PYRIDAZINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS Russian patent published in 2008 - IPC C07D237/20 C07D237/24 A61K31/501 A61P3/06 

Abstract RU 2326118 C2

FIELD: chemistry.

SUBSTANCE: invention pertains to new compounds with formula (II): , where x and y are each independently represent 1, 2 or 3; W is chosen from -C(O)N(R1)- and -N(R1)C(O)-; each R1 is independently chosen from a group, consisting of hydrogen; C1-C6alkyl, optionally substituted with one or more substitutes, chosen from a group consisting of a halogen, methyl or trifluoromethyl; and C2-C6alkyl, optionally substituted with one or more substitutes, chosen from a group consisting of methoxy and hydroxyl; R2 is chosen from a group, consisting of C7-C12alkyl, C3-C12alkenyl, C7-C12hydroxyalkyl, C2-C12alkoxyalkyl, C3-C12hydroxyalkenyl, C3-C12cycloalkyl, C4-C12cycloalkylalkyl, C13-C19aralkyl, C3-C12heterocyclylalkyl and C3-C12heteroaralkyl; or R2 represents a multi-ringed structure, consisting of 2 to 4 rings, where the rings are independently chosen from a group consisting of cycloalkyl, heterocyclyl, aryl and hetero-aryl, where some or all of the rings can be condensed together; R3 is chosen from a group consisting of C3-C12alkyl, C3-C12alkenyl, C3-C12hydroxyalkyl, C3-C12hydroxyalkenyl, C3-C12alkoxy, C3-C12alkoxyalkyl, C3-C12cycloalkyl, C4-C12cycloalkylalkyl, aryl, C7-C12aralkyl, C3-C12heterocyclyl, C3-C12heterocyclylalkyl, C5-C12 heteroaryl and C3-C12heteroarylakyl; or R3 represents a multi-ringed structure, consisting of 2 to 4 rings, where each ring is independently chosen from a group, consisting of cycloalkyl, heterocyclyl, aryl and heteroaryl and where some or all of the rings can be condensed together; R4 and R5 each independently chosen from hydrogen, fluorine, chlorine, methyl, methoxy and trifluoromethyl; and R6, R6a, R7, R7a, R8, R8a, R9 and R9a each independently chosen from hydrogen or C1-C3alkyl; or R6 and R6a together represent an oxo-group, under the condition that, when V represents -C(O)-, then R7 and R7a together or R8 and R8a together do not form an oxo-group, then as the rest of R6, R6a, R7, R7a, R8, R8a, R9 and R9a each independently chosen from hydrogen or C1-C3alkyl; or one of R6 , R6a, R7 and R7a together with one of R8, R8a, R9 and R9a, form an alkylene bridge, then as the rest of R6, R6a, R7, R7a, R8, R8a, R9 and R9a are each independently chosen from hydrogen or C1-C3alkyl; including its pharmaceutically accepted salt. The invention also relates to compounds with formulae (III), (IV), (Va), (Vb), to the method inhibiting activity of human stearol-CoA desaturase (hSCD), to pharmaceutical mixtures, and to use of compounds with formulae (I), (II) (III), (IV), (Va), (Vb).

EFFECT: obtaining of biologically active compounds and pharmaceutical mixtures as their base, with inhibitor action on the activity of the human stearol-CoA desaturase (hSCD).

92 cl, 33 ex

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RU 2 326 118 C2

Authors

Abreo Melvin

Chafeev Mikhail

Chakka Nagasri

Chovdkhuru Sultan

Fu Jan'Min'

Gshvend Khajnts U.

Kholladej Mark U.

Khou Duan'Tse

Kamboj Rajehnder

Kodumuru Vishnumurtu

Li Ven'Bao

Lju Shifehn

Rajna Vandna

Sun' Sen'Gen'

Sun' Shaoi

Sviridov Sergej

Tu Chi

Uinter Majkl D.

Chzhan Zajsjuj

Dates

2008-06-10Published

2004-07-29Filed