Provided herein are conjugates of nucleoside antimetabolites and their analogs with ibandronate, pharmaceutical compositions including one or more of said conjugates, methods of synthesizing the same as well as methods of treating diseases and or conditions using the same.
Provided herein is a novel method for creating fixed, non-antagonistic molar ratios of drugs in and around the bone environment for desired periods of time. This method enables treating bone and bone-related disease by administering a pharmaceutical composition comprising a bone-targeted therapeutic agent able to release a drug payload from the bone surface, in addition to a second therapeutic agent. Such methods are useful in the treatment of bone and bone-related diseases, such as cancer-induced bone disease, osteomyelitis and bone infection, bone pain and inflammatory bone disease, metabolic disease, as well as others.
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
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 35/04 - Antineoplastic agents specific for metastasis
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
Provided herein are conjugates of nucleoside antimetabolites and their analogs with ibandronate, pharmaceutical compositions including one or more of said conjugates, methods of synthesizing the same as well as methods of treating diseases and or conditions using the same.
C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
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
A61K 31/7042 - Compounds having saccharide radicals and heterocyclic rings
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 35/04 - Antineoplastic agents specific for metastasis
C07H 19/04 - Heterocyclic radicals containing only nitrogen as ring hetero atom
Provided herein are conjugates of nucleoside antimetabolites and their analogs with ibandronate, pharmaceutical compositions including one or more of said conjugates, methods of synthesizing the same as well as methods of treating diseases and or conditions using the same.
Provided herein is a novel method for creating fixed, non-antagonistic molar ratios of drugs in and around the bone environment for desired periods of time. This method enables treating bone and bone-related disease by administering a pharmaceutical composition comprising a bone-targeted therapeutic agent able to release a drug payload from the bone surface, in addition to a second therapeutic agent. Such methods are useful in the treatment of bone and bone-related diseases, such as cancer-induced bone disease, osteomyelitis and bone infection, bone pain and inflammatory bone disease, metabolic disease, as well as others.
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
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 31/663 - Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
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
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 35/04 - Antineoplastic agents specific for metastasis
6.
DRUG COMBINATION TREATMENTS USING BONE-TARGETING THERAPEUTICS FOR BONE AND BONE-RELATED DISEASE
Provided herein is a novel method for creating fixed, non-antagonistic molar ratios of drugs in and around the bone environment for desired periods of time. This method enables treating bone and bone-related disease by administering a pharmaceutical composition comprising a bone-targeted therapeutic agent able to release a drug payload from the bone surface, in addition to a second therapeutic agent. Such methods are useful in the treatment of bone and bone-related diseases, such as cancer-induced bone disease, osteomyelitis and bone infection, bone pain and inflammatory bone disease, metabolic disease, as well as others.
The present invention provides novel bisphosphonate conjugates, pharmaceutical compositions comprising bisphosphonate conjugates and methods of using such analogs in the treatment of bone cancer, bone-related diseases, bone infection, bone inflammation, and diseases of the soft tissues surrounding bones.
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 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
C07F 9/6512 - Six-membered rings having the nitrogen atoms in positions 1 and 3
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
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C07H 19/207 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine-adenine dinucleotide or nicotinamide-adenine dinucleotide
A61K 31/7028 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/546 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine containing further heterocyclic rings, e.g. cephalothin
A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
8.
Vitamin B6 derivatives of nucleotides, acyclonucleotides and acyclonucleoside phosphonates
A01N 43/04 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom
C12N 5/00 - Undifferentiated human, animal or plant cells, e.g. cell linesTissuesCultivation or maintenance thereofCulture media therefor
C12N 5/02 - Propagation of single cells or cells in suspensionMaintenance thereofCulture media therefor
C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C07H 19/23 - Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups
C07H 19/19 - Purine radicals with arabinosyl as the saccharide radical
9.
VITAMIN B6 DERIVATIVES OF NUCLEOTIDES, ACYCLONUCLEOTIDES AND ACYCLONUCLEOSIDE PHOSPHONATES
Compounds, compositions, and methods of using them to treat infections, neoplastic disease, inflammatory disease, and pain. Such compounds are nucleotides, acydonucleotides, and acydic nucleoside phosphonates (ANP) phosphonates conjugated with forms and/or moieties of Vitamin B6 for delivery past the cell membrane and into the cell. Methods of delivering nucleotides, acydonucleotide and ANPs to the inside of the cell by conjugating said compounds with forms and/or moieties of Vitamin B6.
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
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
Compounds, compositions, and methods of using them to treat infections, neoplastic disease, inflammatory disease, and pain. Such compounds are nucleotides, acydonucleotides, and acydic nucleoside phosphonates (ANP) phosphonates conjugated with forms and/or moieties of Vitamin B6 for delivery past the cell membrane and into the cell. Methods of delivering nucleotides, acydonucleotide and ANPs to the inside of the cell by conjugating said compounds with forms and/or moieties of Vitamin B6.
The present invention provides novel bisphosphonate conjugates, pharmaceutical compositions comprising bisphosphonate conjugates and methods of using such analogs in the treatment of bone cancer, bone-related diseases, bone infection, bone inflammation, and diseases of the soft tissues surrounding bones.