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    Alpha-Keto Carbonyl Calpain Inhibitors
    3.
    发明申请
    Alpha-Keto Carbonyl Calpain Inhibitors 审中-公开
    α-酮羰基钙蛋白酶抑制剂

    公开(公告)号：US20080058324A1

    公开(公告)日：2008-03-06

    申请号：US11574035

    申请日：2005-08-22

    申请人： Philipp Weyermann ,  Andreas Von Sprecher ,  Marco Hennebohle ,  Holger Herzner ,  Cyrille Lescop ,  Herve Siendt

    发明人： Philipp Weyermann ,  Andreas Von Sprecher ,  Marco Hennebohle ,  Holger Herzner ,  Cyrille Lescop ,  Herve Siendt

    IPC分类号： A61K31/381 ,  A61K31/4436 ,  A61K31/5377 ,  A61P21/00 ,  A61P25/00 ,  A61P9/00 ,  C07D333/24 ,  C07D409/02 ,  C07D413/02

    CPC分类号： C07K5/0202

    摘要： The present invention relates to novel a-keto carbonyl calpain inhibitors for the treatment of neurodegenerative diseases and neuromuscular diseases including Duchenne Muscular Dystrophy, Becker Muscular Dystrophy and other muscular dystrophies. Disuse atrophy and general muscle wasting can also be treated. Diseases of the eye, in particular cataract, can be treated as well. Generally all condition where elevated levels of calpains are involved can be treated. The compounds of the invention may also inhibit other thiol proteases such as cathepsin B, cathepsin H, cathepsin L, papain or the like. Multicatalytic Protease also known as proteasome may also be inhibited and the compounds can therefore be used to treat cell proliferative diseases such as cancer, psoriasis, and restenosis. The compounds of the present invention are also inhibitors of cell damage by oxidative stress through free radicals can he used to treat mitochondrial disorders and neurodegenerative diseases, where elevated levels of oxidative stress are involved. In addition they induce the expression of utrophin, which is beneficial for the treatment of Duchenne Muscular Dystrophy and Becker Muscular Dystrophy.

    摘要翻译： 本发明涉及用于治疗神经变性疾病和神经肌肉疾病的新型α-酮羰基钙蛋白酶抑制剂，包括Duchenne肌营养不良症，Becker肌营养不良症和其他肌营养不良症。 也可以治疗消除萎缩和一般肌肉消瘦。 眼睛疾病，特别是白内障也可以治疗。 一般来说，所有涉及钙蛋白水平升高的情况都可以被处理。 本发明的化合物还可以抑制其它巯基蛋白酶，例如组织蛋白酶B，组织蛋白酶H，组织蛋白酶L，木瓜蛋白酶等。 也称为蛋白酶体的多分析蛋白酶也可以被抑制，因此化合物可用于治疗细胞增殖性疾病如癌症，牛皮癣和再狭窄。 本发明的化合物也是通过自由基的氧化应激的细胞损伤的抑制剂，可用于治疗线粒体疾病和神经变性疾病，其中涉及氧化应激水平升高。 此外，它们诱导utrophin的表达，其有利于治疗杜氏肌营养不良症和贝克肌营养不良症。

    Alpha-Keto Carbonyl Calpain Inhibitors
    4.
    发明申请
    Alpha-Keto Carbonyl Calpain Inhibitors 审中-公开
    α-酮羰基钙蛋白酶抑制剂

    公开(公告)号：US20070293486A1

    公开(公告)日：2007-12-20

    申请号：US11574095

    申请日：2005-08-22

    申请人： Philipp Weyermann ,  Andreas Von Sprecher ,  Marco Hennebohle ,  Holger Herzner ,  Cyrille Lescop ,  Herve Siendt

    发明人： Philipp Weyermann ,  Andreas Von Sprecher ,  Marco Hennebohle ,  Holger Herzner ,  Cyrille Lescop ,  Herve Siendt

    IPC分类号： A61K31/535 ,  A61K31/38 ,  A61K31/385 ,  C07D339/02 ,  C07D413/00 ,  C07D401/00 ,  C07D333/10 ,  A61K31/44

    CPC分类号： C07K5/0202 ,  A61K38/00

    摘要： The present invention relates to novel α-keto carbonyl calpain inhibitors for the treatment of neurodegenerative diseases and neuromuscular diseases including Duchenne Muscular Dystrophy, Becker Muscular Dystrophy and other muscular dystrophies. Disuse atrophy and general muscle wasting can also be treated. Diseases of the eye, in particular cataract, can be treated as well. Generally all condition where elevated levels of calpains are involved can be treated. The compounds of the invention may also inhibit other thiol proteases such as cathepsin B, cathepsin H, cathepsin L, papain or the like. Multicatalytic Protease also known as proteasome may also be inhibited and the compounds can therefore be used to treat cell proliferative diseases such as cancer, psoriasis, and restenosis. The compounds of the present invention are also inhibitors of cell damage by oxidative stress through free radicals can be used to treat mitochondrial disorders and neurodegenerative diseases, where elevated levels of oxidative stress are involved. In addition they introduce the expression of utrophin, which is beneficial for the treatment of Duchenne Muscular Dystrophy and Becker Muscular Dystrophy.

