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1. 发明申请

WO2009109906A1 PYRIDINE COMPOUNDS 审中-公开
标题翻译：吡啶化合物
公开(公告)号：WO2009109906A1
公开(公告)日：2009-09-11
申请号：PCT/IB2009/050847
申请日：2009-03-03
申请人： ACTELION PHARMACEUTICALS LTD , BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
发明人： BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
IPC分类号： C07D413/04 , A61K31/4427 , A61P37/00
CPC分类号： C07D413/04
摘要： The invention relates to pyridine compounds, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
摘要翻译：本发明涉及吡啶化合物，其制备及其作为药物活性化合物的用途。所述化合物特别充当免疫调节剂。

2. 发明申请

WO2009109907A1 NOVEL PYRIMIDINE-PYRIDINE DERIVATIVES 审中-公开
标题翻译：新型吡咯烷 - 吡啶衍生物
公开(公告)号：WO2009109907A1
公开(公告)日：2009-09-11
申请号：PCT/IB2009/050848
申请日：2009-03-03
申请人： ACTELION PHARMACEUTICALS LTD , BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
发明人： BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
IPC分类号： C07D413/14 , C07D417/14 , A61K31/506 , A61P37/00
CPC分类号： C07D413/14 , C07D417/14
摘要： The invention relates to novel pyrimidine-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula I.
摘要翻译：本发明涉及新颖的嘧啶 - 吡啶衍生物，其制备及其作为药物活性化合物的用途。所述化合物特别充当免疫调节剂。一级方程式

3. 发明申请

WO2009109904A1 NOVEL AMINOMETHYL BENZENE DERIVATIVES 审中-公开
标题翻译：新型氨基苯甲酸衍生物
公开(公告)号：WO2009109904A1
公开(公告)日：2009-09-11
申请号：PCT/IB2009/050844
申请日：2009-03-03
申请人： ACTELION PHARMACEUTICALS LTD , BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
发明人： BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
IPC分类号： C07D271/06 , A61K31/4245 , A61P37/00
CPC分类号： C07D271/06
摘要： The invention relates to novel aminomethyl benzene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. (I) wherein A represents one of the groups (I), (I), (I) and (I).
摘要翻译：本发明涉及新型氨基甲基苯衍生物，其制备及其作为药物活性化合物的用途。所述化合物特别充当免疫调节剂。（I）其中A表示组（I），（I），（I）和（I）中的一种。

4. 发明申请

WO2009109872A1 PYRIDIN-2-YL DERIVATIVES AS IMMUNOMODULATING AGENTS 审中-公开
标题翻译： PYRIDIN-2-YL衍生物作为免疫调节剂
公开(公告)号：WO2009109872A1
公开(公告)日：2009-09-11
申请号：PCT/IB2009/050749
申请日：2009-02-25
申请人： ACTELION PHARMACEUTICALS LTD , BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
发明人： BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
IPC分类号： C07D413/04 , A61K31/4245 , A61P37/02
CPC分类号： C07D413/04
摘要： The invention relates to pyridine derivatives of Formula (I), wherein A, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
摘要翻译：本发明涉及式（I）的吡啶衍生物，其中A，R 1，R 2，R 3，R 4，R 5，R 6和R 7如说明书中所述，其制备及其作为药物活性化合物的用途。所述化合物特别充当免疫调节剂。

5. 发明申请

WO2009057079A2 NOVEL PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：新型吡咯烷衍生物
公开(公告)号：WO2009057079A2
公开(公告)日：2009-05-07
申请号：PCT/IB2008/054543
申请日：2008-10-31
申请人： ACTELION PHARMACEUTICALS LTD , BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
发明人： BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
CPC分类号： C07D413/04 , C07D417/04
摘要： The invention relates to novel pyrimidine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
摘要翻译：本发明涉及新颖的嘧啶衍生物，其制备及其作为药物活性化合物的用途。所述化合物特别充当免疫调节剂。

6. 发明申请

WO2009024905A1 PYRIDINE DERIVATIVES AS S1P1/EDG1 RECEPTOR MODULATORS 审中-公开
标题翻译：吡啶衍生物作为S1P1 / EDG1受体调节剂
公开(公告)号：WO2009024905A1
公开(公告)日：2009-02-26
申请号：PCT/IB2008/053269
申请日：2008-08-14
申请人： ACTELION PHARMACEUTICALS LTD , BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat , VELKER, Jörg
发明人： BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat , VELKER, Jörg
IPC分类号： C07D413/14 , C07D417/14 , A61K31/422 , A61K31/427 , A61K31/4245 , A61K31/433 , A61P37/06
CPC分类号： C07D413/14 , C07D417/14
摘要： The invention relates to novel pyridine derivatives of formula (D, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I) wherein A represents and the other substituants are as defined in the claims.
摘要翻译：本发明涉及式（D，其制备及其作为药物活性化合物的用途）的新颖吡啶衍生物，所述化合物特别充当免疫调节剂，其中A表示的式（I），其它取代基如权利要求中所定义。

