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1. (IN4908/DELNP/2011) 1, 2, 4-OXADIAZOLE DERIVATIVES AND THEIR THERAPEUTIC USE

Office : India
Application Number: 4908/DELNP/2011 Application Date: 27.06.2011
Publication Number: 4908/DELNP/2011 Publication Date: 20.04.2012
Publication Kind : A
Prior PCT appl.: Application Number:PCTEP09008968 ; Publication Number:WO2010072352 Click to see the data
IPC:
C07D 41/04
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
41
Heterocyclic compounds containing one or more rings each consisting of 1 nitrogen atom and more than 5 carbon atoms
02
Hexamethylenimines
04
Substituted hexamethylenimines
Applicants: ALMIRALL, S.A.
Inventors: VICTOR GIULIO MATASSA
NURIA AGUILAR IZQUIERDO
MARTA MIRCEPEDA
MARTA CARRASCAL RIERA
SILVIA FONQUERNA POU
ARANZAZU CARDUS FIGUERAS
JULIO CESAR CASTRO PALOMINO LARIA
MONTSERRAT ERRA SOLA
Priority Data:
Title: (EN) 1, 2, 4-OXADIAZOLE DERIVATIVES AND THEIR THERAPEUTIC USE
Abstract:
(EN) Formula (I)New derivatives of general formula (I), or pharmaceutically acceptable salts or N-oxides thereof wherein,either (i) 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 -0-, with the proviso that two of A, B and C are nitrogen atoms, or (ii) two of A, B and C are -N- and one of A, B and C is -NH-;G1 is selected from the group consisting of-CH2-, -NH- and -0-;G2 is selected from the group consisting of-NR4- and -0-;R1 represents: a 8 to 10 membered bicyclic N-containing heteroaryl group optionally substituted with a C1-4 carboxyalkyl group or a C1-4 aminoalkyl group, a pyridyl group optionally substituted with one or more substituents selected from hydroxy groups, C1-4 alkyl groups, C1-4 carboxyalkyl groups, C1-4 haloalkyl groups, C1-4 alkoxy groups, amino groups, C1-4 aminoalkyl groups and C1-4 aminoalkoxy groups, a pyridone group substituted with one or more C1-4 alkyl groups; C1-4 haloalkyl groups or C1-4 aminoalkyl groups, or a group of formula:wherein:• Ra represents a hydrogen atom, a halogen atom, a C14 alkyl group, C3-4 cycloalkyl group or a -CF3 group;• Rb represents a hydrogen atom, a halogen atom, a C1-4 alkyl group, a -CF3 group or a C1-4 alkoxy group;• Rd represents a hydrogen atom, a C1-4 alkyl group or a C1-4 alkoxy group;• Rc represents:o a hydrogen atom, a C1-4 hydroxyalkyl group, a C1-4 aminoalkyl group which is optionally substituted with one or more substituents selected from halogen atoms, hydroxy groups and -CF3 groups;o a 4 to 6-membered saturated N-containing heterocyclic ring optionally substituted with a C1-2 carboxyalkyl group;o -(CH2)(0-4)-C(O)OR", -(CH2)(0-4)-C(O)NR"R", -(CH2)(0-4)-NHC(0)R", -S(0)2NR"R", -0-(CH2)(2-4)NR"R", -0-(CH2)(1-4)-C(0)OR", -0-(CH2)(1-4)-C(0)NR"R", -(CH2)(0-4)-NR"R", -(CH2)(0-4)-CONHS(O)2R", -(CH2)(0-4)-NHS(0)2R" or-(CH2)(0-3)-NH-(CH2)(1-3)-(NH)(0-1)S(0)2R" wherein,■ R" represents a hydrogen atom or a C1-4 alkyl group,■ R" represents a hydrogen atom, a C1-4 alkyl group, a C3-4 cycloalkyl group, a C1-4 carboxyalkyl group, a C1-4 haloalkyl group, a C1-4 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 form 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 C1-4 carboxyalkyl group,or Rc together with Rd form a C5-6 cycloalkyl group optionally substituted by a -NHRf group, wherein Rf is selected from the group consisting of a hydrogen atom and a carboxymethyl group;R2 and R3 are independently selected from the group consisting of hydrogen atoms, halogen atoms and C1-4 alkyl groups; andR4 is selected from the group consisting of a hydrogen atom, a phenyl group, a C3-4 cycloalkyl-C1-4 alkyl group, C1-4 aminoalkyl group, C1-4 haloalkyl group and a linear or branched C1-4 alkyl group which is optionally substituted by a phenyl or a pyridyl group.
Also published as:
NZ592798UAa201109217IL213168EP2370431MXMX/a/2011/006505SG172152
JP2012513958US20110311485CN102264731CA2748397EA201100975KR1020110104075
BRPI0918194AU2009331959VN28274ID2012/01220MYPI 2011002991WO/2010/072352