    摘要翻译： 本发明涉及用于治疗神经变性疾病和神经肌肉疾病（包括杜氏肌营养不良症，贝克肌营养不良症和其他肌营养不良症）的新型α-酮羰基钙蛋白酶抑制剂。 也可以治疗消除萎缩和一般的肌肉消瘦。 眼睛疾病，特别是白内障也可以治疗。 一般来说，所有涉及钙蛋白水平升高的情况都可以被处理。 本发明的化合物还可以抑制其它巯基蛋白酶，例如组织蛋白酶B，组织蛋白酶H，组织蛋白酶L，木瓜蛋白酶等。 也称为蛋白酶体的多分析蛋白酶也可以被抑制，因此化合物可用于治疗细胞增殖性疾病如癌症，牛皮癣和再狭窄。 本发明的化合物也是通过自由基通过氧化应激的细胞损伤的抑制剂，其可用于治疗涉及氧化应激水平升高的线粒体病症和神经变性疾病。 此外，它们引入utrophin的表达，其有利于治疗Duchenne肌营养不良症和Becker肌营养不良症。

    Aromatic thioethers
    8.
    发明授权
    Aromatic thioethers 失效
    芳香硫醚

    公开(公告)号：US4785004A

    公开(公告)日：1988-11-15

    申请号：US941676

    申请日：1986-12-15

    申请人： Andreas Von Sprecher ,  Werner Breitenstein ,  Andreas Beck ,  Robert W. Lang ,  Konrad Oertle

    发明人： Andreas Von Sprecher ,  Werner Breitenstein ,  Andreas Beck ,  Robert W. Lang ,  Konrad Oertle

    IPC分类号： C07D215/54 ,  C07D311/24 ,  C07C149/40 ,  A61K31/235

    CPC分类号： C07D311/24 ,  C07D215/54

    摘要： Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: R.sup.0 represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted by one or more halogen atoms having an atomic number of at most 17,R.sup.2 represents an aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene, a single bond or vinylene,B.sup.1 represents C.sub.1-7 -alkylene or phenylene,B.sup.2 represents a single bond, ethylene or phenylene, andM represents an aromatic radical of the partial formula ##STR2## in which the symbols have the following meanings: R.sup.3 represents hydrogen or C.sub.1-4 -alkyl,X represents NH, O, S or if R.sup.4 represents hydrogen, a single bond,one of the symbols R.sup.4 and R.sup.5 represents hydrogen and the other represents the group --CO--R.sup.6, orR.sup.4 and R.sup.5 together represent the radical --CO--C(R.sup.6).dbd.C(R.sup.7)--or--CO--C(R.sup.7).dbd.C(R.sup.6)--orR.sup.4 R.sup.5, together with X, represent the radical --N.dbd.C(R.sup.8)--C(R.sup.6).dbd.CH--,in whichR.sup.6 represents --(CH.sub.2).sub.b --COOR.sup.3 (in which b=0 to 2)R.sup.7 represents hydrogen or C.sub.1-4 -alkyl andR.sup.8 represents hydrogen, methyl, mythoxy or halogen,and their salts are active as leucotriene antagonists since they eliminate the contractions of smooth muscles brought about by leucotrienes, and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.

    摘要翻译： 式（I）的新颖的不对称硫醚，其中通式符号具有以下含义：R 0表示氢或C 1-7 - 烷酰基，R 1表示可以被一个或多个具有 原子数最多为17，R 2表示具有5至15个碳原子的脂族基团，A表示乙烯，单键或亚乙烯基，B1表示C1-7 - 亚烷基或亚苯基，B2表示单键，乙烯或亚苯基 ，M表示部分结构式（M）的芳族基团，其中符号具有以下含义：R 3表示氢或C 1-4 - 烷基，X表示NH，O，S或如果R 4表示氢，则 单键，R4和R5之一表示氢，另一个表示-CO-R6基团，或R4和R5一起代表基团-CO-C（R6）= C（R7）-OR-CO-C（ R7）= C（R6） - 或R4R5与X一起代表基团-N = C（R8）-C（R6）= CH-，其中R6表示 - （CH2）b-COOR3（其中b = 0至2）R7表示氢或C1-4烷基，R8表示氢，甲基，乙氧基或卤素，并且它们的盐作为白三烯拮抗剂是有活性的，因为它们消除了由白三烯引起的平滑肌的收缩，因此适用于 治疗过敏，特别是哮喘，病情。