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    Inhibitors of Memapsin 2 and use thereof
    2.
    发明申请
    Inhibitors of Memapsin 2 and use thereof 审中-公开

    公开(公告)号：US20040220079A1

    公开(公告)日：2004-11-04

    申请号：US10773754

    申请日：2004-02-06

    Applicant: Oklahoma Medical Research Foundation ,  The Board of Trustees of the University of Illinois

    Inventor： Gerald Koelsch ,  Jordan J.N. Tang ,  Lin Hong ,  Arun K. Ghosh

    IPC: A61K031/00 ,  G06F019/00 ,  G01N033/48 ,  G01N033/50

    CPC classification number: C07K5/1021 ,  A61K38/00 ,  A61K39/00 ,  C07K1/1136 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/0806 ,  C07K2299/00 ,  C12N9/6421 ,  C12N9/6478 ,  Y02A90/26 ,  Y10S514/879

    Abstract: Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1). The inhibition constant of OM99-2 is 1.6null10null9 M against recombinant pro-memapsin 2. Crystallography of memapsin 2 bound to this inhibitor was used to determine the three dimensional structure of the protein, as well as the importance of the various residues in binding. This information can be used by those skilled in the art to design new inhibitors, using commercially available software programs and techniques familiar to those in organic chemistry and enzymology, to design new inhibitors to memapsin 2, useful in diagnostics and for the treatment and/or prevention of Alzheimer's disease.

    Treatment of skin disorders
    4.
    发明申请
    Treatment of skin disorders 审中-公开
    治疗皮肤病

    公开(公告)号：US20040220075A1

    公开(公告)日：2004-11-04

    申请号：US10403849

    申请日：2003-03-31

    Inventor： Edward R. Ahrens

    IPC: A61K031/00

    CPC classification number: A61K31/225 ,  A61K31/22

    Abstract: The present invention provides a method and composition for treating skin disorders, skin pathologies and pruritus, which includes applying a compound of formula (I) in a suitable formulation to the affected area.

    Abstract translation: 本发明提供用于治疗皮肤病症，皮肤病理学和瘙痒症的方法和组合物，其包括将合适制剂中的式（I）化合物施用于受影响的区域。

    Benzimidazolidinone derivatives
    5.
    发明申请
    Benzimidazolidinone derivatives 失效
    苯并咪唑烷酮衍生物

    公开(公告)号：US20040142850A1

    公开(公告)日：2004-07-22

    申请号：US10470813

    申请日：2003-07-30

    Inventor： Kazuhiko Okazaki ,  Yasuyuki Ueki

    IPC: A61K031/00

    CPC classification number: C07D235/26 ,  C07D405/06

    Abstract: The present invention can provide novel compounds useful as orally administrable growth hormone releaser, more specifically a benzimidazolidinone derivative of formula (1) or a pharmaceutically acceptable salt thereof: (1) wherein R1 is optionally substituted alkyl or the like; R2, R3 and R4 are each hydrogen, optionally substituted alkyl, or the like; R5 is optionally substituted aryl; q is 0 or 1; and W1 is a group represented by formula (2): (2) n is 1, 2 or 3; m is 0, 1, 2 or 3; R6 and R7 are each hydrogen, optionally substituted alkyl, or the like; and R8 and R9 are each hydrogen, optionally substituted alkyl, or the like. 1

    Abstract translation: 本发明可以提供作为口服给药的生长激素释放剂，更具体地是式（1）的苯并咪唑啉酮衍生物或其药学上可接受的盐的新化合物：（1）其中R 1是任选取代的烷基等; R 2，R 3和R 4各自为氢，任选取代的烷基等; R 5是任选取代的芳基; q为0或1; 和W 1是由式（2）表示的基团：（2）n是1,2或3; m为0,1,2或3; R 6和R 7各自为氢，任选取代的烷基等; R 8和R 9各自为氢，任选取代的烷基等。

    Medicinal composition containing 1,3-thiazine derivative
    8.
    发明申请
    Medicinal composition containing 1,3-thiazine derivative 失效
    含有1,3-噻嗪衍生物的药物组合物

    公开(公告)号：US20040116326A1

    公开(公告)日：2004-06-17

    申请号：US10470388

    申请日：2003-07-28

    Inventor： Hiroyuki Kai ,  Takami Murashi ,  Minoru Tomida

    IPC: A61K031/00

    CPC classification number: C07D417/04 ,  C07D279/06 ,  C07D417/12 ,  C07D513/10

    Abstract: A compound of the formula (I) having a binding activity to the cannabinoid type 2 receptor: 1 wherein R1 is optionally substituted heterocyclic group or the like; R2 and R2 each is independently hydrogen or the like; m is an integer of 0 to 2; A is optionally substituted aromatic carbocyclic group or the like.

    Abstract translation: 具有与大麻素2型受体的结合活性的式（I）化合物：其中R 1是任选取代的杂环基等; R 2和R 2各自独立地为氢等; m为0〜2的整数; A是任选取代的芳族碳环基等。

    Combination therapy
    9.
    发明申请
    Combination therapy 审中-公开
    联合治疗

    公开(公告)号：US20040102360A1

    公开(公告)日：2004-05-27

    申请号：US10678565

    申请日：2003-10-03

    Inventor： Stanley F. Barnett ,  Deborah D. DeFeo-Jones ,  George D. Hartman ,  Hans E. Huber ,  Steven M. Stirdivant ,  David C. Heimbrook

    IPC: A61K031/00

    CPC classification number: A61K41/00 ,  A61K45/06

    Abstract: The present invention relates to methods of treating cancer using a combination of at least two Akt inhibitors or a compound which is an inhibitor of Akt and an inhibitor of a protein kinase, which methods comprise administering to a mammal, either sequentially in any order or simultaneously, amounts of at least two therapeutic agents selected from a group consisting of a compound(s) which are inhibitors of Akt and compound(s) which are inhibitors of protein kinases. The invention also relates to methods of preparing such compositions.

    Abstract translation: 本发明涉及使用至少两种Akt抑制剂或作为Akt抑制剂的化合物和蛋白激酶抑制剂的组合来治疗癌症的方法，所述方法包括以任何顺序依次施用于哺乳动物 ，至少两种治疗剂的量，其选自作为Akt抑制剂的化合物和作为蛋白激酶抑制剂的化合物。 本发明还涉及制备这种组合物的方法。

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