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    Compounds For Enzyme Inhibition
    1.
    发明申请
    Compounds For Enzyme Inhibition 审中-公开
    化合物用于酶抑制

    公开(公告)号：US20120277146A1

    公开(公告)日：2012-11-01

    申请号：US13411044

    申请日：2012-03-02

    申请人： Mark S. Smyth ,  Guy J. Laidig ,  Ronald T. Borchardt ,  Barry A. Bunin ,  Craig M. Crews ,  John H. Musser

    发明人： Mark S. Smyth ,  Guy J. Laidig ,  Ronald T. Borchardt ,  Barry A. Bunin ,  Craig M. Crews ,  John H. Musser

    IPC分类号： A61K38/07 ,  A61P31/18 ,  A61P25/28 ,  A61P31/12 ,  A61P35/00 ,  A61P31/00 ,  A61P29/00 ,  A61P37/00 ,  C07K5/107 ,  A61P21/00

    CPC分类号： C07K5/1016 ,  C07K5/0812 ,  C07K5/0827

    摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

    摘要翻译： 包括含杂原子的三元环的基于肽的化合物有效地选择性地抑制N末端亲核试剂（Ntn）水解酶的比活性。 具有多种活性的那些Ntn的活性可被所描述的化合物差别地抑制。 例如，本发明化合物可以选择性地抑制20S蛋白酶体的胰凝乳蛋白酶样活性。 基于肽的化合物包括至少三个肽单元，环氧化物或氮丙啶，并且在N-末端官能化。 除了其他治疗用途之外，预期基于肽的化合物显示抗炎性质和抑制细胞增殖。

    Treatment of Conditions Caused By Calcium Abnormalities
    3.
    发明申请
    Treatment of Conditions Caused By Calcium Abnormalities 审中-公开
    治疗由钙异常引起的病症

    公开(公告)号：US20080188449A1

    公开(公告)日：2008-08-07

    申请号：US11667696

    申请日：2005-11-15

    申请人： Craig M. Crews ,  Stephanie J. Quinn ,  Stefan Somlo ,  Dayne Okuhara

    发明人： Craig M. Crews ,  Stephanie J. Quinn ,  Stefan Somlo ,  Dayne Okuhara

    IPC分类号： A61K31/585 ,  A61P13/12 ,  C12N5/02 ,  C12Q1/02

    CPC分类号： A61K31/366

    摘要： In certain aspects, the invention relates to use of PKD2 agonists, such as triptolide and triptolide derivatives, to regulate calcium release. In other aspects, the invention relates to use of PKD2 agonists to treat or aid in the treatment of any condition in which a calcium channel, such as the gene product of PKD 1 and/or PKD2, is mutated; calcium signaling is abnormal; or both, such as polycystic kidney disease.

    摘要翻译： 在某些方面，本发明涉及使用PKD2激动剂，例如雷公藤内酯和雷公藤内酯衍生物来调节钙的释放。 在其它方面，本发明涉及PKD2激动剂用于治疗或帮助治疗其中钙通道（例如PKD1和/或PKD2的基因产物）突变的任何病症的用途; 钙信号异常; 或两者，如多囊肾病。

    Enzyme inhibition
    5.
    发明授权
    Enzyme inhibition 有权
    酶抑制

    公开(公告)号：US06831099B1

    公开(公告)日：2004-12-14

    申请号：US09569748

    申请日：2000-05-11

    申请人： Craig M. Crews ,  Mikael Elofsson ,  Ute Splittgerber ,  Ny Sin ,  Kyung Bo Kim

    发明人： Craig M. Crews ,  Mikael Elofsson ,  Ute Splittgerber ,  Ny Sin ,  Kyung Bo Kim

    IPC分类号： A01N4320

    CPC分类号： C07K5/1016 ,  C07K5/1008 ,  C07K5/101 ,  C07K7/06

    摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include an electron withdrawing group adjacent to the ring functionality, and the peptide include at least three peptide units. Among other therapeutic utilities, the peptide-based compounds exhibit anti-inflammatory and inhibition of cell proliferation, involving therapeutic applications for these compounds.

