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1. WO2017021823 - CRYSTALLINE FORM OF LORLATINIB FREE BASE

Publication Number WO/2017/021823
Publication Date 09.02.2017
International Application No. PCT/IB2016/054483
International Filing Date 27.07.2016
IPC
C07D 498/18 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12in which the condensed system contains three hetero rings
18Bridged systems
A61K 31/439 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
439the ring forming part of a bridged ring system, e.g. quinuclidine
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
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
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 498/18
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12in which the condensed system contains three hetero rings
18Bridged systems
G01N 21/65
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
21Investigating or analysing materials by the use of optical means, i.e. using infra-red, visible or ultra-violet light
62Systems in which the material investigated is excited whereby it emits light or causes a change in wavelength of the incident light
63optically excited
65Raman scattering
G01N 23/20075
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
23Investigating or analysing materials by the use of wave or particle radiation, e.g. X-rays or neutrons, not covered by groups G01N3/00G01N17/00, G01N21/00 or G01N22/00
20by using diffraction of the radiation by the materials, e.g. for investigating crystal structure; by using scattering of the radiation by the materials, e.g. for investigating non-crystalline materials; by using reflection of the radiation by the materials
20075by measuring interferences of X-rays, e.g. Borrmann effect
Applicants
  • PFIZER INC. [US]/[US]
Inventors
  • BIRCH, Melissa J.
  • PENCHEVA, Klimentina Dimitrova
Agents
  • WALDRON, Roy F.
Priority Data
62/199,41831.07.2015US
62/352,34920.06.2016US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) CRYSTALLINE FORM OF LORLATINIB FREE BASE
(FR) FORME CRISTALLINE DE BASE LIBRE DE LORLATINIB
Abstract
(EN)
This invention relates to acrystalline form of (10R)-7-amino-12-fluoro-2,10,16-trimethyl- 5-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclo- tetradecine-3-carbonitrile (lorlatinib) free base (Form 7). This invention also relates to pharmaceutical compositions comprising Form 7, and to methods of using Form 7 and such compositions in the treatment of abnormal cell growth, such as cancer, in a mammal.
(FR)
La présente invention concerne la forme acristalline forme de la base libre de (10R)-7-amino-12-fluoro-2,10,16-triméthyl- 5-oxo-10,15,16,17-tétrahydro-2H-8,4-(méthéno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclo- tétradécine-3-carbonitrile (lorlatinib) (forme 7). L'invention concerne également des compositions pharmaceutiques comprenant la forme 7 et des procédés d'utilisation de la forme 7 et de telles compositions dans le traitement de la croissance cellulaire anormale, telle que le cancer, chez un mammifère.
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