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1. WO2020194115 - PROCESS FOR THE PREPARATION OF ELAGOLIX SODIUM AND INTERMEDIATES THEREOF

Publication Number WO/2020/194115
Publication Date 01.10.2020
International Application No. PCT/IB2020/052344
International Filing Date 14.03.2020
IPC
A61K 31/505 2006.01
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
C07D 239/54 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02not condensed with other rings
24having three or more double bonds between ring members or between ring members and non-ring members
28with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46Two or more oxygen, sulfur or nitrogen atoms
52Two oxygen atoms
54as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
Applicants
  • MANKIND PHARMA LTD. [IN]/[IN]
Inventors
  • THAKUR, Shelen
  • KUMAR, Sonu
  • BHASHKAR, Bhuwan
  • TATAR, Sagar
  • PANKAJ, Lovleen
  • SHARMA, Kamal Chand
  • BHAVSAR, Jigar
  • KUMAR, Ajay
  • KUMAR, Anil
Agents
  • BHATLA, Durga Das
Priority Data
20191101142225.03.2019IN
20191102985424.07.2019IN
20191104480405.11.2019IN
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR THE PREPARATION OF ELAGOLIX SODIUM AND INTERMEDIATES THEREOF
(FR) PROCÉDÉ DE PRÉPARATION D'ÉLAGOLIX SODIQUE ET D'INTERMÉDIAIRES CORRESPONDANTS
Abstract
(EN)
The present invention relates to compounds of Formula A, isomers, polymorphs and process of preparation thereof, wherein, S is a pharmaceutically acceptable salt, R is selected from hydrogen or C1-C3 alkyl group substituted with R4; wherein R4 is selected from -CN, -COR5; wherein R5 is selected from NR6R7, -OR8; wherein R6 and R7 are selected from hydrogen, straight or branched chain alkyl group, and R8 is selected from straight or branched chain alkyl group. The present invention further provides a process for the preparation of elagolix or pharmaceutical acceptable salt by using compounds of Formula A.
(FR)
La présente invention concerne des composés de formule A, des isomères, des polymorphes et un procédé de préparation correspondant, S représentant un sel pharmaceutiquement acceptable, R étant choisi parmi hydrogène ou un groupe C1-C3-alkyle substitué par R4 ; R4 étant choisi parmi -CN, -COR5 ; R5 étant choisi parmi NR6R7, -OR8 ; R6 et R7 étant choisis parmi hydrogène, un groupe alkyle à chaîne linéaire ou ramifiée et R8 étant choisi parmi un groupe alkyle à chaîne linéaire ou ramifiée. La présente invention concerne en outre un procédé de préparation d'élagolix ou d'un sel pharmaceutiquement acceptable à l'aide de composés de formule A.
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