CD33 ligands which are useful for the synthesis of CD33 ligand-bearing carriers, wherein said CD33 ligand-bearing carriers are directly or indirectly linked to or associated with at least one anti-cancer agent, are described herein. Uses of said CD33 ligand-bearing carriers for treating and/or preventing a disease, disorder, or condition such as acute myeloid leukemia (AML) are also described.
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 47/69 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
C07H 1/00 - Processes for the preparation of sugar derivatives
C07H 17/02 - Heterocyclic radicals containing only nitrogen as ring hetero atoms
Compounds of formula (I), compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of galectin-3 to ligands are disclosed. For example, inhibitors of galectin-3 are described and pharmaceutical compositions comprising at least one such agent are described.
Compounds of formula (I), compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of galectin-3 to ligands are disclosed. For example, inhibitors of galectin-3 are described and pharmaceutical compositions comprising at least one such agent are described.
C07H 17/02 - Heterocyclic radicals containing only nitrogen as ring hetero atoms
C07H 5/10 - Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium to sulfur, selenium, or tellurium to sulfur
C07H 9/02 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing only oxygen as ring hetero atoms
3.
COMPOSITIONS AND METHODS FOR OVERCOMING MICROENVIRONMENT-MEDIATED RESISTANCE VIA E-SELECTIN TARGETING
Methods for treating a cancer (such as, e.g., acute myeloid leukemia) comprising administering to a subject (such as, e.g., a subject who has acquired resistance to a therapy comprising at least one antineoplastic agent and/or at least one hypomethylating agent) at least one E-selectin antagonist, wherein the subject is further administered at least one antineoplastic agent (such as, e.g., venetoclax) and/or at least one hypomethylating agent are disclosed.
A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
A61K 31/706 - 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
A61P 35/02 - Antineoplastic agents specific for leukemia
Compounds of formula (I), compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of galectin-3 to a ligand are disclosed. For example, inhibitors of galectin-3 are described and pharmaceutical compositions comprising at least one such inhibitor are described.
Compounds of formula (I), compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of galectin-3 to a ligand are disclosed. For example, inhibitors of galectin-3 are described and pharmaceutical compositions comprising at least one such inhibitor are described.
C07D 405/04 - 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 directly linked by a ring-member-to-ring- member bond
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, E-selectin antagonists are described and pharmaceutical compositions comprising at least one of the same.
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
6.
HETEROBIFUNCTIONAL INHIBITORS OF E-SELECTIN AND GALECTIN-3
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin, galectin-3, or E-selectin and galectin-3 to ligands are disclosed. For example, heterobifunctional inhibitors of E-selectin and galectin-3 are described and pharmaceutical compositions comprising at least one such agent is described.
A process is provided for the synthesis of an intermediate which is useful in the synthesis of E-selectin inhibitors. Also provided are useful intermediates obtained from the process.
Methods are disclosed for the mobilization of marrow infiltrating cells (MILs) using E-selectin antagonists for the treatment of disorders such as cancer. Methods for treating or preventing cancers using MILs mobilized by E-selectin antagonists are further disclosed.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
Methods for treating or inhibiting cancer and/or one or more related conditions by administering to a subject in need thereof an effective amount of a compound of Formula (I) a prodrug thereof or a pharmaceutically acceptable salt of any of the foregoing. For example, methods for treating AML, MDS, neutropenia, and/or mucositis comprising administering a pharmaceutical composition comprising a compound of Formula (I) are described.
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, highly potent multimeric E-selectin antagonist are dessorbed and pharmaceutical compositions comprising at least one of the same.
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61P 35/04 - Antineoplastic agents specific for metastasis
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
E-selectin ligands which are useful for the synthesis of E-selectin ligand-bearing carriers, wherein said E-selectin ligand-bearing carriers are directly or indirectly linked to or associated with at least one therapeutic agent, diagnostic agent, imaging agent, or radiopharmaceutical are described herein.
A61K 51/12 - Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes
Methods for treating a cancer (such as, e.g., acute myeloid leukemia) comprising administering to a subject (such as, e.g., a subject who has acquired resistance to a therapy comprising at least one antineoplastic agent and/or at least one hypomethylating agent) at least one E-selectin antagonist, wherein the subject is further administered at least one antineoplastic agent (such as, e.g., venetoclax) and/or at least one hypomethylating agent are disclosed.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61P 35/02 - Antineoplastic agents specific for leukemia
A61K 31/706 - 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
17.
