243results about "Dipeptides" patented technology

Provided is an antibody-drug conjugate for use in the treatment of cancer in which one or more KRAS mutants, particularly a KRAS G12V mutant, a KRAS G12D mutant, and a KRAS G12C mutant, are expressed. Also provided are a drug and a drug-linker conjugate for use in the antibody-drug conjugate.　The present inventors have produced an antibody-drug conjugate with which a heterocyclic compound represented by formula (II) and having an activity of inducing the decomposition of KRAS mutant proteins can be delivered to cancer in which EGFRs are expressed, the production being achieved by linking the compound to an anti-EGFR antibody. The present inventors have also discovered a drug-linker conjugate for use in the antibody-drug conjugate or a salt thereof. In cancer in which EGFRs are expressed, the antibody-drug conjugate induces the decomposition of one or more KRAS mutants, particularly a KRAS G12V mutant protein, a KRAS G12D mutant protein, and a KRAS G12C mutant protein, thereby inhibiting the KRAS mutants and exhibiting an anti-tumor effect.

Provided are an antibody-drug conjugate, a preparation method therefor, and use thereof. The antibody-drug conjugate has a structure represented by the formula Ab-[M-L-E-D]x, has a superior drug-to-antibody ratio, and has an excellent targeted killing effect on various cancers or tumors.

Provided are an antibody-drug conjugate, a method for preparing same, and use thereof. The antibody-drug conjugate has a structure represented by formula Ab-[M-L-E-D] x, a superior drug-to-antibody ratio, and an excellent targeted killing effect on various cancers or tumors.

The invention relates to coacervate-forming polymers having defined structural formulae. The invention also relates solutions comprising the coacervate-forming polymers and methods of making solutions comprising the coacervate-forming polymers. The invention also relates to polymer coacervates, comprising the coacervate-forming polymers within the coacervates, including polymer coacervates comprising cargo compounds, and methods for making such polymer coacervates. The coacervates of the invention are capable of penetrating into cells and thereby delivering cargo compounds into cells. The invention further relates to compositions, including pharmaceutical compositions, comprising the polymer coacervates. The invention also relates to uses of the coacervate-forming polymers, including medical uses.

To provide use of compositions in preparation of medicaments for treating or preventing α-synuclein disease or TDP-43 proteinopathy as well as pharmaceutical compositions.SOLUTION: Disclosed is the use of a composition comprising a therapeutically effective amount of a peptidomimetic, (R)-2-amino-N-((S)-1-(((S)-5-amino-1-(3-benzyl-1,2,4-oxadiazol-5-yl)pentyl)amino)-3-(4-hydroxy-2,6-dimethylphenyl)-1-oxopropan-2-yl)-5-guanidinopentanamide or pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate and / or solvate thereof.SELECTED DRAWING: Figure 1A-1B

The present disclosure provides protein degradation targeting chimeras comprising (i) a benzo[c][l,2,5]thiadiazolyl-based targeting ligand capable of binding to toxic peptides and / or protein aggregates (e.g., alpha-synuclein fibrils, amyloid plaques, and / or tau protein tangles) in brain tissue for degradation; (ii) a ubiquitin ligase recruiting ligand; and (iii) a linker between (i) and (ii). These protein degradation targeting chimeras are useful, for example, in the treatment of neurodegenerative disorders such as Parkinson’s disease (PD), multiple system atrophy (MSA), and Lewy body dementia.

The present invention relates to salts of dipeptides and their use in cell culture.The present invention further relates to a culture medium for culturing cells, preferably plant cells, animal cells or mammalian cells, and the use of the culture medium of the present invention, as well as to a method for producing a cell culture product.

The present invention relates to an antibody conjugate that is particularly suitable for targeting Trop-2 expressing cells, especially tumor cells. The antibody conjugate according to the invention has the structure (1), where AB is an antibody capable of targeting Trop-2 expressing tumors, L is a linker connecting Z to D, Z is a connecting group, and L 6 -GlcNAc(Fuc) w -(G) j -S-(L 7 ) w’ -, in which G is a monosaccharide, j is an integer ranging from 0 to 10, S is a sugar or a sugar derivative, GlcNAc is N-acetylglucosamine, Fuc is fucose, w is 0 or 1, w' is 0, 1, or 2, and L 7 is -N(H)C(O)CH2-, -N(H)C(O)CF2-, or -CH2-, D is exatecan, b is 0 or 1, x is 1 or 2, and y is 1, 2, 3, or 4. The present invention further relates to methods for preparing the antibody conjugates of structure (1) and applications of the antibody conjugates of structure (1).

The present disclosure relates to novel folic acid conjugates comprising 5-methyltetrahydrofolic acid, a radiometal chelator that optionally coordinates a radiometal M, and the albumin binder 5-(p-iodophenyl)pentanoate, and further provides uses of such conjugates and / or pharmaceutical compositions thereof in diagnostic imaging, radionuclide therapy, or theragnostic applications.

