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1.发明授权Aldehyde acetal based processes for the manufacture of macrocyclic depsipeptides and new intermediates 有权用于制备大环脱脂肽和新中间体的基于醛缩乙醛的方法公开(公告)号：US08987413B2
公开(公告)日：2015-03-24
申请号：US14042950
申请日：2013-10-01
IPC分类号： A61K38/12 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C07K11/02 , C07D317/30 , C07C229/22 , C07K7/06
CPC分类号： C07K11/02 , C07C43/164 , C07C229/12 , C07C229/22 , C07C233/47 , C07D317/30 , C07K7/02 , C07K7/04 , C07K7/06 , C07K11/00
摘要： The invention relates to a method or process for the chemical manufacture of depsipeptides of the formula I employing an aldehyde acetal intermediate, wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.
摘要翻译： 本发明涉及使用醛缩醛中间体化学制备式I的缩肽的方法或方法，其中符号具有本说明书中定义的含义，新的中间体及其制备以及相关的发明实施方案。
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公开(公告)号：US20150246881A1
公开(公告)日：2015-09-03
申请号：US14715129
申请日：2015-05-18
申请人： David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
发明人： David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
IPC分类号： C07D207/38
CPC分类号： C07D207/38 , C07C271/22 , C07D207/26 , C07D207/263 , C07D207/36 , C07D403/06 , Y02P20/55
摘要： The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are ultimately related to the synthesis of intermediates to prepare the above NEP inhibitors, namely compounds according to formula (1), or salt thereof, wherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, and R3 is a carboxyl group or an ester group, preferably carboxyl group or alkyl ester.
摘要翻译： 本发明涉及生产NEP抑制剂或其前药的新方法，特别是包含γ-氨基-δ-联苯基-α-甲基链烷酸或酸酯主链的NEP抑制剂。 具体而言，根据本发明的新方法最终涉及制备上述NEP抑制剂的中间体的合成，即根据式（1）的化合物或其盐，其中R 1和R 2各自独立地 另一个是氢或氮保护基，R3是羧基或酯基，优选羧基或烷基酯。
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公开(公告)号：US20160060217A1
公开(公告)日：2016-03-03
申请号：US14939513
申请日：2015-11-12
申请人： David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
发明人： David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
IPC分类号： C07D207/38 , C07D403/06
CPC分类号： C07D207/38 , C07C271/22 , C07D207/26 , C07D207/263 , C07D207/36 , C07D403/06 , Y02P20/55
摘要： The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are ultimately related to the synthesis of intermediates to prepare the above NEP inhibitors, namely compounds according to formula (1), or salt thereof, wherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, and R3 is a carboxyl group or an ester group, preferably carboxyl group or alkyl ester.
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公开(公告)号：US09206116B2
公开(公告)日：2015-12-08
申请号：US14627542
申请日：2015-02-20
申请人： David Hook , Thomas Ruch , Bernard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar Murlidhar Waykole
发明人： David Hook , Thomas Ruch , Bernard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar Murlidhar Waykole
IPC分类号： C07C231/02 , C07C227/16 , C07C227/22 , C07C227/32 , C07C229/34 , C07C233/47 , C07C271/22 , C07D207/24 , C07D207/26 , C07D207/267 , C07D207/27 , C07D207/273 , C07D207/277 , C07D207/40 , C07D207/44 , C07F7/10 , C07C219/18 , C07D207/12 , C07C227/20 , C07C231/12 , C07C269/04 , C07D207/404 , C07D403/06 , C07C231/14
CPC分类号： C07C231/02 , C07C219/18 , C07C227/16 , C07C227/20 , C07C227/22 , C07C227/32 , C07C229/34 , C07C231/12 , C07C231/14 , C07C233/47 , C07C269/04 , C07C271/22 , C07C2601/16 , C07D207/12 , C07D207/24 , C07D207/26 , C07D207/267 , C07D207/27 , C07D207/273 , C07D207/277 , C07D207/40 , C07D207/404 , C07D207/44 , C07D403/06 , C07F7/10 , Y02P20/55
摘要： The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
摘要翻译： 本发明涉及式（1）的吡咯烷-2-酮或其盐，其中R1是氢或氮保护基，其制备方法及其在制备NEP-抑制剂中的用途，特别是在 制备N-（3-羧基-1-氧代丙基） - （4S） - （对苯基苯基甲基）-4-氨基 - （2R） - 甲基丁酸乙酯或其盐。
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公开(公告)号：US20150166468A1
公开(公告)日：2015-06-18
申请号：US14627542
申请日：2015-02-20
申请人： David Hook , Thomas Ruch , Bernard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar Murlidhar Waykole
发明人： David Hook , Thomas Ruch , Bernard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar Murlidhar Waykole
IPC分类号： C07C231/02 , C07C231/14
