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    Glucagon antagonists and methods relating thereto
    1.
    发明授权
    Glucagon antagonists and methods relating thereto 失效
    胰高血糖素拮抗剂及其相关方法

    公开(公告)号：US5508304A

    公开(公告)日：1996-04-16

    申请号：US288875

    申请日：1994-08-10

    Applicant: Robert R. West ,  Virender Labroo ,  James R. Piggott ,  Robert A. Smith ,  Patricia A. McKernan

    Inventor： Robert R. West ,  Virender Labroo ,  James R. Piggott ,  Robert A. Smith ,  Patricia A. McKernan

    IPC: A61K31/12 ,  A61K31/122 ,  A61K31/22 ,  A61K31/27 ,  C12P15/00 ,  A61K31/21

    CPC classification number: A61K31/122 ,  A61K31/12 ,  A61K31/22 ,  A61K31/27 ,  C12P15/00

    Abstract: Glucagon antagonists and methods relating thereto are disclosed. The glucagon antagonists include skyrin and skyrin analogs, and serve to inhibit the stimulation of a glucagon-induced response pathway, such as the adenylate cyclase response pathway or the inositol phosphate response pathway. The glucagon antagonists may be used within therapeutic compositions to treat disease states associate with elevated glucose levels, including diabetes and hyperglycemia. The present invention also discloses a biologically pure culture of ATCC accession number 74200, as well as methods relating to the production of glucagon antagonists by cultivating the same in a nutrient medium and recovering the glucagon antagonist therefrom.

    Abstract translation: 公开了胰高血糖素拮抗剂及其相关方法。 胰高血糖素拮抗剂包括天冬氨酸和天冬氨酸类似物，并且用于抑制胰高血糖素诱导的应答途径的刺激，例如腺苷酸环化酶应答途径或肌醇磷酸应答途径。 胰高血糖素拮抗剂可用于治疗组合物内以治疗与升高的葡萄糖水平相关的疾病状态，包括糖尿病和高血糖。 本发明还公开了ATCC保藏号74200的生物纯纯培养物，以及通过在营养培养基中培养并从其中回收胰高血糖素拮抗剂来产生胰高血糖素拮抗剂的方法。

    Method for inhibiting bone loss using centchroman derivatives
    2.
    发明授权
    Method for inhibiting bone loss using centchroman derivatives 失效
    使用间苯二酚衍生物抑制骨丢失的方法

    公开(公告)号：US5464862A

    公开(公告)日：1995-11-07

    申请号：US180728

    申请日：1994-01-13

    Applicant: Virender M. Labroo ,  James R. Piggott ,  Steven D. Bain

    Inventor： Virender M. Labroo ,  James R. Piggott ,  Steven D. Bain

    IPC: C07D311/58 ,  A61K31/35 ,  A61K31/352 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/55 ,  A61P19/10

    CPC classification number: A61K31/35 ,  A61K31/40

    Abstract: Methods and pharmaceutical compositions for reducing bone loss are disclosed. 3,4-diarylchromans and their pharmaceutically acceptable salts are formulated into medicaments for the treatment of bone loss due to osteoporosis or other conditions. An exemplary 3,4-diarylchroman is centchroman (3,4-trans-2,2-dimethyl-3-phenyl-4-[p-(beta-pyrrolidinoethoxy)phenyl]-7-methoxychroman). Formulations include tablets and other forms suitable for oral administration and controlled-release subdermal implants.

    Abstract translation: 公开了减少骨丢失的方法和药物组合物。 将3,4-二芳基苯并二氢吡喃及其药学上可接受的盐配制成用于治疗由骨质疏松症或其他病症引起的骨丢失的药物。 示例性3,4-二芳基苯并二氢吡喃是中性苯并二氢吡喃（3,4-反式-2,2-二甲基-3-苯基-4- [对 - （β-吡咯烷基）乙氧基）苯基] -7-甲氧基苯并二氢吡喃）。 制剂包括适于口服给药和受控释放的皮下植入物的片剂和其它形式。

    Methods for detecting glucagon antagonists
    3.
    发明授权
    Methods for detecting glucagon antagonists 失效
    检测胰高血糖素拮抗剂的方法

    公开(公告)号：US5408037A

    公开(公告)日：1995-04-18

    申请号：US741931

    申请日：1991-08-08

    Applicant: Robert A. Smith ,  James R. Piggott

    Inventor： Robert A. Smith ,  James R. Piggott

    IPC: C07K14/575 ,  C07K14/605 ,  C12N1/19 ,  C12N15/09 ,  C12N15/16 ,  C12P21/02 ,  C12R1/865 ,  G01N33/53 ,  A61K37/00 ,  C07K7/00

    CPC classification number: C07K14/605

    Abstract: Methods for detecting glucagon antagonists through the use of recombinant DNA techniques are provided. Briefly, subsequent to the expression of glucagon analogs within suitable host cells, the analogs are exposed to a glucagon receptor coupled to a response pathway in the presence of native glucagon. A reduction in the stimulation of the response pathway resulting from the binding of the glucagon analog to the glucagon receptor relative to the stimulation of the response pathway by native glucagon alone indicates the presence of a glucagon antagonist. Glucagon antagonists identified and isolated through the methods are also provided.

