CYCLOALKYLENE OR HETEROCYCLOALKYLENE DERIVATIVES, PHARMACEUTICAL COMPOSITION, AEROSOL DEVICE, AND MEDICAL TREATMENT METHOD Russian patent published in 2000 - IPC

Abstract RU 2159229 C2

FIELD: medicine. SUBSTANCE: described are new cycloalkylene or heterocycloalkylene of general formula I: R2-Y-R3 wherein R2 and R3 are independently Z-X1-X2-X3-X4-X5 in which Z is amino, guanidino or amidino; Y is cyclo ((C3-14)) alkylene or heterocyclo ((C6-8)) alkylene, saturated or unsaturated alkylene containing one or two nitrogen oxygen atoms as heteroatoms; X1 is ((C3-6)) alkylene, oxa((C4-6))alkylene or -X6-X7-X8- in which X7 is phenylene, cyclo((C3-6))alkylene or heterocyclo ((C3-6))alkylene, saturated or unsaturated, containing one or two nitrogen atoms as heteroatom, and X6 and X8 are (Cn6) alkylene and heterocyclo ((Cn8))alkylene respectively, wherein sum of n6 and n8 is equal to 1,2,3 or 4 provided that when Z is amino, n6 is other than 0; X2 and X4 are independently , wherein each R1 is independently hydrogen, ((C1-8))alkyl; X3 is ((C1-8))alkylene, -X9-X10- or -X10-X9- wherein X9 is (Cn9) alkylene wherein n9 is 0,1 or 1, and X10 is cyclo ((C3-8))alkylene or heterocyclo ((C3-8))alkylene saturated or unsaturated, containing one or two nitrogen atoms as heteroatom provided that there are no covalent bonds between heteroatoms contained in X10 and heteroatoms contained either in X2 or X4; and X5 is ()alkylene wherein n5 is 0,1 or 2 provided that R2 and R3 are different, and pharmaceutically acceptable salts thereof. Also described are compositions based on compounds of formula I, aerosol device and medical treatment method. Said compositions, compounds and methods are effective for prevention and medical treatment of mastocyte-induced inflammatory disorders, associated with respiratory paths, such as asthma or allergic rhinitis and also other types of immunoinduced inflammatory diseases such as rhemotoidal arthritis, conjutivitis and inflammatory disease of alimentary canal, various dermatological states and also some visual diseases. Compounds include potent and selective inhibitors of protease and triptase of mastocyte. EFFECT: improved properties of the title compounds and pharmacological composition. 48 cl, 8 dwg, 6 ex

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RU 2 159 229 C2

Authors

Ken D. Rajs

Dzheffri M. Dener

Ehntoni R. Gehngloff

Ehlajn I-Lin Kuo

Dates

2000-11-20Published

1995-09-14Filed