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1. WO2017216025 - MPS-1 INHIBITORS

Publication Number WO/2017/216025
Publication Date 21.12.2017
International Application No. PCT/EP2017/063927
International Filing Date 08.06.2017
IPC
C07D 471/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic 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
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/437 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic 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 C07D451/00 - C07D463/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • BAYER PHARMA AKTIENGESELLSCHAFT [DE]/[DE]
Inventors
  • PAULSEN, Holger
  • BOEHMER, Lars
  • BECKER, Guido
  • ZÖLLER, Thomas
  • BIERER, Donald
  • OLENIK, Britta
  • DWORACEK, Sylvia
  • MUENSTER, Uwe
  • STEIN, Sven
  • HOLKENJANS, Wiebke
  • HUCKE, Frank
Agents
  • BIP PATENTS
Priority Data
16174563.315.06.2016EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
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.
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