CPC分类号： C07C231/02 , C07C219/18 , C07C227/16 , C07C227/20 , C07C227/22 , C07C227/32 , C07C229/34 , C07C231/12 , C07C231/14 , C07C233/47 , C07C269/04 , C07C271/22 , C07C2601/16 , C07D207/12 , C07D207/24 , C07D207/26 , C07D207/267 , C07D207/27 , C07D207/273 , C07D207/277 , C07D207/40 , C07D207/404 , C07D207/44 , C07D403/06 , C07F7/10 , Y02P20/55
摘要： The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
摘要翻译： 本发明涉及式（1）的吡咯烷-2-酮或其盐，其中R1是氢或氮保护基，其制备方法及其在制备NEP-抑制剂中的用途，特别是在 制备N-（3-羧基-1-氧代丙基） - （4S） - （对苯基苯基甲基）-4-氨基 - （2R） - 甲基丁酸乙酯或其盐。
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![Process for preparing 1-(4-methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo [2,3-B]pyridin-3-yl-acetic acid](/abs-image/US/2019/12/17/US10508110B2/abs.jpg.150x150.jpg)
公开(公告)号：US10508110B2
公开(公告)日：2019-12-17
申请号：US15763562
申请日：2016-09-27
IPC分类号： C07D471/04 , C07D213/74
摘要： This invention relates to novel processes for synthesizing [1-(4-Methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl]-acetic acid and to intermediates that are used in such processes.
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公开(公告)号：US09403766B2
公开(公告)日：2016-08-02
申请号：US14939513
申请日：2015-11-12
申请人： David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
发明人： David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
IPC分类号： C07D207/26 , C07D207/38 , C07D207/263 , C07D207/36 , C07D403/06 , C07C271/22
CPC分类号： C07D207/38 , C07C271/22 , C07D207/26 , C07D207/263 , C07D207/36 , C07D403/06 , Y02P20/55
摘要： The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are ultimately related to the synthesis of intermediates to prepare the above NEP inhibitors, namely compounds according to formula (1), or salt thereof, wherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, and R3 is a carboxyl group or an ester group, preferably carboxyl group or alkyl ester.
摘要翻译： 本发明涉及生产NEP抑制剂或其前药的新方法，特别是包含γ-氨基-δ-联苯基-α-甲基链烷酸或酸酯主链的NEP抑制剂。 具体而言，根据本发明的新方法最终涉及制备上述NEP抑制剂的中间体的合成，即根据式（1）的化合物或其盐，其中R 1和R 2各自独立地 另一个是氢或氮保护基，R3是羧基或酯基，优选羧基或烷基酯。
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公开(公告)号：US09227934B2
公开(公告)日：2016-01-05
申请号：US14715129
申请日：2015-05-18
申请人： David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
发明人： David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
IPC分类号： C07D207/38
CPC分类号： C07D207/38 , C07C271/22 , C07D207/26 , C07D207/263 , C07D207/36 , C07D403/06 , Y02P20/55
摘要： The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are ultimately related to the synthesis of intermediates to prepare the above NEP inhibitors, namely compounds according to formula (1), or salt thereof, wherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, and R3 is a carboxyl group or an ester group, preferably carboxyl group or alkyl ester.
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公开(公告)号：US09840534B2
公开(公告)日：2017-12-12
申请号：US15198152
申请日：2016-06-30
申请人： Fabrice Gallou , Bernard Riss
发明人： Fabrice Gallou , Bernard Riss
摘要： The present invention relates to processes and intermediates useful for the manufacture of cyclic undecapeptides, such as Alisporivir.
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公开(公告)号：US09061973B2
公开(公告)日：2015-06-23
申请号：US14076302
申请日：2013-11-11
申请人： David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
发明人： David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
IPC分类号： C07C271/22 , C07D207/263 , C07D207/36
CPC分类号： C07D207/38 , C07C271/22 , C07D207/26 , C07D207/263 , C07D207/36 , C07D403/06 , Y02P20/55
摘要： The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are ultimately related to the synthesis of intermediates to prepare the above NEP inhibitors, namely compounds according to formula (1), or salt thereof, wherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, and R3 is a carboxyl group or an ester group, preferably carboxyl group or alkyl ester.
摘要翻译： 本发明涉及生产NEP抑制剂或其前药的新方法，特别是包含γ-氨基-δ-联苯基-α-甲基链烷酸或酸酯主链的NEP抑制剂。 具体而言，根据本发明的新方法最终涉及制备上述NEP抑制剂的中间体的合成，即根据式（1）的化合物或其盐，其中R 1和R 2各自独立地 另一个是氢或氮保护基，R3是羧基或酯基，优选羧基或烷基酯。
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