104 results about "Peptide receptor" patented technology

The present application relates to heterobicyclic compounds having glucagon-like peptide receptor (GLP-1R) agonist activity, processes for their preparation, pharmaceutical compositions comprising them and their use as GLP-1R agonists or for the treatment or prophylaxis of GLP-1R associated diseases or disorders. In particular, the compounds of the present application are useful for body weight management, for lowering blood sugar and / or for the treatment or prevention of diabetes, diabetic complications, obesity, overweight, dyslipidemia, fatty liver diseases (e.g., non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH)), metabolic diseases, cardiovascular diseases, nervous system disorders, mental disorders, kidney diseases, etc. , gastrointestinal diseases, autoimmune diseases, inflammatory diseases, lung diseases, hypothalamic-pituitary-gonad axis related diseases or disorders, cancers and the like.

The invention discloses a formyl peptide receptor 1 polypeptide blocker for resisting acute lung injury and pharmaceutical application thereof. The invention provides a polypeptide with a sequence as shown in Sequence NO.1, and the polypeptide is reported for the first time. Pharmacological activity studies show that the polypeptide shown as Sequence NO.1 can significantly improve lung tissue structure damage of acute lung injury model mice, reduce the level of proinflammatory factors and reduce neutrophil infiltration, and shows an obvious acute lung injury resisting effect. Therefore, the polypeptide as shown in the Sequence NO.1 provided by the invention has a prospect of being developed into the acute lung injury resisting medicine. Specifically, the polypeptide shown as Sequence NO.1 can be used as a unique active ingredient for preparing the medicine for treating and resisting the acute lung injury, and can also be combined with other active ingredients to form a composition for preparing the medicine for treating and resisting the acute lung injury.

To provide a radionuclide complex solution of high concentration and high chemical stability which can be used as a medicine for diagnosis and / or treatment.SOLUTION: Provided is a pharmaceutical composition comprising: (a) a complex formed by: (ai) a radionuclide; and (aii) a gastrin releasing peptide receptor peptide antagonist binding moiety linked to a chelating agent; (b) at least two stabilizers against radiolysis; and (c) optionally a surfactant.SELECTED DRAWING: None

The present invention relates to a process for preparing the compound of Formula I in the form of a base or a salt thereof, and its use as an intermediate for the preparation of calcitonin gene- related peptide (CGRP) receptor antagonist active pharmaceutical ingredients, in particular zavegepant, where the compound of Formula I is the following: (I)

Methods and materials for treating mammals having cardiovascular and / or metabolic disease are provided herein. For example, methods and materials for treating mammals having cardiovascular and / or metabolic disease by administering (a) an analog of a natriuretic peptide (NP), such as atrial natriuretic peptide (ANP) or dendroaspis natriuretic peptide (DNP), and (b) a glucagon-like peptide-1 (GLP-1) receptor / glucose-dependent insulinotropic polypeptide (GIP) receptor agonist are provided herein. The NP analogs used in the methods provided herein can be less than 20 amino acids in length and, in some cases, can have one or more variations in their ring portion (as compared to wild type ANP or DNP) that affect the potency of the analog in activating the particulate guanylyl cyclase (GC-A) receptor.

There is provided a pharmaceutical formulation useful for the treatment of a metabolic disorder or condition, the pharmaceutical formulation comprising a plurality of particles suspended in a carrier system, the particles: (a) having an average diameter based on weight, quantity or volume of between about 10 nm and about 700 [mu] m; and (b) comprises a solid core comprising at least one glucagon-like peptide-1 receptor agonist or a pharmaceutically acceptable salt thereof, said solid core being at least partially coated by an inorganic material coating comprising a mixture of (i) zinc oxide; and (ii) one or more other metal oxides and / or metalloid oxides, wherein the atomic ratio ((i): (ii)) is at least about 1: 10 and up to and including about 10: 1. The mixed oxide coated particles are preferably synthesized by vapor phase coating techniques, such as atomic layer deposition. The formulations may provide delayed or sustained release of a glucagon-like peptide-1 receptor agonist to treat metabolic disorders or conditions, such as type 2 diabetes and / or obesity, without burst release effects. The glucagon-like peptide-1 receptor agonist is preferably a liraglutide (liraglutide), and the glucagon-like peptide-1 receptor agonist is preferably a liraglutide (liraglutide).

