substituted alkynyl of formula R.sup.3 (CH.sub.2).sub.b --C.tbd.C--; in which b is 1-10 and R.sup.3 is H--, HO--, or R.sup.4 O-- in which R.sup.4 is C.sub.1 -C.sub.3 alkyl, phenyl, or benzyl. The alkyl, phenyl, and benzyl portions of R.sup.1 may bear at least one pharmaceutically-acceptable substituent. The subscript n is 2-4. R.sup.5 represents phenyl; imidoyl of 4-12 carbon atoms; (3H)-benzo-1,2,3-triazin-4-on-3-yl; N-saccharinyl; (2H)-phthalazin-1-on-2-yl; 2-benzoxazolin-2-on-3-yl; 5,5-dimethyloxazolidine-2,4-dion-3-yl; and thiazolidine-2,4-dion-3-yl; with the phenyl and benzo portions of R.sup.5 permissibly bearing at least one pharmaceutically-acceptable substituent. Pharmaceutically acceptable salts of these materials are also included.

    摘要翻译： 基质金属蛋白酶抑制剂，含有它们的药物组合物，以及使用它们治疗各种生理条件的方法。 本发明的化合物具有通式（I）其中R 1表示C 6 -C 12烷基; C5-C12烷氧基; C5-C12烷硫基; 苯基或苄基;式R2O（C2H4O）a-的聚醚，其中a为1或2，R2为C1-C5烷基，苯基或苄基; 和式R 3（CH 2）b -C 3的取代的炔基; 其中b为1-10，R3为H，HO-或R4O-，其中R4为C1-C3烷基，苯基或苄基。 R1的烷基，苯基和苄基部分可以具有至少一个药学上可接受的取代基。 下标n为2-4。 R5表示苯基; 4-12个碳原子的亚氨基; （3H） - 苯并-1,2,3-三嗪-4-酮-3-基; N-糖精; （2H） - 酞嗪-1-酮-2-基; 2-苯并恶唑啉-2-酮-3-基; 5,5-二甲基恶唑烷-2,4-二酮-3-基; 和噻唑烷-2,4-二酮-3-基; 其中R 5的苯基和苯并部分容许具有至少一个药学上可接受的取代基。 也包括这些材料的药学上可接受的盐。

    Chiral glycidyl azides as synthetic intermediates to optically active compounds
    10.
    发明授权
    Chiral glycidyl azides as synthetic intermediates to optically active compounds 失效
    手性缩水甘油基叠氮化物作为光学活性化合物的合成中间体

    公开(公告)号：US4877892A

    公开(公告)日：1989-10-31

    申请号：US128287

    申请日：1987-12-03

    申请人： David R. Brittelli

    发明人： David R. Brittelli

    IPC分类号： C07D303/36

    CPC分类号： C07D303/36

    摘要： Chiral glycidyl azides, such as (2S)-glycidyl azide, are prepared, and they are useful as intermediates to prepare optically active compounds, particularly optically active, anti-bacterial oxazolidinones.

    摘要翻译： 制备手性缩水甘油基叠氮化物，如（2S） - 缩水甘油基叠氮化物，它们可用作制备光学活性化合物，特别是光学活性的抗菌恶唑烷酮的中间体。