WO2016113372 PROCESSES FOR PREPARING DOLUTEGRAVIR AND CABOTEGRAVIR AND ANALOGUES THEREOF

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Publication Number WO/2016/113372

Publication Date 21.07.2016

International Application No. PCT/EP2016/050716

International Filing Date 15.01.2016

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Applicants

LEK PHARMACEUTICALS D.D. [SI]/[SI]

Inventors

MARAS, Nenad
SELIC, Lovro
CUSAK, Anja

Agents

KLUSCHANZOFF, Harald

Priority Data

15151449.4

16.01.2015

Publication Language English (en)

Filing Language English (EN)

Designated States

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Title

(EN) PROCESSES FOR PREPARING DOLUTEGRAVIR AND CABOTEGRAVIR AND ANALOGUES THEREOF

(FR) PROCÉDÉS DE PRÉPARATION DE CABOTÉGRAVIR DOLUTÉGRAVIR ET D'ANALOGUES DE CEUX-CI

Abstract

(EN) The present invention relates to processes for preparing substances with antiviral activity, in particular the integrase inhibitors dolutegravir and cabotegravir and analogues thereof, as well as intermediates useful in the processes.

(FR) La présente invention concerne des procédés permettant de préparer des substances ayant une activité antivirale, en particulier les inhibiteurs de l'intégrase dolutégravir et cabotégravir et des analogues de ceux-ci, ainsi que des intermédiaires utiles dans les procédés.

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
498	Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12	in which the condensed system contains three hetero rings
14	Ortho-condensed systems

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
498	Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12	in which the condensed system contains three hetero rings
14	Ortho-condensed systems

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41	having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
42	Oxazoles
421	1,3-Oxazoles, e.g. pemoline, trimethadione

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435	having six-membered rings with one nitrogen as the only ring hetero atom
4353	ortho- or peri-condensed with heterocyclic ring systems
4355	the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495	having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
4985	Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems

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1. WO2016113372 - PROCESSES FOR PREPARING DOLUTEGRAVIR AND CABOTEGRAVIR AND ANALOGUES THEREOF