The present invention is directed to oligonucleotide conjugates, pharmaceutical compositions comprising same and to methods for use thereof, such as for the treatment and/or prevention of a genetic disease, or a viral disease in a subject.
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
2.
PEPTIDE TRANS-MEMBRANE DELIVERY SYSTEMS AND USES THEREOF
The present invention is directed to peptide conjugates of the invention, pharmaceutical composition comprising same and to methods for use thereof, such as for the treatment and/or prevention of a disease in a subject.
A61K 47/50 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
A61K 47/50 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
The present invention is directed to oligonucleotide conjugates, pharmaceutical compositions comprising same and to methods for use thereof, such as for the treatment and/or prevention of a genetic disease, or a viral disease in a subject.
A61K 47/50 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
5.
Compounds and methods for trans-membrane delivery of molecules
The Invention provides a novel delivery system for delivery of drugs across biological membranes. It provides novel chemical conjugates that comprise said delivery system, methods for synthesis of said compounds, and methods for utilization of said delivery system, among others, for delivery of genetic drugs into tissues and cells, in vitro, ex vivo, and in vivo, for the treatment of various medical disorders.
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
6.
Compounds and methods for trans-membrane delivery of molecules
A system for delivery of drugs, and especially genetic drugs such as siRNA or antisense oligonucleotides (ASO) across biological membranes is provided. It comprises a trans-membrane delivery moiety, energized by the membrane internal electrical field, and a redox-sensitive disulfide moiety, designed to be reduced at the cytoplasm, thus releasing the cargo drug to exert its pharmaceutical effects at its target sites.
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
7.
COMPOUNDS, COJUGATES AND COMPOSITIONS FOR USE IN THE METHODS FOR TRANS-MEMBRANE DELIVERY OF MOLECULES
The invention provides a system for the delivery of dmgs across biological membranes, including conjugates thereof, processes for their preparation and methods for their use.
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
8.
COMPOUNDS AND METHODS FOR TRANS-MEMBRANE DELIVERY OF MOLECULES
A61K 47/28 - Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
9.
COMPOUNDS AND METHODS FOR TRANS-MEMBRANE DELIVERY OF MOLECULES
The Invention provides a novel delivery system for delivery of drugs across biological membranes. It provides novel chemical conjugates that comprise said delivery system, methods for synthesis of said compounds, and methods for utilization of said delivery system, among others, for delivery of genetic drugs into tissues and cells, in vitro, ex vivo, and in vivo, for the treatment of various medical disorders.
A61K 47/28 - Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
10.
Compounds and methods for trans-membrane delivery of molecules
A conjugate for delivery of drugs, such as genetic drugs, [e.g., siRNA, dsiRNA, or antisense oligonucleotides (ASO)] across biological membranes is provided. The conjugates of the Invention are capable of delivering drugs in both presence and absence of plasma proteins.
A61K 47/08 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
11.
COMPOUNDS AND METHODS FOR TRANS-MEMBRANE DELIVERY OF MOLECULES
A conjugate for delivery of drugs, such as genetic drugs, [e.g., siRNA, dsiRNA, or antisense oligonucleotides (ASO)] across biological membranes is provided. The conjugates of the Invention are capable of delivering drugs in both presence and absence of plasma proteins.
A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
A61K 47/28 - Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
12.
COMPOUNDS AND METHODS FOR TRANS-MEMBRANE DELIVERY OF MOLECULES
A conjugate for delivery of drugs, such as genetic drugs, [e.g., siRNA, dsiRNA, or antisense oligonucleotides (ASO)] across biological membranes is provided. The conjugates of the Invention are capable of delivering drugs in both presence and absence of plasma proteins.
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
13.
Compounds and methods for trans-membrane delivery of molecules
A novel delivery system for drugs, and especially macromolecules such as proteins or oligonucleotides through biological membranes is provided, and specifically delivery of siRNA. The delivery system comprises conjugation of the macromolecule drug to a moiety that enables effective passage through the membranes. Respectively, novel compounds and pharmaceutical compositions are provided, utilizing said delivery system. In one aspect of the invention, the compounds may be utilized in medical practice, for example, in delivery of siRNA or antisense oligonucleotides across biological membranes for the treatment of medical disorders.
