FIELD: pharmaceutics.
SUBSTANCE: present invention relates to novel substituted dihydrothienopyrimidines, specifically to a compound of general formula (I), where R1 is hydrogen or (C1-C4)alkyl; R2 is selected from the group consisting of tetrahydropyranyl, oxaspiroheptanyl, pyrrolidinyl and piperidinyl, wherein said pyrrolidinyl and piperidinyl are optionally substituted with one or more substitutes, independently selected from R4, where R4 is -C(O)(C1-C4)alkyl; R3 is selected from the group consisting of (C1-C6)alkyl, (C3-C6)cycloalkyl, (C1-C4)alkyl(C3-C6)cycloalkyl, halogen(C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkyl(C1-C6)alkoxy, halogen(C1-C4)alkyloxy, (4–6)-membered heterocycloalkyl, (C1-C4)alkyl(4–6)membered heterocycloalkyl, (5–6)-membered heteroaryl, (C1-C4)alkyl(5–6)-membered heteroaryl, phenyl and (C1-C4)alkylphenyl, where said (4–6)-membered heterocycloalkyl includes 1 heteroatom selected from oxygen, nitrogen, sulfur, S(=O) and S(O)2, where said (5–6)-membered heteroaryl includes 1–2 heteroatoms, selected from oxygen, sulfur and nitrogen, where said alkyl, cycloalkyl, heterocycloalkyl, heteroaryl and phenyl are optionally substituted with one or more substitutes independently selected from R5, where R5 is selected from the group consisting of halogen, hydroxyl, (C1-C4)alkyl, halogen (C1-C4)alkyl, halogen(C1-C4)alkyloxy, ORx, -SRx, -S(O)2Rx, -S(O)2NRaRb, -C(O)Rx, -C(O)(ORx) and -C(O)NRaRb, where Ra and Rb are independently selected from the group consisting of hydrogen, (C1-C4)alkyl and halogen(C1-C4)alkyl, Rx consists of (C1-C4)alkyl, (C3-C6)cycloalkyl, (5–6)membered heterocycloalkyl containing 1–2 heteroatoms, selected from oxygen, nitrogen, sulfur, S(=O) and S(O)2; and where S* is a chiral sulfur atom; and its pharmaceutically acceptable salts, enantiomers, a mixture of enantiomers, diastereomers and a mixture of diastereomers. Also disclosed is a pharmaceutical composition, use of said compound to produce a pharmaceutical composition, methods of treatment.
EFFECT: disclosed compounds have phosphodiesterase inhibitory activity and can be used as therapeutic agents in treating diseases and conditions, susceptible to PDE4 inhibitory activity.
20 cl, 10 tbl, 77 ex
(I)
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