3369results about "Cyclic peptide ingredients" patented technology

Provided is a medicine for treating or preventing cancer that contains a first active ingredient and that is used in combination with a second active ingredient, wherein: the first active ingredient is a compound represented by formula (1), a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof; and the second active ingredient is GDC-6036 or a pharmaceutically acceptable salt thereof.

The present invention relates to four specific macrocyclic compounds for use as inhibitors of KRAS mutant for the treatment of cancer. Example (1): 1-[4-(dimethylamino)-4-methyl-pent-2-ynoyl]-N-[(1S)-1-[[(6S,8S,14S)-22-ethyl-25-fluoro-(21M)-21-[2-[(1S)-1-methoxyethyl]-3-pyridyl]-18,18-dimethyl-9,15-dioxo-5,16-dioxa-2,10,22,28-tetrazapentacyclo[18.5.2.12,6.110,14.023,27]nonacosa-1(26),20,23(27),24-tetraen-8-yl]carbamoyl]-2-methyl-propyl]-4-fluoro-N-methyl-piperidine-4-carboxamide.

This disclosure provides cyclic peptide compounds of formula (A) or formula (II) as inhibitors of Ras kinase, and compositions and use of the same in treating diseases associated with Ras kinase.

The present disclosure provides methods for the treatment of migraine by the administration of atogepant or a pharmaceutically acceptable salt thereof.

The present disclosure provides methods for the treatment of migraine by the administration of atogepant or a pharmaceutically acceptable salt thereof.

Provided herein are sustained release biodegradable intracanalicular inserts comprising a hydrogel and an active agent, methods of treating or preventing an ocular disease in a subject in need thereof by administering such inserts as well as methods of manufacturing such inserts.

A method is disclosed for the treatment of human subjects diagnosed with immune thrombocytopenia (ITP). The method comprises administering to a human subject a human neonatal Fc receptor (hFcRn) antagonist, optionally in combination with standard-of-care ITP treatment. In certain embodiments, the hFcRn antagonist is efgartigimod (ARGX-113). Standard-of-care ITP treatment may comprise administration of corticosteroids, immunosuppressants, and / or thrombopoietin receptor (TPO-R) agonists.

The present disclosure provides methods and reagents useful for analyzing protein-protein interfaces such as interfaces between a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein. In some embodiments, the target and / or presenter proteins are intracellular proteins. In some embodiments, the target and / or presenter proteins are mammalian proteins.

The present inventors found cyclic peptide compounds that interact with Ras, and non-natural amino acids useful for the production of the cyclic peptide compounds. The inventors also found that the cyclic peptide compounds inhibit the binding between Ras and SOS. In addition, the inventors found specific non-natural amino acids contained in the cyclic peptide compounds and methods for production thereof.

The invention belongs to the technical field of medicines, and particularly relates to a disulfide cyclic peptide compound of a melanocortin receptor agonist based on polypeptide small molecules, and the disulfide cyclic peptide compound has the following structure: R2-R1-c (Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-R3-R4, wherein R2 and R4 are respectively and independently selected from an amino group, an acetyl group or a palmitoyl group; r1 and R3 are independently selected from Ile, Arg, D-Phe, Pro or deletion, R1 and R3 are not deleted at the same time, and when R1 or R3 is deleted, at least one of R2 and R4 is a palmitoyl group. The disulfide cyclopeptide compound provided by the invention has relatively good selectivity on melanocortin receptors (MCR1, MCR3, MCR4 and MCR5).

The invention discloses a cyclic hexapeptide for skin care and a composition and application thereof, and relates to the technical field of polypeptides, and the cyclic peptide has the following structure: Cyclo-[Arg-Arg-Gln-D-Met-Glu-Glu]. Specifically, the invention relates to the cyclic peptide or the salt thereof, or a composition of the cyclic peptide and the salt thereof, and application of the cyclic peptide and the salt in preparation of a composition for nursing or treating skin or mucosa.

Provided are methods of using a compound that binds to interleukin- 1 beta (IL- 1β) at a binding pocket of IL- 1β identified herein, which traps the IL- 1β and inhibits its interaction with interleukin- 1 receptor type I (IL-1R1).

The invention provides anti-inflammatory soothing application of cyclic dipeptide. The cyclic dipeptide is selected from cyclic (L-leucine-L-proline) dipeptide, cyclic (D-leucine-L-proline) dipeptide or a combination of the cyclic (L-leucine-L-proline) dipeptide and the cyclic (D-leucine-L-proline) dipeptide. The anti-inflammatory soothing of the present invention is achieved by inhibiting TNF [alpha], IL-1[ beta], IL-6, PGE2, COX2, TSLP and / or IL-33. The invention also relates to an application of the cyclic dipeptide in preparation of external skin agents, medicines and health-care foods with anti-inflammatory and soothing effects. The external skin agents are selected from face cream, emulsion, gel, toning lotion, essence, masks, eye cream, aerosol cleaning foam, spray, shower gel or facial cleanser.

