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US 2006/0235057 A1Published application
Phenyl compounds
AssigneeGlaxo Group Limited
InventorsRino Bit, Gerard Giblin, Adrian Hall, David Hurst, Ian Kilford, Neil Miller, Tiziana Scoccitti
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I) or derivatives thereof: wherein A, B, Z, R1, R2a, R2b, Rx, R8, and R9 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
Claims18
A compound of formula (I):
- wherein:
- A is an optionally substituted aryl, or an optionally substituted 5- or 6-membered heterocyclyl ring, or an optionally substituted bicyclic heterocyclyl group;
- B is a phenyl or pyridyl ring;
- Z is O, S, SO, or SO2;
- R1 is CO2R4, CN, CONR5R6, CH2CO2R4, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted SO2alkyl, SO2NR5R6, NR5CONR5R6, COalkyl, 2H-tetrazol-5-yl-methyl, optionally substituted bicyclic heterocycle or optionally substituted heterocyclyl;
- R2a and R2b independently are hydrogen, halogen, optionally substituted alkyl, optionally substituted alkoxy, CN, SO2alkyl, SR5, NO2, optionally substituted aryl, CONR5R6 or optionally substituted heteroaryl;
- Rx is optionally substituted alkyl wherein 1 or 2 of the non-terminal carbon atoms are optionally replaced by a group independently selected from NR4, O and SOn, wherein n is 0, 1 or 2:
- or Rx represents optionally substituted CQaQb-heterocyclyl, optionally substituted CQaQb-bicyclic heterocyclyl or optionally substituted CQaQb-aryl;
- R4 is hydrogen or an optionally substituted alkyl;
- R5 is hydrogen or an optionally substituted alkyl;
- R6 is hydrogen or optionally substituted alkyl, optionally substituted heteroaryl, optionally substituted SO2aryl, optionally substituted SO2alkyl, optionally substituted SO2 heteroaryl, CN, optionally substituted CQaQbaryl, optionally substituted CQaQb-heteroaryl or COR7;
- R7 is hydrogen, optionally substituted alkyl, optionally substituted heteroaryl or optionally substituted aryl;
- R8 and R9 independently are hydrogen, chloro, fluoro, CF3, C1-3alkoxy or C1-3alkyl;
- Qa and Qb are independently selected from hydrogen and CH3;
- wherein when A is a 6-membered ring the R1 substituent and phenyl ring are attached to carbon atoms 1,2-, 1,3- or 1,4-relative to each other, and when A is a five-membered ring or bicyclic heterocyclyl group the R1 substituent and phenyl ring are attached to substitutable carbon atoms 1,2- or 1,3-relative to each other;
- and derivatives thereof;
- provided that the compound is not 2-benzyloxy[1,1′:2′,1″]terphenyl-4″-carboxylic acid.
14 more elements
A compound of formula (Ia):
- wherein:
- W, X, and Y each are CR12 or N;
- V is CR1, CR12 or N;
- wherein at least two of W, X, Y or V is CR12;
- and R12 is independently selected from hydrogen, halogen, CN, optionally substituted CO2C1-6alkyl, CONR5R6, NR5R6, optionally substituted NR5COC1-6alkyl, optionally substituted NR5COphenyl, optionally substituted NR5COpiperidinyl, optionally substituted NR5COheterocyclyl, optionally substituted NR5SO2C1-6alkyl, OH, optionally substituted OC1-6alkyl, optionally substituted C1-6alkyl and NR10R11;
- Q1 and Q2 each is CH, or one of Q1 and Q2 is N and the other is CH;
- R1 is CO2H, optionally substituted CONHSO2aryl, CH2CO2H, SO2NHCOR7, SO2NHCOC1-6alkyl or tetrazolyl and is positioned 1,2-, or 1,3-relative to the phenyl ring;
- R2a and R2b are independently selected from hydrogen, halo, and CF3;
- Rx is optionally substituted C1-8alkyl, or Rx represents optionally substituted CQaQb-heterocyclyl or optionally substituted CQaQb-phenyl wherein Qa and Qb are independently selected from hydrogen and CH3;
- R4 is hydrogen or an optionally substituted C1-6alkyl;
- R5 is hydrogen or an optionally substituted C1-6alkyl;
- R6 is hydrogen or an optionally substituted C1-6alkyl, optionally substituted SO2phenyl, optionally substituted SO2 heterocyclyl group, CN, optionally substituted CH2phenyl or COR7;
- R7 is hydrogen, optionally substituted heteroaryl or optionally substituted phenyl;
- R8 and R9 independently represent hydrogen, chloro, fluoro, CF3, C1-3alkoxy or C1-3alkyl;
- and
- R10 and R11 together with the nitrogen atom to which they are attached form a morpholine ring, a 5- or 6-membered lactam ring or a 5- or 6-membered cyclic sulphonamide,
- and derivatives thereof.
14 more elements
A compound selected from the compounds of Examples 1-90 or a derivative thereof.
9-10. (canceled)
14-16. (canceled)
(canceled)
Dependencies are inferred from the claim text.