CD33 LIGANDS SUITABLE FOR INCORPORATION INTO CARRIERS
CD33 ligands which are useful for the synthesis of CD33 ligand-bearing carriers, wherein said CD33 ligand-bearing carriers are directly or indirectly linked to or associated with at least one anti-cancer agent, are described herein. Uses of said CD33 ligand-bearing carriers for treating and/or preventing a disease, disorder, or condition such as acute myeloid leukemia (AML) are also described. The CD33 ligands have the structure of formula (I):
CD33 ligands which are useful for the synthesis of CD33 ligand-bearing carriers, wherein said CD33 ligand-bearing carriers are directly or indirectly linked to or associated with at least one anti-cancer agent, are described herein. Uses of said CD33 ligand-bearing carriers for treating and/or preventing a disease, disorder, or condition such as acute myeloid leukemia (AML) are also described. The CD33 ligands have the structure of formula (I):
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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
C07H 15/18 - Acyclic radicals, substituted by carbocyclic rings
C07H 15/203 - Monocyclic carbocyclic rings other than cyclohexane rings; Bicyclic carbocyclic ring systems
18.
CD33 LIGANDS SUITABLE FOR INCORPORATION INTO CARRIERS
CD33 ligands which are useful for the synthesis of CD33 ligand-bearing carriers, wherein said CD33 ligand bearing carriers are directly or indirectly linked to or associated with at least one anti-cancer agent, are described herein. Uses of said CD33 ligand-bearing carriers for treating and/or preventing a disease, disorder, or condition such as acute myeloid leukemia (AML) are also described. The ligands have formula (I) below.
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
C07H 15/18 - Acyclic radicals, substituted by carbocyclic rings
A61K 47/69 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
19.
COMPOUNDS AND METHODS FOR REDUCTION OF CANCER CELL BURDEN AND PROTECTION OF NORMAL HEMATOPOIESIS
Methods for treating cancer (such as, e.g., acute myelogenous leukemia), enhancing maintenance of normal hematopoiesis in bone marrow, and/or mobilizing leukemia blasts in a subject in need thereof comprising administering to the subject at least one FLT3 inhibitor and at least one inhibitor chosen from E-selectin inhibitors, CXCR4 inhibitors, and heterobifunctional inhibitors of E-selectin and CXCR4.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61P 35/02 - Antineoplastic agents specific for leukemia
A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
Methods for treating diseases, disorders, and/or conditions associated with COVID-19 comprising administering at least one E-selectin antagonist and/or composition comprising the same are disclosed. Also disclosed are compounds, compositions, and methods for treating patients with acute respiratory distress syndrome.
A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 31/7068 - 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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 39/215 - Coronaviridae, e.g. avian infectious bronchitis virus
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 11/00 - Drugs for disorders of the respiratory system
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
A61K 31/7032 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a polyol, i.e. compounds having two or more free or esterified hydroxy groups, including the hydroxy group involved in the glycosidic linkage, e.g. monoglucosyl-diacylglycerides, lactobionic acid, gangliosides
21.
COMBINATION OF T-CELL CHECKPOINT INHIBITORS WITH INHIBITORS OF E-SELECTIN OR CXCR4, OR WITH HETEROBIFUNCTIONAL INHIBITORS OF BOTH E-SELECTIN AND CXCR4
Compositions and methods for the treatment of diseases, disorders, and/or conditions associated with the increased regulatory T lymphocyte cell function, comprising the administration of T-cell checkpoint inhibitors in combination with E-selectin inhibitors, C-X-C Motif Chemokine Receptor 4 (CXCR4) receptor inhibitors, and/or heterobifunctional inhibitors that comprise at least one E-selectin inhibitor linked to at least one CXCR4 receptor inhibitor, are disclosed.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 47/61 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid (GABA), beta-alanine, epsilon-aminocaproic acid, pantothenic acid
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/702 - Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
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 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
22.
E-selectin antagonist compounds, compositions, and methods of use
Methods and compositions using E-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of E-selectin to an E-selectin ligand. Described herein are E-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of galectin-3 to ligands are disclosed. For example, inhibitors of galectin-3 are described and pharmaceutical compositions comprising at least one such agent are described.
C07D 405/14 - 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 three or more hetero rings
C07D 405/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Compounds, compositions, and methods for treating and/or preventing at least one disease, disorder, and/or condition N associated with E-selectin, galectin-3, and/or CXCR4 chemokine receptor activity are disclosed herein. For example, multimeric glycomimetic inhibitors of E-selectins, galectin-3, and/or CXCR4 chemokine receptors and their use for treating and/or preventing inflammatory diseases, fibrosis, and cancers are disclosed. Formula (I).
