36 results about "Somatostatin Analogue" patented technology

The invention provides peptide derivatives designed to deliver peptides having growth factor inhibitory activity, especially somatostatin analogs, to the retina by sequential metabolism. The peptide derivatives, which comprise a dihydropyridine<CUSTOM-CHARACTER FILE="US06440933-20020827-P00900.TIF" ALT="custom character" HE="20" WI="20" ID="CUSTOM-CHARACTER-00001"/>pyridinium salt-type redox targetor moiety, a bulky lipophilic function and an amino acid/dipeptide/tripeptide spacer, are used in the prevention and treatment of diabetic retinopathy.

Compounds having somatostatin activity of the following Formula I,

wherein,

• • R¹ is aryl, substituted-aryl, and aryl-(lower-alkyl)-;
  • R² is lower alkyl, amino substituted lower alkyl, -carboxy-(lower-alkyl), -carbamic acid-(lower-alkyl) and -carboxy-(lower-alkyl)-aryl; and
  • R³ and R⁴ are independently, lower-alkyl, aryl, substituted-aryl, (substituted-aryl)-(lower-alkyl)-, heteroaryl, (heteroaryl)-(lower-alkyl)-, substituted-heteroaryl, (substituted heteroaryl)-(lower-alkyl)-, heterocyclic, heterocyclic-(lower-alkyl)-, substituted-heterocyclic, (substituted-heterocylic)-(lower alkyl)-, -carboxy-(lower-alkyl), and -carboxy-(lower-alkyl)-aryl; or a pharmaceutically acceptable, ester, ether, or salt thereof; methods for their use; and preparation.

The invention provides a novel radionuclide labelled somatostatin analogue molecular probe and its application and belongs to the field of radiopharmaceuticals labelling and nuclear medicine technologies. A bifunctional chelator couples cyclic polypeptide Pasireotide, and then radionuclide is used for labelling so as to obtain a radionuclide labelled neuroendocrine neoplasm specific somatostatin analogue radioactive molecular probe. The molecular probe can be combined with a tumor expression somatostatin receptor (SSTR), and SSTR positive tumor tissue can be accurately positioned by means of nuclear medicine. Thus, the purpose of disease target molecular imaging diagnosis and treatment is achieved. The synthesized molecular probe has higher affinity and functional activity for SSTR and is expected to become a somatostatin analogue developer and tumor therapeutic agent with a good prospect.

The invention provides a conjugate of SSA (somatostatin analog), PEG (polyethylene glycol) and anticancer drugs and the preparation thereof. The macromolecule conjugate is made from the targeting group SSA, the hydrophilic long-chain PEG and the anticancer drugs by adopting linking arms through conjugating. The macromolecule conjugate has tumor-targeting property and long circulation function, can obviously improve the antitumor activity, reduces toxic side effect of the drugs, is more suitable for clinical application, and provides new ideas for research and development of the anticancer drugs.

The invention belongs to the field of medicines, and concretely relates to a 123/131I-labeled novel glycosylated somatostatin analogue 123/131I-Gluc-KE108 and a preparation method thereof. The preparation method of the 123/131I-labeled novel glycosylated somatostatin analogue 123/131I-Gluc-KE108 comprises the following steps: (S1) synthesizing a novel glycosylated somatostatin analogue Gluc-KE108;and (S2) labeling the Gluc-KE108 with 123/131I, wherein step (S1) comprises (S1-1) amino acid condensation, (S1-2) removal of Dde from a polypeptide, (S1-3) resection of the polypeptide from resin, (S1-4) cyclisation of the polypeptide, (S1-5) acidolysis of the polypeptide and purification of an intermediate, and (S1-6) glycosylation and purification of the polypeptide; and in step (S2), the Gluc-KE108 is labeled with the 123/131I through adopting an Iodogen technology or a chloramine-T technology.

