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1. WO2016053455 - PYRIMIDINONES AS FACTOR XIA INHIBITORS

Publication Number WO/2016/053455
Publication Date 07.04.2016
International Application No. PCT/US2015/042576
International Filing Date 29.07.2015
IPC
C07D 471/18 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
12in which the condensed system contains three hetero rings
18Bridged systems
A61K 31/4162 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4151,2-Diazoles
4162condensed with heterocyclic ring systems
A61P 7/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
CPC
A61K 31/4162
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
4151,2-Diazoles
4162condensed with heterocyclic ring systems
A61K 31/506
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 ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 13/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
A61P 7/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
Applicants
  • BRISTOL-MYERS SQUIBB COMPANY [US]/[US]
Inventors
  • DILGER, Andrew K.
  • CORTE, James R.
  • DE LUCCA, Indawati
  • FANG, Tianan
  • YANG, Wu
  • WANG, Yufeng
  • PABBISETTY, Kumar Balashanmuga
  • EWING, William R.
  • ZHU, Yeheng
  • WEXLER, Ruth R.
  • PINTO, Donald J.P.
  • ORWAT, Michael J.
  • SMITH II, Leon M.
Agents
  • LIU, Hong
Priority Data
62/058,31601.10.2014US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PYRIMIDINONES AS FACTOR XIA INHIBITORS
(FR) PYRIMIDINES UTILISÉES EN TANT QU'INHIBITEURS DU FACTEUR XIA
Abstract
(EN)
The present invention provides compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
(FR)
La présente invention concerne des composés de formule (I) ou des stéréo-isomères, des tautomères ou des sels de qualité pharmaceutique de ceux-ci; dans la formule, toutes les variables ayant la signification indiquée dans la description. Ces composés sont des inhibiteurs sélectifs du facteur XIa ou des inhibiteurs doubles de FXIa et de la kallicréine du plasma. Cette invention porte également sur des compositions pharmaceutiques comprenant ces composés et sur des méthodes de traitement de troubles thromboemboliques et/ou inflammatoires dans lesquelles on les utilise.
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