426results 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.

Compounds disclosed herein or their pharmaceutically acceptable salts can modulate the G12D mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds disclosed herein or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

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.

Disclosed herein are novel cytotoxic compounds, and cytotoxic conjugates comprising these cytotoxic compounds and cell binding agents. More specifically, the present disclosure relates to novel camptothecin derivatives thereof, intermediates thereof, conjugates thereof, and pharmaceutically acceptable salts thereof, which are useful as medicaments, particularly as antiproliferative agents (anticancer agents).

A compound comprising a prostate-specific membrane antigen (PSMA) targeting moiety of the following formula: R 0 is O or S. 1a , R 1b and R 1c Each of R may be, for example, —COH, —SOH, —SOH, —POH, or —POH. 2 R may be an optionally substituted methylene or a derivative thereof, propylene or a derivative thereof, or a derivative of ethylene. 3 is a linker. When the PSMA targeting moiety is attached to a radiolabeling group, the compound may be used as an imaging agent or a therapeutic agent for diseases / conditions that express PSMA. TIFF2022537773000240.tif2237

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 provides antibodies and antibody-drug conjugates that target claudin-18.2, and their use in the treatment of cancer. The present invention also provides nucleotides encoding the claudin-18.2 antibodies, combinations of polynucleotides, expression vectors, and combinations of expression vectors, pharmaceutical compositions containing the claudin-18.2 antibodies or antibody-drug conjugates, and their use in the manufacture of medicaments for treating or preventing cancer.

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 compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein each R 1 ~R 30 are independently selected from the group consisting of H and deuterium, and R 1 ~R 30 at least one of which is deuterium having an abundance level greater than the naturally occurring abundance of deuterium. The present invention also provides pharmaceutical compositions containing the compounds, and uses of the compounds.

The invention relates to a method of manufacturing an RNA- or DNA-containing virus particle in cell culture, a supplement for a culture medium and a culture medium for use in the production of RNA or DNA-containing virus particles, comprising one or more dipeptides or derivatives thereof, wherein one dipeptide is glycyl-glutamine (Gly-GIn).

To provide constructs such that hydrolysis of the construct by a specified gastrointestinal enzyme directly or indirectly releases an opioid when taken orally as prescribed.SOLUTION: The invention provides constructs such that hydrolysis of the construct by a specified gastrointestinal enzyme directly or indirectly releases an opioid when taken orally as prescribed. The gastrointestinal enzyme mediated release of the opioid from the constructs of the invention is designed to be attenuated in vivo via a saturation or inhibition mechanism when overdoses are ingested. The invention further provides constructs that are highly resistant to oral overdose, chemical tampering, and abuse via non-oral routes of administration.SELECTED DRAWING: Figure 1

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.

Verrucarin A derivatives, linker-verrucarin A derivatives and antibody-drug conjugates thereof are provided herein. In one embodiment, the verrucarin A derivatives, linker-verrucarin A derivatives and antibody-drug conjugates are useful in treating viral diseases.

The present invention relates to the field of bioconjugation of functional entities (payloads) to targeting agents, in particular biological targeting agents such as antibody drug conjugates (ADCs), in which one or more payload molecules are conjugated to a targeting agent, for example a monoclonal antibody. More specifically, the present invention relates to novel hydrophilic tetrazine molecules and their preparation, which allow more efficient conjugation of payload molecules to targeting agents such as monoclonal antibodies. The present invention also relates to certain tetrazine intermediates useful for the preparation of corresponding functionalized payload molecules. The present invention also relates to the respective conjugates, in particular bioconjugates, and methods for their preparation. The present invention also relates to the medical use of such conjugates of the present invention, to the corresponding pharmaceutical compositions, and to the corresponding diagnostic and analytical kits.

The present disclosure provides novel methods for treating, preventing, ameliorating, inhibiting and / or delaying the onset of tauopathy, comprising administering to a subject an effective amount of a small molecule peptidomimetic, such as (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 a pharma- ceutically acceptable salt, stereoisomer, tautomer, hydrate, and / or solvate thereof.

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 compounds of the present invention are represented by the following compounds having Formula I:where the substituents R1, R4, L, M, X, Y, and s are as defined herein. The compounds of the present invention are also represented by the following compounds having Formula (Ia), Formula (Ib), or Formula (Ic):where the substituents R1-R4, Rx, Ry, X, Y, and s are as defined herein.These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders or for providing immunosuppression for transplanted organs or tissues.

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.