2,6-SUBSTUTED-4-MONOSUBSTITUTED AMINO-PYRIMIDINES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS Russian patent published in 2011 - IPC C07D239/46 C07D409/04 C07D413/04 C07D403/04 A61K31/517 A61P37/08 

FIELD: chemistry.

SUBSTANCE: in formula (I) Cy¹ is a 6-member heterocyclyl containing N as a heteroatom, a 5,6-member monocyclic or 9,10-member bicyclic heteroaryl containing 1-3 heteroatoms selected from N, S and O, phenyl or phenyl condensed with a 5-member heterocycle containing O as a heteroatom, each optionally having 1-3 identical or different substituting Cy¹ groups which are: (C₁-C₆)-acyl, cyano, carboxy, hydroxy, (C₁-C₆)alkylsulphonyl, (C₃-C₆)-cycloalkyl, a 6-member heterocyclyl containing 1-2 heteroatoms selected from O and N, phenyl, a 5-member heteroaryl containing 1-3 heteroatoms selected from N, S and O, Y¹Y²N-, Y¹Y²NC(=O)-, Y¹Y²NSO₂-, (C₁-C₆)-alkyl-SO₂-N(R⁵)-C(=O)-, R⁶-C(=O)-N(R⁵)-, R⁷-NH-C(=O)-NH-; (C₁-C₆)-alkoxycarbonyl; (C₁-C₆)-alkyl, which optionally contains 1-3 identical or different substitutes which are halogen, carboxy, cyano, hydroxy, Y¹Y²N-, Y¹Y²N-C(=O)-, R⁶-C(=O)-N(R⁵)-, R⁸-SO₂-N(R⁵)-C(=O)-, 5-member heterocyclyl, containing N as a heteroatom, 5-member heteroaryl containing 1-3 heteroatoms selected from N and O; or (C₁-C₆)-alkoxycarbonyl; as well as (C₁-C₆)-alkoxy which optionally have 1-3 identical or different substitutes which are carboxy, (C₁-C₆)-alkoxycarbonyl, cyano, 3-member heterocyclyl containing O as a heteroatom, or 5-member heteroaryl containing 1-3 heteroatoms selected from N and O; where phenyl or heteroaryl fragments in the substituting Cy¹ groups optionally and independently have substitutes represented by hydroxy, (C₁-C₆)-alkyl, (C₁-C₆)-alkoxy, carboxy, (C₁-C₆)-alkoxycarbonyl or R⁸-SO₂-N(R⁵)-C(=O)-; and where cycloalkyl fragments in the substituting Cy¹ groups which optionally and independently have substitutes represented by (C₁-C₆)-alkoxy, carboxy; Cy² is a 9-member cycloalkenyl, phenyl, 5,6-member monocyclic or 9,10-member bicyclic heteroaryl containing 1-3 heteratoms selected from N, S and O, or phenyl condensed with a 5,6-member heterocycle containing 1-2 heteroatoms selected from N and O, each independently and optionally having 1-3 identical or different substitutes represented by (C₁-C₆)-alkoxy, (C₁-C₃)-alkyl, hydroxy, halogen, halogen-(C₁-C₆)-alkoxy, nitro, Y¹Y²N-; L¹ is an alkylene with a straight or branched chain containing 1-6 carbon atoms, optionally substituted carboxy; or L¹ is -CH₂-(C₁-C₅)halogenalkylene; L² is a bond, -O- or -CH₂-O-. Other values of radicals are given in the formula of invention.

EFFECT: novel compounds have prostaglandin D2 receptor antagonist properties, can be used in treating primarily allergic disorders such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma, food allergy and other diseases.

39 cl, 1 tbl, 99 ex