360results about "Tetrapeptides" patented technology

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.

Compositions and methods for treating diseases associated with dysregulation of miR-21, particularly cancer, are disclosed.

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 present invention provides a novel antithrombotic antibody, which targets FIXa and has unique properties, specifically targets the binding site of blood coagulation factors FIXa and FVIIIa, reduces the formation of FVIIIa-FIXa complex, blocks the conversion of FX to FXa, and exerts antithrombotic effects. The antibody of the present invention has suitable antithrombotic properties, has a wide effective therapeutic concentration window, but does not increase the risk of bleeding; it can realize the demand for moderate antithrombotic properties in clinical applications and effectively avoid bleeding problems caused by excessive effects. The present invention also discloses a method for screening drugs that target the FIXa-FVIIIa binding site.

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 the field of biological medicines and cosmetics, in particular to a composition which takes tetrapeptide and bisabolol as core components and has anti-inflammatory and anti-aging activity.

The present disclosure relates to the technical field of polypeptides. Disclosed are a cyclic peptide, and a composition and the use thereof. The cyclic peptide of the present disclosure has a structure as shown in formula (I): Cyclo-[Gly-His-Lys-Lys] (I). The present disclosure specifically relates to the cyclic peptide or a salt thereof, or a composition thereof, and the use thereof in the preparation of a composition for caring or treating skin or mucosa.

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.

The present invention relates to novel insulin derivatives and their use in the treatment or prevention of medical conditions associated with diabetes. The insulin derivatives are glucose-sensitive and exhibit glucose-sensitive albumin binding. The present invention also relates to novel intermediates. Finally, the present invention provides pharmaceutical compositions comprising the insulin derivatives of the present invention and the use of such compositions in the treatment or prevention of medical conditions associated with diabetes.

The invention described herein pertains to the diagnosis, imaging, and / or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and / or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using compounds capable of targeting PSMA expressing cells.

Peptides and methods of use thereof, are disclosed for use in treating various diseases and disorders, including inflammation, pain, oral mucositis, oral lesions, and cancer. The peptides modulate the activity of the transcription factor NF κB.

The invention relates to a novel polypeptide and application thereof. The polypeptide provided by the invention is short in peptide chain and faster and better in absorption. Experimental results show that the polypeptide provided by the invention shows an obvious enteric cavity dilatation relieving effect in pharmacodynamic tests of a zebra fish inflammatory bowel disease model and a rat inflammatory bowel disease model. The polypeptide provided by the invention has a remarkable colitis relieving effect, and can be used for preparing a medicine for treating enteritis, especially a medicine for treating ulcerative colitis.

Provided is a new polypeptide. The new polypeptide shows a significant effect of relieving intestinal lumen distension in pharmacodynamic tests of a Brachydanio Rerio inflammatory bowel disease model and a rat inflammatory bowel disease model, and can be used for preparing a drug for treating enteritis, especially ulcerative colitis.

A novel PACE4 inhibitor and use thereof in anti-osteoarthritis. A novel PACE4 inhibitory peptide is designed and synthesized, which can effectively inhibit the expression of extracellular PACE4 without affecting normal cells, and is stable in joints and unstable in plasma, so that the PACE4 inhibitory peptide has excellent safety and can be effectively used in the prevention and treatment of OA.

Compounds with the following structures and their analogs are provided. Compositions that include these structures can be used to inhibit glucose transporters and stop or decrease the proliferation of cancer, treat possible organ rejection and treat autoimmune disease.

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).

Compositions comprising specific tetrapeptides, for use in treating, preventing, minimizing, diminishing or reversing various signs of aging of the skin are provided. The compositions are useful in improving the firmness or elasticity of skin, smoothing of fine-lines or wrinkles, reducing skin pores and hyperpigmentation, and increasing skin thickness, radiance and / or softness.

The present invention relates to a new polypeptide and its application. The polypeptide provided by the present invention has a short peptide chain and is absorbed faster and better. Experimental results show that the polypeptide provided in this application exhibits an obvious effect of alleviating intestinal lumen dilation in the zebrafish inflammatory bowel disease model and the rat inflammatory bowel disease model. The polypeptide provided by the present invention has a significant effect of alleviating colitis and can be used to prepare drugs for treating enteritis, especially drugs for ulcerative colitis.

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.

