HETEROCYCLIC COMPOUNDS APPLICABLE AS ALLOSTERIC EFFECTORS IN MUSCARINE RECEPTORS Russian patent published in 2000 - IPC

Abstract RU 2152385 C1

FIELD: biologically-active compounds. SUBSTANCE: invention provides novel pyrrole derivatives of formula I: (I), wherein Z is methylene group, methyne group, group >NH or =N-; W is methylene group, methyne group, sulfur atom, group >SO2 wherein v is 1 or 2 when Z is not >NH group when W is >SO2; each Е defines ordinary or double bond provided that, when W is sulfur atom or >SO2 group, W and Z are linked by ordinary bond; at least one of Y1-Y4 is group of formula (A)p-B1-T1, wherein A is oxygen atom, T1 is optionally protected carboxyl group, protected thiocarboxyl group, protected sulfonamide group, or tetrazolyl group; B1 is C1-C4-alkylene group optionally substituted by at least one α substituent (defined below), and p = 0 or 1; Y1-Y4 can also have other designations indicated in claim 1 of the formula of invention; one of R1 and R2 is hydrogen, C1-C6-alkyl or benzyl group and the other hydrogen or C1-C6-alkyl; or R1 and R2 together form group of formula (I b′): ((I b′)), wherein R10, R11 and R12, identical or different, are hydrogen atom, hydroxy, or C1-C6-alkoxy group; R3 is hydrogen or amino-protection group. Substituent α is selected from group of substituents including: hydroxyl, C2-C7-alkoxycarbonyl, carboxyl, phenyl optionally substituted by at least one substituent selected from halogen and nitro group, aryl-C1-C3-alkyl optionally substituted by phenyl group that can also be substituted by at least one substituent selected from halogen and nitro group. Invention also provides pharmaceutically acceptable salts or esters of compound I. Compounds of invention can be used as allosteric effectors for muscarine receptors. EFFECT: extended choice of biologically-active compounds. 27 cl, 1 dwg, 1 tbl, 235 ex

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RU 2 152 385 C1

Authors

Bedsehll Najdzhel

Lazareno Sebast'Jan

Naruto Siundzhi

Masakhiko Sugimoto

Kojama Kazuo

Marumoto Sindzhi

Dates

2000-07-10Published

1995-07-27Filed