- Method for preparing DOTA derivative
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The present invention discloses a method for preparing DOTA derivative. Firstly, take 1,4,7,10-tetraazacyclododecane and benzyl bromoacetate in a substitution reaction to obtain a first product. And, the first product is coupled to tert-butyl bromoacetate
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Paragraph 0043-0047
(2020/04/24)
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- Targeted Macrocyclic Agents for Dual Modality PET and MRI Imaging of Cancer
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Dual-modality contrast agents are disclosed herein, having the general formula: R1 includes a chelating moiety that is chelated to a Mn2+ isotope. The disclosed contrast agents differentially target a wide range of malignant tumor tissues, and can be simultaneously used as contrast agents for both magnetic resonance imaging (MRI) and positron emission topography (PET) imaging. Accordingly, the disclosed contrast agent can be used in diagnosing and monitoring solid tumor cancers.
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- RADIOACTIVE PHOSPHOLIPID METAL CHELATES FOR CANCER IMAGING AND THERAPY
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Alkylphosphocholine analogs incorporating a chelating moiety that chelates a radioactive metal isotope are disclosed herein. The alkylphophocholine analogs, which can be used to treat or detect solid tumors, have the formula: [Formula should be inserted here]. R1 includes a chelating agent that is chelated to a metal atom, wherein the metal atom is a positron or single photon emitting metal isotope with a half life of greater than or equal to 4 hours, or an alpha, beta or Auger emitting metal isotope with a half life of greater than 6 hours and less than 30 days; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is -H, -OH, -COOH, -COOX, -OCOX, or -OX, wherein X is an alkyl or an arylalkyl; R2 is -N+H3, -N+H2Z, -N+HZ2, or -N+Z3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2.
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- TARGETED RADIOTHERAPY CHELATES FOR IN SITU IMMUNE MODULATED CANCER VACCINATION
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The disclosed method of treating a malignant solid tumor in a subject includes the steps of administering to the subject an immunomodulatory dose of a radioactive phospholipid metal chelate compound that is differentially retained within malignant solid tumor tissue, and performing in situ tumor vaccination in the subject by introducing into at least one of the malignant solid tumors one or more agents capable of stimulating specific immune cells within the tumor microenvironment, or by performing another method of in situ tumor vaccination, In a non-limiting example, the radioactive phospholipid metal chelate compound has the formula (I): wherein R1 comprises a chelating agent that is chelated to a metal atom, wherein the metal atom is an alpha, beta or Auger emitting metal isotope with a half life of greater than 6 hours and less than 30 days. In one such embodiment, a is 1, n is 18, m is 0, b is 1, and R2 is -N+(CH3)3.
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- LONG-LIVED GADOLINIUM BASED TUMOR TARGETED IMAGING AND THERAPY AGENTS
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Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula: (I) or a salt therof. R1 includes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is -H, -OH, -COOH, -COOX, -OCOX, or -OX, wherein X is an alkyl or an arylalkyl; R2 is -N+H3, -N+H2Z, -N+HZ2, or -N+Z3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.
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- NOVEL NITROGEN-CONTAINING COMPOUND OR SALT THEREOF, OR METAL COMPLEX THEREOF
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The present invention provides a compound represented by the formula (1) or a salt thereof, or a complex of the compound or the salt with a metal, in the formula (1), A1 represents a chelate group; R1 represents a hydrogen atom or the like; R2 represents a hydrogen atom or the like; and Z1, Z2, Z3, Z4, and Z5 are the same or different and each represent a nitrogen atom or CR3 or the like wherein R3 represents a hydrogen atom or an optionally substituted C1-6 alkyl group or the like; L1 represents a group represented by the formula (3) wherein R13, R14, R15, and R16 are the same or different and each represent a hydrogen atom or the like; L2 represents an optionally substituted C1-6 alkylene group; and L3 represents an optionally substituted C1-6 alkylene group.
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Paragraph 0275; 0278
(2016/08/17)
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- TREATMENT AGENT FOR DIAGNOSIS OR TREATMENT OF DISEASE ASSOCIATED WITH INTEGRIN
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PROBLEM TO BE SOLVED: To provide a treatment agent for diagnosis or treatment of disease associated with integrin. SOLUTION: A treatment agent comprises a complex of a compound represented by formula (1) or salt thereof and metal. In the formula (1), A1 is a chelate group; R1 and R2 independently represent H, alkyl, or an amino protective group; Z1-Z5 independently represent N or CR3; R3 is H or a substituted/unsubstituted C1-6 alkyl group or the like; L1 is a group represented by formula (3); L2 and L3 independently represent a substituted/unsubstituted C1-6 alkylene group. In the formula (3), R13-R16 independently represent H, alkyl or the like. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
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Paragraph 0310; 0311; 0314
(2018/10/03)
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- Improved syntheses and applicability of different DOTA building blocks for multiply derivatized scaffolds
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DOTA (1,4,7,10-tetraazacyclodocecane-N,N′,N″,N?-tetraacetic acid), which forms extremely stable complexes with a large number of metal ions, is one of the most important and most commonly used chelators for in vivo applications such as cancer diagnosis an
- Waengler,Waengler,Eisenhut,Haberkorn,Mier
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p. 2606 - 2616
(2008/12/22)
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- Solid-Phase Assisted N-1 Functionalization of Azamacrocycles
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A simple solid-phase assisted strategy for the N-1 functionalization of azamacrocycles is described. Compounds such as cyclen, cyclam and piperazine can be selectively modified by temporary attachment to solid-phase resins providing an efficient and clean method to prepare biomedically interesting moieteies.
- Oliver, Morag,Jorgensen, Michael R.,Miller, Andrew D.
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p. 453 - 456
(2007/10/03)
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- Amphipatic polycarboxylic chelates and complexes with paramagnetic metals as MRI contrast agents
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Substituted polycarboxylic ligand molecules and corresponding metal complexes of said ligands, preferably paramagnetic metals complexes for generating responses in the field of magnetic resonance imaging (MRI). The paramagnetic complexes of the polycarboxylic ligands possess advantageous tensioactive properties and are useful as MRI contrast media in formulations for investigating the blood pool.
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Page column 45-46
(2010/11/29)
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