    摘要翻译： 包括含杂原子的三元环的基于肽的化合物有效地选择性地抑制N末端亲核试剂（Ntn）水解酶的比活性。 具有多种活性的那些Ntn的活性可被所描述的化合物差别地抑制。 例如，本发明化合物可以选择性地抑制20S蛋白酶体的胰凝乳蛋白酶样和PGPH活性。 基于肽的化合物包括与环官能团相邻的吸电子基团，并且肽包括至少三个肽单元。 在其他治疗用途中，基于肽的化合物表现出抗炎和抑制细胞增殖，涉及这些化合物的治疗应用。

    Compounds for enzyme inhibition
    6.
    发明授权
    Compounds for enzyme inhibition 有权
    用于酶抑制的化合物

    公开(公告)号：US08088741B2

    公开(公告)日：2012-01-03

    申请号：US11596028

    申请日：2005-05-09

    申请人： Mark S. Smyth ,  Guy J. Laidig ,  Ronald T. Borchardt ,  Barry A. Bunin ,  Craig M. Crews ,  John H. Musser ,  Kevin D. Shenk ,  Peggy A. Radel

    发明人： Mark S. Smyth ,  Guy J. Laidig ,  Ronald T. Borchardt ,  Barry A. Bunin ,  Craig M. Crews ,  John H. Musser ,  Kevin D. Shenk ,  Peggy A. Radel

    IPC分类号： A61K38/06 ,  C12Q1/34

    CPC分类号： C07K5/0812 ,  C07K5/06034 ,  C07K5/0827 ,  Y02A50/412

    摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsinlike activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

    摘要翻译： 包括含杂原子的三元环的基于肽的化合物有效地选择性地抑制N末端亲核试剂（Ntn）水解酶的比活性。 具有多种活性的那些Ntn的活性可被所描述的化合物差别地抑制。 例如，本发明化合物可以选择性地抑制20S蛋白酶体的胰凝乳蛋白酶样活性。 肽类化合物包括环氧化物或氮丙啶，并且在N-末端官能化。 除了其他治疗用途之外，预期基于肽的化合物显示抗炎性质和抑制细胞增殖。

    Enzyme inhibition
    8.
    发明申请
    Enzyme inhibition 审中-公开

    公开(公告)号：US20090099097A1

    公开(公告)日：2009-04-16

    申请号：US12291236

    申请日：2008-11-07

    申请人： Craig M. Crews ,  Mikael Elofsson ,  Ute Splittgerber ,  Kyung Bo Kim

    发明人： Craig M. Crews ,  Mikael Elofsson ,  Ute Splittgerber ,  Kyung Bo Kim

    IPC分类号： A61K38/08

    CPC分类号： C07K5/1016 ,  C07K5/1008 ,  C07K5/101 ,  C07K7/06

    摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include an electron withdrawing group adjacent to the ring functionality, and the peptide include at least three peptide units. Among other therapeutic utilities, the peptide-based compounds exhibit anti-inflammatory and inhibition of cell proliferation, involving therapeutic applications for these compounds.

    Compounds for enzyme inhibition
    9.
    发明授权
    Compounds for enzyme inhibition 有权
    用于酶抑制的化合物

    公开(公告)号：US07232818B2

    公开(公告)日：2007-06-19

    申请号：US11106879

    申请日：2005-04-14

    申请人： Mark S. Smyth ,  Guy J. Laidig ,  Ronald T. Borchardt ,  Barry A. Bunin ,  Craig M. Crews ,  John H. Musser

    发明人： Mark S. Smyth ,  Guy J. Laidig ,  Ronald T. Borchardt ,  Barry A. Bunin ,  Craig M. Crews ,  John H. Musser

    IPC分类号： C07D413/12 ,  C07D405/12 ,  C07D303/36 ,  A61K31/5377 ,  A61K31/4025

    CPC分类号： C07K5/1016 ,  A61K38/00 ,  A61K38/07 ,  C07K5/0812 ,  C07K5/1008 ,  C07K5/1024

    摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

    摘要翻译： 包括含杂原子的三元环的基于肽的化合物有效地选择性地抑制N末端亲核试剂（Ntn）水解酶的比活性。 具有多种活性的那些Ntn的活性可被所描述的化合物差别地抑制。 例如，本发明化合物可以选择性地抑制20S蛋白酶体的胰凝乳蛋白酶样活性。 基于肽的化合物包括至少三个肽单元，环氧化物或氮丙啶，并且在N-末端官能化。 除了其他治疗用途之外，预期基于肽的化合物显示抗炎性质和抑制细胞增殖。