Compounds, compositions, and methods for treating and/or preventing at least one disease, disorder, and/or condition N associated with E-selectin, galectin-3, and/or CXCR4 chemokine receptor activity are disclosed herein. For example, multimeric glycomimetic inhibitors of E-selectins, galectin-3, and/or CXCR4 chemokine receptors and their use for treating and/or preventing inflammatory diseases, fibrosis, and cancers are disclosed. Formula (I).
A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
A61K 31/706 - 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
Compounds of formula (I), compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of galectin-3 to ligands are disclosed. For example, inhibitors of galectin-3 are described and pharmaceutical compositions comprising at least one such agent are described.
C07D 405/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 405/14 - 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 three or more hetero rings
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 25/00 - Drugs for disorders of the nervous system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Compounds of formula (I), compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of galectin-3 to a ligand are disclosed. For example, inhibitors of galectin-3 are described and pharmaceutical compositions comprising at least one such inhibitor are described.
C07D 405/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 405/14 - 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 three or more hetero rings
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 25/00 - Drugs for disorders of the nervous system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
A process is provided for the synthesis of an intermediate of Formula 15 which is useful in the synthesis of E-selectin inhibitors. Also provided are useful intermediates obtained from the process.
A process is provided for the synthesis of an intermediate which is useful in the synthesis of E-selectin inhibitors. Also provided are useful intermediates obtained from the process.
Cancer patients that express high levels of the E-selectin ligand (sialyl Lea/x) on their tumors have a poorer outcome. Interestingly, relapsed/refractory acute myeloid leukemia (AML) patients expressing high levels of sialyl Lex on their blasts show the greatest therapeutic response when treated with the E-selection inhibitor compound of Formula I. Transcriptome profiling of E-selectin ligand-forming glycosylation genes showed that ST3GAL4 and FUT7 were consistently expressed in the majority of cancers evaluated. Poor survival outcomes of FLT3-mutated AML patients that express high levels of ST3GAL4 and FUT7 implicated E-selectin in this disease state. These genes may be predictive biomarkers in AML patients. Methods of treatment of cancer comprising screening AML patients for expression of genes that contribute to the synthesis of the E-selectin ligand sialyl Lex, then treating those patients with an E-selection inhibitor, are disclosed.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
G01N 33/574 - Immunoassay; Biospecific binding assay; Materials therefor for cancer
A process is provided for the synthesis of an intermediate which is useful in the synthesis of E-selectin inhibitors. Also provided are useful intermediates obtained from the process.
Hematopoietic stem cell (HSC) transplantation is a promising treatment for patients with various hematological diseases, immunodeficiency, autoimmune disorders, and other genetic disorders. Considerable work continues to strive toward the identification of critical factors involved in the successful engraftment and reconstitution of HSC recipients. The identification of these critical components and the understanding of how they may be therapeutically targeted would result in improved patient survival. E-selectin inhibitors for use in increasing survival of individuals that receive HSC transplantation or for reconstitution of depleted and compromised bone marrow are disclosed.
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
A61K 31/7028 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
A61K 35/28 - Bone marrow; Haematopoietic stem cells; Mesenchymal stem cells of any origin, e.g. adipose-derived stem cells
Methods for the treatment of sickle cell disease or complications associated therewith, including, for example, vaso-occlusive crisis, by the use of at least one E-selectin inhibitor and compositions comprising the same are disclosed.
A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, E-selectin antagonists are described and pharmaceutical compositions comprising at least one of the same.
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
35.
Heterobifunctional inhibitors of E-selectin and galectin-3
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin, galectin-3, or E-selectin and galectin-3 to ligands are disclosed. For example, heterobifunctional inhibitors of E-selectin and galectin-3 are described and pharmaceutical compositions comprising at least one such agent is described.
E-selectin ligands which are useful for the synthesis of E-selectin ligand-bearing carriers,wherein said E-selectin ligand-bearing carriers are directly or indirectly linked to or associated with at least one therapeutic agent, diagnostic agent, imaging agent, or radiopharmaceutical are described herein.
