VINSSINGER Nikolas (FR),ВИНССИНГЕР Николас (FR),BARLUENGA Sofija (FR),БАРЛУЕНГА София (FR),KARPLAS Martin (US),КАРПЛАС Мартин (US),VINSSINGER NIKOLAS,ВИНССИНГЕР Николас,BARLUENGA SOFIJA,БАРЛУЕНГА София,KARPLAS MARTIN,КАРПЛАС Мартин
申请号：
RU2010133979/04
公开号：
RU0002534527C2
申请日:
2009.01.15
申请国别(地区):
RU
年份:
2014
代理人:
摘要：
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to new macrocyclic compounds of formulaor their tautomer, pharmaceutically acceptable salt, solvate or ester, wherein: X represents O or NR； Y represents -O-(CH2)mCOOR or -O-(CH2)mCON(R)2, wherein groups related to a nitrogen atom, can be in a Z- or E-configuration； R1 and R2 independently represent hydrogen or halogen； R3, R4, R5, R6, R7, R8, R9 and R10 independently represent hydrogen, alkyl, OR, -O(CH2)mC(O)(CH2)pN(R)2, -O(CH2)mN(R)C(O)(CH2)pOR, -(CH2)mN3 or -O(CH2)mN3； and each R independently represents R11, hydrogen, alkyl, alkylamino, dialkylamino, alkoxycarbonyl, phenyl or a protective group； or two R on the same nitrogen are taken together with nitrogen for producing a 5-6-merous heterocyclic or heteroaryl ring； wherein the group contains more than one substitute R； wherein R is optionally substituted, and each R can be identical or different, and wherein the protective group is specified in ethoxymethyl, methoxymethyl, tert-butyldimethylsilyl (TBS), phenylmethylsilyl, trimethylsilyl (TMS), 2-trimethylsilyl ethoxymethyl (SEM), 2-trimethylsilylethyl, benzyl and substituted benzyl； R11 represents a group,wherein Z represents an inorganic or organic counter-ion specified in a halogen, -O-alkyl, toluene sulphonate, methylsulphonate, sulphonate, phosphate, formiate or carboxylate； n represents 0, 1 or 2； m and p independently represent 0, 1 or 2； and dashed lines mean either a single, or a double bond, wherein the necessary conditions of the valence are observed by additional hydrogen atoms； and wherein in formula I′, when n represents 1, and X represents O, and the double bond is present between the carbon atoms having R9 and R10, then at least one of R5, R6, R7, R8, R9 or R10 are other than hydrogen； and wherein in formula I′, when n represents 1, and X represents O, and the bond between the carbon atoms having R9 and R10, represents the single bond, then at least one of R5, R6, R7 or R8 is other than
