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1. 发明申请

US20090143337A1 C2-C5-Alkyl-Imidazole-Bisphosphonates 有权
标题翻译： C2-C5-烷基 - 咪唑 - 二膦酸酯
公开(公告)号：US20090143337A1
公开(公告)日：2009-06-04
申请号：US12323696
申请日：2008-11-26
申请人： Sven Weiler , Leo Widler , Jean-Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
发明人： Sven Weiler , Leo Widler , Jean-Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
IPC分类号： A61K31/675 , C07F9/40 , A61P19/08
CPC分类号： C07F9/6506
摘要： C2-C5-Alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are described. The compounds are able to inhibit excessive or inappropriate bone resorption and for the treatment of other diseases which are caused by excessive prenylation of target proteins, such as Hutchinson-Gilford progeria syndrome. The compounds are of the formula I, wherein one of R1 and R2 is hydrogen and the other is C2-C5-alkyl that is branched or unbranched, and can be in free form, in the form of an ester, and/or of a salt.
摘要翻译： C2-C5-烷基取代的[（咪唑-1-基）-1-羟基-1-膦酰基 - 乙基] - 膦酸，以及其制备方法或方法，它们在药物制剂的制备中的用途，它们描述了用于治疗疾病，用于治疗疾病的方法，包括它们的药物制剂和/或用于治疗疾病的化合物。该化合物能够抑制过度或不适当的骨吸收和用于治疗由靶向蛋白过度异戊二烯化引起的其他疾病，例如Hutchinson-Gilford progeria综合征。该化合物具有式I化合物，其中R 1和R 2之一是氢，另一个是支链或非支链的C 2 -C 5 - 烷基，并且可以是酯的游离形式，和/或盐。

2. 发明授权

US07977323B2 C2-C5-alkyl-imidazole-bisphosphonates 有权
标题翻译： C2-C5-烷基 - 咪唑 - 双膦酸盐
公开(公告)号：US07977323B2
公开(公告)日：2011-07-12
申请号：US12323696
申请日：2008-11-26
申请人： Sven Weiler , Leo Widler , Jean Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
发明人： Sven Weiler , Leo Widler , Jean Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
IPC分类号： A61K31/675 , C07F9/02
CPC分类号： C07F9/6506
摘要： C2-C5-Alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are described. The compounds are able to inhibit excessive or inappropriate bone resorption and for the treatment of other diseases which are caused by excessive prenylation of target proteins, such as Hutchinson-Gilford progeria syndrome. The compounds are of the formula I, wherein one of R1 and R2 is hydrogen and the other is C2-C5-alkyl that is branched or unbranched, and can be in free form, in the form of an ester, and/or of a salt.
摘要翻译： C2-C5-烷基取代的[（咪唑-1-基）-1-羟基-1-膦酰基 - 乙基] - 膦酸，以及其制备方法或方法，它们在药物制剂的制备中的用途，它们描述了用于治疗疾病，用于治疗疾病的方法，包括它们的药物制剂和/或用于治疗疾病的化合物。该化合物能够抑制过度或不适当的骨吸收和用于治疗由靶向蛋白过度异戊二烯化引起的其他疾病，例如Hutchinson-Gilford progeria综合征。该化合物具有式I化合物，其中R 1和R 2之一是氢，另一个是支链或非支链的C 2 -C 5 - 烷基，并且可以是酯的游离形式，和/或盐。

