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US 2007/0185075 A1Published application
Pyrimidine derivatives
AssigneePfizer Inc.
InventorsAndrew Bell, Charlotte Lane, Charles Mowbray
Life of this patent
Estimating the term…
Abstract
A compound of Formula (I): or a pharmaceutically and/or veterinarily acceptable derivative thereof, wherein R1, R2, R3, R4, R5, and R8 are as defined above.
Claims21
A compound of Formula (I):
- or a pharmaceutically and/or veterinarily acceptable salt or solvate thereof, wherein:
- R1 is C1-8alkyl, C3-7cycloalkyl-C0-6alkyl- optionally substituted with methyl, alkoxyalkyl containing 3 to 8 carbon atoms, het-C0-6alkyl-, CF3—C1-6alkyl-, CF3OC2-3alkyl-, aryl-C0-6alkyl- or C1-6-hydroxyalkyl;
- R2 is het, provided that the het group contains at least one nitrogen atom or is substituted by a group which contains at least one nitrogen atom;
- or R2 is NH(CH2)2NH2, NH(CH2)2NHCH3, or N H(CH2)2N H(CH3)2;
- R3 is H, C1-8alkyl, (CH2)pC3-7cycloalkyl, alkoxyalkyl containing 3 to 8 carbon atoms, (CH2)nCF3, (CH2)xOCF3 or C1-6hydroxyalkyl;
- or R3 and R2 together with the nitrogen atom to which they are bound form a 4 to 8 membered non-aromatic heterocyclic group which optionally contains one or more further heteroatoms or groups independently selected from N, O, S, S(O) and S(O)2, wherein the heterocyclic group is optionally a bridged bicyclic group, a spiro bicyclic group or is optionally fused to a 3-, 4-, 5- or 6-membered carbocyclic group or a 4-, 5- or 6-membered heterocyclic group which contains at least one ring member independently selected from N, O, S, S(O) and S(O)2, and wherein the ring system as a whole is optionally substituted by one or more substituents independently selected from C1-6alkyl, NR5R7, (CH2)aC3-7cycloalkyl, alkoxyalkyl containing 2 to 8 carbon atoms, (CH2)bhet1, (CH2)cCF3, (CH2)yOCF3, (CH2)daryl and C1-6hydroxyalkyl, provided that the ring system as a whole contains at least two nitrogen atoms or contains one nitrogen atom and is substituted by a group which contains at least one nitrogen atom;
- R4 is H;
- or R1 and R4 together with the nitrogen atom to which they are bound form a 4 to 8 membered non-aromatic heterocyclic group which optionally contains one or more further heteroatoms or groups independently selected from N, O, S, S(O) and S(O)2, wherein the heterocyclic group is optionally a bridged bicyclic group or is optionally fused to a 3-, 4-, 5- or 6- membered carbocyclic group or a 4-, 5- or 6-membered heterocyclic group which contains at least one ring member independently selected from N, O, S, S(O) and S(O)2, and wherein the ring system as a whole is optionally substituted by one or more substituents independently selected from C1-6alkyl, fluoro, NR9R10, (CH2)eC3-7cycloalkyl, alkoxyalkyl containing 2 to 8 carbon atoms, (CH2)fhet1, (CH2)gCF3, (CH2)zOCF3, (CH2)haryl and C1-6hydroxyalkyl;
- R5 is H or NR11R12;
- R6 and R7 are each independently selected from H, C1-6alkyl and (CH2)jC3-7cycloalkyl;
- or R6 and R7, together with the nitrogen atom to which they are bound, form a 4, 5 or 6 membered heterocyclic group;
- R8 is H or C1-3alkyl;
- R9 and R0 are each independently selected from H, C1-6alkyl and (CH2)kC3-7cycloalkyl;
- or R9 and R10, together with the nitrogen atom to which they are bound, form a 4, 5 or 6 membered heterocyclic group;
- R11 and R12 are each independently selected from H, C1-6alkyl and (CH2)IC3-7cycloalkyl;
- or R11 and R12, together with the nitrogen atom to which they are bound, form a 4, 5 or 6 membered heterocyclic group;
- R13 and R14 are each independently selected from H, C1-6alkyl and (CH2)mC3-7cycloalkyl;
- or R13 and R14, together with the nitrogen atom to which they are bound, form a 4, 5 or 6 membered heterocyclic group;
- a, b, c, d, e, f, g, h, j, k, l, m and p are each independently selected from 0, 1, 2 and 3;
- n is 1, 2 or 3;
- x is 2 or 3, wherein if x is 3, then the (CH2)3 group may be replaced with a branched alkyl group containing 3 carbon atoms;
- y and z are each independently selected from 1, 2 and 3
- aryl is phenyl, naphthyl, anthracyl or phenanthryl, each optionally substituted by one or more groups independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, CHF2, OCF3, OCHF2, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl, C1-4alkyl-S—C1-4alkyl, aryl1, het1, Oaryl1, Ohet1, Saryl1, Shet1, CF2CF3, CH2CF3, CF2CH3, C(O)NR13R14, C3-8cycloalkyl, C3-7cycloalkyl-C1-4alkyl, C3-7cycloalkyl-C1-4alkoxy, C3-7cycloalkyl-O—C1-4alkyl, C3-7cycloalkyl-C1-4alkoxy-C1-4alkyl, OC3-7cycloalkyl and SC3-7cycloalkyl, wherein the aryl1 and het1 groups are optionally substituted by at least one group selected from C1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, OC3-7cycloalkyl, halo, CN, OH, CF3, CHF2, OCF3, OCHF2, hydroxyC1-6alkyl, C1-4alkoxy-C1-4alkyl, SC1-6alkyl and SCF3;
- het is 4 to 8 membered non-aromatic heterocyclic group which contains at least one heteroatom or group independently selected from N, O, S, S(O) and S(O)2, wherein the heterocyclic group is optionally a bridged bicyclic group or is optionally fused to a 3-, 4-, 5- or 6-membered carbocyclic group or a 4-, 5- or 6-membered heterocyclic group which contains at least one ring member independently selected from N, O, S, S(O) and S(O)2, and wherein the ring system as a whole is optionally substituted by one or more substituents independently selected from C1-6alkyl, NR6R7, (CH2)aC3-7cycloalkyl, alkoxyalkyl containing 2 to 8 carbon atoms, (CH2)bhet1, (CH2)CCF3, (CH2)yOCF3, (CH2)daryl and C1-6hydroxyalkyl;
- aryl1 is phenyl, naphthyl, anthracyl or phenanthryl;
- and
- het1 is an aromatic or non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 4-, 5- or 6-membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom.
24 more elements
Dependencies are inferred from the claim text.