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US 2003/0149047 A1Published application
Novel compounds
AssigneeAstraZeneca AB
InventorsTomas Eriksson, Peter Hansen, Martin Hemmerling, Krister Henriksson, Tomas Klingstedt, Lars Pettersson, Michael Bodkin
Life of this patent
Estimating the term…
Abstract
The invention provides compounds of general formula (I) wherein Q, R, R1, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
Claims19
A compound of general formula
- 22
- wherein,
- R represents a group
- 23
- m is 0, 1, 2 or 3;
- each R1 independently represents halogen, cyano, nitro, carboxyl, hydroxyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkoxycarbonyl, C1-C6 haloalkyl, CL-C6 haloalkoxy, —NR9R10, C3-C6 cycloalkylamino, C1-C6alkylthio, C1-C6 alkylcarbonyl, C1-C6 alkylcarbonylamino, sulphonamido, C1-C6 alkylsulphonyl, —C(O)NR11R12, —NR13C(O)—(NH)pR14, phenyl, or C1-C6 alkyl optionally substituted by carboxyl or C1-C6 alkoxycarbonyl;
- p is 0 or 1;
- X represents an oxygen or sulphur atom or a CH2, CH(CH3), OCH2, CH2O, CH2NH, NH or carbonyl group and Y represents a nitrogen atom or a CH or C(OH) group, provided that when X represents an oxygen or sulphur atom or a CH2O, CH2NH or NH group, then Y represents a CH group;
- Z1 represents a bond or a group (CH2)q where q is 1 or 2;
- Z2 represents a bond or a group CH2, with the proviso that Z1 and Z2 do not both simultaneously represent a bond;
- Q represents an oxygen or sulphur atom or a group CH2 or NH;
- R2 represents a group
- 24
- n is 0, 1 or 2;
- each R3 independently represents a C1-C6 alkyl, C1-C6 alkoxycarbonyl, —CH2OH or carboxyl group;
- R4, R5, R6 and R7 each independently represent a hydrogen atom or a C1-C6 alkyl group, or R4, R5, R6 and R7 together represent a C1-C4 alkylene chain linking the two carbon atoms to which they are attached to form a 4- to 7-membered saturated carbocycle, or R5, R6 and R7 each represent a hydrogen atom and R4 and R8 together with the carbon atoms to which they are attached form a 5- to 6-membered saturated carbocycle;
- R8 represents a hydrogen atom, a C1-C6 alkyl group or is linked to R4 as defined above;
- R9 and R10 each independently represent a hydrogen atom or a C1-C6 alkyl group, or R9 and R10 together with the nitrogen atom to which they are attached form a 4- to 7-membered saturated heterocycle;
- R11 and R12 each independently represent a hydrogen atom or a C1-C6 alkyl group optionally substituted by C1-C6 alkoxycarbonyl;
- R13 represents a hydrogen atom or a C1-C6 alkyl group;
- R14 represents a hydrogen atom, or a C1-C6 alkyl group optionally substituted by carboxyl, C1-C6 alkoxy or C1-C6 alkoxycarbonyl;
- R15 is represents carboxyl, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, C1-C6 alkoxycarbonylC1-C6 alkyl or a group —NR17R18, —NHSO2CH3, —NHC(O)CH3, —C(O)NR17R18, —NHC(O)NR17R18, —OC(O)NR17R18, OCH2C(O)NR17R18, —NHC(O)OR17′ or —OR17″;
- t is 0, 1, 2 or 3;
- each R16 independently represents halogen, cyano, nitro, carboxyl, hydroxyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkoxycarbonyl, C1-C6 haloalkyl, C1-C6 haloalkoxy, —NR19R20, C3-C6 cycloalkylamino, C1-C6 alkylthio, C1-C6 alkylcarbonyl, C1-C6 alkylcarbonylamino, sulphonamido (—SO2NH2), C1-C6 alkylsulphonyl, —C(O)NR21R22, —NR23C(O)(NH)vR24, phenyl, or C1-C6 alkyl optionally substituted by carboxyl or C1-C6 alkoxycarbonyl;
- R17 and R18 each independently represent (i) a hydrogen atom, (ii) a 5- to 6-membered saturated or unsaturated ring which may comprise at least one heteroatom chosen from nitrogen, oxygen and sulphur, the ring being optionally substituted with at least one substituent selected from halogen, methyl and trifluoromethyl, or (iii) a C1-C6 alkyl group optionally substituted by at least one substituent selected from halogen, trifluoromethyl, carboxyl, C1-C6 alkoxycarbonyl and a 5- to 6-membered saturated or unsaturated ring which may comprise at least one heteroatom chosen from nitrogen, oxygen and sulphur, the ring being optionally substituted with at least one is substituent selected from halogen, methyl and trifluoromethyl, or
- R17 and R18 together with the nitrogen atom to which they are attached form a 4- to 7-membered saturated heterocycle;
- R17′ represents a hydrogen atom, or a C1-C6 alkyl group optionally substituted by carboxyl or C1-C6 alkoxycarbonyl;
- R17″ is defined as for R17 above except that R17″ does not represent a hydrogen atom;
- R19 and R20 each independently represent a hydrogen atom or a C1-C6 alkyl group, or R19 and R20 together with the nitrogen atom to which they are attached form a 4- to 7-membered saturated heterocycle;
- R21 and R22 each independently represent a hydrogen atom or a C1-C6 alkyl group optionally substituted by C1-C6 alkoxycarbonyl;
- v is 0 or 1;
- R23 represents a hydrogen atom or a C1-C6 alkyl group;
- and
- R24 represents a hydrogen atom, or a C1-C6 alkyl group optionally substituted by carboxyl, C1-C6 alkoxy or C1-C6 alkoxycarbonyl;
- or a pharmaceutically acceptable salt or solvate thereof.
32 more elements
Dependencies are inferred from the claim text.