公开(公告)号：WO2017098430A1

公开(公告)日：2017-06-15

申请号：PCT/IB2016/057435

申请日：2016-12-08

Applicant: NOVARTIS AG

Inventor： KLEINBECK-RINIKER, Florian Karl ,  MARTIN, Benjamin ,  PENN, Gerhard ,  VENTURONI, Francesco ,  SCHLAMA, Thierry ,  RUCH, Thomas ,  ALLMENDINGER, Thomas ,  WIETFELD, Bernhard ,  FILIPPONI, Paolo

IPC: C07D267/02 ,  C07D207/36 ,  C07C57/46

CPC classification number: C07D207/36 ,  C07B2200/07 ,  C07C59/84 ,  C07C69/738 ,  C07C229/34 ,  C07C251/40 ,  C07C251/66 ,  C07C313/06 ,  C07D265/02

Abstract: The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route.

Abstract translation: 本发明涉及用于制备中性溶酶（NEP）抑制剂沙丙胺的新型化学合成，中间体和催化剂。 它进一步涉及新的中间体化合物及其用于所述新化学合成路线的用途。

公开(公告)号：WO2016098070A1

公开(公告)日：2016-06-23

申请号：PCT/IB2015/059779

申请日：2015-12-18

Applicant: NOVARTIS AG ,  GALLAND, Celine ,  GRANDEURY, Arnaud ,  BUDZ, Jerzy Antoni ,  MARTIN, Benjamin ,  SUSANNE, Flavien ,  AUBRY, Michel ,  SEVINC, Serbuelent ,  DECKER, Andrea

Inventor： GALLAND, Celine ,  GRANDEURY, Arnaud ,  BUDZ, Jerzy Antoni ,  MARTIN, Benjamin ,  SUSANNE, Flavien ,  AUBRY, Michel ,  SEVINC, Serbuelent ,  DECKER, Andrea

IPC: C07D401/12 ,  A61K31/506 ,  A61P35/00

CPC classification number: C07D401/12

Abstract: The present invention is directed to a new form of 5-Chloro-N2-(2-isopropoxy-5-methyl-4-piperidin-4-yl-phenyl)-N4-[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2, 4-diamine. The present disclosure also generally relates to a pharmaceutical composition comprising the form, as well of methods for obtaining such form, and methods of using the form as a medicine.

Abstract translation: 本发明涉及新形式的5-氯-N 2 - （2-异丙氧基-5-甲基-4-哌啶-4-基 - 苯基）-N4- [2-（丙烷-2-磺酰基） - 苯基 ] - 嘧啶-2,4-二胺。 本公开内容还通常涉及包含形式以及获得这种形式的方法的药物组合物以及使用该形式作为药物的方法。

公开(公告)号：WO2020016749A3

公开(公告)日：2020-01-23

申请号：PCT/IB2019/056024

申请日：2019-07-15

Applicant: NOVARTIS AG

Inventor： FU, Peng ,  GAI, Yu ,  GAO, Feng ,  KONG, Weiyong ,  LU, Yadong ,  MIN, Zhongcheng ,  RONG, Shaofeng ,  SHU, Chutian ,  WANG, Can ,  WANG, Ruidong ,  ZHAO, Jibin ,  ZHAO, Xianglin ,  ZHAO, Yi ,  ZHOU, Jianguang ,  MARTIN, Benjamin

IPC: C07D401/06

Abstract: The present invention relates to a method of synthesizing a compound of formula (I) also referred to as 4-((2S,4S)-(4-ethoxy-1 -((5-methoxy-7-methyl-1 /-/-indol-4-yl)methyl)piperidin-2-yl) )benzoic acid, or a pharmaceutically acceptable salt thereof, and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof.

公开(公告)号：WO2016128924A1

公开(公告)日：2016-08-18

申请号：PCT/IB2016/050725

申请日：2016-02-11

Applicant: NOVARTIS AG

Inventor： MARTIN, Benjamin ,  MANDRELLI, Francesca ,  VENTURONI, Francesco

IPC: C07C201/12 ,  C07C227/04 ,  C07C335/16

CPC classification number: C07C201/10 ,  B01J31/0237 ,  B01J31/0241 ,  B01J31/0244 ,  B01J31/0265 ,  C07B2200/07 ,  C07C201/12 ,  C07C205/04 ,  C07C205/44 ,  C07C205/51 ,  C07C227/04 ,  C07C335/16 ,  C07C2601/14 ,  C07C2602/08 ,  C07D207/06 ,  C07F7/1852 ,  C07F9/5355 ,  C07C205/53 ,  C07C229/34

Abstract: The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route.