3. 发明申请

US20110257131A1 PHENYLALKYL-IMIDAZOLE-BISPHOSPHONATE COMPOUNDS 审中-公开
标题翻译：苯基 - 咪唑 - 二磷酸酯化合物
公开(公告)号：US20110257131A1
公开(公告)日：2011-10-20
申请号：US13141249
申请日：2009-12-21
申请人： Simona Cotesta , Wolfgang Jahnke , Jean-Michel Rondeau , Sven Weiler , Leo Widler
发明人： Simona Cotesta , Wolfgang Jahnke , Jean-Michel Rondeau , Sven Weiler , Leo Widler
IPC分类号： A61K31/675 , A61P19/00 , A61P43/00 , C07F9/572
CPC分类号： C07F9/6506
摘要： (Unsubstituted or substituted phenyl)-alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are disclosed. The compounds are able to inhibit excessive or inappropriate bone resorption. The compounds are of the formula I, wherein one of R1 and R2 are as defined in the specification, and can be in free form, in the form of an ester, and/or of a salt.
摘要翻译：（未取代或取代的苯基） - 烷基取代的[（咪唑-1-基）-1-羟基-1-膦酰基 - 乙基] - 膦酸，以及其制备方法或方法，它们在制备药物制剂中的用途，它们在疾病治疗中的应用，用于治疗疾病的方法，包括它们的药物制剂和/或用于治疗疾病的化合物。这些化合物能够抑制过量或不适当的骨吸收。化合物是式I化合物，其中R 1和R 2之一如说明书中所定义，并且可以为酯的形式的游离形式和/或盐。

4. 发明申请

US20110224173A1 C2-C5-Alkyl-Imidazole-Bisphosphonates 审中-公开
标题翻译： C2-C5-烷基 - 咪唑 - 二膦酸酯
公开(公告)号：US20110224173A1
公开(公告)日：2011-09-15
申请号：US13116671
申请日：2011-05-26
申请人： Sven Weiler , Leo Widler , Jean-Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
发明人： Sven Weiler , Leo Widler , Jean-Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
IPC分类号： A61K31/675 , C07F9/6506 , A61P19/00
CPC分类号： C07F9/6506
摘要： C2-C5-Alkyl-substituted [imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are described. The compounds are able to inhibit excessive or inappropriate bone resorption and for the treatment of other diseases which are caused by excessive prenylation of target proteins, such as Hutchinson-Gilford progeria syndrome. The compounds are of the formula I, wherein one of R1 and R2 is hydrogen and the other is C2-C5-alkyl that is branched or unbranched, and can be in free form, in the form of an ester, and/or of a salt.
摘要翻译： C2-C5-烷基取代的[咪唑-1-基] -1-羟基-1-膦酰基 - 乙基]膦酸，以及其制备方法或方法，它们在制备药物制剂中的用途，它们的用途在治疗疾病方面，使用它们治疗疾病的方法，包括它们的药物制剂和/或用于治疗疾病的化合物。该化合物能够抑制过度或不适当的骨吸收和用于治疗由靶向蛋白过度异戊二烯化引起的其他疾病，例如Hutchinson-Gilford progeria综合征。该化合物具有式I化合物，其中R 1和R 2之一是氢，另一个是支链或非支链的C 2 -C 5 - 烷基，并且可以是酯的游离形式，和/或盐。

5. 发明申请

US20100063075A1 Aryl-quinazoline/aryl-2amino-phenyl methanone derivatives 失效
标题翻译：芳基 - 喹唑啉/芳基-2-氨基 - 苯基甲酮衍生物
公开(公告)号：US20100063075A1
公开(公告)日：2010-03-11
申请号：US12579735
申请日：2009-10-15
申请人： Eva Altmann , Rene Beerli , Marc Gerspacher , Johanne Renaud , Sven Weiler , Leo Widler
发明人： Eva Altmann , Rene Beerli , Marc Gerspacher , Johanne Renaud , Sven Weiler , Leo Widler
IPC分类号： A61K31/517 , C07D239/72 , C07C211/00 , A61K31/135 , A61P19/00
CPC分类号： C07C17/12 , C07C45/30 , C07C205/37 , C07C205/44 , C07C205/45 , C07C225/22 , C07C229/18 , C07C255/24 , C07C255/25 , C07C317/18 , C07C317/32 , C07C323/25 , C07C2601/02 , C07D213/64 , C07D239/82 , C07D239/93 , C07D317/58 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/10 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07C25/18 , C07C47/277
摘要： A compound of formula (1): wherein R1, R2, R3 and Y are as defined herein, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, useful for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
摘要翻译：式（1）化合物：其中R 1，R 2，R 3和Y如本文所定义，或其药学上可接受的可裂解的酯或其酸加成盐，其可用于促进甲状旁腺激素的释放，例如，用于预防或治疗与钙耗竭或再吸收增加相关的骨质状况或其中期望刺激骨形成和骨固定的刺激。