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
C07H 15/23 - Cyclohexane rings, substituted by at least two nitrogen atoms with at least two saccharide radicals directly attached to the cyclohexane rings attached to adjacent ring-carbon atoms of the cyclohexane rings with only two saccharide radicals in the molecule, e.g. ambutyrosin, butyrosin, xylostatin, ribostamycin
C07H 1/00 - Processes for the preparation of sugar derivatives
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of galectin-3 to ligands are disclosed. For example, inhibitors of galectin-3 are described and pharmaceutical compositions comprising at least one such agent is described.
C07H 19/24 - Heterocyclic radicals containing oxygen or sulfur as ring hetero atom
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
38.
COMPOSITIONS AND METHODS FOR OVERCOMING MICROENVIRONMENT-MEDIATED RESISTANCE VIA E-SELECTIN TARGETING
Methods for treating a cancer (such as, e.g., acute myeloid leukemia) comprising administering to a subject (such as, e.g., a subject who has acquired resistance to a therapy comprising at least one antineoplastic agent and/or at least one hypomethylating agent) at least one E?selectin antagonist, wherein the subject is further administered at least one antineoplastic agent (such as, e.g., venetoclax) and/or at least one hypomethylating agent are disclosed.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 31/706 - 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
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
39.
CD33 LIGANDS SUITABLE FOR INCORPORATION INTO CARRIERS
CD33 ligands which are useful for the synthesis of CD33 ligand-bearing carriers, wherein said CD33 ligand-bearing carriers are directly or indirectly linked to or associated with at least one anti-cancer agent, are described herein. Uses of said CD33 ligand-bearing carriers for treating and/or preventing a disease, disorder, or condition such as acute myeloid leukemia (AML) are also described. The ligands have formula (I) below.
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
C07H 15/18 - Acyclic radicals, substituted by carbocyclic rings
A61P 35/02 - Antineoplastic agents specific for leukemia
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, highly potent multimeric E-selectin antagonist are desorbed and pharmaceutical compositions comprising at least one of the same.
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61P 35/04 - Antineoplastic agents specific for metastasis
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
The application relates to galectin-3 inhibitors of Formula (I), to pharmaceutical compositions comprising them, and their medical use for the treatment and/or prevention of diseases or disorders such as inflammatory diseases, fibrosis, neurodegeneration, thrombosis and cancer.
C07D 405/04 - 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 directly linked by a ring-member-to-ring- member bond
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
C07D 405/14 - 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 three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
42.
Methods of mobilizing marrow infiltrating lymphocytes and uses thereof
Methods are disclosed for the mobilization of marrow infiltrating cells (MILs) using E-selectin antagonists for the treatment of disorders such as cancer. Methods for treating or preventing cancers using MILs mobilized by E-selectin antagonists are further disclosed.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of galectin-3 to ligands are disclosed. For example, inhibitors of galectin-3 are described and pharmaceutical compositions comprising at least one such agent is described.
C07D 405/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 405/14 - 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 three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
44.
Methods for treating acute myeloid leukemia and related conditions
Methods for treating or inhibiting cancer and/or one or more related conditions by administering to a subject in need thereof an effective amount of a compound of Formula (I), a prodrug thereof, or a pharmaceutically acceptable salt of any of the foregoing. For example, methods for treating AML, MDS, neutropenia, and/or mucositis comprising administering a pharmaceutical composition comprising a compound of Formula (I) are described.
A process is provided for the synthesis of an intermediate of Formula 15 which is useful in the synthesis of E-selectin inhibitors. Also provided are useful intermediates obtained from the process.
A process is provided for the synthesis of an intermediate of Formula 15 which is useful in the synthesis of E-selectin inhibitors. Also provided are useful intermediates obtained from the process.
Methods for the treatment of sickle cell disease or complications associated therewith, including, for example, vaso-occlusive crisis, by the use of at least one E-selectin inhibitor and compositions comprising the same are disclosed.
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
48.
USE OF E-SELECTIN ANTAGONISTS TO ENHANCE THE SURVIVAL OF RECONSTITUTED, BONE MARROW-DEPLETED HOSTS
Hematopoietic stem cell (HSC) transplantation is a promising treatment for patients with various hematological diseases, immunodeficiency, autoimmune disorders, and other genetic disorders. Considerable work continues to strive toward the identification of critical factors involved in the successful engraftment and reconstitution of HSC recipients. The identification of these critical components and the understanding of how they may be therapeutically targeted would result in improved patient survival. E-selectin inhibitors for use in increasing survival of individuals that receive HSC transplantation or for reconstitution of depleted and compromised bone marrow are disclosed.
