2407results about "Cyclic peptide ingredients" patented technology

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 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.

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.

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 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 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.

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.

Methods and compositions for inducing long-term tolerance by hybrid nanoparticles are provided. Compositions and formulations comprising hybrid nanoparticles with inherent affinity for innate immune cells are provided.

A method for treating a flavivirus infection includes administering to a subject in need thereof a composition which includes at least one of gentamicin sulfate, netilmicin, tobramycin, paromomycin, amikacin, capreomycin, trifluoperazine, dihydrostreptomycin, hydroxychloroquine, thioridazine HCl, efavirenz, miltefosine, nystatin, micafungin, bleomycin, resminostat, montelukast, norfloxacin, nedaplatin and cephalothin, which can exhibit excellent growth inhibition or killing effects of various species of flavivirus genus.

The invention relates to a turtle-derived cyclic peptide compound with an anti-tumor effect and a preparation method thereof. The preparation method comprises the following steps: crushing tortoise plastron, adding water for reflux extraction, filtering, concentrating and drying to obtain tortoise-shell glue; dissolving the obtained tortoise-shell gelatin in water, adding protease for enzymolysis, and centrifuging after enzyme deactivation to take supernate; carrying out graded filtration on the obtained supernate and collecting components; and separating and purifying the collected components to obtain the cyclic peptide. The obtained compound has remarkable anti-tumor activity and has a good application prospect in preparation of anti-tumor drugs.

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

The invention relates to the field of biological medicine, in particular to a carrier-free nanoparticle which is formed by self-assembly of cyclosporine A and costunolide through intermolecular weak interaction. The invention also provides a preparation method of the traditional Chinese medicine composition and application of the traditional Chinese medicine composition in preparation of medicines for treating xerophthalmia. The carrier-free nano eye drops based on the synergistic effect of Chinese and western medicines are used for anti-inflammatory treatment of the xerophthalmia, a new strategy is provided for precise diagnosis and treatment of the xerophthalmia, the problems of single target spot, limited curative effect and the like in traditional treatment are solved, and more efficient inflammation control is expected to be achieved. While the curative effect is improved, the tolerance risk caused by long-term use is reduced, double optimization of the curative effect and safety is realized, and the limitation of traditional single drug treatment is broken through. By adopting the carrier-free nano preparation, the delivery efficiency of the medicine on the ocular surface is effectively improved, the bioavailability is enhanced, powerful support is provided for improving the curative effect of the medicine, and the carrier limitation bottleneck is broken through.

A protein carrier-based active ingredient transdermal delivery system, which is a small molecule active ingredient-protein-polymer composite structure and comprises a small molecule active ingredient, a protein loaded with the small molecule active ingredient, and a polymer coating a surface of the protein. The protein is modified with a polymerizable double-bond compound. After the loading of the small molecule active ingredient, a polymerization reaction is initiated on the surface of the protein in situ, so that the surface of the protein is coated with a polymer layer. The polymer layer is biologically friendly, and the surface properties of the polymer layer can be regulated and controlled according to the transdermal depth requirement, thereby achieving the targeted transdermal delivery of proteins and active small molecules while breaking through the skin barrier, and significantly overcoming the defect of poor delivery efficiency of previous protein-based delivery systems. The transdermal delivery system has a simple preparation method with a high yield, and thus can be industrially produced on a large scale.

The present invention relates to a root extract of Pseudostellaria heterophylla comprising: - one or more phenolic components, - one or more pseudostellarins, - one or more heterophyllins including heterophyllin B, wherein heterophyllin B represents at least 0.5% by weight relative to the total weight of the dry extract. The invention further relates to the cosmetic use of the said extract.

Provided herein are pharmaceutical formulations and pharmaceutical compound salts which utilize complexing agents as counterions. Such formulations and salts are useful for treating a variety of disease and disorders. Provided herein are also treatment methods using the pharmaceutical compounds, pharmaceutical compositions, and pharmaceutically acceptable salts of the present disclosure.

Described herein are methods and pharmaceutical formulations for treating dry eye disease.

The disclosure describes compounds of Formula (I) and Formula (II), which in non-limiting aspects contain an asialoglycoprotein receptor (ASGPR) binding moiety and an anti-β1AR binding moiety. Compounds of Formula (I) and Formula (II) are useful in preventing, treating and / or ameliorating heart failure in a subject when administered therapeutically effective amounts.

The invention provides an application of a human retina organ in preparation of a medicament for treating traumatic optic neuropathy. According to the invention, the induced and differentiated human retina-like organ is applied to the optic nerve injury area, and the eye and brain nerve connection can be functionally reconstructed, so that the damaged visual function is recovered.

The invention relates to a cyclopeptide inhibitor aiming at human STING (stimulating interferon gene) and application of the cyclopeptide inhibitor. The cyclic peptide can specifically bind to and inhibit activation of human STING. The invention also provides a nanoparticle delivery system for loading the cyclopeptide on a cationic polymer PBAE and an amphiphilic polymer pDMA-pEPEMA, and a preparation method of the nanoparticle delivery system. The cyclic peptide and the nanoparticles thereof can be used for preparing medicines for treating autoimmune diseases (such as systemic lupus erythematosus and the like) caused by excessive activation of the cGAS-STING signal pathway. Compared with the existing small molecule STING inhibitor, the cyclopeptide inhibitor provided by the invention has higher specificity, stability and inhibition effect.

The invention relates to the technical field of biological materials, in particular to a cyclic peptide derivative and a preparation method and application thereof. The cyclopeptide derivative provided by the invention simultaneously comprises a hydrophobic cyclopeptide structure and a hydrophilic pantothenic acid structure which are combined through a covalent ester bond; due to the structure, excellent stability is achieved, and the problems that pantothenic acid is unstable and irritant are effectively solved; after entering the skin, the derivative can be hydrolyzed into pantothenic acid under the action of esterase, and can play a role without oxidative conversion of panthenol. Secondly, the cyclic peptide derivative disclosed by the invention has good biological safety; in an inflammatory cell model, the derivative can more effectively reduce expression of inflammatory factors, and antioxidant activity research shows that the derivative has a strong free radical inhibition effect and can exert excellent anti-inflammatory and antioxidant effects.