Drug compounds containing albumin-binding moieties

Abstract

This application relates to a compound or a pharmaceutically acceptable salt thereof comprising at least one polymer moiety conjugated covalently and reversibly by at least two drug moieties, wherein the drug moieties are conjugated to an albumin-binding moiety. This application also relates to pharmaceutical compositions comprising at least one such compound and their medical uses.

Description

[Technical Field]

[0001] This application relates to a compound or a pharmaceutically acceptable salt thereof comprising at least one polymer moiety conjugated covalently and reversibly by at least two drug moieties, wherein the drug moieties are conjugated to an albumin-binding moiety. This application also relates to pharmaceutical compositions comprising at least one such compound and their medical uses. [Background technology]

[0002] While some classes of therapeutic proteins, including antibodies, have long intrinsic half-lives, many other molecules, particularly proteins or peptide hormones, are often sensitive to enzymatic degradation, renal clearance, and / or rapid receptor-mediated clearance, which leads to short plasma elimination half-lives. Furthermore, due to difficulties associated with oral delivery, the vast majority of peptide or protein-based drugs require parenteral administration, which, combined with their short half-lives, necessitates frequent infusions, causing discomfort and inconvenience to patients. This can negatively impact compliance and ultimately limit therapeutic efficacy and outcomes.

[0003] Infusion of lipid-derived peptides has been demonstrated to have slower absorption from subcutaneous tissue and a longer circulating half-life compared to non-derivative peptides, due to their reversible binding to albumin. The half-life of endogenous albumin in circulation is approximately three weeks. This long half-life may be a result of both its large molecular size, which minimizes renal clearance, and recycling via the neonatal Fc receptor (FcRn). In circulation, the large molecular size protects the bound peptide from renal clearance and reduces its distribution rate to the extravascular compartment.

[0004] The slower absorption is thought to be due to a decrease in the diffusion rate in tissues, mediated by mechanisms including the interaction of fatty acid side chains with cell membranes and / or proteins such as albumin present at the injection site. The diffusion rate in tissues and passage through capillary walls after injection will be reduced, as expected, due to the large molecular size of the albumin-peptide complex. Molecules with a molecular size larger than approximately 16 kDa are preferentially and alternatively absorbed via the lymphatic pathway compared to direct absorption into the bloodstream through capillary walls.

[0005] Therefore, slower absorption and reversible albumin binding have allowed for extensions of the dosing interval for drugs such as peptide drugs, up to a maximum of one week. However, further extensions of the dosing interval may be desirable. [Overview of the project] [Problems that the invention aims to solve]

[0006] The objective of this invention is to overcome, at least partially, the shortcomings of current therapies. [Means for solving the problem]

[0007] The objective is to provide a compound or a pharmaceutically acceptable salt thereof comprising at least one polymer moiety in which at least two parts of formula (I) are conjugated and / or at least one part of formula (I') is conjugated, wherein formulas (I) and (I') are [ka] (In the formula, Each-L 2 - is either an independent spacer part or does not exist. Each-L 1 - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each-L 1' - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each -D- is an independent drug portion. Each -AB is an albumin-binding moiety independently. Each a is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. This is achieved by a compound or a pharmaceutically acceptable salt thereof.

[0008] The applicant discovered that the compounds of the present invention can further extend the half-life and administration frequency. Surprisingly, it was found that compounds of two or more drugs containing albumin-binding moieties can coordinate two or more albumin molecules, resulting in large molecular-sized albumin-drug complexes.

[0009] This results in compounds exhibiting increased albumin-binding ability and slowed absorption of high molecular weight drug-albumin complexes. Such compounds also demonstrate reduced absorption from the administration site, such as from subcutaneous tissue, compared to administration of the corresponding unconjugated drug. Consequently, such compounds have an extended half-life compared to the corresponding unconjugated drug. [Modes for carrying out the invention]

[0010] In this invention, the following terms are used:

[0011] As used herein, the term “GLP-1 receptor agonist” refers to an agonist of the GLP-1 receptor (GLP1R) and, optionally, an agonist of one or more other receptors, such as the receptor for gastric suppressor polypeptide (GIPR), the receptor for glucagon (GCGR), the receptor for amyrin, the receptor for peptide YY (PYYR), or the receptor for glucagon-like peptide 2 (GLP2R). An “agonist” of a receptor, such as a GLP-1 receptor agonist, is a compound that activates such a receptor to produce a biological response. If a GLP-1 receptor agonist is also an agonist of one other receptor besides GLP1R, such as a GIPR, GCGR, amyrin receptor, PYYR, or GLP2R agonist, such a GLP-1 receptor agonist is also called a “dual GLP-1 receptor agonist” or simply a “dual agonist.” Similarly, if a GLP-1 receptor agonist is not only a GLP1R agonist but also an agonist of two other receptors selected from the group consisting of GIPR, GCGR, amyrin receptor, PYYR, or GLP2R, such a GLP-1 receptor agonist is also called a “triple GLP-1 receptor agonist” or simply a “triple agonist.”

[0012] As used herein, the term "peptide" refers to a chain of at least two and up to 50 amino acid monomer moieties linked by peptide (amide) bonds, which may also be called "amino acid residues." Amino acid monomers may be selected from the group consisting of protein-constitutive amino acids and non-protein-constitutive amino acids, and may be D- or L-amino acids. The term "peptide" also includes peptide mimes, such as peptoids, beta-peptides, cyclic peptides, and depsipeptides, encompassing such peptide mimetics chains having up to 50 monomer moieties. Cyclic peptides may be monocyclic, bicyclic, tricyclic, or tetracyclic peptides. The term "peptide" also includes lasso peptides.

[0013] As used herein, the term "protein" preferably refers to a chain of more than 50 amino acid monomers linked by peptide bonds, in which 12,000 or fewer amino acid monomers, for example, 10,000 or fewer amino acid monomer portions, 8,000 or fewer amino acid monomer portions, 5,000 or fewer amino acid monomer portions, or 2,000 or fewer amino acid monomer portions are linked by peptide bonds. These amino acid monomer portions may also be called "amino acid residues."

[0014] As used herein, the term "small molecule drug" refers to a drug that is an organic compound having a molecular weight of less than 1000 Da, for example, less than 900 Da or less than 800 Da. It is understood that drug moieties based on nucleobases, such as adenine or guanine analogs, can also be a type of small molecule drug.

[0015] As used herein, the terms "medium-sized molecular drug" or "medium-sized molecular drug" refer to a drug that is neither a peptide nor a protein, but an organic compound having a molecular weight in the range of 1 kDa to 7.5 kDa.

[0016] As used herein, the term “oligonucleotide” refers to double-stranded or single-stranded RNA and DNA, preferably containing 2 to 1000 nucleotides, and any modifications thereof. Modifications include, for example, those that impart other chemical groups to the nucleic acid ligand base or to the nucleic acid ligand as a whole, incorporating additional charge, polarizability, hydrogen bonding, electrostatic interactions, and fractionality. Such modifications include, for example, 2'-position sugar modifications, 5-position pyrimidine modifications, 8-position purine modifications, extracyclic amine modifications, 4-thiouridine substitutions, 5-bromo or 5-iodouracil substitutions; skeletal modifications, methylation, unusual pair-forming combinations, such as the isobases isocytidine and isoguanidine. Modifications also include 3' and 5' modifications such as capping, and stereochemical changes. The term also includes aptamers.

[0017] As used herein, the term "peptide nucleic acid" refers to an organic polymer having a peptide skeleton, i.e., a skeleton in which monomers are linked to one another through peptide bonds, to which nucleic acid bases such as adenine, cytosine, guanine, thymine, and uracil are bonded. In certain embodiments, the peptide skeleton includes N-(2-aminoethyl)-glycine.

[0018] As used herein, the term "random coil" refers to a conformation of any polymer molecule, including proteins, in which individual monomer elements forming a polymer structure are essentially randomly oriented toward adjacent monomer elements, while still chemically bonded to them. In particular, polypeptides or proteins having a random coil conformation substantially lack defined secondary and tertiary structures. The properties of polypeptide random coils and methods for their experimental identification are known to those skilled in the art. In particular, the absence of secondary and tertiary structures in proteins can be determined by circular dichroism (CD) measurements. CD spectroscopy represents optical absorption spectroscopy in which the difference in absorption of right-circularly polarized and left-circularly polarized light by a substance is measured. The secondary structure of a protein can be determined by CD spectroscopy using far-ultraviolet spectra with wavelengths of approximately 190–250 nm. At these wavelengths, the different secondary structures commonly found in conformations each produce characteristic shapes and amplitudes in the CD spectrum. Thus, by using CD spectroscopy, those skilled in the art can easily determine whether an amino acid polymer adopts a random coil conformation under physiological conditions.

[0019] When determining whether a peptide or protein adopts random coil conformation under experimental conditions using the methods described herein, biophysical parameters such as temperature, pH, osmotic pressure, and protein content may differ from the physiological conditions typically found in vivo. Temperatures of 1°C to 42°C, or preferably 4°C to 25°C, can be considered useful for testing and / or verifying the biophysical properties and biological activity of peptides or proteins under physiological conditions in vitro.

[0020] In particular, several buffers in the buffers, solvents and / or excipients of pharmaceutical compositions in experimental settings (e.g., in determining protein structure, especially in circular dichroism (CD) measurements and other methods that enable those skilled in the art to determine the structural properties of protein / polypeptide or peptide elongations) are considered to represent “physiological solutions” or “physiological conditions” in vitro. Examples of such buffers include, for example, phosphate-buffered saline (PBS: 115 mM NaCl, 4 mM KH2PO4, 16 mM Na2HPO4 pH 7.4), Tris buffer, acetate buffer, citrate buffer, or similar buffers used in the accompanying examples. Generally, the pH of the buffer representing physiological conditions should be in the range of 6.5 to 8.5, preferably 7.0 to 8.0, and most preferably 7.2 to 7.7, and the osmotic pressure should be in the range of 10 to 1000 mmol / kg H2O, more preferably 50 to 500 mmol / kg H2O, and most preferably 200 to 350 mmol / kg H2O. In some cases, the protein content of the buffer representing physiological conditions can be in the range of 0 to 100 g / L, ignoring the biologically active proteins themselves, thereby allowing the use of typical stabilizing proteins, such as human or bovine serum albumin.

[0021] Other established biophysical methods for determining random coil conformation include nuclear magnetic resonance (NMR) spectroscopy, absorption spectroscopy, infrared and Raman spectroscopy, hydrodynamic volume measurement via size exclusion chromatography, analytical ultracentrifugation and dynamic / static light scattering, and measurement of friction coefficient or intrinsic viscosity.

[0022] As used herein, the term "physiological conditions" refers to an aqueous buffer solution at pH 7.4 and 37°C.

[0023] As used herein, the term “pharmaceutical composition” means a composition comprising one or more active ingredients, such as at least one compound of the present invention, and one or more excipients, and any products directly or indirectly arising from combinations, complexes, or aggregations of any two or more components of the composition, or from the dissociation of one or more of the components, or from other types of reactions or interactions of one or more of the components. Accordingly, the pharmaceutical compositions of the present invention encompass any composition produced by mixing one or more compounds of the present invention with one or more pharmaceutically acceptable excipients.

[0024] As used herein, the term “excipient” refers to a therapeutic agent, such as a diluent, adjuvant, or vehicle on which a drug or prodrug is administered. Such pharmaceutical excipients may be sterile solutions, such as water and oils (petroleum, animal, plant, or synthetic oils, including, but not limited to, peanut oil, soybean oil, mineral oil, and sesame oil). Water is an example of an excipient when the pharmaceutical composition is administered orally. Saline solutions and dextrose aqueous solutions are examples of excipients when the pharmaceutical composition is administered intravenously. Saline solutions, as well as dextrose aqueous solutions and glycerol solutions, are used as liquid excipients for injectable solutions in certain embodiments. Suitable pharmaceutical excipients include starch, glucose, lactose, sucrose, mannitol, trehalose, gelatin, malt, rice, wheat flour, chalk, silica gel, sodium stearate, glyceryl monostearate, talc, sodium chloride, skim milk powder, glycerol, propylene glycol, water, and ethanol. The pharmaceutical composition may also optionally contain small amounts of wetting or emulsifying agents, pH buffers such as acetates, succinates, tris, carbonates, phosphates, HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid), MES (2-(N-morpholino)ethanesulfonic acid), or surfactants such as Tween, poloxamer, poloxamine, CHAPS, Igepal, or amino acids such as glycine, lysine, or histidine. These pharmaceutical compositions may take the form of solutions, suspensions, emulsions, tablets, pills, capsules, powders, or sustained-release formulations. The above pharmaceutical compositions may be formulated as suppositories with traditional binders and excipients, such as triglycerides. Oral formulations may contain standard excipients, such as pharmaceutical-grade mannitol, lactose, starch, magnesium stearate, sodium saccharin, cellulose, magnesium carbonate, etc. Such compositions will contain a therapeutically effective amount of the drug or drug portion, along with a suitable amount of excipients to provide a form for appropriate administration to the patient. The formulation should be suitable for the mode of administration.

[0025] As used herein, the term "liquid composition" refers to a mixture comprising a water-soluble compound and one or more solvents, such as water.

[0026] The term "suspension composition" refers to a mixture comprising at least one water-insoluble compound and one or more solvents, such as water.

[0027] As used herein, the term “dried composition” means that the pharmaceutical composition is provided in a dry form. Preferred drying methods are spray drying and freeze-drying. Such a dried composition has a residual moisture content of up to 10%, for example, less than 5% or less than 2%, as determined by Karl Fischer. In certain embodiments, such a dried pharmaceutical composition is dried by freeze-drying.

[0028] As used herein, the term “drug” refers to a substance used in the treatment, cure, prevention, or diagnosis of a disease, or used in any other way to enhance physical or mental well-being. When a drug is conjugated to another part, the resulting product portion derived from that drug is referred to as the “drug portion.”

[0029] As used herein, the term “prodrug” refers to a covalent conjugate in which a drug moiety is reversibly and covalently bonded to a special protecting group via a reversible linker moiety, also called a “reversible prodrug linker moiety” or “reversible linker moiety,” which conjugates the drug moiety by a reversible bond, where the special protecting group alters or removes undesirable properties in the parent molecule. This includes enhancing desirable properties and suppressing undesirable properties in the drug. The special non-toxic protecting group is called a “carrier.” A prodrug releases a reversibly and covalently bonded drug moiety in the form of its corresponding drug. In other words, a prodrug is a compound containing a drug moiety covalently and reversibly conjugated to a carrier moiety via a reversible linker moiety, where the covalent and reversible conjugation of the carrier to the reversible linker moiety is direct or spacer-mediated. Such a compound releases the previously conjugated drug moiety in the form of a free, unmodified drug.

[0030] A "reversible bond" is a bond that can be degraded, or cleaved, under physiological conditions (aqueous buffer, pH 7.4, 37°C) in the absence of an enzyme, with a half-life of 1 hour to 3 months. A "stable bond" is a bond that has a half-life of more than 3 months under physiological conditions (aqueous buffer, pH 7.4, 37°C) in the absence of an enzyme.

[0031] As used herein, the terms “tracesless prodrug linker” or “tracesless linker” mean a reversible prodrug linker that releases the drug in its free form when cleaved, i.e., a linker portion that reversibly and covalently binds the drug portion to the carrier. As used herein, the term “free form” means the drug in its unmodified, pharmacologically active form.

[0032] As used herein, the term “reagent” means a compound containing at least one functional group for reaction with the functional group of another compound or drug. Drugs containing a functional group such as a primary or secondary amine or a hydroxyl functional group are also understood to be reagents.

[0033] As used herein, the term “part” means a portion of a molecule that lacks one or more atoms compared to the corresponding reagent. For example, when a reagent of formula “HXH” reacts with another reagent and becomes part of a reaction product, the corresponding part of the reaction product has the structure “HX-” or “-X-”, where each “-” indicates a bond to another part. Thus, the drug part is released as a drug from the prodrug.

[0034] If the chemical structure of an atomic group bonded to at least one other part is provided, unless otherwise explicitly stated, the chemical structure may be bonded to at least one other part in any orientation. For example, part "-C(O)N(R 1 )-" is "-C(O)N(R 1 )-" or "-N(R 1 )C(O)-" may be joined to two parts. Similarly, part [ka] teeth, [ka] as, or [ka] It may be combined into two parts.

[0035] As used herein, the term "functional group" means a group of atoms that can react with other groups of atoms. Functional groups are selected from the group consisting of, for example, the following groups: carboxylic acids, primary or secondary amines, maleimides, thiols, sulfonic acids, carbonates, carbamates, hydroxyls, aldehydes, ketones, hydrazines, isocyanates, isothiocyanates, phosphoric acids, phosphonic acids, haloacetyls, alkyl halides, acryloyls, aryl fluorides, hydroxylamines, disulfides, sulfonamides, sulfuric acids, vinyl sulfones, vinyl ketones, diazoalkanes, oxiranes, and aziridines.

[0036] As used herein, the term "pharmaceutically acceptable salt" refers to a salt that retains the biological efficacy or properties of the compound and is not typically biologically or otherwise undesirable. In certain embodiments, compounds can form acid / or base salts by the presence of amino and / or carboxyl functional groups or similar groups. Pharmaceutically acceptable acid addition salts can be formed using inorganic and organic acids, for example, acetates, aspartates, benzoates, besilates, bromides / hydrobroms, bicarbonates / carbonates, bisulfates / sulfates, camphor sulfons, chlorides / hydrochlorides, chlortheophyllinates, citrates, ethanedisulfons, fumarates, gluceptates, glucons, glucurons, hippurates, hydroiodides / iodides, etc. These may be cetionic acid, lactate, lactobionate, lauryl sulfate, malate, maleate, malonate, mandelate, mesylate, methyl sulfate, naphthoate, napsylate, nicotinate, nitrate, octadecanoate, oleate, oxalate, palmitate, pamoate, phosphate / hydrogen phosphate / dihydrogen phosphate, polygalacturonate, propionate, stearate, succinate, subsalicylate, tartrate, tosylate, and trifluoroacetate. Examples of inorganic acids from which salts can be derived include hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, and phosphoric acid. Examples of organic acids from which salts can be derived include acetic acid, propionic acid, glycolic acid, oxalic acid, maleic acid, malonic acid, succinic acid, fumaric acid, tartaric acid, citric acid, benzoic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, toluenesulfonic acid, and sulfosalicylic acid. Pharmaceutically acceptable base addition salts can be formed using inorganic and organic bases. Examples of inorganic bases from which salts can be derived include ammonium salts and metals from columns I to XII of the periodic table. In certain embodiments, salts are derived from sodium, potassium, ammonium, calcium, magnesium, iron, silver, zinc, and copper, with ammonium, potassium, sodium, calcium, and magnesium salts being particularly preferred.Examples of organic bases from which salts can be derived include primary, secondary, and tertiary amines, naturally occurring substituted amines and other substituted amines, cyclic amines, and basic ion exchange resins. Specific organic amines include isopropylamine, benzathine, cholinate, diethanolamine, diethylamine, lysine, meglumine, piperazine, or tromethamine. Pharmaceutically acceptable salts can be synthesized from the parent compound, basic or acidic moiety by conventional chemical methods.

[0037] The term "pharmaceutically acceptable" means a substance that does not cause harm when administered to a patient, and in certain embodiments, means that it is authorized for use in animals, and in particular for use in humans, by a regulatory body, such as the EMA (Europe) and / or the FDA (United States) and / or any other national regulatory body.

[0038] In this specification, the terms “about” or “approximately” in combination with numerical values ​​are used to indicate not only the numerical value itself, but also a range of plus or minus 10% or less of the said numerical value. For example, the phrase “about 200” or “approximately 200” is used to mean a range of 200 ± 10%, i.e., a range of 180 to 220. A percentage expressed as “about 20%” or “approximately 20%” is understood not to mean “20% ± 10%,” i.e., a range of 10 to 30%, but rather to mean a range of 18 to 22%, i.e., a range of plus or minus 10% of the numerical value 20.

[0039] As used herein, the term "polymer" means a molecule containing repeating structural units, i.e., monomers, bonded by linear, cyclic, branched, cross-linked or dendrimer-like chemical bonds or combinations thereof, which may be of synthetic or biological origin, or a combination of both. It is understood that a polymer may also contain one or more other chemical groups and / or moieties, such as one or more functional groups for example. In certain embodiments, a soluble polymer has a molecular weight of at least 0.5 kDa, for example, at least 1 kDa, at least 2 kDa, at least 3 kDa or at least 5 kDa. When the polymer is soluble, in certain embodiments, the polymer has a molecular weight of up to 1000 kDa, for example up to 750 kDa, for example up to 500 kDa, for example up to 300 kDa, for example up to 200 kDa, or for example up to 100 kDa. It is understood that for water-insoluble polymers, such as hydrogels, no meaningful molecular weight range can be provided. Peptides or proteins are also understood to be polymers in which the amino acids are the repeating structural units, even though the side chains of each amino acid can be different.

[0040] As used herein, the term "polymeric" means a reagent or moiety that contains one or more polymers or polymer moieties. A polymeric reagent or moiety may optionally also contain one or more other moieties, which in certain embodiments are selected from the group consisting of: - C 1-50 alkyl, C 2-50 alkenyl, C 2-50 alkynyl, C 3-10 cycloalkyl, 3- to 10-membered heterocyclyl, 8- to 11-membered heterobicyclic, phenyl, naphthyl, indenyl, indanyl, and tetralinyl, and - a bond selected from the group comprising

Chemical formula

[0041] Those skilled in the art will understand that polymerization products obtained from polymerization reactions do not necessarily all have the same molecular weight, but rather exhibit a molecular weight distribution. For this reason, the molecular weight range, molecular weight, range of monomer numbers in a polymer, and number of monomers in a polymer as used herein refer to the number-average molecular weight and number-average monomers, i.e., the arithmetic mean of the molecular weight of the polymer or polymer part, and the arithmetic mean of the number of monomers in the polymer or polymer part.

[0042] Therefore, in a polymer portion containing "x" monomer units, any integer represented as "x" corresponds to the arithmetic mean of the monomers. Any range of integers represented as "x" provides a range of integers within which the arithmetic mean of the monomers lies. An integer "x" represented as "about x" means that the arithmetic mean of the monomers lies within the range of integers x ± 10%, x ± 8% in a particular embodiment, x ± 5% in a particular embodiment, and x ± 2% in a particular embodiment.

[0043] As used herein, the term "number-mean molecular weight" refers to the usual arithmetic mean of the molecular weights of individual polymers.

[0044] As used herein with respect to the compounds of the present invention, the term "water-soluble" means that at least 1 g of the compound can dissolve in 1 liter of water at 20°C to form a homogeneous solution. Therefore, the term "water-insoluble" with respect to the compounds means that less than 1 g of the compound can dissolve in 1 liter of water at 20°C to form a homogeneous solution.

[0045] As used herein with respect to a portion or reagent, the term “PEG-based” means that the portion or reagent contains PEG. In a particular embodiment, the PEG-based portion or reagent contains at least 90% (w / w) PEG, such as at least 10% (w / w) PEG, e.g., at least 20% (w / w) PEG, e.g., at least 30% (w / w) PEG, e.g., at least 40% (w / w) PEG, e.g., at least 50% (w / w), e.g., at least 60% (w / w) PEG, e.g., at least 70% (w / w) PEG, e.g., at least 80% (w / w) PEG, e.g., at least 95%, etc. The remaining weight percentage of the PEG-based portion or reagent is, in a particular embodiment, other portions selected from the following portions and conjugates: - C 1-50 Alkyl, C 2-50 Alkenil, C 2-50 Alkinyl, C 3-10 Cycloalkyls, 3-10 membered heterocyclyls, 8-11 membered heterobicyclyls, phenyl, naphthyl, indenyl, indanyl, and tetralinyl, and - A combination selected from the group including the following: [ka] (In the formula, The dashed line indicates binding to a portion or the remainder of the reagent. -R and -R a (These are independently selected from the group consisting of -H, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-methylbutyl, 2,2-dimethylpropyl, n-hexyl, 2-methylpentyl, 3-methylpentyl, 2,2-dimethylbutyl, 2,3-dimethylbutyl, and 3,3-dimethylpropyl).

[0046] As used herein, the term "substituted" means that one or more -H atoms in a molecule or part are substituted by different atoms or groups of atoms, which are called "substituents."

[0047] In certain embodiments, one or more further optional substituents may be halogen, -CN, or -COOR, independently of each other. x1 , -OR x1 , -C(O)R x1 ,-C(O)N(R x1 R x1a ), -S(O)2N(R x1 R x1a ), -S(O)N(R x1 R x1a ), -S(O)2R x1 ,-S(O)R x1 , -N(R x1 )S(O)2N(R x1a R x1b ), -SR x1 , -N(R x1 R x1a ), -NO2, -OC(O)R x1 , -N(R x1 )C(O)R x1a , -N(R x1 )S(O)2R x1a , -N(R x1 )S(O)R x1a , -N(R x1 )C(O)OR x1a , -N(R x1 )C(O)N(R x1a R x1b ), -OC(O)N(R x1 R x1a ), -T 0 , C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T 0 , C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. x2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has -T 0 -, -C(O)O-, -O-, -C(O)-, -C(O)N(R x3 )-,-S(O)2N(R x3 )-,-S(O)N(Rx3 ) -, -S(O)2-, -S(O)-, -N(R x3 )S(O)2N(R x3a ) -, -S-, -N(R x3 ) -, -OC(OR x3 )(R x3a ) -, -N(R x3 )C(O)N(R x3a ) -, and -OC(O)N(R x3 ) - from the group consisting of one or more groups selected may optionally be interrupted, -R x1 , -R x1a , -R x1b are, independently of each other, -H, -T 0 , C 1-50 alkyl, C 2-50 alkenyl, and C 2-50 alkynyl selected from the group consisting of, where, -T 0 , C 1-50 alkyl, C 2-50 alkenyl, and C 2-50 alkynyl are optionally substituted with one or more -R x2 and C 1-50 alkyl, C 2-50 alkenyl, and C 2-50 alkynyl include, -T 0 -, -C(O)O-, -O-, -C(O)-, -C(O)N(R x3 ) -, -S(O)2N(R x3 ) -, -S(O)N(R x3 ) -, -S(O)2-, -S(O)-, -N(R x3 )S(O)2N(R x3a ) -, -S-, -N(R x3 ) -, -OC(OR x3 [[ID=6)5]])(R x3a ) -, -N(R x3 [[ID=6)9]])(R<00)0097>) -, and -OC(O)N(R x3 ) - from the group consisting of one or more groups selected may optionally be interrupted, each T 0 is, independently, phenyl, naphthyl, indenyl, indanyl, tetralinyl, C 3-10Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclyls, and 8-11 membered heterobicyclyls, each T 0 These are independently one or more -Rs, the same or different. x2 It is sometimes replaced by, Each-R x2 These are, independently, halogen, -CN, oxo (=O), and -COOR. x4 , -OR x4 , -C(O)R x4 ,-C(O)N(R x4 R x4a ), -S(O)2N(R x4 R x4a ), -S(O)N(R x4 R x4a ), -S(O)2R x4 ,-S(O)R x4 , -N(R x4 )S(O)2N(R x4a R x4b ), -SR x4 , -N(R x4 R x4a ), -NO2, -OC(O)R x4 , -N(R x4 )C(O)R x4a , -N(R x4 )S(O)2R x4a , -N(R x4 )S(O)R x4a , -N(R x4 )C(O)OR x4a , -N(R x4 )C(O)N(R x4a R x4b ), -OC(O)N(R x4 R x4a ), and C 1-6 Selected from the group consisting of alkyl groups, C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each-R x3 , -R x3a , -R x4 , -R x4a , -R x4b These are independently -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6Alkyl atoms are sometimes substituted with one or more halogens, either the same or different.

[0048] In certain embodiments, one or more further optional substituents may be halogen, -CN, or -COOR, independently of each other. x1 , -OR x1 , -C(O)R x1 ,-C(O)N(R x1 R x1a ), -S(O)2N(R x1 R x1a ), -S(O)N(R x1 R x1a ), -S(O)2R x1 ,-S(O)R x1 , -N(R x1 )S(O)2N(R x1a R x1b ), -SR x1 , -N(R x1 R x1a ), -NO2, -OC(O)R x1 , -N(R x1 )C(O)R x1a , -N(R x1 )S(O)2R x1a , -N(R x1 )S(O)R x1a , -N(R x1 )C(O)OR x1a , -N(R x1 )C(O)N(R x1a R x1b ), -OC(O)N(R x1 R x1a ), -T 0 , C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Selected from the group consisting of alkynnyls, where -T 0 , C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Alkinyl has one or more -Rs, which may be the same or different. x2 In some cases, it is replaced by C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Alkinyl has -T 0-, -C(O)O-, -O-, -C(O)-, -C(O)N(R x3 )-,-S(O)2N(R x3 )-,-S(O)N(R x3 )-, -S(O)2-, -S(O)-, -N(R x3 )S(O)2N(R x3a )-, -S-, -N(R x3 )-, -OC(OR x3 )(R x3a )-,-N(R x3 )C(O)N(R x3a )-, and -OC(O)N(R x3 )- may intersect with one or more groups selected from the group consisting of, Each-R x1 , -R x1a , -R x1b , -R x3 , -R x3a These are independently -H, halogen, and C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Selected from the group consisting of alkynnyls, Each T 0 These are independently phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclyls, and 8-11 membered heterobicyclyls, where each T 0 These are independently one or more -Rs, the same or different. x2 It is sometimes replaced by, Each-R x2 These are, independently, halogen, -CN, oxo (=O), and -COOR. x4 , -OR x4 , -C(O)R x4 ,-C(O)N(R x4 R x4a ), -S(O)2N(R x4 R x4a ), -S(O)N(R x4 R x4a ), -S(O)2R x4 ,-S(O)R x4 , -N(R x4 )S(O)2N(R x4a R x4b), -SR x4 , -N(R x4 R x4a ), -NO2, -OC(O)R x4 , -N(R x4 )C(O)R x4a , -N(R x4 )S(O)2R x4a , -N(R x4 )S(O)R x4a , -N(R x4 )C(O)OR x4a , -N(R x4 )C(O)N(R x4a R x4b ), -OC(O)N(R x4 R x4a ), and C 1-6 Selected from the group consisting of alkyl groups, C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each-R x4 , -R x4a , -R x4b These are independently -H, halogen, and C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Selected from the group consisting of alkynnyls.

[0049] In certain embodiments, one or more further optional substituents may be halogen, -CN, or -COOR, independently of each other. x1 , -OR x1 , -C(O)R x1 ,-C(O)N(R x1 R x1a ), -S(O)2N(R x1 R x1a ), -S(O)N(R x1 R x1a ), -S(O)2R x1 ,-S(O)R x1 , -N(R x1 )S(O)2N(R x1a R x1b ), -SR x1 , -N(R x1 R x1a ), -NO2, -OC(O)R x1 , -N(R x1)C(O)R x1a , -N(R x1 )S(O)2R x1a , -N(R x1 )S(O)R x1a , -N(R x1 )C(O)OR x1a , -N(R x1 )C(O)N(R x1a R x1b ), -OC(O)N(R x1 R x1a ), -T 0 , C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Selected from the group consisting of alkynnyls, where -T 0 , C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Alkinyl has one or more -Rs, which may be the same or different. x2 In some cases, it is replaced by C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Alkinyl has -T 0 -, -C(O)O-, -O-, -C(O)-, -C(O)N(R x3 )-,-S(O)2N(R x3 )-,-S(O)N(R x3 )-, -S(O)2-, -S(O)-, -N(R x3 )S(O)2N(R x3a )-, -S-, -N(R x3 )-, -OC(OR x3 )(R x3a )-,-N(R x3 )C(O)N(R x3a )-, and -OC(O)N(R x3 )- may intersect with one or more groups selected from the group consisting of, Each-R x1 , -R x1a , -R x1b , -R x2 , -R x3 , -R x3a These are independently -H, halogen, and C 1-6 Alkyl, C 2-6 Alkenyl and C2-6 Selected from the group consisting of alkynnyls, Each T 0 These are independently phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclyls, and 8-11 membered heterobicyclyls, where each T 0 These are independently one or more -Rs, the same or different. x2 It is sometimes replaced.

[0050] In certain embodiments, up to six -H atoms of the optionally substituted molecule are independently substituted by substituents, for example, five -H atoms are independently substituted by substituents, four -H atoms are independently substituted by substituents, three -H atoms are independently substituted by substituents, two -H atoms are independently substituted by substituents, or one -H atom is independently substituted by substituents.

[0051] The term “inserted” means that a portion is inserted between two carbon atoms, or, if the insertion is at one of the ends of the portion, between a carbon or heteroatom and a hydrogen atom, or in certain embodiments, between a carbon and a hydrogen atom.

[0052] As used herein, the term "monocyclic or bicyclic aryl" means an aromatic hydrocarbon ring system that may be monocyclic or bicyclic, where a monocyclic aryl ring consists of at least five ring carbon atoms and may contain up to ten ring carbon atoms, and a bicyclic aryl ring consists of at least eight ring carbon atoms and may contain up to twelve ring carbon atoms. Each hydrogen atom of a monocyclic or bicyclic aryl may be substituted by a substituent as defined below.

