830 results about "Cyclic peptide" patented technology

Compositions and methods are provided for treating diseases associated with aberrant silencing of gene expression such as cancer by reestablishing the gene expression through inhibition of DNA hypomethylation and histone deacetylase. The method comprises: administering to a patient suffering from the disease a therapeutically effective amount of a DNA methylation inhibitor such as a cysteine analog such as decitabine, in combination with an effective amount of histone deacetylase inhibitor such as hydroxamic acid, cyclic peptide, benzamide, butyrate, and depudecin.

Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein:wherein m, n, p, R′, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.

The present provides cyclic compounds capable of modulating IgE production, as well as IL-4 induced processes associated therewith, and methods of using the cyclic compounds in a variety of in vitro and in vitro contexts.

Novel protected cyclopeptide intermediates are prepared from polymyxin B are used to synthesize new peptide antibiotics. Intermediates are readily derivatized and deprotected to provide new families of antibiotics, which have potent anti-bacterial activity against gram-negative bacteria; but also are useful and potent against gram-positive bacteria.

Provided herein are cyclic peptide inhibitors of lysine-specific demethylase 1. These cyclic peptides have the potential to treat cancer, diabetes, cardiovascular disease, and neurological disorders.

Small cyclic peptides of the formula X1-X2-X3-X4-X5-X6-X7-R1 comprising 7-12 amino acid residues are provided. Said peptides are MC4 receptor agonists, and thus useful in the treatment of obesity and related diseases.

A cyclic peptide of the structural formula: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, m and p are as defined. Further provided are compositions for treatment of sexual dysfunction in mammals, including male sexual dysfunction, such as erectile dysfunction, and female sexual dysfunction, by administration of a cyclic peptide including a C-terminus —OH group. Routes of administration include injection, oral, urethral, vaginal, nasal and mucosal administration.

This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.

Melanocortin receptor-specific cyclic peptides of the formulawhere R1, R2, R3, R4, x and y are as defined in the specification, compositions and formulations including the peptides of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes, including obesity, diabetes, modulation of feeding behavior and related metabolic syndrome.

Methods are provided for treating hematological disorders by inhibition of DNA hypomethylation and histone deacetylase. Such disorders include, for example, acute promyelocytic leukemia, acute lymphoblastic leukemia, chronic myelogenous leukemia, myelodysplastic syndromes, and sickle cell anemia. The methods comprise: administering to a patient suffering from the disease a therapeutically effective amount of a DNA methylation inhibitor such as a cysteine analog such as decitabine, in combination with an effective amount of histone deacetylase inhibitor such as hydroxamic acid, cyclic peptide, benzamide, butyrate, and depudecin.

The present invention relates to biologically active compositions and methods forelliciting an immune response, particularly against amyloid beta peptides by combinatory use of virosomes as adjuvants and a synthetic beta-peptide antigen.

Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein:wherein m, n, p, R′, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.

The present invention relates to the preparation of cyclic peptide, and is especially new Fmoc-solid phase process of preparing Eptifibatide. The new process is superior to liquid phase process, which has long synthesis period, and BOC solid phase process, which uses virulent and corrosive material. The technological scheme is that the Eptifibatide preparing process includes the following steps: eliminating Fmoc protection of Fmoc-Rink Amide AM resin to obtain H2N-Rink Amide AM resin; connecting various protective amino acids successively to obtain corresponding resin; eliminating Fmoc-protection radical and Kaiser test to detect reaction procedure; preparing S-triphenyl mercapto propionyl-N, N-ditert butyl oxycarbonyl-homoarginine with lysine; grafting S-triphenyl mercapto propionyl-N, N-ditert butyl oxycarbonyl-homoarginine; eliminating side chain protecting radical and resin to reduce into coarse product; and cyclization, oxidation, HPLC tracking purification to obtain pure product.

The invention relates to a multi-function nano prodrug system based on a dendrimer, which belongs to the technical field of biomedicines and nano medical science. The nano system comprises four function parts: an outermost layer RGD (arginyl-glycocoll-aspartate) cyclic peptide as an active targeting head group (1), a polyethylene glycol (PEG) hydrophilic chain segment (2) connected with the targeting head group and the dendrimer, an anti-tumour drug (3) connected with the dendrimer by an acid sensitive chemical bond and a dendrimer kernel (4). The general formula of the nano system is RGD-PEG-Dendrimer-DOX (doxorubicine), wherein the macromolecule attribute of a dendrimer vector makes a vector system passively target to tumor tissues through an EPR (Enhanced Permeability and retention) effect; the RGD cyclic peptide makes the vector system actively target to the tumor tissues through the interaction of a ligand and a receptor and promotes the endocytosis of the tumor tissues; the acid sensitive chemical bond ensures that a drug-carrying system is stable in systemic circulation and releases active drugs after arriving tumor positions and entering an acid organelle to perform the function of cytotoxicity.

The present invention relates to novel cyclic peptides that may be conjugated with imaging agents, including novel imaging agents. Specifically, it includes c(KRGDf) NIR imaging compositions and novel cyclic HWGFTL polypeptides which may be used inter alia in NIR, MRI and nuclear imaging as well as therapy. Additionally, the invention includes novel imaging agents, such as TS-ICG derivatives. The invention also relates to methods of making and using such compounds. Such uses include both pre-operative and intraoperative detection of tumor cells and treatment monitoring.

A melanocortin receptor agonist cyclic peptide of the formulawhere R, x and y are as defined in the specification, compositions and formulations including the peptide of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes, including sexual dysfunction such as male erectile dysfunction and female sexual dysfunction.

