75383-60-7Relevant academic research and scientific papers
12-EPI PLEUROMUTILINS
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Paragraph 0464, (2016/12/01)
A compound selected from 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-sulfanyl)-acetyl]-12-epi-mutilins, or 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-oxy)-acetyl]-12-epi-mutilins, wherein 12-epi-mutilin is characterized in that the mutilin ring at position 12 is substituted by two substituents, the first substituent at position 12 of the mutilin ring is a methyl group which methyl group has the inverse stereochemistry compared with the stereochemistry of the methyl group at position 12 of the naturally occurring pleuromutilin ring, the second substituent at position 12 of the mutilin ring is a hydrocarbon group comprising at least one nitrogen atom and all other substituents of the mutilin ring having the same stereochemistry compared with the stereochemistry of the substituents at the corresponding positions in the naturally occurring pleuromutilin ring; optionally in the form of a salt and/or solvate, wherein the naturally occurring pleuromutilin is of formula processes for the preparation of such compounds and their use as pharmaceuticals.
12-EPI-PLEUROMUTILINS
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Page/Page column 71; 72, (2015/08/06)
A compound selected from 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-sulfanyl)-acetyl]-12-epi-mutilins, or 14-0-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-oxy)-acetyl]-12-epi-mutilins, wherein 12-epi-mutilin is characterized in that the mutilin ring at position 12 is substituted by two substituents, the first substituent at position 12 of the mutilin ring is a methyl group which methyl group has the inverse stereochemistry compared with the stereochemistry of the methyl group at position 12 of the naturally occurring pleuromutilin ring, the second substituent at position 12 of the mutilin ring is a hydrocarbon group comprising at least one nitrogen atom and all other substituents of the mutilin ring having the same stereochemistry compared with the stereochemistry of the substituents at the corresponding positions in the naturally occurring pleuromutilin ring; optionally in the form of a salt and/or solvate, wherein the naturally occurring pleuromutilin is of formula PLEU, processes for the preparation of such compounds and their use as pharmaceuticals.
PTERIDINE DERIVATIVES AS POLO-LIKE KINASE INHIBITORS USEFUL IN THE TREATMENT OF CANCER
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Page/Page column 42, (2008/12/05)
Compound of formula (I) are inhibitors of Polo-like kinases (PLKs), and are useful in treatment of cell proliferative diseases: wherein R1 and R2 are hydrogen, or an optionally substituted (C1-C6)alkyl, (C2- Cs
HYDROXAMIC ACID DERVICATIVES AS INHIBITORS OF HDAC ENZYMATIC ACTIVITY
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Page/Page column 62-63, (2008/06/13)
Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: formula (I) wherein Y1 is a bond, -(C=O)-, -S(O2)-, -C(=O)O-, -OC(=O)-, -(C=O)NR3, -NR3(C=O)-, -S(O2)NR3-, -NR3S(O2)-, or -NR3(C=O)NR5-, wherein R3 and R5 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, AIk1, AIk2 and Q are as defined in the claims; z is O or 1 ; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker]- represents a divalent linker radical; R is a radical of formula (X) or (Y); wherein R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, -(C=O)R3, -(C=O)OR3, or -(C=O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, or heteroary(C1-C6 alkyl)-; R41 is hydrogen or optionally substituted C1-C6 alkyl; and B is a monocyclic heterocyclic ring of 5 or 6 ring atoms wherein R1 is linked to a ring carbon adjacent the ring nitrogen shown, and ring B is optionally fused to a second carbocyclic or heterocyclic ring of 5 or 6 ring atoms in which case the bond shown intersected by a wavy line may be from a ring atom in said second ring.
Synthesis of active principles from the leaves of Moringa oleifera using S-pent-4-enyl thioglycosides
Leuck, Michael,Kunz, Horst
, p. 33 - 44 (2007/10/03)
α-l-Rhamnosides of 4-hydroxy-benzyl compounds with nitrile, carbamate, and thiocarbamate groups occurring in Moringa oleifera leaf extracts and the α-l-rhamnoside of anisaldehyde derivatives were synthesised. Electrophilic activation of S-pent-4-enyl thiorhamnosides was applied for the construction of glycosidic linkages. Copyright (C) 1997 Elsevier Science Ltd.
Efficient Tryptic Hydrolysis of Aryl Esters with a Cationic Center in the Leaving Group. Further Characterization of "Inverse Substrates"
Nakano, Michiharu,Tanizawa, Kazutaka,Nozawa, Masayuki,Kanaoka, Yuichi
, p. 2212 - 2215 (2007/10/02)
The kinetic properties of esters derived from guanidinophenol and aminomethylphenol were investigated with trypsin.These compounds, in which the site-specific groups (positive charge) are of inverse type compared with normal substrates, were demonstrated to be specific substrates, like aminophenyl esters.The behavior of these "inverse substrates" with trypsin and pseudotrypsin was also compared.A dramatic decrease in the efficiency of hydrolysis of the "inverse substrates" by pseudotrypsin as compared to that by trypsin was observed, which was comparable in extent to that observed for specific normal-type substrates.All these observations confirm the view that specific interaction between the positive charge at the leaving moiety of "inverse substrates" and the anionic site of the trypsin active center is an essential feature of the catalysis, just as in the case of normal-type substrates.
