1810results about "Cyclic peptide ingredients" patented technology

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 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 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 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.

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.

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.

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

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 discloses an application of NSC348884 in preparation of an antibacterial drug, the bacteria of the NSC348884 are gram-negative bacteria or drug-resistant gram-negative bacteria, and the gram-negative bacteria are acinetobacter baumannii, escherichia coli, pseudomonas aeruginosa or klebsiella pneumoniae; based on an antibacterial drug high-throughput screening technology, it is found from 1280 small molecule compounds that the benzimidazole compound NSC348884 has direct bacteriostasis and sterilization effects on gram-negative bacteria and drug-resistant gram-negative bacteria, and no drug resistance is generated after the benzimidazole compound NSC348884 is continuously applied for 14 days. Further research shows that NSC348884 can interfere with lipid synthesis of gram-negative bacterium cell membranes, inhibit formation of biological membranes and induce lipid metabolism disorder, so that bacteriostatic and bactericidal effects are achieved. In addition, the NSC348884 can also enhance the sensitivity of the drug-resistant bacteria to the imipenem and the polymyxin B.

The invention provides a pharmaceutical composition, glycyrrhizic acid and polymyxin B self-assembled carrier-free hydrogel as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The invention provides a pharmaceutical composition. The pharmaceutical composition comprises glycyrrhizic acid and polymyxin B. According to the pharmaceutical composition, the inhibition effect on MRSA is enhanced through drug combination, the use of polymyxin B is reduced through the synergistic effect, and the development pressure of antibiotic drug resistance is relieved. According to the hydrogel formed by crosslinking the glycyrrhizic acid and the calcium chloride, the glycyrrhizic acid and the calcium chloride are crosslinked to form the hydrogel, and the calcium chloride is introduced into a glycyrrhizic acid system to increase the mechanical strength of the glycyrrhizic acid hydrogel, so that the glycyrrhizic acid hydrogel can be better attached to a wound. The invention provides a glycyrrhizic acid and polymyxin B self-assembled carrier-free hydrogel and a preparation method of the glycyrrhizic acid and polymyxin B self-assembled carrier-free hydrogel. The hydrogel does not contain any inert carrier component at all, the drug loading rate of 100% is achieved, and adverse reactions possibly caused by a traditional carrier system are effectively avoided.

The present invention relates to a heterotandem bicyclic peptide complex which comprises a first peptide ligand, which binds to Nectin-4, conjugated via a linker to two second peptide ligands, which bind to CD137. The invention also relates to the use of said heterotandem bicyclic peptide complex in preventing, suppressing or treating cancer.

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

Provided are β-eliminative linkers suitable for the conjugation of small molecule, peptide, and protein and compounds comprising the linkers.

The present disclosure provides daptomycin formulations which have improved chemical stability, faster reconstitution times when reconstituted from the solid state and longer in-use stability. The compositions comprise daptomycin, one basic amino acid or its salt and optionally one or more pH adjusting agents.

The present invention relates to a composition comprising a compound represented by general formula (1), a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, and a surfactant. [wherein R1, P1, R2, P3, P4, R5, P6, R10, P10 and P11 are C1 to C6 alkyl or the like; R3 and P9 are hydrogen or the like; R7 is phenethyl optionally substituted by halogen or the like; R8 forms a 4-to 7-membered saturated heterocyclic ring together with a carbon atom bonded to P8 and R8 and a nitrogen atom bonded to P8; R9 forms a 3- to 8-membered alicyclic ring together with Q9 and a carbon atom bonded to R9 and Q9; and R11 is di-C1 to C6 alkylaminocarbonyl or the like].

A nanomedicine composition, preparation method, and use thereof, comprising: a negatively charged nanophospholipid disk and an antimicrobial compound; wherein the negatively charged nanophospholipid disk comprises a negatively charged phospholipid layer and a membrane scaffold protein, wherein the negatively charged phospholipid layer is formed by mixing a neutral phospholipid and a negatively charged phospholipid in a molar ratio of approximately 5:5-7:3. The nanomedicine composition provided herein reduces the toxicity of the antimicrobial compound while enhancing its antimicrobial efficacy, and has great potential for expansion into clinical applications.

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.

Provided herein are non-naturally occurring melanocortin analogs that selectively bind at least a portion of a melanocortin receptor The melanocortin receptor may be a melanocortin 3 receptor (MC3R) or a melanocortin 4 receptor (MC4R). The non-naturally occurring melanocortin analogs may have a dissociation constant (Kd) value for a melanocortin receptor or one or more amino acids thereof that is less than that of a conventional melanocortin analog.

In particular, the present invention provides techniques involving immune cells and antibody-recruiting molecules. In some embodiments, the immune cells are memory-like natural killer cells. In some embodiments, the provided techniques are particularly useful for conditions, disorders, or diseases such as cancer. In some embodiments, the provided techniques provide high efficacy. In some embodiments, the provided techniques provide fewer or less severe side effects associated with natural killer cell therapy.

The invention belongs to the technical field of contact lens care, and provides temperature-sensitive contact lens eye-moistening gel and a preparation method thereof. The temperature-sensitive contact lens eye-moistening gel is prepared from the following raw materials in parts by mass: a gel matrix, a surfactant, an osmotic pressure regulator, an active component, a chelating agent, a buffering agent and the balance of injection water, the composition of the gel matrix is defined. Chitosan, sodium hyaluronate and polyvinyl alcohol are compounded to serve as a gel matrix, a polyelectrolyte compound is formed, gelation time is shortened, gel strength and swelling resistance are improved, biocompatibility is improved, and drug-loaded delivery of active ingredients is achieved; the gel matrix and the surfactant are reasonably selected, the viscosity of the solution is increased, the gelation time is shortened, the excellent effect of relieving eye fatigue and dryness is achieved, the wearing comfort of the contact lens is remarkably improved, and the oxygen permeation effect of the contact lens is not obviously reduced after gel forming.

The invention provides pharmaceutical compositions comprising about 0.05 to 0.1% (w / v) cyclosporine dissolved in 1-perfluorobutyl-pentane for use in the topical treatment of dry eye disease and provides for dosing and treatment methods thereof. The invention further provides kits comprising such compositions.

Provided herein are non-naturally occurring melanocortin analogs. The non-naturally occurring melanocortin analogs of the present technology may be useful in treating, preventing, reducing, or otherwise ameliorating one or more disorders associated with the melanocortin system. In some embodiments, the non-naturally occurring melanocortin analog is administered orally to a subject in need thereof.

The present application provides peptides having affinity for the focal adhesion targeting (FAT) domain of focal adhesion kinase (FAK). In particular, the peptides are modified and derived from the sequences of the LD2 alpha helix domain of paxillin (e.g., LD2 peptide), the LD4 domain of paxillin (e.g., LD4 peptide), and the CD8 peptide. These peptides interfere with the interaction between paxillin and FAK, thereby inhibiting FAK activity associated with FAK-paxillin interaction. The present invention further provides the use of the peptides as therapeutic agents for the treatment of cancer and other diseases characterized by FAK activity and / or expression (e.g., fibrosis).

The present invention relates to novel somatostatin 4 (SST4) selective agonists as non-opioid analgesics. In particular, the present invention relates to peptides having strong SST4-selectivity for use in treatment of pain or inflammation.

Provided are β-eliminative linkers suitable for the conjugation of small molecule, peptide, and protein and compounds comprising the linkers.