The present invention relates to a novel class of diagnostically or therapeutically effective compounds comprising novel aza-bicycloalkane based cyclic peptides, acting as a targeting moiety towards integrin receptors.

The invention discloses a preparation method of RGD-modified ultra-small magnetic iron oxide nanoparticles. The preparation method comprises the following steps: preparing ultra-small magnetic iron oxide nanoparticles by taking ferric acetylacetonate as a reaction raw material and a precursor, taking oleylamine as a surfactant and a reducing agent and taking dibenzyl ether as a solvent; replacing oleylamine molecules wrapped on the surfaces of the nanoparticles by utilizing dopamine-modified HOOC-PEG-COOH to realize PEG-modification of the surfaces of the nanoparticles; and finally, chemically coupling RGD cyclic peptide by virtue of free carboxyl at the tail end of the PEG to obtain the RGD-modified ultra-small magnetic iron oxide nanoparticles. The method of synthesizing the ultra-small magnetic iron oxide nanoparticles has the characteristics of a simple process, a high raw material conversion ratio, strong repeatability and the like. The synthesized magnetic iron oxide nanoparticles have the characteristics of a regular morphology, an ultra-small dimension, good stability, good monodispersity, high biocompatibility, and tumor specific targeting, and the like, and can be used as a T1-weighted imaging high-performance magnetic resonance imaging contrast agent with a tumor active targeting function.

A highly selective melanocortin-4 receptor antagonist cyclic hexapeptide of the formula where R1, R2, R3a, R3b, R4, R5, x, y and z are as defined in the specification, and a method of treating body weight disorders, including cachexia, sarcopenia and wasting syndrome or disease, and treating inflammation and immune disorders.

Disclosed is a process for preparing a compound of formula (I) by protecting the secondary amide nitrogen atom in the compound of formula (III) to obtain (IV) wherein PGN is a suitable nitrogen protecting group, ring-closing the compound of formula (IV) by cyclizing it in the presence of a suitable catalyst in a suitable organic solvent to obtain (V), and then deprotecting the resulting compound of formula (V) to obtain (I), as outlined in the following scheme. The compounds of formula (I) are active agents for the treatment of hepatitis C viral (HCV) infections or are intermediates useful for the preparation of anti-HCV agents.

Disclosed is a cyclic peptide antibiotic in which an enzyme-sensitive bond is replaced by an enzyme-resistant bond.

The present invention relates to compositions and methods comprising genes and peptides associated with cyclic peptide toxins and toxin production in mushrooms. In particular, the present invention relates to using genes and proteins from Amanita species encoding Amanita peptides, specifically relating to amatoxins and phallotoxins. In a preferred embodiment, the present invention also relates to methods for detecting Amanita peptide toxin genes for identifying Amanita peptide-producing mushrooms and for diagnosing suspected cases of mushroom poisoning. Further, the present inventions relate to providing kits for diagnosing and monitoring suspected cases of mushroom poisoning in patients.

The invention relates to novel cyclic compounds which have the ability to modulate the activity of G protein-coupled receptors. The compounds preferably act as antagonists. In preferred embodiments, the invention provides cyclic peptidic and peptidomimetic antagonists of C5a receptors, which are active against C5a receptors on polymorphonuclear leukocytes and macrophages. The compounds of the invention are both potent and selective, and are useful in the treatment of a variety of inflammatory conditions.

A highly selective melanocortin-4 receptor antagonist cyclic peptide of the formulawhere R1, R2, R3, R4a, R4b, R5, R6, R7, x, y and z are as defined in the specification, and a method of treating body weight disorders, including cachexia, sarcopenia and wasting syndrome or disease, and treating inflammation and immune disorders.

The invention relates to an RGD polypeptide radiopharmaceutical and a preparation method thereof. The RGD polypeptide radiopharmaceutical includes an RGD polypeptide and a radionuclide<99m>Tc, wherein, the RGD polypeptide radiopharmaceutical is an RGD cyclopeptide dimmer, that is, E(L-cRGDxK)2 which is synthesized by dimerizing two RGD polypeptide monomers connected with coupling agent L. The radionuclide<99m>Tc serves to mark the RGD cyclopeptide dimmer through a bifunctional chelating agent HYNIC. A pharmacokinetics modified molecule PKM is further connected between the RGD cyclopeptide dimmer and the bifunctional chelating agent. The RGD polypeptide radiopharmaceutical is <99m>Tc-HYNIC-PKM-E(L-cRGDxK)2. The RGD polypeptide radiopharmaceutical is colorless and transparent liquid injection. The RGD polypeptide radiopharmaceutical provided by the invention has the advantages of further reinforcing the binding affinity and the ingestion of drugs by tumor, and achieving better diagnosis effect.

The present invention relates to methods and compositions utilizing inteins to generate libraries of cyclic peptides in vivo. The prevent invention also relates to methods for inhibiting protein-protein interaction.

The present invention relates to methods and compositions utilizing inteins to generate libraries of cyclic peptides in vivo. The prevent invention also relates to methods for inhibiting protein-protein interaction.

The present invention relates to heterotandem bicyclic peptide complexes which comprise a first peptide ligand, which binds to a component present on an immune cell, conjugated via a linker to a second peptide ligand, which binds to a component present on a cancer cell. The invention also relates to the use of said heterotandem bicyclic peptide complexes in preventing, suppressing or treating cancer.