The present invention relates to a method of preparing a salt of a β-turn peptidomimetic cyclic compound of formula (I) where R1, R2, R3, R4, R5, R6, R7, R8, R10, X, Y and n are as defined in the description, in particular a method of preparing a β-turn peptidomimetic cyclic compound having the following structure:

To provide a method for producing a high-purity peptide compound in a high yield under a condensation condition applicable even to a highly rare non-natural amino acid by using an easily available condensing agent and additive capable of suppressing prematurecleavage and also suppressing a side reaction especially in a condensation reaction process of a solid phase synthesis method of a peptide.SOLUTION: Provided is a method for producing a peptide compound, including a step of condensing a first amino acid or peptide and a second amino acid or peptide in the presence of an additive and a condensing agent to obtain a condensate, wherein the number of moles of the additive is smaller than the number of moles of the second amino acid or peptide. By using a small amount of the additive with respect to the amino acid or peptide to be added to the N-terminus, the condensation reaction can be allowed to proceed efficiently even when an amino acid having large steric hindrance is contained, and the target peptide compound can be obtained with high yield and high purity.SELECTED DRAWING: None

The present invention relates to ligand drug conjugates for the treatment of diseases. In particular, the present invention relates to ligand drug conjugates comprising a linker system that allows improved delivery of drugs to target cells while retaining the favorable pharmacokinetic properties of antibodies. The present invention also relates to ligand drug conjugates that achieve high drug-antibody ratios and exhibit excellent pharmacokinetic properties, thus significantly improving efficacy. In one aspect, the present invention also relates to ligand drug conjugates for intracellular delivery of cytotoxic drugs to tumor or cancer cells.

Provided is a method for producing a peptide compound or a salt thereof, including a step (linking step) of linking an amino group of a first amino acid or peptide and a carboxy group of a second amino acid or peptide with an amide bond, wherein a stand-alone condensing agent and one or more additive(s) are used in the linking step, and the additive(s) are one or more selected from the group consisting of HOPO, HOAt, HOOBt, HOCt, PfpOH, Oxyma, Oxyma-B, N-HOSu, and K-Oxyma.

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

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 novel compounds suitable for the detection and / or inhibition of coagulation proteases, specifically APC, flla, fXa, and fXla. The compounds have the structural formala (1) or (X) shown below in which R1, P1, P2, P3, P4, Z, R1x, A1, A2, A3, A4 and Zx are defined herein. The present invention also relates to compositions comprising the compounds of formula (I) or formula (X) defined herein, to processes for synthesising these compounds and to their use for the treatment and / or detection of diseases and conditions in which coagulation proteases, in particular APC, flla, fXa, and fXla, are implicated.

The present invention provides immunoconjugates of formula (I) comprising an antibody linked by conjugation to one or more 8-sulfonyl-2-aminobenzazepine derivatives. The present invention also provides 8-sulfonyl-2-aminobenzazepine derivative intermediate compositions comprising reactive functional groups. Such intermediate compositions are suitable substrates for the formation of the present immunoconjugates via a linker or linking moiety. The present invention further provides methods of treating cancer using the present immunoconjugates.

Disclosed herein is a system that addresses all of the current challenges described above by combining three existing technologies and an improved nuclear RNA delivery system to generate a first-in-class cellular therapy that can secrete a cancer specific suicide gene for the treatment of several cancers. Also disclosed herein is a 'Trojan-Horse' like genetic construct aimed at engineering a chemo-sensitive dominant clone for adaptive therapy in cancers, such as leukemia. In some embodiments, cells, such as cancer cells from a subject, are engineered with suicide genes to promote a bystander effect in neighboring cancer cells once returned to the subject. In some embodiments, these cells are further engineered to be clonally dominant, e.g. by deleting or mutating tumor suppressor genes in the cells, overexpressing oncogenes, or any combination thereof. Once the engineered cells have reached a target clonal dominance, the suicide gene can be induced, thereby promoting the bystander effect.

Methods for treating neurological disorders, central or peripheral nervous system injuries, and / or secondary pathologies thereof are provided. [Solution] The present disclosure also includes methods and compositions related to the use of compounds comprising specific peptides linked to dyes. In certain embodiments, the peptide DIRG is linked to a BODIPY dye. In specific embodiments, the compositions are used to treat neurological conditions and their associated secondary pathologies, such as spinal cord injury and Alzheimer's disease.

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.