221results about "Tripeptides" 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.

The invention provides an anti-wrinkle combined cyclic peptide and application thereof in cosmetics, the anti-wrinkle combined cyclic peptide comprises cyclic pentapeptide-4, cyclic tripeptide-5 and cyclic hexapeptide-9, the combined cyclic peptide has a remarkable synergistic effect in the aspects of promoting expression of collagen genes Collagen I, Collagen III and Collagen IV and inhibiting acetylcholine secretion, the skin elasticity and glossiness are remarkably improved, and the anti-wrinkle combined cyclic peptide has a good anti-wrinkle effect. The generation of wrinkles is inhibited, and good anti-aging and wrinkle-removing effects are achieved.

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.

Use of anti-aging glycopeptides for the treatment of dry eye disease, retinal degenerative disease, or ocular inflammation [Solution] The present specification discloses methods of using a gem-difluorinated C-glycopeptide compound represented by general formula I, or a pharmaceutically acceptable base, acid addition salt, hydrate or solvate of a compound represented by general formula I, for the treatment or prevention of dry eye disease, and / or for the treatment or prevention of retinal degenerative disease, ocular inflammation, or a combination thereof in a subject in need of such treatment or prevention.

An antibody-drug conjugate as shown in formula I, a preparation method therefor, and a use thereof in prevention and / or treatment of diseases related to abnormal cell activity, including but not limited to a use in prevention and / or treatment of tumor diseases.

The present application relates to epitope-targeted SIV and HIV vaccines. The invention provides novel envelope glycoproteins which may be utilized as HIV-1 vaccine immunogens, antigens for crystallization, and for identification of broadly neutralizing antibodies. The invention encompasses preparation and purification of immunogenic compositions which are formulated into vaccines of the present invention.

The invention discloses a CAIX targeted degradation agent. The CAIX targeted degradation agent comprises a CAIX target protein ligand, an integrin ligand and a connector, the CAIX target protein ligand and the integrin ligand are connected through the connecting body. As the carbonic anhydrase IX is enriched in the tumor region, the CAIX targeted degradation agent can specifically target the tumor region; the compound can effectively induce degradation of CAIX and inhibit survival of tumor cells under the hypoxia condition, has the functions of targeting a tumor area and degrading carbonic anhydrase IX by utilizing integrin and lysosome, further changes hypoxia and subacid environments of the internal environment of a tumor patient, and plays a role in inhibiting survival of hypoxia tumor cells; the tumor targeting property is high, the toxic and side effects on normal cells are relatively small, and a relatively good effect can be obtained by using a relatively small dosage.

The present invention relates to a compound of formula (I) R1-W m -X n -AA i -AA2-AA3-AA4-AA5-AA6-Y p -Z q -R a wherein AA1 is Asp, Gly, Asn, Gln, Ala, or no amino acid, AA2 is Val, Ile, Leu, or Ala, AA3 is Tyr, Phe, Trp, Lys, Arg, or His, AA4 is Lys, Arg, His, Pro, or Val, AA5 is Asn, Asp, Gln, or no amino acid, and AA6 is Thr, Ala, Ser, or no amino acid. The compounds are useful for treating and / or preventing symptoms of skin aging, in particular for treating and / or preventing skin wrinkles, treating and / or preventing the appearance of sagging skin, and / or reducing and / or preventing facial asymmetry.

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 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 provides a peptide having a fluoroalkyl group in the side chain. The present invention provides a peptide in which 2 or more amino acids are peptide-bonded in which at least one side chain of an amino acid residue constituting the peptide is represented by the following General Formula (1) [in the formula, Z1 is a divalent, trivalent, or tetravalent linking group other than an alkylene group; Rf is a C1-30 alkyl group substituted with at least two fluorine atoms, -SF5, or -SF4-CR101R102-CR103R104Cl (R101, R102, R103, and R104 are each independently a hydrogen atom, a fluorine atom, or a chlorine atom, and two or more of R101, R102, R103, and R104 are fluorine atoms); n3 is 1, 2, of 3, and the black circle indicates a bonding site].

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 relates to a compound represented by the general formula (I) The present invention provides a viral protease inhibitor having the formula: TIFF2024545135000558.tif3653, wherein the variables are as described herein, compositions comprising the compounds, methods of making the compounds, and methods of using the compounds.

To provide a method of treating an inflammatory neurological disease or condition that can result in destruction or degeneration of axons or myelin.SOLUTION: Provided is a combination comprising a) a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof; and b) one or more drugs selected from the group consisting of I) a compound of a particular formula or a pharmaceutically or veterinarily acceptable salt thereof; ii) a sphingosine-1-phosphate receptor inhibitor (S1PR modulator); and iii) a signal transducer and activator of transcription 3 (STAT3) inhibitor.SELECTED DRAWING: None

Tripeptides (sequence isomers of K / Y / W) and a method for using the same. The tripeptides, upon a process of evaporation-driven self-assembly, undergo two-stage phase separation to form highly porous particles upon drying. These particles readily re-dissolved upon reintroduction of water. The particles can trap molecular payloads that can be readily released in aqueous media.