A61K 31/7028 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
A61K 35/28 - Bone marrow; Haematopoietic stem cells; Mesenchymal stem cells of any origin, e.g. adipose-derived stem cells
Methods for the treatment of sickle cell disease or complications associated therewith, including, for example, vaso-occlusive crisis, by the use of at least one E-selectin inhibitor and compositions comprising the same are disclosed.
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
50.
E-selectin antagonist compounds, compositions, and methods of use
Methods and compositions using E-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of E-selectin to an E-selectin ligand. Described herein are E-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin, galectin-3, or E-selectin and galectin-3 to ligands a disclosed. For example, heterobifunctional inhibitors of E-selectin and galectin-3 are described and pharmaceutical compositions comprising at least one such agent is described.
Compounds, compositions, and methods for treating and/or preventing at least one disease, disorder, and/or condition associated with E-selectin, galectin-3, and/or CXCR4 chemokine receptor activity are disclosed herein. For example, multimeric glycomimetic inhibitors ofE-selectins, galectin-3, and/or CXCR4 chemokine receptors and their use for treating and/or preventing inflammatory diseases, fibrosis, and cancers are disclosed. Formula (I).
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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
C07H 13/10 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals directly attached to heterocyclic rings
C07H 15/18 - Acyclic radicals, substituted by carbocyclic rings
Compounds, compositions, and methods for treating and/or preventing at least one disease, disorder, and/or condition associated with E-selectin, galectin-3, and/or CXCR4 chemokine receptor activity are disclosed herein. For example, multimeric glycomimetic inhibitors ofE-selectins, galectin-3, and/or CXCR4 chemokine receptors and their use for treating and/or preventing inflammatory diseases, fibrosis, and cancers are disclosed. Formula (I).
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
Compounds, compositions, and methods for modulating in vitro and in vivo processes mediated by se lectin binding are described herein. For example, multimeric selectin modulators and their use are described, wherein the multimeric selectin modulators comprise a glycomimetic linked to a member of a class of compounds termed BASAs (Benzyl Amino Sulfonic Acids) or a member of a class of compounds termed BACAs (Benzyl Amino Carboxylic Acids).
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
A61P 35/02 - Antineoplastic agents specific for leukemia
55.
HETEROBIFUNCTIONAL INHIBITORS OF E-SELECTIN AND GALECTIN-3
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin, galectin-3, or E-selectin and galectin-3 to ligands are disclosed. For example, heterobifunctional inhibitors of E-selectin and galectin-3 are described and pharmaceutical compositions comprising at least one such agent is described.
C07H 19/04 - Heterocyclic radicals containing only nitrogen as ring hetero atom
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
A61P 9/00 - Drugs for disorders of the cardiovascular system
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of galectin-3 to ligands are disclosed. For example, inhibitors of galectin-3 are described and pharmaceutical compositions comprising at least one such agent is described.
C07D 405/04 - 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 directly linked by a ring-member-to-ring- member bond
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
C07D 405/14 - 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 three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of galectin-3 to ligands are disclosed. For example, inhibitors of galectin-3 are described and pharmaceutical compositions comprising at least one such agent is described.
C07D 405/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 405/14 - 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 three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
58.
METHODS OF TREATING HIV AND AIDS AND THE ELIMINATION OF LATENT RESERVOIRS OF HIV INFECTION USING SELECTIN, GALECTIN, AND SIGLEC ANTAGONISTS
Methods and compounds for the treatment of HIV and/or AIDS using selectin antagonists, galectin-9 antagonists, and/or Siglec-7 antagonists are disclosed. The disclosed methods and compounds use the disclosed antagonists to target and eliminate quiescent reservoirs of infected cells to treat and/or cure this infection.
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
59.
E-selectin antagonist compounds, compositions, and methods of use
Methods and compositions using E-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of E-selectin to an E-selectin ligand. Described herein are E-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, E-selectin antagonists are described and pharmaceutical compositions comprising at least one of the same.
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
61.
METHODS FOR TREATING ACUTE MYELOID LEUKEMIA AND RELATED CONDITIONS
Methods for treating or inhibiting cancer and/or one or more related conditions by administering to a subject in need thereof an effective amount of a compound of Formula (I) a prodrug thereof or a pharmaceutically acceptable salt of any of the foregoing. For example, methods for treating AML, MDS, neutropenia, and/or mucositis comprising administering a pharmaceutical composition comprising a compound of Formula (I) are described.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61P 35/02 - Antineoplastic agents specific for leukemia
62.
