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1. (WO2018049781) ALKYNYL-SUBSTITUTED HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
PCT Biblio. Data
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Latest bibliographic data on file with the International Bureau
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Pub. No.:
WO/2018/049781
International Application No.:
PCT/CN2017/072570
Publication Date:
22.03.2018
International Filing Date:
25.01.2017
IPC:
C07D 403/04
(2006.01),
C07D 401/04
(2006.01),
C07D 401/06
(2006.01),
C07D 403/06
(2006.01),
C07D 231/14
(2006.01),
A61K 31/415
(2006.01),
A61K 31/4155
(2006.01),
A61K 31/454
(2006.01),
A61P 35/00
(2006.01)
C
CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C
CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C
CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C
CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C
CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
231
Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02
not condensed with other rings
10
having two or three double bonds between ring members or between ring members and non-ring members
14
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
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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
415
1,2-Diazoles
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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
415
1,2-Diazoles
4155
not condensed and containing further heterocyclic rings
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
445
Non-condensed piperidines, e.g. piperocaine
4523
containing further heterocyclic ring systems
454
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A
HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
BEIJING TIANCHENG PHARMA CO., LTD.
[CN/CN]; Room 202, Bldg. 9, No. 1 Community, No. 8 Life Park Rd., ZGC Life Science Park, Changping District Beijing 102206 (CN)
Inventors:
CHEN, Xiangyang
; (CN).
GAO, Yingxiang
; (CN).
KONG, Xianglong, Norman
; (CN)
Agent:
CHINA PATENT AGENT (H.K.) LTD.
; 22/F, Great Eagle Centre 23 Harbour Road, Wanchai Hong Kong (CN)
Priority Data:
201610833890.3
19.09.2016
CN
Title
(EN)
ALKYNYL-SUBSTITUTED HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
(FR)
COMPOSÉ HÉTÉROCYCLIQUE SUBSTITUÉ PAR UN ALCYNYLE, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION MÉDICALE
(ZH)
炔代杂环化合物、其制备方法及其在医药学上的应用
Abstract:
(EN)
The present invention relates to an alkynyl-substituted heterocyclic compound acting as an FGFR inhibitor, a preparation method therefor and the medical use thereof. In particular, the present invention relates to a compound as shown in general formula (I) and a pharmaceutically acceptable salt thereof; a pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof; a method for treating and/or preventing FGFR-associated diseases, particularly tumours, by using the compound or a pharmaceutically acceptable salt thereof; and a preparation method for the compound or a pharmaceutically acceptable salt thereof. The present invention also relates to the use of the compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating and/or preventing FGFR-associated diseases, particularly tumours, wherein the definition of each substituent in general formula (I) is the same as that in the description.
(FR)
La présente invention concerne un composé hétérocyclique substitué par un alcynyle agissant en tant qu'inhibiteur de FGFR, son procédé de préparation et son utilisation médicale. En particulier, la présente invention concerne un composé tel que représenté dans la formule générale (I) et un sel pharmaceutiquement acceptable de celui-ci ; une composition pharmaceutique comprenant le composé ou un sel pharmaceutiquement acceptable de celui-ci ; un procédé de traitement et/ou de prévention de maladies associées à FGFR, en particulier des tumeurs, à l'aide du composé ou d'un sel pharmaceutiquement acceptable de celui-ci ; et un procédé de préparation du composé ou d'un sel pharmaceutiquement acceptable de celui-ci. La présente invention concerne également l'utilisation du composé ou d'un sel pharmaceutiquement acceptable de celui-ci, ou la composition pharmaceutique comprenant le composé ou un sel pharmaceutiquement acceptable de celui-ci dans la préparation d'un médicament pour le traitement et/ou la prévention de maladies associées au FGFR, en particulier des tumeurs, la définition de chaque substituant dans la formule générale (I) étant la même que celle dans la description.
(ZH)
本发明涉及作为FGFR抑制剂的炔代杂环化合物、其制备方法及其在医药学上的应用。具体而言,本发明涉及一种通式(I)所示的化合物及其可药用的盐、含有所述化合物或其可药用的盐的药物组合物、应用所述化合物或其可药用的盐治疗和/或预防FGFR相关性病症、特别是肿瘤的方法以及所述化合物或其可药用的盐的制备方法。本发明还涉及所述化合物或其可药用的盐或含有所述化合物或其可药用的盐的药物组合物在制备用于治疗和/或预防FGFR相关性病症、特别是肿瘤的药物中的用途。其中通式(I)的各取代基与说明书中的定义相同。
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, 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 (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:
Chinese (
ZH
)
Filing Language:
Chinese (
ZH
)