Pharmaceutical composition for prophylaxis and therapy of diseases associated with ocular fundus tissue cytography
    1.
    发明授权
    Pharmaceutical composition for prophylaxis and therapy of diseases associated with ocular fundus tissue cytography 失效
    用于预防和治疗眼底组织细胞病变相关疾病的药物组合物

    公开(公告)号:US06423691B1

    公开(公告)日:2002-07-23

    申请号:US09623393

    申请日:2000-09-05

    IPC分类号: A61K3800

    CPC分类号: A61K38/00 A61K31/18

    摘要: A pharmaceutical composition for the prophylaxis and therapy of a disease arising from ocular fundus tissue cytopathy such as retinochoroidal disease, glaucoma, and posterior complication arising form photocoagulation, which contains, as an active ingredient, a compound of formula (I) wherein R1 represents an alkyl group having 1 to 4 carbon atoms or an aryl group having 6 to 10 carbon atoms which is optionally substituted; R2 and R3 may be the same or different and each represents hydrogen or an alkyl group having 1 to 4 carbon atoms or R2 and R3 may jointly form a ring having 3 to 7 carbon atoms; and R4 represents a lower alkyl group which substituted by aryl, cycloalkyl, or aromatic heterocyclic residue, or a pharmaceutically acceptable salt thereof.

    摘要翻译: 一种用于预防和治疗由眼底组织细胞病变(例如视网膜色素性疾病,青光眼和由光凝产生的后期并发症)引起的疾病的药物组合物,其包含作为活性成分的式(I)化合物,其中R 1表示 具有1至4个碳原子的烷基或任选被取代的具有6至10个碳原子的芳基; R2和R3可以相同或不同,各自表示氢或具有1-4个碳原子的烷基,或者R2和R3可以共同形成具有3至7个碳原子的环; R 4表示被芳基,环烷基或芳香杂环残基取代的低级烷基或其药学上可接受的盐。

    Pharmaceutical composition containing a cysteine protease inhibitor for prophylaxis and therapy of brain tissue impairment
    2.
    发明授权
    Pharmaceutical composition containing a cysteine protease inhibitor for prophylaxis and therapy of brain tissue impairment 失效
    含有用于预防和治疗脑组织损伤的半胱氨酸蛋白酶抑制剂的药物组合物

    公开(公告)号:US06342531B1

    公开(公告)日:2002-01-29

    申请号:US09646529

    申请日:2000-09-19

    IPC分类号: A61K3118

    CPC分类号: A61K31/18 A61K31/16 A61K38/05

    摘要: A pharmaceutical composition for the prophylaxis and therapy of brain tissue impairment, which contains, as an active ingredient, a compound of the following formula (I) wherein R1 represents an alkyl group having 1-4 carbon atoms or an aryl group having 6-10 carbon atoms which is optionally substituted; R2 and R3 may be the same or different and each represents hydrogen or an alkyl group having 1-4 carbon atoms or R2 and R3 may jointly form a ring having 3-7 carbon atoms; and R4 represents a lower alkyl group which is optionally substituted by aryl, cycloalkyl, or aromatic heterocyclic residue, or a pharmaceutically acceptable salt thereof.

    摘要翻译: 一种用于预防和治疗脑组织损伤的药物组合物,其包含作为活性成分的下式(I)的化合物,其中R 1表示具有1-4个碳原子的烷基或具有6-10的芳基 任选取代的碳原子; R2和R3可以相同或不同,各自表示氢或具有1-4个碳原子的烷基,或者R2和R3可以共同形成具有3-7个碳原子的环; R 4表示任选被芳基,环烷基或芳族杂环残基取代的低级烷基或其药学上可接受的盐。

    Preventives/remedies for glaucoma
    3.
    发明授权
    Preventives/remedies for glaucoma 有权
    青光眼的预防/补救措施

    公开(公告)号:US06673812B1

    公开(公告)日:2004-01-06

    申请号:US09529354

    申请日:2000-04-13

    IPC分类号: A61K3144

    摘要: An agent for the prophylaxis and treatment of glaucoma, which contains a compound having a Rho kinase inhibitory activity, particularly an agent for the prophylaxis and treatment of glaucoma, which contains a compound of the formula (I) wherein each symbol is as defined in the specification, as the compound having a Rho kinase inhibitory activity, is provided. The agent for the prophylaxis and treatment of glaucoma of the present invention is a novel agent for the prophylaxis and treatment of glaucoma and has intraocular pressure lowering action, optic disc blood flow improving action and aqueous humor outflow promoting action.

    摘要翻译: 一种用于预防和治疗青光眼的药剂,其含有具有Rho激酶抑制活性的化合物,特别是用于预防和治疗青光眼的药物,其含有式(I)化合物,其中每个符号如 规定,作为具有Rho激酶抑制活性的化合物。 用于预防和治疗本发明青光眼的药剂是用于预防和治疗青光眼的新型药剂,具有降眼压作用,视盘血流改善作用和房水流出促进作用。

    Agent for prophylaxis and treatment of glaucoma
    4.
    发明授权
    Agent for prophylaxis and treatment of glaucoma 失效
    青光眼预防和治疗药物

    公开(公告)号:US06649625B2

    公开(公告)日:2003-11-18

    申请号:US10298674

    申请日:2002-11-19

    IPC分类号: A61K3144

    摘要: An agent for the prophylaxis and treatment of glaucoma, which contains a compound having a Rho kinase inhibitory activity, particularly an agent for the prophylaxis and treatment of glaucoma, which contains a compound of the formula (I) wherein each symbol is as defined in the specification, as the compound having a Rho kinase inhibitory activity, is provided. The agent for the prophylaxis and treatment of glaucoma of the present invention is a novel agent for the prophylaxis and treatment of glaucoma and has intraocular pressure lowering action, optic disc blood flow improving action and aqueous humor outflow promoting action.