[0053] As used herein, the term "monocyclic or bicyclic heteroaryl" means a monocyclic aromatic ring system that may contain 2 to 6 ring carbon atoms and 1 to 3 ring heteroatoms, or a bicyclic aromatic ring system that may contain 3 to 9 ring carbon atoms and 1 to 5 ring heteroatoms, such as nitrogen, oxygen, and sulfur. Examples of monocyclic or bicyclic heteroaryl groups include, but are not limited to, benzofuranyl, benzothiophenyl, furanyl, imidazolyl, indolyl, azaindolyl, azabenzimidazolyl, benzoxazolyl, benzothiazolyl, benzothiadiazolyl, benzotriazolyl, tetradinyl, tetrazolyl, isothiazolyl, oxazolyl, isoxazolyl, pyrazinyl, pyrazolyl, pyridadinyl, pyridinyl, pyrimidinyl, pyrrolyl, quinolinyl, quinazolinyl, quinoxalinyl, triazolyl, thiazolyl, and thiophenyl. Each hydrogen atom in a monocyclic or bicyclic heteroaryl compound may be substituted with a substituent as defined below.

[0054] As used herein, the term "cleavable trigger portion (-Tr)" refers to a portion that can be chemically or enzymatically cleaved under physiological conditions (aqueous buffer solution, pH 7.4, 37°C), and which, upon cleavage of the cleavable trigger portion, releases at least two drug portions, including an albumin-binding portion.

[0055] The term "C" as used herein 1-4 "Alkyl" refers to a linear or branched alkyl moiety, either alone or in combination, having 1 to 4 carbon atoms. When present at the end of a molecule, it refers to a linear or branched C 1-4 Examples of alkyl groups include methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, and tert-butyl. Two parts of the molecule are C 1-4 If bonded by an alkyl group, such C 1-4 Examples of alkyl groups are -CH2-, -CH2-CH2-, -CH(CH3)-, -CH2-CH2-CH2-, -CH(C2H5)-, and -C(CH3)2-. 1-4Each hydrogen atom of the alkyl carbon may optionally be substituted with a substituent as defined above. Optionally, C 1-4 Alkyl may have one or more parts, as defined below, interspersed within it.

[0056] As used herein, the term "nucleophile" refers to a reagent or functional group that forms a bond with its reaction partner, i.e., an electrophile, by donating both bonding electrons.

[0057] The term "C" as used herein 1-6 "Alkyl" refers to a linear or branched alkyl moiety, either alone or in combination, having 1 to 6 carbon atoms. When present at the end of a molecule, it refers to linear and branched C atoms. 1-6 Examples of alkyl groups include methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-methylbutyl, 2,2-dimethylpropyl, n-hexyl, 2-methylpentyl, 3-methylpentyl, 2,2-dimethylbutyl, 2,3-dimethylbutyl, and 3,3-dimethylpropyl. Two parts of the molecule are C 1-6 If bonded by an alkyl group, such C 1-6 Examples of alkyl groups are -CH2-, -CH2-CH2-, -CH(CH3)-, -CH2-CH2-CH2-, -CH(C2H5)-, and -C(CH3)2-. 1-6 Each hydrogen atom of carbon may optionally be substituted with a substituent as defined above. 1-6 Alkyl may have one or more parts, as defined below, interspersed within it.

[0058] Therefore, "C 1-10 Alkyl," "C 1-20 "Alkyl" or "C 1-50 "Alkyl" refers to an alkyl chain having 1 to 10, 1 to 20, or 1 to 50 carbon atoms, respectively. 1-10 , C 1-20 or C 1-50Each hydrogen atom of carbon may optionally be substituted with a substituent as defined above. 1-10 or C 1-50 Alkyl may have one or more parts, as defined below, interspersed within it.

[0059] The term "C" as used herein 2-6 An "alkenyl" refers to a straight-chain or branched hydrocarbon moiety, either alone or in combination, containing 2 to 6 carbon atoms and at least one carbon-carbon double bond. When present at the ends of a molecule, examples include -CH=CH2, -CH=CH-CH3, -CH2-CH=CH2, -CH=CHCH2-CH3, and -CH=CH-CH=CH2. Two parts of a molecule are C 2-6 When bonded by an alkenyl group, such C 2-6 An example of an alkenil is -CH=CH-. 2-6 Each hydrogen atom of the alkenyl moiety may optionally be substituted with a substituent as defined above. Optionally, C 2-6 An alkenil may have one or more parts, as defined below, inserted into it.

[0060] Therefore, the term "C 2-10 Alkenil, "C 2-20 "Alkenil" or "C 2-50 "Alkenyl" means a linear or branched hydrocarbon moiety, either alone or in combination, having 2 to 10, 2 to 20, or 2 to 50 carbon atoms and containing at least one carbon-carbon double bond. 2-10 Alkenil, C 2-20 Alkenyl or C 2-50 Each hydrogen atom of the alkenyl group may optionally be substituted with a substituent as defined above. Optionally, C 2-10 Alkenil, C 2-20 Alkenyl or C 2-50 An alkenil may have one or more parts, as defined below, inserted into it.

[0061] The term "C" as used herein 2-6"Alkynyl" refers to a linear or branched hydrocarbon moiety, either alone or in combination, containing 2 to 6 carbon atoms and at least one carbon-carbon triple bond. When present at the end of a molecule, examples include -C≡CH, -CH2-C≡CH, CH2-CH2-C≡CH, and CH2-C≡C-CH3. When two parts of a molecule are linked by an alkynyl group, an example is -C≡C-. 2-6 Each hydrogen atom of the alkynyl group may optionally be substituted with a substituent as defined above. Optionally, one or more double bonds may be present. Optionally, C 2-6 Alkinyl may have one or more parts, as defined below, inserted into it.

[0062] Therefore, the term "C" as used herein 2-10 Alkinyl, C 2-20 "Alkinyl" and "C 2-50 "Alkynyl" means a linear or branched hydrocarbon moiety, either alone or in combination, containing at least one carbon-carbon triple bond, each having 2 to 10, 2 to 20, or 2 to 50 carbon atoms, respectively. 2-10 Alkinyl, C 2-20 Alkinyl or C 2-50 Each hydrogen atom of the alkynyl group may optionally be substituted with a substituent as defined above. Optionally, one or more double bonds may be present. Optionally, C 2-10 Alkinyl, C 2-20 Alkinyl or C 2-50 Alkinyl may have one or more parts, as defined below, inserted into it.

[0063] As stated above, C 1-4 Alkyl, C 1-6 Alkyl, C 1-10 Alkyl, C 1-20 Alkyl, C 1-50 Alkyl, C 2-6 Alkenil, C 2-10 Alkenil, C 2-20 Alkenil, C 2-50 Alkenil, C 2-6 Alkinyl, C 2-10 Alkinyl, C2-20 Alkenyl or C 2-50 Alkinyl may have one or more parts interspersed in it, and in certain embodiments, these one or more parts are [ka] (In the formula, The dashed line indicates binding to a portion or the remainder of the reagent. -R and -R a (These are independently selected from the group consisting of -H, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-methylbutyl, 2,2-dimethylpropyl, n-hexyl, 2-methylpentyl, 3-methylpentyl, 2,2-dimethylbutyl, 2,3-dimethylbutyl, and 3,3-dimethylpropyl.) It is selected from the group consisting of the following.

[0064] The term "C" as used herein 3-10 "Cycloalkyl" means a cyclic alkyl chain having 3 to 10 carbon atoms, which may be saturated or unsaturated, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, cycloheptyl, cyclooctyl, cyclononyl, or cyclodecyl. 3-10 Each hydrogen atom of the cycloalkyl carbon may be substituted with a substituent as defined above. 3-10 "Cycloalkyl" also includes cross-linked birings such as norbornane or norbornene.

[0065] The term “8-30 membered carbopolycyclil” or “8-30 membered carbopolycycle” refers to a cyclic portion of two or more rings having 8 to 30 ring atoms, where two adjacent rings share at least one ring atom and may contain up to a maximum number of double bonds (fully saturated, partially saturated, or unsaturated aromatic or non-aromatic rings). In certain embodiments, an 8-30 membered carbopolycyclil refers to a cyclic portion of 2, 3, 4, or 5 rings, and in certain embodiments, a cyclic portion of 2, 3, or 4 rings.

[0066] As used herein, the terms “3- to 10-membered heterocyclil” or “3- to 10-membered heterocycle” mean a ring (fully saturated, partially saturated, or unsaturated aromatic or non-aromatic ring) having 3, 4, 5, 6, 7, 8, 9, or 10 ring atoms and potentially containing up to a maximum number of double bonds, wherein at least one ring atom and up to four ring atoms are substituted with heteroatoms selected from the group consisting of sulfur (including -S(O)- and -S(O)2-), oxygen, and nitrogen (including =N(O)-), and the ring is bonded to the remainder of the molecule via carbon or nitrogen atoms. Examples of heterocycles with 3 to 10 members include, but are not limited to, aziridine, oxirane, thiirane, azirine, oxilen, thiirane, azetidine, oxetane, thietan, furan, thiophene, pyrrole, pyrroline, imidazole, imidazoline, pyrazole, pyrazoline, oxazole, oxazoline, isoxazole, isoxazoline, thiazole, thiazoline, isothiazole, isothiazoline, thiadiazole, thiadiazole, tetrahydrofuran Examples include tetrahydrothiophene, pyrrolidine, imidazolidine, pyrazolidine, oxazolidine, isoxazolidine, thiazolidin, isothiazolidine, thiadiazolidin, sulfolane, pyran, dihydropyran, tetrahydropyran, imidazolidine, pyridine, pyridazine, pyrazine, pyrimidine, piperazine, piperidine, morpholine, tetrazole, triazole, triazolidine, tetrazolidin, diazepane, azepine and homopiperazine. Each hydrogen atom of a 3-10 membered heterocyclyl or 3-10 membered heterocyclic group may be substituted with substituents defined below.

[0067] As used herein, the terms “8- to 11-membered heterobicyryl” or “8- to 11-membered heterobicyclic” mean a bicyclic heterocyclic portion having 8 to 11 ring atoms (fully saturated, partially saturated, or unsaturated aromatic or non-aromatic ring) in which at least one ring atom is shared by both rings and may contain up to a maximum number of double bonds, wherein at least one ring atom and up to six ring atoms are substituted with heteroatoms selected from the group consisting of sulfur (including -S(O)-, -S(O)2-), oxygen, and nitrogen (including =N(O)-), and the ring is bonded to the remainder of the molecule via carbon or nitrogen atoms. Examples of 8- to 11-membered heterobicyclic compounds include indole, indoline, benzofuran, benzothiophene, benzoxazole, benzoisoxazole, benzothiazole, benzoisothiazole, benzimidazole, benzimidazolin, quinoline, quinazoline, dihydroquinazoline, quinoline, dihydroquinoline, tetrahydroquinoline, decahydroquinoline, isoquinoline, decahydroisoquinoline, tetrahydroisoquinoline, dihydroisoquinoline, benzazepine, purine, and pteridine. The term 8- to 11-membered heterobicyclic compound also includes bicyclic spiro structures such as 1,4-dioxa-8-azaspiro[4.5]decane, or bridging heterocyclic compounds such as 8-aza-bicyclo[3.2.1]octane. Each hydrogen atom of the carbon atom of an 8- to 11-membered heterobicyclyl or 8- to 11-membered heterobicyclic compound may be substituted with substituents as defined below.

[0068] Similarly, the term “8-30 membered heteropolycyclil” or “8-30 membered heteropolycycle” means a heterocyclic moiety (fully saturated, partially saturated, or unsaturated aromatic or non-aromatic ring) having more than two rings, or in particular embodiments, three, four, or five rings, wherein two adjacent rings share at least one ring atom and may contain up to a maximum number of double bonds, wherein at least one ring atom, up to a maximum of ten ring atoms, is substituted with a heteroatom selected from the group consisting of sulfur (including -S(O)- and -S(O)2-), oxygen, and nitrogen (including =N(O)-), and the ring is bonded to the remainder of the molecule via carbon or nitrogen atoms.

[0069] structure [ka] Regarding the part, "Pair R x / R y Together with the atoms to which they are bonded, C 3-10 The phrase "forms a cycloalkyl or a 3-10 member heterocycline" is R x and R y However, it is understood that this means forming the following structure: [ka] (In the formula, R is C 3-10 (It is a cycloalkyl or a 3- to 10-membered heterocycline.)

[0070] structure [ka] Regarding the part, "Pair R x / R y The phrase "they, together with the atoms to which they are bonded, form ring A" is R x and R y However, it is also understood that this means forming the following structure: [ka]

[0071] As used herein, "halogen" means fluoro, chloro, bromo, or iodine. In certain embodiments, the halogen is fluoro or chloro.

[0072] Generally, the terms "comprise" or "comprising" also include "consist of" or "consisting of."

[0073] The compound of the present invention is -L 1 When the bond between - and -D- is broken, the compound HD-AB is released, where H- is hydrogen. The compound of the present invention is, for example, -L 1 - or -L 1' When semaglutide is included in a combined form, such as being conjugated to -, the semaglutide moiety-D-AB may be referred to as semaglutide in this specification for simplicity, even though strictly speaking it is a "semaglutide moiety".

[0074] The compound releases the corresponding free drug of partial-D-AB, which is HD-AB, where H- is hydrogen.

[0075] In certain embodiments, the compound comprises at least one polymer moiety conjugated with at least two moieties of formula (I), where formula (I) is [ka] (In the formula, Each-L 2 - is either an independent spacer part or does not exist. Each-L 1 - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each -D- is an independent drug portion. Each -AB is an independently albumin-binding moiety. That is the case.

[0076] In certain embodiments, the compound comprises at least one polymer moiety conjugated with at least one portion of formula (I'), where formula (I') is [ka] (In the formula, Each-L 2 - is either an independent spacer part or does not exist. Each-L 1' - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each -D- is an independent drug portion. Each -AB is an albumin-binding moiety independently. Each a is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. That is the case.

[0077] In certain embodiments, the compound comprises two parts of formula (I). In certain embodiments, the compound comprises three parts of formula (I). In certain embodiments, the compound comprises four parts of formula (I). In certain embodiments, the compound comprises five parts of formula (I). In certain embodiments, the compound comprises six parts of formula (I). In certain embodiments, the compound comprises seven parts of formula (I). In certain embodiments, the compound comprises eight parts of formula (I).

[0078] In certain embodiments, at least one polymer portion of the compound of the present invention is a linear polymer portion -P-.

[0079] In certain embodiments, the portion of formula (I) or (I') is conjugated to each of the two ends of such a linear portion -P-.

[0080] In certain embodiments, the compound is of formula (Ia) or (I-a') [ka] (In the formula, Each-L 2 - is either an independent spacer part or does not exist. Each-L 1 - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each-L 1' - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each -D- is an independent drug portion. Each -AB is an albumin-binding moiety independently. -P- is the polymer part, Each a is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. It belongs to them.

[0081] In certain embodiments, the compound is of formula (Ia). In certain embodiments, the compound is of formula (I-a').

[0082] Part-L 1' - is conjugated into two or more parts -D-, -L 1' It is understood that all bonds between - and part-D- are covalent and reversible.

[0083] In certain embodiments, both a in formula (I-a') are the same integer. In certain embodiments, both a in formula (I-a') are 2. In certain embodiments, both a in formula (I-a') are 3. In certain embodiments, both a in formula (I-a') are 4. In certain embodiments, both a in formula (I-a') are 5. In certain embodiments, both a in formula (I-a') are 6. In certain embodiments, both a in formula (I-a') are 7. In certain embodiments, both a in formula (I-a') are 8. In certain embodiments, both a in formula (I-a') are 9. In certain embodiments, both a in formula (I-a') are 10. In certain embodiments, both a in formula (I-a') are 11. In certain embodiments, both a in formula (I-a') are 12. In certain embodiments, both a in formula (I-a') are 13. In certain embodiments, both a's in formula (I-a') are 14. In certain embodiments, both a's in formula (I-a') are 15. In certain embodiments, both a's in formula (I-a') are 16.

[0084] In some cases, further parts of equation (I) or (I') are conjugated to the -P- of equation (Ia) or (I-a').

[0085] In certain embodiments, further parts of formula (I) or (I') are not conjugated to the -P- of formula (Ia) or (I-a').

[0086] The part -P- in formula (Ia) or (I-a') is one or more polymers, e.g., poly(2-methacryloyloxyethylphosphoryl(phosphoyl)choline), poly(acrylic acid), poly(acrylate), poly(acrylamide), poly(alkoxy)polymer, poly(amide), poly(amideamine), poly(amino acid), poly(acid anhydride), poly(aspartamide), poly(hydroxybutyrate), poly(glycolic acid), polybutylene terephthalate, poly(caprolactone), poly(carbonate), poly(cyanoacrylate), poly(dimethylacrylamide), poly(ester), poly(ethylene), poly(ethylene glycol), poly(ethylene oxide), poly(ethylene phosphate), poly(ethyl oxazoline), poly(glycolic acid), poly(hydroxyethyl acrylate), poly(hydroxyethyl oxazoline), poly(2-hydroxyethyl methacrylate), poly(N-(2-hydroxypropyl)methacrylamide The polymers include polymers selected from the group consisting of poly(hydroxypropyl methacrylate), poly(hydroxypropyl oxazoline), poly(iminocarbonate), poly(lactic acid), poly(lactic acid-co-glycolic acid), poly(methacrylamide), poly(methacrylate), poly(methyloxazoline), poly(organophosphazene), poly(orthoester), poly(oxazoline), poly(propylene glycol), poly(siloxane), poly(urethane), poly(vinyl alcohol), poly(vinylamine), poly(vinyl methyl ether), poly(vinylpyrrolidone), cellulose, carboxymethylcellulose, hydroxypropyl methylcellulose, chitin, chitosan, dextran, dextrin, gelatin, hyaluronic acid and its derivatives, functionalized hyaluronic acid, mannan, pectin, rhamnogalacturonan, starch, hydroxyalkyl starch, hydroxyethyl starch and other carbohydrate polymers, xylan, and copolymers thereof.

[0087] In certain embodiments, -P- in formula (Ia) or (I-a') is 2-methacryloyloxyethyl phosphorylcholine, poly(acrylic acid), poly(acrylate), poly(acrylamide), poly(alkyloxy)polymer, poly(amide), poly(amideamine), poly(amino acid), poly(acid anhydride), poly(aspartamide), poly(butyric acid), poly(glycolic acid), polybutylene terephthalate, poly(caprolactone), poly(carbonate), poly(cyanoacrylate), poly(dimethylacrylamide), poly(ester), poly(ethylene), poly(ethylene glycol), poly(ethylene oxide), poly(ethyl phosphate), poly(ethyl oxazoline), poly(glycolic acid), poly(hydroxyethyl acrylate), poly(hydroxyethyl oxazoline), poly(hydroxymethacrylate), poly(hydroxypropyl methacrylamide), poly(hydroxypropyl methacrylate) The polymer comprises one or more polymers selected from the group consisting of poly(hydroxypropyl oxazoline), poly(iminocarbonate), poly(lactic acid), poly(lactic acid-co-glycolic acid), poly(methacrylamide), poly(methacrylate), poly(methyl oxazoline), poly(organophosphazene), poly(orthoester), poly(oxazoline), poly(propylene glycol), poly(siloxane), poly(urethane), poly(vinyl alcohol), poly(vinylamine), poly(vinyl methyl ether), poly(vinylpyrrolidone), silicone, cellulose, carbomethylcellulose, hydroxypropyl methylcellulose, chitin, chitosan, dextran, dextrin, gelatin, hyaluronic acid and its derivatives, functionalized hyaluronic acid, mannan, pectin, rhamnogalacturonan, starch, hydroxyalkyl starch, hydroxyethyl starch and other carbohydrate polymers, xylan, and copolymers thereof.

[0088] In certain embodiments, the -P- in formula (Ia) or (I-a') is a PEG-based or hyaluronic acid-based portion. In certain embodiments, the -P- in formula (Ia) or (I-a') is a PEG-based portion. In certain embodiments, the -P- in formula (Ia) or (I-a') is a hyaluronic acid-based portion.

[0089] In certain embodiments, -P- in formula (Ia) or (I-a') is equivalent to formula (I-ai) [ka] (In the formula, The dashed line is -L 2 - indicates binding to n is an integer such that the molecular weight of the PEG portion is in the range of approximately 1 to approximately 20 kDa. -X 1 - and -X 2 - are independent of each other: -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O)2N(R y1 )-,-S(O)N(R y1 )-, -S(O)2-, -S(O)-, -N(R y1 )S(O)2N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R)y3 )-,-S(O)2N(R y3 )-,-S(O)N(R y3 )-, -S(O)2-, -S(O)-, -N(R y3 )S(O)2N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3 )(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(R y3 )- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a These are -H, -T, and C, which are independent of each other. 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynyls, where -T, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y4 )-,-S(O)2N(R y4 )-,-S(O)N(R y4 )-, -S(O)2-, -S(O)-, -N(R y4 )S(O)2N(R y4a )-, -S-, -N(R y4 )-, -OC(OR y4 )(R y4a )-,-N(R y4 )C(O)N(R y4a )-, and -OC(O)N(R y4 )- may intersect with one or more groups selected from the group consisting of, Each T independently consists of phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C. 3-10Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, where each T is independently one or more identical or different -R y2 It is sometimes replaced by, Each-R y2 These are, independently, halogen, -CN, oxo (=O), and -COOR. y5 , -OR y5 , -C(O)R y5 ,-C(O)N(R y5 R y5a ), -S(O)2N(R y5 R y5a ), -S(O)N(R y5 R y5a ), -S(O)2R y5 ,-S(O)R y5 , -N(R y5 )S(O)2N(R y5a R y5b ), -SR y5 , -N(R y5 R y5a ), -NO2, -OC(O)R y5 , -N(R y5 )C(O)R y5a , -N(R y5 )S(O)2R y5a , -N(R y5 )S(O)R y5a , -N(R y5 )C(O)OR y5a , -N(R y5 )C(O)N(R y5a R y5b ), -OC(O)N(R y5 R y5a ), and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each-R y3 , -R y3a , -R y4 , -R y4a , -R y5 , -R y5a and -R y5b These are independently -H and C1-6 Selected from the group consisting of alkyl groups, where C 1-6 (Alkyl is sometimes substituted with one or more halogens, either the same or different.) It belongs to them.

[0090] In certain embodiments, n in formula (I-ai) is in the range of 2 to 22.

[0091] In a particular embodiment, -X in formula (I-ai) 1 - and -X 2 - are independent of each other: -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O)2N(R y1 )-,-S(O)N(R y1 )-, -S(O)2-, -S(O)-, -N(R y1 )S(O)2N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T-, C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y3 )-,-S(O)2N(R y3 )-,-S(O)N(R y3 )-, -S(O)2-, -S(O)-, -N(R y3 )S(O)2N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3)(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(R y3 )- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a These are -H, -T, and C, which are independent of each other. 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Selected from the group consisting of alkynyls, where -T, C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y4 )-,-S(O)2N(R y4 )-,-S(O)N(R y4 )-, -S(O)2-, -S(O)-, -N(R y4 )S(O)2N(R y4a )-, -S-, -N(R y4 )-, -OC(OR y4 )(R y4a )-,-N(R y4 )C(O)N(R y4a )-, and -OC(O)N(R y4 )- may intersect with one or more groups selected from the group consisting of, Each T independently consists of phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C. 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, where each T is independently one or more identical or different -R y2 It is sometimes replaced by, -R y2 These are halogen, -CN, oxo (=O), and -COOR.y5 , -OR y5 , -C(O)R y5 ,-C(O)N(R y5 R y5a ), -S(O)2N(R y5 R y5a ), -S(O)N(R y5 R y5a ), -S(O)2R y5 ,-S(O)R y5 , -N(R y5 )S(O)2N(R y5a R y5b ), -SR y5 , -N(R y5 R y5a ), -NO2, -OC(O)R y5 , -N(R y5 )C(O)R y5a , -N(R y5 )S(O)2R y5a , -N(R y5 )S(O)R y5a , -N(R y5 )C(O)OR y5a , -N(R y5 )C(O)N(R y5a R y5b ), -OC(O)N(R y5 R y5a ), and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each-R y3 , -R y3a , -R y4 , -R y4a , -R y5 , -R y5a and -R y5b These are, independently of each other, -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl atoms are sometimes substituted with one or more halogens, either the same or different.

[0092] In a particular embodiment, -X in formula (I-ai) 1 - and -X 2- are independent of each other: -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O)2N(R y1 )-,-S(O)N(R y1 )-, -S(O)2-, -S(O)-, -N(R y1 )S(O)2N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y3 )-,-S(O)2N(R y3 )-,-S(O)N(R y3 )-, -S(O)2-, -S(O)-, -N(R y3 )S(O)2N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3 )(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(R y3 )- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a These are independently -H, -T, and C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Selected from the group consisting of alkynnyls, Each T independently consists of phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C. 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, Each-R y2 These are, independently, halogen and C 1-6 Selected from the group consisting of alkyl groups, Each-R y3 , -R y3a , -R y4 , -R y4a , -R y5 , -R y5a and -R y5b These are, independently of each other, -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl atoms are sometimes substituted with one or more halogens, either the same or different.

[0093] In certain embodiments, -P- in formula (Ia) or (I-a') is equivalent to formula (I-ai-i) [ka] [In the formula, The dashed line is -L 2 - indicates binding to Each-X A - is independent, [ka] TIFF2026509252000018.tif245168TIFF2026509252000019.tif245168TIFF2026509252000020.tif233167T IFF2026509252000021.tif233167TIFF2026509252000022.tif233167TIFF2026509252000023.tif87168(in the formula, The dashed line is -L 2 - indicates a connection to the remainder of the part of expression (I-ai-i), Each-R 04, -R 04a , -R 04b and -R 04c These are, independently, halogen, -H, -CN, and -T 0 , C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T 0 , C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. 06 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has -T 0 -, -C(O)O-, -O-, -C(O)-, -C(O)N(R0 7 )-,-S(O)2N(R 07 )-,-S(O)N(R 07 )-, -S(O)2-, -S(O)-, -N(R 07 )S(O)2N(R 07a )-, -S-, -N(R 07 )-, -OC(OR 07 )(R 07a )-,-N(R 07 )C(O)N(R 07a )-, and -OC(O)N(R 07 )- may intersect with one or more groups selected from the group consisting of, Each T 0 These are independently phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclyls, and 8-11 membered heterobicyclyls, where each T 0 These are independently one or more -Rs, the same or different. 06 It is sometimes replaced by, Each-R 06 , -R 07 and -R 07a These are independently -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6(Alkyl is sometimes substituted with one or more halogens, either the same or different.) Selected from the group consisting of, Each b is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. Each c is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. n is an integer such that the molecular weight of the PEG portion is in the range of approximately 1 kDa to approximately 20 kDa. It belongs to them.

[0094] In certain embodiments, n in formula (I-ai-i) is in the range of 2 to 22, i.e., n is selected from the group consisting of 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, and 22 in certain embodiments. Generally, based on the number of ethylene glycol units, the molecular weight of the PEG portion can be calculated by multiplying the number of ethylene glycol units by 0.044 kDa.

[0095] In a particular embodiment, both parts - X A - is identical. In certain embodiments, part -X A - is different from each other.

[0096] In a particular embodiment, part-X A - is selected from the group consisting of equations (x-1), (x-2), (x-3), (x-4), (x-5), (x-6), (x-7), (x-8), (x-9), (x-10), (x-11), (x-12), (x-13), (x-14), (x-15), (x-16), (x-17), (x-18), (x-19), (x-20), (x-21), (x-22), and (x-23). ​​In certain embodiments, part -X A- is selected from the group consisting of equations (x-1), (x-2), (x-3), (x-5), (x-6), (x-7), (x-8), (x-12), (x-13), (x-14), (x-15), (x-16), (x-17), (x-18), (x-19), (x-20), (x-21), (x-22), and (x-23). ​​In certain embodiments, part -X A - is selected from the group consisting of equations (x-1), (x-2), (x-3), (x-5), (x-6), (x-7), (x-8), (x-12), (x-13), (x-14), (x-15), (x-16), (x-17), (x-18), (x-19), (x-20), and (x-21). In certain embodiments, part -X A - is selected from the group consisting of equations (x-1), (x-2), (x-3), (x-5), (x-12), (x-13), (x-14), (x-15), (x-16), (x-17), and (x-18).

[0097] In certain embodiments, the formula -R 04 is -H. In certain embodiments, -R 04a is -H. In certain embodiments, -R 04b is -H. In certain embodiments, -R 04c It is -H.

[0098] In a particular embodiment, both -X A - is equation (x-1), and in particular equation (x-1') [ka] (In the formula, the dashed line with an asterisk represents -L) 2 (The dashed line without a mark indicates a connection to the remainder of -P-.) In certain embodiments, the dashed line with an asterisk represents -L 2 This shows the association with the (x-2) part of the equation.

[0099] In certain embodiments, -P- in formula (Ia) or (I-a') is equivalent to formula (I-aii) [ka] (In the formula, The dashed line is -L 2 - indicates binding to Each b is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. Each c is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. n is used as defined for n in equation (I-ai). It belongs to them.

[0100] In certain embodiments, -P- in formula (Ia) or (I-a') is equivalent to formula (I-aii') [ka] (In the formula, The dashed line is -L 2 - indicates binding to n is an integer such that the molecular weight of the PEG portion is in the range of approximately 1 to approximately 20 kDa. It belongs to them.

[0101] In certain embodiments, -P- in formula (Ia) or (I-a') is [ka] TIFF2026509252000028.tif242160TIFF2026509252000029.tif66161 (in the formula, The dashed line is -L 2 - indicates binding to -R 04 It is defined as described above, n is an integer such that the molecular weight of the PEG portion is in the range of approximately 1 to approximately 20 kDa. It is selected from the group consisting of the following.

[0102] In certain embodiments, the -R of formula (I-aii'-xiii), (I-aii'-xiv), (I-aii'-xv), or (I-aii'-xvi) 04 It is -H.

[0103] In certain embodiments, formulas (I-aii'-i), (I-aii'-ii), (I-aii'-iii), (I-aii'-iv), (I-aii'-v), (I-aii 'vi), (I-aii'-vii), (I-aii'-viii), (I-aii'-ix), (I-aii'-x), (I-aii'-xi), (I-aii'-xii In (I-aii'-xiii), (I-aii'-xiv), (I-aii'-xv), and (I-aii'-xvi), n is in the range of 2 to 22, that is, in a particular embodiment, n is selected from the group consisting of 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 32, and 22.

[0104] The dashed line in any one of the equations (I-aii'-i), (I-aii'-ii), (I-aii'-iii), and (I-aii'-vi) preferably represents -L via the part of equation (x-2). 2 - This shows the bond to, which is part of equation (x-162'). [ka] (In the formula, the dashed line with an asterisk represents -L) 2 (The dashed line indicates the connection to the remainder of -P-, and the unmarked dashed line indicates the connection to the remainder of -P-) It brings about.

[0105] The dashed line in any one of the equations (I-aii'-v), (I-aii'-vi), (I-aii'-vii), and (I-aii'-viii) preferably represents -L via the part of equation (x-1). 2 - This shows the bond to the part of equation (x-162'') [ka] (In the formula, the dashed line with an asterisk represents -L) 2 (The dashed line indicates the connection to the remainder of -P-, and the unmarked dashed line indicates the connection to the remainder of -P-) It brings about.

[0106] The dashed line in any one of the formulas (I-aii''-ix), (I-aii''-x), (I-aii''-xi), and (I-aii''-xii) preferably represents -L via the part of formula (x-13). 2 - This shows the bond to, which is part of equation (x-12'). [ka] (In the formula, the dashed line with an asterisk represents -L) 2 - indicates connection to the remainder, and the unmarked dashed line indicates connection to the remainder of -P-, and -R 04 (It is used as defined in equation (I-ai-i)) This results in -R of formula (x-12'). Preferably, 04 It is -H.

[0107] The dashed line in any one of the equations (I-aii''-xiii), (I-aii''-xiv), (I-aii''-xv), and (I-aii''-xvi) preferably represents -L via the part of equation (x-14). 2 - This shows the bond to the (x-12'') part of the equation. [ka] (In the formula, the dashed line with an asterisk represents -L) 2 - indicates connection to the remainder, and the unmarked dashed line indicates connection to the remainder of -P-, and -R 04 (It is used as defined in equation (I-ai-i)) This results in -R of formula (x-12''). Preferably, the -R of formula (x-12'') 04 It is -H.

