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1. (WO2019041026) NOVEL CRYSTALLINE FORMS OF ACALABRUTINIB
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Pub. No.: WO/2019/041026 International Application No.: PCT/CA2018/051015
Publication Date: 07.03.2019 International Filing Date: 23.08.2018
IPC:
C07D 487/04 (2006.01) ,A61K 31/455 (2006.01) ,A61K 31/4985 (2006.01) ,A61K 9/48 (2006.01) ,A61P 35/00 (2006.01) ,A61P 35/02 (2006.01) ,C07D 213/82 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed 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
44
Non-condensed pyridines; Hydrogenated derivatives thereof
455
Nicotinic acid, i.e. niacin; Derivatives thereof, e.g. esters, amides
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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4985
Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
48
Preparations in capsules, e.g. of gelatin, of chocolate
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
02
specific for leukemia
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
82
in position 3
Applicants:
APOTEX INC. [CA/CA]; 150 Signet Drive Toronto, Ontario M9L 1T9, CA
Inventors:
SOUZA, Fabio E. S.; CA
KHALILI, Bahareh; CA
BHATTACHARYYA, Annyt; CA
GUO, Wancheng; CN
ZHANG, Jingda; CN
CHENG, Kun; CN
LI, Kangying; CN
Agent:
SCOTT, Carl; CA
CLARIZIO, Dino; CA
GOODMANS LLP; 333 Bay Street, Suite 3400 Toronto, Ontario M5H 2S7, CA
Priority Data:
62/551,41829.08.2017US
Title (EN) NOVEL CRYSTALLINE FORMS OF ACALABRUTINIB
(FR) NOUVELLES FORMES CRISTALLINES D'ACALABRUTINIB
Abstract:
(EN) The present invention provides novel crystalline forms of Acalabrutinib, Specific crystalline forms provided by the present invention include Acalabrutinib Form APO-I, a co-crystal of Acalabrutinib and urea; APO-II, a co-crystal of Acalabrutinib and nicotinamide; APO-III, a co-crystal of Acalabrutinib and L- sorbitol; APO-IV, a crystalline form of Acalabrutinib; and APO-V, a co-crystal of Acalabrutinib and urea.
(FR) La présente invention concerne de nouvelles formes cristallines d'acalabrutinib, des formes cristallines spécifiques fournies par la présente invention comprennent la forme APO-I d'acalabrutinib, un co-cristal d'acalabrutinib et d'urée ; APO-II, un co-cristal d'acalabrutinib et de nicotinamide ; APO-III, un co-cristal d'acalabrutinib et de L-sorbitol ; APO-IV, une forme cristalline d'acalabrutinib ; et APO-V, un co-cristal d'acalabrutinib et d'urée.
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, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, 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 Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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)