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US 2009/0023738 A1Published application
Diaminopyrimidines as modulators of the ep2 receptor
OwnerNico Braeuer, Bernd Buchmann +6inventors
InventorsNico Braeuer, Bernd Buchmann, Marcus Koppitz, Antonius Ter Laak, Gernot Langer, Bernhard Lindenthal, Olaf Peters, Tim Wintermantel
Life of this patent
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Abstract
The present invention relates to diaminopyrimidines of the general formula I, process for their preparation, and the use thereof for the manufacture of pharmaceutical compositions for the treatment of disorders and indications connected with the EP2 receptor.
Claims18
A compound of the formula I
- where
- Y is a CH group or a C(C1-C4-alkyl) group,
- V is a hydrogen, a C1-C4-alkyl group,
- n is 0, 1 or 2,
- W is a 6-10-membered, mono- or bicyclic aryl ring which is in each case unsubstituted or optionally substituted once to three times,
- a 5-10-membered, mono- or bicyclic heteroaryl ring which is in each case unsubstituted or optionally substituted once to three times,
- an 8-12-membered aryl- or heteroaryl-cycloalkyl or -cycloalkenyl group which is in each case unsubstituted or optionally substituted once to three times,
- an 8-12-membered aryl- or heteroaryl-heterocyclyl or -heterocyclenyl group which is in each case unsubstituted or optionally substituted once to three times,
- a 3-12-membered, mono-, bi- or tricyclic cycloalkyl radical which is in each case unsubstituted or optionally substituted once, where the substituents are linked either directly or via a spacer U to W and may be selected from the group of halogen, cyano, R4, OR4, OC(O)R4, S(O)nR4, where n is 0, 1, 2, SO2NR4R5, SO2NR5C(O)R4, NR4R5, NR5C(O)R4, NR5SO2R4, C(O)NR5SO2R4, C(OH)R4R5, C(O)R4, C(NOH)R4, CO2R4,C(O)NR4R5,
- or
- in the case where n=0 together with V is a pyrrolidine, piperidine, morpholine or thiomorpholine residue which is in each case unsubstituted or optionally substituted once,
- or else
- in the case where n=0 together with V is a piperazine residue, which is unsubstituted or optionally N-substituted, where the substituents are linked either directly or via a spacer U to W and may be selected from the group of halogen, cyano, R4, OR4, OC(O)R4, S(O)NR4 where n is 0, 1, 2, SO2NR4R5, SO2NR5C(O)R4, NR4R5, NR5C(O)R4, NR5SO2R4, C(O)NR5SO2R4, C(OH)R4R5, C(O)R4, C(NOH)R4, CO2R4, C(O)NR4R5,
- U is a C1-C4-alkylene, C2-C4-alkenylidene, C2-C4-alkynylidene, O—C1-C4-alkylene, C(O)—C1-C4-alkylene, S(O)n—C1-C4-alkylene, where n is 0, 1, 2, N(R5)—C1-C4-alkylene, C(O)—N(R5)—C1-C4-alkylene, N(R5)—C(O)—C1-C4-alkylene spacer,
- R1 is a C1-C4-alkyl group or cyano,
- R2 is a hydrogen, halogen, cyano, a C1-C4-alkyl group,
- R3 is a hydrogen, halogen, cyano, a C1-C4-alkyl group,
- R4 is a hydrogen, a C1-C4-alkyl group, a C2-C4-alkenyl group, a C2-C4-alkynyl group, a C3-C6-cycloalkyl group, a CH2—C3-C6-cycloalkyl group, a 6-membered aryl ring, a 5-6-membered heteroaryl ring or a CH2-aryl or heteroaryl group, where the aryl radical is 6-membered and the heteroaryl radical is 5 or 6-membered,
- R5 is a hydrogen, a C1-C4-alkyl group and
- R4, R5 together form a 3-6-membered cycloalkyl or a heteroatom-containing ring,
- and the isomers, diastereomers, enantiomers and salts thereof, and cyclodextrin clathrates.
18 more elements
Dependencies are inferred from the claim text.