[0108] In certain embodiments, n in formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is an integer such that the molecular weight of the PEG portion is in the range of 1 to 15 kDa. In certain embodiments, n in formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is an integer such that the molecular weight of the PEG portion is in the range of 1 to 10 kDa. In certain embodiments, n in formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is an integer such that the molecular weight of the PEG portion is approximately 1 kDa. In certain embodiments, n in formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is an integer such that the molecular weight of the PEG portion is approximately 2 kDa. In certain embodiments, n in formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is an integer such that the molecular weight of the PEG portion is approximately 2.5 kDa. In certain embodiments, n in formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is an integer such that the molecular weight of the PEG portion is approximately 3 kDa. In certain embodiments, n in formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is an integer such that the molecular weight of the PEG portion is approximately 4 kDa. In certain embodiments, n in formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is an integer such that the molecular weight of the PEG portion is approximately 5 kDa. In certain embodiments, n in formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is an integer such that the molecular weight of the PEG portion is approximately 7.5 kDa.In certain embodiments, n in formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is an integer such that the molecular weight of the PEG portion is approximately 10 kDa. In certain embodiments, n in formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is an integer such that the molecular weight of the PEG portion is approximately 15 kDa. In certain embodiments, n in formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is an integer such that the molecular weight of the PEG portion is approximately 20 kDa.

[0109] Generally, the molecular weight of the PEG portion is determined by the number of ethylene glycol units (for example, formula (I-ai), (I-ai-i), (I-aii), (I-aii'), (I-aii'-i), (I-aii'-ii), (I-aii'-iii), (I-aii'-iv), (I-aii'-v), (I-aii'-vi), (I-aii'-vii), (I-aii'-viii), (I-aii' The conversion to n) in (-ix), (I-aii'-x), (I-aii'-xi), (I-aii'-xii), (I-aii'-xiii), (I-aii'-xiv), (I-aii'-xv), and (I-aii'-xvi) can be easily performed by dividing the molecular weight of the PEG portion in kDa by 0.044 (molecular weight of one ethylene glycol unit: 44 Da).

[0110] In certain embodiments, n in the formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is an integer between approximately 22 and approximately 450. In certain embodiments, n in the formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is approximately 22. In certain embodiments, n in the formulas (I-ai), (I-ai-i), (I-aii), or (I-aii') is approximately 23. In certain embodiments, n in the formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is approximately 45. In certain embodiments, n in formula (I-ai) is about 57. In certain embodiments, n in formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is about 68. In certain embodiments, n in formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is about 90. In certain embodiments, n in formula (I-ai) is about 113. In certain embodiments, n in formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is about 170. In certain embodiments, n in the formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is about 230. In certain embodiments, n in the formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is about 340. In certain embodiments, n in the formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is about 450.

[0111] In certain embodiments, n in the formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is an integer between 2 and 21. In certain embodiments, n in the formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is 2. In certain embodiments, n in the formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is 2. In a particular embodiment, n in the formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is 3. In a particular embodiment, n in the formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is 4. In a particular embodiment, n in the formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is 5. In a particular embodiment, n in the formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is 6. In certain embodiments, n in the formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is 7. In certain embodiments, n in the formulas (I-ai), (I-ai-i), (I-aii), (I-aii'), or (I-aii'-i)~(I-aii'-xvi) is 2.

[0112] In certain embodiments, -P- in formula (Ia) or (I-a') is equivalent to formula (Pi) [ka] (In the formula, The dashed line is -L 2 - indicates binding to n is in the range of 50 to 200. It belongs to them.

[0113] In certain embodiments, -P- in formula (Ia) or (I-a') is equivalent to formula (P-ii) [ka] (In the formula, The dashed line is -L 2 - indicates binding to n is in the range of 50 to 200. It belongs to them.

[0114] In certain embodiments, n in formulas (Pi) and (P-ii) is in the range of 60-180, 70-160, 80-160, 90-140, 95-130, or 100-125. In certain embodiments, n in formulas (Pi) and (P-ii) is selected such that P has a molecular weight of approximately 5 kDa.

[0115] In certain embodiments, n in formula (Pi) or (P-ii) is in the range of 2 to 22, that is, n is 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, or 22 in certain embodiments.

[0116] In a particular embodiment, n in formula (Pi) or (P-ii) is in the range of 23 to 49, that is, in a particular embodiment, n is 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, or 49.

[0117] In certain embodiments, -P- in formula (Ia) or (I-a') is equivalent to formula (I-aiv) [ka] (In the formula, The dashed line indicates a connection to -BP-. Each-X A - is used independently, as defined in equation (I-ai-i), d, e, f, and g are integers independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10. Each m is an independent integer between 1 and 100. n is an integer such that the molecular weight of the PEG portion is in the range of approximately 1 to approximately 20 kDa. It belongs to them.

[0118] In a particular embodiment, d in formula (I-aiv) is an integer from 1 to 8. In a particular embodiment, d in formula (I-aiv) is an integer from 1 to 6. In a particular embodiment, d in formula (I-aiv) is 1. In a particular embodiment, d in formula (I-aiv) is 2. In a particular embodiment, d in formula (I-aiv) is 3. In a particular embodiment, d in formula (I-aiv) is 4. In a particular embodiment, d in formula (I-aiv) is 5. In a particular embodiment, d in formula (I-aiv) is 6.

[0119] In a particular embodiment, g in formula (I-aiv) is an integer from 1 to 8. In a particular embodiment, g in formula (I-aiv) is an integer from 1 to 6. In a particular embodiment, g in formula (I-aiv) is 1. In a particular embodiment, g in formula (I-aiv) is 2. In a particular embodiment, g in formula (I-aiv) is 3. In a particular embodiment, g in formula (I-aiv) is 4. In a particular embodiment, g in formula (I-aiv) is 5. In a particular embodiment, g in formula (I-aiv) is 6.

[0120] In certain embodiments, d and g in formula (I-aiv) are the same integer. In certain embodiments, both d and g in formula (I-aiv) are 1. In certain embodiments, both d and g in formula (I-aiv) are 2. In certain embodiments, both d and g in formula (I-aiv) are 3. In certain embodiments, both d and g in formula (I-aiv) are 4.

[0121] In a particular embodiment, e in formula (I-aiv) is an integer from 1 to 8. In a particular embodiment, e in formula (I-aiv) is an integer from 1 to 6. In a particular embodiment, e in formula (I-aiv) is 1. In a particular embodiment, e in formula (I-aiv) is 2. In a particular embodiment, e in formula (I-aiv) is 3. In a particular embodiment, e in formula (I-aiv) is 4. In a particular embodiment, e in formula (I-aiv) is 5. In a particular embodiment, e in formula (I-aiv) is 6.

[0122] In a particular embodiment, f in formula (I-aiv) is an integer from 1 to 8. In a particular embodiment, f in formula (I-aiv) is an integer from 1 to 6. In a particular embodiment, f in formula (I-aiv) is 1. In a particular embodiment, f in formula (I-aiv) is 2. In a particular embodiment, f in formula (I-aiv) is 3. In a particular embodiment, f in formula (I-aiv) is 4. In a particular embodiment, f in formula (I-aiv) is 5. In a particular embodiment, f in formula (I-aiv) is 6.

[0123] In certain embodiments, e and f in formula (I-aiv) are the same integer. In certain embodiments, both e and f in formula (I-aiv) are 1. In certain embodiments, both e and f in formula (I-aiv) are 2. In certain embodiments, both e and f in formula (I-aiv) are 3. In certain embodiments, both e and f in formula (I-aiv) are 4.

[0124] In certain embodiments, n in formula (I-aiv) is an integer such that the molecular weight of the PEG portion is in the range of 1 to 15 kDa. In certain embodiments, n in formula (I-aiv) is an integer such that the molecular weight of the PEG portion is in the range of 1 to 10 kDa. In certain embodiments, n in formula (I-aiv) is an integer such that the molecular weight of the PEG portion is approximately 1 kDa. In certain embodiments, n in formula (I-aiv) is an integer such that the molecular weight of the PEG portion is approximately 2 kDa. In certain embodiments, n in formula (I-aiv) is an integer such that the molecular weight of the PEG portion is approximately 2.5 kDa. In certain embodiments, n in formula (I-aiv) is an integer such that the molecular weight of the PEG portion is approximately 3 kDa. In certain embodiments, n in formula (I-aiv) is an integer such that the molecular weight of the PEG portion is approximately 4 kDa. In certain embodiments, n in formula (I-aiv) is an integer such that the molecular weight of the PEG portion is approximately 5 kDa. In certain embodiments, n in formula (I-aiv) is an integer such that the molecular weight of the PEG portion is approximately 7.5 kDa. In certain embodiments, n in formula (I-aiv) is an integer such that the molecular weight of the PEG portion is approximately 10 kDa. In certain embodiments, n in formula (I-aiv) is an integer such that the molecular weight of the PEG portion is approximately 15 kDa. In certain embodiments, n in formula (I-aiv) is an integer such that the molecular weight of the PEG portion is approximately 20 kDa.

[0125] In certain embodiments, n in formula (I-aiv) is an integer between approximately 22 and approximately 450. In certain embodiments, n in formula (I-aiv) is approximately 22. In certain embodiments, n in formula (I-aiv) is approximately 23. In certain embodiments, n in formula (I-aiv) is approximately 45. In certain embodiments, n in formula (I-ai) is approximately 57. In certain embodiments, n in formula (I-aiv) is approximately 68. In certain embodiments, n in formula (I-aiv) is approximately 90. In certain embodiments, n in formula (I-ai) is approximately 113. In certain embodiments, n in formula (I-aiv) is approximately 170. In certain embodiments, n in formula (I-aiv) is approximately 230. In certain embodiments, n in formula (I-aiv) is approximately 340. In certain embodiments, n in equation (I-aiv) is approximately 450.

[0126] In certain embodiments, at least one polymer portion is a linear polymer portion -P- including first and second ends, and at least two portions of formula (I) and / or at least one portion of formula (I') are conjugated to -P- at a portion selected from the group consisting of an internal portion, a first end, and a second end.

[0127] In certain embodiments, at least one polymer portion of the compound of the present invention is [ka] (In the formula, Unmarked dashed lines indicate bonding points to adjacent units or hydrogen atoms in the dashed lines marked with #. The dashed lines marked with a # indicate bonding points to adjacent units or hydroxyls in the unmarked dashed lines. The dashed line with an asterisk indicates -L 2 - indicates binding to -P- Unit Z 2 The total number is at least 2, Unit Z 1 and Z 2 The total number is at least 5, -Ra 1 and -Ra 2 These are, independently, hydrogen and C 1-4 Selected from the group consisting of alkyl, alkali metal ions, ammonium ions, alkaline earth metal ions, or other suitable counterions, -X 3 - stands for -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O)2N(R y1 )-,-S(O)N(R y1 )-, -S(O)2-, -S(O)-, -N(R y1 )S(O)2N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y3 )-,-S(O)2N(R y3 )-,-S(O)N(R y3 )-, -S(O)2-, -S(O)-, -N(R y3 )S(O)2N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3 )(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(R y3)- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a These are -H, -T, and C, which are independent of each other. 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynyls, where -T, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y4 )-,-S(O)2N(R y4 )-,-S(O)N(R y4 )-, -S(O)2-, -S(O)-, -N(R y4 )S(O)2N(R y4a )-, -S-, -N(R y4 )-, -OC(OR y4 )(R y4a )-,-N(R y4 )C(O)N(R y4a )-, and -OC(O)N(R y4 )- may intersect with one or more groups selected from the group consisting of, Each T independently consists of phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C. 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, where each T is independently one or more identical or different -R y2 It is sometimes replaced by, Each-R y2 These are, independently, halogen, -CN, oxo (=O), and -COOR. y5 , -OR y5 , -C(O)R y5 ,-C(O)N(R y5 R y5a), -S(O)2N(R y5 R y5a ), -S(O)N(R y5 R y5a ), -S(O)2R y5 ,-S(O)R y5 , -N(R y5 )S(O)2N(R y5a R y5b ), -SR y5 , -N(R y5 R y5a ), -NO2, -OC(O)R y5 , -N(R y5 )C(O)R y5a , -N(R y5 )S(O)2R y5a , -N(R y5 )S(O)R y5a , -N(R y5 )C(O)OR y5a , -N(R y5 )C(O)N(R y5a R y5b ), -OC(O)N(R y5 R y5a ), and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each-R y3 , -R y3a , -R y4 , -R y4a , -R y5 , -R y5a and -R y5b These are independently -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 (Alkyl is sometimes substituted with one or more halogens, either the same or different.) It contains multiple linearly linked units selected from the group consisting of the following.

[0128] In a particular embodiment, -X 3 - stands for -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O)2N(R y1 )-,-S(O)N(Ry1 )-, -S(O)2-, -S(O)-, -N(R y1 )S(O)2N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T-, C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y3 )-,-S(O)2N(R y3 )-,-S(O)N(R y3 )-, -S(O)2-, -S(O)-, -N(R y3 )S(O)2N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3 )(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(R y3 )- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a These are -H, -T, and C, which are independent of each other. 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Selected from the group consisting of alkynyls, where -T, C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Alkinyl has one or more -Rs, which may be the same or different. y2and is optionally substituted, C 1-10 alkyl, C 2-10 alkenyl, and C 2-10 alkynyl may optionally be interrupted by one or more groups selected from the group consisting of -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y4 ), -S(O)2N(R y4 ), -S(O)N(R y4 ), -S(O)2-, -S(O)-, -N(R y4 )S(O)2N(R y4a ), -S-, -N(R y4 ), -OC(OR y4 )(R y4a ), -N(R y4 )C(O)N(R y4a ), and -OC(O)N(R y4 ), each T is independently selected from the group consisting of phenyl, naphthyl, indenyl, indanyl, tetralinyl, C 3-10 cycloalkyl, 3- to 10-membered heterocyclyl, 8- to 11-membered heterobicyclic, 8- to 30-membered carbopolycyclic, and 8- to 30-membered heteropolycyclic, where each T is independently optionally substituted with one or more of the same or different -R y2 s, -R y2 is halogen, -CN, oxo(=O), -COOR y5 , -OR y5 , -C(O)R y5 , -C(O)N(R y5 R y5a ), -S(O)2N(R y5 R y5a ), -S(O)N(R y5 R y5a ), -S(O)2R y5 , -S(O)R y5 , -N(R y5 )S(O)2N(R y5a R y5b ), -SR y5 , -N(R y5 R y5a ), -NO2, -OC(O)R y5 , -N(R y5)C(O)R y5a , -N(R y5 )S(O)2R y5a , -N(R y5 )S(O)R y5a , -N(R y5 )C(O)OR y5a , -N(R y5 )C(O)N(R y5a R y5b ), -OC(O)N(R y5 R y5a ), and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each-R y3 , -R y3a , -R y4 , -R y4a , -R y5 , -R y5a and -R y5b These are, independently of each other, -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl atoms are sometimes substituted with one or more halogens, either the same or different.

[0129] In a particular embodiment, -X 3 - stands for -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O)2N(R y1 )-,-S(O)N(R y1 )-, -S(O)2-, -S(O)-, -N(R y1 )S(O)2N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T-, C 1-50 Alkyl, C 2-50Alkenyl, and C 2-50 Alkynyl is optionally substituted with one or more -R y2 wherein C 1-50 Alkyl, C 2-50 Alkenyl, and C 2-50 Alkynyl may optionally contain one or more groups selected from the group consisting of -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y3 )-, -S(O)2N(R y3 )-, -S(O)N(R y3 )-, -S(O)2-, -S(O)-, -N(R y3 )S(O)2N(R y3a [[ID=​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​Alkyl atoms are sometimes substituted with one or more halogens, either the same or different.

[0130] In a particular embodiment, the unit Z 1 and Z 2 The total number of such particles is such that -P- has a molecular weight of approximately 1 to approximately 20 kDa. In certain embodiments, the unit Z 1 and Z 2 The total number of such particles has a molecular weight of approximately 1 to 15 kDa. In certain embodiments, the unit Z 1 and Z 2 The total number of such that -P- has a molecular weight of approximately 1 kDa. In certain embodiments, the unit Z 1 and Z 2 The total number of such that -P- has a molecular weight of approximately 2 kDa. In certain embodiments, the unit Z 1 and Z 2 The total number of such that -P- has a molecular weight of approximately 3 kDa. In certain embodiments, the unit Z 1 and Z 2 The total number of such that -P- has a molecular weight of approximately 4 kDa. In a particular embodiment, the unit Z 1 and Z 2 The total number of such that -P- has a molecular weight of approximately 5 kDa. In certain embodiments, the unit Z 1 and Z 2 The total number of such particles is such that -P- has a molecular weight of approximately 7.5 kDa. In certain embodiments, the unit Z 1 and Z 2 The total number of such that -P- has a molecular weight of approximately 10 kDa. In certain embodiments, the unit Z 1 and Z 2 The total number of such that -P- has a molecular weight of approximately 15 kDa. In certain embodiments, the unit Z 1 and Z 2 The total number of such molecules is such that -P- has a molecular weight of approximately 20 kDa.

[0131] In a particular embodiment, -X 3 - is equation (Ib) [ka] (In the formula, Dashed lines without a mark are Z 2 It shows the bond to the carbonyl, The dashed line with an asterisk indicates -L 2 - indicates binding to d1 is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. d2 is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. It belongs to them.

[0132] In a particular embodiment, d1 in formula (Ib) is 1. In a particular embodiment, d1 in formula (Ib) is 2. In a particular embodiment, d1 in formula (Ib) is 3. In a particular embodiment, d1 in formula (Ib) is 4. In a particular embodiment, d1 in formula (Ib) is 5. In a particular embodiment, d1 in formula (Ib) is 6.

[0133] In a particular embodiment, d2 in formula (Ib) is 1. In a particular embodiment, d2 in formula (Ib) is 2. In a particular embodiment, d2 in formula (Ib) is 3. In a particular embodiment, d2 in formula (Ib) is 4. In a particular embodiment, d2 in formula (Ib) is 5. In a particular embodiment, d2 in formula (Ib) is 6.

[0134] In a particular embodiment, -X 3 - is the expression (I-b') [ka] (In the formula, Dashed lines without a mark are Z 2 It shows the bond to the carbonyl, The dashed line with an asterisk indicates -L 2(Indicates a connection to -) It belongs to them.

[0135] In certain embodiments, the compound is of formula (Ic) or (I-c') [ka] (In the formula, Each-L 2 - is either an independent spacer part or does not exist. Each-L 1 - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each-L 1' - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each -D- is an independent drug portion. Each -AB is an albumin-binding moiety independently. -P- is the polymer part, Each BP is an independent branching point. Each a is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. p and q are integers independently selected from the group consisting of 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. It belongs to them.

[0136] In certain embodiments, the compound is of formula (Ic). In certain embodiments, the compound is of formula (I-c').

[0137] Part-L 1' - is conjugated into two or more parts -D-, -L 1' It is understood that all bonds between - and part-D- are covalent and reversible.

[0138] In certain embodiments, both a in formula (I-c') are the same integer. In certain embodiments, both a in formula (I-c') are 2. In certain embodiments, both a in formula (I-c') are 3. In certain embodiments, both a in formula (I-c') are 4. In certain embodiments, both a in formula (I-c') are 5. In certain embodiments, both a in formula (I-c') are 6. In certain embodiments, both a in formula (I-c') are 7. In certain embodiments, both a in formula (I-c') are 8. In certain embodiments, both a in formula (I-c') are 9. In certain embodiments, both a in formula (I-c') are 10. In certain embodiments, both a in formula (I-c') are 11. In certain embodiments, both a in formula (I-c') are 12. In certain embodiments, both a in formula (I-c') are 13. In certain embodiments, both a in formula (I-c') is 14. In certain embodiments, both a in formula (I-c') is 15. In certain embodiments, both a in formula (I-c') is 16.

[0139] In certain embodiments, p and q in formula (Ic) or (I-c') are the same integer. In certain embodiments, p and q in formula (Ic) or (I-c') are different integers.

[0140] Embodiments relating to -P- are described elsewhere in this specification with respect to formulas (Ia) and (I-a').

[0141] Each BP in formulas (Ic) and (I-c') is an independent branching point. In certain embodiments, both BPs are identical. In certain embodiments, both BPs are different. The BP points may be single atoms, e.g., nitrogen or carbon, or groups of atoms, e.g., di-, tri-, or tetraamino acids. The diamino acids may be selected from the group consisting of lysine, ornithine, 2,3-diaminopropionic acid, and 2,4-diaminobutyric acid, each of which may have either an R or S configuration.

[0142] In certain embodiments, BP of formula (I-c') includes lysine, particularly s-configured lysine. In certain parts, both parts BP of formula (I-c') include lysine, particularly s-configured lysine.

[0143] In a particular embodiment, both parts BP have the structure of formula (Ici). [ka] (In the formula, Dashed lines without a mark are -L 2 - indicates binding to The dashed line with an asterisk indicates a connection to -P-. Each h is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10. Each i is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10. It holds.

[0144] In certain embodiments, both h in equation (Ici) are the same integer. In certain embodiments, both h in equation (Ici) are 2 and i in equation (Ici) is 4. In certain embodiments, both h in equation (Ici) are 3 and i in equation (Ici) is 4. In certain embodiments, both h in equation (Ici) are 4 and i in equation (Ici) is 4.

[0145] In certain embodiments, both parts BP have the structure of formula (Ic-i'). [ka] (In the formula, Dashed lines without a mark are -L 2 - indicates binding to (The dashed line with an asterisk indicates a connection to -P-) It holds.

[0146] In certain embodiments, one BP of formula (I-c') is lysine, in particular s-configured lysine. In certain embodiments, both partial BPs of formula (I-c') are lysine, in particular s-configured lysine.

[0147] In a particular embodiment, the partial BP-P-BP is given by formula (I-d') [ka] (In the formula, The dashed line is -L 2 - indicates binding to Each m is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, and 8. n is an integer between 2 and 200. Each o is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, and 8. Each p is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, and 8. It belongs to them.

[0148] In a particular embodiment, the partial BP-P-BP is formula (Id) [ka] (In the formula, The dashed line is -L 2 - indicates binding to Each m is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, and 8. Each p is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, and 8. n is an integer between 2 and 200. It belongs to them.

[0149] In certain embodiments, n in formulas (Id) and (I-d') is in the range of 60-180, 70-160, 80-160, 90-140, 95-130, or 100-125. In certain embodiments, n in formulas (Id) and (I-d') is selected such that P has a molecular weight of approximately 5 kDa.

[0150] In a particular embodiment, the partial BP-P-BP is given by formula (Ie) [ka] (In the formula, the dashed line represents -L) 2 - indicates binding to n is an integer between 2 and 200. It belongs to them.

[0151] In certain embodiments, n in formula (Ie) is in the range of 60-180, 70-160, 80-160, 90-140, 95-130, or 100-125. In certain embodiments, n in formula (Ie) is selected such that P has a molecular weight of approximately 5 kDa.

[0152] In certain embodiments, at least one polymer portion of the compound of the present invention is a multi-arm polymer portion. Such a multi-arm polymer portion includes at least one branch point. Thus, in certain embodiments, the compound includes at least one branch point B conjugated by at least two portions of formula (Ib) and / or at least one portion of formula (Ib'), where formulas (Ib) and (Ib') are [ka] (In the formula, The dashed line indicates the connection to branch point B. -A- is the polymer part, Each-L 2 - is either an independent spacer part or does not exist. Each-L 1 - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each-L 1' - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each -D- is an independent drug portion. Each -AB is an albumin-binding moiety independently. Each a is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. That is the case.

[0153] In a particular embodiment, the compound comprises at least one branch point B, where at least two parts of formula (Ib) are conjugated, [ka] (In the formula, The dashed line indicates the connection to branch point B. -A- is the polymer part, Each-L 2 - is either an independent spacer part or does not exist. Each-L 1 - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each -D- is an independent drug portion. Each -AB is an independently albumin-binding moiety. That is the case.

[0154] In a particular embodiment, the compound comprises at least one branch point B to which at least one portion of formula (Ib') is conjugated, and formula (Ib') is [ka] (In the formula, The dashed line indicates the connection to branch point B. -A- is the polymer part, Each-L 2 - is either an independent spacer part or does not exist. Each-L1' - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each -D- is an independent drug portion. Each -AB is an albumin-binding moiety independently. Each a is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. That is the case.

[0155] Part A of formula (Ib) or (Ib') is one or more polymers, e.g., 2-methacryloyloxyethyl phosphorylcholine, poly(acrylic acid), poly(acrylate), poly(acrylamide), poly(alkyloxy)polymer, poly(amide), poly(amideamine), poly(amino acid), poly(acid anhydride), poly(aspartamide), poly(butyric acid), poly(glycolic acid), polybutylene terephthalate, poly(caprolactone), poly(carbonate), poly(cyanoacrylate), poly(dimethylacrylamide), poly(ester), poly(ethylene), poly(ethylene glycol), poly(ethylene oxide), poly(ethyl phosphate), poly(ethyl oxazoline), poly(glycolic acid), poly(hydroxyethyl acrylate), poly(hydroxyethyl oxazoline), poly(hydroxymethacrylate), poly(hydroxypropyl methacrylamide), poly(hydroxypropyl methacrylamide) The polymers include polymers selected from the group consisting of poly(hydroxypropyl oxazoline), poly(iminocarbonate), poly(lactic acid), poly(lactic acid-co-glycolic acid), poly(methacrylamide), poly(methacrylate), poly(methyloxazoline), poly(organophosphazene), poly(orthoester), poly(oxazoline), poly(propylene glycol), poly(siloxane), poly(urethane), poly(vinyl alcohol), poly(vinylamine), poly(vinyl methyl ether), poly(vinylpyrrolidone), silicone, cellulose, carbomethylcellulose, hydroxypropylmethylcellulose, chitin, chitosan, dextran, dextrin, gelatin, hyaluronic acid and its derivatives, functionalized hyaluronic acid, mannan, pectin, rhamnogalacturonan, starch, hydroxyalkyl starch, hydroxyethyl starch and other carbohydrate polymers, xylan, and copolymers thereof.

[0156] In certain embodiments, -A- in formula (Ib) or (Ib') comprises a PEG-based polymer or a hyaluronic acid-based polymer. In certain embodiments, -A- in formula (Ib) or (Ib') comprises a PEG-based polymer. In certain embodiments, -A- in formula (Ib) or (Ib') comprises a hyaluronic acid-based polymer.

[0157] In certain embodiments, -A- in formula (Ib) or (Ib') is equivalent to formula (I-ba) [ka] (In the formula, The unmarked dashed lines indicate connections to branch point B. The dashed line with an asterisk indicates -L 2 - indicates binding to z is an integer selected such that the molecular weight of -A- is in the range of approximately 0.5 kDa to approximately 10 kDa. -X 8 - stands for -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O)2N(R y1 )-,-S(O)N(R y1 )-, -S(O)2-, -S(O)-, -N(R y1 )S(O)2N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y3 )-,-S(O)2N(R y3 )-,-S(O)N(R y3 )-, -S(O)2-, -S(O)-, -N(R y3 )S(O)2N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3 )(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(R y3 )- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a These are -H, -T, and C, which are independent of each other. 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynyls, where -T, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y4 )-,-S(O)2N(R y4 )-,-S(O)N(R y4 )-, -S(O)2-, -S(O)-, -N(R y4 )S(O)2N(R y4a )-, -S-, -N(R y4 )-, -OC(OR y4 )(R y4a )-,-N(R y4 )C(O)N(R y4a )-, and -OC(O)N(R y4 )- may intersect with one or more groups selected from the group consisting of, Each T independently consists of phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C.3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, where each T is independently one or more identical or different -R y2 It is sometimes replaced by, Each-R y2 These are, independently, halogen, -CN, oxo (=O), and -COOR. y5 , -OR y5 , -C(O)R y5 ,-C(O)N(R y5 R y5a ), -S(O)2N(R y5 R y5a ), -S(O)N(R y5 R y5a ), -S(O)2R y5 ,-S(O)R y5 , -N(R y5 )S(O)2N(R y5a R y5b ), -SR y5 , -N(R y5 R y5a ), -NO2, -OC(O)R y5 , -N(R y5 )C(O)R y5a , -N(R y5 )S(O)2R y5a , -N(R y5 )S(O)R y5a , -N(R y5 )C(O)OR y5a , -N(R y5 )C(O)N(R y5a R y5b ), -OC(O)N(R y5 R y5a ), and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each-R y3 , -R y3a , -R y4 , -R y4a , -R y5 , -R y5a and -R y5bThese are independently -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 (Alkyl is sometimes substituted with one or more halogens, either the same or different.) It belongs to them.

[0158] In a particular embodiment, -X 8 - stands for -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O)2N(R y1 )-,-S(O)N(R y1 )-, -S(O)2-, -S(O)-, -N(R y1 )S(O)2N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T-, C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y3 )-,-S(O)2N(R y3 )-,-S(O)N(R y3 )-, -S(O)2-, -S(O)-, -N(R y3 )S(O)2N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3 )(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(R y3)- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a These are -H, -T, and C, which are independent of each other. 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Selected from the group consisting of alkynyls, where -T, C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y4 )-,-S(O)2N(R y4 )-,-S(O)N(R y4 )-, -S(O)2-, -S(O)-, -N(R y4 )S(O)2N(R y4a )-, -S-, -N(R y4 )-, -OC(OR y4 )(R y4a )-,-N(R y4 )C(O)N(R y4a )-, and -OC(O)N(R y4 )- may intersect with one or more groups selected from the group consisting of, Each T independently consists of phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C. 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, where each T is independently one or more identical or different -R y2 It is sometimes replaced by, -R y2 These are halogen, -CN, oxo (=O), and -COOR. y5 , -OR y5 , -C(O)R y5 ,-C(O)N(R y5 R y5a), -S(O)2N(R y5 R y5a ), -S(O)N(R y5 R y5a ), -S(O)2R y5 ,-S(O)R y5 , -N(R y5 )S(O)2N(R y5a R y5b ), -SR y5 , -N(R y5 R y5a ), -NO2, -OC(O)R y5 , -N(R y5 )C(O)R y5a , -N(R y5 )S(O)2R y5a , -N(R y5 )S(O)R y5a , -N(R y5 )C(O)OR y5a , -N(R y5 )C(O)N(R y5a R y5b ), -OC(O)N(R y5 R y5a ), and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each-R y3 , -R y3a , -R y4 , -R y4a , -R y5 , -R y5a and -R y5b These are, independently of each other, -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl atoms are sometimes substituted with one or more halogens, either the same or different.

[0159] In a particular embodiment, -X 8 - stands for -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O)2N(R y1 )-,-S(O)N(R y1 )-, -S(O)2-, -S(O)-, -N(R y1)S(O)2N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y3 )-,-S(O)2N(R y3 )-,-S(O)N(R y3 )-, -S(O)2-, -S(O)-, -N(R y3 )S(O)2N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3 )(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(R y3 )- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a These are independently -H, -T, and C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Selected from the group consisting of alkynnyls, Each T independently consists of phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C. 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, Each-R y2 These are, independently, halogen and C 1-6 Selected from the group consisting of alkyl groups, Each-R y3 , -R y3a , -R y4 , -R y4a , -R y5 , -R y5a and -R y5b These are, independently of each other, -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl atoms are sometimes substituted with one or more halogens, either the same or different.

[0160] In certain embodiments, -A- in formula (Ib) or (Ib') is equivalent to formula (I-bb) or (I-bb') [ka] TIFF2026509252000051.tif24160 (in the formula, The unmarked dashed lines indicate connections to branch point B. The dashed line with an asterisk indicates -L 2 - indicates binding to z is an integer selected such that the molecular weight of -A- is in the range of approximately 0.5 kDa to approximately 10 kDa. z1 is selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 and 16. z2 is selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. It belongs to them.

[0161] In certain embodiments, -A- in formula (Ib) or (Ib') is the same as in formula (I-bb). In certain embodiments, -A- in formula (Ib) or (Ib') is the same as in formula (I-bb').

[0162] In certain embodiments, -A- in formula (Ib) or (Ib') is equivalent to formula (I-bc) or (I-bc') [ka] (In the formula, The unmarked dashed lines indicate connections to branch point B. The dashed line with an asterisk indicates -L 2 - indicates binding to z is an integer selected such that the molecular weight of -A- is in the range of approximately 0.5 kDa to approximately 10 kDa. z1 is selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 and 16. z2 is selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. It belongs to them.

[0163] In certain embodiments, -A- in formula (Ib) or (Ib') is the same as in formula (I-bc'). In certain embodiments, -A- in formula (Ib) or (Ib') is the same as in formula (I-bc').

[0164] In a particular embodiment, z1 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 1. In a particular embodiment, z1 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 2. In a particular embodiment, z1 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 3. In a particular embodiment, z1 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 4. In a particular embodiment, z1 of formula (I-bb), (I-bb'), (I-bc), or (I-bc) is 5. In a particular embodiment, z1 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 6. In a particular embodiment, z1 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 7. In a particular embodiment, z1 of formula (I-bb), (I-bb'), (I-bc), or (I-bc) is 8. In a particular embodiment, z1 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 9. In a particular embodiment, z1 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 10. In a particular embodiment, z1 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 11. In a particular embodiment, z1 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 12. In a particular embodiment, z1 in formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 13. In a particular embodiment, z1 in formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 14. In a particular embodiment, z1 in formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 15. In a particular embodiment, z1 in formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 16.