The application belongs to the field of marine biotechnology, and specifically discloses a preparation method of a long oyster insulin-like peptide receptor (ILPR) polyclonal antibody and application thereof. The method is characterized by the following steps: specific antigen epitopes of the long oyster ILPR protein are screened through bioinformatics analysis, a pET32a-ILPR recombinant plasmid is constructed and induced to express in Escherichia coli; the purified recombinant protein is used as an immunogen to immunize New Zealand white rabbits, and rabbit antisera are collected after four times of booster immunization; specific polyclonal antibodies are purified by using antigen affinity chromatography technology, and can specifically recognize the ILPR protein in long oyster tissues. The antibody prepared by the application has high specificity and sensitivity, and provides an important biological tool for studying the insulin signal transduction pathway, growth regulation and energy metabolism mechanism of long oysters.

Methods and compositions for controlling, treating, preventing, or ameliorating arthropod infection are provided. Compositions can comprise one or more active agents of small molecules antagonists of arthropod kinin receptor. Methods of preventing disease development and infestation by arthropods are disclosed as well as methods of making, using, and producing such compositions.

The present invention relates to a WKYMVm peptide analogue and uses thereof, and the WKYMVm peptide analogues have increased stability due to an increased in vivo degradation half-life, enhance activity of neutrophils as a formylpeptide receptor agonist, and regulate the activity of immune cells mediating pathology of multiple sclerosis so that they can be effectively used for enhancing immunity or preventing or treating multiple sclerosis.

In certain embodiments, the present invention provides compounds of formula I: TLX and methods of using the same, T is an SST2R targeting ligand; L is a linker, X is a chelating agent.

The present invention discloses a method for alleviating gastrointestinal side effects resulting from the administration of pharmaceutical agents selected from the group including non-steroidal anti-inflammatory drugs (NSAIDs), glucagon-like peptide-1 (GLP-1) receptor agonists, gastric inhibitory polypeptide (GIP) receptor agonists, dual GIP / GLP-1 receptor co-agonists, and combinations thereof, by administering a composition containing colostrum product, bovine colostrum, or combinations thereof to a subject. The present invention discloses compositions and kits related to alleviating gastrointestinal side effects resulting from the administration of pharmaceutical agents selected from a group including non-steroidal anti-inflammatory drugs (NSAIDs), glucagon-like peptide-1 (GLP -1) receptor agonists, gastric inhibitory polypeptide (GIP) receptor agonists, dual GIP / GLP -1 receptor co-agonists, and combinations thereof. This method provides a novel approach to mitigate gastrointestinal side effects associated with the use of these pharmaceutical agents, enhancing patient comfort and compliance during treatment.

The disclosure relates to compounds of formula I, which are formyl peptide 2 (FPR2) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.

This invention discloses umami peptides derived from Litopenaeus vannamei and their applications, belonging to the field of bioactive peptide technology. Seven umami peptides are described, with amino acid sequences as follows: ASRM, RCNG, DNCY, GAEF, DEGF, EDMQF, and PNRMPY, as shown in SEQ ID NO. 1–7. The invention also discusses the application of these umami peptides as or in the preparation of umami enhancers. This invention utilizes virtual screening and molecular simulation techniques to discover new umami peptides from the protein sequences of Litopenaeus vannamei, enriching the marine umami peptide library. Furthermore, it investigates the key amino acids and mechanisms of action of umami peptide receptor binding, providing a reference for studying the umami presentation mechanisms of peptides with different structures.

A pharmaceutical formulation useful for treating metabolic disorders or conditions is provided, comprising a plurality of particles suspended in a carrier system, the particles (a) having an average diameter based on weight, number, or volume of about 10 nm to about 700 μm, and (b) a solid core comprising at least one glucagon-like peptide-1 receptor agonist or a pharmaceutically acceptable salt thereof, at least partially coated with a coating of an inorganic material comprising a mixture of (i) zinc oxide and (ii) one or more other metal and / or metalloid oxides, wherein the atomic ratio ((i):(ii)) is at least about 1:10 and not more than about 10:1. The mixed oxide-coated particles are preferably synthesized by a vapor-phase coating technique, such as atomic layer deposition. The formulation may provide delayed or sustained release of the glucagon-like peptide-1 receptor agonist for treating metabolic disorders or conditions, such as type 2 diabetes and / or obesity, without a burst effect. The glucagon-like peptide-1 receptor agonist is preferably liraglutide.

