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1. (WO2017216025) MPS-1 INHIBITORS
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Pub. No.: WO/2017/216025 International Application No.: PCT/EP2017/063927
Publication Date: 21.12.2017 International Filing Date: 08.06.2017
IPC:
C07D 471/04 (2006.01) ,A61K 31/437 (2006.01) ,A61P 35/00 (2006.01)
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
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:
BAYER PHARMA AKTIENGESELLSCHAFT [DE/DE]; Müllerstr. 178 13353 Berlin, DE
Inventors:
PAULSEN, Holger; DE
BOEHMER, Lars; DE
BECKER, Guido; DE
ZÖLLER, Thomas; DE
BIERER, Donald; DE
OLENIK, Britta; DE
DWORACEK, Sylvia; DE
MUENSTER, Uwe; DE
STEIN, Sven; DE
HOLKENJANS, Wiebke; DE
HUCKE, Frank; DE
Agent:
BIP PATENTS; Alfred-Nobel-Str. 10 40789 Monheim am Rhein NRW, DE
Priority Data:
16174563.315.06.2016EP
Title (EN) MPS-1 INHIBITORS
(FR) INHIBITEURS DE MPS-1
Abstract:
(EN) The present invention covers crystalline, anhydrous (2R)-2-(4-fluorophenyl)-N-[4-(2-{[2- methoxy-4-(methylsulfonyl)phenyl]amino}[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]propan- amide 4-toluenesulfonate, and crystalline (2R)-2-(4-fluorophenyl)-N-[4-(2-{[2-methoxy-4- (methylsulfonyl)phenyl]amino}[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]propanamide 4- toluenesulfonate monohydrate, as compounds per se, a method of preparing said crystalline, anhydrous compound, pharmaceutical compositions and pharmaceutical combinations comprising said crystalline, anhydrous compound, and uses of said crystalline, anhydrous compound in the treatment or prophylaxis of a cancer, in particular pancreatic cancer, glioblastoma, ovarian cancer, non-small cell lung carcinoma, breast cancer, and/or gastric cancer.
(FR) La présente invention concerne le (2R)-2-(4-fluorophényl)-N-[4-(2-{[2- méthoxy-4-(méthylsulfonyl)phényl]amino}[1,2,4]triazolo[1,5-a]pyridin-6-yl)phényl]propan-amide 4-toluènesulfonate anhydre, cristallin, et le (2R)-2-(4-fluorophényl)-N-[4-(2-{[2-méthoxy-4- (méthylsulfonyl)phényl]amino}[1,2,4]triazolo[1,5-a]pyridin-6-yl)phényl]propanamide 4-toluènesulfonate monohydraté cristallin, en tant que composés en soi, un procédé de préparation dudit composé anhydre cristallin, des compositions pharmaceutiques et des combinaisons pharmaceutiques comprenant ledit composé anhydre cristallin, et des utilisations dudit composé anhydre cristallin dans le traitement ou la prophylaxie d'un cancer, notamment le cancer du pancréas, le glioblastome, le cancer de l'ovaire, le carcinome du poumon non à petites cellules, le cancer du sein et/ou le cancer de l'estomac.
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, 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)