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1. 发明授权

US06399599B1 Substituted 2-oxo-1,4-diazacycloalkanes 失效
标题翻译：取代的2-氧代-1,4-二氮杂环烷烃
公开(公告)号：US06399599B1
公开(公告)日：2002-06-04
申请号：US09686511
申请日：2000-10-11
申请人： Rainer Albert , Josef G. Meingassner , Sompong Wattanasin , Gabriele Weitz-Schmidt , Karl Welzenbach , Ulrich Hommel , Claus Ehrhardt , Didier Roche , Joerg Kallen
发明人： Rainer Albert , Josef G. Meingassner , Sompong Wattanasin , Gabriele Weitz-Schmidt , Karl Welzenbach , Ulrich Hommel , Claus Ehrhardt , Didier Roche , Joerg Kallen
IPC分类号： C07D40106
CPC分类号： C07K5/06034 , A61K38/00 , C07D243/08 , C07K5/02 , C07K5/06078
摘要： Compounds of formula I wherein n is 1, 2 or 3; R1 is H, C1-4alkyl, aryl, or aryl-C1-4alkyl; Y is C1-4alkylene, —CO—C1-4alkylene, —CO—C2-5alkenylene, —CO—NH—, —CO—C1-3alkylene-NH—, or —CO—O—; R2 is an aromatic or heteroaromatic residue, each being optionally substituted by CF3, halogen, OH, C1-4alkoxy, amino, mono- or di-C1-4alkyl substituted amino, phenyl, benzyl or C1-4alkyl optionally substituted by amino; R3is the side chain present on the C&agr; of an &agr;-amino acid; R4 is biphenylyl, benzyl, hydroxy-benzyl, &agr;- or &bgr;-naphthyl-methyl, 5,6,7,8-tetrahydro-&bgr;-naphthyl-methyl or indolyl-methyl, each being optionally substituted on the ring by CF3, halogen, OH, C1-4alkoxy, amino, mono- or di-C1-4alkyl substituted amino, phenyl, benzyl or C1-4alkyl optionally substituted by amino; and X is —CN, —NR5R6 or —O—R8 wherein R5 is H, C1-6alkyl, aryl or aryl-C1-4alkyl; R6 is H or C1-6alkyl; and R8 is H, C1-4alkyl, aryl or aryl-C1-4alkyl; in free form or in salt form; which are useful in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1, -ICAM-2 or -ICAM-3 interactions.
摘要翻译：其中n为1,2或3的式I化合物; R 1是H，C 1-4烷基，芳基或芳基-C 1-4烷基; Y是C1-4亚烷基，-CO-C1-4亚烷基，-CO-C2-5亚烯基，-CO-NH-，-CO-C1-3亚烷基-NH-或-CO-O-; R 2是芳族或杂芳族残基，其各自任选被CF 3，卤素，OH，C 1-4烷氧基，氨基，单或二C 1-4烷基取代的氨基，苯基，苄基或任选被氨基取代的C 1-4烷基取代; R3是存在于α-氨基酸的Calpha上的侧链; R4是联苯基，苄基，羟基 - 苄基，α-或β-萘基 - 甲基，5,6,7,8-四氢-β-萘基 - 甲基或吲哚基 - 甲基，其各自在环上被CF 3任选取代，卤素，OH，C 1-4烷氧基，氨基，单或二-C 1-4烷基取代的氨基，苯基，苄基或任选被氨基取代的C 1-4烷基; 并且X是-CN，-NR 5 R 6或-O-R 8，其中R 5是H，C 1-6烷基，芳基或芳基-C 1-4烷基; R6是H或C1-6烷基; 且R 8为H，C 1-4烷基，芳基或芳基-C 1-4烷基; 以游离形式或盐形式; 其可用于预防或治疗由LFA-1 / ICAM-1，-ICAM-2或-ICAM-3相互作用介导的疾病或疾病。

2. 发明授权

US08859535B2 Hydroxy substituted isoquinolinone derivatives 有权
标题翻译：羟基取代的异喹啉酮衍生物
公开(公告)号：US08859535B2
公开(公告)日：2014-10-14
申请号：US14127155
申请日：2012-06-19
申请人： Nicole Buschmann , Pascal Furet , Philipp Holzer , Joerg Kallen , Keiichi Masuya , Stefan Stutz
发明人： Nicole Buschmann , Pascal Furet , Philipp Holzer , Joerg Kallen , Keiichi Masuya , Stefan Stutz
IPC分类号： C07D409/10 , A61K31/472 , A61K31/4725 , C07D217/24 , C07D401/04 , C07D401/10 , C07D401/14 , C07D405/10 , C07D405/14 , C07D491/08 , C07D493/08 , C07D451/14 , C07D413/08 , C07D451/02
CPC分类号： A61K31/4725 , A61K31/472 , C07D217/24 , C07D401/04 , C07D401/10 , C07D401/14 , C07D405/10 , C07D405/14 , C07D409/10 , C07D413/08 , C07D451/02 , C07D451/14 , C07D491/08 , C07D493/08
摘要： The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
摘要翻译：本发明涉及式（I）化合物：如申请中所定义。这些化合物适用于治疗由MDM2和/或MDM4或其变体的活性介导的病症或疾病。