The invention relates to a 177Lu-DOTATATE peptide receptor radionuclide curative effect prediction model and application thereof, the model is used for performing multicolor immunofluorescent staining on tissue slices of a neuroendocrine tumor (NET) patient, and the model at least comprises specific staining antibodies of cytokeratin (CK +) cells, CD8 cells and TIM-3 molecules; then carrying out image acquisition and analysis, and identifying two positive cells, namely CK < + > and CD8 < + > TIM-3 < + >; calculating an under-curve area difference AUC (CK) (CD8 + TIM-3 +) between an observation curve of a nearest neighbor distance accumulation function (G function) between CK + and CD8 + TIM-3 + and a Poisson distribution curve according to an R language software package, determining a response scoring formula and threshold division based on single-factor logistic regression of PRRT response degree of case data, and substituting the difference into the response scoring formula, and the response score can be used for curative effect prediction.

The present invention provides, in certain embodiments, a cancer-targeting conjugate comprising Formula I: wherein T is a SST2R-targeting ligand, L is a linker, and X is a chelator, for use in the therapeutic treatment of cancer; and methods of use thereof.

The invention discloses a modularized pathogenic microorganism targeting fluorescent probe, an antibacterial drug delivery oligopeptide and a preparation method and application thereof, the probe is composed of the following functional modules: a chemotactic module: formyl-D-Phe-Leu-D-Met, which realizes active migration to an infectious inflammation microenvironment by combining with a formyl peptide receptor; the targeting module comprises D-Trp-D-Trp-Arg and RWWR which are specifically combined with the surfaces of the pathogenic microorganisms through cationic interaction and hydrophobic interaction; the fluorescence activation module is a double Cy5.5 fluorophore which is covalently connected through lysine side chain amino; and the connection and stability module is a PEG4-GGSG flexible linker, has C-terminal amidation and key site D-type amino acid modification, and is used for enhancing the stability of the probe. The probe can actively migrate to an infectious inflammation microenvironment, is specifically combined with the surface of pathogenic microorganisms, and triggers fluorescence activation after combination, so that accurate imaging of an infected part is realized.

The invention provides a conjugate comprising a peptide that binds to the Calcitonin Gene-Related Peptide Receptor that is linked to a therapeutic or a detectable radionuclide. The conjugates are useful for imaging the Calcitonin Gene-Related Peptide Receptor and for treating diseases wherein the activity of the Calcitonin Gene-Related Peptide Receptor is implicated.

There is provided peptidic compounds of Formula I, A or B(Rradn6-[linker]-RL-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-ψ-Xaa9-NH2). Xaa1 is D-Phe, Cpa, D-Cpa, Nal, D-Nal, 2-Nal, or D-2-Nal; Xaa2 is Asn, Gln, Hse, Cit or His. Xaa3 is Trp, Bta, Trp(Me), Trp(7-Me), Trp(6-Me), Trp(5-Me), Trp(4-Me), Trp(2-Me), Trp(7-F), Trp(6-F), Trp(5-F), Trp(4-F), Trp(5-OH), or αMe-Trp. Xaa4 is Ala or Ser. Xaa5 is Val, Cpg, or Tle. Xaa6 is Gly, NMe-Gly, or D-Ala. Xaa7 is His or NMe-His. Xaa8 is Leu or Phe. Xaa9-NH2 is a C-terminally amidated amino acid residue selected from Pro, 4-oxa-L-Pro, Me2Thz, or Thz. ψ represents a peptide bond or reduced peptide bond joining Xaa8 to Xaa9. Rradn6 is 1-5 radiolabeling groups. There is also provided the use of such compounds as imaging agents or therapeutic agents.

The invention discloses a selective nematicidal compound I based on a bursaphelenchus xylophilus neuropeptide receptor and application of the selective nematicidal compound I. The invention relates to a small molecular lead compound for killing bursaphelenchus xylophilus and application of the small molecular lead compound, the chemical formula of the small molecular lead compound is C25H27 Cl N2 O3 S, and the median lethal concentration of the small molecular lead compound for killing the bursaphelenchus xylophilus is 9.30 mg / L. The micromolecular lead compound can effectively inhibit the feeding capacity and population number of pine wood nematodes, and shows good nematode killing potential. The small molecular lead compound has a good application prospect in the aspect of preventing and treating pine wood nematode diseases.