[0165] In a particular embodiment, z2 in formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 1. In a particular embodiment, z2 in formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 2. In a particular embodiment, z2 in formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 3. In a particular embodiment, z2 in formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 4. In a particular embodiment, z2 in formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 5. In a particular embodiment, z2 in formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 6. In a particular embodiment, z2 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 7. In a particular embodiment, z2 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 8. In a particular embodiment, z2 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 9. In a particular embodiment, z2 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 10. In a particular embodiment, z2 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 11. In a particular embodiment, z2 of formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 12. In certain embodiments, z2 in formulas (I-bb), (I-bb'), (I-bc), or (I-bc') is 13. In certain embodiments, z2 in formulas (I-bb), (I-bb'), (I-bc), or (I-bc') is 14. In certain embodiments, z2 in formulas (I-bb), (I-bb'), (I-bc), or (I-bc') is 15. In certain embodiments, z2 in formulas (I-bb), (I-bb'), (I-bc), or (I-bc') is 16.

[0166] In a particular embodiment, z1 in formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 3, and z2 in formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 2. In a particular embodiment, z1 in formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 2, and z2 in formula (I-bb), (I-bb'), (I-bc), or (I-bc') is 2.

[0167] In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer such that the molecular weight of -A- is approximately 0.5 kDa to approximately 10 kDa. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer such that the molecular weight of -A- is approximately 0.5 kDa. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer such that the molecular weight of -A- is approximately 1 kDa. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer such that the molecular weight of -A- is approximately 1.5 kDa. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer such that the molecular weight of -A- is approximately 2 kDa. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer such that the molecular weight of -A- is approximately 2.5 kDa. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer such that the molecular weight of -A- is approximately 3 kDa. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer such that the molecular weight of -A- is approximately 3.5 kDa. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer such that the molecular weight of -A- is approximately 4 kDa. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer such that the molecular weight of -A- is approximately 5 kDa. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer such that the molecular weight of -A- is approximately 6 kDa. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer such that the molecular weight of -A- is approximately 7 kDa.In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer such that the molecular weight of -A- is approximately 8 kDa. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer such that the molecular weight of -A- is approximately 9 kDa. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer such that the molecular weight of -A- is approximately 10 kDa.

[0168] In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer between about 11 and about 230. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is an integer between about 11 and about 225. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is about 11. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is about 12. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is about 22. In certain embodiments, z for formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is about 23. In certain embodiments, z for formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is about 34. In certain embodiments, z for formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is about 45. In certain embodiments, z for formulas (I-ba), (I-bb), or (-I-bc) is about 57. In certain embodiments, z for formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is about 68. In certain embodiments, z for formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is about 79. In certain embodiments, z for formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is about 90. In certain embodiments, z for formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is about 102. In certain embodiments, z for formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is about 113. In certain embodiments, z for formulas (I-bb) or (I-bc) is about 135. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is about 160. In certain embodiments, z in formulas (I-bb) or (I-bc) is about 180.In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is about 205. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is about 225. In certain embodiments, z in formulas (I-ba), (I-bb), (I-bb'), (I-bc), or (I-bc') is about 230.

[0169] In a particular embodiment, the compound has one branch point B, for example, [ka] (In the formula, The dashed line indicates the connection of equation (Ib) to -A-, -R 1 It is used as defined with respect to the term "substituent". -X 4 -, -X 5 -, -X 6 - and -X 7 - is independent of -X in equation (I-ai). 1 - and -X 2 (Used as defined in relation to -) Includes a branching point selected from the group consisting of

[0170] In certain embodiments, -X in formulas (I-b1) and (I-b2) 4 -, -X 5 - and -X 6 - is identical. In certain embodiments, -X in formulas (I-b1) and (I-b2) 4 -, -X 5 - and -X 6 - represents the same entity and is selected from the group consisting of -CH2-, -CH2CH2-, and -CH2CH2CH2-.

[0171] In certain embodiments, the compound includes one branch point of formula (I-b1). In certain embodiments, the compound includes one branch point of formula (I-b2). In certain embodiments, the compound includes one branch point of formula (I-b3). In certain embodiments, the compound includes one branch point of formula (I-b3) and -X 4 -, -X 5 -, -X 6 - and -X 7 - is identical. In a particular embodiment, the compound includes one branch point of formula (I-b3) and -X 4 -, -X 5 -, -X 6 - and -X 7 - is selected from the group consisting of -CH2-, -CH2CH2- and -CH2CH2CH2-. In certain embodiments, the compound includes one branch point of formula (I-b3) and -X 4 -, -X 5 -, -X 6 - and -X 7 - is -CH2-.

[0172] In a particular embodiment, the compound is of formula (I-b4) [ka] (In the formula, Each -A- is a polymer portion, Each-L 2 - is either an independent spacer part or does not exist. Each-L 1 - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each -D- is an independent drug portion. Each -AB is an albumin-binding moiety independently. -X 4 -, -X 5 -, -X 6 - and -X 7 - are independent of each other: -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O)2N(R y1)-,-S(O)N(R y1 )-, -S(O)2-, -S(O)-, -N(R y1 )S(O)2N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y3 )-,-S(O)2N(R y3 )-,-S(O)N(R y3 )-, -S(O)2-, -S(O)-, -N(R y3 )S(O)2N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3 )(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(R y3 )- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a These are -H, -T, and C, which are independent of each other. 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynyls, where -T, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y4 )-,-S(O)2N(R y4 )-,-S(O)N(R y4 )-, -S(O)2-, -S(O)-, -N(R y4 )S(O)2N(R y4a )-, -S-, -N(R y4 )-, -OC(OR y4 )(R y4a )-,-N(R y4 )C(O)N(R y4a )-, and -OC(O)N(R y4 )- may intersect with one or more groups selected from the group consisting of, Each T independently consists of phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C. 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, where each T is independently one or more identical or different -R y2 It is sometimes replaced by, Each-R y2 These are, independently, halogen, -CN, oxo (=O), and -COOR. y5 , -OR y5 , -C(O)R y5 ,-C(O)N(R y5 R y5a ), -S(O)2N(R y5 R y5a ), -S(O)N(R y5 R y5a ), -S(O)2R y5 ,-S(O)R y5 , -N(R y5 )S(O)2N(R y5a R y5b ), -SR y5 , -N(R y5 R y5a ), -NO2, -OC(O)R y5 , -N(R y5)C(O)R y5a , -N(R y5 )S(O)2R y5a , -N(R y5 )S(O)R y5a , -N(R y5 )C(O)OR y5a , -N(R y5 )C(O)N(R y5a R y5b ), -OC(O)N(R y5 R y5a ), and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each-R y3 , -R y3a , -R y4 , -R y4a , -R y5 , -R y5a and -R y5b These are independently -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 (Alkyl is sometimes substituted with one or more halogens, either the same or different.) It belongs to them.

[0173] In a particular embodiment, -X of formula (I-b4) 4 -, -X 5 -, -X 6 - and -X 7 - are independent of each other: -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O)2N(R y1 )-,-S(O)N(R y1 )-, -S(O)2-, -S(O)-, -N(R y1 )S(O)2N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T-, C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y3 )-,-S(O)2N(R y3 )-,-S(O)N(R y3 )-, -S(O)2-, -S(O)-, -N(R y3 )S(O)2N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3 )(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(R y3 )- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a These are -H, -T, and C, which are independent of each other. 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Selected from the group consisting of alkynyls, where -T, C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y4 )-,-S(O)2N(R y4 )-,-S(O)N(R y4 )-, -S(O)2-, -S(O)-, -N(R y4 )S(O)2N(R y4a)-, -S-, -N(R y4 )-, -OC(OR y4 )(R y4a )-,-N(R y4 )C(O)N(R y4a )-, and -OC(O)N(R y4 )- may intersect with one or more groups selected from the group consisting of, Each T independently consists of phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C. 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, where each T is independently one or more identical or different -R y2 It is sometimes replaced by, -R y2 These are halogen, -CN, oxo (=O), and -COOR. y5 , -OR y5 , -C(O)R y5 ,-C(O)N(R y5 R y5a ), -S(O)2N(R y5 R y5a ), -S(O)N(R y5 R y5a ), -S(O)2R y5 ,-S(O)R y5 , -N(R y5 )S(O)2N(R y5a R y5b ), -SR y5 , -N(R y5 R y5a ), -NO2, -OC(O)R y5 , -N(R y5 )C(O)R y5a , -N(R y5 )S(O)2R y5a , -N(R y5 )S(O)R y5a , -N(R y5 )C(O)OR y5a , -N(R y5 )C(O)N(R y5a R y5b ), -OC(O)N(R y5 R y5a ), and C1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each-R y3 , -R y3a , -R y4 , -R y4a , -R y5 , -R y5a and -R y5b These are, independently of each other, -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl atoms are sometimes substituted with one or more halogens, either the same or different.

[0174] In a particular embodiment, -X of formula (I-b4) 4 -, -X 5 -, -X 6 - and -X 7 - are independent of each other: -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O)2N(R y1 )-,-S(O)N(R y1 )-, -S(O)2-, -S(O)-, -N(R y1 )S(O)2N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y3 )-,-S(O)2N(R y3 )-,-S(O)N(R y3 )-, -S(O)2-, -S(O)-, -N(R y3 )S(O)2N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3 )(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(R y3 )- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a These are independently -H, -T, and C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Selected from the group consisting of alkynnyls, Each T independently consists of phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C. 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, Each-R y2 These are, independently, halogen and C 1-6 Selected from the group consisting of alkyl groups, Each-R y3 , -R y3a , -R y4 , -R y4a , -R y5 , -R y5a and -R y5b These are, independently of each other, -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl atoms are sometimes substituted with one or more halogens, either the same or different.

[0175] In certain embodiments, -X in formulas (I-b3) and (I-b4) 4 -, -X 5 -, -X6 - and -X 7 - is identical. In certain embodiments, -X in formulas (I-b3) and (I-b4) 4 -, -X 5 -, -X 6 - and -X 7 - represents the same entity and is selected from the group consisting of -CH2-, -CH2CH2-, and -CH2CH2CH2-.

[0176] In certain embodiments, partial [ka] is equation (I-b5) [ka] (In the formula, The dashed line is -L 2 - indicates binding to n1, n2, n3, and n4 are integers independently ranging from about 10 to about 300, and in certain embodiments, from about 10 to about 230. It belongs to them.

[0177] In certain embodiments, partial [ka] is equation (I-b6) [ka] (In the formula, The dashed line is -L 2 - indicates binding to n1, n2, n3, and n4 are independent integers between approximately 10 and approximately 230. It belongs to them.

[0178] In certain embodiments, n1, n2, n3, and n4 in formula (I-b5) or (I-b6) are the same integer. In certain embodiments, n1, n2, n3, and n4 in formula (I-b5) or (I-b6) are about 11. In certain embodiments, n1, n2, n3, and n4 in formula (I-b5) or (I-b6) are about 12. In certain embodiments, n1, n2, n3, and n4 in formula (I-b5) or (I-b6) are about 22. In certain embodiments, n1, n2, n3, and n4 in formula (I-b5) or (I-b6) are about 23. In certain embodiments, n1, n2, n3, and n4 in formula (I-b5) or (I-b6) are about 28. In certain embodiments, n1, n2, n3, and n4 of formula (I-b5) or (I-b6) are about 29. In certain embodiments, n1, n2, n3, and n4 of formula (I-b5) or (I-b6) are about 34. In certain embodiments, n1, n2, n3, and n4 of formula (I-b5) or (I-b6) are about 45. In certain embodiments, n1, n2, n3, and n4 of formula (I-b5) or (I-b6) are about 56. In certain embodiments, n1, n2, n3, and n4 of formula (I-b5) or (I-b6) are about 68. In certain embodiments, n1, n2, n3, and n4 of formula (I-b5) or (I-b6) are about 80. In certain embodiments, n1, n2, n3, and n4 of formula (I-b5) or (I-b6) are about 90. In certain embodiments, n1, n2, n3, and n4 of formula (I-b5) or (I-b6) are about 100. In certain embodiments, n1, n2, n3, and n4 of formula (I-b5) or (I-b6) are about 115. In certain embodiments, n1, n2, n3, and n4 of formula (I-b5) or (I-b6) are about 135. In certain embodiments, n1, n2, n3, and n4 of formula (I-b5) or (I-b6) are about 160. In certain embodiments, n1, n2, n3, and n4 of formula (I-b5) or (I-b6) are about 180. In certain embodiments, n1, n2, n3, and n4 in formula (I-b5) or (I-b6) are about 200. In certain embodiments, n1, n2, n3, and n4 in formula (I-b5) or (I-b6) are about 225.In certain embodiments, n1, n2, n3, and n4 in formula (I-b5) or (I-b6) are approximately 230.

[0179] In certain embodiments, the compound includes two or more branch points B, for example, two or more branch points selected from the group consisting of (I-b1), (I-b2), and (I-b3).

[0180] In a particular embodiment, -D- is a drug moiety selected from the group consisting of a small molecule drug moiety, a medium-sized molecule drug moiety, an oligonucleotide drug moiety, a peptide nucleic acid drug moiety, a peptide drug moiety, and a protein drug moiety.

[0181] In certain embodiments, -D- is a peptide drug moiety. In certain embodiments, -D- is a small molecule drug moiety. In certain embodiments, -D- is a medium-sized drug moiety. In certain embodiments, -D- is an oligonucleotide drug moiety. In certain embodiments, -D- is a peptide nucleic acid drug moiety. In certain embodiments, -D- is a protein drug moiety.

[0182] In certain embodiments, -D- or -D-AB is a GLP-1 receptor agonist moiety. Therefore, the compounds of the present invention may be GLP-1 receptor agonist compounds.

[0183] In certain embodiments, -D- or -D-AB is a mono agonist of the GLP-1 receptor, i.e., it activates only the GLP-1 receptor.

[0184] In certain embodiments, -D- or -D-AB is an agonist of the GLP-1 receptor and an agonist of a further receptor, i.e., -D- or -D-AB is a dual GLP-1 receptor agonist. Such further receptors can be selected from the group consisting of GIP receptor, GCG receptor, amyrin receptor, PYY receptor and GLP-2 receptor.

[0185] In certain embodiments, -D- or -D-AB is an agonist of the GLP-1 receptor and the GIP receptor. In certain embodiments, -D- or -D-AB is an agonist of the GLP-1 receptor and the GCG receptor. In certain embodiments, -D- or -D-AB is an agonist of the GLP-1 receptor and the amyrin receptor. In certain embodiments, -D- or -D-AB is an agonist of the GLP-1 receptor and the PYY receptor. In certain embodiments, -D- or -D-AB is an agonist of the GLP-1 receptor and the GLP-2 receptor.

[0186] In certain embodiments, -D- or -D-AB is a GLP-1 receptor agonist and growth / differentiation factor 15 (GDF15). In certain embodiments, -D- or -D-AB is a GLP-1 receptor agonist and fibroblast growth factor 21 (FGF21).

[0187] In certain embodiments, -D- or -D-AB is an agonist of the GLP-1 receptor and an agonist of two further receptors, i.e., -D- or -D-AB is a triple GLP-1 receptor agonist. These further receptors are selected in certain embodiments from the group consisting of the GIP receptor (GIPR), GCG receptor (GCGR), amyrin receptor, PYY receptor (PYYR), and GLP-2 receptor (GLP2R).

[0188] In certain embodiments, -D- or -D-AB is a triple GLP-1 receptor agonist that activates the GLP-1 receptor, GIP receptor, and GCG receptor. In certain embodiments, -D- or -D-AB is a triple GLP-1 receptor agonist that activates the GLP-1 receptor, GIP receptor, and amyrin receptor. In certain embodiments, -D- or -D-AB is a triple GLP-1 receptor agonist that activates the GLP-1 receptor, GIP receptor, and PYY receptor. In certain embodiments, -D- or -D-AB is a triple GLP-1 receptor agonist that activates the GLP-1 receptor, GIP receptor, and GLP-2 receptor. In certain embodiments, -D- or -D-AB is a triple GLP-1 receptor agonist that activates the GLP-1 receptor, GCG receptor, and amyrin receptor. In certain embodiments, -D- or -D-AB is a triple GLP-1 receptor agonist that activates the GLP-1 receptor, GCG receptor, and PYY receptor. In certain embodiments, -D- or -D-AB is a triple GLP-1 receptor agonist that activates the GLP-1 receptor, GCG receptor, and GLP-2 receptor. In certain embodiments, -D- or -D-AB is a triple GLP-1 receptor agonist that activates the GLP-1 receptor, amyrin receptor, and PYY receptor. In certain embodiments, -D- or -D-AB is a triple GLP-1 receptor agonist that activates the GLP-1 receptor, amyrin receptor, and GLP-2 receptor. In certain embodiments, -D- or -D-AB is a triple GLP-1 receptor agonist that activates the GLP-1 receptor, PYY receptor, and GLP-2 receptor.

[0189] In a particular embodiment, -D- is human GLP-1 of Sequence ID No. 1: HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG

[0190] In certain embodiments, -D- is a human GLP-1 analog of SEQ ID NO: 1, wherein the peptide sequence may contain one or more amino acid changes compared to SEQ ID NO: 1. Such amino acid changes may be the addition of one or more amino acid residues, the deletion of one or more amino acid residues, the substitution of one or more amino acid residues, or a combination thereof. Such amino acid changes may be at the N-terminus, C-terminus, and / or internal sites of GLP-1 of SEQ ID NO: 1. In certain embodiments, such a human GLP-1 analog may have up to three amino acid changes compared to SEQ ID NO: 1, i.e., up to three amino acids are added, deleted, or substituted compared to the sequence of SEQ ID NO: 1.

[0191] In a particular embodiment, -D- is an array HX1EGTFTSDVSSYLEGQAAKEFIAWLVRGRG(Sequence ID 2) (In the formula, X1 is 2-aminoisobutyric acid (Aib)) It holds.

[0192] In a particular embodiment, -D- is an array HX1EGTFTSDVSSYLEGQAAKEFIAWLVRGRG(Sequence ID 3) (In the formula, X1 is Aib, and the C-terminal glycine, i.e., the glycine at position 31, is amidated as a C-terminal primary amide.) It holds.

[0193] In certain embodiments, -D- is exenatide. Exenatide is sequence HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS(Sequence No. 4) It holds.

[0194] In a particular embodiment, -D- is an array HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS(Sequence No. 5) (In the formula, the C-terminal serine, i.e., the serine at position 39, is amidated as a C-terminal primary amide.) It holds.

[0195] In certain embodiments, -D- is lixisenatide. Lixisenatide is sequence HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK(Sequence No. 6) (In the formula, the C-terminal lysine, i.e., the lysine at position 44, is amidated as a C-terminal primary amide.) It holds.

[0196] In a particular embodiment, -D- is an array HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK(Sequence ID 7) It holds.

[0197] In a particular embodiment, -D- is an array HX1EGTFTSDLSKQX2EEEAVRLFIEWLKQGGPSSGAPPPC (Sequence ID 8) (In the formula, X1 is D-alanine and X2 is norleucine (Nle)) It holds.

[0198] In a particular embodiment, -D- is an array HX1EGTFTSDLSKQX2EEEAVRLFIEWLKQGGPSSGAPPPC (Sequence ID 9) (In the formula, X1 is D-alanine, X2 is Nle, and the C-terminal cysteine, i.e., the cysteine ​​at position 39, is amidated as a C-terminal primary amide.) It holds.

[0199] In certain embodiments, -D- is PEG-loxenatide. PEG-loxenatide is sequence HX1EGTFTSDLSKQX2EEEAVRLFIEWLKQGGPSSGAPPPC (Sequence ID 10) [In the formula, X1 is D-alanine, X2 is Nle, and the cysteine ​​at position 39 is, [ka] (In the formula, the dashed line indicates the bond of the cysteine ​​side chain of the cysteine ​​at position 39 to the thiol group, and each mPEG is methoxypoly(ethylene glycol) with a molecular weight of approximately 20 kDa.) [It is chemically modified through the conjugation of the cysteine ​​side chain to the thiol group.] It holds.

[0200] In a particular embodiment, -D- is an array HX1EGTFTSDLSKQX2EEEAVRLFIEWLKQGGPSSGAPPPC (Sequence ID 11) [In the formula, X1 is D-alanine, X2 is Nle, and the cysteine ​​at position 39 is, [ka] (In the formula, the dashed line indicates the bond of the cysteine ​​side chain of the cysteine ​​at position 39 to the thiol group, each mPEG is a methoxypoly(ethylene glycol) with a molecular weight of approximately 20 kDa, and the C-terminal cysteine, i.e., the cysteine ​​at position 39, is amidated as a C-terminal primary amide.) [It is chemically modified through the conjugation of the cysteine ​​side chain to the thiol group.] It holds.

[0201] In a particular embodiment, -D- is an array HAEGTFTSDVSSYLEGQAAKEFIAWLVRGRG(Sequence ID 12) It holds.

[0202] In a particular embodiment, -D- is an array HAEGTFTSDVSSYLEGQAAKEFIAWLVRGRG(Sequence ID 13) It has a C-terminal glycine, i.e., the glycine at position 31, which is amidated as a C-terminal primary amide.

[0203] In a particular embodiment, -D- is an array HVEGTFTSDVSSYLEEQAAREFIKWLVRGRG (Sequence ID 14) It holds.

[0204] In a particular embodiment, -D- is an array HVEGTFTSDVSSYLEEQAAREFIKWLVRGRG (Sequence ID 15) (In the formula, the C-terminal glycine, i.e., the glycine at position 31, is amidated as a C-terminal primary amide.) It holds.

[0205] In a particular embodiment, -D- is an array HGEGTFTSDVSSYLEGQAAKEFIAWLVRGRG(Sequence ID 16) It holds.

[0206] In a particular embodiment, -D- is an array HGEGTFTSDVSSYLEGQAAKEFIAWLVRGRG(Sequence ID 17) It has a C-terminal glycine, i.e., the glycine at position 31, which is amidated as a C-terminal primary amide.

[0207] In a particular embodiment, -D- is an array HX1EGTFTSDVSSYLEGQAAKEFIAWLVRGRGL (Sequence ID 18) (In the equation, X1 is Aib) It holds.

[0208] In a particular embodiment, -D- is an array HX1EGTFTSDVSSYLEGQAAKEFIAWLVRGRGL (Sequence ID 19) (In the formula, X1 is Aib, and the C-terminal leucine, i.e., the leucine at position 32, is amidated as a C-terminal primary amide.) It holds.

[0209] In a particular embodiment, -D- is an array YX1EGTFTSDYSIX2LDKIAQKAFVQWLIAGGPSSGAPPPS(Sequence ID 20) (In the formula, X1 is Aib, X2 is Aib, and the C-terminal serine, i.e., the serine at position 39, is amidated as a C-terminal primary amide.) It holds.

[0210] In a particular embodiment, -D- is an array YX1EGTFTSDYSIX2LDKIAQKAFVQWLIAGGPSSGAPPPS(Sequence ID 21) (In the equation, X1 is Aib and X2 is Aib.) It holds.

[0211] In a particular embodiment, -D- is an array HSQGTFTSDKSEYLDSERARDFVAWLEAGG (Sequence ID 22) It holds.

[0212] In a particular embodiment, -D- is an array HSQGTFTSDKSEYLDSERARDFVAWLEAGG (Sequence ID 23) (In the formula, the C-terminal glycine, i.e., the glycine at position 30, is amidated as a C-terminal primary amide.) It holds.

[0213] In a particular embodiment, -D- is an array HX1QGTFTSDYSKYLDERAAKDFIKWLESA (Sequence ID 24) (In the formula, X1 is 1-amino-cyclobutanecarboxylic acid (Ac4c), and the C-terminal alanine, i.e., the alanine at position 29, is amidated as a C-terminal primary amide.) It holds.

[0214] In a particular embodiment, -D- is an array HX1QGTFTSDYSKYLDERAAKDFIKWLESA (Sequence ID 25) (In the formula, X1 is 1-amino-cyclobutanecarboxylic acid (Ac4c)) It holds.

[0215] In a particular embodiment, -D- is an array HX1QGTFTSDYSKYLDEKAAKEFIQWLLQT (Sequence ID 26) (In the formula, X1 is Aib, and the glutamic acid at position 16 and the lysine at position 20 are linked via a lactam crosslink.) It holds.

[0216] In a particular embodiment, -D- is an array HX1QGTFTSDYSKYLDEKAAKEFIQWLLQT (Sequence ID 27) (In the formula, X1 is Aib, and the glutamic acid at position 16 and the lysine at position 20 are linked via a lactam crosslink, and the C-terminal threonine, i.e., the threonine at position 29, is amidated as a C-terminal primary amide.) It holds.

[0217] In a particular embodiment, -D- is an array HX1QGTFTSDYSKYLDEKKAKEFVEWLLEGGPSSG (Sequence ID 28) (In the formula, X1 is Aib, and the C-terminal glycine, i.e., the glycine at position 34, is amidated as a C-terminal primary amide.) It holds.

[0218] In a particular embodiment, -D- is an array HX1QGTFTSDYSKYLDEKKAKEFVEWLLEGGPSSG (Sequence ID 29) (In the equation, X1 is Aib) It holds.

[0219] In a particular embodiment, -D- is an array HX1EGSFTSELATILDKQAARDFIAWLIQHKITD (Sequence ID 30) (In the equation, X1 is Aib) It holds.

[0220] In a particular embodiment, -D- is an array HX1EGSFTSELATILDKQAARDFIAWLIQHKITD (Sequence ID 31) (In the formula, X1 is Aib, and the C-terminal aspartic acid, i.e., the aspartic acid at position 33, is amidated as a C-terminal primary amide.) It holds.

[0221] In a particular embodiment, -D- is an array YX1QGTFTSDYSIX2LDKKAQX3AFIEYLLEGGPSSGAPPPS (Sequence ID 32) (In the formula, X1 is Aib, X2 is α-methylleucine (αMeL), X3 is Aib, and the C-terminal serine, i.e., the serine at position 39, is amidated as a C-terminal primary amide.) It holds.

[0222] In a particular embodiment, -D- is an array YX1QGTFTSDYSIX2LDKKAQX3AFIEYLLEGGPSSGAPPPS (Sequence ID 33) (In the formula, X1 is Aib, X2 is α-methylleucine (αMeL), and X3 is Aib.) It holds.

[0223] In a particular embodiment, -D- is an array HX1EGTFTSDVSSYLEEEAAKEFIAWLVRGGPSSGAPPPSK (Sequence ID 54) (In the equation, X1 is Aib) It holds.

[0224] In a particular embodiment, -D- is an array HX1EGTFTSDVSSYLEEQAAKEFIAWLVRGGG (Sequence ID 55) (In the equation, X1 is Aib) It holds.

[0225] In a particular embodiment, -D- is an array HX1EGTFTSDVSSYLEEQAAKEFIAWLVRGGGGAQPGAQPGAQPGAQPGAQPGAQPGAQPGAQPGAQPGQKP(Sequence ID 56) (In the equation, X1 is Aib) It holds.

[0226] In a particular embodiment, -D- is an array HX1EGTFTSDVSSYLEEQAAKEFIAWLVRGGGGAQPGAQPGAQPGAQPGAQPGAQPGAQPGAQPGAQPGQKP(Sequence ID 56) (In the equation, X1 is Aib) It holds.

[0227] In certain embodiments, -D- is a drug selected from the group consisting of insulin, amylin and amylin / calcitonin, PYY, GIP, MSH, C5a binders, GDF15, PCSK9 I, immunostimulants, urocortin 2, MIC-1, IL-1R antagonists, leptin, gastrin, glucagon, exendin-4, GLP-1, GLP-2, and GIP.

[0228] In certain embodiments, -D- is a drug portion selected from the group consisting of insulin, insulin analogs, amylin, biamylin / calcitonin agonists, PYY, GIP, MSH, C5 inhibitors or modifiers, GDF15, PCSK9 inhibitors (inhibitors), immunostimulants, urocortin II, MIC-1, IL-1R antagonists, leptin, gastrin, glucagon, oxytomodulin, neurokinin A, tachykinin / neurokinin receptor 2 (NK2R) agonists, neurokinin receptor (NKR) agonists, and GLP-2.

[0229] In certain embodiments, -D- is insulin, e.g., insulin detemir, insulin degludec, and insulin. In certain embodiments, -D- is amylin and amylin / calcitonin, e.g., caglilintide. In certain embodiments, -D- is PYY, e.g., NNC0165-1875. In certain embodiments, -D- is GIP. In certain embodiments, -D- is MSH. In certain embodiments, -D- is a C5a binder, e.g., zircoplan. In certain embodiments, -D- is GDF15, e.g., NN LA-GDF15. In certain embodiments, -D- is PCSK9 i. In certain embodiments, -D- is an immunostimulant, e.g., romultide or mifamultide. In certain embodiments, -D- is muramil dipeptide. In certain embodiments, -D- is urocortin 2. In certain embodiments, -D- is MIC-1. In certain embodiments, -D- is an IL-1R antagonist. In certain embodiments, -D- is leptin. In certain embodiments, -D- is gastrin.

[0230] In certain embodiments, -D- is selected from a list consisting of growth hormones, such as human growth hormone, FGF21, EGF(a), and coagulation factors.

[0231] In certain embodiments, -D- is a growth hormone, e.g., human growth hormone, e.g., somapsitan. In certain embodiments, -D- is FGF21, e.g., NNC0194 0499. In certain embodiments, -D- is EGF(a). In certain embodiments, -D- is a coagulation factor.

[0232] In certain embodiments, -D- is selected from cytotoxic small molecule drugs, chemotherapeutic small molecule drugs, and immunoactivating small molecule drugs.

[0233] In certain embodiments, -D- is a cytotoxic small molecule drug. In certain embodiments, -D- is a chemotherapeutic small molecule drug. In certain embodiments, -D- is an immunoactivating small molecule drug, such as tellatrimod.

[0234] In certain embodiments, -D- is paclitaxel. In certain embodiments, -D- is doxorubicin. In certain embodiments, -D- is 5-FU.

[0235] In certain embodiments, -D- is the PTH portion.

[0236] In certain embodiments, -AB is an albumin-binding moiety based on a fatty acid.

[0237] Part-AB binds to albumin, such as human albumin, under physiological conditions (aqueous buffer, pH 7.4, 37°C).

[0238] Part D may be conjugated to one part AB. Part D may be conjugated to two or more parts AB. In certain embodiments, the bond between D and part AB is a stable bond. If D contains two parts AB, the bond between D and the first part AB may be reversible, and the bond between D and the second part AB may be stable. Alternatively, if D contains two parts AB, the bond between D and both parts AB may be stable.

[0239] In a particular embodiment, -AB is formula (A): [ka] [In the formula, The dashed line indicates a connection to -D-. -F 0 is equation (a-1) [ka] (In the formula, The dashed line is -L A - indicates binding to -R 0 -CR 1 R 1a R 1b ,-COOR 1 , [ka] Selected from the group consisting of, -R 1 , -R 1a and -R 1b It is selected from the group consisting of -H, methyl, ethyl, propyl and isopropyl, n is an integer between 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, and 22. It is, -L A - is either nonexistent or expression (a-2) [ka] (In the formula, Dashed lines without a mark are -L B - indicates binding to The dashed line with an asterisk indicates -F 0 This shows a connection to, -R a -teeth, [ka] (In the formula, The dashed line with an asterisk indicates -F 0 This shows a connection to, Dashed lines without a mark are -L A (Indicates connection to the remainder) Selected from the group consisting of, -R b -teeth, [ka] And, m is an integer selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10. p is an integer selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10. It is, -L B - is either nonexistent or expression (a-3) [ka] (In the formula, Unmarked dashed lines indicate connections to -D-. The dashed line with an asterisk indicates -L A This shows a connection to, -R c -teeth, [ka] And, -R d - is C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl can have one or more -Rs, which may be the same or different. 1 It can be replaced with C 1-50 Alkyl, C 2-50 Alkenyl or C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) 2 )-,-S(O)2N(R 2 )-,-S(O)N(R 2 )-, -S(O)2-, -S(O)-, -N(R 2 )S(O)2N(R 2a )-, -S-, -N(R 2 )-, -OC(OR 2 )(R 2a )-,-N(R 2 )C(O)N(R 2a )-, and -OC(O)N(R 2)- may have one or more groups selected from the group consisting of these groups, Each -T- is independently phenyl, naphthyl, indenyl, indanyl, tetralinyl, C 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, where each -T- is independently one or more -R which may be the same or different. 1 It can be replaced with Each-R 1 These are, independently, halogen, -CN, oxo (=O), and -COOR. 3 , -OR 3 , -C(O)R 3 ,-C(O)N(R 3 R 3a ), -S(O)2N(R 3 R 3a ), -S(O)N(R 3 R 3a ), -S(O)2R 3 ,-S(O)R 3 , -N(R 3 )S(O)2N(R 3a R 3b ), -SR 3 , -N(R 3 R 3a ), -NO2, -OC(O)R 3 , -N(R 3 )C(O)R 3a , -N(R 3 )S(O)2R 3a , -N(R 3 )S(O)R 3a , -N(R 3 )C(O)OR 3a , -N(R 3 )C(O)N(R 3a R 3b ), -OC(O)N(R 3 R 3a ), and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each-R 2 , -R2a , -R 3 , -R 3a and -R 3b These are independently -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl can be substituted with one or more halogens, which may be the same or different. -R e - is -CH2-, [ka] (Selected from the group consisting of) [It belongs to] It belongs to them.

