Title:
1,2,4-オキサジアゾール誘導体およびそれらの治療的使用
Document Type and Number:
Japanese Patent JP2012513958
Kind Code:
A
Abstract:
New derivatives of general formula (I), or pharmaceutically acceptable salts or N-oxides thereof wherein,
A is selected from the group consisting of -N-, -O- and -S-;
B and C are independently selected from the group consisting of-N- and -O-, with the proviso that at least two of A, B and C are nitrogen atoms;
G 1 is selected from the group consisting of -CH 2 -, -NH- and -O-;
G 2 is selected from the group consisting of -NR 4 - and -O-;
R 1 represents:
¢ a 8 to 10 membered bicyclic N-containing heteroaryl group optionally substituted with a C 1-4 carboxyalkyl group or a C 1-4 aminoalkyl group,
¢ a pyridyl group optionally substituted with one or more substituents selected from hydroxy groups, C 1-4 alkyl groups, C 1-4 carboxyalkyl groups, C 1-4 haloalkyl groups, C 1-4 alkoxy groups, amino groups, C 1-4 aminoalkyl groups and C 1-4 aminoalkoxy groups,
¢ a pyridone group substituted with one or more C 1-4 alkyl groups; C 1-4 haloalkyl groups or C 1-4 aminoalkyl groups, or
¢ a group of formula:
wherein:
¢ R a represents a hydrogen atom, a halogen atom, a C 1-4 alkyl group, C 3-4 cycloalkyl group or a -CF 3 group;
¢ R b represents a hydrogen atom, a halogen atom, a C 14 alkyl group, a -CF 3 group or a C 1-4 alkoxy group;
¢ R d represents a hydrogen atom, a C 1-4 alkyl group or a C 1-4 alkoxy group;
¢ R c represents:
a hydrogen atom, a C 1-4 hydroxyalkyl group, a C 1-4 aminoalkyl group which is optionally substituted with one or more substituents selected from halogen atoms, hydroxy groups and -CF 3 groups;
a 4 to 6-membered saturated N-containing heterocyclic ring optionally substituted with a C 1-2 carboxyalkyl group;
-(CH 2 ) (0-4) -C(O)OR', -(CH 2 ) (0-4) -C(O)NR'R", -(CH 2 ) (0-4) -NHC(O)R", -S(O) 2 NR'R", -O-(CH 2 ) (2-4) NR'R", -O-(CH 2 ) (1-4) C(O)OR", -O-(CH 2 ) (1-4) -C(O)NR'R", -(CH 2 ) (0-4) -NR'R", -(CH 2 ) (0-4) -CONHS(O) 2 R', -(CH 2 ) (0-4) -NHS(O) 2 R' or -(CH 2 ) (0-3) -N H-(CH 2 ) (1-3) -(NH) (0-1) S(O) 2 R' wherein,
R' represents a hydrogen atom or a C 1-4 alkyl group,
R" represents a hydrogen atom, a C 1-4 alkyl group, a C 3-4 cycloalkyl group, a C 1-4 carboxyalkyl group, a C 1-4 haloalkyl group, a C 1-4 hydroxyalkyl group or a 6 membered, saturated N-containing heterocyclic ring, or
R' and R" together with the nitrogen atom to which they are attached from a 4 to 6 membered heterocyclic group which contains, as heteroatoms, one N atom and, optionally, one further atom selected from N and O, and which is optionally substituted with a carboxy or a C 1-4 carboxyalkyl group,
or R c together with R d form a C 5-6 cycloalkyl group optionally substituted by a -NHR f group, wherein R f is selected from the group consisting of a hydrogen atom and a carboxymethyl group;
R 2 and R 3 are independently selected from the group consisting of hydrogen atoms, halogen atoms and C 1-4 alkyl groups; and
R 4 is selected from the group consisting of a hydrogen atom, a phenyl group, a C 3-4 cycloalkyl-C 1-4 alkyl group, C 1-4 aminoalkyl group, C 1-4 haloalkyl group and a linear or branched C 1-4 alkyl group which is optionally substituted by a phenyl or a pyridyl group.
Inventors:
Victor Giulio Matassa
Nuria Aguilar Isquierdo
Malta Mill Sepeda
Marta Callaskar Liera
Sylvia Fonquerna Pou
Aransas Caldus Figueras
Julio Cesar Castro Palomino Laria
Montserrat Ella Sora
Nuria Aguilar Isquierdo
Malta Mill Sepeda
Marta Callaskar Liera
Sylvia Fonquerna Pou
Aransas Caldus Figueras
Julio Cesar Castro Palomino Laria
Montserrat Ella Sora
Application Number:
JP2011542702A
Publication Date:
June 21, 2012
Filing Date:
December 15, 2009
Export Citation:
Assignee:
Almirall, S.A.
International Classes:
C07D401/14; A61K31/4245; A61K31/4439; A61K31/454; A61K31/496; A61K31/5377; A61K45/00; A61P1/04; A61P9/00; A61P11/06; A61P17/06; A61P19/02; A61P25/00; A61P25/04; A61P29/00; A61P31/04; A61P31/12; A61P35/00; A61P37/02; A61P37/06; A61P43/00; C07D413/04; C07D413/14; C07D417/04; C07D471/04; C07D491/052
Attorney, Agent or Firm:
Aoyama Aoi
Takuji Yamada
Michiko Matsutani
Mitsutaka Iwasaki
Yasushi Ochiai
Takuji Yamada
Michiko Matsutani
Mitsutaka Iwasaki
Yasushi Ochiai