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78 results about "DOTA" patented technology

DOTA (also known as tetraxetan) is an organic compound with the formula (CH₂CH₂NCH₂CO₂H)₄. The molecule consists of a central 12-membered tetraaza (i.e., containing four nitrogen atoms) ring. DOTA is used as a complexing agent, especially for lanthanide ions. Its complexes have medical applications as contrast agents and cancer treatments.

Backbone-substituted bifunctional DOTA ligands, complexes and compositions thereof, and methods of using same

Backbone-substituted 1,4,7,10-tetraaza cyclododecane-N,N′,N″,N′″-tetraacetic acid compounds, metal complexes thereof, compositions thereof, conjugates thereof, and methods of use in diagnostic imaging and treatment of a cellular disorder.
Owner:GOVERNMENT OF THE US REPRESENTED BY THE SEC

Chiral cyclen compounds and their uses

The present invention relates to the preparation of a series of chiral DOTA, D03A, D02A, DO1A, cyclen and their metal complexes, which display properties superior to those of previous DOTA- based compounds, and hence are potentially valuable as a platform for diagnostic applications. The chiral DOTAs reveal a high abundance of twisted square antiprism (TSA) geometry favoring them to be used as potential MRI contrast agents, whereas their rapid labelling properties at mild conditions make them excellent candidates for use as radiometal chelators.
Owner:THE HONG KONG POLYTECHNIC UNIV

Process for producing 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid and complexes thereof

A process for producing 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) including salts and hydrates thereof of general formula (I) from the respective cyclen.The process involves the use of cationic- and anionic exchange resins and solvent treatments to remove the organic and inorganic contaminants. Any cations present in the raw DOTA or other contaminants resulting from the reaction of cyclen are largely reduced in early stages of the process allowing to obtain good yields of DOTA in a purified grade and in an easier and reliable way. The process is useful for the production of DOTA, of macrocyclic compounds including metal ions complexes thereof and of compositions including the macrocyclic compounds that can be used as contrast agents for magnetic resonance imaging.
Owner:T2PHARMA GMBH

Magnetic nanometer material and application thereof to phosphopeptide enrichment

The invention discloses a magnetic nanometer material and application thereof to phosphopeptide enrichment. 4-carboxyphenyl porphyrin (TCPP) and 1,4,7,10-tetraazacycl ododecane-N,N,N,N-tetraacetate (DOTA) are in covalent linkage to the surface of an amino-modified magnetic nanometer material modified through ethanediamine, and lanthanide series metal ions are immobilized on the surface of the material to synthesize a novel magnetic nanometer material. The metal ion-modified magnetic nanometer material has higher selectivity, sensitivity and enrichment efficiency in the phosphopeptide enrichment process. Compared with the traditional TiO2 method, the metal ion-modified magnetic nanometer material has higher phosphopeptide enrichment specificity and selectivity.
Owner:BEIJING PROTEOME RES CENT

Preparation method of heavy metal cadmium artificial antigen and application of DOTA in preparation of heavy metal cadmium artificial antigen reagent

The invention discloses a preparation method of heavy metal cadmium artificial antigen, which applies 2-S-(4- aminobenzene)-1, 4, 7, 10 tetraazacyclo cyclononane-1, 4, 7, 10-acetate tetrahydrate(p-NH2-Bn-DOTA, DOTA for short) as cheating agent, and couples cadmium ion chelating agent composite with carrier protein bovine serum albumin BSA or egg albumin OVA; thus the artificial antigen is prepared. The method adds the sodium borohydride processing step on the basis of traditional method, and improves the coupling efficiency and antiserum titre. The invention further discloses an application ofDOTA in preparation of the heavy metal cadmium artificial antigen.
Owner:ZHEJIANG GONGSHANG UNIVERSITY

Diagnosis and treatment integrated PSMA inhibitor, compound and preparation method and application thereof

