1021results about "Cyclic peptide ingredients" patented technology

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.

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 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 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.

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 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].

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

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 a cyclic peptide compound BIM 23042 or a preparation thereof in preparation of medicines for treating bacterial infectious diseases, and belongs to the technical field of medicines. The invention discloses a cyclic peptide compound BIM 23042 as an antibiotic synergist for the first time, and the cyclic peptide compound BIM 23042 is used for treating bacterial infectious diseases. According to the application disclosed by the invention, the cyclopeptide compound BIM 23042 and polymyxin are combined for use, so that the growth of gram-negative bacteria can be effectively and synergistically inhibited. The combined medication scheme shows a remarkable advantage in coping with acinetobacter baumannii. The cyclic peptide compound BIM 23042 disclosed by the invention has an anti-infection capability, and the anti-infection capability is specifically shown as reducing the inflammatory response of macrophage RAW 264.7 induced by LPS (Lipopolysaccharide) and also reducing the apoptosis of the macrophage RAW 264.7 caused by the LPS. The invention provides a new perspective for developing a novel drug-resistant gram-negative bacterium prevention and control strategy, and also provides a new treatment scheme for coping with bacterial infection.

A pharmaceutical composition for treating triple-negative breast cancer is provided. The active ingredients of the pharmaceutical composition include actinomycin D and doxorubicin, both of which are chemotherapy drugs. The synergistic effect between actinomycin D and doxorubicin enables the pharmaceutical composition to bind to a specific nucleic acid sequence in a targeted manner, thereby treating or suppressing triple-negative breast cancer not only with a reduced dose of doxorubicin, but also with effectively reduced side effects of those chemotherapy drugs.

The present disclosure provides methods of treating inflammatory indications with complement inhibitor compounds and compositions. Included are compounds and methods of treating neuromuscular inflammatory indications, such as Immune-Mediated Necrotizing Myopathy.

This invention relates to soba tertide (N succinyl-[Glu 9 ,Ala 11,15 This invention relates to a composition for promoting the proliferation and protection of existing neuroepithelium of cochlear and vestibular cells located within the otolaryngeal vesicle using endothelin B receptor agonists such as endothelin 1 (IRL-1620). The composition is administered systemically via transtympanic membrane, cochlear fenestration, or intravenously or intramuscularly. This invention also relates to a method for treating sensorineural hearing loss and vestibular symptoms caused by inner ear cell degeneration by using compounds containing endothelin analogs, through mechanisms of neuroprotection and neurogenesis of cochlear vestibular hair cells and synapses.

The present invention relates to solid state forms of lenicortafusp (RCF), pharmaceutical compositions comprising the solid state forms and methods of manufacturing pharmaceutical dosage forms utilizing the solid state forms.

The present invention relates to the technical field of medicine, and specifically relates to a disulfide cyclic peptide compound of a polypeptide small molecule-based melanocortin receptor (MCR) agonist. 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 each independently selected from an amino group, an acetyl group or a palmitoyl group, R1 and R3 are each independently selected from Ile, Arg, D-Phe, or Pro, or deleted, 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 cyclic peptide compound provided by the present invention has good selectivity to MCRs (MCR1, MCR3, MCR4, and MCR5).

The invention provides novel pharmaceutical compositions of polymyxin B / trimethoprim and rifampin, as well as methods of their preparation and topical ophthalmic uses (e.g., treatment of ophthalmic infections).

Providing nanoparticles for use in the treatment of eye diseases. [Solution] The present invention relates to nanoparticles for use in a method of effectively preventing or treating one or more inflammatory components, immune response components, angiogenic components and neuropathic components of retinal disease or optic neuropathy in patients, comprising: a core containing a drug having one or more of the following: anti-inflammatory activity, immunosuppressive activity, anti-angiogenic activity, neuroprotective activity, gene therapy activity and gene expression regulatory activity; an amphiphilic shell surrounding the core, the amphiphilic shell comprising at least one phospholipid and optionally at least one surfactant; and a targeted ligand covalently bound to the amphiphilic shell, which binds to receptors expressed on the surface of retinal pigment epithelial (RPE) cells and / or endothelial cells and / or optic nerve cells.

This disclosure provides methods and reagents useful for analyzing protein-protein interfaces, such as the interface between a presenter protein (e.g., a member of the FKBP family, a member of the cyclophyllin family, or PIN1) and a target protein. [Solution] In some embodiments, the target and / or presenter protein is an intracellular protein. In some embodiments, the target and / or presenter protein is a mammalian protein.

