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1. WO2022009235 - PROCESS FOR THE PREPARATION OF GILTERITINIB FUMARATE

Publication Number WO/2022/009235
Publication Date 13.01.2022
International Application No. PCT/IN2021/050676
International Filing Date 12.07.2021
IPC
C07D 401/14 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
14containing three or more hetero rings
A61K 31/497 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4965Non-condensed pyrazines
497containing further heterocyclic rings
A61K 31/517 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
517ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61P 35/02 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
02specific for leukemia
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
  • MSN LABORATORIES PRIVATE LIMITED, R&D CENTER [IN]/[IN]
  • SRINIVASAN, Thirumalai Rajan [IN]/[IN]
Inventors
  • SRINIVASAN, Thirumalai Rajan
  • SAJJA, Eswaraiah
  • MATHAD, Vijayavitthal T
  • SAGYAM, Rajeshwar Reddy
  • MACHARLA, Prabhakar
  • SHERI, Venkata Reddy
  • SALADI, Venkata Narasayya
  • KAMMARI, Bal Raju
Common Representative
  • SRINIVASAN, Thirumalai Rajan
Priority Data
20204102943910.07.2020IN
20204104372807.10.2020IN
20214101577802.04.2021IN
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR THE PREPARATION OF GILTERITINIB FUMARATE
(FR) PROCÉDÉ DE PRÉPARATION DE FUMARATE DE GILTÉRITINIB
Abstract
(EN) The present invention provides process for the preparation of 2-pyrazine carboxamide, 6-ethyl-3-[[3-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl] phenyl] amino]-5-[ (tetra hydro-2H-pyran-4-yl) amino]-, (2E)-2-butenedioate (2:1) of formula (I) and its crystalline and / or amorphous forms there of. 2-Pyrazinecarboxamide, 6-ethyl-3-[ [ 3- methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl] phenyl] amino]-5-[(tetrahydro-2H-pyran-4-yl) amino]-, (2E)-2-butenedioate (2:1) (I) is represented by the following structural formula.
(FR) La présente invention concerne un procédé de préparation de 2-pyrazinecarboxamide, 6-éthyl-3-[[3-méthoxy-4-[4-(4-méthyl-1-pipérazinyle)-1-pipéridinyle] phényle] amino]-5-[(tétra hydro-2H-pyrane-4-yl) amino]-, (2E)-2-butènedioate (2:1) de formule (I) et ses formes cristallines et/ou amorphes. Le 2-pyrazinecarboxamide, 6-éthyl-3-[[3-méthoxy-4-[4-(4-méthyl-1-pipérazinyle)-1-pipéridinyle] phényle] amino]-5-[(tétra hydro-2H-pyrane-4-yl) amino]-, (2E)-2-butènedioate (2:1) (I) est représenté par la formule développée suivante.
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