[0240] -R b -but [ka] and -L B -If not absent, -R c -teeth [ka] And, -R b -but [ka] and -L B -If not absent, -R c -teeth [ka] That is the case.

[0241] In certain embodiments, -L A - is of formula (a-2), i.e., not absent. In certain embodiments, -L A - does not exist.

[0242] In certain embodiments, -R a -teeth, [ka] (In the formula, the dashed line with an asterisk indicates -F) 0 The dashed line without a mark indicates a connection to -L. A (Indicates connection to the remainder) That is the case.

[0243] In certain embodiments, -R a -teeth, [ka] (In the formula, the dashed line with an asterisk indicates -F) 0 The dashed line without a mark indicates a connection to -L. A (Indicates connection to the remainder) That is the case.

[0244] In certain embodiments, -R b -teeth, [ka] In certain embodiments, -R b -teeth, [ka] That is the case.

[0245] In a particular embodiment, m in formula (a-2) is 1. In a particular embodiment, m in formula (a-2) is 2. In a particular embodiment, m in formula (a-2) is 3. In a particular embodiment, m in formula (a-2) is 4. In a particular embodiment, m in formula (a-2) is 5. In a particular embodiment, m in formula (a-2) is 6. In a particular embodiment, m in formula (a-2) is 7. In a particular embodiment, m in formula (a-2) is 8. In a particular embodiment, m in formula (a-2) is 9. In a particular embodiment, m in formula (a-2) is 10.

[0246] In a particular embodiment, p in formula (a-2) is 1. In a particular embodiment, p in formula (a-2) is 2. In a particular embodiment, p in formula (a-2) is 3. In a particular embodiment, p in formula (a-2) is 4. In a particular embodiment, p in formula (a-2) is 5. In a particular embodiment, p in formula (a-2) is 6. In a particular embodiment, p in formula (a-2) is 7. In a particular embodiment, p in formula (a-2) is 8. In a particular embodiment, p in formula (a-2) is 9. In a particular embodiment, p in formula (a-2) is 10.

[0247] In certain embodiments, -L B - is from formula (a-3). In a particular embodiment, -L B - does not exist. -L B If the - does not exist, the unmarked dashed line in equation (a-2) indicates a connection to -D-.

[0248] In certain embodiments, -R c -teeth, [ka] In certain embodiments, -R c -teeth, [ka] That is the case.

[0249] In certain embodiments, -R e - is -CH2-. In certain embodiments, -R e -teeth, [ka] In certain embodiments, -R e -teeth, [ka] That is the case.

[0250] In certain embodiments, -L A - and -L B -Neither exists. -L A - and -L B If neither of the above exists, the dashed line in equation (a-1) indicates a connection to -D-.

[0251] In a particular embodiment, -F 0 teeth, [ka] TIFF2026509252000083.tif237161TIFF2026509252000084.tif195161(In the formula, the dashed line is -L) A (Indicates a connection to -) It is selected from the group consisting of the following.

[0252] -L A If - does not exist, the dashed line in equations (a-4) to (a-39) represents -L B - Indicates a binding to -L A - and -L B If neither of the above exists, the dashed lines in equations (a-4) to (a-39) indicate a connection to -D-.

[0253] In a particular embodiment, -F 0 This is the formula (a-4). In a particular embodiment, -F 0 This is the one in formula (a-5). In a particular embodiment, -F 0 This is the one in formula (a-6). In a particular embodiment, -F 0 This is the formula (a-7). In a particular embodiment, -F 0 This is the formula (a-8). In a particular embodiment, -F 0 This is the formula (a-9). In a particular embodiment, -F 0 This is the formula (a-10). In a particular embodiment, -F 0 This is the formula (a-11). In a particular embodiment, -F 0This is the formula (a-12). In a particular embodiment, -F 0 This is the formula (a-13). In a particular embodiment, -F 0 This is the formula (a-14). In a particular embodiment, -F 0 This is the formula (a-15). In a particular embodiment, -F 0 This is the formula (a-16). In a particular embodiment, -F 0 This is the formula (a-17). In a particular embodiment, -F 0 This is the formula (a-18). In a particular embodiment, -F 0 This is the formula (a-19). In a particular embodiment, -F 0 This is the formula (a-20). In a particular embodiment, -F 0 This is the formula (a-21). In a particular embodiment, -F 0 This is the formula (a-22). In certain embodiments, -F 0 This is the formula (a-23). ​​In a particular embodiment, -F 0 This is the formula (a-24). In a particular embodiment, -F 0 This is the formula (a-25). In certain embodiments, -F 0 This is the formula (a-26). In certain embodiments, -F 0 This is the formula (a-27). In a particular embodiment, -F 0 This is the formula (a-28). In a particular embodiment, -F 0 This is the formula (a-29). In a particular embodiment, -F 0 This is the formula (a-30). In a particular embodiment, -F 0 This is the formula (a-31). In a particular embodiment, -F 0 This is the formula (a-32). In a particular embodiment, -F 0 This is the formula (a-33). In a particular embodiment, -F 0 This is the formula (a-34). In a particular embodiment, -F 0This is the formula (a-35). In a particular embodiment, -F 0 This is the formula (a-36). In a particular embodiment, -F 0 This is the formula (a-37). In a particular embodiment, -F 0 This is the formula (a-38). In a particular embodiment, -F 0 This is the result of equation (a-39).

[0254] In a particular embodiment, -F 0 This is from equation (a-4), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-5), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-6), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-7), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-8), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-9), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-10), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-11), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-12), and -L A - and -L B-Neither of these exists. In certain embodiments, -F 0 This is from equation (a-13), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-14), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-15), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-16), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-17), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-18), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-19), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-20), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-21), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-22), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-23), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-24), and -LA - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-25), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-26), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-27), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-28), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-29), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-30), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-31), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-32), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-33), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-34), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-35), and -L A - and -L B -Neither of these exists. In certain embodiments, -F0 This is from equation (a-36), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-37), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-38), and -L A - and -L B -Neither of these exists. In certain embodiments, -F 0 This is from equation (a-39), and -L A - and -L B -Neither exists.

[0255] In certain embodiments, -L A -teeth, [ka] TIFF2026509252000086.tif230168TIFF2026509252000087.tif114168(In the formula, the dashed line with an asterisk is -F) 0 The dashed line without a mark indicates a connection to -L. B - Indicates bonding to the remainder. -L B (If no dash is present, an unmarked dashed line indicates a connection to -D-) It is selected from the group consisting of the following.

[0256] In certain embodiments, -L A - is from formula (a-40). In a particular embodiment, -L A - is from formula (a-41). In a particular embodiment, -L A - is from formula (a-42). In a particular embodiment, -L A - is from formula (a-43). In a particular embodiment, -L A - is from formula (a-44). In a particular embodiment, -L A - is from formula (a-45). In a particular embodiment, -LA - is from formula (a-46). In a particular embodiment, -L A - is from formula (a-47). In a particular embodiment, -L A - is from formula (a-48). In a particular embodiment, -L A - is from formula (a-49). In a particular embodiment, -L A - is from formula (a-50). In a particular embodiment, -L A - is from formula (a-51). In a particular embodiment, -L A - is from formula (a-52). In a particular embodiment, -L A - is from formula (a-53). In a particular embodiment, -L A - is from formula (a-54). In a particular embodiment, -L A - is from formula (a-55). In a particular embodiment, -L A - is from formula (a-56). In certain embodiments, -L A - is from formula (a-57). In a particular embodiment, -L A - is from formula (a-58). In certain embodiments, -L A - is from formula (a-59). In a particular embodiment, -L A - is from formula (a-60). In certain embodiments, -L A - is from formula (a-61). In certain embodiments, -L A - is from formula (a-62). In certain embodiments, -L A - is from formula (a-63). In certain embodiments, -L A - is from formula (a-64). In a particular embodiment, -L A - is from formula (a-65). In certain embodiments, -L A - is from formula (a-66). In certain embodiments, -L A - is from formula (a-67). In a particular embodiment, -L A- is from formula (a-68). In a particular embodiment, -L A - is from formula (a-69). In certain embodiments, -L A - is from formula (a-70). In a particular embodiment, -L A - is from formula (a-71). In a particular embodiment, -L A - is from formula (a-72). In a particular embodiment, -L A - is from formula (a-73). In a particular embodiment, -L A - is from formula (a-74). In a particular embodiment, -L A - is from formula (a-75). In a particular embodiment, -L A - is from formula (a-76). In certain embodiments, -L A - is from formula (a-77). In a particular embodiment, -L A - is of formula (a-78). In a particular embodiment, -L A - is from formula (a-79). In a particular embodiment, -L A - is from formula (a-80). In a particular embodiment, -L A - is of formula (a-81). In a particular embodiment, -L A - is from equation (a-82).

[0257] In certain embodiments, -L B -teeth, [ka] TIFF2026509252000089.tif122168 (in the formula, The dashed line with an asterisk indicates -L A - indicates binding to Unmarked dashed lines indicate connections to -D-. (q is an integer between 2 and 50) It is selected from the group consisting of the following.

[0258] -L AIf - does not exist, the dashed lines with asterisks in equations (a-83) to (a-94) represent -F 0 This indicates a connection to [the specified location].

[0259] In a particular embodiment, q in formula (a-84) is an integer between 3 and 45. In a particular embodiment, q in formula (a-84) is an integer between 4 and 40. In a particular embodiment, q in formula (a-84) is an integer between 5 and 35. In a particular embodiment, q in formula (a-84) is an integer between 6 and 30. In a particular embodiment, q in formula (a-84) is an integer between 7 and 25. In a particular embodiment, q in formula (a-84) is an integer between 10 and 20. In a particular embodiment, q in formula (a-84) is 23.

[0260] In certain embodiments, -L B - is from formula (a-83). In a particular embodiment, -L B - is from formula (a-84). In a particular embodiment, -L B - is from equation (a-84) where q=23. In certain embodiments, -L B - is from formula (a-85). In a particular embodiment, -L B - is from formula (a-86). In certain embodiments, -L B - is from formula (a-87). In a particular embodiment, -L B - is from formula (a-88). In a particular embodiment, -L B - is from formula (a-89). In a particular embodiment, -L B - is from formula (a-90). In certain embodiments, -L B - is of formula (a-91). In a particular embodiment, -L B - is from formula (a-92). In certain embodiments, -L B - is from formula (a-93). In certain embodiments, -L B - is from equation (a-94).

[0261] In a particular embodiment, -AB is given by formula (i) [ka] (In the formula, the dashed line indicates a connection to -D-, n is an integer between 14 and 22. (A stereocenter marked with an asterisk is either in S or R configuration.) It belongs to them.

[0262] In a particular embodiment, -AB is of formula (i) and n is 14. In a particular embodiment, -AB is of formula (i) and n is 15. In a particular embodiment, -AB is of formula (i) and n is 16. In a particular embodiment, -AB is of formula (i) and n is 17. In a particular embodiment, -AB is of formula (i) and n is 18. In a particular embodiment, -AB is of formula (i) and n is 19. In a particular embodiment, -AB is of formula (i) and n is 20. In a particular embodiment, -AB is of formula (i) and n is 21. In a particular embodiment, -AB is of formula (i) and n is 22.

[0263] In a particular embodiment, -AB is from formula (i), n is 14, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from formula (i), n is 15, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from formula (i), n is 16, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from formula (i), n is 17, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from formula (i), n is 18, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from formula (i), n is 19, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from formula (i), n is 20, and the stereocenter with an asterisk is in the R configuration. In certain embodiments, -AB is from formula (i), n is 21, and the stereocenters marked with an asterisk are in the R configuration. In certain embodiments, -AB is from formula (i), n is 22, and the stereocenters marked with an asterisk are in the R configuration.

[0264] In a particular embodiment, -AB is from formula (i), n is 14, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is from formula (i), n is 15, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is from formula (i), n is 16, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is from formula (i), n is 17, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is from formula (i), n is 18, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is from formula (i), n is 19, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is from formula (i), n is 20, and the stereocenter with an asterisk is in the S configuration. In certain embodiments, -AB is from equation (i), n is 21, and the stereocenters marked with an asterisk are in an S configuration. In certain embodiments, -AB is from equation (i), n is 22, and the stereocenters marked with an asterisk are in an S configuration.

[0265] In a particular embodiment, -AB is given by formula (ia): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0266] In a particular embodiment, -AB is given by formula (ib): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0267] In a particular embodiment, -AB is formula (ic): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0268] In a particular embodiment, -AB is formula (id): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0269] In a particular embodiment, -AB is given by formula (ie): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0270] In a particular embodiment, -AB is given by formula (if): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0271] In a particular embodiment, -AB is formula (ii) [ka] (In the formula, The dashed line indicates a connection to -D-. n is an integer between 14 and 22. (A stereocenter marked with an asterisk is either in S or R configuration.) It belongs to them.

[0272] In a particular embodiment, -AB is of formula (ii) and n is 14. In a particular embodiment, -AB is of formula (ii) and n is 15. In a particular embodiment, -AB is of formula (ii) and n is 16. In a particular embodiment, -AB is of formula (ii) and n is 17. In a particular embodiment, -AB is of formula (ii) and n is 18. In a particular embodiment, -AB is of formula (ii) and n is 19. In a particular embodiment, -AB is of formula (ii) and n is 20. In a particular embodiment, -AB is of formula (ii) and n is 21. In a particular embodiment, -AB is of formula (ii) and n is 22.

[0273] In a particular embodiment, -AB is of formula (ii), n is 14, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (ii), n is 15, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (ii), n is 16, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (ii), n is 17, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (ii), n is 18, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (ii), n is 19, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (ii), n is 20, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from formula (ii), n is 21, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from formula (ii), n is 22, and the stereocenter with an asterisk is in the R configuration.

[0274] In a particular embodiment, -AB is of formula (ii), n is 14, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (ii), n is 15, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (ii), n is 16, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (ii), n is 17, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (ii), n is 18, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (ii), n is 19, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (ii), n is 20, and the stereocenter with an asterisk is in the S configuration. In certain embodiments, -AB is from equation (ii), n is 21, and the stereocenters marked with an asterisk are in an S configuration. In certain embodiments, -AB is from equation (ii), n is 22, and the stereocenters marked with an asterisk are in an S configuration.

[0275] In a particular embodiment, -AB is formula (ii-a): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0276] In a particular embodiment, -AB is formula (ii-b): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0277] In a particular embodiment, -AB is formula (ii-c): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0278] In a particular embodiment, -AB is formula (ii-d): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0279] In a particular embodiment, -AB is formula (ii-e): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0280] In a particular embodiment, -AB is formula (ii-f): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0281] In a particular embodiment, -AB is formula (iii) [ka] (In the formula, The dashed line indicates a connection to -D-. t is an integer between 14 and 22. (A stereocenter marked with an asterisk is either in S or R configuration.) It belongs to them.

[0282] In a particular embodiment, -AB is of formula (iii) and t is 14. In a particular embodiment, -AB is of formula (iii) and t is 15. In a particular embodiment, -AB is of formula (iii) and t is 16. In a particular embodiment, -AB is of formula (iii) and t is 17. In a particular embodiment, -AB is of formula (iii) and t is 18. In a particular embodiment, -AB is of formula (iii) and t is 19. In a particular embodiment, -AB is of formula (iii) and t is 20. In a particular embodiment, -AB is of formula (iii) and t is 21. In a particular embodiment, -AB is of formula (iii) and t is 22.

[0283] In a particular embodiment, -AB is of formula (iii), t is 14, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (iii), t is 15, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (iii), t is 16, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (iii), t is 17, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (iii), t is 18, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (iii), t is 19, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (iii), t is 20, and the stereocenter with an asterisk is in the R configuration. In certain embodiments, -AB is of formula (iii), t is 21, and the stereocenter with an asterisk is in the R configuration. In certain embodiments, -AB is of formula (iii), t is 22, and the stereocenter with an asterisk is in the R configuration.

[0284] In a particular embodiment, -AB is of formula (iii), t is 14, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (iii), t is 15, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (iii), t is 16, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (iii), t is 17, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (iii), t is 18, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (iii), t is 19, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (iii), t is 20, and the stereocenter with an asterisk is in the S configuration. In certain embodiments, -AB is of formula (iii), t is 21, and the stereocenter with an asterisk is in the S configuration. In certain embodiments, -AB is of formula (iii), t is 22, and the stereocenter with an asterisk is in the S configuration.

[0285] In a particular embodiment, -AB is formula (iii-a) [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0286] In a particular embodiment, -AB is formula (iii-b) [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0287] In a particular embodiment, -AB is formula (iii-c) [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0288] In a particular embodiment, -AB is given by formula (iii-d) [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0289] In a particular embodiment, -AB is formula (iii-e) [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0290] In a particular embodiment, -AB is given by formula (iii-f) [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0291] In a particular embodiment, -AB is formula (iv) [ka] (In the formula, The dashed line indicates a connection to -D-. (u is an integer between 14 and 22) It belongs to them.

[0292] In a particular embodiment, -AB is of formula (iv) and u is 14. In a particular embodiment, -AB is of formula (iv) and u is 15. In a particular embodiment, -AB is of formula (iv) and u is 16. In a particular embodiment, -AB is of formula (iv) and u is 17. In a particular embodiment, -AB is of formula (iv) and u is 18. In a particular embodiment, -AB is of formula (iv) and u is 19. In a particular embodiment, -AB is of formula (iv) and u is 20. In a particular embodiment, -AB is of formula (iv) and u is 21. In a particular embodiment, -AB is of formula (iv) and u is 22.

[0293] In a particular embodiment, -AB is given by formula (v) [ka] (In the formula, The dashed line indicates a connection to -D-. v is an integer between 14 and 22. (A stereocenter marked with an asterisk is either in S or R configuration.) It belongs to them.

[0294] In a particular embodiment, -AB is of formula (v), where v is 14. In a particular embodiment, -AB is of formula (v), where v is 15. In a particular embodiment, -AB is of formula (v), where v is 16. In a particular embodiment, -AB is of formula (v), where v is 17. In a particular embodiment, -AB is of formula (v), where v is 18. In a particular embodiment, -AB is of formula (v), where v is 19. In a particular embodiment, -AB is of formula (v), where v is 20. In a particular embodiment, -AB is of formula (v), where v is 21. In a particular embodiment, -AB is of formula (v), where v is 22.

[0295] In a particular embodiment, -AB is of formula (v), v is 14, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (v), v is 15, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (v), v is 16, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (v), v is 17, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (v), v is 18, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (v), v is 19, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (v), v is 20, and the stereocenter with an asterisk is in the R configuration. In certain embodiments, -AB is of equation (v), where v is 21, and the stereocenter with an asterisk is in the R configuration. In certain embodiments, -AB is of equation (v), where v is 22, and the stereocenter with an asterisk is in the R configuration.

[0296] In a particular embodiment, -AB is of formula (v), v is 14, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (v), v is 15, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (v), v is 16, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (v), v is 17, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (v), v is 18, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (v), v is 19, and the stereocenter with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (v), v is 20, and the stereocenter with an asterisk is in the S configuration. In certain embodiments, -AB is of equation (v), where v is 21, and the stereocenters marked with an asterisk are in the S configuration. In certain embodiments, -AB is of equation (v), where v is 22, and the stereocenters marked with an asterisk are in the S configuration.

[0297] In a particular embodiment, -AB is given by formula (va) [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0298] In a particular embodiment, -AB is formula (vb) [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0299] In a particular embodiment, -AB is of formula (vc) [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0300] In a particular embodiment, -AB is formula (vd) [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0301] In a particular embodiment, -AB is given by formula (vi-e) [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0302] In a particular embodiment, -AB is given by formula (vi-f) [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0303] In a particular embodiment, -AB is given by formula (vii) [ka] (In the formula, The dashed line indicates a connection to -D-. w is an integer between 14 and 22. (A stereocenter marked with an asterisk is either in S or R configuration.) It belongs to them.

[0304] In a particular embodiment, -AB is of formula (vii) and w is 14. In a particular embodiment, -AB is of formula (vii) and w is 15. In a particular embodiment, -AB is of formula (vii) and w is 16. In a particular embodiment, -AB is of formula (vii) and w is 17. In a particular embodiment, -AB is of formula (vii) and w is 18. In a particular embodiment, -AB is of formula (vii) and w is 19. In a particular embodiment, -AB is of formula (vii) and w is 20. In a particular embodiment, -AB is of formula (vii) and w is 21. In a particular embodiment, -AB is of formula (vii) and w is 22.

[0305] In a particular embodiment, -AB is from formula (vii), w is 14, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from formula (vii), w is 15, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from formula (vii), w is 16, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from formula (vii), w is 17, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from formula (vii), w is 18, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from formula (vii), w is 19, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from formula (vii), w is 20, and the stereocenter with an asterisk is in the R configuration. In certain embodiments, -AB is from equation (vii), w is 21, and the stereocenters marked with an asterisk are in the R configuration. In certain embodiments, -AB is from equation (vii), w is 22, and the stereocenters marked with an asterisk are in the R configuration.

[0306] In a particular embodiment, -AB is from equation (vii), w is 14, and the solid center with an asterisk is in the S configuration. In a particular embodiment, -AB is from equation (vii), w is 15, and the solid center with an asterisk is in the S configuration. In a particular embodiment, -AB is from equation (vii), w is 16, and the solid center with an asterisk is in the S configuration. In a particular embodiment, -AB is from equation (vii), w is 17, and the solid center with an asterisk is in the S configuration. In a particular embodiment, -AB is from equation (vii), w is 18, and the solid center with an asterisk is in the S configuration. In a particular embodiment, -AB is from equation (vii), w is 19, and the solid center with an asterisk is in the S configuration. In a particular embodiment, -AB is from equation (vii), w is 20, and the solid center with an asterisk is in the S configuration. In certain embodiments, -AB is from equation (vii), w is 21, and the stereocenters marked with an asterisk are in an S configuration. In certain embodiments, -AB is from equation (vii), w is 22, and the stereocenters marked with an asterisk are in an S configuration.

[0307] In a particular embodiment, -AB is given by formula (vii-a): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0308] In a particular embodiment, -AB is given by formula (vii-b): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0309] In a particular embodiment, -AB is given by formula (vii-c): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0310] In a particular embodiment, -AB is given by formula (vii-d): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0311] In a particular embodiment, -AB is given by formula (vii-e): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0312] In a particular embodiment, -AB is given by formula (vii-f): [ka] (In the formula, (The dashed line indicates a connection to -D-) It belongs to them.

[0313] In a particular embodiment, -AB is formula (viii) [ka] (In the formula, the dashed line indicates a connection to -D-, w is an integer between 14 and 22. (A stereocenter marked with an asterisk is either in S or R configuration.) It belongs to them.

[0314] In a particular embodiment, -AB is of formula (viii) and x is 14. In a particular embodiment, -AB is of formula (viii) and x is 15. In a particular embodiment, -AB is of formula (viii) and x is 16. In a particular embodiment, -AB is of formula (viii) and x is 17. In a particular embodiment, -AB is of formula (viii) and x is 18. In a particular embodiment, -AB is of formula (viii) and x is 19. In a particular embodiment, -AB is of formula (viii) and x is 20. In a particular embodiment, -AB is of formula (viii) and x is 21. In a particular embodiment, -AB is of formula (viii) and x is 22.

[0315] In a particular embodiment, -AB is of formula (viii), x is 14, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (viii), x is 15, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (viii), x is 16, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (viii), x is 17, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (viii), x is 18, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (viii), x is 19, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is of formula (viii), x is 20, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from equation (viii), x is 21, and the stereocenter with an asterisk is in the R configuration. In a particular embodiment, -AB is from equation (viii), x is 22, and the stereocenter with an asterisk is in the R configuration.

[0316] In a particular embodiment, -AB is of formula (viii), x is 14, and the solid center with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (viii), x is 15, and the solid center with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (viii), x is 16, and the solid center with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (viii), x is 17, and the solid center with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (viii), x is 18, and the solid center with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (viii), x is 19, and the solid center with an asterisk is in the S configuration. In a particular embodiment, -AB is of formula (viii), x is 20, and the solid center with an asterisk is in the S configuration. In a particular embodiment, -AB is from equation (viii), x is 21, and the stereocenter with an asterisk is in an S configuration. In a particular embodiment, -AB is from equation (viii), x is 22, and the stereocenter with an asterisk is in an S configuration.

[0317] In a particular embodiment, -AB is given by formula (viii-a) [ka] (In the formula, the dashed line indicates a connection to -D-) It belongs to them.

[0318] In a particular embodiment, -AB is formula (viii-b) [ka] (In the formula, the dashed line indicates a connection to -D-) It belongs to them.

[0319] In a particular embodiment, -AB is given by formula (viii-c) [ka] (In the formula, the dashed line indicates a connection to -D-) It belongs to them.

[0320] In a particular embodiment, -AB is given by formula (viii-d) [ka] (In the formula, the dashed line indicates a connection to -D-) It belongs to them.

[0321] In a particular embodiment, -AB is given by formula (viii-e) [ka] (In the formula, the dashed line indicates a connection to -D-) It belongs to them.

[0322] In a particular embodiment, -AB is given by formula (viii-f) [ka] (In the formula, the dashed line indicates a connection to -D-) It belongs to them.

[0323] In certain embodiments, -AB is formula (ix-i) [ka] (In the formula, X 1 -teeth, [ka] And, -X 2 teeth, [ka] And, Ph stands for phenyl, a is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10. b is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10. c is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10. d is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10. m is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10. n is 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, or 24. p is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10. It belongs to them.

[0324] In a particular embodiment, -AB is of formula (ix-i), where a is 1, b is 1, c is 1, d is 1, m is 1, n is 18, and m is 1.

[0325] In certain embodiments, -AB is of formula (ix-i), and X 1 -teeth, [ka] And -X 2 teeth, [ka] In certain embodiments, -AB is of formula (ix-i), and X 1 -teeth, [ka] And -X 2 teeth, [ka] In certain embodiments, -AB is of formula (ix-i), and X 1 -teeth, [ka] And -X 2 teeth, [ka] In certain embodiments, -AB is of formula (ix-i), and X 1 -teeth, [ka] And -X 2 teeth, [ka] In certain embodiments, -AB is of formula (ix-i), and X 1 -teeth, [ka] And -X 2 teeth, [ka] In certain embodiments, -AB is of formula (ix-i), and X 1 -teeth, [ka] And -X 2 teeth, [ka] In certain embodiments, -AB is of formula (ix-i), and X 1 -teeth, [ka] And -X 2 teeth, [ka] In certain embodiments, -AB is of formula (ix-i), and X 1 -teeth, [ka] And -X 2 teeth, [ka] In certain embodiments, -AB is of formula (ix-i), and X 1 -teeth, [ka] And -X 2 teeth, [ka] In certain embodiments, -AB is of formula (ix-i), and X 1 -teeth, [ka] And -X 2 teeth, [ka] In certain embodiments, -AB is of formula (ix-i), and X 1 -teeth, [ka] And -X 2 teeth, [ka] In certain embodiments, -AB is of formula (ix-i), and X 1 -teeth, [ka] And -X 2 teeth, [ka] That is the case.

[0326] In certain embodiments, -AB is a peptidoalbumin-binding moiety.

[0327] If -D- is a peptide or protein drug moiety, such a peptidic moiety -AB may be fused to the N or C terminus of -D-, either directly or with a peptidic spacer between -D- and -AB.

[0328] In a particular embodiment, -AB is WWEQDRDWDFDVFGGGTP (Sequence ID 34), DICLPRWGCLW (Sequence ID 35) (In the formula, the cysteine ​​at positions 3 and 9 are linked via disulfide bridges.) RLIEDICLPRWGCLWEDD (Sequence ID 36) (In the formula, the cysteine ​​at positions 7 and 13 are linked via disulfide bridges.) LAEAKVLANRELDKYGVSDFYKRLINKAKTVEGVEALKLHILAALP (Sequence ID 37), IAEAKEAANAELDSYGVSDFYKRLIDKAKTVEGVEALKDAILAALP (Sequence ID 38), and X1EYEX2EYE (Sequence ID 39) (In the formula, X1 is fluorescein-(AEEA), X2 is K(palmitate), and AEEA is 2-(2-(2-aminoethoxy)acetyl) It is selected from the group consisting of the following.

[0329] In certain embodiments, -AB is the same as sequence number 34. In certain embodiments, -AB is the same as sequence number 35. In certain embodiments, -AB is the same as sequence number 36. In certain embodiments, -AB is the same as sequence number 37. In certain embodiments, -AB is the same as sequence number 38. In certain embodiments, -AB is the same as sequence number 39.

[0330] In a particular embodiment, -AB is formula (Aa): [ka] (In the formula, The dashed line indicates a connection to -D-. -F 0 and -L A - is used as defined in equation (A), -L B' - is the polymer part.) It belongs to them.

[0331] Part-L B'- indicates a polymer portion, which means that it contains at least one polymer portion. In a particular embodiment, one or more polymer portions have a molecular weight of at least 450 kDa. In a particular embodiment, one or more polymer portions have a molecular weight of at least 1 kDa. In a particular embodiment, one or more polymer portions have a molecular weight of at least 1.5 kDa. In a particular embodiment, one or more polymer portions have a molecular weight of at least 2 kDa. In a particular embodiment, one or more polymer portions have a molecular weight of at least 2.5 kDa. In a particular embodiment, one or more polymer portions have a molecular weight of at least 3 kDa. In a particular embodiment, one or more polymer portions have a molecular weight of at least 3.5 kDa. In a particular embodiment, one or more polymer portions have a molecular weight of at least 4 kDa. In a particular embodiment, one or more polymer portions have a molecular weight of at least 5 kDa. In a particular embodiment, one or more polymer portions have a maximum molecular weight of 160 kDa. In a particular embodiment, one or more polymer portions have a maximum molecular weight of 120 kDa. In a particular embodiment, one or more polymer portions have a maximum molecular weight of 100 kDa. In certain embodiments, one or more polymer portions have a maximum molecular weight of 80 kDa. In certain embodiments, one or more polymer portions have a maximum molecular weight of 70 kDa. In certain embodiments, one or more polymer portions have a maximum molecular weight of 60 kDa. In certain embodiments, one or more polymer portions have a maximum molecular weight of 50 kDa. In certain embodiments, one or more polymer portions have a maximum molecular weight of 40 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 450 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 1 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 1.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 2 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 2.5 kDa.In certain embodiments, one or more polymer portions have a molecular weight of approximately 3 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 3.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 4 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 4.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 5.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 6 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 6.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 7 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 7.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 8 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 8.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 9 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 9.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 10 kDa. -L. B' -If - contains one polymer moiety, the minimum and maximum molecular weights provided above apply to this one polymer moiety, -L B' If - contains two or more polymer moieties, it is understood that the minimum and maximum molecular weights provided above refer to the minimum and maximum molecular weights of all polymer moieties combined.

[0332] In certain embodiments, -L B' -One or more polymer portions have a flowy radius of at least 1.2 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of at least 1.5 nm. In certain embodiments, -L B'-One or more polymer portions have a flowy radius of at least 2 nm. In certain embodiments, -L B' -One or more polymer portions have a flowy radius of at least 2.5 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of at least 3 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of at least 3.5 nm. In certain embodiments, -L B' -One or more polymer portions have a flory radius of at least 4 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of at least 4.5 nm. In certain embodiments, -L B' -One or more polymer portions have a flory radius of at least 5 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of 200 nm or less. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of 175 nm or less. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of 150 nm or less. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of 125 nm or less. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of 100 nm or less. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of 75 nm or less. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of 50 nm or less. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of 45 nm or less. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of 40 nm or less. In certain embodiments, -L B'-One or more polymer portions have a flowly radius of 35 nm or less. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of 30 nm or less. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of approximately 1.2 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of about 1.5 nm. In certain embodiments, -L B' -One or more polymer portions have a flowy radius of about 2 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of approximately 2.5 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of about 3 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of approximately 3.5 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of about 4 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of approximately 4.5 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of about 5 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of approximately 5.5 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of about 6 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of approximately 6.5 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of about 7 nm. In certain embodiments, -L B' -One or more polymer portions have a flowly radius of approximately 8.5 nm. In certain embodiments, -L B'-One or more polymer portions have a flowly radius of about 9 nm. In certain embodiments, -L B' -One or more polymer portions have a flory radius of approximately 10 nm. -L B' -If it contains one polymer portion, the flory radius provided above applies to this one polymer portion, -L B' If - contains two or more polymer parts, it is understood that the flory radius provided above refers to the flory radius of all combined polymer parts.

