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1.发明申请METHOD FOR TREATING OPHTHALMIC DISEASES USING RHO KINASE INHIBITOR COMPOUNDS 审中-公开使用RHO激酶抑制剂化合物治疗眼底疾病的方法公开(公告)号：US20090325959A1
公开(公告)日：2009-12-31
申请号：US12492603
申请日：2009-06-26
IPC分类号： A61K31/5377 , A61K31/454 , A61K31/416 , A61K31/496 , A61K31/4725 , A61P27/02 , A61P27/14
CPC分类号： A61K31/416 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/5377
摘要： This invention is directed to methods of preventing or treating ocular diseases with inflammation, excessive cell proliferation, remodeling, neurite retraction, corneal neurodegeneration, excessive vaso-permeability and edema. Particularly, this invention relates to methods treating ocular diseases such as allergic conjunctivitis, corneal hyposensitivity, neurotrophic keratopathy, dry eye disease, proliferative vitreal retinopathy, macular edema, macular degeneration, and blepharitis, using novel Rho kinase inhibitor compounds. The method comprises identifying a subject in need of the treatment, and administering to the subject an effective amount of a novel Rho kinase inhibitor compound to treat the disease.
摘要翻译： 本发明涉及预防或治疗具有炎症，过度细胞增殖，重塑，神经突回缩，角膜神经变性，过度血管通透性和水肿的眼部疾病的方法。 特别地，本发明涉及使用新型Rho激酶抑制剂化合物治疗眼部疾病如过敏性结膜炎，角膜过敏症，神经营养性角膜病，干眼病，增殖性玻璃体视网膜病变，黄斑水肿，黄斑变性和睑炎的治疗方法。 该方法包括鉴定需要治疗的受试者，并向受试者施用有效量的新型Rho激酶抑制剂化合物以治疗该疾病。
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2.发明申请CYTOSKELETAL ACTIVE RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE 有权CYPOSKELETAL活性RHO激酶抑制剂化合物，组合物和用途公开(公告)号：US20080214614A1
公开(公告)日：2008-09-04
申请号：US11958214
申请日：2007-12-17
申请人： John W. Lampe , Paul S. Watson , David J. Slade , Ward M. Peterson , Christopher S. Crean , Jason L. Vittitow , Jonathan Bryan DeCamp , Nicholas F. Pelz
发明人： John W. Lampe , Paul S. Watson , David J. Slade , Ward M. Peterson , Christopher S. Crean , Jason L. Vittitow , Jonathan Bryan DeCamp , Nicholas F. Pelz
IPC分类号： A61K31/454 , C07D401/12 , C07D403/12 , A61K31/416 , A61P27/02
CPC分类号： C07D401/12 , A61F9/00781 , A61K9/0048 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14
摘要： The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. 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 cytoskeletal reorganization. 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 Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.
摘要翻译： 本发明涉及作为rho相关蛋白激酶抑制剂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细胞骨架重组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或式II的细胞骨架活性化合物，其中所述量可有效影响肌动球蛋白相互作用，例如通过导致细胞松弛和细胞粘附的变化。
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公开(公告)号：US08604218B2
公开(公告)日：2013-12-10
申请号：US13273043
申请日：2011-10-13
申请人： John W. Lampe , Paul S. Watson , David J. Slade , Ward M. Peterson , Christopher S. Crean , Jason L. Vittitow , Jonathan Bryan DeCamp , Nicholas F. Pelz
发明人： John W. Lampe , Paul S. Watson , David J. Slade , Ward M. Peterson , Christopher S. Crean , Jason L. Vittitow , Jonathan Bryan DeCamp , Nicholas F. Pelz
IPC分类号： C07D231/56 , C07D421/00
CPC分类号： C07D401/12 , A61F9/00781 , A61K9/0048 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14
摘要： The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. 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 cytoskeletal reorganization. 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 Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.
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4.发明申请CYTOSKELETAL ACTIVE RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE 有权CYPOSKELETAL活性RHO激酶抑制剂化合物，组合物和用途公开(公告)号：US20130012543A1
公开(公告)日：2013-01-10
申请号：US13614641
申请日：2012-09-13
申请人： John W. LAMPE , Paul S. Watson , David J. Slade , Ward M. Peterson , Christopher S. Crean , Jason L. Vittitow , Jonathan Bryan DeCamp , Nicholas F. Pelz
发明人： John W. LAMPE , Paul S. Watson , David J. Slade , Ward M. Peterson , Christopher S. Crean , Jason L. Vittitow , Jonathan Bryan DeCamp , Nicholas F. Pelz
IPC分类号： C07D401/14 , A61P27/02 , C07D409/14 , A61K31/454 , C07D405/14
CPC分类号： C07D401/12 , A61F9/00781 , A61K9/0048 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14
摘要： The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. 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 cytoskeletal reorganization. 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 Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.
