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1. (WO2001034574) STABLE POLYMORPH OF N-(3-ETHYNYLPHENYLAMINO)-6,7-BIS(2-METHOXYETHOXY)-4-QUINAZOLINAMINE HYDROCHLORIDE, METHODS OF PRODUCTION, AND PHARMACEUTICAL USES THEREOF
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2001/034574 International Application No.: PCT/US2000/031009
Publication Date: 17.05.2001 International Filing Date: 09.11.2000
Chapter 2 Demand Filed: 11.06.2001
IPC:
A61K 31/517 (2006.01) ,A61K 45/06 (2006.01) ,C07D 239/94 (2006.01)
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
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
517
ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45
Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06
Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70
condensed with carbocyclic rings or ring systems
72
Quinazolines; Hydrogenated quinazolines
86
with hetero atoms directly attached in position 4
94
Nitrogen atoms
Applicants:
OSI PHARMACEUTICALS, INC. [US/US]; 106 Charles Lindbergh Boulevard Uniondale, NY 11553-3649, US
Inventors:
CONNELL, Richard, D.; US
MOYER, James, D.; US
MORIN, Michael, J.; US
KAJIJI, Shama, M.; US
FOSTER, Barbara, A.; US
FERRANTE, Karen, J.; US
NORRIS, Timothy; US
RAGGON, Jeffrey, W.; US
SILBERMAN, Sandra, L.; US
Agent:
WHITE, John, P.; Cooper & Dunham LLP 1185 Avenue of the Americas New York, NY 10036, US
Priority Data:
60/164,90711.11.1999US
60/193,19130.03.2000US
60/206,42023.05.2000US
Title (EN) STABLE POLYMORPH OF N-(3-ETHYNYLPHENYLAMINO)-6,7-BIS(2-METHOXYETHOXY)-4-QUINAZOLINAMINE HYDROCHLORIDE, METHODS OF PRODUCTION, AND PHARMACEUTICAL USES THEREOF
(FR) POLYMORPHE STABLE DE CHLORHYDRATE DE N-(3-ETHYNYLPHENYLAMINO)-6,7-BIS(2-METHOXYETHOXY)-4-QUINAZOLINAMINE, ET METHODES DE PRODUCTION ET UTILISATIONS PHARMACEUTIQUES DUDIT POLYMORPHE
Abstract:
(EN) The present invention relates to a stable crystalline form of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride designated the B polymorph, its production in essentially pure form, and its use. The invention also relates to the pharmaceutical compositions containing the stable polymorph B form of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine as hydrochloride, as well as other forms of the compound, and to methods of treating hyperproliferative disorders, such as cancer, by administering the compound.
(FR) La présente invention concerne une forme cristalline stable de chlorhydrate de N-(3-éthynylphényl)-6,7-bis(2-méthoxyéthoxy)-4-quinazolinamine appelée polymorphe B, ainsi que sa production sous une forme sensiblement pure et son utilisation. L'invention concerne également des compositions pharmaceutiques contenant ladite forme polymorphique stable B de N-(3-éthynylphényl)-6,7-bis(2-méthoxyéthoxy)-4-quinazolinamine comme chlorhydrate et d'autres formes du composé, ainsi que des méthodes de traitement de maladies hyperprolifératives, notamment le cancer, basées sur l'administration dudit composé.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CR, CU, CZ, DE, DK, DM, DZ, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, UZ, VN, YU, ZA, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
CZPV2002-2019HRP20020388AIS6359NO20021910PLP.355235RSP-342/02
SK5812002UZ20020397YUP-342/02MXPA/a/2002/004667APAP 1434KR1020020063889
SG88434VN7786ZA2002/03130IL177827IL149222EP1233948
JP4689916 JP2003523949 CN1414954CA2389333EA200200546NZ518406
DK1233948AU2001017621