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    Alpha-Keto Carbonyl Calpain Inhibitors
    1.
    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
    2.
    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。

    Alkanophenones useful for treating allergies
    6.
    发明授权
    Alkanophenones useful for treating allergies 失效
    用于治疗过敏的苯胺酮

    公开(公告)号：US5149717A

    公开(公告)日：1992-09-22

    申请号：US795227

    申请日：1991-11-15

    申请人： Andreas von Sprecher ,  Andreas Beck ,  Bruno Schaub ,  Robert W. Lang

    发明人： Andreas von Sprecher ,  Andreas Beck ,  Bruno Schaub ,  Robert W. Lang

    IPC分类号： C07D311/24 ,  C07D405/04

    CPC分类号： C07D405/04 ,  C07D311/24

    摘要： Substituted alkanophenones of general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is phenyl that is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterified or amidated carboxy, or is lower alkyl that is unsubstituted, substituted by fluoro and chloro or substituted by free esterified or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties and can be used as anti-allergic active ingredients in medicaments.

    摘要翻译： 其中R 1为未取代或氟化的低级烷基，R 2为氢或未取代或氟化的低级烷基或低级烯基，X为低级亚烷基，氧基，硫基或直接键的通式为（Ⅰ）的取代的烷基苯醌， 低级亚烷基，n是1或2，R3是未取代的或被未取代或氟化的低级烷基取代的苯基，被醚化或酯化的羟基，被未取代或低级烷基化的氨基和/或被游离的，酯化的或酰胺化的羧基取代，或者是 未取代的低级烷基，被氟和氯取代或被游离的酯化或酰胺化的羧基取代，R4是游离的，酯化的或酰胺化的羧基或5-四唑基，R 5是氢或低级烷基，具有白三烯拮抗性质，并且可以使用 作为药物中的抗过敏活性成分。

    Alkanophenones useful for treating allergies
    8.
    发明授权
    Alkanophenones useful for treating allergies 失效
    用于治疗过敏的苯胺酮

    公开(公告)号：US5145868A

    公开(公告)日：1992-09-08

    申请号：US794608

    申请日：1991-11-15

    申请人： Andreas von Sprecher ,  Andreas Beck

    发明人： Andreas von Sprecher ,  Andreas Beck

    IPC分类号： C07D333/16 ,  A61K8/00 ,  A61K8/49 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61P7/02 ,  A61P11/00 ,  A61P17/00 ,  A61P37/08 ,  A61Q17/04 ,  C07D311/24 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14

    CPC分类号： C07D405/04 ,  C07D311/24 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14

    摘要： Substituted alkanophenones of the general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is a 5-membered heteroaryl radical that contains 1N, O or S atom as hetero atom and is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterfied or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties can e used as antiallergic active ingredients in medicaments.

    摘要翻译： 其中R 1为未取代或氟化的低级烷基，R 2为氢，或未取代或氟化的低级烷基或低级烯基，X为低级亚烷基，氧基，硫基或直接键合的取代的烷基苯甲酮 键，alk是低级亚烷基，n是1或2，R3是含有1N，O或S原子作为杂原子的5元杂芳基，未被取代或被未取代或氟化的低级烷基取代，通过醚化或酯化的羟基 通过未取代或低级烷基化的氨基和/或游离的酯化或酰胺化的羧基，R 4是游离的，酯化的或酰胺化的羧基或5-四唑基，R 5是氢或低级烷基，具有白三烯拮抗性能可以用作抗过敏活性 药物成分。

    Benzocycloalkenecarboxylic acid and process for its preparation
    10.
    发明授权
    Benzocycloalkenecarboxylic acid and process for its preparation 失效
    苯并二恶唑酸及其制备方法

    公开(公告)号：US5177257A

    公开(公告)日：1993-01-05

    申请号：US776385

    申请日：1991-11-20

    申请人： Andreas von Sprecher ,  Hansjurg Wetter

    发明人： Andreas von Sprecher ,  Hansjurg Wetter

    IPC分类号： A61K31/19 ,  A61P29/00 ,  A61P43/00 ,  C07B57/00 ,  C07C51/487 ,  C07C62/38

    CPC分类号： C07C62/38 ,  C07C51/487

    摘要： The novel (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic i.e. the compound of the formula ##STR1## in free form or in salt form, can be used as active ingredient in pharmaceutical preparations and can be prepared by a novel process, which is characterized in that racemic 4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic acid is reacted at elevated temperature with at least the equimolar amount of quinine in an alcoholic solvent for from approximately 6 to approximately 48 hours, the quinine salt of the (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic acid, precipitated in crystalline form as the direct reaction product, is separated from the reaction mixture, and the (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic acid is set free from this salt by acid treatment in a customary manner, and, if desired, this free acid is converted into a salt.

    摘要翻译： PCT No.PCT / CH91 / 00064 Sec。 371日期1991年11月20日 102（e）1991年11月20日日期PCT 1991年3月19日PCT公布。 WO91 / 14671 PCT出版物 日期为1991年10月3日。新型（S）-4-（2-溴苯甲酰基）-5-羟基 - 苯并环丁烯-1-羧酸，即游离形式或盐形式的式（I）化合物， 可以用作药物制剂中的活性成分，并且可以通过一种新的方法制备，其特征在于外消旋的4-（2-溴苯甲酰基）-5-羟基 - 苯并环丁烯-1-羧酸在升高的温度下至少与 在酒精溶剂中等摩尔量的奎宁约6至约48小时，（S）-4-（2-溴苯甲酰基）-5-羟基 - 苯并环丁烯-1-羧酸的奎宁盐以晶体形式沉淀 作为直接反应产物，与反应混合物分离，并以常规方式通过酸处理使（S）-4-（2-溴苯甲酰基）-5-羟基 - 苯并环丁烯-1-羧酸不含该盐 ，如果需要，将该游离酸转化成盐。