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
C07J 9/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
C07J 51/00 - Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups
C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
The invention relates to Pro-drugs, comprising red-ox-sensitive cleavage sites. The compounds may be utilized in medical practice for targeting of si RNA, antisense oligonucleotides or protein-based therapeutics to the cytoplasmatic compartment of cells both in vitro or in vivo, in a subject in need.
C07C 271/56 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
A system for delivery of drugs, and especially genetic drugs such as siRNA or antisense oligonucleotides (ASO) across biological membranes is provided. It comprises a trans- membrane delivery moiety, energized by the membrane internal electrical field, and a redox-sensitive disulfide moiety, designed to be reduced at the cytoplasm, thus releasing the cargo drug to exert its pharmaceutical effects at its target sites.
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
C12N 15/87 - Introduction of foreign genetic material using processes not otherwise provided for, e.g. co-transformation
16.
COMPOUNDS AND METHODS FOR TRANS-MEMBRANE DELIVERY OF MOLECULES
A system for delivery of drugs, and especially genetic drugs such as siRNA or antisense oligonucleotides (ASO) across biological membranes is provided. It comprises a trans- membrane delivery moiety, energized by the membrane internal electrical field, and a redox-sensitive disulfide moiety, designed to be reduced at the cytoplasm, thus releasing the cargo drug to exert its pharmaceutical effects at its target sites.
A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
17.
Compounds and methods for trans-membrane delivery of molecules
A novel delivery system for drugs, and especially macromolecules such as proteins or oligonucleotides through biological membranes is provided, and specifically delivery of siRNA. The delivery system comprises conjugation of the macromolecule drug to a moiety that enables effective passage through the membranes. Respectively, novel compounds and pharmaceutical compositions are provided, utilizing said delivery system. In one aspect of the invention, the compounds may be utilized in medical practice, for example, in delivery of siRNA or antisense oligonucleotides across biological membranes for the treatment of medical disorders.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
A61K 47/28 - Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
A novel delivery system for drugs, and especially macromolecules such as proteins or oligonucleotides through biological membranes is provided, and specifically delivery of siRNA. The delivery system comprises conjugation of the macromolecule drug to a moiety that enables effective passage through the membranes. Respectively, novel compounds and pharmaceutical compositions are provided, utilizing said delivery system. In one aspect of the invention, the compounds may be utilized in medical practice, for example, in delivery of siRNA or antisense oligonucleotides across biological membranes for the treatment of medical disorders.
A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
The invention relates to Pro-drugs, comprising red-ox-sensitive cleavage sites. The compounds may be utilized in medical practice for targeting of si RNA, antisense oligonucleotides or protein-based therapeutics to the cytoplasmatic compartment of cells both in vitro or in vivo, in a subject in need.
A novel delivery system for drugs, and especially macromolecules such as proteins or oligonucleotides through biological membranes is provided, and specifically delivery of siRNA The delivery system comprises conjugation of the macromolecule drug to a moiety that enables effective passage through the membranes. Respectively, novel compounds and pharmaceutical compositions are provided, utilizing said delivery system. In one aspect of the invention, the compounds may be utilized in medical practice, for example, in delivery of siRNA or antisense oligonucleotides across biological membranes for the treatment of medical disorders.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
C07F 9/6553 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
C07J 9/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
C07J 51/00 - Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
21.
Compounds and methods for trans-membrane delivery of molecules
A novel delivery system for drugs, and especially macromolecules such as proteins or oligonucleotides through biological membranes is provided, and specifically delivery of siRNA The delivery system comprises conjugation of the macromolecule drug to a moiety that enables effective passage through the membranes. Respectively, novel compounds and pharmaceutical compositions are provided, utilizing said delivery system. In one aspect of the invention, the compounds may be utilized in medical practice, for example, in delivery of siRNA or antisense oligonucleotides across biological membranes for the treatment of medical disorders.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
C07J 51/00 - Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
C12N 9/96 - Stabilising an enzyme by forming an adduct or a compositionForming enzyme conjugates
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
C12N 15/87 - Introduction of foreign genetic material using processes not otherwise provided for, e.g. co-transformation
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
C07J 9/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
22.