Abstract translation: 本发明涉及一种新的化学合成，中间体和催化剂，可用于制备尼泊尔溶液（NEP）抑制剂赛比普利。 它还涉及新的中间体化合物及其用于所述新的化学合成途径。

公开(公告)号：WO2020016749A2

公开(公告)日：2020-01-23

申请号：PCT/IB2019/056024

申请日：2019-07-15

Applicant: NOVARTIS AG

Inventor： FU, Peng ,  GAI, Yu ,  GAO, Feng ,  KONG, Weiyong ,  LU, Yadong ,  MIN, Zhongcheng ,  RONG, Shaofeng ,  SHU, Chutian ,  WANG, Can ,  WANG, Ruidong ,  ZHAO, Jibin ,  ZHAO, Xianglin ,  ZHAO, Yi ,  ZHOU, Jianguang ,  MARTIN, Benjamin

IPC: C07D401/06

Abstract: The present invention relates to a method of synthesizing a compound of formula (I) also referred to as 4-((2S,4S)-(4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl))benzoic acid, or a pharmaceutically acceptable salt thereof, and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof.

公开(公告)号：WO2018116139A1

公开(公告)日：2018-06-28

申请号：PCT/IB2017/058081

申请日：2017-12-18

Applicant: NOVARTIS AG

Inventor： HEINZ, Thomas ,  MARTIN, Benjamin ,  RAMPF, Florian Andreas ,  ZAUGG, Werner

IPC: C07D213/79 ,  C07D213/81

Abstract: The present invention relates to new picolinic acid derivatives of formula (I) and their use as intermediates in the process of making pyridine derivatives, including (S)-3-amino-6- methoxy-N-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)picolinamide that are useful for the treatment of respiratory disorders. (I)

公开(公告)号：WO2018033866A1

公开(公告)日：2018-02-22

申请号：PCT/IB2017/054976

申请日：2017-08-16

Applicant: NOVARTIS AG

Inventor： MARTIN, Benjamin ,  KLEINBECK-RINIKER, Florian Karl ,  PENN, Gerhard ,  VENTURONI, Francesco ,  SEDELMEIER, Joerg ,  SEDELMEIER, Gottfried ,  MAFLI, Ives

IPC: C07C67/38 ,  C07C69/738 ,  C07C201/06 ,  C07C201/12 ,  C07C201/16 ,  C07C205/51 ,  C07C205/53 ,  C07C227/18 ,  C07C231/02 ,  C07C249/08 ,  C07C251/38 ,  C07C269/00 ,  C07C271/22 ,  C07D207/12 ,  C07D213/36

Abstract: The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril, inter alia via nitro 5 compounds. It further relates to new intermediate compounds and their use for said new chemical synthesis route, as well as a new catalyst ligand.

Abstract translation: 本发明涉及一种新的化学合成，用于制备中性溶酶（NEP）抑制剂沙丙胺醇尤其是通过硝基化合物的中间体和催化剂。 它还涉及新的中间体化合物及其用于所述新的化学合成路线以及新的催化剂配体。

公开(公告)号：WO2017051326A1

公开(公告)日：2017-03-30

申请号：PCT/IB2016/055628

申请日：2016-09-21

Applicant: NOVARTIS AG ,  MARTIN, Benjamin ,  PENN, Gerhard ,  SCHENKEL, Berthold ,  BOURNE, Samuel ,  LAU, Shing-Hing ,  LEY, Steven

Inventor： MARTIN, Benjamin ,  PENN, Gerhard ,  SCHENKEL, Berthold ,  BOURNE, Samuel ,  LAU, Shing-Hing ,  LEY, Steven

IPC: C07C69/653 ,  C07C313/06 ,  C07C229/34 ,  C07C47/23

CPC classification number: C07C313/06 ,  C07B2200/07 ,  C07C2/861 ,  C07C45/36 ,  C07C45/41 ,  C07C67/31 ,  C07C67/317 ,  C07C67/343 ,  C07C227/20 ,  C07C381/00 ,  C07C2523/44 ,  C07C2531/04 ,  C07C229/34 ,  C07C69/738 ,  C07C69/732 ,  C07C69/616 ,  C07C47/23 ,  C07C15/50

Abstract: The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors such as sacubitril, and prodrugs thereof.

Abstract translation: 本发明涉及可用于合成药物活性化合物，特别是中性肽链内切酶（NEP）抑制剂例如茜素的新方法，新工艺步骤和新型中间体及其前药。

公开(公告)号：WO2010015675A1

公开(公告)日：2010-02-11

申请号：PCT/EP2009/060203

申请日：2009-08-06

Applicant: NOVARTIS AG ,  MARTIN, Benjamin

Inventor： MARTIN, Benjamin

IPC: C07D401/04 ,  A61K39/385 ,  A61P25/34

CPC classification number: C07D401/04 ,  A61K39/0013

Abstract: A process for preparing a nicotine-based hapten of formula (I) or a salt or solvate thereof, wherein n, R 1 and R 2 have the meanings as indicated in the specification. The nicotine-based hapten forms part of a smoking cessation vaccine.

Abstract translation: 制备式（I）的基于尼古丁的半抗原或其盐或溶剂合物的方法，其中n，R 1和R 2具有说明书中指出的含义。 尼古丁的半抗原形成戒烟疫苗的一部分。

公开(公告)号：EP3256444B1

公开(公告)日：2019-03-27

申请号：EP16704711.7

申请日：2016-02-11

Applicant: Novartis AG

Inventor： MARTIN, Benjamin ,  MANDRELLI, Francesca ,  VENTURONI, Francesco

IPC: C07C201/12 ,  C07C227/04 ,  C07C335/16