    Abstract translation: 提供了通过使用重组DNA技术检测胰高血糖素拮抗剂的方法。 简而言之，在合适的宿主细胞内表达胰高血糖素类似物之后，类似物暴露于在天然胰高血糖素存在下偶联至应答途径的胰高血糖素受体。 由胰高血糖素类似物与胰高血糖素受体的结合引起的反应途径的刺激相对于单独的天然胰高血糖素刺激反应途径的降低表明存在胰高血糖素拮抗剂。 还提供了通过该方法鉴定和分离的胰高血糖素拮抗剂。

    Methods for reducing bone loss using centchroman derivatives
    4.
    发明授权
    Methods for reducing bone loss using centchroman derivatives 失效
    使用分散染料衍生物减少骨丢失的方法

    公开(公告)号：US5280040A

    公开(公告)日：1994-01-18

    申请号：US29729

    申请日：1993-03-11

    Applicant: Virender M. Labroo ,  James R. Piggott ,  Steven D. Bain

    Inventor： Virender M. Labroo ,  James R. Piggott ,  Steven D. Bain

    IPC: C07D311/58 ,  A61K31/35 ,  A61K31/352 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/55 ,  A61P19/10

    CPC classification number: A61K31/35 ,  A61K31/40

    Abstract: Methods and pharmaceutical compositions for reducing bone loss are disclosed. 3,4-diarylchromans and their pharmaceutically acceptable salts are formulated into medicaments for the treatment of bone loss due to osteoporosis or other conditions. An exemplary 3,4-diarylchroman is centchroman (3,4-trans-2,2-dimethyl-3-phenyl-4-[p-(beta-pyrrolidinoethoxy)phenyl]-7-methoxy-chroman). Formulations include tablets and other forms suitable for oral administration and controlled-release subdermal implants.

    Abstract translation: 公开了减少骨丢失的方法和药物组合物。 将3,4-二芳基苯并二氢吡喃及其药学上可接受的盐配制成用于治疗由骨质疏松症或其他病症引起的骨丢失的药物。 示例性的3,4-二芳基苯并二氢吡喃是中性色满（3,4-反式-2,2-二甲基-3-苯基-4-（对 - （β-吡咯烷基乙氧基）苯基）-7-甲氧基 - 苯并二氢吡喃）。 制剂包括适于口服给药和受控释放的皮下植入物的片剂和其它形式。

    3,4-diarylchromans for treatment of dermatitis
    6.
    发明授权
    3,4-diarylchromans for treatment of dermatitis 失效
    3,4-二芳基苯并二氢吡喃治疗皮炎

    公开(公告)号：US5451603A

    公开(公告)日：1995-09-19

    申请号：US29739

    申请日：1993-03-11

    Applicant: James R. Piggott

    Inventor： James R. Piggott

    IPC: C07D311/58 ,  A61K31/35 ,  A61K31/352 ,  A61K31/40 ,  A61P43/00

    CPC classification number: A61K31/35 ,  A61K31/40

    Abstract: Methods for the treatment of dermatitis are disclosed wherein 3,4-diarylchromans and their pharmaceutically acceptable salts are formulated into medicaments, including oral and topical medicaments, and are administered to a patient suffering from dermatitis.

    Abstract translation: 公开了治疗皮炎的方法，其中3,4-二芳基苯并二氢吡喃及其药学上可接受的盐被配制成药物，包括口服和局部药物，并且给予患有皮炎的患者。

    Piperazine derivatives for treating bone deficit conditions
    7.
    发明授权
    Piperazine derivatives for treating bone deficit conditions 失效
    哌嗪衍生物用于治疗骨缺损病症

    公开(公告)号：US06268367B1

    公开(公告)日：2001-07-31

    申请号：US09027570

    申请日：1998-02-23

    Applicant: James R. Piggott

    Inventor： James R. Piggott

    IPC: A61K3150

    CPC classification number: A61K31/495

    Abstract: Piperazine derivatives useful in treating osteoporosis, bone fracture or deficiency, primary or secondary hyperparathyroidism, periodontal disease or defect, metastatic bone disorder, osteolytic bone disease, post-plastic surgery, post-prosthetic joint surgery and post-dental implantation.

    Abstract translation: 可用于治疗骨质疏松症，骨折或缺陷，原发性或继发性甲状旁腺功能亢进，牙周病或缺损，转移性骨病，溶骨性骨病，整形外手术，假体后关节外科手术和牙植入后的哌嗪衍生物。

    Glucagon antagonists
    9.
    发明授权
    Glucagon antagonists 失效
    胰高血糖素拮抗剂

    公开(公告)号：US5510459A

    公开(公告)日：1996-04-23

    申请号：US937132

    申请日：1992-08-27

    Applicant: Robert A. Smith ,  James R. Piggott

    Inventor： Robert A. Smith ,  James R. Piggott

    IPC: C07K14/575 ,  C07K14/605 ,  C12N1/19 ,  C12N15/09 ,  C12N15/16 ,  C12P21/02 ,  C12R1/865 ,  G01N33/53 ,  A61K38/26 ,  C07K14/00

    CPC classification number: C07K14/605

    Abstract: Methods for detecting glucagon antagonists through the use of recombinant DNA techniques are provided. Briefly, subsequent to the expression of glucagon analogs within suitable host cells, the analogs are exposed to a glucagon receptor coupled to a response pathway in the presence of native glucagon. A reduction in the stimulation of the response pathway resulting from the binding of the glucagon analog to the glucagon receptor relative to the stimulation of the response pathway by native glucagon alone indicates the presence of a glucagon antagonist. Glucagon antagonists identified and isolated through the methods are also provided.

    Abstract translation: 提供了通过使用重组DNA技术检测胰高血糖素拮抗剂的方法。 简而言之，在合适的宿主细胞内表达胰高血糖素类似物之后，类似物暴露于在天然胰高血糖素存在下偶联至应答途径的胰高血糖素受体。 由胰高血糖素类似物与胰高血糖素受体的结合引起的反应途径的刺激相对于单独的天然胰高血糖素刺激反应途径的降低表明存在胰高血糖素拮抗剂。 还提供了通过该方法鉴定和分离的胰高血糖素拮抗剂。

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