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1. WO2019075108 - CRYSTALLINE FORMS

Publication Number WO/2019/075108
Publication Date 18.04.2019
International Application No. PCT/US2018/055279
International Filing Date 10.10.2018
IPC
C07D 471/04 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
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61K 31/437 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
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
CPC
A61K 9/0053
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0012Galenical forms characterised by the site of application
0053Mouth and digestive tract, i.e. intraoral and peroral administration
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07B 2200/13
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
13Crystalline forms, e.g. polymorphs
C07D 471/04
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 C07D451/00 - C07D463/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 471/08
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 C07D451/00 - C07D463/00
02in which the condensed system contains two hetero rings
08Bridged systems
Applicants
  • ARRAY BIOPHARMA INC. [US]/[US]
Inventors
  • METCALF, Andrew T.
  • FRY, David
  • MCFADDIN, Elizabeth A.
  • KOLAKOWSKI, Gabrielle R.
  • HAAS, Julia
  • TANG, Tony P.
  • JIANG, Yutong
Agents
  • MYERS, James, B.
Priority Data
62/570,57310.10.2017US
62/643,95016.03.2018US
62/656,66812.04.2018US
62/669,28809.05.2018US
62/676,41725.05.2018US
62/712,70731.07.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) CRYSTALLINE FORMS
(FR) FORMES CRISTALLINES
Abstract
(EN)
Provided herein are compound of Formula I-IV and pharmaceutically acceptable salts thereof which exhibit rearranged during transfection (RET) kinase inhibition. In particular, provided herein are novel crystalline forms of 4-(6-(4-((6-methoxypyridin-3-yl)methyl)piperazin-1-yl)pyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula I), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula II), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-(6-methoxynicotinoyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula III), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(4-hydroxy-4-(pyridin-2-ylmethyl)piperidin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula IV), and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds, processes for making the compounds, and the use of the compounds in therapy. More particularly, the application relates to novel crystalline forms of Formula I-IV and pharmaceutically acceptable salts thereof useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
(FR)
L'invention concerne un composé de formule I-IV et des sels pharmaceutiquement acceptables de celui-ci qui présentent une inhibition de la kinase réarrangée au cours de la transfection (RET). En particulier, l'invention concerne de nouvelles formes cristallines de 4-(6-(4-((6-méthoxypyridin-3-yl) méthyl) pipérazin-1-yl)pyridin-3-yl)-6-(1-méthyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (formule I), de 6-(2-hydroxy-2-méthylpropoxy)-4-(6-(6-((6-méthoxypyridin-3-yl)méthyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (formule II), de 6- (2-hydroxy-2-méthylpropoxy)-4-(6-(6-(6-méthoxynicotinoyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (formule III), de 6- (2-hydroxy-2-méthylpropoxy)-4-(6-(4-hydroxy-4-(pyridin-2-yl-méthyl))pipéridin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (formule IV), et des sels pharmaceutiquement acceptables de ceux-ci, des compositions pharmaceutiques comprenant les composés, des procédés de fabrication des composés, et l'utilisation des composés en thérapie. Plus particulièrement, l'invention concerne de nouvelles formes cristallines de formule I-IV et des sels pharmaceutiquement acceptables de celles-ci, utiles dans le traitement et la prévention de maladies qui peuvent être traitées avec un inhibiteur de kinase RET, y compris des maladies et des troubles associés à RET.
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