6. 发明授权

US07696216B2 Aryl-quinazoline/aryl-2-amino-phenyl methanone derivatives 失效
标题翻译：芳基 - 喹唑啉/芳基-2-氨基 - 苯基甲酮衍生物
公开(公告)号：US07696216B2
公开(公告)日：2010-04-13
申请号：US10540359
申请日：2003-12-22
申请人： Eva Altmann , Rene Beerli , Marc Gerspacher , Johanne Renaud , Sven Weiler , Leo Widler
发明人： Eva Altmann , Rene Beerli , Marc Gerspacher , Johanne Renaud , Sven Weiler , Leo Widler
IPC分类号： A61K31/517 , C07D239/78 , C07D239/80 , C07D239/82 , C07D401/04
CPC分类号： C07C17/12 , C07C45/30 , C07C205/37 , C07C205/44 , C07C205/45 , C07C225/22 , C07C229/18 , C07C255/24 , C07C255/25 , C07C317/18 , C07C317/32 , C07C323/25 , C07C2601/02 , C07D213/64 , C07D239/82 , C07D239/93 , C07D317/58 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/10 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07C25/18 , C07C47/277
摘要： A compound of formula (I): wherein R1, R2, R3 and Y are as defined herein, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, useful for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
摘要翻译：式（I）的化合物：其中R 1，R 2，R 3和Y如本文所定义，或其药学上可接受的可裂解的酯或其酸加成盐，其可用于促进甲状旁腺激素的释放，例如，用于预防或治疗与钙耗竭或再吸收增加相关的骨质状况或其中期望刺激骨形成和骨固定的刺激。

7. 发明授权

US08569317B2 Aryl-quinazoline/aryl-2amino-phenyl methanone derivatives 失效
标题翻译：芳基 - 喹唑啉/芳基-2-氨基 - 苯基甲酮衍生物
公开(公告)号：US08569317B2
公开(公告)日：2013-10-29
申请号：US12579735
申请日：2009-10-15
申请人： Eva Altmann , Rene Beerli , Marc Gerspacher , Johanne Renaud , Sven Weiler , Leo Widler
发明人： Eva Altmann , Rene Beerli , Marc Gerspacher , Johanne Renaud , Sven Weiler , Leo Widler
IPC分类号： A01N43/54 , A61K31/517 , C07D239/72 , C07D401/00
CPC分类号： C07C17/12 , C07C45/30 , C07C205/37 , C07C205/44 , C07C205/45 , C07C225/22 , C07C229/18 , C07C255/24 , C07C255/25 , C07C317/18 , C07C317/32 , C07C323/25 , C07C2601/02 , C07D213/64 , C07D239/82 , C07D239/93 , C07D317/58 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/10 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07C25/18 , C07C47/277
摘要： A compound of formula (1): wherein R1, R2, R3 and Y are as defined herein, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, useful for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
摘要翻译：式（1）化合物：其中R 1，R 2，R 3和Y如本文所定义，或其药学上可接受的可裂解的酯或其酸加成盐，其可用于促进甲状旁腺激素的释放，例如，用于预防或治疗与钙耗竭或再吸收增加相关的骨质状况或其中期望刺激骨形成和骨固定的刺激。

