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US 6,555,541 B1Granted
Substituted phenyl compounds with immunosuppressing activity and pharmaceutical compositions
AssigneeAstraZeneca UK Limited
InventorsMark Furber, Timothy J Luker, Michael P Mortimore, Philip Thorne, Premji Meghani
Life of this patent
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Abstract
The invention provides substituted phenyl compounds of general formula wherein R1, T, U and Ar are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.
Claims14
A compound of formula
- wherein:
- each R1 independently represents a hydrogen or halogen atom, or a trifluoromethyl, cyano, nitro, C1-C6 alkyl or C1-C6 alkoxy group;
- T represents a group NH;
- U represents an oxygen or sulphur atom or a group NH;
- Ar represents a group
- X represents a bond, an oxygen atom or a group CO, CH2, CH2O O(CH2)m, CH2OCH2, NR5, CH2NR5, NR5CH2, CH2NR5CH2, CONR5, S(O)n or SO2NR5;
- m is 1, 2 or 3;
- n is 0, 1 or 2;
- one of R2 and R3 represents a halogen, cyano, nitro, amino, hydroxyl, or a group selected from
- (i) C1-C6 alkyl optionally substituted by at least one C3-C6 cycloalkyl,
- (ii) C3-C8 cycloalkyl,
- (iii) C1-C6 alkyloxy optionally substituted by at least one C3-C6 cycloalkyl,
- (iv) C3-C8 cycloalkyloxy,
- (v) S(O)pC1-C6 alkyl, or
- (vi) S(O)qC3-C8 cycloalkyl,
- each of these groups being optionally substituted by one or more fluorine atoms, and the other of R2 and R3 represents a hydrogen or halogen atom or a methyl group;
- p is 0, 1 or 2;
- q is 0, 1 or 2;
- R4 represents a 3- to 9-membered saturated heterocyclic ring system containing one or two nitrogen atoms, the heterocyclic ring system being optionally substituted by one or more substitutents independently selected from fluorine atoms, hydroxyl, C1-C6 alkyl, acetyl, hydroxyC1-C6 alkyl, —NR6R7, —(CH2)rNR6R7, —CONR6R7 and pyrimidinyl;
- r is 1, 2, 3, 4, 5 or 6;
- R5 represents a hydrogen atom or a C1-C6 alkyl or C3-C8 cycloalkyl group;
- and
- R6 and R7 each independently represent a hydrogen atom or a C1-C6 alkyl or C3-C8 cycloalkyl group, or R6 and R7 together with the nitrogen atom to which they are attached to form a 3- to 8-membered saturated heterocyclic ring, provided that when R3 represents a cyano group, then X is other than a bond;
- or a pharmaceutically acceptable salt or solvate thereof.
21 more elements
Dependencies are inferred from the claim text.