The invention relates to the field of cancer therapy. In particular, a highly effective chemotherapy is provided in the form of liposome-encapsulated 2-deamino-2-pyrrolino-daunorubicin, which has been found to eliminate cancer cells and to support overall survival without causing severe undesired effects in mouse models of different types of cancer.
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
SYNTHESIS OF α,β-UNSATURATED CARBONYLS FROM ALKENES VIA SULFONIUM INTERMEDIATES AND THEIR APPLICATION IN THE SYNTHESIS OF CONJUGATED DIENE PHEROMONES, KAIROMONES, AND RELATED COMPOUNDS
α,β-Unsaturated aldehydes are useful products as such in agrochemistry, but also potential intermediates for the preparation of important insect pheromones and kairomones. Until now, primarily the thermodynamically more stable (E)-α,β-unsaturated aldehydes have been identified as useful intermediates in the production of conjugated diene pheromone compounds, however, their practical and cost-effective synthesis on an industrial scale remains challenging. The problem to be solved by the present invention is to provide a method for selective oxidation of alkenes to α,β-unsaturated carbonyls which can be further transformed into pheromones and kairomones preferably without isolation and significant loss of the existing stereochemical purity.
C07C 45/56 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds from heterocyclic compounds
C07C 51/373 - Preparation of carboxylic acids or their salts, halides, or anhydrides by reactions not involving formation of carboxyl groups by introduction of functional groups containing oxygen only in doubly bound form
C07C 67/29 - Preparation of carboxylic acid esters by modifying the hydroxylic moiety of the ester, such modification not being an introduction of an ester group by introduction of oxygen-containing functional groups
C07C 67/313 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by introduction of doubly bound oxygen containing functional groups, e.g. carboxyl groups
C07C 253/30 - Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
C07C 309/73 - Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
C07D 209/48 - Iso-indolesHydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
C07D 309/06 - Radicals substituted by oxygen atoms
C07C 47/21 - Unsaturated compounds having —CHO groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
C07C 47/228 - Unsaturated compounds having —CHO groups bound to acyclic carbon atoms containing six-membered aromatic rings, e.g. phenylacetaldehyde
C07C 47/225 - Unsaturated compounds having —CHO groups bound to acyclic carbon atoms containing rings other than six-membered aromatic rings
C07C 47/277 - Unsaturated compounds having —CHO groups bound to acyclic carbon atoms containing ether groups, groups, groups, or groups
C07C 47/26 - Unsaturated compounds having —CHO groups bound to acyclic carbon atoms containing hydroxy groups
C07C 47/24 - Unsaturated compounds having —CHO groups bound to acyclic carbon atoms containing halogen
C07C 49/597 - Unsaturated compounds containing a keto group being part of a ring of a five-membered ring
C07C 49/603 - Unsaturated compounds containing a keto group being part of a ring of a six-membered ring, e.g. quinone methides
C07C 49/607 - Unsaturated compounds containing a keto group being part of a ring of a seven- to twelve-membered ring
C07C 59/74 - Unsaturated compounds containing —CHO groups
C07C 69/73 - Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
C07C 255/17 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and doubly-bound oxygen atoms bound to the same acyclic carbon skeleton
The present invention relates to visible light sensitive photoremovable protecting groups and their parent compounds X including a xanthene, xanthenium or related cores, represented by formula (Xa): (Xa) wherein the substituents are as defined in the description. The invention also relates to a process for the preparation of compounds of formula (Xa). Said compounds are parent compounds of visible light sensitive photoremovable protecting groups. They can be attached to any desired chemically or biologically active agent either via a covalent bond, or a linker. In the resulting conjugates the active agent is rendered inactive (or less active). Irradiation of such photoactivatable conjugates with visible light leads to the release of the agent with restored biological activity. Therefore, invention further relates to photoactivatable conjugates and pharmaceutical compositions containing them, which are suitable for use e.g. in photoactivated therapy.
C07D 207/46 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
C07D 295/096 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
C07C 213/00 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
4.