ActiveCN112898270AAccelerated excretion of radioactivityReduce non-specific uptakeIron organic compoundsRadioactive preparation carriersAntigenNeoplasm diagnosis
The invention discloses a diagnosis and treatment integrated PSMA inhibitor, a compound and a preparation method and application thereof. The structure of the compound is shown as a formula A in the specification, wherein the R1 is DOTA or NODA used for complexing (radioactive) metal ions, radioactive metal nuclide is used for diagnosis or treatment, non-radioactive metal nuclide is used for being combined with radionuclide, and R2 is a coupling agent which is benzylamine, cyclohexylmethylamine or butylamine. The invention also provides a preparation method and application of the compound. The compound has very high affinity with prostate cancer specific membrane antigen (PSMA), and compared with existing PSMA treatment and imaging agents, the compound has the advantages that high swelling uptake is maintained, radioactive excretion of in-vivo non-target regions is accelerated, non-specific uptake of glands is reduced, and treatment and imaging of tumors are facilitated; and meanwhile, when the developing agent is marked by nuclide, the effect of integrating tumor diagnosis and treatment can be achieved, and the PSMA inhibitor is particularly suitable for treatment, diagnosis, staging and the like of prostate cancer.
Owner:北京瑞达福明科技有限公司

Targeted tumor PD-L1 PET imaging agent as well as labeled precursor, preparation method and application thereof

The invention discloses a tumor PD-L1 targeting PET imaging agent as well as a labeled precursor, a preparation method and application thereof, and belongs to the technical field of radiopharmaceutical chemistry. The structure of a labeled precursor of the tumor PD-L1 targeting PET developer is shown as a formula I, and the structure of the tumor PD-L1 targeting PET developer is shown as a formula II. According to the invention, a bifunctional chelating agent DOTA and a cyclic peptide inhibitor SETSKSF are creatively connected together, and a labeled precursor of a PET imaging agent of a targeted tumor PD-L1 as shown in a formula I is synthesized. After the precursor compound is marked with Ga-68, a compound shown in a formula II can be obtained, and the compound has good stability, excellent pharmacokinetics, good binding specificity with tumor PD-L1 and easy synthesis.
Owner:THE AFFILIATED HOSPITAL OF SOUTHWEST MEDICAL UNIV

Magnetic signal probe of magnetic relaxation time immunosensor and application of magnetic signal probe

ActiveCN111198267AAvoid the disadvantages of step-by-step readoutImprove detection efficiencyBiological testingCoatingsParticle physicsPolylysine
The invention discloses a magnetic signal probe of a magnetic relaxation time immunosensor. The probe comprises a Gd < 3 + > chelate, polylysine and a superparamagnetic nano-particle of an antibody which are coupled. By coupling polylysine and an antibody to the surfaces of superparamagnetic nano-particles,the antibody-superparamagnetic nanoparticle-polylysine conjugate with the multi-dimensionalspace reticular dendritic structure is obtained; then, succinimide-tetraazacyclododecane tetraacetic acid with chelating performance is coupled to the surface of polylysine, and paramagnetic Gd < 3 +> ions are added; gd < 3 + > is captured through DOTA, and finally, a large number of Gd < 3 + > ions are chelated on the surfaces of the superparamagnetic nano-particles, so that the magnetic relaxation time immunosensing magnetic signal probe with multiple signal amplification is obtained. According to the invention, magnetic separation and magnetic sensing integrated nano magnetic particles andparamagnetic Gd < 3 + > ions are controllably assembled into the multifunctional nano magnetic probe for the first time, so that multiple amplification of sensing signals is realized, and the sensitivity and detection speed of the sensor are greatly improved.
Owner:富德赛科技(武汉)有限公司

PSMA inhibitor, compound as well as preparation method and application of compound

The invention discloses a PSMA inhibitor, a compound as well as a preparation method and application of the compound. The structure of the compound is shown as a formula A defined in the description, wherein R1 is cyclohexane methylamine or benzylamine, R2 is DOTA(I) or NODA(II) used for complexing (radioactive) metal ions, radioactive metal nuclides are used for diagnosis or treatment, and non-radioactive metal nuclides are used for being combined with radioactive nuclides. The invention also provides a preparation method and application of the compound. The compound has high affinity with prostate specific membrane antigen (PSMA), has the characteristic of rapid removal, and is especially suitable for tumor radionuclide target diagnosis, staging, treatment and the like.
Owner:北京瑞达福明科技有限公司