3. 发明授权

US09670193B2 Trifluoromethyl-oxadiazole derivatives and their use in the treatment of disease 有权
公开(公告)号：US09670193B2
公开(公告)日：2017-06-06
申请号：US14360013
申请日：2012-11-26
申请人： Christina Hebach , Joerg Kallen , Joachim Nozulak , Marina Tintelnot-Blomley , Leo Widler
发明人： Christina Hebach , Joerg Kallen , Joachim Nozulak , Marina Tintelnot-Blomley , Leo Widler
IPC分类号： A61K31/4245 , C07D413/04 , C07D413/14 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/506
CPC分类号： C07D413/14 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/506 , C07D413/04
摘要： The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or diabetes/metabolic syndrome via inhibition of HDAC4.

4. 发明申请

US20140329825A1 NOVEL TRIFLUOROMETHYL-OXADIAZOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE 有权
标题翻译：新型三氟甲基 - 氧杂唑衍生物及其在治疗疾病中的应用
公开(公告)号：US20140329825A1
公开(公告)日：2014-11-06
申请号：US14360013
申请日：2012-11-26
申请人： Christina Hebach , Joerg Kallen , Joachim Nozulak , Marina Tintelnot-Blomley , Leo Widler
发明人： Christina Hebach , Joerg Kallen , Joachim Nozulak , Marina Tintelnot-Blomley , Leo Widler
IPC分类号： C07D413/14 , C07D413/04 , A61K31/444 , A61K31/4439 , A61K31/497 , A61K31/506
CPC分类号： C07D413/14 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/506 , C07D413/04
摘要： The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or diabetes/metabolic syndrome via inhibition of HDAC4.
摘要翻译：本发明涉及式（I）的新型三唑 - 恶二唑衍生物及其药学上可接受的盐，其中所有变量如说明书，其药物组合物，其药物组合，及其作为药物的用途，特别是通过抑制HDAC4治疗神经变性，肌肉萎缩或糖尿病/代谢综合征。

5. 发明申请

US20140275158A1 CYCLOHEXYL ISOQUINOLINONE COMPOUNDS 有权
标题翻译：环辛基异喹啉化合物
公开(公告)号：US20140275158A1
公开(公告)日：2014-09-18
申请号：US14127159
申请日：2012-06-19
申请人： Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Keiichi Masuya , Stefan Stutz
发明人： Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Keiichi Masuya , Stefan Stutz
IPC分类号： C07D217/24 , C07D405/08 , A61K31/4725 , A61K31/472 , C07D401/08
CPC分类号： C07D217/24 , A61K31/472 , A61K31/4725 , C07D217/04 , C07D401/08 , C07D405/08
摘要： The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
摘要翻译：本发明涉及式（I）化合物：如申请中所定义。这些化合物适用于治疗由MDM2和/或MDM4或其变体的活性介导的病症或疾病。

6. 发明申请

US20140142105A1 NOVEL TRIFLUOROMETHYL-OXADIAZOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE 有权
标题翻译：新型三氟甲基 - 氧杂唑衍生物及其在治疗疾病中的应用
公开(公告)号：US20140142105A1
公开(公告)日：2014-05-22
申请号：US14131558
申请日：2012-07-06
申请人： Christina Hebach , Emilie Joly , Joerg Kallen , James Gilbert Ternois , Marina Tintelnot-Blomley
发明人： Christina Hebach , Emilie Joly , Joerg Kallen , James Gilbert Ternois , Marina Tintelnot-Blomley
IPC分类号： C07D271/06 , A61K31/5377 , A61K31/4439 , A61K31/454 , C07D413/12 , C07D413/10 , A61K31/4245 , A61K31/496
CPC分类号： C07D271/06 , A61K31/4245 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , C07D413/10 , C07D413/12
摘要： The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, (I) in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or metabolic syndrome via inhibition of HDAC4.
摘要翻译：本发明涉及式（I）的新型三唑 - 恶二唑衍生物及其药学上可接受的盐，其中所有变量如本说明书中所定义，其药物组合物，其药物组合及其作为药物的用途，特别是通过抑制HDAC4治疗神经变性，肌肉萎缩或代谢综合征。

