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1. (WO2018067423) BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS
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Pub. No.: WO/2018/067423 International Application No.: PCT/US2017/054688
Publication Date: 12.04.2018 International Filing Date: 02.10.2017
IPC:
C07D 333/60 (2006.01) ,C07D 409/12 (2006.01) ,C07D 498/04 (2006.01) ,A61K 31/381 (2006.01) ,A61K 31/385 (2006.01) ,A61K 31/424 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
333
Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
50
condensed with carbocyclic rings or ring systems
52
Benzo [b] thiophenes; Hydrogenated benzo [b] thiophenes
54
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
60
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
498
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
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
38
having sulfur as a ring hetero atom
381
having five-membered 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
38
having sulfur as a ring hetero atom
385
having two or more sulfur atoms in the same 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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
42
Oxazoles
424
condensed with heterocyclic ring systems, e.g. clavulanic acid
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
ALTMAN, Michael, D. [US/US]; US (US)
CASH, Brandon, D. [US/US]; US (US)
CHANG, Wonsuk [US/US]; US (US)
CUMMING, Jared, N. [US/US]; US (US)
HAIDLE, Andrew, M. [US/US]; US (US)
HENDERSON, Timothy, J. [US/US]; US (US)
JEWELL, James, P. [US/US]; US (US)
LARSEN, Matthew, A. [US/US]; US (US)
LIANG, Rui [US/US]; US (US)
LIM, Jongwon [US/US]; US (US)
LU, Min [CN/US]; US (US)
OTTE, Ryan, D. [US/US]; US (US)
SIU, Tony [US/US]; US (US)
TROTTER, Benjamin Wesley [US/US]; US (US)
TYAGARAJAN, Sriram [US/US]; US (US)
MERCK SHARP & DOHME CORP. [US/US]; 126 East Lincoln Avenue Rahway, New Jersey 07065-0907, US
Inventors:
ALTMAN, Michael, D.; US
CASH, Brandon, D.; US
CHANG, Wonsuk; US
CUMMING, Jared, N.; US
HAIDLE, Andrew, M.; US
HENDERSON, Timothy, J.; US
JEWELL, James, P.; US
LARSEN, Matthew, A.; US
LIANG, Rui; US
LIM, Jongwon; US
LU, Min; US
OTTE, Ryan, D.; US
SIU, Tony; US
TROTTER, Benjamin Wesley; US
TYAGARAJAN, Sriram; US
Common
Representative:
MERCK SHARP & DOHME CORP.; 126 East Lincoln Avenue Rahway, New Jersey 07065-0907, US
Priority Data:
62/404,06204.10.2016US
Title (EN) BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS
(FR) COMPOSÉS DE BENZO [ B ] THIOPHÈNE EN TANT QU'AGONISTES DE PIQÛRE
Abstract:
(EN) Compounds of general formula (la), compounds of general formula (la'), compounds of general formula (lb), compounds of general formula (lb'), compounds of general formula (I), compounds of general formula (Ι'), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, R6, R8, R9, X1, X2, and X3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds of the disclosure.
(FR) La présente invention concerne des composés de formule générale (la), des composés de formule générale (la'), des composés de formule générale (lb), des composés de formule générale (lb'), des composés de formule générale (I), des composés de formule générale (I'), et leurs sels pharmaceutiquement acceptables, où R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 8 , R 9 , X 1 , X 2 , et X 3 sont définis dans la description, qui peuvent être utiles en tant qu'inducteurs de la production d'interféron de type I, spécifiquement en tant qu'agents actifs STING. L'invention concerne également des procédés pour la synthèse et l'utilisation de ces composés.
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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)