[0333] -L B'- is one or more polymer moieties, for example, poly(2-methacryloyl-oxyethyl phosphorylcholine), poly(acrylic acid), poly(acrylate), poly(acrylamide), poly(alkyloxy)polymer, poly(amide), poly(amideamine), poly(amino acid), poly(acid anhydride), poly(aspartamide), poly(butyric acid), poly(glycolic acid), polybutylene terephthalate, poly(caprolactone), poly(carbonate), poly(cyanoacrylate), poly(dimethylacrylamide), poly(ester), poly(ethylene), poly(ethylene glycol), poly(ethylene oxide), poly(ethyl phosphate), poly(ethyl oxazoline), poly(glycolic acid), poly(hydroxyethyl acrylate), poly(hydroxyethyl oxazoline), poly(hydroxymethacrylate), poly(hydroxypropyl methacrylamide), poly(hydroxypropyl methacrylate), poly(hydroxypropyl methacrylate), poly(hydroxypropyl methacrylate) The polymer contains polymer portions selected from the group consisting of oxypropyl oxazoline, poly(iminocarbonate), poly(lactic acid), poly(lactic acid-co-glycolic acid), poly(methacrylamide), poly(methacrylate), poly(methyloxazoline), poly(organophosphazene), poly(orthoester), poly(oxazoline), poly(propylene glycol), poly(siloxane), poly(urethane), poly(vinyl alcohol), poly(vinylamine), poly(vinyl methyl ether), poly(vinylpyrrolidone), silicone, cellulose, carbomethylcellulose, hydroxypropylmethylcellulose, chitin, chitosan, dextran, dextrin, gelatin, hyaluronic acid and derivatives, functionalized hyaluronic acid, alginate, mannan, pectin, rhamnogalacturonan, starch, hydroxyalkyl starch, hydroxyethyl starch and other carbohydrate polymers, xylan, and copolymers thereof.

[0334] In certain embodiments, -L B' - contains a PEG-based polymer. In certain embodiments, -L B' - contains a hyaluronic acid-based polymer. In certain embodiments, -L B'- comprises a random coil polymer. In certain embodiments, -L B' - contains polysarcosine polymer.

[0335] In a particular embodiment, -L of formula (Aa) B' - is equation (a-3') [ka] (In the formula, Unmarked dashed lines indicate connections to -D-. The dashed line with an asterisk indicates -L A This shows a connection to, -R c -teeth, [ka] And, -R d' - is the polymer part, -R e - is -CH2-, [ka] (Selected from the group consisting of) It belongs to them.

[0336] -R of equation (Aa) b -but [ka] If so, then -R in equation (a-3') c -teeth [ka] And the -R of equation (Aa) b -but [ka] If so, then -R in equation (a-3') c -teeth [ka] That is the case.

[0337] Part of equation (a-3') -R d'- indicates a polymer portion, meaning that it contains at least one polymer portion. In certain embodiments, one or more polymer portions have a molecular weight of at least 450 kDa. In certain embodiments, one or more polymer portions have a molecular weight of at least 1 kDa. In certain embodiments, one or more polymer portions have a molecular weight of at least 1.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of at least 2 kDa. In certain embodiments, one or more polymer portions have a molecular weight of at least 2.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of at least 3 kDa. In certain embodiments, one or more polymer portions have a molecular weight of at least 3.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of at least 4 kDa. In certain embodiments, one or more polymer portions have a molecular weight of at least 5 kDa. In certain embodiments, one or more polymer portions have a maximum molecular weight of 160 kDa. In certain embodiments, one or more polymer portions have a maximum molecular weight of 120 kDa. In certain embodiments, one or more polymer portions have a maximum molecular weight of 100 kDa. In certain embodiments, one or more polymer portions have a maximum molecular weight of 80 kDa. In certain embodiments, one or more polymer portions have a maximum molecular weight of 70 kDa. In certain embodiments, one or more polymer portions have a maximum molecular weight of 60 kDa. In certain embodiments, one or more polymer portions have a maximum molecular weight of 50 kDa. In certain embodiments, one or more polymer portions have a maximum molecular weight of 40 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 450 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 1 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 1.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 2 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 2.5 kDa.In certain embodiments, one or more polymer portions have a molecular weight of approximately 3 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 3.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 4 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 4.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 5.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 6 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 6.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 7 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 7.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 8 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 8.5 kDa. In certain embodiments, one or more polymer portions have a molecular weight of approximately 9 kDa. In certain embodiments, one or more polymer moieties have a molecular weight of approximately 9.5 kDa. In certain embodiments, one or more polymer moieties have a molecular weight of approximately 10 kDa. -R of formula (a-3'). d' -If it contains one polymer moiety, the minimum and maximum molecular weights provided above apply to this one polymer moiety, and -R of formula (a-3') d' If - contains two or more polymer moieties, it is understood that the minimum and maximum molecular weights provided above refer to the minimum and maximum molecular weights of all polymer moieties combined.

[0338] In certain embodiments, the -R of formula (a-3') d'-One or more polymer portions have a flowly radius of at least 1.2 nm. In a particular embodiment, one or more polymer portions have a flowly radius of at least 1.5 nm. In a particular embodiment, one or more polymer portions have a flowly radius of at least 2 nm. In a particular embodiment, one or more polymer portions have a flowly radius of at least 2.5 nm. In a particular embodiment, one or more polymer portions have a flowly radius of at least 3 nm. In a particular embodiment, one or more polymer portions have a flowly radius of at least 3.5 nm. In a particular embodiment, one or more polymer portions have a flowly radius of at least 4 nm. In a particular embodiment, one or more polymer portions have a flowly radius of at least 4.5 nm. In a particular embodiment, one or more polymer portions have a flowly radius of at least 5 nm. In a particular embodiment, one or more polymer portions have a flowly radius of 200 nm or less. In a particular embodiment, one or more polymer portions have a flowly radius of 175 nm or less. In a particular embodiment, one or more polymer portions have a flowly radius of 150 nm or less. In a particular embodiment, one or more polymer portions have a flowly radius of 125 nm or less. In certain embodiments, one or more polymer portions have a flowly radius of 100 nm or less. In certain embodiments, one or more polymer portions have a flowly radius of 75 nm or less. In certain embodiments, one or more polymer portions have a flowly radius of 50 nm or less. In certain embodiments, one or more polymer portions have a flowly radius of 45 nm or less. In certain embodiments, one or more polymer portions have a flowly radius of 40 nm or less. In certain embodiments, one or more polymer portions have a flowly radius of 35 nm or less. In certain embodiments, one or more polymer portions have a flowly radius of 30 nm or less. In certain embodiments, one or more polymer portions have a flowly radius of approximately 1.2 nm. In certain embodiments, one or more polymer portions have a flowly radius of approximately 1.5 nm.In certain embodiments, one or more polymer portions have a flowly radius of approximately 2 nm. In certain embodiments, one or more polymer portions have a flowly radius of approximately 2.5 nm. In certain embodiments, one or more polymer portions have a flowly radius of approximately 3 nm. In certain embodiments, one or more polymer portions have a flowly radius of approximately 3.5 nm. In certain embodiments, one or more polymer portions have a flowly radius of approximately 4 nm. In certain embodiments, one or more polymer portions have a flowly radius of approximately 4.5 nm. In certain embodiments, one or more polymer portions have a flowly radius of approximately 5 nm. In certain embodiments, one or more polymer portions have a flowly radius of approximately 5.5 nm. In certain embodiments, one or more polymer portions have a flowly radius of approximately 6 nm. In certain embodiments, one or more polymer portions have a flowly radius of approximately 6.5 nm. In certain embodiments, one or more polymer portions have a flowly radius of approximately 7 nm. In certain embodiments, one or more polymer portions have a flowly radius of approximately 8.5 nm. In certain embodiments, one or more polymer portions have a flowly radius of approximately 9 nm. In certain embodiments, one or more polymer moieties have a flowly radius of approximately 10 nm. -R of formula (a-3'). d' -If it contains one polymer part, the flory radius provided above applies to this one polymer part and the -R of formula (a-3') d' If - contains two or more polymer parts, it is understood that the flory radius provided above refers to the flory radius of all combined polymer parts.

[0339] -R in equation (a-3') d'- is one or more polymer moieties, for example, poly(2-methacryloyl-oxyethyl phosphorylcholine), poly(acrylic acid), poly(acrylate), poly(acrylamide), poly(alkyloxy)polymer, poly(amide), poly(amideamine), poly(amino acid), poly(acid anhydride), poly(aspartamide), poly(butyric acid), poly(glycolic acid), polybutylene terephthalate, poly(caprolactone), poly(carbonate), poly(cyanoacrylate), poly(dimethylacrylamide), poly(ester), poly(ethylene), poly(ethylene glycol), poly(ethylene oxide), poly(ethyl phosphate), poly(ethyl oxazoline), poly(glycolic acid), poly(hydroxyethyl acrylate), poly(hydroxyethyl oxazoline), poly(hydroxymethacrylate), poly(hydroxypropyl methacrylamide), poly(hydroxypropyl methacrylate), poly(hydroxypropyl methacrylate), poly(hydroxypropyl methacrylate) The polymer contains polymer portions selected from the group consisting of oxypropyl oxazoline, poly(iminocarbonate), poly(lactic acid), poly(lactic acid-co-glycolic acid), poly(methacrylamide), poly(methacrylate), poly(methyloxazoline), poly(organophosphazene), poly(orthoester), poly(oxazoline), poly(propylene glycol), poly(siloxane), poly(urethane), poly(vinyl alcohol), poly(vinylamine), poly(vinyl methyl ether), poly(vinylpyrrolidone), silicone, cellulose, carbomethylcellulose, hydroxypropylmethylcellulose, chitin, chitosan, dextran, dextrin, gelatin, hyaluronic acid and derivatives, functionalized hyaluronic acid, alginate, mannan, pectin, rhamnogalacturonan, starch, hydroxyalkyl starch, hydroxyethyl starch and other carbohydrate polymers, xylan, and copolymers thereof.

[0340] In certain embodiments, the -R of formula (a-3') d' - contains PEG-based polymers. In certain embodiments, -R of formula (a-3') d'- contains a hyaluronic acid-based polymer. In certain embodiments, -R of formula (a-3') d' - comprises a random coil polymer. In certain embodiments, -R of formula (a-3') d' - contains polysarcosine polymer.

[0341] In certain embodiments, the distance between any two parts-AB of a compound is such that they can bind to two different binding sites on the same albumin molecule, or to two different albumin molecules. All or some of the parts-AB may bind to different albumin molecules, and / or two or more parts-AB may bind to one albumin molecule. Generally, if a compound has x parts-AB, they can bind to up to x albumin molecules. It is understood that not all parts-AB of a compound can be bound to one albumin molecule at any given time.

[0342] The ability to bind to two or more different albumin molecules significantly increases the molecular weight of the compound, which has a favorable effect on its cyclic half-life.

[0343] In certain embodiments, -D- is a protein or peptide drug moiety, and -AB is conjugated to a functional group of -D- provided by a side chain of an N-terminal amine, C-terminal carboxyl, or amino acid residue. In certain embodiments, -AB is conjugated to the N-terminal amine functional group of -D-. In certain embodiments, -AB is conjugated to the C-terminal carboxyl functional group. In certain embodiments, -AB is conjugated to a functional group of -D- provided by an amino acid residue, for example, lysine, serine, aspartic acid, glutamic acid, arginine, histidine, threonine, glutamine, asparagine, cysteine, proline, tyrosine, or tryptophan. In certain embodiments, -AB is conjugated to the functional group of the lysine side chain of -D-. In certain embodiments, -AB is conjugated to the functional group of the serine side chain of -D-. In certain embodiments, -AB is conjugated to the functional group of the side chain of -D- aspartic acid. In certain embodiments, -AB is conjugated to the functional group of the side chain of -D- glutamic acid. In certain embodiments, -AB is conjugated to the functional group of the side chain of -D- arginine. In certain embodiments, -AB is conjugated to the functional group of the side chain of -D- histidine. In certain embodiments, -AB is conjugated to the functional group of the side chain of -D- threonine. In certain embodiments, -AB is conjugated to the functional group of the side chain of -D- glutamine. In certain embodiments, -AB is conjugated to the functional group of the side chain of -D- asparagine. In certain embodiments, -AB is conjugated to the functional group of the side chain of -D- cysteine. In certain embodiments, -AB is conjugated to the functional group of the side chain of -D- proline. In certain embodiments, -AB is conjugated to the functional group of the tyrosine side chain of -D-. In certain embodiments, -AB is conjugated to the functional group of the tryptophan side chain of -D-.

[0344] In certain embodiments, -D-AB is selected from the group consisting of semaglutide, liraglutide, echnoglutide, GZR18, GL0034, tilzepatide, cotadutide, BI-456906, pembidutide, mazdutide, dapiglutide, and letatoltide.

[0345] In certain embodiments, -D-AB is selected from the group consisting of semaglutide, liraglutide, echnoglutide, GZR18, and GL0034.

[0346] In certain embodiments, -D-AB is semaglutide. Semaglutide is a compound of the formula HX1EGTFTSDVSSYLEGQAAKEFIAWLVRGRG (Sequence ID 40) [In the formula, X1 is α-aminoisobutyric acid (Aib), Lysine, ranked 20th, [ka] (In the formula, (The dashed line indicates the bond of the lysine side chain of lysine at position 20 to the ε-amine group.) [It is chemically modified via conjugation of the lysine side chain to the ε-amine group.] It is a compound of [the compound].

[0347] Semaglutide can be prepared using methods known to those skilled in the art, such as those described in WO2006 / 097537.

[0348] In certain embodiments, -D-AB is liraglutide. Liraglutide is a compound of the formula HAEGTFTSDVSSYLEGQAAKEFIAWLVRGRG(Sequence ID 41) [In the formula, Lysine, ranked 20th, [ka] (In the formula, (The dashed line indicates the bond of the lysine side chain of lysine at position 20 to the ε-amine group.) [It is chemically modified via conjugation of the lysine side chain to the ε-amine group.] It is a compound of [the compound].

[0349] In certain embodiments, -D-AB is echnoglutide. Echnoglutide is a compound of the formula HVEGTFTSDVSSYLEEQAAREFIKWLVRGRG (Sequence ID 42) [In the formula, Lysine, ranked 24th, [ka] (In the formula, the dashed line indicates the bond of the lysine side chain of lysine at position 24 to the ε-amine group.) [It is chemically modified via conjugation of the lysine side chain to the ε-amine group.] It is a compound of [the compound].

[0350] In a particular embodiment, -D-AB is GZR18. GZR18 is a formula HGEGTFTSDVSSYLEGQAAKEFIAWLVRGRG (Sequence No. 43) [In the formula, Lysine, ranked 20th, [ka] (In the formula, the dashed line indicates the bond of the lysine side chain of lysine at position 20 to the ε-amine group.) [It is chemically modified via conjugation of the lysine side chain to the ε-amine group.] It is a compound of [the compound].

[0351] In certain embodiments, -D-AB is GL0034. GL0034 is also known as utreglutide and has the formula HX1EGTFTSDVSSYLEGQAAKEFIAWLVRGRGL (Sequence ID 44) [In the formula, X1 is Aib, Lysine, ranked 20th, [ka] (In the formula, the dashed line indicates the bond of the lysine side chain of lysine at position 20 to the ε-amine group.) [It is chemically modified via conjugation of the lysine side chain to the ε-amine group.] It is a compound of [the compound].

[0352] In certain embodiments, -D- or -D-AB is a dual GLP-1 receptor agonist selected from the group consisting of tylzepatide, cotadutide, BI-456906, pembidutide, and mazdutide.

[0353] In certain embodiments, -D-AB is a dual GLP-1 receptor agonist that activates both the GLP-1 receptor and the GIP receptor. An example of such a dual GLP-1 receptor agonist is tilzepatide. In certain embodiments, -D-AB is tilzepatide. Tilzepatide is a compound of the formula YX1EGTFTSDYSIX2LDKIAQKAFVQWLIAGGPSSGAPPPS(Sequence ID 45) (In the formula, X1 is Aib, X2 is Aib, Lysine, ranked 20th, is ([2-(2-amino-ethoxy)-ethoxy]-acetyl)2-(γGlu)1-CO-(CH2) 18 It is chemically modified via conjugation of the lysine side chain to the ε-amine group by -CO2H, The C-terminal serine, specifically the serine at position 39, is amidated as a C-terminal primary amide. It is a compound of [the compound].

[0354] Partial ([2-(2-amino-ethoxy)-ethoxy]-acetyl)2-(γGlu)1-CO-(CH2) 18 -CO2H has the following structure [ka] (In the formula, the dashed line indicates a connection to -D-) It holds.

[0355] In certain embodiments, -D-AB is a dual GLP-1 receptor agonist that activates both the GLP-1 receptor and the glucagon receptor, selected from the group consisting of cotadutide, BI-456906, pembidutide, and mazdutide.

[0356] In certain embodiments, -D-AB is cotadutide. Cotadutide is a compound of the formula HSQGTFTSDKSEYLDSERARDFVAWLEAGG (Sequence ID 46) (In the formula, The lysine at position 10 is chemically modified via conjugation of the lysine side chain to the ε-amine group by γ-Glu-palmitoyl. It is a compound of [the compound].

[0357] Partial γ-Glu-palmitoyl has the following structure: [ka] (In the formula, the dashed line indicates a connection to -D-) It holds.

[0358] In certain embodiments, -D-AB is BI-456906. BI-456906 is also known as sulfodutide and has the formula HX1QGTFTSDYSKYLDERAAKDFIKWLESA (Sequence ID 47) (In the formula, X1 is 1-amino-cyclobutanecarboxylic acid (Ac4c), The lysine at position 24 is chemically modified via conjugation of the lysine side chain to the ε-amine group by [l7-carboxy-heptadecanoyl]-isoGlu-GSGSGG. The C-terminal alanine, specifically the alanine at position 29, is amidated as a primary C-terminal amide. It is a compound of [the compound].

[0359] The partial [l7-carboxy-heptadecanoyl]-isoGlu-GSGSGG has the following structure: [ka] (In the formula, the dashed line indicates a connection to -D-) It holds.

[0360] In certain embodiments, -D-AB is pembidutide. Pembidutide is a compound of the formula HX1QGTFTSDYSKYLDEKAAKEFIQWLLQT (Sequence ID 48) [In the formula, X1 is Aib, The glutamic acid at position 16 and the lysine at position 20 are linked via lactam crosslinking. Lysine, ranked 17th, is... [ka] (In the formula, the dashed line indicates the bond of lysine at position 17 to the ε-amine group.) This part is chemically modified via conjugation of the ε-amine group of the lysine side chain by glucuronic acid C-18. The C-terminal threonine, specifically the threonine at position 29, is amidated as a primary amide at the C-terminus. It is a compound of [the compound].

[0361] In certain embodiments, -D-AB is mazdutide. Mazdutide is a compound of the formula HX1QGTFTSDYSKYLDEKKAKEFVEWLLEGGPSSG (Sequence ID 49) (In the formula, X1 is Aib, Lysine, ranked 20th, is ([2-(2-amino-ethoxy)-ethoxy]-acetyl)2-(γGlu)-CO-(CH2) 18 It is chemically modified by conjugation of the ε-amine group of the lysine side chain with -CO2H, The C-terminal glycine, specifically the glycine at position 34, is amidated. It is a compound of [the compound].

[0362] Partial ([2-(2-amino-ethoxy)-ethoxy]-acetyl)2-(γGlu)-CO-(CH2) 18 -CO2H has the following structure: [ka] (In the formula, the dashed line indicates a connection to -D-) It holds.

[0363] In certain embodiments, -D-AB is a dual GLP-1 receptor agonist that activates both GLP-1 and GLP-2 receptors, such as dapiglutide. Dapiglutide is formulated as follows: HX1EGSFTSELATILDKQAARDFIAWLIQHKITD (Sequence ID 50) (In the formula, X1 is Aib, The lysine at position 16 is chemically modified by conjugation of the ε-amine group of the lysine side chain with [17-carboxy-heptadecanoyl]-isoGlu. It is a compound of [the compound].

[0364] The partial [17-carboxy-heptadecanoyl]-isoGlu has the following structure: [ka] (In the formula, the dashed line indicates a connection to -D-) It holds.

[0365] In certain embodiments, -D-AB is letatoltide, a triple GLP-1 receptor agonist that activates the GLP-1 receptor, GIP receptor, and GCG receptor. Letatoltide is formulated as follows: YX1QGTFTSDYSIX2LDKKAQX3AFIEYLLEGGPSSGAPPPS (Sequence ID 51) (In the formula, X1 is Aib, X2 is α-methylleucine (αMeL), X3 is Aib, Lysine, ranked 17th, is (2-[2-(2-amino-ethoxy)-ethoxy]-acetyl)-(γGlu)-CO-(CH2) 18 It is chemically modified by conjugation of the ε-amine group of the lysine side chain with -CO2H, The C-terminal serine, specifically the serine at position 39, is amidated. It is a compound of [the compound].

[0366] Letatoltide is Y-Aib-QGTFTSDYSI-αMeL-LDKK ((2-[2-(2-amino-ethoxy)-ethoxy]-acetyl)-(γGlu)-CO-(CH2) 18 It can also be written as -CO2H) AQ-Aib-AFIEYLLEGGPSSGAPPPS-NH2 (Sequence ID 51).

[0367] Partial (2-[2-(2-amino-ethoxy)-ethoxy]-acetyl)-(γGlu)-CO-(CH2) 18 -CO2H has the following structure: [ka] It holds.

[0368] In certain embodiments, -D-AB is a noiiglutide, also known as SHR20004.

[0369] In a particular embodiment, -D-AB is ZT002.

[0370] In certain embodiments, -D-AB is selected from the group consisting of semaglutide, liraglutide, echnoglutide, GZR18, GL0034, tilzepatide, cotadutide, BI-456906, pembidutide, mazdutide, dapiglutide, and letatoltide.

[0371] In a particular embodiment, -D-AB is given by formula (b-1) [ka] (In the formula, X 1 -teeth, [ka] And, -X 2 teeth, [ka] And, (Ph stands for phenyl) It belongs to them.

[0372] Part D of formula (b-1) has sequence YX1EGTFTSDYSIX2LDKIAQKAFVQWLIAGGPSSGAPPPS, sequence number 57, where X1 and X2 are Aib.

[0373] The compound of formula (b-1) is disclosed in WO2022159395 and WO2023 / 044290, the contents of which are incorporated herein by reference in their entirety.

[0374] In certain embodiments, -D-AB is of formula (b-1), and X 1 -teeth [ka] And -X 2 teeth [ka] In a particular embodiment, -D-AB is of formula (b-1), and X 1 -teeth [ka] And -X 2 teeth [ka] In a particular embodiment, -D-AB is of formula (b-1), and X 1 -teeth [ka] And -X 2 teeth [ka] In a particular embodiment, -D-AB is of formula (b-1), and X 1 -teeth [ka] And -X 2 teeth [ka] In a particular embodiment, -D-AB is of formula (b-1), and X 1 -teeth [ka] And -X 2 teeth [ka] In a particular embodiment, -D-AB is of formula (b-1), and X 1 -teeth [ka] And -X 2 teeth [ka] In a particular embodiment, -D-AB is of formula (b-1), and X 1 -teeth [ka] And -X 2teeth [ka] In a particular embodiment, -D-AB is of formula (b-1), and X 1 -teeth [ka] And -X 2 teeth [ka] In a particular embodiment, -D-AB is of formula (b-1), and X 1 -teeth [ka] And -X 2 teeth [ka] In a particular embodiment, -D-AB is of formula (b-1), and X 1 -teeth [ka] And -X 2 teeth [ka] In a particular embodiment, -D-AB is of formula (b-1), and X 1 -teeth [ka] And -X 2 teeth [ka] In a particular embodiment, -D-AB is of formula (b-1), and X 1 -teeth [ka] And -X 2 teeth [ka] That is the case.

[0375] In a particular embodiment, -D-AB is a formula k(γE-(miniPEG)2-γE-COC 16 H 32 CO2H)(N-Me)GSVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHK(γE-(miniPEG)2-γE-COC 16 H 32 CO2H)-OH (SEQ ID NO: 52) (In the formula, k is d-Lys, γE is the l-isomer of gamma glutamic acid, miniPEG is COCH2OCH2CH2OCH2CH2NH, COC 16 H 32 CO2H is a C18 diacid. (N-Me)G is sarcosine, K is the l-isomer of lysine, -OH indicates that the C-terminal amino acid has a terminal carboxylic acid. It is a compound of [the compound].

[0376] In a particular embodiment, -D-AB is a formula k(γE-(miniPEG)2-γE-COC 16 H 32 CO2H)(N-Me)GSVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHK(γE-(miniPEG)2-γE-COC 16 H 32 CO2H)-OH (SEQ ID NO: 53) (In the formula, k is d-Lys, γE is the l-isomer of gamma glutamic acid, (miniPEG)2 is COCH2OCH2CH2OCH2CH2NH, COC 16 H 32 CO2H is a C18 diacid. (N-Me)G is sarcosine, K is the l-isomer of lysine, -OH indicates that the C-terminal amino acid has a terminal carboxylic acid. It is a compound of [the compound].

[0377] -D- is a peptide or protein drug portion, -L 1 - is conjugated to a functional group in the side chain of an amino acid residue of -D-, or to the N-terminal amine functional group or C-terminal carboxyl functional group of -D-, or to a nitrogen atom in the backbone chain of -D-.

[0378] -D- is a peptide or protein drug portion, -L 1 -In certain embodiments, -D- is conjugated to a functional group selected from the group consisting of carboxylic acids, primary amines, secondary amines, maleimides, thiols, sulfonic acids, carbonates, carbamates, hydroxyls, aldehydes, ketones, hydrazines, isocyanates, isothiocyanates, phosphoric acids, phosphonic acids, haloacetyls, alkyl halides, acryloyls, aryl fluorides, hydroxylamines, sulfates, disulfides, vinyl sulfones, vinyl ketones, diazoalkanes, oxiranes, guanidines, and aziridines.When -D- is a peptide or protein drug moiety, -L 1 - is conjugated in certain embodiments to a functional group of -D- selected from the group consisting of hydroxyl, primary amine, secondary amine, and guanidine. When -D- is a peptide or protein drug moiety, -L 1 - is conjugated in certain embodiments to a functional group of -D- selected from the group consisting of primary and secondary amines. When -D- is a peptide or protein drug moiety, -L 1 - is conjugated to a primary amine -D- in certain embodiments.

[0379] -D- is a peptide or protein drug portion, -L 1 - can be conjugated to a functional group on the side chain of an amino acid residue of -D-, which may be a protein-constituting amino acid residue or a non-protein-constituting amino acid residue.

[0380] -D- is a peptide or protein drug portion, -L 1 - is conjugated in certain embodiments to the functional group of the side chain of the protein constituent amino acid residue of -D-. In certain embodiments, such amino acid residues are selected from the group consisting of histidine, lysine, tryptophan, serine, threonine, tyrosine, aspartic acid, glutamic acid, and arginine. In certain embodiments, such amino acid residues are selected from the group consisting of lysine, aspartic acid, arginine, and serine. In certain embodiments, such amino acid residues are selected from the group consisting of lysine, arginine, and serine.

[0381] -D- is a peptide or protein drug portion, -L 1 - is conjugated to the functional group of the lysine residue of -D- in certain embodiments. When -D- is a peptide or protein drug moiety, -L 1 - is conjugated to the functional group of the histidine residue of -D- in certain embodiments. When -D- is a peptide or protein drug moiety, -L 1 - is conjugated to the functional group of the tryptophan residue of -D- in certain embodiments. When -D- is a peptide or protein drug moiety, -L 1 - is conjugated to the functional group of the serine residue of -D- in certain embodiments. When -D- is a peptide or protein drug moiety, -L 1 - is conjugated to the threonine residue functional group of -D- in certain embodiments. When -D- is a peptide or protein drug moiety, -L 1- is conjugated to the functional group of the tyrosine residue of -D- in certain embodiments. When -D- is a peptide or protein drug moiety, -L 1 - is conjugated to the functional group of the aspartic acid residue of -D- in certain embodiments. When -D- is a peptide or protein drug moiety, -L 1 - is conjugated to the functional group of the glutamic acid residue of -D- in certain embodiments. When -D- is a peptide or protein drug moiety, -L 1 - is conjugated to the functional group of the arginine residue of -D- in certain embodiments.

[0382] -D- is a peptide or protein drug portion, -L 1 - is conjugated in certain embodiments to the functional group of the side chain of a non-protein constituent amino acid residue of -D-.

[0383] It should be understood that not all peptide or protein drug moieties -D- may contain all of these amino acid residues.

[0384] -D- is a peptide or protein drug portion, -L 1 - is conjugated to the N-terminal amine functional group of -D- in certain embodiments.

[0385] -D- is a peptide or protein drug portion, -L 1 - is conjugated to the C-terminal functional group of -D- in certain embodiments.

[0386] Part-L 1 - can be coupled to -D- by any type of coupling, provided that it is reversible. In certain embodiments, -L 1 - is bonded to -D- by a bond selected from the group consisting of amide, ester, carbamate, acetal, aminal, imine, oxime, hydrazone, disulfide, and acylguanidine. In certain embodiments, -L 1- is bonded to -D- by a bond selected from the group consisting of amide, ester, carbamate and acylguanidine. Some of these bonds are not themselves reversible, however, in the present invention the adjacent groups present in -L 1 - are understood to reversibly cause these bonds.

[0387] In certain embodiments, -L 1 - is bonded to -D- by an amide bond. In certain embodiments, -L 1 - is bonded to -D- by a carbamate bond. In certain embodiments, -L 1 - is bonded to -D- by an ester bond. In certain embodiments, -L 1 - is bonded to -D- by an acylguanidine bond.

[0388] The moiety -L 1 - is a reversible prodrug linker from which the drug, i.e. H-D-AB, is released in its free form, i.e. a prodrug linker that leaves no trace. It is understood that "H-" in "H-D-AB" is hydrogen. Suitable prodrug linkers, for example, the reversible prodrug linker moieties disclosed in WO  2005 / 099768 A2, WO 2006 / 136586 A2, WO 2011 / 089216 A1 and WO 2013 / 024053 A1 are known in the art and these documents are incorporated herein by reference.

[0389] In certain embodiments, -L 1 - is disclosed in WO 2009 / 095479 A2. Thus, in certain embodiments, the moiety -L 1 - has the formula (II):

Chemical formula

[0390] In a particular embodiment, -L of formula (II) 1 - is one part -L 2 It is replaced with -.

[0391] In a particular embodiment, -L of formula (II) 1 - has not been further replaced.

[0392] -R in equation (II) 3 / -R 3a However, when they combine with the nitrogen atom to which they are bonded to form a 3-10 member heterocycle, the atom directly bonded to the nitrogen is SP 3 It is understood that only such 3- to 10-membered heterocycles, which are hybrid carbon atoms, can be formed. In other words, -R 3 / -R 3a As a result, such 3- to 10-membered heterocycles formed together with the nitrogen atoms to which they are bonded have the following structure: [ka] (In the formula, The dashed line is -L 1 - indicates the connection to the remainder, The ring contains 3 to 10 atoms, including at least one nitrogen atom. R # and R ## is, sp 3 This refers to hybridized carbon atoms.

[0393] It is also understood that the above 3- to 10-member complex rings can be further permuted.

[0394] -R in equation (II) 3 / -R 3a The following are exemplary embodiments of preferred 3- to 10-membered heterocycles formed by these together with the nitrogen atoms to which they are bonded: [ka] (In the formula, The dashed line indicates the bond to the rest of the molecule. -R is -H and C 1-6 (Selected from the group consisting of alkyl groups).

[0395] -L in equation (II) 1 - may be further substituted depending on the case. In general, any substituent can be used as long as it does not affect the principle of cleavage, i.e., the hydrogen with an asterisk in formula (II) is not substituted and part of formula (II) [ka] The nitrogen remains as part of the primary, secondary, or tertiary amine, i.e., -R 3 and -R 3a These are either -H independently of each other, or sp 3 It is bonded to -N< via hybridized carbon atoms.

[0396] In one embodiment, the -R of formula (II) 1 or -R1a is, -L 2 It is replaced by -. In another embodiment, the -R of formula (II) 2 or -R 2a is, -L 2 It is replaced by -. In another embodiment, the -R of formula (II) 3 or -R 3a is, -L 2 It is replaced by -. In another embodiment, the -R of formula (II) 4 is, -L 2 It is replaced by -. In another embodiment, the -R of formula (II) 5 or -R 5a is, -L 2 It is replaced by -. In another embodiment, the -R of formula (II) 6 is, -L 2 It is replaced by -. In another embodiment, the -R of formula (II) 7 or -R 7a is, -L 2 It is replaced by -. In another embodiment, the -R of formula (II) 8 or -R 8a is, -L 2 It is replaced by -. In another embodiment, the -R of formula (II) 9 or -R 9a is, -L 2 It is replaced by -R 10 is, -L 2 It is replaced by -R 11 is, -L 2 It is replaced by - in certain embodiments, -R in formula (II) 3 is, -L 2 It is replaced with -.