7. 发明申请

US20140135306A1 HDYROXY SUBSTITUTED ISOQUINOLINONE DERIVATIVES 有权
标题翻译： HDYROXY取代的异喹啉酮衍生物
公开(公告)号：US20140135306A1
公开(公告)日：2014-05-15
申请号：US14127155
申请日：2012-06-19
申请人： Nicole Buschmann , Pascal Furet , Philipp Holzer , Joerg Kallen , Keiichi Masuya , Stefan Stutz
发明人： Nicole Buschmann , Pascal Furet , Philipp Holzer , Joerg Kallen , Keiichi Masuya , Stefan Stutz
IPC分类号： C07D409/10 , A61K31/472 , C07D401/04 , A61K31/4725 , C07D401/10 , C07D405/10 , C07D405/14 , C07D217/24 , C07D401/14
CPC分类号： A61K31/4725 , A61K31/472 , C07D217/24 , C07D401/04 , C07D401/10 , C07D401/14 , C07D405/10 , C07D405/14 , C07D409/10 , C07D413/08 , C07D451/02 , C07D451/14 , C07D491/08 , C07D493/08
摘要： The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
摘要翻译：本发明涉及式（I）化合物：如申请中所定义。这些化合物适用于治疗由MDM2和/或MDM4或其变体的活性介导的病症或疾病。

8. 发明授权

US09365576B2 Pyrrolopyrrolidinone compounds 有权
标题翻译：吡咯并吡咯烷酮化合物
公开(公告)号：US09365576B2
公开(公告)日：2016-06-14
申请号：US13900061
申请日：2013-05-22
申请人： Simona Cotesta , Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Robert Mah , Keiichi Masuya , Achim Schlapbach , Stefan Stutz , Andrea Vaupel
发明人： Simona Cotesta , Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Robert Mah , Keiichi Masuya , Achim Schlapbach , Stefan Stutz , Andrea Vaupel
IPC分类号： C07D487/04 , A61K31/407 , A61K31/44 , A61K31/5377 , A61K31/506 , A61K31/41 , A61K31/4439 , A61K45/06
CPC分类号： C07D487/04 , A61K31/407 , A61K31/41 , A61K31/4439 , A61K31/506 , A61K31/5377 , A61K45/06
摘要： The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
摘要翻译：本发明涉及式（I）化合物：如本文所述，包含这些化合物的药物制剂，用于治疗由MDM2和/或MDM4的活性介导的疾病或疾病的这些化合物的用途和方法，以及包含这些化合物的组合。

9. 发明授权

US09056843B2 Trifluoromethyl-oxadiazole derivatives and their use in the treatment of disease 有权
标题翻译：三氟甲基 - 恶二唑衍生物及其在治疗疾病中的应用
公开(公告)号：US09056843B2
公开(公告)日：2015-06-16
申请号：US14131558
申请日：2012-07-06
申请人： Christina Hebach , Emilie Joly , Joerg Kallen , James Gilbert Ternois , Marina Tintelnot-Blomley
发明人： Christina Hebach , Emilie Joly , Joerg Kallen , James Gilbert Ternois , Marina Tintelnot-Blomley
IPC分类号： C07D271/06 , C07D413/12 , C07D413/10 , A61K31/5377 , A61K31/4439 , A61K31/454 , A61K31/4245 , A61K31/496
CPC分类号： C07D271/06 , A61K31/4245 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , C07D413/10 , C07D413/12
摘要： The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, (I) in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or metabolic syndrome via inhibition of HDAC4.
摘要翻译：本发明涉及式（I）的新型三唑 - 恶二唑衍生物及其药学上可接受的盐，其中所有变量如本说明书中所定义，其药物组合物，其药物组合及其作为药物的用途，特别是通过抑制HDAC4治疗神经变性，肌肉萎缩或代谢综合征。

10. 发明申请

US20140018376A1 Use of 1H-Quinazoline-2,4-Diones 审中-公开
标题翻译：使用1H-喹唑啉-2,4-二酮
公开(公告)号：US20140018376A1
公开(公告)日：2014-01-16
申请号：US13502765
申请日：2010-10-20
申请人： Hans Allgeier , Yves Auberson , Thomas Blaettler , David Carcache , Philipp Floersheim , Wolfgang Froestl , Christel Guibourdenche , Hans o Kalkman , Joerg Kallen , Manuel Koller , Kurt Lingenhohl , Henri Mattes , Joachim Nozulak , David Orain , Johanne Renaud , Christine Strohmaier
发明人： Hans Allgeier , Yves Auberson , Thomas Blaettler , David Carcache , Philipp Floersheim , Wolfgang Froestl , Christel Guibourdenche , Hans o Kalkman , Joerg Kallen , Manuel Koller , Kurt Lingenhohl , Henri Mattes , Joachim Nozulak , David Orain , Johanne Renaud , Christine Strohmaier
IPC分类号： C07D239/96 , C07D403/04 , C07D405/04
CPC分类号： C07D239/96 , C07D403/04 , C07D405/04
摘要： The invention concerns the use of competitive AMPA receptor antagonists for the treatment, prevention or delay of progression of Rasmussen's encephalitis and/or certain forms of epilepsy.
摘要翻译：本发明涉及竞争性AMPA受体拮抗剂用于治疗，预防或延缓拉斯穆森脑炎和/或某些形式的癫痫发展的用途。

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