The invention provides an oral medication path of a somatostatin analogue polypeptide drug, and in particularly relates to an oral medication path of three somatostatin analogue polypeptides, including octreotide, vapreotide and lanreotide, belonging to the field of medicine. The invention provides the stability of the three somatostatin analogues in in-vitro artificial gastric juice and artificial intestinal juice, and the experiments prove that the three somatostatin analogue polypeptides are stable in the artificial gastric juice and can not be degraded; in the artificial intestinal juice, the three polypeptides are gradually degraded along with time, the sequences of the stabilities of the three polypeptides from high to low are as follows: octreotide, vapreotide and lanreotide. The invention further provides the absorbing states of the three polypeptides after the three polypeptides are given to a rat through intragastric administration, and describes the oral pharmacokinetic behaviors of the three polypeptides. According to the invention, on the basis of the original injection paths of the three polypeptides, the oral medication path of the three polypeptides is increased, so that the compliance of a patient is improved.

The present invention provides a combined drug for an injectable depot formulation having a superior effect of preventing and/or treating polycystic kidney disease. More specifically, the present invention relates to a drug for preventing and/or treating polycystic kidney disease, which is an injectable depot formulation comprising a particle containing tolvaptan or a prodrug thereof and a somatostatin analogue. The present invention also relates to a method for preventing and/or treating polycystic kidney disease using the drug.

The invention belongs to the field of biotechnology and microbe and animal cell lines and specifically relates to a humanized drug-resistant GH-type pituitary tumor cell strain huashanc-CH, especially to a first international humanized drug-resistant GH-type pituitary tumor cell strain huashanc-CH and its establishment method and application. Through isolated culture of pituitary tumor cells from a patient with clinical drug-resistant GH-type pituitary tumor, the humanized drug-resistant GH-type pituitary tumor cell strain huashanc-CH is obtained. The cell strain is passaged for 50 times for the first time and is mostly round or elliptical, cytoplasm is abundant, and nucleus is large and round. It shows through experimental results that the cell strain can be passaged stably, can secrete growth hormones continuously, is drug-resistant to somatostatin analogue, can be used to provide a necessary cell test tool for researches on pathogenic and drug-resistance mechanisms of pituitary tumor, research and development and screening of new drugs and new biotherapy and detection of related bio-engineering products and the like, and has exploring potential and application value.

The invention provides a somatostatin analogue and application thereof. The structure of the somatostatin analogue is as shown in formula I), a Phe-D-Trp-Lys-Thr motif with high affinity to a somatostatin receptor is reserved in the structure of the somatostatin analogue, the probe structure is modified through different chelating agents and different nuclides, and a broad-spectrum radiolabeled somatostatin molecular probe targeting a somatostatin receptor is designed. All subtypes of somatostatin receptors are targeted, and the probe is used as an early diagnosis probe for broad-spectrum neuroendocrine tumors. Therefore, precise medical treatment of early diagnosis, early discovery and early treatment of neuroendocrine tumors is realized.

The invention belongs to the field of biological medicines, and particularly relates to an oral pharmaceutical composition of somatostatin or analogues thereof. The pharmaceutical composition is prepared from somatostatin and/or the somatostatin analogues and a pharmaceutical composition for promoting small intestine absorption, wherein the pharmaceutical composition for promoting small intestineabsorption is prepared from lauryl sodium sulfate, carbomer, chitosan and sodium citrate. A composite auxiliary material is prepared from the pharmaceutical composition for promoting small intestine absorption, and after the auxiliary material is combined with somatostatin and/or the somatostatin analogues, the absorption of the effective component in small intestines can be improved.

A pharmaceutical formulation including a chelator-somatostatin receptor ligand and a transchelator is provided. The chelator-somatostatin receptor ligand is conjugated with a metal source or a radionuclide source, whereas the transchelator is capable of capturing free metal source or radionuclide source that is not conjugated to the chelator-somatostatin receptor ligand. By using such pharmaceutical formulation, the preparation of radiolabeled somatostatin analogues could be made more efficient, and is feasible for imaging of SSTR pathway-activated systems in cancers and neurological diseases.

The invention relates to a process for the preparation of injectable pharmaceutical compositions for the sustained release of somatostatin analogues and to pharmaceutical compositions prepared according to the process. In a preferred aspect the process comprises the steps of combining lanreotide acetate and acetic acid, lyophilizing the resulting mixture only once, and hydrating the lyophilizate. Acetic acid may be added to a desired pH during the final step of the process.