METHODS FOR TREATING ACUTE MYELOID LEUKEMIA AND RELATED CONDITIONS
Methods for treating or inhibiting cancer and/or one or more related conditions by administering to a subject in need thereof an effective amount of a compound of Formula (I) a prodrug thereof or a pharmaceutically acceptable salt of any of the foregoing. For example, methods for treating AML, MDS, neutropenia, and/or mucositis comprising administering a pharmaceutical composition comprising a compound of Formula (I) are described.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61P 35/02 - Antineoplastic agents specific for leukemia
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, highly potent multimeric E-selectin antagonist are desorbed and pharmaceutical compositions comprising at least one of the same.
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
A61P 35/04 - Antineoplastic agents specific for metastasis
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
64.
HETEROBIFUNCTIONAL INHIBITORS OF E-SELECTIN AND GALECTIN-3
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin, galectin-3, or E-selectin and galectin-3 to ligands are disclosed. For example, heterobifunctional inhibitors of E-selectin and galectin-3 are described and pharmaceutical compositions comprising at least one such agent is described.
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
Compositions and methods for the treatment of diseases, disorders, and/or conditions associated with the increased regulatory T lymphocyte cell function, comprising the administration of T-cell checkpoint inhibitors in combination with E-selectin inhibitors, C—X—C Motif Chemokine Receptor 4 (CXCR4) receptor inhibitors, and/or heterobifunctional inhibitors that comprise at least one E-selectin inhibitor linked to at least one CXCR4 receptor inhibitor, are disclosed.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 47/61 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid (GABA), beta-alanine, epsilon-aminocaproic acid, pantothenic acid
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/702 - Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
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 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
A61K 39/00 - Medicinal preparations containing antigens or antibodies
66.
HETEROBIFUNCTIONAL INHIBITORS OF E-SELECTIN AND GALECTIN-3
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin, galectin-3, or E-selectin and galectin-3 to ligands are disclosed. For example, heterobifunctional inhibitors of E-selectin and galectin-3 are described and pharmaceutical compositions comprising at least one such agent is described.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
67.
METHODS OF MOBILIZING MARROW INFILTRATING LYMPHOCYTES AND USES THEREOF
Methods are disclosed for the mobilization of marrow infiltrating cells (MILs) using E-selectin antagonists for the treatment of disorders such as cancer. Methods for treating or preventing cancers using MILs mobilized by E-selectin antagonists are further disclosed.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61P 11/00 - Drugs for disorders of the respiratory system
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
G01N 33/569 - Immunoassay; Biospecific binding assay; Materials therefor for microorganisms, e.g. protozoa, bacteria, viruses
A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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
69.
GALACTOPYRANOSYL-CYCLOHEXYL DERIVATIVES AS E-SELECTIN ANTAGONISTS
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, E-selectin antagonists are described and pharmaceutical compositions comprising at least one of the same.
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, E-selectin antagonists are described and pharmaceutical compositions comprising at least one of the same.
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, highly potent multimeric E-selectin antagonist are dessorbed and pharmaceutical compositions comprising at least one of the same.
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, highly potent multimeric E-selectin antagonist are dessorbed and pharmaceutical compositions comprising at least one of the same.
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
Compositions and methods for the treatment of diseases, disorders, and/or conditions associated with the increased regulatory T lymphocyte cell (Treg cell) function, comprising the administration of T-cell checkpoint inhibitors in combination with E-selectin inhibitors, CXCR4 receptor inhibitors, and/or heterobifunctional inhibitors that comprise at least one E-selectin inhibitor linked to at least one CXCR4 receptor inhibitor, are disclosed.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 39/00 - Medicinal preparations containing antigens or antibodies
Compounds of Formula (I), compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, haloalkyl fucose-containing E-selectin antagonists and compositions comprising at least one such agent are described.
New methods for treating and/or preventing cardiovascular disease including, for example, myocardial infarction and atherosclerosis, by the use of at least one E-selectin inhibitor and compositions comprising the same are disclosed.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
76.
GLYCOMIMETIC INHIBITORS OF PA-IL AND PA-IIL LECTINS
Compounds, compositions, and methods for the diagnosis and/or treaimeni of medical conditions involving infections with and colonization by Fseudomonas bacteria including, for example, Fseudomonas aeruginosa in the lungs of patients with cystic fibrosis are described.
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
Compounds, compositions, and methods for the diagnosis and/or treaimeni of medical conditions involving infections with and colonization by Fseudomonas bacteria including, for example, Fseudomonas aeruginosa in the lungs of patients with cystic fibrosis are described.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
78.