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.

The invention relates to a compound of general formula I wherein A is an amino acid selected from the group consisting of wherein the amino acids are optionally substituted: k is 0, 1, or 2 independently at each occurrence; m is 1, 2, 3, 4 or 5 independently at each occurrence; n is 0, 1, 2 or 3 independently at each occurrence; p is 1, 2 or 3 independently at each occurrence; q is 1, 2 or 3 independently at each occurrence; X and Y are substituted or unsubstituted amino acids; Z is selected from the group consisting of where v is 0, 1 or 2; G 1 N or CR a is; G 2 N or CR b is; G 3 N or CR c is; G 4 N or CR d is; where 0, 1 or 2 of G 1 , G2 , G 3 and G 4 N is / are; R a , R b , R c and, if present, are in each case independently selected from the group consisting of hydrogen, halogen, hydroxy, carboxyl, C 1 -C 6 -Alkyl, C 1 -C 6 -Alkoxy, cyano, nitro and Si(tBu) 2 F exists, provided that only 1 or 2 of R a , R b , R c and R d Halogen is / are; and R is selected from the group consisting of hydrogen, halogen, hydroxy, C 1 -C 6 -alkyl and C 1 -C 6 -alkoxy.

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.

The invention relates to a compound of general formula I wherein A is an amino acid selected from the group consisting of wherein the amino acids are optionally substituted: k is 0, 1, or 2 independently at each occurrence; m is 1, 2, 3, 4 or 5 independently at each occurrence; n is 0, 1, 2 or 3 independently at each occurrence; p is 1, 2 or 3 independently at each occurrence; q is 1, 2 or 3 independently at each occurrence; X and Y are substituted or unsubstituted amino acids; Z is selected from the group consisting of where v is 0, 1 or 2; G1 N or CR a is; G2 N or CR b is; G3 N or CR c is; G4 N or CR a is; where 0, 1 or 2 of G1, G2, G3 and G4 is / are N; R a , R b , Rc and R d , if present, are in each case independently selected from the group consisting of hydrogen, halogen, hydroxy, carboxyl, C1-C6 alkyl, C1-C6 alkoxy, cyano, nitro and Si(tBu)2F, provided that only 1 or 2 of R a , R b , R c and R d Halogen is / are; and R is selected from the group consisting of hydrogen, halogen, hydroxy, C1-C6 alkyl and C1-C6 alkoxy.

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.

Provided are 3-4 residue non-natural macrocyclic oligoamides comprising species of 3 or 4 monomer residues selected from the group consisting of monomers a, b, c, d, e, f, g, h, I, j, k, l, m, n, o, p, q, r, s, t, u, and v as defined in Table 1, and methods for designing such macrocyclic oligoamides.

Compositions and methods for stimulating endogenous hyaluronic acid production are provided herein, which can improve skin hydration and elasticity. TIFF2023544824000002.tif76156

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.

The present disclosure relates to antibody drug conjugates (ADCs) comprising an antibody or antigen-binding fragment thereof covalently linked to two pharma- ceutically active drugs via a dual linker. Linker-drug conjugates comprising a dual linker and a pharma- ceutically active drug are also disclosed. Such linkers are a conventional way to deliver two (e.g., two different or the same) drugs bound to a single antibody. Such linkers may be particularly useful for improving the solubility of antibody drug conjugates (ADCs) that contain one or more hydrophobic drug compounds.

Provided in the present application are antibody-drug conjugates, and methods for their preparation and use. The antibody-drug conjugates have the formula Ab-[MLED] x and the drug is selected from antitubulin agents, DNA intercalators, DNA topoisomerase inhibitors and RNA polymerase inhibitors. The prepared antibody-drug conjugate has a better drug-to-antibody ratio and has good target killing effect on colon cancer and non-small cell lung cancer (e.g., lung adenocarcinoma).

This disclosure deals with macrocyclic compounds of formulas (Ia) and (Ib) that can inhibit the Ras protein, as well as pharmaceutical compositions and protein conjugates thereof, and their use in the treatment of cancer. JPEG2026515696000242.jpg54170

The present disclosure provides a cyclic peptide derivative, a method for producing the same, and a composition. The present disclosure relates to a compound for modulating nervous system cell activity. More specifically, the compound of the present disclosure is capable of modulating the proliferation activity of astrocytes. The compound of the present disclosure has the effect of enhancing the proliferation activity of astrocytes. The features provided by the present disclosure can be used for a cyclic peptide derivative for modulating nervous system cell activity and a method for producing said cyclic peptide derivative.