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1. (WO2019049061) 5-(1 H-BENZO[D]IMIDAZO-2-YL)-PYRIDIN-2-AMINE AND 5-(3H-IMIDAZO[4,5-B]PYRIDIN-6-YL)-PYRIDIN-2-AMINE DERIVATIVES AS C-MYC AND P300/CBP HISTONE ACETYLTRANSFERASE INHIBITORS FOR TREATING CANCER
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Pub. No.: WO/2019/049061 International Application No.: PCT/IB2018/056806
Publication Date: 14.03.2019 International Filing Date: 06.09.2018
IPC:
C07D 401/04 (2006.01) ,C07D 471/04 (2006.01) ,A61K 31/4439 (2006.01) ,A61K 31/437 (2006.01) ,A61P 35/00 (2006.01)
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
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
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
4427
containing further heterocyclic ring systems
4439
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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
4353
ortho- or peri-condensed with heterocyclic ring systems
437
the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED [GB/GB]; 980 Great West Road Brentford Middlesex TW89GS, GB
Inventors:
MEDINA, Jesus Raul; US
TIAN, Xinrong; US
NG DI MARCO, Christina; US
GRAYBILL, Todd L.; US
HEERDING, Dirk A.; US
LI, William Hoi Hong; US
MANGATT, Biju; US
MARTYR, Cuthbert D.; US
RIVERO, Raphael Anthony; US
Priority Data:
62/555,16407.09.2017US
62/587,00416.11.2017US
Title (EN) 5-(1 H-BENZO[D]IMIDAZO-2-YL)-PYRIDIN-2-AMINE AND 5-(3H-IMIDAZO[4,5-B]PYRIDIN-6-YL)-PYRIDIN-2-AMINE DERIVATIVES AS C-MYC AND P300/CBP HISTONE ACETYLTRANSFERASE INHIBITORS FOR TREATING CANCER
(FR) DÉRIVÉS DE 5-(1 H-BENZO[D]IMIDAZO-2-YL)-PYRIDIN-2-AMINE ET DE 5-(3H-IMIDAZO[4,5-B]PYRIDIN-6-YL)-PYRIDIN-2-AMINE UTILISÉS EN TANT QU'INHIBITEURS D'HISTONE ACÉTYLTRANSFÉRASE DE C-MYC ET P300/CBP POUR LE TRAITEMENT DU CANCER
Abstract:
(EN) The invention is directed to substituted 5-(1H-benzo[d]imidazo-2-yl)- pyridin-2-amine and 5-(3H-imidazo[4,5-b]pyridin-6-yl)-pyridin-2-amine derivatives. Specifically, the invention is directed to compounds according to Formula (lb) wherein R', R2', R3', R4', Rs', R6', R7', and X1' are as defined herein; or a salt thereof including a pharmaceutically acceptable salt thereof. The compounds of the invention decrease MYC protein (c-MYC) in cells and/or inhibit p300/CBP histone acetyltransferase and can be useful in the treatment of cardiac hypertrophy, diabetes, obesity & nonalcoholic fatty liver disease, HIV, polycystic kidney disease, inflammatory diseases, ankylosing spondylitis, psoriasis, psoriatic arthritis, rheumatoid arthritis, Crohn's disease, multiple sclerosis, cancer and pre-cancerous syndromes, and diseases associated with dysregulation of Myc or inhibition of p300/CBP histone acetyltransferase. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention still further discloses methods of reducing MYC protein (c-MYC) in cells and inhibiting p300/CBP histone acetyltransferase 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 5-(1H-benzo[d]imidazo-2-yl)- pyridin-2-amine et de 5-(3H-imidazo[4,5-b]pyridin-6-yl)-pyridin-2-amine substitués. En particulier, l'invention concerne des composés représentés par la formule (lb) dans laquelle R', R2', R3', R4', Rs', R6', R7' et X1' sont tels que définis dans la description; ou un sel de ceux-ci, y compris un sel pharmaceutiquement acceptable de ceux-ci. Les composés selon l'invention permettent de réduire la protéine MYC (c-MYC) dans des cellules et/ou inhibent l'histone acétyltransférase p300/CBP et peuvent être utiles dans le traitement de l'hypertrophie cardiaque, du diabète, de l'obésité, de la stéatose hépatique non alcoolique, du VIH, de la polykystose rénale, de maladies inflammatoires, de la spondylarthrite ankylosante, du psoriasis, de l'arthrite psoriasique, de la polyarthrite rhumatoïde, de la maladie de Crohn, de la sclérose en plaques, du cancer et des syndromes précancéreux, ainsi que de maladies associées à un dérèglement de Myc ou à l'inhibition de l'histone acétyltransférase p300/CBP. Par conséquent, l'invention concerne également des compositions pharmaceutiques comprenant un composé selon l'invention. L'invention concerne par ailleurs des procédés permettant de réduire la protéine MYC (c-MYC) dans des cellules et d'inhiber l'activité de l'histone acétyltransférase p300/CBP, l'invention concerne également le traitement de troubles apparentés au moyen d'un composé selon l'invention ou d'une composition pharmaceutique comprenant un composé fourni par la présente 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, 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)