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    MONOCLONAL ANTIBODY SPECIFIC FOR 'beta'A4 PEPTIDE
    11.
    发明申请
    MONOCLONAL ANTIBODY SPECIFIC FOR 'beta'A4 PEPTIDE 审中-公开
    βA4肽的单克隆抗体特异性

    公开(公告)号：WO1996025435A1

    公开(公告)日：1996-08-22

    申请号：PCT/US1996002491

    申请日：1996-02-14

    Applicant: BAYER CORPORATION

    Inventor： BAYER CORPORATION ,  KONIG, Gerhard ,  GRAHAM, Paul

    IPC: C07K16/18

    CPC classification number: C07K16/18 ,  A61K38/00 ,  A61K2039/505 ,  C07K14/4711

    Abstract: The instant invention provides for monoclonal antibody which is specific for the beta A4 peptide, and in particular the free C-terminus of beta A4 "1-42" but not "1-43", and stains diffuse and fibrillar amyloid, vascular amyloid, and neurofibrillary tangles. The instant invention further provides for antibody fragments and constructs thereof which have the same binding specificity. The instant invention also provides for methods of diagnosis, screening and therapeutics for treating unique forms of beta A4 peptide, using the antibodies of the instant invention.

    Abstract translation: 本发明提供对βA4肽特异性的单克隆抗体，特别是βA4“1-42”但不是“1-43”的游离C末端，并且染色扩散和纤维状淀粉样蛋白，血管淀粉样蛋白， 和神经原纤维缠结。 本发明进一步提供具有相同结合特异性的抗体片段及其构建体。 本发明还提供了使用本发明的抗体来治疗独特形式的β-A4肽的诊断，筛选和治疗方法。

    SECRETORY LEUKOCYTE PROTEASE INHIBITOR AS AN INHIBITOR OF TRYPTASE
    13.
    发明申请
    SECRETORY LEUKOCYTE PROTEASE INHIBITOR AS AN INHIBITOR OF TRYPTASE 审中-公开
    作为TRYPTASE的抑制剂的秘密的低密度脂蛋白酶抑制剂

    公开(公告)号：WO1996008275A1

    公开(公告)日：1996-03-21

    申请号：PCT/US1995011445

    申请日：1995-09-11

    Applicant: BAYER CORPORATION

    Inventor： BAYER CORPORATION ,  MULLER, Daniel, K. ,  BROWNELL, Elise ,  DELARIA, Katherine, A.

    IPC: A61K48/00

    CPC classification number: C12N9/6424 ,  A61K38/00 ,  A61K48/00 ,  C07K14/57563 ,  C07K14/811

    Abstract: Secretory leukocyte protease inhibitor (SLPI) and active fragments thereof have been found to inhibit the proteolytic activity of tryptase. A method for treating a mast-cell mediated condition in a mammal comprises administering to the mammal an effective amount of a pharmacologically active fragment or mutein of SLPI. Treatment of asthma or allergic rhinitis in a mammal comprises administering to the mammal an effective amount of SLPI or a pharmacologically active fragment or mutein thereof. Treatment of a mast-cell mediated condition in a mammal by gene therapy comprises introducing DNA coding for SLPI or a pharmacologically active fragment thereof into the mammal by means of a vector capable of delivering DNA to the cell nucleus, resulting in secretion of SLPI or an active fragment thereof. Certain fragments and muteins of SLPI, as well as methods for inhibiting tryptase and for identifying inhibitors of tryptase are also disclosed and claimed.

    Abstract translation: 已经发现分泌型白细胞蛋白酶抑制剂（SLPI）及其活性片段抑制类胰蛋白酶的蛋白水解活性。 用于在哺乳动物中治疗肥大细胞介导的病症的方法包括向哺乳动物施用有效量的SLPI的药理活性片段或突变蛋白。 在哺乳动物中治疗哮喘或过敏性鼻炎包括向哺乳动物施用有效量的SLPI或其药理学活性片段或突变蛋白。 通过基因治疗在哺乳动物中治疗肥大细胞介导的病症包括通过能够向细胞核递送DNA的载体将编码SLPI或其药理学活性片段的DNA引入哺乳动物中，导致SLPI的分泌或 其活性片段。 还公开并要求保护SLPI的某些片段和突变蛋白，以及抑制类胰蛋白酶和鉴定类胰蛋白酶抑制剂的方法。

    IMPROVED EFFERVESCENT DELIVERY SYSTEM
    14.
    发明申请
    IMPROVED EFFERVESCENT DELIVERY SYSTEM 审中-公开
    改进的消费者交付系统

    公开(公告)号：WO1996003980A1

    公开(公告)日：1996-02-15

    申请号：PCT/US1995009540

    申请日：1995-07-28

    Applicant: BAYER CORPORATION ,  DASKALAKIS, Stefanos, A.