Improved synthesis method of heavy metal lead artificial antigen and application of DOTA (2-S-(4-amino-benzene)-1,4,7,10-tetraazacyclononane-1,4,7,10-tetraacetic acid) to preparation of heavy metal lead artificial antigen reagent

The invention provides a synthesis method for preparing a heavy metal lead artificial antigen based on a novel difunctional chelating agent DOTA (2-S-(4-amino-benzene)-1,4,7,10-tetraazacyclononane-1,4,7,10-tetraacetic acid). According to the preparation method, DOTA is taken as the chelating agent, a lead ion chelating agent compound is coupled with BSA (bovine serum albumin) as carrier protein orKHL (human serum albumin), and the artificial antigen is prepared. According to the method, the step of sodium borohydride reduction is added on the original traditional basis, so that the coupling efficiency is improved. The invention further provides an application of DOTA to preparation of the heavy metal lead artificial antigen.
Owner:ZHEJIANG GONGSHANG UNIVERSITY

Preparation method of folate-targeted 99mTc marked manganese-based chelate MR/SPECT dual-mode probe

InactiveCN104645363AAchieve specific targetingRealize multi-functional modificationRadioactive preparation carriersCancer cellReceptor
The invention relates to a preparation method of a folate-targeted 99mTc marked manganese-based chelate MR / SPECT dual-mode probe. The method comprises the following steps of: modifying G5 surface with a chelating reagent DOTA-NHS; connecting a targeting molecule to the G5 surface; marking the G5 with FI; chelating manganese ions in coordination with DOTA; converting G5 surface amino into acetyl through acetylation reaction; finally, marking the residual DOTA with radioactive nucleus 99mTc, thus obtaining the probe. The molecular imaging probe prepared by the invention realizes MR / SPECT dual-mode imaging at the cell level and the animal level; moreover, by mediation of FA, the probe prepared by the invention has remarkable targeting effect on a Hela cell tumor model of high-expression cancer cell strain of an FA receptor, and is expected to be used for realizing dual-mode targeting diagnosis on cancer.
Owner:DONGHUA UNIV +1

Radionuclide labeled FAPI compound and synthesis process method thereof

According to the invention, liquid nuclide < 18 > F-labeled FAPI (< 18 > F-FAPI) is fitted, specifically, the < 18 > F-FAPI with a relatively long half-life period is synthesized by utilizing a strong complexing and bridging effect of Al < 3 + > ions on < 18 > F ions and cyclic coordination groups (DOTA and NOTA), and a radiochemical purity synthesis process of the Al< 18 > F-FAPI of 99% or above and a single yield of more than 100 mCi are realized, so that clinical requirements are met.
Owner:上海市质子重离子临床技术研发中心

Process for preparing a pharmaceutical formulation of contrast agents

The invention relates to a process for preparing a liquid pharmaceutical formulation containing a complex of macrocyclic chelate with a lanthanide and a mol / mol amount offree macrocyclic chelate of between 0.002% and 0.4%, advantageously between 0.02% and 0.3% and very advantageously between 0.025% and 0.25%, the macrocyclic chelate advantageously being chosen from DOTA, NOTA, DOTAGA, DO3A, BT-DO3A, HP-DO3A and PCTA, and is preferably DOTA, the said process comprising the following successive steps: b) preparation of a liquid pharmaceutical composition containing, firstly, the complex of macrocyclic chelate with a lanthanide, and, secondly, free macrocyclic chelate and / or free lanthanide; c) measurement in the pharmaceutical formulation obtained in step b) of the concentration of free macrocyclic chelate C chl and / or of free lanthanide C lanl; d)adjustmentof C chl and / or of C lanl so as to obtain C chl = C tchl and C lanl = 0, wherein C t chl is the target concentration of free macrocyclic chelate in the final liquid pharmaceutical formulation.
Owner:GUERBET SA