Embodiments of the present invention relate to a novel compound of Formula (I)or stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, for use in treatment of infection caused by Gram-negative bacteria.

The present invention relates to novel compositions, in particular aqueous solution compositions having a pH in the range of 4.0 to 7.5 comprising: a peptide therapeutic agent; optionally one or more buffering agents, which are substances having at least one ionizable group with a pKa in the range of 3.0 to 8.5 and the pKa is within 2 pH units of the pH of the composition; and a stabilizer; wherein the peptide therapeutic agent does not contain an ionizable group with a pKa in the range of 3.0 to 8.5 and wherein the buffering agent(s) is present in the composition in a total concentration of 0 to 5 mM.

The present disclosure relates to a process for preparing anidulafungin derivatives, particularly to a process for preparing anidulafungin derivatives represented by formula (I) and intermediates thereof. JPEG2024520500000021.jpg82170

A polyclonal antibody composition specifically binds the pTonB epitope (SEQ ID NO: 11) from Acinetobacter baumannii and is elicited by immunization with a multi-epitope antigen comprising thioredoxin leader, rigid linker, and kernels including SEQ ID NOs: 6, 7, 11, 12, and 8. These antibodies enhance opsonophagocytic killing of A. baumannii Ci79 via classical complement activation and Fey receptor-mediated phagocytosis by bone marrow-derived macrophages. Absorption of pTonB-specific antibodies reduces killing by >70%, confirming epitope dominance. Passive transfer of the composition protects >60% of mice in a lethal intranasal challenge model. Pharmaceutical compositions, treatment methods (alone or with antibiotics like colistin), prophylactic uses, diagnostic kits, and polyclonal compositions are disclosed for combating multidrug-resistant A. baumannii infections.

The present invention relates to a composition comprising tigolaner and, optionally endoparasiticidal agents, a method for its manufacture and its use as a medicament for controlling parasites. Compositions can include tigolaner and 1,2-isopropylideneglycerol, or the composition can include praziquantel, emodepside a solvent component, and tigolaner. The composition can be used in the treatment and / or prevention of parasite infections in animals.

The present application relates to the technical field of medicine, and specifically includes the application of immunosuppressants in the preparation of drugs for treating pulmonary hypoperfusion type congenital heart disease, and further provides a premature infant pulmonary hypoperfusion animal model, and results show that lung development is significantly improved after using immunosuppressants. The present application verifies the Wnt pathway which is critical for lung development, indicates that immunosuppressants can improve the Wnt pathway changes caused by pulmonary hypoperfusion, confirms that immunosuppressants have a therapeutic effect on the pulmonary hypoperfusion type congenital heart disease caused by pulmonary hypoplasia, provides a new method and idea for improving lung development of such children, and thereby improves the long-term survival quality of congenital heart disease children in China.

The invention relates to a sulfur-containing tryptophan cyclic peptide compound as well as a synthesis method and application thereof. The synthesis method comprises the following steps: carrying out electrolytic reaction on a tryptophan peptide compound with a structure as shown in a formula I or a stereoisomer thereof and a thiosulfonate compound with a structure as shown in a formula II to obtain the sulfur-containing tryptophan cyclic peptide compound with a structure as shown in a formula III or a stereoisomer thereof. The sulfur-containing tryptophan cyclic peptide compound can be obtained by directly electrolyzing the tryptophan peptide compound by adopting an electrochemical method, so that the use of a transition metal catalyst and stoichiometric alkali is avoided, the generation of chemical wastes is avoided, and the realization of atom economy is facilitated. The method has the advantages of simple operation, high product purity, easy purification, high efficiency and yield, low production cost, mild reaction conditions, no need of inert gas protection, greener reaction system, environmental protection, safety, economy, energy saving and environmental protection, and is more conducive to realization of industrial production.

The present invention provides a cyclic peptide and a method of using the cyclic peptide for, among other things, ameliorating or treating K63Ub-related diseases in a subject in need thereof.

To provide peptides and compositions useful for treatment of gastrointestinal disorders or for colon cleansing.SOLUTION: The present invention provides compositions and methods of treating gastrointestinal disorders as well as pharmaceutical compositions for accomplishing the same. In some embodiments, these pharmaceutical compositions include oral dosage forms. The present invention features peptides, compositions and related methods for colon cleansing treatment as well as other conditions and disorders described herein. In one embodiment, the peptides may be used to prepare subjects for colonoscopy treatment. In some embodiments, the peptides or pharmaceutically acceptable salts may be used to prepare subjects for surgery, such as bowel surgery.SELECTED DRAWING: None