300results 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.

The invention provides collagen tripeptide as well as a preparation method and application thereof, and belongs to the technical field of active peptide. The invention provides a preparation method of collagen tripeptide, which comprises the following steps: carrying out enzymolysis treatment on tilapia scales and high-temperature-resistant protease, then carrying out enzymolysis treatment by using alkaline protease and neutral protease in sequence, filtering enzymatic hydrolysate by using a ceramic membrane and an organic filter membrane in sequence, and intercepting by using a 400Da nanofiltration membrane to obtain collagen tripeptide. The permeate contains active peptide mainly composed of collagen tripeptide. After the permeate is concentrated and dried, the collagen tripeptide powder is detected, and the protein content reaches 96.2%, the GPH content is 3.8%, and the CTP content is 35.09%. The collagen tripeptide powder has better DPPH (1, 1-diphenyl-2-picrylhydrazyl) scavenging activity; the traditional Chinese medicine composition has an obvious ROS removing effect, a beta-galactosidase activity inhibiting effect and a telomerase activity enhancing promoting effect on a hydrogen peroxide induced zebrafish aging model, and shows an obvious anti-aging effect.

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.

Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.

The invention relates to a preparation method and application of collagen tripeptide liquid, and belongs to the technical field of bioactive peptides, the preparation method comprises the following steps: A1, pretreating fish skin raw materials to obtain fish skin homogenate; a2, the pH value of the fish skin homogenate is adjusted to be neutral, compound protease accounting for 1-4% of the mass of the fish skin is added for enzymolysis, and a collagen peptide crude extracting solution is obtained; a3, performing enzyme deactivation and centrifugation, collecting supernate, and performing nanofiltration to obtain a filtered component 1 and an intercepted component 1; a4, putting the interception component 1 into a hydrochloric acid solution, and hydrolyzing to obtain hydrolysate; adjusting the hydrolysate to be neutral, and then carrying out nanofiltration to obtain a filtered component 2 and an intercepted component 2; and A5, mixing the filtered component 1 and the filtered component 2, carrying out nanofiltration, and collecting an intercepted component 3 to obtain a collagen tripeptide solution. The collagen tripeptide in the prepared collagen tripeptide liquid is high in yield, and the purity is also effectively improved.

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

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 invention relates to a camptothecin compound with anti-tumor activity, a preparation method therefor and use thereof. In particular, the present invention relates to a compound of the following formula or a pharmaceutically acceptable form thereof, a pharmaceutical composition thereof, a preparation method thereof and use thereof. The compound can be used as a medicine for treating diseases in abnormal cell proliferation,

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

The present disclosure provides compounds with increased metabolic stability for inhibiting a virus infection, such as a Baltimore Group IV RNA virus infection, such as rhinovirus, coxsackievirus, norovirus and coronavirus. Aspects of the present disclosure also include methods of treating the virus infection in a subject with compounds with increased metabolic stability.

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.

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 invention discloses a preparation method of fishbone collagen tripeptide, which comprises the following steps: soaking fishbone dust (30-60 meshes) in a choline-arginine eutectic solvent, stirring, centrifuging or filtering, and collecting supernate; adding pure water with the volume 3-6 times that of the supernatant into the supernatant, standing for more than 24 hours, centrifuging or filtering again, and collecting the supernatant; carrying out tangential filtration treatment by adopting a nanofiltration membrane with the molecular weight cutoff of 200Da, recovering the eutectic solvent in the filtrate through vacuum concentration, adding pure water into the trapped fluid, carrying out repeated nanofiltration treatment to remove solvent residues, and collecting the trapped fluid; and carrying out spray drying on the trapped fluid to obtain a powder product with the collagen tripeptide content of more than 50%. Compared with a traditional enzyme method for preparing fishbone collagen tripeptide, the method disclosed by the invention has the advantages that the extraction rate is high, a deliming step is not needed, the enzyme cost is saved, an extraction solvent is green and can be recycled, and the like.

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 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.

Bifunctional compounds (degradation inducers) that target LRKK2 for degradation are disclosed. Pharmaceutical compositions containing the degradation inducers and methods of using the degradation inducers for treating neurodegenerative diseases and disorders such as Parkinson's disease and brain cancers (e.g., glioma and glioblastoma) are also disclosed.

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.