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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
Applicant: David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
Inventor： David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
IPC: C07C271/22 , C07D207/263 , C07D207/36
CPC classification number: C07D207/38 , C07C271/22 , C07D207/26 , C07D207/263 , C07D207/36 , C07D403/06 , Y02P20/55
Abstract: 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.
Abstract translation: 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：US20110046397A1
公开(公告)日：2011-02-24
申请号：US12863213
申请日：2009-01-16
Applicant: David Hook , Bernhard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Phillippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
Inventor： David Hook , Bernhard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Phillippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
IPC: C07D403/06 , C07D207/38 , C07C229/34
CPC classification number: C07D207/38 , C07C271/22 , C07D207/26 , C07D207/263 , C07D207/36 , C07D403/06 , Y02P20/55
Abstract: 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.
Abstract translation: 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
Applicant: David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
Inventor： David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
IPC: C07D207/38 , C07D403/06
CPC classification number: C07D207/38 , C07C271/22 , C07D207/26 , C07D207/263 , C07D207/36 , C07D403/06 , Y02P20/55
Abstract: 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
Applicant: David Hook , Thomas Ruch , Bernard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar Murlidhar Waykole
Inventor： David Hook , Thomas Ruch , Bernard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar Murlidhar Waykole
IPC: 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 classification number: 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
Abstract: 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.
Abstract translation: 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
Applicant: David Hook , Thomas Ruch , Bernard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar Murlidhar Waykole
Inventor： David Hook , Thomas Ruch , Bernard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar Murlidhar Waykole
IPC: C07C231/02 , C07C231/14
CPC classification number: 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
Abstract: 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.
Abstract translation: 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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Patent Agency Ranking
公开(公告)号：US20150246881A1
公开(公告)日：2015-09-03
申请号：US14715129
申请日：2015-05-18
Applicant: David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
Inventor： David Hook , Bernard Riss , Daniel Kaufmann , Matthias Napp , Erhard Bappert , Philippe Polleux , Jonathan Medlock , Antonio Zanotti-Gerosa
IPC: C07D207/38
CPC classification number: C07D207/38 , C07C271/22 , C07D207/26 , C07D207/263 , C07D207/36 , C07D403/06 , Y02P20/55
Abstract: 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.
Abstract translation: 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：US08716495B2
公开(公告)日：2014-05-06
申请号：US13333437
申请日：2011-12-21
Applicant: David Hook , Thomas Ruch , Bernhard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar M Waykole
Inventor： David Hook , Thomas Ruch , Bernhard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar M Waykole
IPC: C07D207/26 , C07C219/18 , C07D207/12
CPC classification number: 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
Abstract: 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.
Abstract translation: 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：US08115016B2
公开(公告)日：2012-02-14
申请号：US12522767
申请日：2008-01-10
Applicant: David Hook , Thomas Ruch , Bernhard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar M Waykole
Inventor： David Hook , Thomas Ruch , Bernhard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar M Waykole
IPC: C07D207/26 , C07D207/27 , C07D207/263 , C07D207/267 , C07F7/10
CPC classification number: 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
Abstract: 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.
Abstract translation: 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） - （对苯基苯甲基）-4-氨基 - （2R） - 甲基丁酸乙酯或其盐。
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公开(公告)号：US20110112121A1
公开(公告)日：2011-05-12
申请号：US12827218
申请日：2010-06-30
Applicant: Joerg BERGHAUSEN , Claire HAUG , Michael HERBIG , Bin HU , Stéphane JONAT , Rajender LELETI , Josef Gottfried MEINGASSNER , Stéphanie MONNIER , Matthias NAPP , Mahavir PRASHAD , Anton STÜTZ , Ranjit THAKUR
Inventor： Joerg BERGHAUSEN , Claire HAUG , Michael HERBIG , Bin HU , Stéphane JONAT , Rajender LELETI , Josef Gottfried MEINGASSNER , Stéphanie MONNIER , Matthias NAPP , Mahavir PRASHAD , Anton STÜTZ , Ranjit THAKUR
IPC: A61K31/505 , A61P17/00 , A61P17/06 , C07D239/02
CPC classification number: A61K31/505 , A61K9/0014 , A61K47/06 , A61K47/10 , A61K47/14 , C07D239/34
Abstract: The present invention relates to pharmaceutical compositions of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide, to the use of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide and compositions of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide in therapeutic applications, especially indications with a dysregulation/overexpression of VEFG, (neo)-vascularisation and VEGF driven angiogenesis and to methods for manufacturing such compositions, the invention further relates to specific forms of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide and to the manufacturing and use of such forms. The present invention also relates to a new process to produce 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide.
Abstract translation: 本发明涉及6-（6-羟基甲基 - 嘧啶-4-基氧基） - 萘-1-羧酸（3-三氟甲基 - 苯基） - 酰胺的药物组合物，其用于6-（6-羟甲基 - 嘧啶 -4-基氧基） - 萘-1-羧酸（3-三氟甲基 - 苯基） - 酰胺和6-（6-羟基甲基 - 嘧啶-4-基氧基） - 萘-1-甲酸（3-三氟甲基 - 苯基） ） - 酰胺在治疗应用中，特别是VEFG（neo）血管形成和VEGF驱动的血管发生的失调/过度表达的适应症以及制备这种组合物的方法，本发明还涉及6-（6-羟甲基嘧啶 -4-基氧基） - 萘-1-羧酸（3-三氟甲基 - 苯基） - 酰胺，并且制备和使用这种形式。 本发明还涉及产生6-（6-羟甲基 - 嘧啶-4-基氧基） - 萘-1-羧酸（3-三氟甲基 - 苯基） - 酰胺的新方法。
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公开(公告)号：US08993785B2
公开(公告)日：2015-03-31
申请号：US14224700
申请日：2014-03-25
Applicant: David Hook , Thomas Ruch , Bernard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar Murlidhar Waykole
Inventor： David Hook , Thomas Ruch , Bernard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar Murlidhar Waykole
IPC: C07D207/38 , C07D207/267 , C07D207/44 , C07C269/04 , C07C227/16 , C07C227/22 , C07C227/32 , C07C229/34 , C07C231/02 , C07C233/47 , C07C271/22 , C07D207/24 , C07D207/26 , C07D207/27 , C07D207/273 , C07D207/277 , C07D207/40 , C07F7/10 , C07C219/18 , C07D207/12 , C07C227/20 , C07C231/12 , C07D207/404 , C07D403/06
CPC classification number: 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
Abstract: 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.
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