[0397] In a particular embodiment, -X- in formula (II) is -C(R 4 R 4a )-,-N(R 4 )- and -C(R 7 R 7a Selected from the group consisting of )-. In a particular embodiment, -X- in formula (II) is -C(R 4 R 4a)-. In a particular embodiment, -X- in formula (II) is -C(R 7 R 7a )-is.

[0398] In certain embodiments, -R of formula (II) 7 -NR 10 -(C=O)-R 11 That is the case.

[0399] In certain embodiments, -R of formula (II) 7a is selected from -H, methyl and ethyl. In certain embodiments, -R of formula (II) 7a It is -H.

[0400] In certain embodiments, -R 10 is selected from -H, methyl and ethyl. In certain embodiments, -R 10 It is methyl.

[0401] In certain embodiments, -R 11 is selected from -H, methyl and ethyl. In certain embodiments, -R 11 is -H. In certain embodiments, -R 11 is, -L 2 It is replaced with -.

[0402] In a particular embodiment, -X- in formula (II) is -N(R 4 )-is.

[0403] In certain embodiments, -R 4 is selected from the group consisting of -H, methyl, and ethyl. In certain embodiments, -R 4 It is -H.

[0404] In a particular embodiment, X of formula (II) 1 It is C.

[0405] In a particular embodiment, equation (II) = X 3 The answer is = O.

[0406] In a particular embodiment, -X of formula (II) 2 - is -C(R 8 R 8a )-is.

[0407] In certain embodiments, -R of formula (II) 8 and -R 8a The is independently selected from the group consisting of -H, methyl, and ethyl. In certain embodiments, the -R of formula (II) 8 and -R 8a At least one of them is -H. In certain embodiments, -R of formula (II) 8 and -R 8a Both are -H.

[0408] In certain embodiments, -R of formula (II) 1 and -R 1a This is independently selected from the group consisting of -H, methyl, and ethyl.

[0409] In certain embodiments, -R of formula (II) 1 and -R 1a At least one of them is -H. In certain embodiments, -R of formula (II) 1 and -R 1a It is -H.

[0410] In certain embodiments, -R of formula (II) 1 and -R 1a At least one of them is methyl. In certain embodiments, -R of formula (II) 1 and -R 1a Both are methyl.

[0411] In certain embodiments, -R of formula (II) 2 and -R 2a The is independently selected from the group consisting of -H, methyl, and ethyl. In certain embodiments, the -R of formula (II) 2 and -R 2a At least one of them is -H. In certain embodiments, -R of formula (II)2 and -R 2a Both are H.

[0412] In certain embodiments, -R of formula (II) 3 and -R 3a This is independently selected from the group consisting of -H, methyl, ethyl, propyl, and butyl.

[0413] In certain embodiments, -R of formula (II) 3 and -R 3a At least one of them is methyl. In certain embodiments, -R of formula (II) 3 It is methyl, and -R in formula (II) 3a is -H.

[0414] In certain embodiments, -R of formula (II) 3 and -R 3a Both are -H.

[0415] In certain embodiments, -D- is linked to -L via nitrogen by forming an amide bond. 1 It is connected to -.

[0416] In certain embodiments, -L 1 - is from equation (II), where X is -C(R 7 R 7a )- and X 1 is C, and -X 2 - is -C(R 8 R 8a )-C(R 9 R 9a )- and =X 3 is = O, and -R 1 and -R 1a is -H and -R 2 and -R 2a is -H and -R 3 and -R 3a It is methyl, and -R 7 is -N(R 10 R 10a ) and -R 7a is -H and -R 8, -R 8a , -R 9 and -R 9a is -H and -R 10 It is methyl, and -R 10a is -H.

[0417] In certain embodiments, -L 1 - is equation (IIa) [ka] (In the formula, The dashed line with an asterisk indicates the bond to nitrogen of -D-. Dashed lines without a mark are -L 2 (Indicates a connection to -) It belongs to them.

[0418] In certain embodiments, -L 1 - is equation (IIa-a) [ka] (In the formula, The dashed line with an asterisk indicates the bond to nitrogen of -D-. Dashed lines without a mark are -L 2 (Indicates a connection to -) It belongs to them.

[0419] In certain embodiments, -L 1 - is equation (IIa-b) [ka] (In the formula, The dashed line with an asterisk indicates the bond to nitrogen of -D-. Dashed lines without a mark are -L 2 (Indicates a connection to -) It belongs to them.

[0420] The parts of formulas (IIa), (IIa-a), and (IIa-b) are bonded to -D- via amide bonds formed by the nitrogen of the amine functional group and the carbonyl to the left of the dashed line with an asterisk.

[0421] In certain embodiments, -L 1 - is from equation (II), where X is -C(R 7 R 7a )- and X 1 is C, and -X 2 - is -C(R 8 R 8a )-C(R 9 R 9a )- and =X 3 is = O, and -R 1 and -R 1a is -H and -R 2 and -R 2a is -H and -R 3 and -R 3a It is methyl, and -R 7 -NR 10 -(C=O)-R 11 And, -R 7a is -H and -R 8 , -R 8a , -R 9 and -R 9a is -H and -R 10 It is methyl, and -R 11 is -H.

[0422] In certain embodiments, -L 1 - is from equation (II), where X is -C(R 7 R 7a )- and X 1 is C, and -X 2 - is -C(R 8 R 8a )-C(R 9 R 9a )- and =X 3 is = O, and -R 1 and -R 1a is -H and -R 2 and -R 2a is -H and -R 3and -R 3a It is methyl, and -R 7 -NR 10 -(C=O)-R 11 And, -R 7a is -H and -R 8 , -R 8a , -R 9 and -R 9a is -H and -R 10 is -H and -R 11 is -H.

[0423] In certain embodiments, -L 1 - is equation (IIab) [ka] (In the formula, The dashed line with an asterisk indicates the bond to nitrogen of -D-. Dashed lines without a mark are -L 2 (Indicates a connection to -) It belongs to them.

[0424] In certain embodiments, -L 1 - is equation (IIab-a) [ka] (In the formula, The dashed line with an asterisk indicates the bond to nitrogen of -D-. Dashed lines without a mark are -L 2 (Indicates a connection to -) It belongs to them.

[0425] In certain embodiments, -L 1 - is equation (IIab-b) [ka] (In the formula, The dashed line with an asterisk indicates the bond to nitrogen of -D-. Dashed lines without a mark are -L 2 (Indicates a connection to -) It belongs to them.

[0426] The parts of formulas (IIab), (IIab-a), and (IIab-b) are bonded to -D- via amide bonds formed by the nitrogen of the amine functional group and the carbonyl to the left of the dashed line with an asterisk.

[0427] In certain embodiments, -L 1 - is disclosed in WO2016 / 020373A1. Therefore, in certain embodiments, part -L 1 - is equation (III): [ka] (In the formula, The dashed lines indicate bonding to a -D- primary or secondary amine or hydroxyl group via an amide bond or ester bond, respectively. -R 1 , -R 1a , -R 2 , -R 2a , -R 3 and -R 3a These are -H and -C(R) independently of each other. 8 R 8a R 8b ), -C(=O)R 8 -C≡N, -C(=NR) 8 )R 8a ,-CR 8 (=CR 8a R 8b ), -C≡CR 8 Selected from the group consisting of and -T, -R 4 , -R 5 and -R 5a These are -H and -C(R) independently of each other. 9 R 9a R 9b Selected from the group consisting of ) and -T, a1 and a2 are independently 0 or 1. Each-R 6 , -R 6a , -R 7 , -R 7a , -R 8, -R 8a , -R 8b , -R 9 , -R 9a , and -R 9b These are -H, halogen, -CN, and -COOR, which are independent of each other. 10 , -OR 10 , -C(O)R 10 ,-C(O)N(R 10 R 10a ), -S(O)2N(R 10 R 10a ), -S(O)N(R 10 R 10a ), -S(O)2R 10 ,-S(O)R 10 , -N(R 10 )S(O)2N(R 10a R 10b ), -SR 10 , -N(R 10 R 10a ), -NO2, -OC(O)R 10 , -N(R 10 )C(O)R 10a , -N(R 10 )S(O)2R 10a , -N(R 10 )S(O)R 10a , -N(R 10 )C(O)OR 10a , -N(R 10 )C(O)N(R 10a R 10b ), -OC(O)N(R 10 R 10a ), -T, C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Selected from the group consisting of alkynyls, where -T, C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Alkinyl has one or more -Rs, which may be the same or different. 11 In some cases, it is replaced by C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) 12 )-,-S(O)2N(R12 )-,-S(O)N(R 12 )-, -S(O)2-, -S(O)-, -N(R 12 )S(O)2N(R 12a )-, -S-, -N(R 12 )-, -OC(OR 12 )(R 12a )-,-N(R 12 )C(O)N(R 12a )-, and -OC(O)N(R 12 )- may intersect with one or more groups selected from the group consisting of, Each-R 10 , -R 10a , and -R 10b These are independently -H, -T, and C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Selected from the group consisting of alkynyls, where -T, C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Alkinyl has one or more -Rs, which may be the same or different. 11 In some cases, it is replaced by C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) 12 )-,-S(O)2N(R 12 )-,-S(O)N(R 12 )-, -S(O)2-, -S(O)-, -N(R 12 )S(O)2N(R 12a )-, -S-, -N(R 12 )-, -OC(OR 12 )(R 12a )-,-N(R 12 )C(O)N(R 12a )-, and -OC(O)N(R 12 )- may intersect with one or more groups selected from the group consisting of, Each T is independently phenyl, naphthyl, indenyl, indanyl, tetralinyl, C 3-10Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclyls, and 8-11 membered heterobicyclyls, each T independently has one or more identical or different -R groups. 11 It is sometimes replaced by, Each-R 11 These are, independently of each other, halogen, -CN, oxo (=O), and -COOR. 13 , -OR 13 , -C(O)R 13 ,-C(O)N(R 13 R 13a ), -S(O)2N(R 13 R 13a ), -S(O)N(R 13 R 13a ), -S(O)2R 13 ,-S(O)R 13 , -N(R 13 )S(O)2N(R 13a R 13b ), -SR 13 , -N(R 13 R 13a ), -NO2, -OC(O)R 13 , -N(R 13 )C(O)R 13a , -N(R 13 )S(O)2R 13a , -N(R 13 )S(O)R 13a , -N(R 13 )C(O)OR 13a , -N(R 13 )C(O)N(R 13a R 13b ), -OC(O)N(R 13 R 13a ), and C 1-6 Selected from alkyl, where C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each-R 12 , -R 12a , -R 13 , -R 13a , and -R 13b These are independently -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6Alkyl is optionally substituted with one or more halogens, either the same or different. Depending on the circumstances, Pair-R 1 / -R 1a , -R 2 / -R 2a , -R 3 / -R 3a , -R 6 / -R 6a , and -R 7 / -R 7a One or more of them, together with the atom they are bonded to, C 3-10 Forming a cycloalkyl or 3-10 membered heterocycline, Depending on the circumstances, Pair-R 1 / -R 2 , -R 1 / -R 3 , -R 1 / -R 4 , -R 1 / -R 5 , -R 1 / -R 6 , -R 1 / -R 7 , -R 2 / -R 3 , -R 2 / -R 4 , -R 2 / -R 5 , -R 2 / -R 6 , -R 2 / -R 7 , -R 3 / -R 4 , -R 3 / -R 5 , -R 3 / -R 6 , -R 3 / -R 7 , -R 4 / -R 5 , -R 4 / -R 6 , -R 4 / -R 7 , -R 5 / -R 6 , -R 5 / -R 7 , and -R 6 / -R 7One or more of these, together with the atoms to which they are bonded, form ring A. A is phenyl, naphthyl, indenyl, indanyl, tetralinyl, C 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclyls, and 8-11 membered heterobicyclyls, Here, -L 1 - is at least one -L 2 - is replaced by -L 1 - is sometimes further replaced.) It belongs to them.

[0428] -L in equation (III) 1 Further optional substituents of - are, in certain embodiments, as described above.

[0429] In certain embodiments, -L of formula (III) 1 - is one part -L 2 It is replaced with -.

[0430] In certain embodiments, -L of formula (III) 1 - has not been further replaced.

[0431] In certain embodiments, -L 1 - is disclosed in European Patent No. 1536334B1, WO2009 / 009712A1, WO2008 / 034122A1, WO2009 / 143412A2, WO2011 / 082368A2, and U.S. Patent No. 8,618,124B2, all of which are incorporated herein by reference.

[0432] In certain embodiments, -L 1 - is disclosed in U.S. Patent No. 8,946,405 B2 and U.S. Patent No. 8,754,190 B2, which are incorporated herein by reference in their entirety. Thus, in certain embodiments, -L 1 - is equation (IV): [ka] (In the formula, The dashed line indicates a bond to -D-, where the bond is via a functional group of -D- selected from the group consisting of -OH, -SH, and -NH2. m is either 0 or 1. -R 1 and -R 2 At least one or both of these are, independently of each other, -CN, -NO2, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkenyl, optionally substituted alkynyl, -C(O)R 3 ,-S(O)R 3 -S(O)2R 3 , and -SR 4 Selected from the group consisting of, -R 1 and -R 2 One or only one of these is selected from the group consisting of -H, optionally substituted alkyl, optionally substituted arylalkyl, and optionally substituted heteroarylalkyl. -R 3 -H, optionally substituted alkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, -OR 9 and -N(R 9 Selected from the group consisting of )2, -R 4 This is selected from the group consisting of optionally substituted alkyls, optionally substituted aryls, optionally substituted arylalkyls, optionally substituted heteroaryls, and optionally substituted heteroarylalkyls. Each-R 5These are independently selected from the group consisting of -H, optionally substituted alkyl, optionally substituted alkenylalkyl, optionally substituted alkynylalkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl, and optionally substituted heteroarylalkyl. -R 9 This is selected from the group consisting of -H and optionally substituted alkyl groups, -Y- does not exist, and -X- is either -O- or -S-, or -Y- is -N(Q)CH2- and -X- is -O-, Q is selected from the group consisting of optionally substituted alkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl, and optionally substituted heteroarylalkyl. Depending on the case, -R 1 and -R 2 They may come together to form a ring of 3 to 8 members. Depending on the case, both -R 9 These, together with the nitrogen atoms to which they are bonded, form a heterocyclic ring. Here, -L 1 - is at least one -L 2 - is replaced by -L 1 - is sometimes further replaced.) It belongs to them.

[0433] The term used exclusively in relation to formula (IV) has the following meanings: As used herein, the term "alkyl" includes linear, branched, or cyclic saturated hydrocarbon groups comprising 1 to 8 carbon atoms, or in certain embodiments, 1 to 6 or 1 to 4 carbon atoms.

[0434] The term "alkoxy" encompasses alkyl groups bonded to oxygen, including methoxy, ethoxy, isopropoxy, cyclopropoxy, cyclobutoxy, and similar groups.

[0435] The term "alkenyl" encompasses non-aromatic unsaturated hydrocarbons that contain a carbon-carbon double bond.

[0436] The term "alkynyl" encompasses non-aromatic unsaturated hydrocarbons that have a carbon-carbon triple bond.

[0437] The term "aryl" encompasses aromatic hydrocarbon groups with 6 to 18 carbon atoms, for example, 6 to 10 carbon atoms, and includes groups such as phenyl, naphthyl, and anthracenyl. The term "heteroaryl" encompasses aromatic rings with 3 to 15 carbon atoms containing at least one N, O, or S atom, for example, 3 to 7 carbon atoms containing at least one N, O, or S atom, and includes groups such as pyrrolyl, pyridyl, pyrimidinyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, quinolyl, indolyl, indenyl, and similar groups.

[0438] In some examples, the alkenyl, alkynyl, aryl, or heteroaryl moiety may be coupled to the rest of the molecule via an alkylene bond. In these circumstances, the substituent is called an alkenylalkyl, alkynylalkyl, arylalkyl, or heteroarylalkyl, indicating that the alkylene moiety lies between the alkenyl, alkynyl, aryl, or heteroaryl moiety and the molecule to which the alkenyl, alkynyl, aryl, or heteroaryl is coupled.

[0439] The term "halogen" includes bromo, fluoro, chloro, and iodine.

[0440] The term “heterocyclic ring” refers to a 4-8 membered aromatic or non-aromatic ring containing 3-7 carbon atoms and at least 1 N, O, or S atom. Examples include piperidinyl, piperazinyl, tetrahydropyranyl, pyrrolidine, and tetrahydrofuranyl, as well as the exemplary groups provided for the term “heteroaryl” above.

[0441] If the ring system is optionally substituted, preferred substituents are selected from the group consisting of alkyl, alkenyl, alkynyl, or further rings, each optionally further substituted. Optional substituents on any of the above-mentioned groups include halo, nitro, cyano, -OR, -SR, -NR2, -OCOR, -NRCOR, -COOR, -CONR2, -SOR, -SO2R, -SONR2, and -SO2NR2, where each R is independently alkyl, alkenyl, alkynyl, aryl, or heteroaryl, or two R groups together with the atom to which they are bonded form a ring.

[0442] In certain embodiments, -L of formula (IV) 1 - is one part -L 2 It is replaced with -.

[0443] In certain embodiments, -L of formula (IV) 1 - has not been further replaced.

[0444] In certain embodiments, -L 1 - is disclosed in WO2013 / 036857A1, which is incorporated herein by reference in its entirety. Thus, in certain embodiments, -L 1 - is equation (V): [ka] (In the formula, The dashed line indicates the bond to -D- via the amine functional group of -D-. -R 1 These include optionally substituted C1-C6 linear, branched, or cyclic alkyl groups; optionally substituted aryl groups; optionally substituted heteroaryl groups; alkoxy groups; and -NR 5 Selected from a group consisting of 2, -R 2 This is selected from the group consisting of -H, optionally substituted C1-C6 alkyl, optionally substituted aryl, and optionally substituted heteroaryl. -R 3 This is selected from the group consisting of -H, optionally substituted C1-C6 alkyl, optionally substituted aryl, and optionally substituted heteroaryl. -R 4 This is selected from the group consisting of -H, optionally substituted C1-C6 alkyl, optionally substituted aryl, and optionally substituted heteroaryl. Each-R 5 These are independently selected from the group consisting of -H, optionally substituted C1-C6 alkyl, optionally substituted aryl, and optionally substituted heteroaryl, or, if combined, two -R 5 It can be a cycloalkyl or cycloheteroalkyl, Here, -L 1 - is at least one -L 2 - is replaced by -L 1 - is sometimes further replaced.) It belongs to them.

[0445] The term used exclusively in relation to the expression (V) has the following meanings: "Alkyl," "alkenyl," and "alkynyl" encompass linear, branched, or cyclic hydrocarbon groups of 1 to 8 carbon atoms, 1 to 6 carbon atoms, or 1 to 4 carbon atoms, where alkyl is a saturated hydrocarbon, alkenyl contains one or more carbon-carbon double bonds, and alkynyl contains one or more carbon-carbon triple bonds. Unless otherwise specified, these contain 1 to 6 carbon atoms.

[0446] "Aryl" refers to an aromatic hydrocarbon group containing 6 to 18 carbon atoms, for example, 6 to 10 carbon atoms, such as phenyl, naphthyl, and anthracene. "Heteroaryl" refers to an aromatic ring containing 3 to 15 carbon atoms, for example, 3 to 7 carbon atoms, containing at least one N, O, or S atom, such as pyrrolyl, pyridyl, pyrimidinyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, quinolyl, indolyl, indenyl, and similar groups.

[0447] The term "substituted" refers to an alkyl, alkenyl, alkynyl, aryl, or heteroaryl group that contains one or more substituents in place of one or more hydrogen atoms. Substituents generally include halogens (including F, Cl, Br, and I), lower alkyls (including linear, branched, and cyclic lower alkyls), lower haloalkyls (including fluoroalkyls, chloroalkyls, bromoalkyls, and iodoalkyls), OH, lower alkoxys (including linear, branched, and cyclic lower alkoxys), SH, lower alkylthios (including linear, branched, and cyclic lower alkylthios), aminos, alkylaminos, dialkylaminos, silyls (including alkylsilyls, alkoxysilyls, and arylsilyls), nitros, cyanos, carbonyls, carboxylic acids, carboxylic acid esters, carboxylic acid amides, and aminocarboxyl groups. The following can be selected: bonyl, aminoacyl, carbamate, urea, thiocarbamate, thiourea, ketone, sulfone, sulfonamide, aryl (including phenyl, naphthyl, and anthracenyl), heteroaryl (including 5-membered heteroaryls such as pyrrole, imidazole, furan, thiophene, oxazole, thiazole, isoxazole, isothiazole, thiadiazole, triazole, oxadiazole, and tetrazole, 6-membered heteroaryls such as pyridine, pyrimidine, pyrazine, and condensed heteroaryls such as benzofuran, benzothiophene, benzoxazole, benzimidazole, indole, benzothiazole, benzoisoxazole, and benzoisothiazole).

[0448] In certain embodiments, -L of formula (V) 1 - is one part -L 2 It is replaced with -.

[0449] In certain embodiments, -L of formula (V) 1 - has not been further replaced.

[0450] In certain embodiments, -L 1- is disclosed in U.S. Patent No. 7,585,837 B2, which is incorporated herein by reference in its entirety. Therefore, in certain embodiments, -L 1 - is equation (VI): [ka] (In the formula, The dashed line indicates the bond to -D- via the amine functional group of -D. R 1 and R 2 These are independently hydrogen, alkyl, alkoxy, alkoxyalkyl, aryl, alkalyl, aralkyl, halogen, nitro, -SO3H, -SO2HH 5 Selected from the group consisting of amino, ammonium, carboxyl, PO3H2, and OPO3H2, R 3 , R 4 , and R 5 These are independently selected from the group consisting of hydrogen, alkyl, and aryl. Here, -L 1 - is at least one -L 2 - is replaced by -L 1 - is sometimes further replaced.) It belongs to them.

[0451] Suitable substituents for formula (VI) are alkyl (e.g., C 1-6 Alkyl), alkenyl (e.g., C 2-6 Alkenyl), Alkinyl (for example, C 2-6 The moiety is an alkynyl, aryl (e.g., phenyl), heteroalkyl, heteroalkenyl, heteroalkynyl, heteroaryl (e.g., an aromatic 4-7 membered heterocycle), or halogen moiety.

[0452] The term used exclusively in relation to formula (VI) has the following meanings: The terms "alkyl," "alkoxy," "alkoxyalkyl," "aryl," "alkalil," and "aralkyl" refer to alkyl groups with 1 to 8 carbon atoms, for example, 1 to 4 carbon atoms, such as methyl, ethyl, propyl, isopropyl, and butyl, and aryl groups with 6 to 10 carbon atoms, such as phenyl and naphthyl. The term "halogen" includes bromo, fluoro, chloro, and iodine.

[0453] In certain embodiments, -L of formula (VI) 1 - is one part -L 2 It is replaced with -.

[0454] In certain embodiments, -L of formula (VI) 1 - has not been further replaced.

[0455] -L 1 Further preferred embodiments of - are disclosed in WO2002 / 089789A1, which is incorporated herein by reference in its entirety. Therefore, preferred portion - L 1 - is equation (VII): [ka] (In the formula, The dashed line indicates the bond to -D- via the amine functional group of -D-. L1 is a bifunctional bonding group, Y1 and Y2 are independently O, S, or NR 7 And, R 2 , R 3 , R 4 , R 5 , R 6 and R 7 These are, independently, hydrogen and C 1-6 Alkyl, C 3-12 Branched alkyl, C 3-8 Cycloalkyl, C 1-6 Substituting alkyl, C 3-8 Substituted cycloalkyl, aryl, substituted aryl, aralkyl, C 1-6 Heteroalkyl, substituted C 1-6Heteroalkyl, C 1-6 Alkoxy, phenoxy, and C 1-6 Selected from the group consisting of heteroalkoxys, When Ar is included in formula (VII), it is the part that forms a polysubstituted aromatic hydrocarbon or a polysubstituted heterocyclic group. X is a chemical bond, or a portion that is actively transported to the target cell, a hydrophobic portion, or a combination thereof. y is either 0 or 1. Here, -L 1 - is at least one -L 2 - is replaced by -L 1 - is sometimes further replaced.) It belongs to them.

[0456] The term used exclusively in relation to formula (VII) has the following meanings: The term "alkyl" refers to, for example, linear, branched, or substituted C atoms. 1-12 Alkyl, for example, alkoxy, C 3-8 It will be understood that this includes cycloalkyl or substituted cycloalkyl groups, etc.

[0457] The term "substituted" should be understood to include adding one or more different atoms to one or more atoms contained in a functional group or compound, or replacing one or more atoms contained in a functional group or compound with one or more different atoms.

[0458] Substitutive alkyls include carboxyalkyl, aminoalkyl, dialkylamino, hydroxyalkyl, and mercaptoalkyl; substituted cycloalkyls include parts such as 4-chlorocyclohexyl; aryls include parts such as naphthyl; substituted aryls include parts such as 3-bromophenyl; aralkyls include parts such as toluyl; heteroalkyls include parts such as ethylthiophene; substituted heteroalkyls include parts such as 3-methoxythiophene; alkoxys include parts such as methoxy; and phenoxys include parts such as 3-nitrophenoxy. Halos are understood to include fluoro, chloro, iodo, and bromo.

[0459] In certain embodiments, -L of formula (VII) 1 - is one part -L 2 It is replaced with -.

[0460] In certain embodiments, -L of formula (VII) 1 - has not been further replaced.

[0461] In certain embodiments, -L 1 - is a substructure of equation (VIII) [ka] (In the formula, The dashed line with an asterisk indicates the bond of -D- to nitrogen via an amide bond. Dashed lines without a mark are -L 1 - indicates the connection to the remainder, Here, -L 1 - is at least one -L 2 - is replaced by -L 1 - is sometimes further replaced.) Includes.

[0462] In certain embodiments, the -L of formula (VIII) 1 - is one part -L 2 It is replaced with -.

[0463] In certain embodiments, the -L of formula (VIII) 1 - has not been further replaced.

[0464] In certain embodiments, -L 1 - is a substructure of equation (IX) [ka] (In the formula, The dashed lines with asterisks indicate the bonding of -D- to nitrogen via a carbamate bond. Dashed lines without a mark are -L 1 - Indicates connection to the remainder Here, -L 1 - is at least one -L 2 - is replaced by -L 1 - is sometimes further replaced.) Includes.

[0465] In certain embodiments, -L of formula (IX) 1 - is one part -L 2 It is replaced with -.

[0466] In certain embodiments, -L of formula (IX) 1 - has not been further replaced.

[0467] In certain embodiments, -L 1 - has the structure disclosed in WO2020 / 206358 A1. Therefore, in certain embodiments, part -L 1 - is equation (X): [ka] (In the formula, Unmarked dashed lines indicate connections to -D-. The dashed line with an asterisk indicates -L 2 - indicates binding to n is an integer selected from the group consisting of 0, 1, 2, 3, 4, 5, and 6. -R 1 and -R 2 These are independently electron-withdrawing groups, alkyl groups, or -H groups, and -R 1 or -R 2 At least one of them is an electron-withdrawing group, Each-R 4 These are independently C1-C3 alkyl groups or two -R groups. 4 These, together with the carbon atoms to which they are bonded, form a ring with 3 to 6 members. -Y- is absent if -D- is a drug moiety bonded via an amine, or -Y- is -N(R) if -D- is a drug moiety bonded via a phenol, alcohol, thiol, thiophenol, imidazole, or non-basic amine. 6 )CH2-, where -R 6 (These are, in some cases, substituted C1-C6 alkyl groups, in some cases, substituted aryl groups, or in some cases, substituted heteroaryl groups.) It belongs to them.

[0468] In certain embodiments, n in formula (X) is an integer selected from 1, 2, 3, 4, 5, and 6. In certain embodiments, n in formula (X) is an integer selected from 1, 2, and 3. In certain embodiments, n in formula (X) is an integer from 0, 1, 2, and 3. In certain embodiments, n in formula (X) is 1. In certain embodiments, n in formula (X) is 2. In certain embodiments, n in formula (X) is 3.

[0469] In certain embodiments, -R of formula (X) 1 and -R 2 The electron-withdrawing groups are -CN;-NO2; optionally substituted aryl; optionally substituted heteroaryl; optionally substituted alkenyl; optionally substituted alkynyl;-COR 3 -SOR 3 , or -SO2R 3 (In the formula, -R 3-H, optionally substituted alkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, -OR 8 or -NR 8 2, and each -R 8 These are independently -H or optionally substituted alkyl, or both -R 8 The groups, together with the nitrogen atoms to which they are bonded, form a heterocyclic ring; or -SR 9 (In the formula, -R 9 (which is optionally substituted alkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl, or optionally substituted heteroarylalkyl) is selected from the group consisting of these.

[0470] In certain embodiments, -R of formula (X) 1 and -R 2 The electron-withdrawing group is -CN. In certain embodiments, -R of formula (X) 1 and -R 2 The electron-withdrawing group is -NO2. In certain embodiments, -R of formula (X) 1 and -R 2 The electron-withdrawing group is an optionally substituted aryl group containing 6 to 10 carbon atoms. In certain embodiments, the -R of formula (X) 1 and -R 2 The electron-withdrawing group is optionally substituted phenyl, naphthyl, or anthracenyl. In certain embodiments, -R of formula (X) 1 and -R 2 The electron-withdrawing group is an optionally substituted heteroaryl containing 3 to 7 carbon atoms and at least one N, O, or S atom. In certain embodiments, the -R of formula (X) 1 and -R 2The electron-withdrawing group is optionally substituted pyrrolyl, pyridyl, pyrimidinyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, quinolyl, indolyl, or indenyl. In certain embodiments, -R of formula (X) 1 and -R 2 The electron-withdrawing group is an optionally substituted alkenyl containing 2 to 20 carbon atoms. In certain embodiments, the -R of formula (X) 1 and -R 2 The electron-withdrawing group is an optionally substituted alkynyl containing 2 to 20 carbon atoms. In certain embodiments, the -R of formula (X) 1 and -R 2 The electron-withdrawing group is -COR 3 -SOR 3 , or -SO2R 3 And here, -R 3 -H, optionally substituted alkyl containing 1 to 20 carbon atoms, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, -OR 8 or -NR 8 2, and each -R 8 These are either alkyl groups independently substituted with -H or containing 1 to 20 carbon atoms, or both -R groups. 8 The groups, together with the nitrogen atoms to which they are bonded, form a heterocyclic ring. In certain embodiments, the -R of formula (X) 1 and -R 2 The electron-withdrawing group is -SR 9 And here, -R 9 This is an optionally substituted alkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl, or optionally substituted heteroarylalkyl, which contains 1 to 20 carbon atoms.

[0471] In certain embodiments, -R of formula (X) 1 or -R 2At least one of them is -CN, -SOR 3 or -SO2R 3 In certain embodiments, -R of formula (X) 1 and -R 2 At least one of them is -CN or -SO2R 3 In certain embodiments, -R of formula (X) 1 and -R 2 At least one of them is -CN or -SO2R 3 And, -R 3 This may be a substituted alkyl, may be a substituted aryl, or -NR 8 2. In certain embodiments, -R of formula (X) 1 and -R 2 At least one of them is -CN, -SO2N(CH3)2, -SO2CH3, phenyl substituted with -SO2, phenyl substituted with -SO2 and -Cl, -SO2N(CH2CH2)2O, -SO2CH(CH3)2, -SO2N(CH3)(CH2CH3), or -SO2N(CH2CH2OCH3)2.

[0472] In a particular embodiment, each -R of formula (X) 4 These are independently C1-C3 alkyl groups. In certain embodiments, both -R 4 It is methyl.

[0473] In certain embodiments, -Y- in formula (X) does not exist. In certain embodiments, -Y- in formula (X) is -N(R 6 It is CH2-.

[0474] In certain embodiments, -L 1 - means that n in the expression is 1, -R 1 -CN and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - means that n in the expression is 1, -R 1 is -SO2N(CH3)2, and -R 2 -H and -R4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - means that n in the expression is 1, -R 1 It is SO2CH3, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - means that n in the expression is 1, -R 1 is -SO2N(CH2CH2)2CHCH3, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - means that n in the expression is 1, -R 1 However, it is a phenyl compound substituted with -SO2, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - means that n in the expression is 1, -R 1 However, it is a phenyl substituted with -SO2 and -Cl, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - means that n in the expression is 1, -R 1 is -SO2N(CH2CH2)2O, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - means that n in the expression is 1, -R 1 is -SO2CH(CH3)2, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - means that n in the expression is 1, -R 1 is -SO2N(CH3)(CH2CH3), and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - means that n in the expression is 1, -R1 is -SO2N(CH2CH2OCH3)2, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - means that n in the expression is 1, -R 1 However, it is a phenyl substituted with -SO2 and -CH3, and -R 2 -H and -R 4 This is the one in equation (X) where -CH3 is present.