    摘要翻译: 一种用于预防和治疗青光眼的药剂,其含有具有Rho激酶抑制活性的化合物,特别是用于预防和治疗青光眼的药物,其含有式(I)的化合物,其中每个符号如 规定,作为具有Rho激酶抑制活性的化合物。 用于预防和治疗本发明青光眼的药剂是用于预防和治疗青光眼的新型药剂,具有降眼压作用,视盘血流改善作用和房水流出促进作用。

    Angiogenesis inhibitor
    5.
    发明授权
    Angiogenesis inhibitor 失效
    血管生成抑制剂

    公开(公告)号:US06214800B1

    公开(公告)日:2001-04-10

    申请号:US09282501

    申请日:1999-04-09

    IPC分类号: A61K3800

    摘要: An angiogenesis inhibitor comprising a cysteine protease inhibitory compound. As the preferable cysteine protease inhibitory compound, epoxysuccinic acid compounds, peptide halohydrazide compounds, calpain inhibitory compounds, compounds of the formula (I) and compounds of the formula (VI) can be used. The angiogenesis inhibitor of the present invention suppresses new formation of blood vessels in the living tissues, so that it can be used as a superior therapeutic or prophylactic agent of angiogenesis associated with wound healing, inflammation, growth of tumor and the like; and angiogenesis as seen in diabetic retinopathy, prematurity retinopathy, retinal venous occlusion, senile discoid macular degeneration and the like, as well as for prevention of metastasis of tumors.

    摘要翻译: 一种包含半胱氨酸蛋白酶抑制化合物的血管生成抑制剂。 作为优选的半胱氨酸蛋白酶抑制化合物,可以使用环氧琥珀酸化合物,肽卤代酰肼化合物,钙蛋白酶抑制化合物,式(I)的化合物和式(VI)的化合物。 本发明的血管发生抑制剂抑制活组织中血管的新形成,可以用作与伤口愈合,炎症,肿瘤生长等有关的血管生成的优异治疗或预防剂。 和血管生成,如糖尿病视网膜病变,早产儿视网膜病变,视网膜静脉闭塞,老年性盘状黄斑变性等,以及用于预防肿瘤转移。

    Angiogenesis inhibitor
    7.
    发明授权
    Angiogenesis inhibitor 失效
    血管生成抑制剂

    公开(公告)号:US06551999B1

    公开(公告)日:2003-04-22

    申请号:US09243822

    申请日:1999-02-03

    IPC分类号: C07K506

    摘要: An angiogenesis inhibitor comprising a cysteine protease inhibitory compound. As the preferable cysteine protease inhibitory compound, epoxysuccinic acid compounds, peptide halohydrazide compounds, calpain inhibitory compounds, compounds of the formula (I) and compounds of the formula (VI) can be used. The angiogenesis inhibitor of the present invention suppresses new formation of blood vessels in the living tissues, so that it can be used as a superior therapeutic or prophylactic agent of angiogenesis associated with wound healing, inflammation, growth of tumor and the like; and angiogenesis as seen in diabetic retinopathy, prematurity retinopathy, retinal venous occlusion, senile discoid macular degeneration and the like, as well as for prevention of metastasis of tumors.

    摘要翻译: 一种包含半胱氨酸蛋白酶抑制化合物的血管生成抑制剂。 作为优选的半胱氨酸蛋白酶抑制化合物,可以使用环氧琥珀酸化合物,肽卤代酰肼化合物,钙蛋白酶抑制化合物,式(I)的化合物和式(VI)的化合物。 本发明的血管发生抑制剂抑制活组织中血管的新形成,可以用作与伤口愈合,炎症,肿瘤生长等有关的血管生成的优异治疗或预防剂。 和血管生成,如糖尿病视网膜病变,早产儿视网膜病变,视网膜静脉闭塞,老年性盘状黄斑变性等,以及用于预防肿瘤转移。

    Angiogenesis inhibitor
    9.
    发明授权
    Angiogenesis inhibitor 失效
    血管生成抑制剂

    公开(公告)号:US6057290A

    公开(公告)日:2000-05-02

    申请号:US740069

    申请日:1996-10-24

    摘要: An angiogenesis inhibitor comprising a cysteine protease inhibitory compound. As the preferable cysteine protease inhibitory compound, epoxysuccinic acid compounds, peptide halohydrazide compounds, calpain inhibitory compounds, compounds of the formula (I) ##STR1## and compounds of the formula (VI) ##STR2## can be used. The angiogenesis inhibitor of the present invention suppresses new formation of blood vessels in the living tissues, so that it can be used as a superior therapeutic or prophylactic agent of angiogenesis associated with wound healing, inflammation, growth of tumor and the like; and angiogenesis as seen in diabetic retinopathy, prematurity retinopathy, retinal venous occlusion, senile discoid macular degeneration and the like, as well as for prevention of metastasis of tumors.

    摘要翻译: 一种包含半胱氨酸蛋白酶抑制化合物的血管生成抑制剂。 作为优选的半胱氨酸蛋白酶抑制化合物,可以使用环氧琥珀酸化合物,肽卤代酰肼化合物,钙蛋白酶抑制化合物,式(I)的化合物和式(VI)的化合物。 本发明的血管发生抑制剂抑制活组织中血管的新形成,可以用作与伤口愈合,炎症,肿瘤生长等有关的血管生成的优异治疗或预防剂。 和血管生成,如糖尿病视网膜病变,早产儿视网膜病变,视网膜静脉闭塞,老年性盘状黄斑变性等,以及用于预防肿瘤转移。