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1. WO2017067447 - A SALT OF EGFR INHIBITOR, CRYSTALLINE FORM AND USES THEREOF

Publication Number WO/2017/067447
Publication Date 27.04.2017
International Application No. PCT/CN2016/102453
International Filing Date 18.10.2016
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
056
with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
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
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
04
specific for metastasis
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
10
for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11
Drugs for disorders of the respiratory system
C07D 491/056 (2006.01)
A61K 31/517 (2006.01)
A61P 35/00 (2006.01)
A61P 35/04 (2006.01)
A61P 9/10 (2006.01)
A61P 11/00 (2006.01)
CPC
A61K 2300/00
A61K 31/337
A61K 31/427
A61K 31/436
A61K 31/517
A61K 31/5355
Applicants
  • SUNSHINE LAKE PHARMA CO., LTD. [CN/CN]; Northern Industrial Area, Songshan Lake Dongguan, Guangdong 523000, CN
Inventors
  • LIU, Bing; CN
  • ZHANG, Weihong; CN
  • ZHANG, Yingjun; CN
Agents
  • TSINGYIHUA INTELLECTUAL PROPERTY LLC; Room 301 Trade Building, Zhaolanyuan, Tsinghua University, Qinghuayuan, Haidian District Beijing 100084, CN
Priority Data
201510677405.319.10.2015CN
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) A SALT OF EGFR INHIBITOR, CRYSTALLINE FORM AND USES THEREOF
(FR) SEL D'UN INHIBITEUR D'EGFR, FORME CRISTALLINE CORRESPONDANTE ET UTILISATIONS CORRESPONDANTES
Abstract
(EN)
The invention relates to a salt, a hydrate or a crystalline form of an EGFR inhibitor, and use thereof. Specifically it relates to 4-[ (3-chloro-4-fluorophenyl) amino] -7-methoxy-6- [3-[ (1R, 6S) -2, 5-dioxa-8-azabicyclo [4.3.0] nonan-8-yl] propoxy] quinazoline dimethanesulfonate, hydrate and a crystalline form thereof; the invention also relates to a preparation method of the crystalline form disclosed herein, a pharmaceutical composition containing the crystalline form, and uses thereof for treating proliferative disorders.
(FR)
L'invention concerne un sel, un hydrate ou une forme cristalline d'un inhibiteur d'EGFR et une utilisation correspondante. En particulier, l'invention concerne un diméthanesulfonate de 4-[(3-chloro-4-fluorophényl)-amino]-7-méthoxy-6-[3-[(1R,6S)-2,5-dioxa-8-azabicyclo[4.3.0]nonan-8-yl]-propoxy]-quinazoline, un hydrate correspondant et une forme cristalline correspondante; l'invention concerne également un procédé de préparation de la forme cristalline selon la présente invention, une composition pharmaceutique contenant la forme cristalline et des utilisations correspondantes pour le traitement de troubles prolifératifs.
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