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1. 发明申请

US20080076735A1 CYTOSKELETAL ACTIVE COMPOUNDS, COMPOSITION AND USE 失效
标题翻译： CYTOSKELETAL活性化合物，组合物和用途
公开(公告)号：US20080076735A1
公开(公告)日：2008-03-27
申请号：US11950327
申请日：2007-12-04
申请人： John Lampe , Robert Plourde , Jin She , Jason Vittitow , Paul Watson , Michael Crimmins , David Slade
发明人： John Lampe , Robert Plourde , Jin She , Jason Vittitow , Paul Watson , Michael Crimmins , David Slade
IPC分类号： A61K31/695 , A61K31/19 , A61K31/215 , C07C229/00 , C07D277/02 , C07F7/02 , C07C69/00 , A61P27/00 , A61K31/426
CPC分类号： C07D491/08 , C07D277/06 , C07D277/14 , C07D277/16 , C07D277/34 , C07D277/56 , C07D417/04 , C07D493/08 , C07D497/18
摘要： The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.
摘要翻译：本发明涉及与天然的秋水仙素A或梭菌素B相关的合成细胞骨架活性化合物。本发明还涉及包含这些化合物和药学上可接受的载体的药物组合物。本发明另外涉及预防或治疗与肌动蛋白聚合相关的疾病或病症的方法。在本发明的一个实施方案中，该方法治疗增加的眼内压，例如原发性开角型青光眼。该方法包括向受试者施用治疗有效量的式I或II的细胞骨架活性化合物，其中所述量有效影响细胞骨架，例如通过抑制肌动蛋白聚合。

2. 发明申请

US20060217427A1 Cytoskeletal active compounds, compositions and use 失效
标题翻译：细胞骨架活性化合物，组合物和用途
公开(公告)号：US20060217427A1
公开(公告)日：2006-09-28
申请号：US11389665
申请日：2006-03-23
申请人： John Lampe , Robert Plourde , Jin She , Jason Vittitow , Paul Watson , Michael Crimmins , David Slade
发明人： John Lampe , Robert Plourde , Jin She , Jason Vittitow , Paul Watson , Michael Crimmins , David Slade
IPC分类号： A61K31/426 , A61K31/422 , A61K31/4178 , C07D413/02 , C07D417/02 , C07D405/02
CPC分类号： C07D491/08 , C07D277/06 , C07D277/14 , C07D277/16 , C07D277/34 , C07D277/56 , C07D417/04 , C07D493/08 , C07D497/18
摘要： The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.
摘要翻译：本发明涉及与天然的秋水仙素A或梭菌素B相关的合成细胞骨架活性化合物。本发明还涉及包含这些化合物和药学上可接受的载体的药物组合物。本发明另外涉及预防或治疗与肌动蛋白聚合相关的疾病或病症的方法。在本发明的一个实施方案中，该方法治疗增加的眼内压，例如原发性开角型青光眼。该方法包括向受试者施用治疗有效量的式I或II的细胞骨架活性化合物，其中所述量有效影响细胞骨架，例如通过抑制肌动蛋白聚合。

3. 发明申请

US20070265247A1 METHOD OF REDUCING CONTACT LENS INTOLERANCE WITH NON-DRYING ANTIHISTAMINES 审中-公开
标题翻译：使用非干性抗生素降低接触镜片不透明度的方法
公开(公告)号：US20070265247A1
公开(公告)日：2007-11-15
申请号：US11766702
申请日：2007-06-21
申请人： Benjamin Yerxa , Jason Vittitow , John Ice , Ramesh Krishnamoorthy
发明人： Benjamin Yerxa , Jason Vittitow , John Ice , Ramesh Krishnamoorthy
IPC分类号： A61K31/55 , A61P27/14
CPC分类号： A61K31/55 , Y10S514/912
摘要： A method and preparation for reducing dry eye symptoms and promoting tear secretion in a subject in need of such treatment is disclosed. The method is useful in treating dry eye diseases. The method is also useful in reducing contact lens intolerance in the eyes. The method comprises administering to the eyes of a subject in need thereof a non-drying antihistamine compound, such as epinastine hydrochloride, in an amount effective to reduce dry eye symptoms and stimulate tear fluid secretion. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the compound include topical administration via a liquid, gel, cream, or as part of a contact lens or a continuous or selective release device; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form, injectable, intra-operative instillation or suppository form.
摘要翻译：公开了减少需要这种治疗的受试者的干眼症状和促进泪液分泌的方法和制剂。该方法可用于治疗干眼病。该方法也可用于减少眼睛中的隐形眼镜不耐受。该方法包括以有效减少干眼症状并刺激泪液分泌的量向有需要的受试者的眼睛施用非干燥的抗组胺药化合物，例如盐酸依诺斯汀。还公开了药物制剂及其制备方法。施用化合物的方法包括通过液体，凝胶，霜剂或作为隐形眼镜或连续或选择性释放装置的一部分的局部给药; 或通过鼻滴或喷雾进行全身给药，通过喷雾器或其他装置吸入，口服形式，可注射的，术中滴注或栓剂形式。

4. 发明申请

US20070043025A1 Method of treating dry eye disease with non-drying antihistamines 失效
公开(公告)号：US20070043025A1
公开(公告)日：2007-02-22
申请号：US11503029
申请日：2006-08-10
申请人： Benjamin Yerxa , Jason Vittitow , John Ice
发明人： Benjamin Yerxa , Jason Vittitow , John Ice
IPC分类号： A61K31/55
CPC分类号： A61K31/55 , Y10S514/912
摘要： A method and preparation for reducing dry eye symptoms and promoting tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the eyes of the subject a non-drying antihistamine compound, such as epinastine hydrochloride, in an amount effective to reduce dry eye symptoms and stimulate tear fluid secretion. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the compound include topical administration via a liquid, gel, cream, or as part of a contact lens or a continuous or selective release device; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.

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