HETEROBIFUNCTIONAL PAN-SELECTIN ANTAGONISTS HAVING A TRIAZOLE LINKER
Compounds, compositions, and methods for modulating in vitro and in vivo processes mediated by selectin binding. For example, heterobifunctional compounds that inhibit both E-selectins and P-selectins are described, wherein the selectin modulators that modulate (e.g., inhibit or enhance) a selectin-mediated function comprise particular glycomimetics linked to a member of a class of compounds termed BASAs (Benzyl Amino Sulfonic Acids). The compounds are of formula (la) wherein the substituents are as defined in the claims.
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
A61P 35/02 - Antineoplastic agents specific for leukemia
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
Methods and compositions for the discovery and production of antibodies that can be used to identify and/or isolate hematopoietic stem cells (HSCs), for example, HSCs with high reconstitution potential. Methods and compositions are further provided for the treatment of patients with hematologic or genetic disorders, patients with cardiovascular disorders, patients recovering from wounds, or patients recovering from chemotherapy or radiation exposure using HSCs or genetically modified HSCs, for example, HSCs and/or genetically modified HSCs with high reconstitution potential.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/00 - Medicinal preparations containing antigens or antibodies
Methods and systems for identifying and treating patients with cancers that can bind E-selectin are disclosed. E-selectin-binding cancers are identified by their cell surface expression sialyl Le3 and sialyl Lex carbohydrate epitopes, and such cancers can be identified by antibodies that bind to sialyl Lea/x, such as HECA-452. Such cancers can be treated with antagonists of E-selectin such as glycomimetic compounds and with immunotherapies targeting the cell surface carbohydrates containing the sialyl Lea/x domains to block and/or disrupt the binding of E-selectin.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
The disclosure provides a new source of peripheral blood naive/memory stem cells (i.e. (TN)/TSCM//TCM) T-cells with enhanced reconstitution potential and/or longer life spans. It discloses that this particular subset of T-cells can be mobilized by administration of at least one mobilizer in combination with at least one E-Seiectin inhibitor.
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed, For example, E-selectin antagonist therapeutic agents and compositions comprising at least one such agent are described: wherein RX-is chosen from halogens.
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
Methods are provided herein for use of E-selectin antagonists for mobilizing cells, such as hematopoietic cells, hematopoietic stem cells and progenitor cells, white blood cells, and malignant cells, and hematopoietic tumor cells from the bone marrow. More specifically, methods are provided for using E-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers, and peptides for mobilizing cells from the bone marrow to the peripheral vasculature and tissues.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
84.
HETEROBIFUNCTIONAL INHIBITORS OF E-SELECTINS AND CXCR4 CHEMOKINE RECEPTORS
Compounds, compositions, and methods for treatment and/or prevention of cancer and inflammatory diseases, and for releasing cells such as stem cells (e.g., bone marrow progenitor cells) into circulating blood and enhancing retention of the cells in the blood are disclosed. For example, heterobifunctional compounds that inhibit both E-selectins and CXCR4 chemokine receptors are described and pharmaceutical compositions comprising at least one of the same.
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
85.
HETEROBIFUNCTIONAL INHIBITORS OF E-SELECTINS AND CXCR4 CHEMOKINE RECEPTORS
Compounds, compositions, and methods for treatment and/or prevention of cancer and inflammatory diseases, and for releasing cells such as stem cells (e.g., bone marrow progenitor cells) into circulating blood and enhancing retention of the cells in the blood are disclosed. For example, heterobifunctional compounds that inhibit both E-selectins and CXCR4 chemokine receptors are described and pharmaceutical compositions comprising at least one of the same.
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
86.
E-selectin antagonist compounds, compositions, and methods of use
Methods and compositions using E-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of E-selectin to an E-selectin ligand. Described herein are E-selection antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
87.
E-SELECTIN ANTAGONISTS MODIFIED BY MACROCYCLE FORMATION TO THE GALACTOSE
Provided herein are glycomimetic E-selectin antagonist compounds of formula (I)) and pharmaceutical compositions comprising at least one of the same. The compounds of the present disclosure include trisaccharide domain mimics comprising at least one macrocycle created through the 2nd and 3rd positions on a galactose within the mimic. Methods are also provided comprising using at least one of such compounds and compositions comprising at least one of the same to treat and/or prevent diseases and disorders treatable by inhibiting binding of an E-selectin to an E-selectin ligand.