Preparation method of T1 strengthened nuclear magnetic resonance nanometer contrast agent

The invention discloses a T1 strengthened nanometer magnetic contrast agent having the function of activating targeting properties of blood platelets and a preparation method of the T1 strengthened nanometer magnetic contrast agent belonging to the field of nuclear magnetic resonance contrast agents. The characteristics of "dissociation-self-assembly" and surface modificability of an apoferritin nanometer cage under different pH environment are utilized, paramagnetic Gd-DOTA is loaded into the apoferritin nanometer cage, ligand-KGDS tetrapeptide specifically targeting and activating the bloodplatelets is coupled to the surface of Gd-loaded apoferritin, and therefore, nanometer particles which can actively target and activate the blood platelets and have nuclear magnetic resonance T1 weighted imaging strengthened contrast effects can be obtained. The particle diameter of the nanometer contrast agent is about 10nm, the nanometer contrast agent has favorable contrast effects, targeting properties for activating the blood platelets, and biocompatibility; precise visualization of thrombosis is hopefully realized through targeting and activating the blood platelets, and more comprehensive molecule information is provided for early prevention, diagnosis and treatment of cardiovascular diseases.
Owner:广州市番禺区中心医院

DZ-1-Lys-DOTA conjugate compounded with radioactive metal and application of DZ-1-Lys-DOTA conjugate

The invention discloses a DZ-1-Lys-DOTA conjugate compounded with radioactive metal. The DZ-1-Lys-DOTA conjugate comprises a heptamethyl cyanine dye group coupled with a DOTA group through a lysine cross-linking agent, wherein the DOTA group is compounded with the radioactive metal M; the radioactive metal M adopts one or more radioactive metal groups of lutetium -177, yttrium -90 and gallium- 68; the invention also discloses application of the DZ-1-Lys-DOTA conjugate compounded with the radioactive metal. The DZ-1-Lys-DOTA conjugate comprises improved imaging, improved treatment, improved image-guided treatment, improved serum stability, improved penetrability of tumors (especially solid tumors) and / or affinity of therapeutic and diagnostic pairs. Through the scheme, the DZ-1-Lys-DOTA conjugate has very high practical value and popularization value in the technical field of the DZ-1-Lys-DOTA conjugate.
Owner:DEZHEN (CHINA) MEDICAL TECH CO LTD

Rare-earth cage-like coordination compound metal fluorescent dual-mode label for flow cytometry and preparation method of rare-earth cage-like coordination compound metal fluorescent dual-mode label

The invention discloses a rare-earth cage-like coordination compound metal fluorescent dual-mode label for flow cytometry, which is obtained by coupling a polymer with a rare-earth cage-like coordination compound as shown in the a formula (I-8) defined in the description with a monoclonal antibody, wherein Ln<3+> is a lanthanide rare earth metal ion. Different from an existing mass spectrum flow type polymer metal chelating label, a DOTA coordination group is ingeniously replaced with a cage-shaped coordination group, on the one hand, the coordination capacity of rare earth ions is improved, leakage of the rare earth ions can be reduced, and signals of the metal label in a flow type mass spectrum are stronger; on the other hand, due to the antenna effect of the cage-like coordination compound, the fluorescence intensity of the rare-earth coordination compound is greatly improved, and the rare-earth coordination compound can be detected by a flow cytometry. According to the invention, the rare earth cage-like coordination compound metal fluorescent dual-mode label for flow cytometry can be prepared at a lower cost, so that the use cost of a mass spectrum flow detection reagent can be greatly reduced.
Owner:SUZHOU INST OF BIOMEDICAL ENG & TECH CHINESE ACADEMY OF SCI +1

Radiometal-labeled amino acid analogs, imaging and therapeutic agents incorporating the same, and methods using the same