    Inventor： BAYER CORPORATION

    IPC: A61K09/46

    CPC classification number: A61K31/616 ,  A61K9/0007

    Abstract: An improved effervescent tablet is provided. The tablet contains acetylisylic acid, a critical ratio of bicarbonate to acid, flavors, sweeteners, tableting aids, and optionally other medicinals. The tablet has improved hardness and stability and can be readily compressed into a relatively small (by weight and diameter) effervescent tablet.

    Abstract translation: 提供改进的泡腾片剂。 片剂含有乙酰基酸，碳酸氢盐与酸的关键比例，香料，甜味剂，压片辅助剂和任选的其它药物。 片剂具有改善的硬度和稳定性，并且可以容易地压缩成相对较小（重量和直径）的泡腾片剂。

    AMINE-INITIATED POLYETHER POLYOLS AND A PROCESS FOR THEIR PRODUCTION
    15.
    发明申请
    AMINE-INITIATED POLYETHER POLYOLS AND A PROCESS FOR THEIR PRODUCTION 审中-公开
    胺引发聚醚多元醇及其生产工艺

    公开(公告)号：WO1998020061A1

    公开(公告)日：1998-05-14

    申请号：PCT/US1997018725

    申请日：1997-10-21

    Applicant: BAYER CORPORATION

    Inventor： BAYER CORPORATION ,  SCHILLING, Steven, L. ,  DOERGE, Herman, P. ,  HANUSA, Lotar, H.

    IPC: C08G65/26

    CPC classification number: C08G18/5021 ,  C08G65/2627 ,  C08G65/30 ,  C08G2101/0025 ,  C08G2101/005

    Abstract: Clear, amine-initiated polyether polyols are made by epoxidizing an amine in the presence of an alkali metal hydroxide catalyst. After the desired degree of epoxidation has been achieved, a hydroxy-carboxylic acid is added to the epoxidized mixture in an amount sufficient to neutralize any remaining alkali metal hydroxide. The polyols produced in this manner are particularly useful for the production of polyurethane and polyisocyanurate foams.

    Abstract translation: 通过在碱金属氢氧化物催化剂存在下使胺环氧化，制备了胺引发的聚醚多元醇。 在达到所希望的环氧化程度之后，将羟基羧酸以足以中和任何残留的碱金属氢氧化物的量加到环氧化混合物中。 以这种方式制备的多元醇特别可用于生产聚氨酯和聚异氰脲酸酯泡沫。

    T-CELL SELECTIVE INTERLEUKIN-4 AGONISTS
    16.
    发明申请
    T-CELL SELECTIVE INTERLEUKIN-4 AGONISTS 审中-公开
    T细胞选择性白细胞介素-4激动剂

    公开(公告)号：WO1997047744A2

    公开(公告)日：1997-12-18

    申请号：PCT/US1997009286

    申请日：1997-05-30

    Applicant: BAYER CORPORATION

    Inventor： BAYER CORPORATION ,  SHANAFELT, Armen, B. ,  GREVE, Jeffrey ,  GUNDEL, Robert

    IPC: C12N15/24

    CPC classification number: C07K14/5406 ,  A61K38/00 ,  Y02A50/401

    Abstract: The invention is directed to human IL-4 muteins numbered in accordance with wild-type IL-4 having T-cell activating activity, but having reduced endothelial cell activating activity. In particular, the invention is related to human IL-4 muteins wherein the surface-exposed residues of the D helix of the wild-type IL-4 are mutated whereby the resulting mutein causes T-cell proliferation, and causes reduced IL-6 secretion from HUVECs, relative to wild-type IL-4. This invention realizes a less toxic IL-4 mutant that allows greater therapeutic use of this interleukin. Further, the invention is directed to IL-4 muteins having single, double and triple mutations represented by the designators R121A, R121D, R121E, R121F, R121H, R121I, R121K, R121N, R121P, R121T, R121W; Y124A, Y124Q, Y124R, Y124S, Y124T; Y124A/S125A, T13D/R121E; and R121T/E122F/Y124Q, when numbered in accordance with wild-type IL-4 (His=1). The invention also includes polynucleotides coding for the muteins of the invention, vectors containing the polynucleotides, transformed host cells, pharmaceutical compositions comprising the muteins, and therapeutic methods of treatment.

