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    • 1. 发明授权
    • Angiogenesis inhibitor
    • 血管生成抑制剂
    • US06214800B1
    • 2001-04-10
    • US09282501
    • 1999-04-09
    • Chiho FukiageMitsuyoshi AzumaJun InoueMasayuki NakamuraYuka Yoshida
    • Chiho FukiageMitsuyoshi AzumaJun InoueMasayuki NakamuraYuka Yoshida
    • A61K3800
    • A61K38/55C07C311/19C07D303/48
    • 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.
    • 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。
    • 3. 发明授权
    • Angiogenesis inhibitor
    • 血管生成抑制剂
    • US06551999B1
    • 2003-04-22
    • US09243822
    • 1999-02-03
    • Chiho FukiageMitsuyoshi AzumaJun InoueMasayuki NakamuraYuka Yoshida
    • Chiho FukiageMitsuyoshi AzumaJun InoueMasayuki NakamuraYuka Yoshida
    • C07K506
    • A61K38/55C07C311/19C07D303/48
    • 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.
    • 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。
    • 4. 发明授权
    • Piperazine derivatives and use as cysteine inhibitors
    • 哌嗪衍生物并用作半胱氨酸抑制剂
    • US5935959A
    • 1999-08-10
    • US983034
    • 1998-01-07
    • Jun InoueYuka YoshidaYing-She CuiMitsuyoshi Azuma
    • Jun InoueYuka YoshidaYing-She CuiMitsuyoshi Azuma
    • C07D303/48A61K31/495C07D405/06C07D405/14
    • C07D303/48
    • The present invention is directed to a compound of the following formula (I) inclusive of its salt ##STR1## �wherein R.sup.1 represents either carboxy which may be esterified or amidated carboxy which may be substituted; R.sup.2 represents hydrogen or lower alkyl and may be linked to R.sup.3 or R.sup.4 to form a ring; R.sup.3 and R.sup.4 may be the same or different and each represents hydrogen, lower alkyl which may be substituted, or a sulfide group which may be substituted, and R.sup.3 and R.sup.4 may conjoinedly form a ring; R.sup.5 represents a substituted phenyl group of formula (II) ##STR2## (wherein R.sup.6 represents halogen or alkoxy) or a substituted sulfonyl group of formula (III)--SO.sub.2 --R.sup.7 (III)(wherein R.sup.7 represents either aryl which may be substituted by lower alkyl or amino which may be substituted); n is to 0 or 1! and to a method for producing the same compound, which is useful for the treatment of cysteine protease-associated diseases.
    • PCT No.PCT / JP96 / 01884第 371日期:1998年1月7日 102(e)1998年1月7日PCT PCT 1996年7月4日PCT公布。 公开号WO97 / 03060 PCT 日本1997年1月30日本发明涉及下述式(I)的化合物,其中包括其盐[其中R 1表示可以被酯化或酰胺化的羧基的羧基; R 2表示氢或低级烷基,并且可以与R 3或R 4连接形成环; R 3和R 4可以相同或不同,各自表示氢,可被取代的低级烷基或可被取代的硫基,R3和R4可以结合形成环; R 5表示式(II)的取代苯基(其中R 6表示卤素或烷氧基)或式(III)-SO 2 -R 7(III)的取代磺酰基(其中R 7表示可被低级烷基取代的芳基或 可以被取代的氨基); n为0或1]以及可用于治疗半胱氨酸蛋白酶相关疾病的相同化合物的制备方法。