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1. (WO2018189553) COMPOUNDS USEFUL AS RET INHIBITORS
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Pub. No.: WO/2018/189553 International Application No.: PCT/GB2018/050986
Publication Date: 18.10.2018 International Filing Date: 13.04.2018
IPC:
C07D 487/04 (2006.01) ,A61P 35/00 (2006.01) ,A61K 31/519 (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
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
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
519
ortho- or peri-condensed with heterocyclic rings
Applicants:
CANCER RESEARCH TECHNOLOGY LIMITED [GB/GB]; Angel Building 407 St John Street London EC1V 4AD, GB
Inventors:
JORDAN, Allan; GB
NEWTON, Rebecca; GB
HYND, George; GB
SUTTON, Jonathan Mark; GB
WASZKOWYCZ, Bohdan; GB
Agent:
HGF LIMITED; 4th Floor, Merchant Exchange 17-19 Whitworth Street West Manchester M1 5WG, GB
Priority Data:
1705971.813.04.2017GB
Title (EN) COMPOUNDS USEFUL AS RET INHIBITORS
(FR) COMPOSÉS UTILISÉS COMME INHIBITEURS DE RET
Abstract:
(EN) The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity : Formula I wherein HET, bonds a, b, c and d, X1, X2, X3, X4, R2, and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which RET kinase activity is implicated.
(FR) La présente invention concerne des composés de formule I qui agissent en tant qu'inhibiteurs de l'activité enzymatique de la kinase RET (réarrangée durant la transfection). Formule I, dans laquelle, HET, les liaisons a, b, c et d, X1, X2, X3, X4, R2 et R3 sont chacun tels que définis dans la description. La présente invention concerne également des procédés pour la préparation de ces composés, des compositions pharmaceutiques les comprenant, et leur utilisation dans le traitement de troubles prolifératifs, notamment le cancer, ainsi que d'autres maladies ou états pathologiques dans lesquels l'activité de la kinase RET est impliquée.
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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)