InactiveUS8293207B2High yield and stability and purityBetter quantizationIsotope introduction to heterocyclic compoundsRadioactive preparation carriersImaging agentMoiety
An amino acid analog is provided, in syn-stereoisomeric form, anti-stereoisomeric form, or a combination thereof. The amino acid analog includes a cyclobutane ring with at least one of an amine group and a carboxyl group attached to one carbon node of the cyclobutane ring. A chain of moieties X, Y, and Z attached to one of remaining three carbon nodes of the cyclobutane ring. X is a chelating agent selected from a group comprising DCTA, DOTA, DTPA, EDTA, NOTA, PCTA, and TETA. Y is a linking moiety selected from a group comprising —NH—CO— and —NH-p-CHSN-Bn- where the linking moiety facilitates incorporation of the chelating agent into the amino acid analog. Z is a metal radioisotope selected from a group comprising Cu-60, Cu-61, Cu-62, Cu-64, Cu-67, Ga-67, Ga-68, Y-86, Y-88, Y-90, Sr-85, Sr-89, Gd-153, Gd-157, Sm-153, Lu-177, W-185, Re-186, Re-188, and Ir-192.
Owner:ZAVARZIN VALERY +1

Complex comprising a psma-targeting compound linked to a lead or thorium radionuclide

The present invention relates to complexes comprising a prostate-specific membrane antigen (PSMA) targeting compound linked to a radionuclide, such as 212Pb or 227Th, through a TCMC or DOTA chelating moiety. These compounds, and pharmaceutical compositions comprising them, can be used for medical applications. These applications include the treatment of prostate cancer, and the complexes allow for dual targeting of cancers.
Owner:SCIENCONS AS

Small molecule inhibitors for early diagnosis of prostate specific membrane antigen cancers and neurodegenerative diseases

Accordingly, embodiments herein disclose a compound and method of small molecule inhibitors or ligands for diagnosis and treatment of cancers such as prostate, brain, breast, etc., and neurodegenerative diseases. A new class of PSMA inhibitors called as aminoacetamide, 1, has been designed by extensive in silico studies. A simple, mild and high yielding synthetic methodology is developed for 1 and shown to have high affinity for PSMA protein. Fluorescent conjugates 22 and 25 derived from 1 show selective uptake in prostate cancer cell lines and can be used for surgical removal of tumors during intra-operative surgery. Conjugates 31 and 34 for tagging 99mTc radioisotope were synthesized. Macrocyclic chelating cores such as DOTA, NOTA or prosthetic groups can be introduced to tag radionuclides 68Ga, 64Cu, 18F and 177Lu for diagnosis and treatment of PCa, incurable mCRPC and neurodegenerative diseases such as ALS, schizophrenia and neuropathic pain that over-express PSMA protein.
Owner:INDIAN INST OF TECH INDORE

Annular Gd (III) complex as well as preparation method and application thereof

The invention provides a cyclic Gd (III) complex which has a chemical structure as shown in a formula I, a ring structure of 1, 4, 7, 10-tetraazacyclododecane-1, 4, 7, 10-tetraacetic acid, namely DOTA, is taken as a mother ring, lipophilic groups R'and R ''in the formula I are respectively introduced to an alpha position and a benzene ring structure of phenylacetic acid, and chiral groups are introduced to a large ring position of DOTA, the chiral group R is utilized to increase the rigidity of the macrocyclic structure and improve the stability of the complex, and the lipophilic groups R'and R '' can be combined with organic anion transport polypeptide of hepatocytes, so that the distribution of the cyclic Gd (III) complex as a contrast agent in the liver and gall is greatly improved, namely, the targeting property is good.
Owner:WENZHOU INST UNIV OF CHINESE ACAD OF SCI

