58 results about "Somatostatin" patented technology

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.

A pharmaceutical composition comprising biodegradable polymer microparticles comprising a somatostatin analogue or a pharmaceutically acceptable salt thereof, in which the pharmaceutical composition preferably provides sustained release of a somatostatin analogue or a pharmaceutically acceptable salt thereof over 30 days or more.

Described herein are pharmaceutically acceptable salts of a somatostatin modulator, crystalline forms of the pharmaceutically acceptable salts of the somatostatin modulator, methods of making such salts and crystalline forms, pharmaceutical compositions and medicaments comprising such salts and crystalline forms, and methods of using such salts and crystalline forms in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.

A pharmaceutical composition comprising biodegradable polymer microparticles comprising a somatostatin analogue or a pharmaceutically acceptable salt thereof, wherein said pharmaceutical composition preferably provides a sustained release of the somatostatin analogue, or a pharmaceutically acceptable salt thereof, over 30 days or more.

Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.

Methods for generating mature somatostatin+ interneurons from human forebrain neural progenitor cells are provided using chemically-defined culture media in a two-stage culture protocol. The mature somatostatin+ interneurons are generated from medial ganglionic eminence neural progenitor cells (MGE-NPCs), which themselves are differentiated from pluripotent stem cells. Culture media, isolated cell populations and kits are also provided.

The invention discloses application of serum MSTN (myostatin) as a marker in preparation of a metabolism-related steatohepatitis diagnosis product, and belongs to the technical field of biomedical detection. The biomarker for noninvasive diagnosis of the metabolism-related steatohepatitis is serum myosostatin MSTN, and the biomarker can be used as a detection target for preparing a noninvasive diagnosis product of the metabolism-related steatohepatitis. As an independent biomarker, the MSTN is higher in diagnosis efficiency in AST normal patients; the MSTN and the ALT or the AST are jointly applied, so that the specificity and the positive predictive value (PPV) of single use of the ALT or the AST can be improved, the misdiagnosis rate of the ALT or the AST can be reduced, non-MASH patients can be more accurately excluded, and unnecessary, invasive or expensive subsequent examinations are reduced.

The present invention discloses a somatostatin type 2 receptor inhibitor, its radionuclide complex, preparation method and application. The somatostatin type 2 receptor inhibitor has a structure shown in the following formula I: wherein, n is a natural number selected from 1 to 7. Based on the somatostatin type 2 receptor inhibitor, the complexes formed by labeling <supgt;99m< / supgt;Tc or <supgt;188< / supgt;Re can be respectively used for specific SPECT / CT imaging of somatostatin type 2 receptors or the treatment of neuroendocrine tumors. The complexes have the characteristics of high labeling rate, good stability and good tumor tissue targeting, providing a new idea for the integrated diagnosis and treatment of neuroendocrine tumors.

Described herein are uses of the somatostatin modulator 3-[4-(4-amino-piperidin-1-yl)-3-(3,5-difluoro-phenyl)-quinolin-6-yl]-2-hydroxy-benzonitrile, or a pharmaceutically acceptable salt thereof, in the treatment of carcinoid syndrome.

The invention relates to the technical field of polypeptide synthesis, discloses a semaglutide large-fragment coupling process based on an SPPS-LPPS mixing method, and aims to solve the problems that an SPPS fragment is easy to fold and the LPPS coupling efficiency is low when semaglutide is synthesized by an existing SPPS-LPPS mixing method. SPPS is adopted for solid-phase synthesis of a semaglutide 1-21 site fragment I and a semaglutide 22-31 site fragment II, and the fragment quality is guaranteed through optimization of a solid-phase carrier, staged conformation washing and differential activation; according to the method, peptide chain folding and activating agent hydrolysis can be inhibited, the coupling efficiency and the fragment utilization rate can be improved, the purity of a coupling intermediate can be guaranteed, meanwhile, the process stability and economical efficiency can be enhanced, and the industrial production requirements of semaglutide can be met.