8. 发明授权

US08476286B2 Quinazoline derivatives which promote the release of parathyroid hormone 失效
标题翻译：促进甲状旁腺激素释放的喹唑啉衍生物
公开(公告)号：US08476286B2
公开(公告)日：2013-07-02
申请号：US10480559
申请日：2002-06-14
申请人： René Beerli , Ruben A Tommasi , Sven Weiler , Leo Widler
发明人： René Beerli , Ruben A Tommasi , Sven Weiler , Leo Widler
IPC分类号： A61K31/517 , C07D239/82 , C07D239/80 , C07D229/34
CPC分类号： C07D401/06 , C07D213/88 , C07D239/74 , C07D239/78 , C07D239/82 , C07D239/84 , C07D265/36 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/06 , C07D405/12 , C07D417/06
摘要： Use of compound of formula (I), wherein, is, or, and wherein the symbols are as defined, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, for the preparation of a medicament for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
摘要翻译：在制备用于促进释放的药物的药物中使用式（I）化合物，其中，是，或其中符号如所定义，或其药学上可接受的和可切除的酯或其酸加成盐，甲状旁腺激素，例如用于预防或治疗与钙耗竭或再吸收增加相关的骨质状况或其中期望刺激骨形成和骨固定的刺激。

9. 发明申请

US20060079685A1 Aryl-quinazoline/aryl-2amino-phenyl methanone derivatives 失效
标题翻译：芳基 - 喹唑啉/芳基-2-氨基 - 苯基甲酮衍生物
公开(公告)号：US20060079685A1
公开(公告)日：2006-04-13
申请号：US10540359
申请日：2003-12-22
申请人： Eva Altmann , Rene Beerli , Marc Gerspacher , Johanne Renaud , Sven Weiler , Leo Widler
发明人： Eva Altmann , Rene Beerli , Marc Gerspacher , Johanne Renaud , Sven Weiler , Leo Widler
IPC分类号： A61K31/517 , C07D239/80
CPC分类号： C07C17/12 , C07C45/30 , C07C205/37 , C07C205/44 , C07C205/45 , C07C225/22 , C07C229/18 , C07C255/24 , C07C255/25 , C07C317/18 , C07C317/32 , C07C323/25 , C07C2601/02 , C07D213/64 , C07D239/82 , C07D239/93 , C07D317/58 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/10 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07C25/18 , C07C47/277
摘要： A compound of formula (I): wherein R1, R2, R3 and Y are as defined herein, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, useful for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
摘要翻译：式（I）的化合物：其中R 1，R 2，R 3和Y如本文所定义，或其药学上可接受的可裂解的酯或其酸加成盐，其可用于促进甲状旁腺激素的释放，例如，用于预防或治疗与钙耗竭或再吸收增加相关的骨质状况或其中期望刺激骨形成和骨固定的刺激。

10. 发明申请

US20100166765A1 BENZOQUINAZOLINE DERIVATIVES 审中-公开
标题翻译：苯并噻唑衍生物
公开(公告)号：US20100166765A1
公开(公告)日：2010-07-01
申请号：US12063526
申请日：2006-08-14
申请人： Sandra Ammon , Rene Beerli , Leo Widler
发明人： Sandra Ammon , Rene Beerli , Leo Widler
IPC分类号： A61K31/517 , C07D239/72 , C07D403/12 , A61P19/08 , C07D237/30 , A61K31/502 , A61K33/06 , A61K38/23 , A61K31/56 , A61K39/395 , A61K31/59
CPC分类号： C07D409/06 , C07D217/12 , C07D217/26 , C07D239/70 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D417/06 , C07D417/12
摘要： A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof, wherein the groups R2, R3, R4, Q, X and Y are as defined in the specification, is useful in the treatment of bone conditions related to increased calcium depletion or resorption.
摘要翻译：式（I）化合物或其药学上可接受的盐或前药酯，其中基团R 2，R 3，R 4，Q，X和Y如说明书中所定义，可用于治疗与增加的钙相关的骨条件耗尽或吸收。

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