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US 6,306,863 B1Granted
Pyrrolo[3,4-d]pyrimidinone derivatives and their use as medicaments
AssigneeAstraZeneca AB
InventorsMartin E Cooper, David R Cheshire, David K Donald, Mark Furber, Matthew W. D Perry, Richard P Harrison, Nicholas P Tomkinsson
Life of this patent
Estimating the term…
Abstract
Compounds of the formula W, Q, R1, R2 and R10 are as defined in the specification. A process for their preparation and pharmaceutical compositions and methods of treatment involving their use in the treatment of respiratory disease including, for example, asthma, are also provided.
Claims11
A method of treating asthma in a patient in need of such treatment, said method comprising the step of administering to said patient a therapeutically effective amount of a compound of formula (I)
- wherein—
- W represents —CH2— or a bond;
- Q represents an aryl group Ar1 or Ar2;
- in the case where W represents —CH2—, Q represents Ar1 wherein Ar1 represents naphthyl, phenyl, quinolyl, isoquinolyl, indolyl, benzofuranyl or benzothienyl;
- in the case where W represents a bond, Q represents an aryl group Ar2 wherein Ar2 represents acenaphthenyl, fluorenyl or indanyl;
- wherein the ring systems which Ar1 and Ar2 represent may all be optionally substituted by one or more substituents selected from C1-4 alkyl, C1-4 alkoxy, halogen, or trifluoromethyl;
- R10 represents X—(A)p—Y;
- X represents S(O)n, C≡C, (CH2)2, CH═CH or CH2CH═CH;
- n represents 0, 1 or 2;
- A represents C1-6 alkylene;
- p is 0 or 1;
- Y represents CN, OR11, CO2R12, CONR13R14, NR15R16, NHSO2R17, NHCOR18 or an optionally substituted aryl or heteroaryl group, provided that when X represents S(O)n and Y is other than an optionally substituted aryl or heteroaryl group, then p is 1 and also provided that when X represents S(O)n, p is 1 and Y represents OH, then n is not 0;
- R13 and R14 independently represent H, C1-5 alkyl or phenyl, which latter group may be substituted by one or more substituents selected from C1-4 alkyl, C1-4 alkoxy, halogen, or CO2R21;
- and R1, R2, R11, R12, R15, R16, R17, R18 and R21 independently represent H or C1-5 alkyl;
- or a pharmaceutically acceptable derivative thereof.
12 more elements
Dependencies are inferred from the claim text.