The present invention relates to a pharmaceutical composition for preventing or treating cognitive dysfunction or degenerative brain disease, the composition comprising: somatostatin or a somatostatin derivative or a pharmaceutically acceptable salt thereof as a first active ingredient; and hesperidin or a hesperidin derivative or a pharmaceutically acceptable salt thereof as a second active ingredient. The composition comprising somatostatin or a somatostatin derivative and hesperidin or a hesperidin derivative as active ingredients according to one specific embodiment of the present invention not only improves behavior related to reduced cognitive ability and degenerative brain diseases, but also has a neuroprotective effect and the effect of alleviating cognitive dysfunction or degenerative brain diseases through decreased production of inflammatory transcription factors and increased production of anti-inflammatory transcription factors, and can thus be effectively used as a therapeutic agent for cognitive dysfunction or degenerative brain diseases.

Disclosed are compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof. The variables of structural formula (I) are described herein. The compound of the invention can be attached to chelating groups for radionuclide binding and are therefore suitable for radioimaging and / or radiotherapy applications, for example the disclosed compounds can be radiolabeled with a positron emitter such as 18F, 68Ga or 64Cu, and used for positron emission tomography (PET). Alternatively, the compounds can be radiolabeled with an alpha particle emitter such as 223 Ac, a beta particle emitter such as 67Cu or 177Lu, or an Auger electron emitter (e.g. 111In, 67Ga, 99mTc, 195mPt, 125I, 123I and 161Tb) for use as a radiotherapeutic.

The application of FBH1 protein in judging the efficacy of postoperative somatostatin analogue adjuvant therapy for pancreatic neuroendocrine tumors relates to the fields of proteomics and clinical detection technology. The present invention finds that the disease-free survival and total survival time of the postoperative SSA adjuvant therapy group of PNETs patients with high FBH1 expression are significantly better than those of the non-adjuvant therapy group. By detecting the relative content of FBH1 protein in the tumor tissue of PNETs patients, it is effective to evaluate whether the patients use SSA drug adjuvant therapy after surgery, which is of great significance for the guidance of postoperative medication for patients.

Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat conditions, diseases, or conditions that would benefit from modulation of somatostatin activity.

The present invention is based, at least in part, on the discovery that replacing a key bond in a NIR fluorophore with a carbon-carbon bond conjugated to a targeting ligand results in greatly improved stability while retaining ligand and zwitterion properties compared to near infrared fluorophores that do not contain a carbon-carbon bond conjugated to a targeting ligand. In at least one aspect, the present invention provides an imaging agent dye comprising a charge balancing imaging agent conjugated to a targeting vector, wherein the targeting vector is a PSMA binding vector such as dPSMA-617 or KUE, a FAP binding vector, a xenopsin receptor binding vector, or a somatostatin receptor binding vector, and the charge balancing imaging agent is ZW-800-1, ZW-830-1, or ZW-700-1-Forte.

To provide SC-β cells and compositions as well as methods for generating the same.SOLUTION: Disclosed is a composition for use in a method for administering to a human subject with type I diabetes, where the composition comprises a plurality of cell clusters, where the method comprises a step of administering the composition to the subject, where the plurality of cell clusters comprise a plurality of glucagon-expressing cells, all of the cell clusters in the composition have a diameter less than 300 μm, at least 20% of the cells in the plurality of cell clusters are non-native pancreatic β cells that: (a) express chromogranin A, ISL1, PDX1 and C-peptide, and one or more of the following genes ZNT8, MNX1 or ABCC8; and (b) do not express somatostatin or glucagon.SELECTED DRAWING: None

