AZABICYCLES MODULATING INHIBITION OF CELLULAR ADHESION, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD FOR TREATMENT Russian patent published in 2004 - IPC

Abstract RU 2226526 C2

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to compound of the formula (I): wherein R1 represents: (i) R3-Z3- or: (ii) R3-L3-Ar1-L4-Z3-; R2 represents hydrogen atom; R3 represents alkyl, aryl optionally substituted with one or two substituents taken among halogen atom and C1-4-alkyl, arylalkyl; R5 represents hydrogen atom; R7 and R7a represent hydrogen atom; R8 represents hydrogen atom; R9 represents alkyl optionally substituted with halogen atom, aryl, heteroaryl comprising up to 2 heteroatoms taken among nitrogen and oxygen atoms, or alkyl substituted with aryl or heteroaryl; A1 represents unsubstituted C1-3-alkylene bond with linear chain; Ar1 represents arylene that can be substituted optionally with C1-4-alkoxy-group or heteroaryldiyl comprising up to 2 heteroatoms taken among nitrogen and oxygen atoms; L1 represents alkylene bond that is substituted optionally with ; L3 represents -NR5-C(=Z)-NR5-, -Z-, -NR5-, -NR5-C(= O)-O-, or O- C(=O)-NR5- L4 represents alkylene bond; Z represents oxygen atom; Z1 represents C(R7)(R7a); Z3 represents C(=O) or SO2; Y represents carboxy-group under condition that when R1 represents R3 or R3-C(=O) then R3 can't represent alkyl; or its corresponding N-oxide or ester that can be converted to the primary molecule in vivo by metabolism, or pharmaceutically acceptable salt of such compound, or its N-oxide, or its ester. Invention relates also to pharmaceutical composition eliciting inhibitory effect on cellular adhesion and comprising effective amount of compound of the formula (I) and pharmaceutically acceptable carrier or excipient. Invention relates also to the application of compound of the general formula (I): wherein R1 represents R3 or R3--C(=O) wherein R3 represents alkyl; , Z, Z1, Z3 and Y are given above; or its corresponding N-oxide or ester that can be converted to the primary molecule in vivo by metabolism; or pharmaceutically acceptable salt of such compound or its N-oxide or ester used for preparing a medicinal agent used for treatment of patient suffering with states or subjected for states that can be relieved by administration of inhibitor of α4β1-mediated cellular adhesion. Invention relates also to method for treatment of patient suffering with states or subjected for states that can be relieved by administration of inhibitor of α4β1-mediated cellular adhesion involving administration to the indicated patient the effective dose of compound of the formula (I). Invention provides preparing new compounds eliciting inhibitory effect on cellular adhesion. EFFECT: improved treatment method, valuable medicinal properties of compounds. 65 cl, 3 tbl, 40 ex

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Authors

Burza Zhan-Dominik

Kommerson Alen

Filosh Brjuno Zhak Kristof

Kharris Nejl Viktor

Makkarti Klajv

Dates

2004-04-10Published

1999-08-26Filed