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1. WO2002022587 - PYRIDAZINONES AND TRIAZINONES AND MEDICINAL USE THEREOF

Publication Number WO/2002/022587
Publication Date 21.03.2002
International Application No. PCT/JP2001/008058
International Filing Date 17.09.2001
Chapter 2 Demand Filed 26.02.2002
IPC
C07D 237/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
237Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
02not condensed with other rings
06having three double bonds between ring members or between ring members and non-ring members
10with 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 to ring carbon atoms
14Oxygen atoms
C07D 237/24 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
237Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
02not condensed with other rings
06having three double bonds between ring members or between ring members and non-ring members
10with 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 to ring carbon atoms
24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 401/04 2006.01
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
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
C07D 491/04 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
CPC
A61P 1/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
A61P 1/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
08for nausea, cinetosis or vertigo; Antiemetics
A61P 1/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
12Antidiarrhoeals
A61P 13/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
A61P 13/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
02of urine or of the urinary tract, e.g. urine acidifiers
A61P 21/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
21Drugs for disorders of the muscular or neuromuscular system
Applicants
  • EISAI CO., LTD. [JP]/[JP] (AllExceptUS)
  • NAGATO, Satoshi [JP]/[JP] (UsOnly)
  • KAWANO, Koki [JP]/[JP] (UsOnly)
  • ITO, Koichi [JP]/[JP] (UsOnly)
  • NORIMINE, Yoshihiko [JP]/[JP] (UsOnly)
  • UENO, Kohshi [JP]/[JP] (UsOnly)
  • HANADA, Takahisa [JP]/[JP] (UsOnly)
  • AMINO, Hiroyuki [JP]/[JP] (UsOnly)
  • OGO, Makoto [JP]/[JP] (UsOnly)
  • HATAKEYAMA, Shinji [JP]/[JP] (UsOnly)
  • UENO, Masataka [JP]/[JP] (UsOnly)
  • GROOM, Anthony, John [GB]/[GB] (UsOnly)
  • RIVERS, Leanne [GB]/[GB] (UsOnly)
  • SMITH, Terence [GB]/[GB] (UsOnly)
Inventors
  • NAGATO, Satoshi
  • KAWANO, Koki
  • ITO, Koichi
  • NORIMINE, Yoshihiko
  • UENO, Kohshi
  • HANADA, Takahisa
  • AMINO, Hiroyuki
  • OGO, Makoto
  • HATAKEYAMA, Shinji
  • UENO, Masataka
  • GROOM, Anthony, John
  • RIVERS, Leanne
  • SMITH, Terence
Agents
  • FURUYA, Kaoru
Priority Data
0102822.405.02.2001GB
0102824.005.02.2001GB
2000-28263618.09.2000JP
2000-28941222.09.2000JP
2000-34261409.11.2000JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) PYRIDAZINONES AND TRIAZINONES AND MEDICINAL USE THEREOF
(FR) PYRIDAZINONES ET TRIAZINONES AINSI QUE LEUR UTILISATION MEDICALE
Abstract
(EN)
Provided are novel compounds exhibiting excellent inhibitory activities against AMPA receptor and/or kainate receptor, i.e., compounds of the general formula (I), salts thereof, or hydrates of both wherein A1, A2 and A3 are each independently C3-8 cycloalkyl, C3-8 cycloalkenyl, a 5- to 14-membered nonoaromatic heterocyclic group, a C6-14 aromatic carbocyclic group, or a 5- to 14-membered aromatic heterocyclic group, any of which may be substituted; Q is O, S, or NH; Z is C or N; X1, X2 and X3 are each independently a single bond, optionally substituted C1-6 alkylene, optionally substituted C2-6 alkenylene, optionally substituted C2-6 alkynylene, -NH-, -O-, -NHCO-, -CONH-, -SO0-2-, or the like; R1 and R2 are each independently hydrogen or optionally substituted C1-6 alkyl, or alternatively R1 and R2 may be united in such a way that CR2-ZR1 forms C=C; and R3 is hydrogen, optionally substituted C1-6 alkyl, or the like, or alternatively R3 may unite with any atom on the ring A1 or A3 to form together with the atom an optionally substituted C5-8 carbocycle or an optionally substituted 5- to 8-membered heterocycle.
(FR)
L'invention concerne de nouveaux composés ayant d'excellentes activités inhibitrices contre le récepteur AMPA et/ou le récepteur du kainate, notamment les composés de la formule (I), leurs sels ou hydrates ou bien les deux. Dans la formule (I), A1, A2 et A3 représentent indépendamment cycloalkyle C3-8, cycloalcényle C3-8, un groupe hétérocyclique monoaromatique de 5 à 14 chaînons, un groupe carbocyclique aromatique C6-14, ou un groupe hétérocyclique aromatique de 5 à 14 chainons, chacun d'entre eux pouvant être substitué ; Q représente un oxygène, un soufre ou NH ; Z représente C ou N ; X1, X2 et X3 représentent respectivement et indépendamment une liaison simple, alkylène C1-6 éventuellement substitué, alcénylène C2-6 éventuellement substitué, alkynylène C2-6 éventuellement substitué, -NH-, -O-, -NHCO-, -CONH-, -SO0-2-, ou équivalent ; R1 et R2 représentent indépendamment un hydrogène ou alkyle C1-6 éventuellement substitué, ou en variante R1 et R2 peuvent être réunis de telle façon que CR2-ZR1 forme C=C ; et R3 représente un hydrogène, alkyle C1-6 éventuellement substitué ou équivalent, ou en variante R3 peut s'unir avec n'importe quel atome du cycle A1 ou A3 pour former un carbocycle C5-8 éventuellement substitué ou un hétérocycle de 5 à 8 chainons éventuellement substitué.
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