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1. (WO2017098421) BENZOTHIADIAZINE COMPOUNDS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/098421 International Application No.: PCT/IB2016/057415
Publication Date: 15.06.2017 International Filing Date: 07.12.2016
IPC:
C07D 417/12 (2006.01) ,A61K 31/549 (2006.01) ,C07D 471/04 (2006.01) ,C07D 285/28 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
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
54
having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
549
having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
285
Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/-C07D283/183
15
Six-membered rings
16
Thiadiazines; Hydrogenated thiadiazines
18
1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines
20
condensed with carbocyclic rings or ring systems
22
condensed with one six-membered ring
24
with oxygen atoms directly attached to the ring sulfur atom
26
substituted in position 6 or 7 by sulfamoyl or substituted sulfamoyl radicals
28
with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached in position 3
Applicants:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED [GB/GB]; 980 Great West Road Brentford Middlesex TW89GS, GB
Inventors:
ADAMS, Jerry Leroy; US
ATOR, Laura E.; US
DUFFY, Kevin J.; US
GRAYBILL, Todd L.; US
KIESOW, Terence John; US
LIAN, Yiqian; US
MOORE, Michael Lee; US
RALPH, Jeffrey M.; US
RIDGERS, Lance Howard; US
Priority Data:
62/264,41908.12.2015US
Title (EN) BENZOTHIADIAZINE COMPOUNDS
(FR) COMPOSÉS BENZOTHIADIAZINE
Abstract:
(EN) The invention is directed to substituted benzothiadiazine derivatives. Specifically, the invention is directed to compounds according to Formula (I):wherein R, R1, R2, R3, R4 and R5 are as defined herein. The compounds of the invention are inhibitors of CD73 and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with CD73 inhibition, such as AIDS, autoimmune diseases, infections, atherosclerosis, and ischemia-reperfusion injury. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CD73 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
(FR) L'invention concerne des dérivés de benzothiadiazine substitués. L'invention concerne en particulier des composés de formule (I), dans lesquels R, R1, R2, R3, R4 et R5 sont tels que définis dans la description. Les composés de l'invention sont des inhibiteurs de CD73 et peuvent être utiles dans le traitement du cancer, de syndromes précancéreux et de maladies associées à l'inhibition de CD73, telles que le SIDA, les maladies auto-immunes, les infections, l'athérosclérose, et une lésion de reperfusion ischémique. Par conséquent, l'invention concerne en outre des compositions pharmaceutiques comprenant un composé de l'invention. L'invention concerne en outre des procédés d'inhibition de l'activité de CD73 et le traitement de troubles associés à celui-ci à l'aide d'un composé de l'invention ou d'une composition pharmaceutique comprenant un composé de l'invention.
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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, JP, KE, KG, 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 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: English (EN)
Filing Language: English (EN)