The present invention relates to a controlled-release CNP agonist from which CNP agonist is released with a release half-life of at least 6 hours under physiological conditions and which controlled-release CNP agonist has an EC50 that is at least 20-fold higher than the EC50 of the corresponding free CNP agonist and which released CNP agonist has an EC50 that is at most 3-fold higher than the EC50 of the corresponding free CNP agonist; to pharmaceutical compositions comprising said controlled-release CNP agonist; their use; and to methods of treatment.

The present disclosure provides methods for the treatment of migraine by the administration of atogepant or a pharmaceutically acceptable salt thereof.

Described herein are cyclic peptides targeting fibroblast activation protein (FAP), and their incorporation into compounds for radioligand imaging and therapies, as well as methods and / or uses of such compounds for the imaging, treatment and / or prevention of FAP-implicated diseases and disorders.

The invention belongs to the technical field of gene engineering, and particularly relates to a mutant of polymyxin efflux transporter and application of the mutant. The mutant is a PmxD transporter mutant, the amino acid sequence of the PmxD transporter mutant is shown as SEQ ID NO: 1, and compared with wild type PmxD, the polymyxin transport capacity of the PmxD transporter mutant (T38W) is improved by 450.46%; and the total discharge amount of polymyxin is increased by 85.72%. Meanwhile, the mutant can significantly improve the growth ability of the strain on a plate containing 250 [mu] g / mL of polymyxin B, namely significantly improve the autoresistance of paenibacillus polymyxa to polymyxin.

Provided herein are novel cyclic peptides, their synthetic process, compositions, properties including stability and pharmacokinetic profiles, and applications for treating solid tumor cancers.

Disclosed herein are methods and compositions for preventing or reducing adverse events associated with administration of a RAS(ON) inhibitors. Thus, disclosed are compositions and methods for treating or preventing RAS(ON) inhibitor therapy-associated rash or mucositis. The methods involve administering a compound that binds to cyclophilin A (CypA) to compete with a RAS(ON) inhibitor for CypA binding, thereby reducing tri-complex formation in non-tumor tissues. These approaches may improve the tolerability of RAS(ON) inhibitor therapies without compromising efficacy.

The present application provides stable peptide-based Botulinum neurotoxin (BoNT) serotype A capture agents and methods of use as detection and diagnosis agents and in the treatment of diseases and disorders. The application further provides methods of manufacturing BoNT serotype A capture agents using iterative on-bead in situ click chemistry.

The present disclosure provides methods for the treatment of migraine by the administration of atogepant or a pharmaceutically acceptable salt thereof.

The invention provides a cyclic peptide as well as a preparation method and application thereof. The cyclic peptide has an amino acid sequence # imgabs0 # represented by formula (1) (wherein X is a Lys residue modified with a fatty acid molecule, and a line connecting Arg and Lys represents an amide bond. The cyclic peptide prepared by the invention has wide antifungal activity and antibacterial activity on drug-resistant bacteria; meanwhile, the biotoxicity and the protease degradation resistance are high, and the in-vivo antibacterial effect of the cyclopeptide can be prolonged. The cyclic peptide can be applied to preparation of anti-bacterial and anti-fungal infection drugs, and can be used as an excellent substitute drug or an auxiliary drug of existing antibiotics. The method for preparing the cyclic peptide is simple, raw materials are easy to obtain, and industrial production can be achieved.

The invention belongs to the technical field of biological medicine, and discloses application of magnolol as a polymyxin synergist in inhibition of salmonella. The application finds that the combination of magnolol and polymyxin has a good synergistic effect on salmonella in vitro and in vivo experiments. Compared with the traditional method of killing salmonella through combination of antibiotics, the method has the advantages that the magnolol and the polymyxin which are plant-derived synergistically kill bacteria, the generation of bacterial drug resistance is not easy to induce, and the magnolol has the characteristics of wide source, low price and good treatment effect; the method has good research and application significance for excavating antibiotic synergistic substitution and solving bacterial drug resistance.

The invention belongs to the technical field of medicines, and provides application of Nintedanib and a plant-derived cyclic peptide and radix pseudostellariae cyclic peptide B combined medicine in preparation of a medicine for treating pulmonary fibrosis, the Nintedanib and the plant-derived cyclic peptide and radix pseudostellariae cyclic peptide B combined medicine can play a synergistic effect, and the inhibition effect on the pulmonary fibrosis process is remarkably improved. The toxic and side effects of diarrhea and intestinal mucosa injury caused by nintedanib are reduced, and a good choice is provided for clinical treatment of pulmonary fibrosis.

