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1. (WO2017021823) CRYSTALLINE FORM OF LORLATINIB FREE BASE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/021823 International Application No.: PCT/IB2016/054483
Publication Date: 09.02.2017 International Filing Date: 27.07.2016
IPC:
C07D 498/18 (2006.01) ,A61K 31/439 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
498
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12
in which the condensed system contains three hetero rings
18
Bridged systems
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, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
439
the ring forming part of a bridged ring system, e.g. quinuclidine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
PFIZER INC. [US/US]; 235 East 42nd Street New York, NY 10017, US
Inventors:
BIRCH, Melissa J.; GB
PENCHEVA, Klimentina Dimitrova; GB
Agent:
WALDRON, Roy F.; US
Priority Data:
62/199,41831.07.2015US
62/352,34920.06.2016US
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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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)