SELECTIVE FLUORESCENT PROBES FOR MEASURING MULTIDRUG TRANSPORTER ACTIVITY
Selective fluorescent probes for measuring multidrug transporter activity The present invention relates to a fluorescent dye accumulation assay for parallel measurements of ABC multidrug transporters, as efflux pump, capable of extruding cyanine dyes. In particular, the invention relates to measurements of the ABCB1 multidrug transporter functions via detecting accumulation of the fluorescent dye in a cell. The invention also includes a diagnostic application of the functional assays in normal and malignant human cells, preferably blood cells.
The invention relates to algal extracellular vesicles (EVs) for use in therapy and in restoring or maintaining health of a subject. In particular the invention relates to uses of algal EVs in therapy, wherein the EVs themselves have favourable effects for the health of the subject to whom they are administered. In particular the algal EV s are for use in therapy in conditions or disorders associated with cell proliferation, and/or cell migration and/or non-physiological ECM production and deposition. The disorders also include in particular inflammation, neoplastic disorders, fibroproliferative diseases and the like. The invention also relates to methods of treatment of the subject as well as pharmaceutical and nutraceutical compositions. The invention also relates to cosmetic methods wherein algal EVs are applied to the affected skin.
alphaalpha alpha alpha-olefins - namely, the homogeneous or heterogeneous catalytic ethenolysis by using a ruthenium complex metathesis catalyst (i.e., metathesis using excess ethylene or ethylene metathesis), and/or tandem isomerization and metathesis reactions by using homogeneous or heterogenized homogeneous ruthenium complex metathesis catalyst in combination with a homogeneous or heterogeneous olefin isomerization catalyst (i.e., isomerization metathesis, hereinafter referred to as ISOMET), and/or tandem isomerization and ethylene metathesis by using a homogeneous or heterogenized homogeneous ruthenium complex metathesis catalyst in combination with homogeneous or heterogeneous olefin isomerization catalyst (i.e., isomerization ethylene metathesis, hereinafter referred to as ethylene ISOMET).
The invention relates to cancer biology, more specifically to the treatment of KRAS mutant cancers. A potent cancer therapy is provided by the combination of a farnesyl transferase inhibitor compound and a KRAS inhibitor compound.
The invention relates to the field of cancer therapy. In particular, a highly effective chemotherapy is provided in the form of liposome-encapsulated 2-deamino-2-pyrrolino-daunorubicin, which has been found to eliminate cancer cells and to support overall survival without causing severe undesired effects in mouse models of different types of cancer.
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
The invention relates to the application of a skin patch test for the detection of the specific cellular immune response against the SARS-CoV-2 (Severe Acute Respiratory Syndrome Coronavirus-2). The skin patch contains a formulated version of the recombinant form of SARS-CoV-2 antigenic protein. The application of the skin patch allows to follow the local skin reaction reflecting the strength of the cellular immune reaction against SARS-CoV-2, thus the skin test is applicable to a diagnostic evaluation of the specific cellular immunity evoked by previous virus infection or by vaccination against COVID-19.
ABC multidrug transporters are key players in cancer multidrug resistance and in general xenobiotic elimination, thus their functional assays provide important tools for research and diagnostic applications. It has been found that in cells expressing functional ABCG2, ABCB1, or ABCC1 transporters, cellular PG fluorescence is strongly reduced. The invention relates to methods and uses of fluorescein derivative ester compounds of formula Ia which are analogs of PG for assessing ABC transporter activity of ABC multidrug transporters. The present accumulation assay is a novel tool for the parallel determination of the function of the multidrug transporters, in particular ABCG2, ABCB1, and ABCC1. The assay is applicable for diagnostic purposes and also allows the selection, separation and culturing of selected cell populations expressing such transporters.
The invention relates to cancer biology, more specifically to the treatment of KRAS mutant cancers. A potent cancer therapy is provided by the combination of a farnesyl transferase inhibitor compound and a KRAS inhibitor compound.
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