The present invention relates to the use of the compound of formula (I) or the pharmaceutically acceptable salts and / or solvates thereof in the treatment of SSTR3 expressing tumors, selected from non-functioning pituitary adenomas (NFPAs) or other neuroendocrine-related malignancies, selected from pancreatic tumors, pheochromocytomas, paragangliomas, lung carcinoids or breast cancer. More specifically, the present invention provides to the use of pharmaceutical compositions comprising the compound of formula (I) or the pharmaceutically acceptable salts and / or solvates thereof and at least one physiologically acceptable excipient in the treatment of a patient affected by SSTR3 expressing tumors, selected from non-functioning pituitary adenomas (NFPAs) or other neuroendocrine-related malignancies, selected from pancreatic tumors, pheochromocytomas, paragangliomas, lung carcinoids or breast cancer.

Described herein are somatostatin subtype-2 receptor (SST2R) non-peptide drug conjugates (NDC) that target tumor cells expressing SST2R and their use in the treatment and / or diagnosis of cancer.

The present invention relates to genetic engineering, biotechnology, immunology, and microbiology. Recombinant GBD-SSTad-SSTad protein and a method for preparation thereof on glucan are described, including the binding of GBD-SSTad-SSTad protein in cell extracts of E. coli BL21 [pGBD-SSTad-SSTad] strain to an alpha-glycan-containing sorbent due to affinity interaction during the incubation procedure, subsequent washing from unbound bacterial proteins and isolation of the desired product. The invention also relates to an immunogenic composition and a kit comprising said peptide. The invention also relates to the use of the obtained protein to increase the number of maturing follicles and improve the quality of sperm. This technical result, an increase in the number of maturing follicles and an improvement in the quality of sperm is based on the use of the KNFFWKTFTS peptide, which is part of a recombinant protein that is capable of eliciting autoantibodies to somatostatin.

The invention relates to cortistatin analogues and their uses. The compounds of the invention are peptide ligands with potential application in the diagnosis, prevention or therapy of those pathologies where receptors capable of binding to cortistatin, specific or shared with other molecules such as somatostatin and / or ghrelin (GHSR), are expressed, being in addition more stable in serum than cortistatin.

The present invention discloses compounds of Formula (I) and their complexes with radionuclides that can recognize both Somatostatin type 2 receptor (SSTR2) and cholecystokinin 2 receptor (CCK2R) and can be used in the diagnosis and treatment of diseases where either or both receptors are overexpressed.

A spray-dried solid dispersion comprising: (a) 3-[4-(4-amino-piperidin-l-yl)-3-(3,5-difluoro-phenyl)-quinolin-6-yl]-2-hydroxy-benzonitrile or a pharmaceutically acceptable salt or solvate thereof; and (b) a pharmaceutically acceptable polymer; wherein the API is dispersed in a polymer matrix formed by the pharmaceutically acceptable polymer. A tablet comprising the spray-dried solid dispersion and one or more pharmaceutically acceptable ingredients selected from one or more diluents, one or more disintegrants, one or more lubricants, one or more glidants. The tablet is for use in the treatment of acromegaly or a neuroendocrine tumor or both in a human by oral administration.

Methods for generating mature somatostatin+ interneurons from human forebrain neural progenitor cells are provided using chemically-defined culture media in a two-stage culture protocol. The mature somatostatin+ interneurons are generated from medial ganglionic eminence neural progenitor cells (MGE-NPCs), which themselves are differentiated from pluripotent stem cells. Culture media, isolated cell populations and kits are also provided.

The invention discloses application of FBH1 protein in judgment of auxiliary treatment effect of somatostatin analogues after pancreatic neuroendocrine tumor operation, and relates to the technical field of proteomics and clinical detection. It is found that the disease-free survival time and the total survival time of a postoperative SSA adjuvant therapy group of a PNETs patient with high expression of FBH1 are remarkably superior to those of a group without adjuvant therapy, whether the patient is subjected to SSA drug adjuvant therapy or not after an operation can be effectively evaluated by detecting the relative content of FBH1 protein in tumor tissue of the PNETs patient, and the method has important significance on postoperative medication guidance of the patient.

