利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

76 条记录 (耗时 0.026 秒)

    Piperazine derivatives and use as cysteine inhibitors
    1.
    发明授权
    Piperazine derivatives and use as cysteine inhibitors 失效
    哌嗪衍生物并用作半胱氨酸抑制剂

    公开(公告)号：US5935959A

    公开(公告)日：1999-08-10

    申请号：US983034

    申请日：1998-01-07

    申请人： Jun Inoue ,  Yuka Yoshida ,  Ying-She Cui ,  Mitsuyoshi Azuma

    发明人： Jun Inoue ,  Yuka Yoshida ,  Ying-She Cui ,  Mitsuyoshi Azuma

    IPC分类号： C07D303/48 ,  A61K31/495 ,  C07D405/06 ,  C07D405/14

    CPC分类号： C07D303/48

    摘要： 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.

    摘要翻译： 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。

    Angiogenesis inhibitor
    2.
    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

    申请人： Chiho Fukiage ,  Mitsuyoshi Azuma ,  Jun Inoue ,  Masayuki Nakamura ,  Yuka Yoshida

    发明人： Chiho Fukiage ,  Mitsuyoshi Azuma ,  Jun Inoue ,  Masayuki Nakamura ,  Yuka Yoshida

    IPC分类号： A61K3800

    CPC分类号： A61K38/55 ,  C07C311/19 ,  C07D303/48

    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
    3.
    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

    申请人： Chiho Fukiage ,  Mitsuyoshi Azuma ,  Jun Inoue ,  Masayuki Nakamura ,  Yuka Yoshida

    发明人： Chiho Fukiage ,  Mitsuyoshi Azuma ,  Jun Inoue ,  Masayuki Nakamura ,  Yuka Yoshida

    IPC分类号： C07K506

    CPC分类号： A61K38/55 ,  C07C311/19 ,  C07D303/48

    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
    4.
    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

    申请人： Chiho Fukiage ,  Mitsuyoshi Azuma ,  Jun Inoue ,  Masayuki Nakamura ,  Yuka Yoshida

    发明人： Chiho Fukiage ,  Mitsuyoshi Azuma ,  Jun Inoue ,  Masayuki Nakamura ,  Yuka Yoshida

    IPC分类号： A61K38/55 ,  C07C311/19 ,  C07D303/48 ,  A61K38/00 ,  C07K5/00 ,  C07K7/00

    CPC分类号： A61K38/55 ,  C07C311/19 ,  C07D303/48

    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。

    Remedy for corneal failure
    6.
    发明申请
    Remedy for corneal failure 审中-公开
    角膜失败的补救措施

    公开(公告)号：US20060234922A1

    公开(公告)日：2006-10-19

    申请号：US10533115

    申请日：2003-10-22

    申请人： Yoshiko Takayama ,  Yoshikuni Nakamura ,  Jun Inoue ,  Mitsuyoshi Azuma

    发明人： Yoshiko Takayama ,  Yoshikuni Nakamura ,  Jun Inoue ,  Mitsuyoshi Azuma

    IPC分类号： A61K31/4545 ,  A61K31/454 ,  A61K38/12 ,  A61K38/10

    CPC分类号： A61K38/31 ,  A61K31/00

    摘要： The present invention provides a new type of pharmaceutical agent that recovers corneal sensitivity after corneal surgery or improves the condition of dry eye. Application of a somatostatin receptor agonist is expected to provide an improvement effect on decreased corneal sensitivity after cataract surgery or LASIK surgery, decreased corneal sensitivity and dry eye associated with corneal neurodegeneration such as neuroparalytic keratopathy, corneal ulcer, diabetic keratopathy and the like.

    摘要翻译： 本发明提供了在角膜手术后恢复角膜敏感性或改善干眼症状的新型药剂。 预期生长抑素受体激动剂的应用对于白内障手术或LASIK手术后的角膜敏感性降低，与角膜神经变性如神经麻痹性角膜病，角膜溃疡，糖尿病性角膜病等相关的角膜敏感性和干眼症的降低有改善作用。

    Pharmaceutical composition for prophylaxis and therapy of diseases associated with ocular fundus tissue cytography
    8.
    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

    申请人： Mitsuyoshi Azuma ,  Yukuo Yoshida ,  Yuji Sakamoto ,  Jun Inoue

    发明人： Mitsuyoshi Azuma ,  Yukuo Yoshida ,  Yuji Sakamoto ,  Jun Inoue

    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
    10.
    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

    申请人： Mitsuyoshi Azuma ,  Yukuo Yoshida ,  Yuji Sakamoto ,  Jun Inoue

    发明人： Mitsuyoshi Azuma ,  Yukuo Yoshida ,  Yuji Sakamoto ,  Jun Inoue

    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。