[0475] In certain embodiments, -L 1 - is where n in the formula is 2, and -R 1 -CN and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 2, and -R 1 is -SO2N(CH3)2, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 2, and -R 1 It is SO2CH3, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 2, and -R 1 is -SO2N(CH2CH2)2CHCH3, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 2, and -R 1 However, it is a phenyl compound substituted with -SO2, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 2, and -R 1 However, it is a phenyl substituted with -SO2 and -Cl, and -R2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 2, and -R 1 is -SO2N(CH2CH2)2O, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 2, and -R 1 is -SO2CH(CH3)2, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 2, and -R 1 is -SO2N(CH3)(CH2CH3), and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 2, and -R 1 is -SO2N(CH2CH2OCH3)2, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 2, and -R 1 However, it is a phenyl substituted with -SO2 and -CH3, and -R 2 -H and -R 4 This is the one in equation (X) where -CH3 is present.

[0476] In certain embodiments, -L 1 - is where n in the formula is 3, and -R 1 -CN and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 3, and -R 1 is -SO2N(CH3)2, and -R 2 -H and -R 4It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 3, and -R 1 It is SO2CH3, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 3, and -R 1 is -SO2N(CH2CH2)2CHCH3, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 3, and -R 1 However, it is a phenyl compound substituted with -SO2, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 3, and -R 1 However, it is a phenyl substituted with -SO2 and -Cl, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 3, and -R 1 is -SO2N(CH2CH2)2O, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 3, and -R 1 is -SO2CH(CH3)2, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 3, and -R 1 is -SO2N(CH3)(CH2CH3), and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 3, and -R 1is -SO2N(CH2CH2OCH3)2, and -R 2 -H and -R 4 It is of formula (X), where is -CH3. In a particular embodiment, -L 1 - is where n in the formula is 3, and -R 1 However, it is a phenyl substituted with -SO2 and -CH3, and -R 2 -H and -R 4 This is the one in equation (X) where -CH3 is present.

[0477] The term used exclusively in relation to formula (X) has the following meanings: The term "alkyl" refers to a linear, branched, or cyclic saturated hydrocarbon group having 1 to 20, 1 to 12, 1 to 8, 1 to 6, or 1 to 4 carbon atoms. In certain embodiments, alkyl groups are linear or branched. Examples of linear or branched alkyl groups include methyl, ethyl, n-propyl, isopropyl, n-butyl, t-butyl, isobutyl, sec-butyl, n-pentyl, n-hexyl, n-heptyl, n-octyl, n-nonyl, and n-decyl. In certain embodiments, alkyl groups are cyclic. Examples of cyclic alkyl groups include cyclopropyl, cyclobutyl, cyclopentyl, cyclopentadienyl, and cyclohexyl.

[0478] The term "alkoxy" refers to an alkyl group bonded to oxygen, such as methoxy, ethoxy, isopropoxy, cyclopropoxy, and cyclobutoxy.

[0479] The term "alkenyl" refers to a non-aromatic unsaturated hydrocarbon having a carbon-carbon double bond and 2-20, 2-12, 2-8, 2-6, or 2-4 carbon atoms.

[0480] The term "alkynyl" refers to a non-aromatic unsaturated hydrocarbon having a carbon-carbon triple bond and 2-20, 2-12, 2-8, 2-6, or 2-4 carbon atoms.

[0481] The term "aryl" refers to an aromatic hydrocarbon group having 6 to 18 carbon atoms, preferably 6 to 10 carbon atoms, such as phenyl, naphthyl, and anthracenyl groups. The term "heteroaryl" refers to an aromatic ring having 3 to 15 carbon atoms, preferably 3 to 7 carbon atoms, including at least one N, O, or S atom, such as pyrrolyl, pyridyl, pyrimidinyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, quinolyl, indolyl, and indenyl groups.

[0482] In certain embodiments, an alkenyl, alkynyl, aryl, or heteroaryl moiety may be coupled to the remainder of the molecule by an alkyl bond. Under these circumstances, the substituent is referred to as an alkenylalkyl, alkynylalkyl, arylalkyl, or heteroarylalkyl, indicating that the alkylene moiety lies between the alkenyl, alkynyl, aryl, or heteroaryl moiety and the molecule to which the alkenyl, alkynyl, aryl, or heteroaryl is coupled.

[0483] The term "halogen" refers to bromo, fluoro, chloro, and iodine.

[0484] The term “heterocyclic ring” or “heterocyclyl” refers to a 3- to 15-membered aromatic or non-aromatic ring containing at least one N, O, or S atom. Examples include piperidinyl, piperazinyl, tetrahydropyranyl, pyrrolidine, and tetrahydrofuranyl, as well as exemplary groups provided for the term “heteroaryl” above. In certain embodiments, the heterocyclic ring or heterocyclyl is non-aromatic. In certain embodiments, the heterocyclic ring or heterocyclyl is aromatic.

[0485] The term "optionally substituted" means that the group may be unsubstituted, or may be substituted with one or more substituents (e.g., 1, 2, 3, 4, or 5) that may be the same or different. Examples of substituents include alkyl, alkenyl, alkynyl, halogen, -CN, and -OR. aa , -SR aa , -NR aa R bb -NO2, -C=NH(OR aa ), -C(O)R aa -OC(O)R aa , -C(O)OR aa -C(O)NR aa R bb -OC(O)NR aa R bb , -NR aa C(O)R bb , -NR aa C(O)OR bb ,-S(O)R aa -S(O)2R aa , -NR aa S(O)R bb -C(O)NR aa S(O)R bb , -NR aa S(O)2R bb -C(O)NR aa S(O)2R bb -S(O)NR aa R bb -S(O)2NR aa R bb , -P(O)(OR aa )(OR bb Examples include heterocyclyl, heteroaryl, or aryl, where alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, heteroaryl, and aryl are each independently -R cc It is sometimes replaced by -R aa and -R bb Each of these is independently either -H, alkyl, alkenyl, alkynyl, heterocyclyl, heteroaryl, or aryl, or -R aa and -R bbThese, together with the nitrogen atom to which they are bonded, form a heterocycline, which is optionally substituted with alkyl, alkenyl, alkynyl, halogen, hydroxyl, alkoxy, or -CN, where each -R cc These are independently alkyl, alkenyl, alkynyl, halogen, heterocyclyl, heteroaryl, aryl, -CN, or -NO2.

[0486] In certain embodiments, -L 1 - has the structure disclosed in formula I of WO2021 / 242756 A1. Therefore, in certain embodiments, part -L 1 - is equation (XIIa): [ka] (In the formula, Unmarked dashed lines indicate connections to -D-. The dashed line with an asterisk indicates -L 2 - indicates binding to -R 2 , -R 4 and -R 8 These are independently -H or C 1-4 Selected from the group consisting of alkyl groups, -R 3 is C 1-4 Alkyl or -R 3 and -R 4 These, together with the atoms to which they are bonded, form a 5- or 6-membered heterocyclic ring. -R 5 It is NH2, However, -R 4 and -R 3 However, when they combine with the atoms to which they are bonded to form a 5- or 6-membered heterocyclic ring (from), -R 2 is not -H, Here, -L in equation (XIIa) 1 (- is sometimes replaced) It belongs to them.

[0487] In certain embodiments, -R of formula (XIIa) 4 and -R 8 Both are -H.

[0488] In certain embodiments, -R 3 is methyl. In certain embodiments, -R 3 It is -H.

[0489] In certain embodiments, -R 2 It is -H.

[0490] In certain embodiments, -L 1 - is equation (XIIa-i) [ka] (In the formula, Unmarked dashed lines indicate connections to -D-. The dashed line with an asterisk indicates -L 2 (Indicates a connection to -) It belongs to them.

[0491] In certain embodiments, -L 1 - is equation (XIIa-ii) [ka] (In the formula, Unmarked dashed lines indicate connections to -D-. The dashed line with an asterisk indicates -L 2 (Indicates a connection to -) It belongs to them.

[0492] In certain embodiments, -L 1 - is equation (XIIa-iii) [ka] (In the formula, Unmarked dashed lines indicate connections to -D-. The dashed line with an asterisk indicates -L 2(Indicates a connection to -) It belongs to them.

[0493] In certain embodiments, -L 1 - has the structure disclosed in Formula II of WO2022 / 096636 A1. Therefore, in certain embodiments, part -L 1 - is equation (XIIb): [ka] (In the formula, Unmarked dashed lines indicate connections to -D-. The dashed line with an asterisk indicates -L 2 (Indicates a connection to -) It belongs to them.

[0494] In certain embodiments, -L 2 - does not exist.

[0495] In certain embodiments, -L 2 - is especially suitable for -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O)2N(R y1 )-,-S(O)N(R y1 )-, -S(O)2-, -S(O)-, -N(R y1 )S(O)2N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 A spacer portion selected from the group consisting of alkynnyls, where -T-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y3 )-,-S(O)2N(R y3 )-,-S(O)N(R y3 )-, -S(O)2-, -S(O)-, -N(R y3 )S(O)2N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3 )(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(R y3 )- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a These are -H, -T, and C, which are independent of each other. 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynyls, where -T, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y4 )-,-S(O)2N(R y4 )-,-S(O)N(R y4 )-, -S(O)2-, -S(O)-, -N(R y4 )S(O)2N(R y4a )-, -S-, -N(R y4 )-, -OC(OR y4 )(R y4a )-,-N(R y4 )C(O)N(R y4a )-, and -OC(O)N(R y4 )- may intersect with one or more groups selected from the group consisting of, Each T independently consists of phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C. 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, where each T is independently one or more identical or different -R y2 It is sometimes replaced by, Each-R y2 These are, independently, halogen, -CN, oxo (=O), and -COOR. y5 , -OR y5 , -C(O)R y5 ,-C(O)N(R y5 R y5a ), -S(O)2N(R y5 R y5a ), -S(O)N(R y5 R y5a ), -S(O)2R y5 ,-S(O)R y5 , -N(R y5 )S(O)2N(R y5a R y5b ), -SR y5 , -N(R y5 R y5a ), -NO2, -OC(O)R y5 , -N(R y5 )C(O)R y5a , -N(R y5 )S(O)2R y5a , -N(R y5 )S(O)R y5a , -N(R y5 )C(O)OR y5a , -N(R y5 )C(O)N(R y5a R y5b ), -OC(O)N(R y5 R y5a ), and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each-R y3 , -R y3a , -R y4 , -R y4a , -Ry5 , -R y5a and -R y5b These are independently -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl atoms are sometimes substituted with one or more halogens, either the same or different.

[0496] In certain embodiments, -L 2 - stands for -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O)2N(R y1 )-,-S(O)N(R y1 )-, -S(O)2-, -S(O)-, -N(R y1 )S(O)2N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from alkinyl, where -T-, C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-20 Alkyl, C 2-20 Alkenyl and C 2-20 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y3 )-,-S(O)2N(R y3 )-,-S(O)N(R y3 )-, -S(O)2-, -S(O)-, -N(R y3 )S(O)2N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3 )(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(Ry3 )- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a These are -H, -T, and C, which are independent of each other. 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Selected from the group consisting of alkynyls, where -T, C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y4 )-,-S(O)2N(R y4 )-,-S(O)N(R y4 )-, -S(O)2-, -S(O)-, -N(R y4 )S(O)2N(R y4a )-, -S-, -N(R y4 )-, -OC(OR y4 )(R y4a )-,-N(R y4 )C(O)N(R y4a )-, and -OC(O)N(R y4 )- may intersect with one or more groups selected from the group consisting of, Each T independently consists of phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C. 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, where each T is independently one or more identical or different -R y2 It is sometimes replaced by, -R y2 These are halogen, -CN, oxo (=O), and -COOR. y5 , -OR y5 , -C(O)R y5 ,-C(O)N(R y5 Ry5a ), -S(O)2N(R y5 R y5a ), -S(O)N(R y5 R y5a ), -S(O)2R y5 ,-S(O)R y5 , -N(R y5 )S(O)2N(R y5a R y5b ), -SR y5 , -N(R y5 R y5a ), -NO2, -OC(O)R y5 , -N(R y5 )C(O)R y5a , -N(R y5 )S(O)2R y5a , -N(R y5 )S(O)R y5a , -N(R y5 )C(O)OR y5a , -N(R y5 )C(O)N(R y5a R y5b ), -OC(O)N(R y5 R y5a ), and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each-R y3 , -R y3a , -R y4 , -R y4a , -R y5 , -R y5a and -R y5b These are, independently of each other, -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl atoms are sometimes substituted with one or more halogens, either the same or different.

[0497] In certain embodiments, -L 2 - stands for -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O)2N(R y1 )-,-S(O)N(R y1 )-, -S(O)2-, -S(O)-, -N(Ry1 )S(O)2N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y3 )-,-S(O)2N(R y3 )-,-S(O)N(R y3 )-, -S(O)2-, -S(O)-, -N(R y3 )S(O)2N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3 )(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(R y3 )- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a These are independently -H, -T, and C 1-10 Alkyl, C 2-10 Alkenyl and C 2-10 Selected from the group consisting of alkynnyls, Each T independently consists of phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C. 3-10Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, Each-R y2 These are, independently, halogen and C 1-6 Selected from the group consisting of alkyl groups, Each-R y3 , -R y3a , -R y4 , -R y4a , -R y5 , -R y5a and -R y5b These are, independently of each other, -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl atoms are sometimes substituted with one or more halogens, either the same or different.

[0498] In certain embodiments, -L 2 - are -O-, -S-, -T- and -C(O)N(R y1 )- where one or more elements selected independently of C may interrupt 1-20 It is an alkyl chain, and this C 1-20 The alkyl chain consists of -OH, -T, and -C(O)N(R) y6 R y6a ) is optionally substituted with one or more elements independently selected from, where -R y1 , -R y6 , -R y6a H and C are independent of each other. 1-4 Selected from the group consisting of alkyl groups, T is phenyl, naphthyl, indenyl, indanyl, tetralinyl, C 3-10 The group is selected from cycloalkyls, 3-10 member heterocyclils, 8-11 member heterobicyclils, 8-30 member carbopolycyclils, and 8-30 member heteropolycyclils.

[0499] In certain embodiments, -L 2 - has a molecular weight in the range of 14 g / mol to 750 g / mol.

[0500] In certain embodiments, -L 2 - includes the portion selected from the following: [ka] TIFF2026509252000231.tif161169 (in the formula, -R and -R a (These are independently selected from the group consisting of -H, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-methylbutyl, 2,2-dimethylpropyl, n-hexyl, 2-methylpentyl, 3-methylpentyl, 2,2-dimethylbutyl, 2,3-dimethylbutyl, and 3,3-dimethylpropyl).

[0501] In certain embodiments, -L 2 - has a chain length of 1 to 20 atoms. In certain embodiments, -L 2 - has a chain length of 2 to 10 atoms.

[0502] In certain embodiments, -L 2 - has a chain length of at least 35 atoms. In certain embodiments, -L 2 - has a chain length of at least 50 atoms. In certain embodiments, -L 2 - has a chain length of at least 75 atoms. In certain embodiments, -L 2 - has a chain length of at least 100 atoms. In certain embodiments, -L 2 - has a chain length of at least 150 atoms. In certain embodiments, -L 2 - has a chain length of at least 200 atoms. In certain embodiments, -L 2 - has a chain length of at least 250 atoms. In certain embodiments, -L 2 - has a chain length of at least 300 atoms. In certain embodiments, -L 2 - has a chain length of up to 3000 atoms. In certain embodiments, -L 2- has a chain length of up to 2500 atoms. In certain embodiments, -L 2 - has a chain length of up to 2000 atoms. In certain embodiments, -L 2 - has a chain length of up to 1500 atoms. In certain embodiments, -L 2 - has a chain length in the range of 35 to 3000 atoms. In certain embodiments, -L 2 - has a chain length in the range of 50 to 2500 atoms. In certain embodiments, -L 2 - has a chain length in the range of 75 to 2000 atoms. In certain embodiments, -L 2 - has a chain length in the range of 100 to 1500 atoms. In certain embodiments, -L 2 - has a chain length ranging from 125 to 1000 atoms.

[0503] In certain embodiments, -L 2 - is equation (XI) [ka] (In the formula, Dashed lines without a mark are -L 1 - indicates binding to The dashed line with an asterisk indicates a bond to at least one polymer moiety. h is an integer selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. It belongs to them.

[0504] In certain embodiments, -L 2 - is from formula (XI), where h is 1. In certain embodiments, -L 2 - is from formula (XI), where h is 2. In certain embodiments, -L 2 - is from formula (XI), where h is 3. In certain embodiments, -L 2 - is from formula (XI), where h is 4. In certain embodiments, -L 2- is from formula (XI), and h is 5. In certain embodiments, -L 2 - is from formula (XI), where h is 6. In certain embodiments, -L 2 - is from formula (XI), where h is 7. In certain embodiments, -L 2 - is from formula (XI), and h is 8. In certain embodiments, -L 2 - is from formula (XI), and h is 9. In certain embodiments, -L 2 - is from formula (XI), where h is 10. In certain embodiments, -L 2 - is from formula (XI), where h is 11. In certain embodiments, -L 2 - is from formula (XI), where h is 12. In certain embodiments, -L 2 - is from formula (XI), where h is 13. In certain embodiments, -L 2 - is from formula (XI), where h is 14. In certain embodiments, -L 2 - is from equation (XI), and h is 15.

[0505] In certain embodiments, -L 2 - has a molecular weight of at least 450 Da. In certain embodiments, -L 2 - has a mol...

Claims

1. A compound or a pharmaceutically acceptable salt thereof comprising at least one polymer moiety in which at least two parts of formula (I) are conjugated and / or at least one part of formula (I') is conjugated, wherein formulas (I) and (I') are 【Chemistry 1】 (In the formula, Each-L 2 - is either an independent spacer part or does not exist. Each-L 1 - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each-L 1' - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each -D- is an independent drug portion. Each -AB is an albumin-binding moiety independently. Each a is an integer selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. A compound or a pharmaceutically acceptable salt thereof.

2. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein at least one polymer portion of the compound of the present invention is a linear polymer portion -P-.

3. The compound is of formula (Ia) or (I-a') 【Chemistry 2】 (In the formula, Each-L 2 - is either an independent spacer part or does not exist. Each-L 1 - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each-L 1' - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each -D- is an independent drug portion. Each -AB is an albumin-binding moiety independently. -P- is the polymer part, Each a is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. A compound according to claim 1 or 2, or a pharmaceutically acceptable salt thereof.

4. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein at least one polymer portion of the compound of the present invention is a multi-arm polymer portion.

5. The compound includes at least one branch point B, which is conjugated by at least two parts of formula (Ib) and / or at least one part of formula (Ib'), and formulas (Ib) and (Ib') are 【Transformation 3】 (In the formula, The dashed line indicates the connection to branch point B. -A- is the polymer part, Each-L 2 - is either an independent spacer part or does not exist. Each-L 1 - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each -L 1' - is, independently, a linker moiety that is covalently and reversibly conjugated to -D- Each -D- is an independent drug portion. Each -AB is an albumin-binding moiety independently. Each a is an integer independently selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. The compound according to claim 1 or 4, or a pharmaceutically acceptable salt thereof.

6. The compound is given by formula (I-b4) 【Chemistry 4】 (In the formula, -X 4 -, -X 5 -, -X 6 - are independent of each other: -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O) 2 N(R y1 )-,-S(O)N(R y1 )-,-S(O) 2 -, -S(O)-, -N(R y1 )S(O) 2 N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynnyls, where -T-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y3 )-,-S(O) 2 N(R y3 )-,-S(O)N(R y3 )-,-S(O) 2 -, -S(O)-, -N(R y3 )S(O) 2 N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3 )(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(R y3 )- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a These are -H, -T, and C, which are independent of each other. 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynyls, where -T, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y4 )-,-S(O) 2 N(R y4 )-,-S(O)N(R y4 )-,-S(O) 2 -, -S(O)-, -N(R y4 )S(O) 2 N(R y4a )-, -S-, -N(R y4 )-, -OC(OR y4 )(R y4a )-,-N(R y4 )C(O)N(R y4a )-, and -OC(O)N(R y4 )- may intersect with one or more groups selected from the group consisting of, Each T independently consists of phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C. 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, where each T is independently one or more identical or different -R y2 It is sometimes replaced by, Each -R y2 is independently halogen, -CN, oxo(=O), -COOR y5 , -OR y5 , -C(O)R y5 , -C(O)N(R y5 R y5a ), -S(O) 2 N(R y5 R y5a ), -S(O)N(R y5 R y5a ), -S(O) 2 R y5 , -S(O)R y5 , -N(R y5 )S(O) 2 N(R y5a R y5b ), -SR y5 , -N(R y5 R y5a ), -NO 2 , -OC(O)R y5 , -N(R y5 )C(O)R y5a , -N(R y5 )S(O) 2 R y5a , -N(R y5 ​​​​​​​​​​​​​​​​​​​​​ Each-R y3 ,-R y3a ,-R y4 ,-R y4a ,-R y5 ,-R y5a and -R y5b These are independently -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each -A- is a polymer portion, Each-L 2 - is either an independent spacer part or does not exist. Each-L 1 - is a linker portion that is independently and covalently and reversibly conjugated to -D-. Each -D- is an independent drug portion. Each -AB is an independently albumin-binding moiety. A compound according to any one of claims 1, 4, or 5, or a pharmaceutically acceptable salt thereof.

7. -L 1 -But equation (II): 【Transformation 5】 (In the formula, The dashed line indicates the bond of -D- to nitrogen, hydroxyl, or thiol. -X- is -C(R 4 R 4a )-,-N(R 4 )-, -O-, -C(R 4 R 4a )-C(R 5 R 5a )-,-C(R 5 R 5a )-C(R 4 R 4a )-,-C(R 4 R 4a )-N(R 6 )-,-N(R 6 )-C(R 4 R 4a )-,-C(R 4 R 4a )-O-, -OC(R 4 R 4a )-, and -C(R 7 R 7a Selected from the group consisting of )-, X 1 It is selected from the group consisting of C and S(O), -X 2 - is -C(R 8 R 8a )-, and -C(R 8 R 8a )-C(R 9 R 9a Selected from the group consisting of )-, =X 3 It is selected from the group consisting of =O, =S, and =N-CN, -R 1 ,-R 1a ,-R 2 ,-R 2a ,-R 4 ,-R 4a ,-R 5 ,-R 5a ,-R 6 ,-R 8 ,-R 8a ,-R 9 , and -R 9a These are independently -H and C 1-6 Selected from the group consisting of alkyl groups, -R 3 and -R 3a These are independently -H and C 1-6 Selected from the group consisting of alkyl, except -R 3 ,-R 3a If one or both of them are not -H, then they are SP to the N to which they are bonded. 3 Bonded by hybrid carbon atoms, -R 7 is -N(R 10 R 10a ), and -NR 10 -(C=O)-R 11 Selected from the group consisting of, -R 7a ,-R 10 ,-R 10a , and -R 11 These are, independently of each other, -H and C 1-6 Selected from the group consisting of alkyl groups, Depending on the circumstances, Pair-R 1a / -R 4a ,-R 1a / -R 5a ,-R 1a / -R 7a ,-R 4a / -R 5a , and -R 8a / -R 9a One or more of them form a chemical bond, Depending on the circumstances, Pair-R 1 / -R 1a ,-R 2 / -R 2a ,-R 4 / -R 4a ,-R 5 / -R 5a ,-R 8 / -R 8a , and -R 9 / -R 9a One or more of them, together with the atom they are bonded to, C 3-10 Forming a cycloalkyl or 3-10 membered heterocycline, Depending on the circumstances, Pair-R 1 / -R 4 ,-R 1 / -R 5 ,-R 1 / -R 6 ,-R 1 / -R 7a ,-R 4 / -R 5 ,-R 4 / -R 6 ,-R 8 / -R 9 , and -R 2 / -R 3 One or more of these, together with the atoms to which they are bonded, form ring A. Depending on the case, R 3 / R 3a These, together with the nitrogen atoms to which they are bonded, form a heterocycle of 3 to 10 members. A is phenyl, naphthyl, indenyl, indanyl, tetralinyl, C 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclyls, and 8-11 membered heterobicyclyls, -L 1 - is at least one -L 2 - is replaced by -L 1 - is sometimes further substituted, except that the hydrogen with an asterisk in formula (II) is -L 2 -or not substituted by a substituent) A compound according to any one of claims 1 to 6, or a pharmaceutically acceptable salt thereof.

8. -L 1 -but, equation (IIa) 【Transformation 6】 (In the formula, The dashed line with an asterisk indicates the bond to nitrogen of -D-. Dashed lines without a mark are -L 2 (Indicates a connection to -) A compound according to any one of claims 1 to 7 or a pharmaceutically acceptable salt thereof.

9. -L 1 -But, equation (IIab) 【Transformation 7】 (In the formula, The dashed line with an asterisk indicates the bond to nitrogen of -D-. Dashed lines without a mark are -L 2 (Indicates a connection to -) A compound according to any one of claims 1 to 7 or a pharmaceutically acceptable salt thereof.

10. -L 2 - is -T-, -C(O)O-, -O-, -C(O)-, -C(O)N(R y1 )-,-S(O) 2 N(R y1 )-,-S(O)N(R y1 )-,-S(O) 2 -, -S(O)-, -N(R y1 )S(O) 2 N(R y1a )-, -S-, -N(R y1 )-, -OC(OR y1 )(R y1a )-,-N(R y1 )C(O)N(R y1a )-,-OC(O)N(R y1 )-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 A spacer portion selected from the group consisting of alkynnyls, where -T-, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y3 )-,-S(O) 2 N(R y3 )-,-S(O)N(R y3 )-,-S(O) 2 -, -S(O)-, -N(R y3 )S(O) 2 N(R y3a )-, -S-, -N(R y3 )-, -OC(OR y3 )(R y3a )-,-N(R y3 )C(O)N(R y3a )-, and -OC(O)N(R y3 )- may intersect with one or more groups selected from the group consisting of, -R y1 and -R y1a However, -H, -T, C are independent of each other. 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Selected from the group consisting of alkynyls, where -T, C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyl has one or more -Rs, which may be the same or different. y2 In some cases, it is replaced by C 1-50 Alkyl, C 2-50 Alkenyl and C 2-50 Alkinyls include -T-, -C(O)O-, -O-, -C(O)-, and -C(O)N(R) y4 )-,-S(O) 2 N(R y4 )-,-S(O)N(R y4 )-,-S(O) 2 -, -S(O)-, -N(R y4 )S(O) 2 N(R y4a )-, -S-, -N(R y4 )-, -OC(OR y4 )(R y4a )-,-N(R y4 )C(O)N(R y4a )-, and -OC(O)N(R y4 )- may intersect with one or more groups selected from the group consisting of, Each T independently comprises phenyl, naphthyl, indenyl, indanyl, tetralinyl, and C. 3-10 Selected from the group consisting of cycloalkyls, 3-10 membered heterocyclils, 8-11 membered heterobicyclils, 8-30 membered carbopolycyclils, and 8-30 membered heteropolycyclils, where each T is independently one or more identical or different -R y2 It is sometimes replaced by, Each-R y2 However, independently, halogen, -CN, oxo (=O), -COOR y5 , -OR y5 , -C(O)R y5 ,-C(O)N(R y5 R y5a ), -S(O) 2 N(R y5 R y5a ), -S(O)N(R y5 R y5a ), -S(O) 2 R y5 ,-S(O)R y5 , -N(R y5 )S(O) 2 N(R y5a R y5b ), -SR y5 , -N(R y5 R y5a ), -NO 2 -OC(O)R y5 , -N(R y5 )C(O)R y5a , -N(R y5 )S(O) 2 R y5a , -N(R y5 )S(O)R y5a , -N(R y5 )C(O)OR y5a , -N(R y5 )C(O)N(R y5a R y5b ), -OC(O)N(R y5 R y5a ), and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 Alkyl is optionally substituted with one or more halogens, either the same or different. Each-R y3 ,-R y3a ,-R y4 ,-R y4a ,-R y5 ,-R y5a and -R y5b However, independently, -H and C 1-6 Selected from the group consisting of alkyl groups, where C 1-6 The compound according to any one of claims 1 to 9, wherein the alkyl is optionally substituted with one or more halogens, one or more of the same or different.

11. L 2 -But, equation (XI) 【Transformation 8】 (In the formula, Dashed lines without a mark are -L 1 - indicates binding to The dashed line with an asterisk indicates a bond to at least one polymer moiety. h is an integer selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, and 16. A compound according to any one of claims 1 to 10 or a pharmaceutically acceptable salt thereof.

12. A compound according to any one of claims 1 to 11, wherein -D-AB is a GLP-1 receptor agonist moiety, or a pharmaceutically acceptable salt thereof.

13. The compound according to claim 12 or a pharmaceutically acceptable salt thereof, wherein the GLP-1 receptor agonist moiety is selected from the group consisting of semaglutide, liraglutide, echnoglutide, GZR18, GL0034, tylzepatide, cotadutide, BI-456906, pembidutide, mazdutide, dapiglutide, and letatoltide.

14. -The compound according to claim 12 or 13, or a pharmaceutically acceptable salt thereof, wherein D-AB is semaglutide.

15. The compound is given by formula (2c'') 【Chemistry 9】 (In the formula, The dashed line indicates the binding of semaglutide to the N-terminal amine functional group. n1, n2, n3, and n4 are independent integers between approximately 11 and approximately 115. A compound according to claim 1 or any one of claims 4 to 14, or a pharmaceutically acceptable salt thereof.

16. The compound is given by formula (2c') 【Chemistry 10】 (In the formula, The dashed line indicates the binding of semaglutide to the N-terminal amine functional group. n1, n2, n3, and n4 are independent integers between approximately 11 and approximately 115. A compound according to claim 1 or any one of claims 4 to 15, or a pharmaceutically acceptable salt thereof.

17. The compound according to claim 15 or 16 or a pharmaceutically acceptable salt thereof, wherein n1, n2, n3, and n4 are independently integers of about 28.

18. The compound according to claim 15 or 16 or a pharmaceutically acceptable salt thereof, wherein n1, n2, n3, and n4 are independently integers of about 56.

19. The compound is given by formula (2g') 【Chemistry 11】 [In the formula, n is an independent integer between approximately 22 and approximately 230. The dashed line indicates a part. 【Chemistry 12】 (In the formula, The unmarked dashed lines indicate the connection of equation (2g') to the unmarked dashed lines. (The dashed line with an asterisk indicates the binding of semaglutide to the N-terminal amine functional group.) [Shows a connection to] A compound according to any one of claims 1, 2, or 7 to 14, or a pharmaceutically acceptable salt thereof.

20. The compound is given by formula (2g) 【Chemistry 13】 [In the formula, n is an independent integer between approximately 22 and approximately 230. The dashed line indicates a part. 【Chemistry 14】 (In the formula, The unmarked dashed lines indicate the connection of equation (2g) to the unmarked dashed lines. (The dashed line with an asterisk indicates the binding of semaglutide to the N-terminal amine functional group.) [Shows a connection to] A compound according to any one of claims 1, 2, or 7 to 14, or a pharmaceutically acceptable salt thereof.

21. A compound according to claim 19 or 20, or a pharmaceutically acceptable salt thereof, wherein n is approximately 112.

22. A pharmaceutical composition comprising one or more compounds described in any one of claims 1 to 21 or a pharmaceutically acceptable salt thereof.

23. A compound according to any one of claims 1 to 21 or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition according to claim 22, for the manufacture of a pharmaceutical.

24. A compound according to any one of claims 1 to 21 or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition according to claim 22, for use in the treatment of diseases that can be treated with -D-AB.

25. A pharmaceutical composition comprising any one of the compounds described in claim 12 to 21 or a pharmaceutically acceptable salt thereof, or one or more compounds described in any one of claim 12 to 21, for use in the treatment of a disease selected from the group consisting of (i) all forms of diabetes mellitus, (ii) obesity, (iii) non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH), (iv) cardiovascular disease, (v) neurodegenerative disorders, (vi) chronic kidney disease (CKD), (vii) diabetic nephropathy (DKD), (viii) peripheral artery disease (PAD), and / or (ix) heart failure (HF).

26. A pharmaceutical composition comprising a compound according to any one of claims 12 to 21 or a pharmaceutically acceptable salt thereof, or one or more compounds according to any one of claims 12 to 21, for use in the treatment of a disease selected from the group consisting of X syndrome, atherosclerosis, myocardial infarction, coronary heart disease, reperfusion injury, stroke, cerebral ischemia, early heart disease or early cardiovascular disease, left ventricular hypertrophy, coronary artery disease, hypertension, essential hypertension, acute hypertensive emergency, cardiomyopathy, cardiac dysfunction, exercise intolerance, acute and / or chronic heart failure, arrhythmia, cardiac rhythm disorder, syncope, angina pectoris, cardiac bypass and / or stent reocclusion, intermittent claudication (obstructive arteriosclerosis), diastolic dysfunction and / or systolic dysfunction; and hypotension such as hypotension.

27. A compound or a pharmaceutically acceptable salt or pharmaceutical composition thereof for use according to claim 25 or 26, wherein the compound or a pharmaceutically acceptable salt thereof or pharmaceutical composition thereof is administered in combination with a growth hormone.

28. A compound for use according to claim 27, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition, wherein the growth hormone is lonapegsomatropin.

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