The present invention provides biomolecular glass and its use. The biomolecular glass is obtained by volatilizing a solvent from a solution of biomolecular raw materials, the solution of biomolecular raw materials comprising biomolecular raw materials, a modifier, and a solvent. The biomolecular raw materials include natural amino acids, peptides, amino acid derivatives, peptide derivatives, or mixtures of two or more of the above. The soluble biomolecular glass of the present invention has excellent biocompatibility, high light transmittance, good mechanical strength, flexible processability, and biodegradability, and can be processed into implantable or non-implantable medical materials and / or devices, fillers and stent materials, electronic sensing materials and / or devices, temporary electronic materials and / or devices, etc., and can be decomposed by living organisms or nature, with decomposition products being non-contaminating.

Novel compounds that act as inhibitors of alpha4beta7 integrin are disclosed. Pharmaceutical compositions and methods of use of inhibitors of [alpha] 4 [beta] 7 integrin are disclosed. In particular, methods of using the [alpha] 4 [beta] 7 inhibitors in the treatment of diseases or conditions associated with inflammatory bowel diseases, including ulcerative colitis and Crohn's disease.

The objective of this invention is to provide a highly safe, long-term-use, and excellent food-derived Netrin-1 production promoter. [Solution] White fungus exhibits excellent Netrin-1 production-promoting activity, and the combination of white fungus and imidazole dipeptide showed a particularly remarkable Netrin-1 production-promoting activity compared to white fungus and imidazole dipeptide alone. Therefore, white fungus, white fungus, and imidazole dipeptide can be used as foods, quasi-drugs, and pharmaceuticals with excellent Netrin-1 production-promoting activity.

The present invention provides an antibody-payload conjugate having a payload antibody ratio of 1. The antibody-payload conjugate has the structure (1): Formula (1) (wherein a, b, and c are each independently 0 or 1; L 1 , L 2 and L 3 is a linker; D is a payload; BM is a branching moiety; and Z is a connecting group obtainable by a cycloaddition reaction. The present invention further provides methods for preparing antibody-payload conjugates according to the invention, intermediate compounds in the preparation methods, and medical uses of antibody-payload conjugates according to the invention.

The invention provides an application of hederagenin in preparation of a medicine used as an SKP2 degradation agent, and particularly provides an application of hederagenin in preparation of a medicine used as an SKP2 degradation agent. The invention also provides a PROTAC compound, which comprises a target protein POI ligand, an E3 ubiquitin ligase ligand and a linking chain Linker, the general formula of the ligand-Linker-E3 ligase ligand is as follows: a POI ligand-Linker-E3 ligase ligand. The invention also provides a preparation method and application of the PROTAC compound. The PROTAC design based on HED improves the tumor tissue targeting property, and shows low toxicity in an in-vivo experiment. The invention provides a novel SKP2 (SKP2) degradation agent. The degradation agent is expected to be capable of efficiently inducing ubiquitination degradation of SKP2 protein, and a treatment strategy with higher potential and clinical application prospect is provided for overcoming the limitation of the prior art by enhancing the specific killing capability on SKP2 high-expression tumor cells and verifying the remarkable tumor inhibition effect and good safety of the degradation agent in an animal model.

To provide an amphiphilic compound capable of suppressing phase separation of a phospholipid membrane and stabilizing a phospholipid structure.SOLUTION: The present invention provides an amphiphilic compound for use as a stabilizer of two or more phospholipid compounds having different phase transition temperatures, the amphiphilic compound being represented by the following general formula (1).SELECTED DRAWING: Figure 2B

The present invention provides a flavor enhancing composition that can enhance a flavor of a food product when blended with the aforesaid food product, a method for producing the same, and a method for enhancing a flavor of a food product. A first embodiment of the present invention relates to a flavor enhancing composition containing one or more heat-treated spices selected from cumin, paprika, asafoetida and mustard seed. A second embodiment of the present invention relates to a method for producing the aforesaid flavor enhancing composition, comprising heating, under a specified condition, the one or more spices selected from cumin, paprika, asafoetida and mustard seed. A third embodiment of the present invention relates to a method for enhancing a flavor of a food product, comprising blending the aforesaid flavor enhancing composition with the food product.

This invention provides novel antibody compounds and methods for using them. [Solution] Manipulated antibody compounds and their conjugates are provided, which are useful as agents for cancer immunotherapy.

Compositions that comprise a solvent (e.g., an aqueous solvent) and a plurality of aromatic peptides that are soluble in the solvent, and non-crystalline materials formed thereof, which can be glassy and / or adhesive materials, are provided. Uses of the compositions and the non crystalline materials formed thereof, and articles-of-manufacturing made of the non-crystalline materials are also provided.

The present invention provides a composition and method for increasing muscle mass, preventing muscle atrophy, and promoting muscle growth. [Solution] In certain aspects, the disclosed composition comprises dileucine and leucine and pharmaceutically acceptable salts thereof. In certain aspects, the disclosed composition is administered to subjects in need to increase muscle mass, prevent muscle atrophy, and / or promote muscle growth.