In some aspects, the present invention provides cell-reactive compstatin analogs and compositions comprising cell-reactive compstatin analogs. In some aspects, the invention further provides methods of using cell-reactive compstatin analogs, e.g., treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides long-acting compstatin analogs and compositions comprising long-acting compstatin analogs. In some aspects, the invention further provides methods of using long-acting compstatin analogs, e.g., to treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides targeted compstatin analogs and compositions comprising targeted compstatin analogs. In some aspects, the invention further provides methods of using targeted compstatin analogs, e.g., to treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ.

In some aspects, the present invention provides cell-reactive compstatin analogs and compositions comprising cell-reactive compstatin analogs. In some aspects, the invention further provides methods of using cell-reactive compstatin analogs, e.g., treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides long-acting compstatin analogs and compositions comprising long-acting compstatin analogs. In some aspects, the invention further provides methods of using long-acting compstatin analogs, e.g., to treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides targeted compstatin analogs and compositions comprising targeted compstatin analogs. In some aspects, the invention further provides methods of using targeted compstatin analogs, e.g., to treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ.

The invention provides a coordination nano assembly of chiral cyclopeptide and manganese ions as well as a preparation method and application of the coordination nano assembly. According to the method, a manganese superoxide dismutase protein structural domain and a unique tumor microenvironment of melanoma high tyrosinase are combined, and polypeptide sequences L-YD-hL-DD-h, L-YL-HL-DL-H and D-yD-hD-dD-h with different chirality are designed for the first time; the chirality of the polypeptide is regulated and controlled, the in-vivo circulation stability and the cell entry efficiency of the nano assembly are improved, the coordination self-assembly of manganese and different chiral cyclopeptides is realized, and the in-situ oxidation of an in-vivo tumor microenvironment is simulated for photo-thermal therapy and cell membrane coating. The method disclosed by the invention is simple, mild in experimental condition and easy to operate, the prepared cell membrane coated nano assembly not only has long circulation stability and high cell entry efficiency, but also can realize mild photo-thermal therapy through in-situ oxidation, releases manganese ions to activate a CGAS-STING pathway for immunotherapy of tumors, and has a wide application prospect. The potential application value is realized in the field of combined treatment of tumors.

A method of preparing patients for cataract surgery includes topical administration of a cyclosporine solution. The administration may occur twice daily and may occur over the course of 28 days. The method results in an improved error prediction for 1-month spherical equivalent refractive outcome and improved ocular surface irregularity.

The present disclosure provides methods for the treatment of migraine by the administration of atogepant or a pharmaceutically acceptable salt thereof.

The invention discloses application of polypeptide compounds in prevention and treatment of pathogenic microorganisms. The compound has a synergistic effect on agricultural fungi such as rhizoctonia solani, Sclerotinia sclerotiorum, Botrytis cinerea, Fusarium graminearum, Pyricaria oryzae, pyricularia oryzae, pyricularia oryzae, pyricularia oryzae, pyricularia oryzae, pyricularia oryzae, pyricularia oryzae, pyricularia oryzae, pyricularia oryzae, pyricularia oryzae, pyricularia oryzae, pyricularia oryzae and pyricularia oryzae. The method comprises the following steps: carrying out sterilization on plant bacteria such as Xanthomonas oryzae PXO99A, Xanthomonas axonophora dispsp.citrijx-6, Pseudomonas solanacearum (Smith) BNCC335855, Pseudomonas sp. The method is characterized by comprising the following steps of: killing Aspergillus flavus ACCC32601 (Aspergillus flavus), Penicillium expansum ACCC 30898 (Penicillium expansum. EXPANSum ACCC 30898), Monilinia coerulea ACCC 36263 (Aspergillus oryzae, Aspergillus niger, Aspergillus niger, Aspergillus niger, Aspergillus niger, Aspergillus niger, Aspergillus niger, Aspergillus niger and Aspergillus niger); the compound disclosed by the invention has a certain inhibition activity on various diseases caused by streptococcus agalactiae ATCC 27956, streptococcus dysgalactiae ATCC27957, Escherichia coli ATCC 25922 and Staphylococcus aureus, particularly, the compound Thiostreptin has a particularly remarkable inhibition effect on agricultural pathogenic bacteria, food-borne germs and cow mastitis germs, and is expected to be developed into a novel antibacterial drug, so that the compound disclosed by the invention can be used for preparing the antibacterial agent for preventing and treating various diseases caused by the streptococcus agalactiae ATCC 27956, the streptococcus dysgalactiae ATCC27957, the Escherichia coli ATCC 25922 and the Staphylococcus aureus.