WO2018116139 NEW PICOLINIC ACID DERIVATIVES AND THEIR USE AS INTERMEDIATES

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Publication Number WO/2018/116139

Publication Date 28.06.2018

International Application No. PCT/IB2017/058081

International Filing Date 18.12.2017

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Applicants

NOVARTIS AG [CH]/[CH]

Inventors

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

Agents

NOVARTIS AG

Priority Data

62/436,222

19.12.2016

Publication Language English (en)

Filing Language English (EN)

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Title

(EN) NEW PICOLINIC ACID DERIVATIVES AND THEIR USE AS INTERMEDIATES

(FR) NOUVEAUX DÉRIVÉS D'ACIDE PICOLINIQUE ET LEUR UTILISATION EN TANT QU'INTERMÉDIAIRES

Abstract

(EN) 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)

(FR) La présente invention concerne de nouveaux dérivés d'acide picolinique de formule (I) et leur utilisation en tant qu'intermédiaires dans le procédé de fabrication de dérivés de pyridine, y compris (S)-3-amino-6-méthoxy-N-(3,3,3-trifluoro-2-hydroxy-2-méthylpropyl)-5-(trifluorométhyl)picolinamide qui sont utiles pour le traitement de troubles respiratoires. (I)

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
213	Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02	having three double bonds between ring members or between ring members and non-ring members
04	having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60	with 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
78	Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
79	Acids; Esters

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
213	Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02	having three double bonds between ring members or between ring members and non-ring members
04	having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60	with 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
78	Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
81	Amides; Imides

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
213	Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02	having three double bonds between ring members or between ring members and non-ring members
04	having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60	with 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
78	Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
79	Acids; Esters

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
213	Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02	having three double bonds between ring members or between ring members and non-ring members
04	having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60	with 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
78	Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
81	Amides; Imides

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

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1. WO2018116139 - NEW PICOLINIC ACID DERIVATIVES AND THEIR USE AS INTERMEDIATES

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11	Drugs for disorders of the respiratory system