Preparation method of DOTATATE

The invention discloses a preparation method of DOTATATE. The method comprises the following specific steps of: sequentially coupling solid-phase carrier resin to amino acids, the N ends and side chains of which have protecting groups, according to the amino acid sequence of DOTATATE, and then, coupling DOTA(tBu)<3> so as to obtain linear peptide resin of DOTATATE; then, adding lysis solution to remove the protecting groups and cutting the resin to obtain linear peptide of DOTATATE; and finally, performing oxidization by using an oxidizing agent to obtain DOTATATE crude peptide. According to the preparation method in the invention, hydroxyl resin with easily available raw materials and low-price amino acids with side chain protection are adopted to synthesize the linear peptide resin; then, the linear peptide is cracked; the oxidizing agent easy to control is adopted to oxidize the linear peptide so as to obtain the target crude peptide; use of a highly toxic reagent is avoided; and finally, purification, salt conversion, concentration and drying are carried out, so that refined peptide is obtained. The method in the invention has the advantages of short synthesis route, easily controlled linear peptide quality, low synthesis cost, high yield and high finished product purity, and is suitable for large-scale production.
Owner:BEIJING SINOTAU INT PHARMA TECH CO LTD

Tumor targeted radionuclide therapy and molecular imaging of her2+ cancers and other neoplasms

Methods and compositions for treating, diagnosing and staging cancers, in particular overexpressing the Human Epidermal growth factor Receptor 2 protein (HER2+) given rise to in breast, gastric, gastroesophageal, ovarian, pancreatic cancer and brain tumors, which may be metastatic to the brain or other site. More specifically, the invention provides for Targeted Radionuclide Therapy (TRNT) with a compound of the invention having a peptide that targets the HER2+ cells, a second component for combining metals into complexes through a ring structure (DOTA), and a third radioisotope component, Lu-177 and Ga-68, in which embodiments further include a companion diagnostic, and in which embodiments further include anti-integrin precision medicines for cancers expressing αvβ3 and αvβ5 integrins, HER2+, vascular endothelial growth factor, vitronectin, fibronectin, tenascin, reelin, kindlin and talin. TRNT may be administered alone or in combination with standard-of-care; an immunooncologic and / or chemotherapeutic, adjuvantly or neoadjuvantly.
Owner:SATZ STANLEY

Refining method of gadadotec acid meglumine

The invention provides a preparation process and a purification process of gadadotec acid meglumine. The preparation process comprises the steps of adding purified DOTA into pure water, stirring and dissolving at room temperature, adding gadolinium oxide and microporous calcium silicate particles, adding meglumine until the pH value of the solution is 7-9, carrying out ultrasonic oscillation, filtering, heating the filtrate to the temperature of 40-50 DEG C, stirring, reacting for 2-4 hours, filtering the precipitate, and performing vacuum drying to obtain the product. The purification method provided by the invention comprises the steps of dissolving a crude product gadadotec acid meglumine in 100ml of methanol, heating while stirring until the gadadotec acid meglumine is dissolved, adding 50ml of water while stirring, stopping stirring, naturally cooling, slowly separating out fine crystals, cooling to the temperature of 5-10 DEG C after 3 hours, adding 30ml of water while stirring, stopping stirring after adding, standing for crystallization, and carrying out suction filtration on the separated white crystals, washing with a small amount of methanol, and carrying out vacuum drying at the temperature of 60 DEG C to obtain crystalline powder.
Owner:ANHUI POLY PHARM CO LTD +1

A method for detecting compounds containing dota rings or nota rings in samples

The present invention provides a method for detecting compounds containing a DOTA ring or a NOTA ring contained in a sample, wherein the compound containing a DOTA ring is, for example, (S, E)-2,2',2'-(10-(2- ((6‑amino‑1‑((4'‑((8‑amino‑1‑hydroxy‑5,7‑dithiophthalocyanine‑2‑yl)diazo)‑3,3'‑dimethyl‑ [1,1'-biphenyl]-4-yl)amino)-1-oxalkane-2-yl)amino)-2-oxyethyl)-1,4,7,10-tetraazacycle Dodecane-1,4,7-triacyl)triacetic acid or oxyoctreotide, the method comprises the steps of: using a diluent to dilute the sample, and using high performance liquid chromatography to detect the diluted sample, wherein The diluent comprises pentetic acid. The method of the invention solves the problem of the accuracy of content determination of compounds containing DOTA rings or NOTA rings. Among other things, method specificity, sensitivity, linearity and range, and solution stability were all verified to be good.
Owner:BEIJING SINOTAU INT PHARMA TECH CO LTD
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