7. 发明申请

WO2012098505A1 2-METHOXY-PYRIDIN-4-YL DERIVATIVES 审中-公开
标题翻译： 2-甲氧基 - 吡啶-4-基衍生物
公开(公告)号：WO2012098505A1
公开(公告)日：2012-07-26
申请号：PCT/IB2012/050241
申请日：2012-01-18
申请人： ACTELION PHARMACEUTICALS LTD , BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MORRISON, Keith , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
发明人： BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MORRISON, Keith , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
IPC分类号： C07D413/04 , A61K31/4439 , A61P37/00
CPC分类号： C07D413/14 , C07D413/04
摘要： The invention relates to pyridine derivatives of Formula (I) wherein A, R 1 , R 2 , R 3 , and R 4 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
摘要翻译：本发明涉及式（I）的吡啶衍生物，其中A，R 1，R 2，R 3和R 4如说明书中所述，其制备及其作为药物活性化合物的用途。所述化合物特别充当免疫调节剂。

8. 发明申请

WO2011007324A1 PYRIDIN-4-YL DERIVATIVES 审中-公开
标题翻译：吡啶-4-YL衍生物
公开(公告)号：WO2011007324A1
公开(公告)日：2011-01-20
申请号：PCT/IB2010/053224
申请日：2010-07-15
申请人： ACTELION PHARMACEUTICALS LTD , BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MORRISON, Keith , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
发明人： BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MORRISON, Keith , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
IPC分类号： C07D413/04 , A61K31/4439 , A61P37/00
CPC分类号： C07D413/04
摘要： The invention relates to pyridine derivatives of Formula (I), wherein A, R 1 , R 2 , R 3 , and R 4 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
摘要翻译：本发明涉及式（I）的吡啶衍生物，其中A，R 1，R 2，R 3和R 4如说明书所述，其制备及其作为药物活性化合物的用途。所述化合物特别充当免疫调节剂。

9. 发明申请

WO2009074950A2 NOVEL THIOPHENE DERIVATIVES 审中-公开
标题翻译：新型噻吩衍生物
公开(公告)号：WO2009074950A2
公开(公告)日：2009-06-18
申请号：PCT/IB2008/055156
申请日：2008-12-09
申请人： ACTELION PHARMACEUTICALS LTD , BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
发明人： BOLLI, Martin , LESCOP, Cyrille , MATHYS, Boris , MUELLER, Claus , NAYLER, Oliver , STEINER, Beat
CPC分类号： C07D413/04 , C07D413/14
摘要： The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
摘要翻译：本发明涉及新的噻吩衍生物，其制备及其作为药物活性化合物的用途。所述化合物特别充当免疫调节剂。

10. 发明申请

WO2004078908A2 ALPHA-KETO CARBONYL CALPAIN INHIBITORS 审中-公开
标题翻译： ALPHA-KETO CARBONYL CALPAIN抑制剂
公开(公告)号：WO2004078908A2
公开(公告)日：2004-09-16
申请号：PCT/EP2004/002142
申请日：2004-03-03
申请人： MYOCONTRACT LTD. , HERZNER, Holger , WEYERMANN, Philipp , VON SPRECHER, Andreas , HENNEBÖHLE, Marco , LESCOP, Cyrille , SIENDT, Hervé
发明人： HERZNER, Holger , WEYERMANN, Philipp , VON SPRECHER, Andreas , HENNEBÖHLE, Marco , LESCOP, Cyrille , SIENDT, Hervé
IPC分类号： C12N
CPC分类号： C07K5/06026 , A61K38/00 , C07D233/54 , C07D339/04 , C07K5/0202 , C07K5/0606
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 conditions 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 (MCP) 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 and can be used to treat mitochondrial disorders and neurodegenerative diseases, where elevated levels of oxidative stress are involved.
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，涉及钙蛋白水平升高的所有条件都可以被处理。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（MCP）也可以被抑制，因此化合物可以是。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，并且可以用于治疗涉及氧化应激水平升高的线粒体疾病和神经变性疾病。

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