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1. WO2011009897 - FUSED AMINODIHYDROPYRIMIDONE DERIVATIVES

Publication Number WO/2011/009897
Publication Date 27.01.2011
International Application No. PCT/EP2010/060586
International Filing Date 21.07.2010
IPC
C07D 491/048 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
044with only one oxygen atom as ring hetero atom in the oxygen-containing ring
048the oxygen-containing ring being five-membered
A61K 31/522 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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
52Purines, e.g. adenine
522having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61P 25/28 2006.01
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
CPC
C07D 491/048
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
044with only one oxygen atom as ring hetero atom in the oxygen-containing ring
048the oxygen-containing ring being five-membered
Applicants
  • EISAI R&D MANAGEMENT CO., LTD [JP]/[JP] (AllExceptUS)
  • CASTRO PINEIRO, Jose, Luis [ES]/[GB] (UsOnly)
  • HALL, Adrian [GB]/[GB] (UsOnly)
  • MADIN, Andrew [GB]/[GB] (UsOnly)
  • VO, Ngoc-Tri [FR]/[GB] (UsOnly)
Inventors
  • CASTRO PINEIRO, Jose, Luis
  • HALL, Adrian
  • MADIN, Andrew
  • VO, Ngoc-Tri
Agents
  • CROOKS, Elizabeth, Caroline
Priority Data
0912777.022.07.2009GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) FUSED AMINODIHYDROPYRIMIDONE DERIVATIVES
(FR) DÉRIVÉS D'AMINODIHYDROPYRIMIDONE CONDENSÉE
Abstract
(EN)
A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is -NReCO- or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1, R2 and Rx are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
(FR)
La présente invention concerne un composé représenté par la formule générale (I) : ou un sel pharmaceutiquement acceptable de celui-ci ou un solvate de celui-ci, dans lequel le cycle A est un groupe aryle en C6-14 ou similaire, L est -NReCO- ou similaire (dans lequel Re est un atome d'hydrogène ou similaire), le cycle B est un groupe aryle en C6-14 ou similaire, X est un groupe alkylène en C1-3 ou similaire, Y est une liaison simple ou similaire, Z est un groupe alkylène en C1-3 ou similaire, R1, R2 et Rx sont chacun indépendamment un atome d'hydrogène ou similaire, et R3, R4, R5 et R6 sont indépendamment un atome d'hydrogène, un atome d'halogène ou similaire, qui a un effet inhibiteur de production de Aβ ou un effet inhibiteur de BACE1 et qui est utile en tant qu'agent prophylactique ou thérapeutique pour une maladie neurodégénérative causée par Aβ et typifiée par la démence de type Alzheimer.
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