C07H 9/00 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical
C07H 9/02 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing only oxygen as ring hetero atoms
A61K 31/7028 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
Methods and compositions using E-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of E-selectin to an E-selectin ligand. Described herein are E-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation.
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
C07H 11/00 - Compounds containing saccharide radicals esterified by inorganic acids; Metal salts thereof
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
89.
METHODS AND COMPOSITIONS FOR TREATING AND/OR PREVENTING MUCOSITIS
Methods for treating and/or preventing mucositis comprising administering to a subject in need thereof an effective amount of at least one compound chosen from E-selectin antagonists, pharmaceutically acceptable salts of E-selectin antagonists, prodrugs of E- selectin antagonists, and pharmaceutically acceptable salts of prodrugs of E-selectin antagonists, and compositions comprising at least one of such compound.
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
90.
Pan-selectin inhibitor with enhanced pharmacokinetic activity
Compounds, compositions and methods are provided for treatment of diseases or complications associated therewith, in which a selectin plays a role. More specifically, particular glycomimetics and uses thereof are described. For example, use of particular glycomimetics for treating sickle cell disease or a cancer involving a selectin, or complications associated with either, is described.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
A61K 31/7064 - 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
C07H 15/22 - Cyclohexane rings, substituted by nitrogen atoms
91.
COMPOUNDS AND METHODS TO ENHANCE THE ORAL AVAILABILITY OF GLYCOMIMETICS
Potent E-selecting antagonist compounds are described herein. In certain embodiments, compounds and methods are provided for enhancing the oral availability of glycomimetics. More specifically, in an embodiment, a glyeomimetic is modified to decrease the polar surface area of the glyeomimetic in order to increase absorption from the GI tract, in another embodiment, a glyeomimetic is targeted to an active transport system, such as the bile acid active transport system, that provides transport across a biological membrane in order to increase absorption of the glyeomimetic from the GI tract.
Methods are provided herein for use of E-selectin antagonists for mobilizing cells, such as hematopoietic cells, hematopoietic stem cells and progenitor cells, white blood cells, and malignant cells, and hematopoietic tumor cells from the bone marrow. More specifically, methods are provided for using E-se!ectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers, and peptides for mobilizing cells from the bone marrow to the peripheral vasculature and tissues.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
Methods are provided herein for use of E-selectin antagonists for mobilizing cells, such as hematopoietic cells, hematopoietic stem cells and progenitor cells, white blood cells, and malignant cells, and hematopoietic tumor cells from the bone marrow. More specifically, methods are provided for using E-se!ectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers, and peptides for mobilizing cells from the bone marrow to the peripheral vasculature and tissues.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
Compounds and methods are provided for enhancing the oral availability of glycomimetics. More specifically, in an embodiment, a glycomimetic is modified to decrease the polar surface area of the glycomimetic in order to increase absorption from the GI tract. In another embodiment, a glycomimetic is targeted to an active transport system, such as the bile acid active transport system, that provides transport across a biological membrane in order to increase absorption of the glycomimetic from the Gl tract.
C07H 15/234 - Cyclohexane rings, substituted by at least two nitrogen atoms with at least two saccharide radicals directly attached to the cyclohexane rings attached to non-adjacent ring carbon atoms of the cyclohexane rings, e.g. kanamycins, tobramycin, nebramycin, gentamicin A2
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
95.
GALACTOPYRANOSYL-CYCLOHEXYL DERIVATIVES AS E-SELECTIN ANTAGONISTS
Provided herein are E-selectin antagonist therapeutic agents and improvements thereto and compositions comprising these E-selectin antagonists. Methods are also provided for using these E-selectin antagonist therapeutic agents to treat and/or prevent diseases and disorders treatable by inhibiting binding of an E-selectin to an E-selectin ligand. Also provided herein improvements to E-selectin antagonist giycomimetic compounds that improve the oral bioavailability of the giycomimetic compounds.
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
Compounds and methods are provided for modulating in vitro and in vivo processes mediated by selectin binding. More specifically, selectin modulators and their use are described, wherein the selectin modulators that modulate (e.g., inhibit or enhance) a selectin-mediated function comprise particular glycomimetics alone or linked to a member of a class of compounds termed BASAs (Benzyl Amino Sulfonic Acids) or a member of a class of compounds termed BACAs (Benzyl Amino Carboxylic Acids).
Compounds, compositions and methods are provided for inhibiting in vitro and in vivo processes mediated by E-selectin binding. More specifically, particular glycomimetic compounds are described, wherein the compounds are E-selectin antagonists.
