摘要:
The invention concerns borneol derivatives of general formula (I), wherein: R represents C(O)-CH(OR )-CH(NR R )-R , C(O)-CH(OR )-CH[NH(C(O)-CH(OR )-CH(NR R )-R )] -R ; R and R are identical or different and the same as R ; R and R are identical or different and the same as R ; R is -C(O)R , -SO2R , -C(O)OR , -C(O)SR , -C(O)NHR , -C(O)NR R , (a), alkyl; R is phenyl; R and R are identical or different and stand for alkyl, cycloalkyl, aryl or aralkyl; R are identical or different and stand for hydrogen, alkyl, aryl, acyl, aralkyl, -SO2R , -P(O) (OH)2; R stands for hydrogen, alkyl, aryl, aralkyl. The invention also concerns salts of the said compounds with physiologically tolerable bases, alpha -, beta - or gamma -cyclodextrine clathrates of the said compounds and compounds of formula (I) encapsulated with liposomes. The compounds are active as tubulin polymerisation antagonists.
摘要:
Die Erfindung betrifft neue Übergangsmetallkomplexe der Formel (I) und (II), Verfahren zur Herstellung dieser Übergangsmetallkomplexe, Zwischenprodukte zur Herstellung, sowie die Verwendung der Übergangsmetallkomplexe als Katalysatoren in organischen Reaktionen, besonders in Metathesereaktionen.
摘要:
The invention concernes borneol esters of general formula (I), in which R means T-C(O)-CH(OR )-CH(NR R )-R , C(O)-CH(OR )-CH[NR (C(O)-CH(OR )-CH(NR R )-R )]-R ; R R are identical or different and means R ; R means hydrogen, A, -C(O)R , -C(O)OR , -C(O)SR , -C(O)NHR , -C(O)NR R , -SO2R , C1-C10 alkyl; R , R are identical or different and mean R ; R means (i), heteroaryl substituted by X , C7-C16 aralkyl, alkyl; A is B-[O-(CH2)t-C(O)]0 or 1-, farnesyl-P(O)(OR )-O-(CH2)t-C(O)-; B means protein kinase-inhibitors or farnesyl protein transferase-inhibitors such as for example farnesyl (ii); and T is a bond, Z or a group (iii). The borneol esters can influence tubulin polymerisation and tubulin depolymerisation.
摘要:
The invention relates to immobilizable ruthenium(II)-catalysts having general formulae (I) and (II), containing an SiR' n (OR') 3-n structural group on at least one of the two anions. The invention also relates to a method for the production and use of compounds in a method for the production of ruthenium (II)-catalysts having general formulae (I) and (II) immobilized on inorganic oxide carriers. The invention further relates to the use of compounds having general formulae (I), (la), (II) and (IIa) as catalysts in organic and metalorganic synthesis. Said compounds can be used as catalysts in C-C coupling reactions, hydrogenations, isomerizations, silylations and hydroformylations. They can be used in particular as catalysts in olefin metathetical reactions such as cross metathesis (CM), ring closure metathesis (RCM), ring opening metathesis (ROM), ring opening metathesis-polymerization (ROMP), acyclic diene metathesis-polymerization (ADMET) and En-In metathesis or in a combination of various metathetical reactions.
摘要:
Die Erfindung betrifft immobilisierbare Ruthenium(II)-Katalysatoren der allgemeinen Formeln (I) und (II), die eine SiR' n (OR') 3-n tragende Gruppe an mindestens einem der beiden Anionen enthalten. Die Erfindung betrifft weiterhin ein Verfahren zu deren Herstellung und die Verwendung der Verbindungen in einem Verfahren zur Herstellung von auf anorganischen Oxid-Trägern immobilisierten Ruthenium(II)-Katalysatoren der allgemeinen Formeln (Ia) und (IIa). Gegenstand der Erfindung ist auch die Verwendung der Verbindungen der allgemeinen Formeln (I), (la), (II) und (IIa) als Katalysatoren in der organischen und metallorganischen Synthese. Sie können als Katalysatoren in C-C-Kupplungsreaktionen, Hydrierungen, Isomerisierungen, Silylierungen und Hydroformylierungen eingesetzt werden. Insbesondere dienen sie als Katalysatoren in Olefinmetathesereaktionen, wie der Kreuzmetathese (CM), Ringschlussmetathese (RCM), Ringöffnungsmetathese (ROM), Ringöffnungsmetathese-Polymerisation (ROMP), azyklische Dienmetathese-Polymerisation (ADMET) und En-In-Metathese oder in einer Kombination verschiedenartiger Metathesereaktionen.
摘要:
The disclosure relates to borneol derivatives of general formula (I) wherein: R represents a phenyl residue optionally substituted by halogen atoms, C1-C4 alkyl groups, C1-C4 alkoxy groups, C1-C6 alkoxycarbonyl groups or C1-C8 acyloxy groups; R stands for a hydrogen atom, a C1-C4 alkyl group, substituted aryl, a C1-C6 alkoxycarbonyl group or a C1-C8 acyl group; R stands for a hydrogen atom, a C1-C4 alkyl group, a C1-C4 acyl group or a tri-C1-C4 alkylsilyl group; R and R represent a hydrogen atom, a C1-C4 alkyl residue or a phenyl residue optionally substituted by halogen atoms, C1-C4 alkyl group, C1-C9 alkoxy groups, C1-C4 alkoxycarbonyl groups or C1-C8 acyloxy groups; R and R stand for a hydrogen atom, hydroxy group or a C1-C8 acyloxy group, or together represent a carbon-carbon bond or oxygen atom; or R and R and/or R and R respectively stand together for a carbonyl group, a C1-C4 alkylidene group or if required an oxirane group substituted by a C1-C3 alkyl group. Also disclosed are the salts of these derivatives with physiologically tolerable acids, their alpha -, beta - or gamma -cyclodextrin clathrates and compounds of general formula (I) encapsulated in liposomes.
摘要:
The invention relates to borneol derivatives of the general formula (I) in which R is C(O)-CH(OR )-CH(NHR )-R , R is hydrogen, -OH, C1-C10-Alkyl, C1-C10-alkoxy, -OC(O)R , -OP(O)(OH)2 or R and R are together an oxygen atom, R is hydrogen, C1-C10-alkyl, -(CH2)n-OR , R is hydrogen, C1-C10-alkyl, -(CH2)p-OR , or R and R together are an oxygen atom, a =CHR group, n is 0 to 8, p is 1 to 8, R is -C(O)R , -SO2R , -C(O)NHR , -C(O)NR R , (formula), R is aryl, R and R are the same or different and represent C1-C10-akyl, C4-C8-cycloalkyl, aryl, C7-C16-aralkyl, R is hydrogen, C1-C10-alkyl, -(CH2)s-OR , s is 1 to 8, R , R and R are the same or different and represent hydrogen, C1-C10-alkyl, aryl, C7-C16 aralkyl, SO2R , -P(O)(OH)2, R and R are the same or different and represent hydrogen, C1-C10-alkyl, aryl, C7-C16-aralkyl, X and X are the same or different and mean X, X may be hydrogen, halogen, -OH, -NO2, -N3, -CN, -NR R , -NHSO2R , -CO2R , C1-C10-alkyl, C1-C10-alkoxy, C1-C10-acyloxy, C1-C10-acyl and, if R is hydrogen, their salts with physiologically tolerable bases, and alpha -, beta - or gamma -cyclodextrin clathrates, and the compounds of the general formula (I) encapsulated with liposomes.