AMINOALKYLPYRIMIDINE DERIVATIVES AS HISTAMINE H RECEPTOR ANTAGONISTS Russian patent published in 2016 - IPC C07D401/14 C07D403/04 C07D403/14 C07D409/14 A61K31/506 A61P29/00 A61P35/00 A61P37/08 A61P11/00 A61P11/16 A61P27/04 A61P27/12 A61P17/00 A61P17/06 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new aminoalkylpyrimidine derivatives of formula (I) or their pharmaceutically acceptable salts exhibiting the properties of histamine H₄ receptor antagonists. The compounds are applicable in respiratory diseases, including asthma, allergic rhinitis, chronic obstructive pulmonary disease (COPD); ophthalmic diseases, including conjunctivitis, dry eye syndrome, cataract; dermatological diseases, including eczema, dermatitis (e.g., atopic dermatitis), psoriasis, urticaria, pemphigus, dermatitis herpetiformis, cutaneous vasculitis, itch; inflammatory intestinal diseases, including nonspecific ulcerative colitis, Crohn's disease; and autoimmune diseases, including rheumatoid arthritis, multiple sclerosis, cutaneous lupus, systemic lupus erythematosus, widespread vasculitis and graft rejection. In formula I

R₁ and R₂ form together with N atom to which they are bound, a saturated heterocyclic group containing one nitrogen atom and free frpm any other heteroatoms; the above heterocyclic group is substituted by one -NR_aR_b group and optionally substituted by one or more C_1-4alkyl groups; wherein the heterocyclic group represents a 4-7-merous monocyclic group; R_a represents H or C_1-4alkyl; R_b represents H or C_1-4alkyl; R₃ represents H or C_1-8alkyl; R₄ represents a) C_1-8alkyl optionally substituted by one or more halogens; b) C_3-10cycloalkyl-C_0-4alkyl; c) aryl-C_0-4alkyl or d) 5-6-merous heteroaryl-C_0-4alkyl, wherein the radicals b), c) or d) may be substituted as specified in the patent claim; n equals to 1 or 2; each R₅ independently represents H or C_1-8alkyl.

EFFECT: compounds can find application in treating or preventing an allergic, immune system or inflammatory disease, pain or cancer.

22 cl, 18 ex