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1. NZ518406 - Stable polymorph of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof

Organismo Nova Zelândia
Número do pedido 518406
Data do pedido 09.11.2000
Número da publicação 518406
Data de publicação 30.01.2004
№ da concessão
Data da concessão 10.05.2004
Tipo de publicação B
CIP
C07D 239/04
CQUÍMICA; METALURGIA
07QUÍMICA ORGÂNICA
DCOMPOSTOS HETEROCÍCLICOS
239Compostos heterocíclicos contendo anéis 1,3-diazina ou 1,3-diazina hidrogenada
02não-condensados com outros anéis
04não tendo duplas ligações entre membros do anel ou entre membros do anel e não membros do anel
A61K 31/505
ANECESSIDADES HUMANAS
61CIÊNCIA MÉDICA OU VETERINÁRIA; HIGIENE
KPREPARAÇÕES PARA FINALIDADES MÉDICAS, ODONTOLÓGICAS OU HIGIÊNICAS
31Preparações medicinais contendo ingredientes ativos orgânicos
33Compostos heterocíclicos
395tendo nitrogênio como heteroátomo do anel, p. ex. guanetidina, rifamicinas
495tendo anéis de seis membros com dois átomos de nitrogênio como os únicos heteroátomos de um anel, p. ex. piperazinas
505Pirimidinas; Pirimidinas hidrogenadas, p. ex. trimetoprim
CPC
A61K 31/517
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
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
517ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 9/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
10for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 35/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
04specific for metastasis
A61P 37/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
Requerentes OSI PHARMACEUTICALS, LLC
Inventores Connell, Richard D
Moyer James D
Morin, Michael J
Kajiji, Shama M
Foster, Barbara A
Ferrante, Karen J
Norris, Timothy
Raggon, Jeffrey W
Silberman, Sandra L
Mandatários AJ PARK
Dados da prioridade 00 193191 30.03.2000 US
00 206420 23.05.2000 US
99 164907 11.11.1999 US
Título
(EN) Stable polymorph of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof
Resumo
(EN)
Patent 518406 A homogeneous crystalline polymorph of the hydrochloride salt of N- (3-ethynylphenyl)-6,7-bis(2 methoxyethoxy)-4-quinazolinamine designated the B polymorph that exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2-theta at approximately 6.26, 12.48, 13.39, 16.96, 20.20, 21.10, 22.98, 24.46, 25.14 and 26. 91. The compound is used to treat abnormal cell growth such as cancer and atherosclerosis. N- (3-ethynylphenyl)-6,7-bis(2 methoxyethoxy)-4-quinazolinamine in anhydrous from or hydrate form is used in the manufacture of a medicament to treat non small cell lung cancer, pediatric malignancies, cervical and other tumours caused or promoted by human papilloma virus, endometrial cancer, Barrett���s esophagus (pre malignant syndrome) or neoplastic cutaneous diseases.

Também publicado como
GE6493
GE6493/1
HRP20020388A
ININ/PCT/2002/00497/DEL
ININ/PCT/2002/00507/DEL
IS6359
NO20021910
PLP.355235
UZ20020397
YUP-342/02
ZA200203130