39 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.

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.

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 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.

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 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.

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.

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.

The present application relates to a kind of high drug loading density somatostatin oral nanoparticles, the nanoparticles are spherical hydrophobic polyester material as carrier, several hydrophobic somatostatin ion pair complex particles are uniformly wrapped inside, and hydrophilic hydroxyethyl starch is grafted on the outer surface of polyester material, wherein the hydrophobic somatostatin ion pair complex is composed of somatostatin and counterion compound, and the counterion compound is at least one of sodium dodecyl sulfate, 8- (2-hydroxybenzamide) sodium octanoate, sodium oleate, sodium octanoate, sodium caprate, sodium laurate, sodium dodecyl sulfonate, sodium dioctyl sulfosuccinate;The hydrophobic polyester material is lactic acid-glycolic acid copolymer, polycaprolactone, polylactic acid.The nanoparticles are modified by hydroxyethyl starch, can quickly penetrate mucus barrier during oral delivery, and have high enterocyte penetration efficiency, can effectively improve the oral bioavailability of somatostatin.

The invention relates to a somatostatin powder injection and a powder injection preparation method, and belongs to the technical field of somatostatin, the powder injection comprises the following components by weight: 3-5% of somatostatin, 1-5% of sodium carboxymethyl cellulose, 1-5% of sodium carboxymethyl cellulose, 1-5% of sodium carboxymethyl cellulose, and the balance of water. Mannitol with a weight percentage of 45%-55%; 5%-10% by weight of a cyclodextrin derivative; 4%-8% by weight of a pH regulator; the pH value of the final system is 3.5-5.0 due to the addition amount of the additive; the weight part of the antioxidant is 0.01%-0.05%; the total weight of the components is 100%. The powder injection is packaged in a PTFE (Polytetrafluoroethylene) lined glass bottle after being subjected to 0.22 mu m filtration, semi-stoppered filling and vacuum landslide type freeze-drying, and is sealed under a nitrogen filling condition. A new half-stoppered filling freeze-drying process is adopted, and under the action of a cyclodextrin derivative eutectic matrix and a trace amount of antioxidant, the freeze-dried somatostatin powder injection can be stored for 12 months or more. The somatostatin freeze-dried powder injection has a remarkable effect of prolonging the storage time of the freeze-dried somatostatin powder injection.

The application relates to the technical field of polypeptide synthesis, and discloses a somatostatin large fragment coupling process based on an SPPS-LPPS mixed method, which aims to solve the problems that SPPS fragments are prone to folding and LPPS coupling efficiency is low when somatostatin is synthesized by using the existing SPPS-LPPS mixed method. Fragments I of 1-21 and fragments II of 22-31 of somatostatin are synthesized by using SPPS, and the fragment quality is guaranteed by optimizing a solid-phase carrier, performing phased conformation washing and performing differential activation; then, the fragments are connected by realizing conformation regulation, precise activation and gradient temperature coupling in the LPPS stage, and the unreacted fragments are recovered synchronously; the application can inhibit peptide chain folding and activation agent hydrolysis, improve coupling efficiency and fragment utilization rate, guarantee the purity of a coupling intermediate, simultaneously enhance process stability and economy, and adapt to the industrialized production demand of somatostatin.

Compositions and methods are provided for generation of a population of monohormonal from human pluripotent cells. The method comprises sequentially exposing pluripotent stem cells to medium comprising CHIR99021 and Activin A; medium comprising Activin A; medium comprising FGF7; medium comprising retinoic acid, LDN193189, SANT1; medium comprising retinoic acid, LDN193189, SANT1, EGF and FGF2; and differentiation medium. A majority of cells in the population are monohormonal cells produce insulin, but not glucagon, somatostatin or ghrelin.

Described herein are compounds that are somatostatin type 3 receptor (SSTR3) agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat conditions, diseases, or disorders that would benefit from modulation of SSTR3 activity.

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.

Described herein are somatostatin subtype-2 receptor (SST2R)-targeted therapeutics that target tumor cells that express SST2R and their use in the treatment of cancer.

The invention relates to a preparation of a somatostatin regulator, in particular to a spray-dried solid dispersion, and the spray-dried solid dispersion comprises: (a) 3-[4-(4-amino-piperidine-1-yl)-3-(3, 5-difluoro-phenyl)-quinoline-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 from the pharmaceutically acceptable polymer. A tablet comprising the spray-dried solid dispersion and one or more pharmaceutically acceptable ingredients selected from the group consisting of one or more diluents, one or more disintegrants, one or more lubricants, and one or more glidants. The tablets are used for treating acra hypertrophy or neuroendocrine tumors or both in humans by oral administration.

The invention relates to a somatostatin powder injection and a preparation method thereof, and belongs to the technical field of somatostatin, the powder injection comprises the following components by weight: 3-5% of somatostatin, 1-5% of sodium carboxymethyl cellulose, 1-5% of sodium carboxymethyl cellulose, 1-5% of sodium carboxymethyl cellulose, and the balance of water. Mannitol with a weight percentage of 45%-55%; 5%-10% by weight of a cyclodextrin derivative; the pH regulator is a combination of lactic acid and sodium bicarbonate, the volume ratio of the combination is 1: (0.8-1.2), and the addition amount of the pH regulator enables the pH of the final system to be 3.5-5.0; the weight part of the antioxidant is 0.01%-0.05%; the total weight of the components is 100%. The powder injection is packaged in a PTFE (Polytetrafluoroethylene) lined glass bottle after being subjected to 0.22 mu m filtration, semi-stoppered filling and vacuum landslide type freeze-drying, and is sealed under a nitrogen filling condition. Under the action of a double-buffer acid-base hedging system, a cyclodextrin derivative eutectic matrix, a new freeze-drying process and a trace amount of antioxidant, the freeze-dried somatostatin powder injection can be stored for 12 months or more. The somatostatin freeze-dried powder injection has a remarkable effect of prolonging the storage time of the freeze-dried somatostatin powder injection.

The present invention relates to a somatostatin analogue composition for radiopharmaceutical use, in particular for diagnostic or therapeutic use. More specifically the somatostatin analogue is a receptor-selective somatostatin peptide antagonist.

The present invention relates to antibodies that bind to somatostatin receptor 2 (SSTR2), comprising a novel antigen binding domain and a heterodimeric antibody.

Provided are a somatostatin derivative and a method for preparing the same. Specifically, provided is a fusion protein comprising a green fluorescent protein folding unit and a somatostatin precursor or an active fragment thereof, and the expression amount of the fusion protein is significantly improved. Also, the green fluorescent protein folding unit in the fusion protein can be digested into small fragments by a protease, and the molecular weight difference is large compared to the target protein, and it is easy to separate. Also provided is a method for preparing somatostatin and an intermediate using the fusion protein.