摘要翻译： 本发明涉及作为rho相关蛋白激酶抑制剂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细胞骨架重组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或式II的细胞骨架活性化合物，其中所述量可有效影响肌动球蛋白相互作用，例如通过导致细胞松弛和细胞粘附的变化。
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5.发明申请CYTOSKELETAL ACTIVE RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE 有权CYPOSKELETAL活性RHO激酶抑制剂化合物，组合物和用途公开(公告)号：US20120046275A1
公开(公告)日：2012-02-23
申请号：US13273043
申请日：2011-10-13
申请人： John W. Lampe , Paul S. Watson , David J. Slade , Ward M. Peterson , Christopher S. Crean , Jason L. Vittitow , Jonathan Bryan DeCamp , Nicholas F. Pelz
发明人： John W. Lampe , Paul S. Watson , David J. Slade , Ward M. Peterson , Christopher S. Crean , Jason L. Vittitow , Jonathan Bryan DeCamp , Nicholas F. Pelz
IPC分类号： A61K31/416 , C07D401/12 , A61P27/02 , A61K31/4725 , C07D403/12 , A61K31/55 , C07D231/56 , A61K31/454
CPC分类号： C07D401/12 , A61F9/00781 , A61K9/0048 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14
摘要： The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. 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 cytoskeletal reorganization. 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 Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.
摘要翻译： 本发明涉及作为rho相关蛋白激酶抑制剂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细胞骨架重组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或式II的细胞骨架活性化合物，其中所述量可有效影响肌动球蛋白相互作用，例如通过导致细胞松弛和细胞粘附的变化。
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6.发明授权公开(公告)号：US08604205B2
公开(公告)日：2013-12-10
申请号：US13614641
申请日：2012-09-13
申请人： John W. Lampe , Paul S. Watson , David J. Slade , Ward M. Peterson , Christopher S. Crean , Jason L. Vittitow , Jonathan Bryan DeCamp , Nicholas F. Pelz
发明人： John W. Lampe , Paul S. Watson , David J. Slade , Ward M. Peterson , Christopher S. Crean , Jason L. Vittitow , Jonathan Bryan DeCamp , Nicholas F. Pelz
IPC分类号： C07D211/32 , A01N43/40
CPC分类号： C07D401/12 , A61F9/00781 , A61K9/0048 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14
摘要： The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. 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 cytoskeletal reorganization. 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 Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.
摘要翻译： 本发明涉及作为rho相关蛋白激酶抑制剂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细胞骨架重组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或式II的细胞骨架活性化合物，其中所述量可有效影响肌动球蛋白相互作用，例如通过导致细胞松弛和细胞粘附的变化。
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7.发明授权公开(公告)号：US08071779B2
公开(公告)日：2011-12-06
申请号：US11958214
申请日：2007-12-17
申请人： John W. Lampe , Paul S. Watson , David J. Slade , Ward M. Peterson , Christopher S. Crean , Jason L. Vittitow , Jonathan Bryan DeCamp , Nicholas F. Pelz
发明人： John W. Lampe , Paul S. Watson , David J. Slade , Ward M. Peterson , Christopher S. Crean , Jason L. Vittitow , Jonathan Bryan DeCamp , Nicholas F. Pelz
IPC分类号： C07D211/32 , C07D231/56
CPC分类号： C07D401/12 , A61F9/00781 , A61K9/0048 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14
摘要： The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. 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 cytoskeletal reorganization. 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 Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.
摘要翻译： 本发明涉及作为rho相关蛋白激酶抑制剂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细胞骨架重组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或式II的细胞骨架活性化合物，其中所述量可有效影响肌动球蛋白相互作用，例如通过导致细胞松弛和细胞粘附的变化。
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公开(公告)号：US20100130572A1
公开(公告)日：2010-05-27
申请号：US12695348
申请日：2010-01-28
申请人： John W. LAMPE , Robert Plourde, JR. , Jin She , Jason L. Vittitow , Paul S. Watson , Michael T. Crimmins , David J. Slade
发明人： John W. LAMPE , Robert Plourde, JR. , Jin She , Jason L. Vittitow , Paul S. Watson , Michael T. Crimmins , David J. Slade
IPC分类号： A61K31/427 , C07D417/04 , C07D493/08 , A61K31/426 , A61P27/00
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。
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公开(公告)号：US08039465B2
公开(公告)日：2011-10-18
申请号：US12695348
申请日：2010-01-28
申请人： John W. Lampe , Robert Plourde, Jr. , Jin She , Jason L. Vittitow , Paul S. Watson , Michael T. Crimmins , David J. Slade
发明人： John W. Lampe , Robert Plourde, Jr. , Jin She , Jason L. Vittitow , Paul S. Watson , Michael T. Crimmins , David J. Slade
IPC分类号： A61K31/54
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。
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公开(公告)号：US07666861B2
公开(公告)日：2010-02-23
申请号：US11950327
申请日：2007-12-04
申请人： John W. Lampe , Robert Plourde, Jr. , Jin She , Jason L. Vittitow , Paul S. Watson , Michael T. Crimmins , David J. Slade
发明人： John W. Lampe , Robert Plourde, Jr. , Jin She , Jason L. Vittitow , Paul S. Watson , Michael T. Crimmins , David J. Slade
IPC分类号： A61K31/351 , A61K31/357 , C07D309/06 , C07D313/02 , C07D313/16
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。
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