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1.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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3.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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4.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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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：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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6.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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7.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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公开(公告)号：US06881725B2
公开(公告)日：2005-04-19
申请号：US10355699
申请日：2003-01-31
IPC分类号： C07H19/20 , A61K31/675 , A61K31/7072 , A61K31/7076 , A61K31/7084 , A61P23/00 , A61P25/04 , A61P25/06 , A61P29/00 , C07H19/207 , C07H21/00 , A61K31/70
CPC分类号： A61K31/7076 , A61K31/675 , A61K31/7072 , A61K31/7084 , Y10S514/851
摘要： The present invention is directed to a method of treating pain. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a P2X receptor antagonist. The methods of the present invention are useful in reducing pain, such as traumatic pain, neuropathic pain, organ pain and pain associated with diseases. The P2X receptor antagonists particularly useful for this invention are mononucleoside polyphosphate derivatives or dinucleoside polyphosphate derivatives of general Formula I. The compounds of the present method can be used alone to treat pain. The compounds of the present method can also be used in conjunction with other therapeutic agents or adjunctive therapies commonly used to treat pain, thus enhancing the overall pain-reducing effect in a subject in need of such treatment.
摘要翻译： 本发明涉及治疗疼痛的方法。 该方法包括向受试者施用包含有效量的P2X受体拮抗剂的药物组合物。 本发明的方法可用于减轻疼痛，例如创伤性疼痛，神经性疼痛，器官疼痛和与疾病相关的疼痛。 特别可用于本发明的P2X受体拮抗剂是通式I的单核苷多磷酸衍生物或二核苷多磷酸衍生物。本发明方法的化合物可单独用于治疗疼痛。 本发明方法的化合物还可以与通常用于治疗疼痛的其它治疗剂或辅助疗法结合使用，从而增强需要这种治疗的受试者的整体疼痛减轻作用。
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公开(公告)号：US07612047B2
公开(公告)日：2009-11-03
申请号：US12208265
申请日：2008-09-10
申请人： James G. Douglass, III , Benjamin R. Yerxa , Sammy R. Shaver , Ward M. Peterson , Edward G. Brown , Christopher S. Crean , José L. Boyer
发明人： James G. Douglass, III , Benjamin R. Yerxa , Sammy R. Shaver , Ward M. Peterson , Edward G. Brown , Christopher S. Crean , José L. Boyer
摘要： The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation-resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation-resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides. The mononucleoside phosphate compounds of the present invention are useful in preventing and treating epithelial tissue diseases or diseases or disorders associated with platelet aggregation.
摘要翻译： 本发明涉及具有二核苷酸药物益处的单核苷磷酸化合物。 这些单核苷酸磷酸酯可以由已经通过在聚磷酸酯单核苷酸的末端磷酸酯上连接降解抗性取代基而被修饰的单核苷酸制成。 通过连接该降解抗性的取代基，降解的稳定性与某些二核苷酸的匹配或超过某些二核苷酸。 本发明的单核苷磷酸化合物可用于预防和治疗与血小板聚集有关的上皮组织疾病或疾病或病症。
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公开(公告)号：US20090076256A1
公开(公告)日：2009-03-19
申请号：US12208265
申请日：2008-09-10
申请人： James G. Douglass, III , Benjamin R. Yerxa , Sammy R. Shaver , Ward M. Peterson , Edward G. Brown , Christopher S. Crean , Jose L. Boyer
发明人： James G. Douglass, III , Benjamin R. Yerxa , Sammy R. Shaver , Ward M. Peterson , Edward G. Brown , Christopher S. Crean , Jose L. Boyer
IPC分类号： C07H19/20
摘要： The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation-resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation-resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides. The mononucleoside phosphate compounds of the present invention are useful in preventing and treating epithelial tissue diseases or diseases or disorders associated with platelet aggregation.
摘要翻译： 本发明涉及具有二核苷酸药物益处的单核苷磷酸化合物。 这些单核苷酸磷酸酯可以由已经通过在聚磷酸酯单核苷酸的末端磷酸酯上连接降解抗性取代基而被修饰的单核苷酸制成。 通过连接该降解抗性的取代基，降解的稳定性与某些二核苷酸的匹配或超过某些二核苷酸。 本发明的单核苷磷酸化合物可用于预防和治疗与血小板聚集有关的上皮组织疾病或疾病或病症。
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