WO2016153996 DEUTERIUM-ENRICHED HYPOXIA-INDUCIBLE FACTOR PROLYL HYDROXYLASE ENZYME INHIBITORS

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Publication Number WO/2016/153996

Publication Date 29.09.2016

International Application No. PCT/US2016/023132

International Filing Date 18.03.2016

IPC

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Applicants

AKEBIA THERAPEUTICS, INC. [US]/[US]

Inventors

HANSELMANN, Roger

Agents

BRUNER, Michael, J.

Priority Data

62/136,078

20.03.2015

Publication Language English (en)

Filing Language English (EN)

Designated States

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Title

(EN) DEUTERIUM-ENRICHED HYPOXIA-INDUCIBLE FACTOR PROLYL HYDROXYLASE ENZYME INHIBITORS

(FR) INHIBITEURS DE L'ENZYME PROLYL HYDROXYLASE DU FACTEUR INDUCTIBLE PAR HYPOXIE ENRICHIS EN DEUTÉRIUM

Abstract

(EN) Provided herein are deuterium-enriched compounds of Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V), and Formula (VI). Pharmaceutical compositions comprising the isotope-enriched compounds, and methods of using such compounds are also provided.

(FR) La présente invention concerne des composés enrichis en deutérium de Formule (I), de Formule (II), de Formule (III), de Formule (IV), de Formule (V), et de Formule (VI). La présente invention concerne également des compositions pharmaceutiques comprenant les composés enrichis en isotopes, ainsi que des procédés d'utilisation de ces composés.

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
44	Non-condensed pyridines; Hydrogenated derivatives thereof
4412	having oxo groups directly attached to the heterocyclic ring

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
62	Oxygen or sulfur atoms
63	One oxygen atom
65	attached in position 3 or 5

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
44	Non-condensed pyridines; Hydrogenated derivatives thereof
4412	having oxo groups directly attached to the heterocyclic ring

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
62	Oxygen or sulfur atoms
63	One oxygen atom
65	attached in position 3 or 5

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1. WO2016153996 - DEUTERIUM-ENRICHED HYPOXIA-INDUCIBLE FACTOR PROLYL HYDROXYLASE ENZYME INHIBITORS

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7	Drugs for disorders of the blood or the extracellular fluid
06	Antianaemics

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
B	GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200	Indexing scheme relating to specific properties of organic compounds
05	Isotopically modified compounds, e.g. labelled