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    SACUBITRIL CALCIUM SALTS
    3.
    发明申请
    SACUBITRIL CALCIUM SALTS 审中-公开

    公开(公告)号：US20180296519A1

    公开(公告)日：2018-10-18

    申请号：US15737985

    申请日：2015-07-02

    申请人： NOVARTIS AG

    发明人： David Hook

    IPC分类号： A61K31/22 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  A61P25/06

    摘要： The invention relates to polymorphic forms of the calcium salt of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester. The calcium salt of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester is useful in the treatment of various conditions and disorders responsive to the inhibition of neutral endopeptidases.

    Process for preparing biaryl substituted 4-amino butyric acid or derivatives thereof and their use in the production of NEP inhibitors
    6.
    发明授权
    Process for preparing biaryl substituted 4-amino butyric acid or derivatives thereof and their use in the production of NEP inhibitors 有权
    联芳基取代的4-氨基丁酸或其衍生物的制备方法及其在NEP抑制剂生产中的应用

    公开(公告)号：US08946481B2

    公开(公告)日：2015-02-03

    申请号：US13661991

    申请日：2012-10-26

    申请人： Novartis AG

    发明人： David Hook ,  Bernhard Wietfeld ,  Matthias Lotz

    IPC分类号： C07C211/00 ,  C07C269/06

    CPC分类号： C07C269/06 ,  Y02P20/55 ,  C07C271/22

    摘要： The invention relates to a process for producing a compound according to formula (i) or salt thereof, wherein R1 and R1′ are independently hydrogen or an amine protecting group and R2 is a carboxyl group or an ester group, comprising reacting a compound according to formula (ii) or salt thereof, wherein R1, R1′ and R2 are defined as above, with hydrogen in the presence of a transition metal catalyst and a chiral ligand, wherein the transition metal is selected from group 7, 8 or 9 of the periodic table. Furthermore, the invention relates to products obtainable by said process and to their use in the production of NEP inhibitors. Moreover, the invention relates to the use of transition metal catalyst in the preparation of NEP inhibitors or prodrugs thereof.

    摘要翻译： 本发明涉及一种制备式（ⅰ）化合物或其盐的方法，其中R1和R1'独立地是氢或胺保护基，R2是羧基或酯基，包括使根据 式（ⅱ）或其盐，其中R 1，R 1'和R 2如上所定义，与氢在过渡金属催化剂和手性配体的存在下反应，其中过渡金属选自第7,8或9族 周期表。 此外，本发明涉及可通过所述方法获得的产品及其在生产NEP抑制剂中的用途。 此外，本发明涉及过渡金属催化剂在制备NEP抑制剂或其前体药物中的用途。

    PROCESS FOR PREPARING BIARYL SUBSTITUTED 4-AMINO BUTYRIC ACID OR DERIVATIVES THEREOF AND THEIR USE IN THE PRODUCTION OF NEP INHIBITORS
    7.
    发明申请
    PROCESS FOR PREPARING BIARYL SUBSTITUTED 4-AMINO BUTYRIC ACID OR DERIVATIVES THEREOF AND THEIR USE IN THE PRODUCTION OF NEP INHIBITORS 有权
    制备二价取代的4-氨基丁酸或其衍生物的方法及其在制备NEP抑制剂中的用途

    公开(公告)号：US20130066101A1

    公开(公告)日：2013-03-14

    申请号：US13661991

    申请日：2012-10-26

    申请人： Novartis AG

    发明人： David Hook ,  Bernhard Wietfeld ,  Matthias Lotz

    IPC分类号： C07C269/04

    CPC分类号： C07C269/06 ,  Y02P20/55 ,  C07C271/22

    摘要： The invention relates to a process for producing a compound according to formula (i) or salt thereof, wherein R1 and R1′ are independently hydrogen or an amine protecting group and R2 is a carboxyl group or an ester group, comprising reacting a compound according to formula (ii) or salt thereof, wherein R1, R1′ and R2 are defined as above, with hydrogen in the presence of a transition metal catalyst and a chiral ligand, wherein the transition metal is selected from group 7, 8 or 9 of the periodic table. Furthermore, the invention relates to products obtainable by said process and to their use in the production of NEP inhibitors. Moreover, the invention relates to the use of transition metal catalyst in the preparation of NEP inhibitors or prodrugs thereof.

    摘要翻译： 本发明涉及一种制备式（ⅰ）化合物或其盐的方法，其中R1和R1'独立地是氢或胺保护基，R2是羧基或酯基，包括使根据 式（ⅱ）或其盐，其中R 1，R 1'和R 2如上所定义，与氢在过渡金属催化剂和手性配体的存在下反应，其中过渡金属选自第7,8或9族 周期表。 此外，本发明涉及可通过所述方法获得的产品及其在生产NEP抑制剂中的用途。 此外，本发明涉及过渡金属催化剂在制备NEP抑制剂或其前药中的用途。