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1. WO2020142486 - KINASE INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE

Publication Number WO/2020/142486
Publication Date 09.07.2020
International Application No. PCT/US2019/069059
International Filing Date 31.12.2019
IPC
A61K 31/4184 2006.1
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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41641,3-Diazoles
4184condensed with carbocyclic rings, e.g. benzimidazoles
C07D 209/34 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
30with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
32Oxygen atoms
34in position 2
C07D 235/26 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
235Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02condensed with carbocyclic rings or ring systems
04Benzimidazoles; Hydrogenated benzimidazoles
24with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
26Oxygen atoms
CPC
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 3/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
A61P 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
C07D 401/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic 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
14containing three or more hetero rings
C07D 403/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
02containing two hetero rings
04directly linked by a ring-member-to-ring-member bond
Applicants
  • ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI [US]/[US]
Inventors
  • DEVITA, Robert, J.
  • STEWART, Andrew, F.
  • SUEBSUWONG, Chalada
  • KUMAR, Kunal
  • WANG, Peng
  • SANCHEZ, Roberto, J.
  • WANG, Hui
Agents
  • TISCHNER, Tate, L.
  • MERKEL, Edwin, V.
  • GOLDMAN, Michael, L.
  • O'GARA, Megan, T.
  • JONES, Shelley, A.
Priority Data
62/786,99131.12.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) KINASE INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE
(FR) COMPOSÉS INHIBITEURS DE KINASE, COMPOSITIONS ET MÉTHODES D'UTILISATION
Abstract
(EN)
Disclosed are kinase inhibitor compounds having the following structure: (I), or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where R1, R2, R3,R4, R5, R6, N-Ar, X, Y, Z, and AA are as defined herein. Also disclosed are compositions containing the kinase inhibitor compounds, methods of inhibiting activity of a kinase in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.
(FR)
L'invention concerne des composés inhibiteurs de kinase ayant la structure suivante : (I), ou un stéréoisomère, un sel, un oxyde ou un solvate pharmaceutiquement acceptable de celui-ci, où R1, R2, R3, R4, R5, R6, N-Ar, X, Y, Z, et AA sont tels que définis dans la description. L'invention concerne également des compositions contenant les composés inhibiteurs de kinase, des méthodes d'inhibition de l'activité d'une kinase dans une cellule, des méthodes d'augmentation de la prolifération cellulaire dans une population de cellules bêta pancréatiques, des méthodes de traitement d'un sujet présentant un état associé à une sécrétion insuffisante d'insuline, et des méthodes de traitement d'un sujet présentant un trouble neurologique.
Also published as
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