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1. (WO2018198077) 6-6 FUSED BICYCLIC HETEROARYL COMPOUNDS AND THEIR USE AS LATS INHIBITORS
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Pub. No.: WO/2018/198077 International Application No.: PCT/IB2018/052919
Publication Date: 01.11.2018 International Filing Date: 26.04.2018
IPC:
C07D 487/04 (2006.01) ,C07D 519/00 (2006.01) ,A61K 35/30 (2015.01) ,C12N 5/079 (2010.01) ,A61P 17/02 (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
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
519
Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/ or C07D455/257
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
35
Medicinal preparations containing material or reaction products thereof with undetermined constitution
12
Materials from mammals or birds
30
Nerves; Brain
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
N
MICRO-ORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICRO-ORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
5
Undifferentiated human, animal or plant cells, e.g. cell lines; Tissues; Cultivation or maintenance thereof; Culture media therefor
07
Animal cells or tissues
071
Vertebrate cells or tissues, e.g. human cells or tissues
079
Neural cells
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17
Drugs for dermatological disorders
02
for treating wounds, ulcers, burns, scars, keloids, or the like
Applicants:
NOVARTIS AG [CH/CH]; Lichtstrasse 35 4056 Basel, CH
Inventors:
BEHNKE, Dirk; CH
BERENSHTEYN, Frada; US
HAO, Xueshi; US
HOFFMAN, Timothy; US
JIN, Qihui; US
LACOSTE, Arnaud; US
LEE, Cameron; US
LIU, Jun; US
LIU, Yahu; US
MAIBAUM, Juergen Klaus; CH
MO, Tingting; US
PAN, Jianfeng; US
QU, Xin; US
TCHORZ, Jan; CH
XIE, Yun Feng; US
YAN, Shanshan; US
ZOU, Yefen; US
Priority Data:
62/491,47528.04.2017US
62/491,48428.04.2017US
62/491,52628.04.2017US
62/491,57328.04.2017US
62/650,23229.03.2018US
Title (EN) 6-6 FUSED BICYCLIC HETEROARYL COMPOUNDS AND THEIR USE AS LATS INHIBITORS
(FR) COMPOSÉS HÉTÉROARYLE BICYCLIQUES FUSIONNÉS EN 6-6 ET LEUR UTILISATION COMME INHIBITEURS DE LATS
Abstract:
(EN) The present invention is related to 6-6 Fused Bicyclic Heteroaryl Compounds of the Formula A2 or A1 and their Use as LATS Inhibitors, or a salt, stereoisomer or pharmaceutical composition thereof; wherein the variables are as defined herein (A1 & A2). The present invention further relates to a method of LATS inhibition in a cell population using a compound of Formula A1, or a salt, stereoisomer or pharmaceutical composition thereof. The present invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, their use in the treatment and management of diseases or disorders.
(FR) L'invention concerne des composés hétéroaryle bicycliques fusionnés en 6-6, représentés par la formule A2 ou A1, et leur utilisation comme inhibiteurs de LATS, ou un sel, un stéréoisomère ou une composition pharmaceutique de ceux-ci; les variables étant telles que définies dans la description (A1 et A2). Elle concerne également une méthode d'inhibition de LATS dans une population cellulaire, au moyen d'un composé de formule A1, ou d'un sel, d'un stéréoisomère ou d'une composition pharmaceutique de celui-ci. L'invention concerne également un procédé de production de composés de l'invention, et leurs utilisations thérapeutiques. Elle concerne en outre des méthodes se rapportant à leur préparation, à leur utilisation médicale et leur utilisation dans le traitement et la gestion de maladies ou troubles.
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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)