    Abstract translation: 本发明涉及根据具有T细胞活化活性但具有降低的内皮细胞活化活性的野生型IL-4编号的人IL-4突变蛋白。 特别地，本发明涉及人IL-4突变蛋白，其中野生型IL-4的D螺旋的表面暴露残基被突变，由此产生的突变蛋白导致T细胞增殖，并导致IL-6分泌减少 来自HUVECs，相对于野生型IL-4。 本发明实现了一种毒性较小的IL-4突变体，可以更好地治疗这种白介素。 此外，本发明涉及具有由指示符R121A，R121D，R121E，R121F，R121H，R121I，R121K，R121N，R121P，R121T，R121W表示的单，双和三重突变的IL-4突变蛋白; Y124A，Y124Q，Y124R，Y124S，Y124T; Y124A / S125A，T13D / R121E; 和R121T / E122F / Y124Q，根据野生型IL-4（His = 1）进行编号。 本发明还包括编码本发明的突变蛋白的多核苷酸，含有多核苷酸的载体，转化的宿主细胞，包含突变蛋白的药物组合物和治疗方法。

    INHIBITION OF MATRIX METALLOPROTEASES BY ACETYLENE CONTAINING COMPOUNDS
    17.
    发明申请
    INHIBITION OF MATRIX METALLOPROTEASES BY ACETYLENE CONTAINING COMPOUNDS 审中-公开
    含乙烯基化合物对基质金属微球的抑制作用

    公开(公告)号：WO1997043245A1

    公开(公告)日：1997-11-20

    申请号：PCT/US1997007921

    申请日：1997-05-12

    Applicant: BAYER CORPORATION ,  DIXON, Brian, R. ,  CHEN, Jinshan

    Inventor： BAYER CORPORATION

    IPC: C07C229/34

    CPC classification number: C07D209/48 ,  C07C59/90 ,  C07C229/34

    Abstract: 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 formula (I) where R is selected from the group comprising: HOCH2, MeOCH2, (n-Pr)2NCH2, CH3CO2CH2, EtOCO2CH2, HO(CH2)2, CH3CO2(CH2)2, HO2C(CH2)2, OHC(CH2)3, HO(CH2)4, Ph, 3-HO-Ph, and PhCH2OCH2; and R is (a) or (b). 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 plate rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.

    Abstract translation: 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通式（I），其中R 15选自HOCH 2，MeOCH 2，（n-Pr）2 NCH 2，CH 3 CO 2 CH 2，EtOCO 2 CH 2，HO（CH 2）2，CH 3 CO 2（CH 2）2 ，HO2C（CH2）2，OHC（CH2）3，HO（CH2）4，Ph，3-HO-Ph和PhCH2OCH2; R 16为（a）或（b）。 这些化合物可用于抑制基质金属蛋白酶，因此可用于抗MMP的作用，例如骨关节炎，类风湿性关节炎，脓毒性关节炎，牙周病，角膜溃疡，蛋白尿，动脉瘤性主动脉疾病，疏水性表皮松解症，大疱疹，导致炎症的病症 反应，MMP活性介导的骨质减少，颞下颌关节疾病，神经系统脱髓鞘疾病，创伤性关节损伤后的肿瘤转移或退行性软骨损失，以及来自冠状动脉板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。

    NEUROPEPTIDE Y RECEPTOR Y5 AND NUCLEIC ACID SEQUENCE
    18.
    发明申请
    NEUROPEPTIDE Y RECEPTOR Y5 AND NUCLEIC ACID SEQUENCE 审中-公开
    神经元Y受体Y5和核酸序列

    公开(公告)号：WO1997037998A2

    公开(公告)日：1997-10-16

    申请号：PCT/US1997005781

    申请日：1997-04-08

    Applicant: BAYER CORPORATION

    Inventor： BAYER CORPORATION ,  HU, Yinghe ,  McCALEB, Michael, L. ,  BLOOMQUIST, Brian, T. ,  FLORES-RIVEROS, Jaime, R. ,  CORNFIELD, Linda, J.

    IPC: C07H00/00

    CPC classification number: G01N33/6893 ,  A01K2217/05 ,  A61K38/1709 ,  C07K14/70571 ,  G01N2800/303

    Abstract: The present invention provides novel NPY/PYY receptor proteins and the nucleic acid sequence encoding them. The invention is directed to the isolation, characterization, and pharmacological use of these receptors and nucleic acids. In particular, this invention provides human and rat NPY/PYY receptors (which we call the NPY Y5 receptor) and nucleic acids. Also provided are recombinant expression constructs useful for transfecting cells and expressing the protein in vitro and in vivo. The invention further provides methods for detecting expression levels of the protein as well as methods for screening for receptor antagonists and agonists to be used for the treatment of obesity or anorexia, respectively.

    Abstract translation: 本发明提供新的NPY / PYY受体蛋白质和编码它们的核酸序列。 本发明涉及这些受体和核酸的分离，表征和药理学应用。 特别地，本发明提供人和大鼠NPY / PYY受体（我们称之为NPY Y5受体）和核酸。 还提供了可用于转染细胞并在体外和体内表达蛋白质的重组表达构建体。 本发明还提供了用于检测蛋白质的表达水平的方法以及分别用于治疗肥胖症或厌食症的受体拮抗剂和激动剂的筛选方法。

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