http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2826398-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a71caf66bd467412cc746f6147db0025 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K2039-505 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K2317-94 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-6885 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-549 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-60 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-6883 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-6851 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-6817 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K38-05 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-6819 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K16-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K16-2878 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-351 |
| filingDate | 2014-10-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2021-05-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_145478c6b532988889c17a64b8465465 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_275d226337adc950a2e10cdb0e03b559 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_55075f7b24318d95cc55d3067e607545 |
| publicationDate | 2021-05-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2826398-T3 |
| titleOfInvention | Pegylated drug-linkers for better pharmacokinetics of ligand-drug conjugates |
| abstract | A ligand-drug conjugate compound wherein the ligand-drug conjugate compound is composed of a ligand unit and one or more linker-drug portions covalently attached to the ligand unit, wherein each linker-drug portion is composed by a parallel connector unit, wherein the parallel connector unit is a trifunctional chemical portion that connects the ligand unit to one or more drug units through a releasable assembly unit for each drug unit, and connects a unit of polyethylene glycol in parallel orientation with respect to the drug units of each linker-drug portion, wherein each of the drug units is hydrophobic, wherein the polyethylene glycol unit comprises one or more polyethylene glycol chains, and the unit of polyethylene glycol has one end that is covalently connected to the parallel connector unit, wherein the releasable assembly units can release rar the free drug in the vicinity of a target site directed by the ligand unit, where the linker-drug portions provide the loading of one to thirty-two drug units on the ligand-drug conjugate, where the compound of Ligand-drug conjugate has the structure represented by formula (I), (II) or (III): ** (See formula) ** or a pharmaceutically acceptable salt thereof, where, L is the ligand unit, in where the ligand unit is selected from an antibody, an interferon, a lymphokine, a hormone, a growth factor, a colony stimulating factor, a vitamin, or a nutrient transport molecule, where the ligand unit is an agent targeting that specifically binds to a target moiety, wherein said binding presents the drug unit of the ligand-drug conjugate to the particular target cell population characterized by the target moiety with which the l unit interacts. igando; D is the hydrophobic drug unit, where the drug unit is a cytotoxic, cytostatic, or immunosuppressive drug having a hydrophobicity greater than or within 20% of monomethyl auristatin E when measured using SlogP; PEG is the polyethylene glycol unit, wherein the PEG unit comprises from 4 to 72 subunits (OCH2CH2); Z is an extension unit that acts to link the ligand unit to the connector unit in parallel; X is the releasable assembly unit, wherein X comprises a peptide, disulfide, or glycosidic bond; LP is the parallel connecting unit, which serves to connect the ligand unit to the polyethylene glycol unit and the hydrophobic drug unit so that the polyethylene glycol unit and the drug unit are in a parallel orientation, wherein the polyethylene glycol in said parallel orientation masks the hydrophobicity of the hydrophobic drug unit; A is an optional branching unit, when present, each A is from one to 10 independently selected amino acid, amino alcohol or aminoaldehyde or polyamine residues, or a combination of these, covalently linked to each other; AD is a drug binding unit, when present, each AD is from one to 10 independently selected amino acid or amino alcohol or aminoaldehyde or polyamine residues, or a combination of these, covalently linked to each other; the subscript p is an integer ranging from 1 to 14, preferably 2 to 12, preferably 6 to 14, 6 to 12, 8 to 14 or 8 to 12; the subscript t is an integer ranging from 0 to 8, preferably 0, 1, 2 or 3; the subscript m is an integer ranging from 1 to 4, preferably 1 or 2; and the subscript s is 0 or 1, with the condition that when the subscript s is 0, the subscript m is 1 and when the subscript s is 1, the subscript m is 2, 3 or 4, in addition, where each unit Parallel linker (Lp) is (i) or (ii) below: (i) each parallel linker unit (Lp) comprises an amino acid, aminoalcohol, aminoaldehyde or polyamine residue, particularly where each parallel linker unit (Lp ) has the structure of: ** (See formula) ** where wavy lines indicate covalent binding sites of Lp within the ligand-drug conjugate compound, particularly where each parallel connecting unit (Lp) has the structure of ** (See formula) ** where wavy lines indicate the covalent binding sites of Lp within the ligand-drug conjugate compound; and wherein AA1 is independently selected from an amino acid, optionally substituted C1-20 heteroalkylene, optionally substituted C3-8 heterocycle, optionally substituted C6-14 arylene, or optionally substituted C3-C8 carbocycle, each with functional groups for inter-subunit linkages. of Formula A and within the ligand-drug conjugate; and the subscript u is an integer independently selected from 0 to 4; wherein at least one AA1 of each Lp unit has a functional group-added side chain that provides a binding site to a PEG, AD, A or Z unit or an XD portion, particularly AA1 is an independently selected amino acid or is an optionally substituted C1-20 heteroalkylene, optionally substituted C3-8 heterocycle, optionally substituted C6-14 arylene, or optionally substituted C3-C8 carbocycle, provided no more than 2 of AA1 is an optionally substituted C1-20 heteroalkylene, C3-8 heterocycle optionally substituted, optionally substituted C6-14 arylene or optionally substituted C3-C8 carbocycle. |
| priorityDate | 2013-10-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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