The present invention provides a conjugate of an antibody and a functional substance, said conjugate having excellent desired properties, or a salt thereof. More particularly, the present invention provides a conjugate of an antibody and a functional substance, said conjugate containing a structural unit represented by formula (1) [wherein: Ig represents an immunoglobulin unit containing two heavy chains and two light chains and bonded to LA adjacent to Ig via thiol groups in the side chains of a plurality of cysteine residues in the two heavy chains and two light chains; HG represents a hydrophilic group or a monovalent group containing a hydrophilic group; CS represents a divalent group containing a cleavable moiety; ring A represents a divalent aromatic ring group which may have a substituent (wherein the divalent aromatic ring group constitutes a π-electron conjugated system together with the aforesaid cleavable moiety); V represents an oxygen atom, a sulfur atom or an amino(NH) group; LA and LB independently represent a divalent group; D represents a functional substance; and the average number n of the aforesaid bonds per immunoglobulin unit is 1.5 or more] or a salt thereof, and substances related thereto.

The present disclosure provides therapeutic agents comprising VLA-4 (α4β1) and α4β? inhibitors as defined herein. Methods of using the therapeutic agents are also provided. The present disclosure further provides combinations of VLA-4 inhibitors with one or more agents that interact with one or more chemokine receptors, and methods of using the same. In some embodiments, the disclosed combinations can be used in methods of mobilizing hematopoietic stem cells. In some embodiments, the disclosed methods can be used in the treatment of conditions that require collection of hematopoietic stem cells for transfusion or in chemotherapy. The present disclosure further provides methods of treating a patient comprising administering an agent that interacts with a chemokine, such as G-CSF, plerixafor, BL-8040 (motixafortide), or Crop and a VLA-4 inhibitor.

The present invention relates to certain macrocyclic compounds of formula (I) and pharma- ceutically acceptable salts thereof, which are useful for the treatment or prevention of diseases associated with and / or caused by the proteasome or immunoproteasome, selected from cancer, infectious diseases, inflammatory diseases, and autoimmune diseases. [Formula 1] TIFF2024534613001006.tif71170

The crystalline form II of erobicixibat. The X-ray powder diffraction pattern of crystalline form II has specific peaks at 2θ values of 9.4±0.2° and 7.8±0.2°, and has one or more of the following characteristic peaks: 3.9±0.2°, 11.7±0.2°, 16.1±0.2°, 17.6±0.2°, 18.3±0.2°, 19.6±0.2°, 20.9±0.2°, 22.1±0.2°, and 25.8±0.2°. Crystalline form II is stable, has low hygroscopicity, and when exposed to a high humidity environment of 25°C / 92.5%RH, the chemical purity of crystalline form II does not change significantly, and the X-ray powder diffraction pattern of the crystalline form also does not change accordingly. Furthermore, crystalline form II is accompanied by a simple and convenient preparation method, has low requirements for the preparation process and storage conditions, and has high medical value.

[Problem] To provide a novel compound promising as a prodrug-type anticancer agent that exhibits a sufficient anticancer effect and is capable of reducing adverse effects. [Solution] A compound represented by general formula (I) or a pharmaceutically acceptable salt of the compound. Formula (I): Y-T-(X1)n

The present invention provides a RAS inhibitor that selectively binds to or selectively inhibits Ras(ON). [Solution] A compound having the structure of formula Ia, or a pharmaceutically acceptable salt thereof. JPEG2026090276000524.jpg80170

The present invention relates to: a neuropsychological function improver which contains, as an active ingredient, a dipeptide containing proline or a tripeptide containing glycine and proline; and a neuropsychological function improver which comprises a soybean peptide and / or a collagen peptide. The present invention also relates to: a pharmaceutical composition for improving a neuropsychological function or a food or beverage composition for improving a neuropsychological function, which contains the improver; and a method for preventing and / or ameliorating a condition and / or a disease associated with the deterioration in a neuropsychological function, the method comprising a step of administering the improver to a patient or a potential patient to whom the improver is needed.

The present application relates to steroid compounds and conjugates thereof, in particular to the compounds and conjugates thereof, or their tautomers, mesomers, racemates, enantiomers or diastereoisomers, or mixtures thereof, or pharma- ceutically acceptable salts thereof. The present application also relates to the preparation and use of the compounds and conjugates thereof.

The present invention relates to peptides for the treatment or prevention of nonalcoholic fatty liver disease (NAFLD), non-alcoholic fatty liver (NAFL), non-alcoholic steatohepatitis (NASH), hepatic steatosis (fatty liver), liver inflammation, cirrhosis, hepatocellular carcinoma or fibrosis, especially liver fibrosis.

To provide compounds, compositions thereof, and methods of using the same.SOLUTION: The present invention provides compounds, compositions thereof, and methods of using the same. The present invention relates to compounds and methods useful for modulating the Sestrin-GATOR2 interaction thereby selectively modulating mTORC1 activity indirectly. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders. Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful for treating a variety of diseases, disorders or conditions, associated with mTORC1. Such diseases, disorders, or conditions include diabetes, epilepsy, neurodegeneration, immune response, suppressed skeletal muscle growth, and cellular proliferative disorders (e.g., cancer) such as those described herein.SELECTED DRAWING: None