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1. WO2022009098 - MANUFACTURE OF COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF SHP2

Publication Number WO/2022/009098
Publication Date 13.01.2022
International Application No. PCT/IB2021/056057
International Filing Date 06.07.2021
IPC
C07D 491/107 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02in which the condensed system contains two hetero rings
10Spiro-condensed systems
107with only one oxygen atom as ring hetero atom in the oxygen-containing ring
C07D 211/60 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
36with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 241/20 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
241Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
02not condensed with other rings
10having three double bonds between ring members or between ring members and non-ring members
14with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
20Nitrogen atoms
C07D 401/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
Applicants
  • NOVARTIS AG [CH]/[CH]
Inventors
  • FEI, Zhongbo
  • LI, Wei
  • YU, Huangchao
  • JIA, Huanqing
  • WANG, Jianhua
Agents
  • NOVARTIS AG
Priority Data
PCT/CN2020/10088208.07.2020CN
PCT/CN2021/09413917.05.2021CN
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) MANUFACTURE OF COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF SHP2
(FR) FABRICATION DE COMPOSÉS ET DE COMPOSITIONS POUR INHIBER L'ACTIVITÉ DE SHP2
Abstract
(EN) The present invention relates to a method for the manufacture of a compound of Formula I or a pharmaceutically acceptable salt, acid co-crystal, hydrate or other solvate thereof, said method comprising reacting a compound of the formula II with a compound of the formula III according to the following reaction scheme:. wherein LG, A, n, m and p are as defined in the Summary of the Invention, said manufacture including the manufacture and use of a compound of the formula VI; wherein R1 is a secondary amino protecting group and R5 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl or unsubstituted or substituted aryl.
(FR) La présente invention concerne un procédé de fabrication d'un composé de formule I ou d'un sel pharmaceutiquement acceptable, un co-cristal d'acide, un hydrate ou un autre solvate de celui-ci, ledit procédé comprenant la réaction d'un composé de formule II avec un composé de formule III selon le schéma de réaction suivant : LG, A, n, m et p étant tels que définis dans le résumé de l'invention, ladite fabrication comprenant la production et l'utilisation d'un composé de formule VI : ; R1 représente un groupe protecteur amino secondaire et R5 représente alkyle non substitué ou substitué, cycloalkyle non substitué ou substitué ou aryle non substitué ou substitué.
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