The application relates to a small molecule lead compound for killing Bursaphelenchus xylophilus and application thereof, and the chemical formula of the small molecule lead compound is respectively C 25 H 27 ClN2O3S、C 30 H 32 N2O 6、 C 27 H 30 N6O, and the semi-lethal concentrations of the small molecule lead compound for killing Bursaphelenchus xylophilus are respectively 9.30 mg / L, 8.76 mg / L and 9.19 mg / L. The small molecule lead compound can effectively inhibit the feeding capacity and population quantity of Bursaphelenchus xylophilus, and shows good nematode killing potential. The small molecule lead compound has good application prospect in the prevention and treatment of Bursaphelenchus xylophilus disease.

The present disclosure relates to compounds of formula (I) as formyl peptide 2 (FPR2) receptor agonists and / or formyl peptide 1 (FPR1) receptor agonists. The present disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, and related diseases.

The invention provides a conjugate comprising a peptide that binds to the Calcitonin Gene-Related Peptide Receptor that is linked to a therapeutic or a detectable radionuclide. The conjugates are useful for imaging the Calcitonin Gene-Related Peptide Receptor and for treating diseases wherein the activity of the Calcitonin Gene-Related Peptide Receptor is implicated.

This invention relates to a polypeptide compound and its applications, and more specifically, to a dual or triple agonist polypeptide drug that activates glucagon-like peptide-1 receptor and optionally glucose-dependent insulinotropic peptide receptor and glucagon receptor, and its application in the treatment of metabolic syndrome.

The invention relates to the field of medical biology, in particular to a tri-agonist polypeptide compound which has triple agonist activity on a glucagon-like peptide-1 receptor (GLP-1 R), a glucose-dependent insulinotropic polypeptide receptor (GIP R) and a glucagon receptor (GCG R) and is shown in a general formula (I) or salt or solvate of the tri-agonist polypeptide compound, and relates to application of the tri-agonist polypeptide compound in treatment of metabolic syndromes.

Convergent pathways for the preparation of a peptide by solid phase peptide synthesis or liquid phase peptide synthesis, as well as peptide fragments suitable for use in such pathways, are provided. The convergent pathways may be utilized for the synthesis of agonists of the glucagon-like peptide 1 receptor (GLP-1R) such as the peptide component of maridebart cafraglutide.

Described herein is a rsew method for treating diseases such as non-alcoholic fatty liver disease and non-alcoholic steatohepatitis with a growth hormone secretagogue alone or in combination with a drug selected from a dipeptidyl peptidase-4 antagonist a glucagon-like peptide receptor agonist, a thiazolidinedione, a sodium glucose transport protein 2 antagonist, arid metformin. Compositions relating to the same are also provided.

The invention provides a GLP-1R / GIPR / GCGR triple receptor agonist and an application of the GLP-1R / GIPR / GCGR triple receptor Specifically, the invention provides a polypeptide with GLP-1 (glucagon-like peptide-1) R / GIPR / GCGR triple receptor agonist activity or a pharmaceutically acceptable salt thereof, and the polypeptide or the pharmaceutically acceptable salt thereof has obvious triple agonist activity of a glucagon-like peptide-1 (GLP-1) receptor, a gastric inhibitory polypeptide (GIP) receptor and a glucagon (GCG) receptor. The compound can be used for preparing pharmaceutical compositions for preventing or treating metabolic diseases such as type I diabetes mellitus, type II diabetes mellitus, gestational diabetes mellitus, obesity, non-alcoholic fatty liver disease (NAFLD), obesity, hyperlipidemia and the like.

The present invention relates to a use of a triazole compound as a ghrelin receptor agonist and, more specifically, to a composition for preventing or treating diseases mediated by the ghrelin receptor, the composition being of a triazole compound which strongly binds to the ghrelin receptor with very high specificity. The compound provided by the present invention exhibits a strong binding force to the ghrelin receptor with very high specificity, and thus may be very usefully employed for preventing or developing a therapeutic agent for diseases mediated by the ghrelin receptor.

The present invention provides novel piperidinyl-containing pain-sensitive peptide receptor ligand compounds and pharmaceutical compositions that are useful in the treatment of neurological diseases and disorders wherein such ligands address the negative effects of such disorders. Such neurological diseases and conditions include acute and chronic pain, substance abuse / dependence, alcohol addiction, anxiety, depression, sleep disorders, gastrointestinal disorders, kidney disease, cardiovascular disease, and Parkinson's disease.