COMPOUNDS AND METHODS FOR TRANS-MEMBRANE DELIVERY OF MOLECULES
A novel delivery system for macromolecules such as proteins and oligonucleotides, and specifically siRNA through biological membranes is provided, comprising conjugation of the macromolecule to a moiety, which enables effective crossing through the membranes. Respectively, novel compounds and pharmaceutical compositions are provided, utilizing said delivery system. In one aspect of the invention, the compounds may be utilized in medical practice, for example, in delivery of siRNA or antisense oligonucleotides across biological membranes for the treatment of medical disorders.
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
C07C 22/02 - Cyclic compounds containing halogen atoms bound to an acyclic carbon atom having unsaturation in the rings
C07C 13/66 - Polycyclic hydrocarbons or acyclic hydrocarbon derivatives thereof with condensed rings with more than three condensed rings the condensed ring system contains only four rings
23.
COMPOUNDS AND METHODS FOR TRANS-MEMBRANE DELIVERY OF MOLECULES
A novel delivery system for macromolecules such as proteins and oligonucleotides, and specifically siRNA through biological membranes is provided, comprising conjugation of the macromolecule to a moiety, which enables effective crossing through the membranes. Respectively, novel compounds and pharmaceutical compositions are provided, utilizing said delivery system. In one aspect of the invention, the compounds may be utilized in medical practice, for example, in delivery of siRNA or antisense oligonucleotides across biological membranes for the treatment of medical disorders.
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
C07J 5/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane, and substituted in position 21 by only one singly bound oxygen atom
C07J 9/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice for treating pancreatic cancer.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
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
Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice, for example, in treatment of cancer and immune disorders.
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
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
26.
NOVEL TARGETING AGENTS FOR DIAGNOSTIC AND THERAPEUTIC INDICATIONS
The invention relates to compounds and use thereof in the diagnosis and/or in treatment of medical disorders. In some embodiments, the compounds may be used for detecting a cancer. The compound may include a di-acid moiety. In some embodiments the di-acid moiety comprises a di-carboxylic acid and in some embodiments the di- acid moiety comprises a di-tetrazole.
Substituted alkyl methyl malonate compounds are produced in an essentially one step method, the method suitable for large scale production of alkyl malonate compounds. According to one embodiment the method comprises reacting a methyl malonate with a di-functional, doubly tosylated, alkyl chain.
Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice, for example, in treatment of cancer and immune disorders.
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice, for example, in treatment of cancer and immune disorders.
Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice, for example, in treatment of cancer and immune disorders.
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
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
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice, for example, in treatment of cancer and immune disorders. In another aspect of the invention there is provided a conjugate, comprising a cytotoxic agent and a modulating moiety, the modulating moiety serving to target apoptotic cells.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
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
The invention relates to compounds comprising an ester group for the detection in vivo of cells undergoing cell death ('dying cells') such as, for example, cells undergoing apoptosis. These compounds are selectively retained in dying cells relative to normal cells. Thus, the compounds may be used in the detection, diagnosis and treatment of clinical conditions manifested by a cell death process.
A61B 5/055 - Detecting, measuring or recording for diagnosis by means of electric currents or magnetic fieldsMeasuring using microwaves or radio waves involving electronic [EMR] or nuclear [NMR] magnetic resonance, e.g. magnetic resonance imaging
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations, substances and agents; pharmaceutical agents for use in connection with detection, imaging, diagnosing, monitoring and treating medical disorders and diseases, namely, cancer, neurological disorders, multiple sclerosis, heart disease, atherosclerosis, cerebral stroke and traumatic brain injury, liver cirrhosis, renal failure, and solid organ transplantation; pharmaceutical preparations and diagnostic compositions for in vitro and in vivo recognition, targeting, and imaging of cells undergoing cell death.