This article describes a method for generating mature somatostatin-interneurons from human forebrain neural progenitor cells in a two-stage culture protocol using a chemically defined culture medium. Mature somatostatin-interneurons are generated from medial ganglion ridge neural progenitor cells (MGE-NPC), which themselves are derived from pluripotent stem cells. The article also provides the culture medium, isolated cell populations, and kits.

The present invention discloses compounds of Formula (I) and their complexes with radionuclides that can recognize both Somatostatin type 2 receptor (SSTR2) and cholecystokinin 2 receptor (CCK2R) and can be used in the diagnosis and treatment of diseases where either or both receptors are overexpressed.

The invention discloses a somatostatin peptide analogue, the somatostatin peptide analogue has a cyclic or non-cyclic hexapeptide unit, and the residue sequence at the position numbered 2 to 5 in the hexapeptide unit is-X1-(D / L-) Trp-X2-X3-, and the residue sequence at the position numbered 2 to 5 in the hexapeptide unit is-X1-(D / L-) Trp-X2-X3-, or, the somatostatin peptide analogue has a ring-forming or non-ring-forming octapeptide unit, and the residue sequence at the position numbered 2 to 7 in the octapeptide unit is-Cys-X1-(D / L-) Trp-X2-X3-Cys-, and the residue sequence at the position numbered 2 to 7 in the octapeptide unit is-Cys-X1-(D / L-) Trp-X2-X3-Cys-; wherein X1 is an alpha-amino acid residue with an aryl group on a C alpha side chain, X3 is an alpha-amino acid residue, and the compound is characterized in that X2 is a Lys-variation residue: # imgabs0 #. The invention breaks through the'taboo 'that the Lys9 residue cannot be replaced, otherwise, the biological activity is greatly reduced. According to the present invention, the Lys9 residue in the somatostatin peptide analogue is changed, and the Lys9 residue is subjected to change variation, such that the somatostatin peptide analogue of the present invention has high (at least similar) binding affinity with SSTR2 due to the change variation;

The invention relates to the technical field of medicines, and discloses a preparation method of a pharmaceutical composition for delayed release of somatostatin analogues. The pharmaceutical composition comprises the following main components: lanreotide acetate and an acetic acid aqueous solution, the preparation method comprises the following steps: taking lanreotide acetate, adding an acetic acid aqueous solution to dissolve the lanreotide acetate, filtering and sterilizing after the lanreotide acetate is completely dissolved, and preparing the filled and sterile pre-filled lanreotide acetate sustained-release gel by adopting a one-step vacuum volatilization method. And the concentration of lanreotide in terms of free alkali reaches 23.4-27.1% (w / w). The preparation method has the advantages that the preparation method is simple and easy to implement, and the time cost and the production cost are reduced; sterile operation is performed in the whole process, and sterilization cost is reduced; on the basis of simplifying the operation steps, the prepared lanreotide acetate sustained-release composition has the same release effect as the original lanreotide acetate sustained-release composition.

Artificial expression constructs are provided.SOLUTION: Artificial expression constructs are provided that selectively regulate gene expression in selected central nervous system cell types. Such artificial expression constructs can be used to selectively express synthetic genes or alter the expression of genes in inhibitory neocortical GABAergic neurons, including somatostatin GABAergic neurons, parvalmine GABAergic neurons, vasoactive intestinal peptide GABAergic neurons, Lamp5GABA GABAergic neurons, or in some instances astrocytes.SELECTED DRAWING: Figure 2-1

To provide a method for treating a disease. [Solution] A 2B Compounds, compositions, formulations, and methods for modulating adenosine receptors are disclosed in this specification. The specification includes compounds, methods for producing such compounds, pharmaceutical compositions and formulations containing such compounds, and somatostatin A 2B Methods of using such compounds in the treatment of diseases, disorders, or conditions for which adenosine receptor activity is to be beneficial are described.