The present invention provides a bivalent bispecific antibody targeting an EGFR and a c-MET and a radioactive label thereof. The research shows that the bivalent bispecific antibody provided by the present invention has good targeting affinity, and an antibody-radionuclide conjugate (taking 177Lu radioactive label as an example) of the bivalent bispecific antibody has an excellent SPECT imaging result, can be continuously accumulated in tumors over time, is more quickly removed in organs such as the liver and normal tissues, and can exhibit lower toxic and side effects. This also indirectly shows that the bivalent bispecific antibody provided by the present invention can clinically exhibit higher safety potential.
G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer
G01N 33/68 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des protéines, peptides ou amino-acides
G01N 33/60 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des substances marquées faisant intervenir des substances marquées radioactives
G01N 33/534 - Production de composés immunochimiques marqués avec un marqueur radioactif
A61K 51/10 - Anticorps ou immunoglobulinesLeurs fragments
A GRPR and integrin αVβ3 heterodimer radionuclide drug conjugate of a novel structure, which has relatively high specificity for two receptors integrin αVβ3 and GRPR. Compared with conjugates involving single receptors, said conjugate exhibits stronger tumor uptake capacity and longer tumor retention time, and has excellent safety in clinical use. Said conjugate has a higher tumor uptake ratio and a ratio of tumors to non-target points, and further has a great potential in distinguishing a primary tumor site and a metastatic focus. Therefore, said conjugate will provide more accurate information for tumor diagnosis and staging and monitor metastasis during treatment, thereby achieving great prospects in clinical use.
The present invention provides an RGD dimer compound, a preparation method therefor and use thereof, and relates to the fields of nuclear medicine and molecular imaging. The RGD dimer compound has a structure shown in Formula (I) or Formula (I-1). The present invention further provides a radionuclide labeled compound with the RGD dimer compound shown in Formula (I-1) as a ligand, a pharmaceutical composition containing or composed of the RGD dimer compound, and a kit containing or composed of the RGD dimer compound or the pharmaceutical composition. The present invention further provides use of the RGD dimer compound or the pharmaceutical composition in diagnosis or treatment of diseases characterized by over-expression of an integrin αvβ3. The RGD dimer compound and the radionuclide labeled compound of the present invention have higher tumor uptake and a longer retention time and are expected to be used in diagnosis or treatment of diseases characterized by over-expression of the integrin αvβ3.
Disclosed is a method for treating thyroid cancer by using a fibroblast activation protein inhibitor modified with radiolabeled truncated Evans blue. The drug demonstrates good safety and tolerability in thyroid cancer patients, offering excellent therapeutic prospects in the treatment of thyroid cancer.
C07D 401/14 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant au moins trois hétérocycles
C07K 5/078 - Dipeptides le premier amino-acide étant hétérocyclique, p. ex. Pro, His, Trp
The present invention relates to a dual-targeting compound capable of targeting fibroblast activation protein (FAP) and integrin αvβ. The targeting compound of the present invention and a radionuclide marker thereof can synergistically target an FAP target and an integrin αvβ3 target in tumors, such that the number and utilization efficiency of effective receptors in tumors can be improved. The present invention further provides a radionuclide marker based on the targeting compound, a preparation method therefor and use thereof in diagnosis or treatment of diseases characterized by overexpression of fibroblast activation protein (FAP) and/or integrin αvβ3.
A method for diagnosing or imaging renal cell carcinoma using a FAPI-RGD heterodimeric radioactive compound. Compared with [18F]FDG/[68Ga]Ga-PSMA, the method has a better detection efficiency and can effectively identify pathological features of the invasiveness of RCC. For RCC patients with a higher WHO/ISUP grade, a higher pT staging, a higher clinical staging and adverse pathological features, there is a significanat increase in the uptake of the heterodimericic radioactive compound, which indicates that the heterodimeric radioactive compound has good potential for predicting the prognosis of RCC. In addition, the heterodimer radioactive compound has a prolonged residence time in tumors, and has a certain therapeutic potential.
123n2mq222-, -NH(CO)-, or -(CO)-NH-. Also provided is a radionuclide marker based on the compound structure. The compounds and the radionuclide marker have high tumor uptake and retention times and therefore are suitable for radionuclide therapy and imaging of tumors highly-expressing PSMA.
C07K 7/06 - Peptides linéaires ne contenant que des liaisons peptidiques normales ayant de 5 à 11 amino-acides
C07C 311/42 - Sulfonamides, le squelette carboné de la partie acide étant substitué de plus par des atomes d'azote liés par des liaisons simples, ne faisant pas partie de groupes nitro ou nitroso ayant l'atome de soufre d'au moins un des groupes sulfonamide lié à un atome de carbone d'un cycle aromatique à six chaînons ayant des atomes de soufre de groupes sulfonamide et des groupes amino liés à des atomes de carbone de cycles aromatiques à six chaînons du même squelette carboné ayant l'atome d'azote d'au moins un des groupes sulfonamide lié à des atomes d'hydrogène ou à un atome de carbone acyclique à un atome de carbone acyclique d'un radical hydrocarboné substitué par des groupes carboxyle
C07C 303/40 - Préparation d'esters ou d'amides d'acides sulfuriquesPréparation d'acides sulfoniques ou de leurs esters, halogénures, anhydrides ou amides d'amides d'acides sulfoniques par des réactions n'impliquant pas la formation de groupes sulfonamide
The present disclosure provides a truncated Evans Blue modified fibroblast activation protein inhibitor compound. The compound is formed by connecting truncated Evans Blue, a fibroblast activation protein inhibitor and a nuclide chelating group by means of connecting groups L1, L2, L3, L4 and X. The compound has the following structure shown in Formula (I), where R1 is a fibroblast activation protein inhibitor; L1 is lysine, glutamic acid, or a derivative structure thereof; L2 is —(CH2)n—, n is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O—, —NH—, —(CO)—, —NH(CO)—, or —(CO)—NH—; L3 is —(CH2)m—, m is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O— or —(CO)—; L4 is —(CH2)p—, p is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O—, —NH—, —(CO)—, —NH(CO)—, or —(CO)—NH—; X is selected from N, C, O, S, or
The present disclosure provides a truncated Evans Blue modified fibroblast activation protein inhibitor compound. The compound is formed by connecting truncated Evans Blue, a fibroblast activation protein inhibitor and a nuclide chelating group by means of connecting groups L1, L2, L3, L4 and X. The compound has the following structure shown in Formula (I), where R1 is a fibroblast activation protein inhibitor; L1 is lysine, glutamic acid, or a derivative structure thereof; L2 is —(CH2)n—, n is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O—, —NH—, —(CO)—, —NH(CO)—, or —(CO)—NH—; L3 is —(CH2)m—, m is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O— or —(CO)—; L4 is —(CH2)p—, p is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O—, —NH—, —(CO)—, —NH(CO)—, or —(CO)—NH—; X is selected from N, C, O, S, or
The present disclosure provides a truncated Evans Blue modified fibroblast activation protein inhibitor compound. The compound is formed by connecting truncated Evans Blue, a fibroblast activation protein inhibitor and a nuclide chelating group by means of connecting groups L1, L2, L3, L4 and X. The compound has the following structure shown in Formula (I), where R1 is a fibroblast activation protein inhibitor; L1 is lysine, glutamic acid, or a derivative structure thereof; L2 is —(CH2)n—, n is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O—, —NH—, —(CO)—, —NH(CO)—, or —(CO)—NH—; L3 is —(CH2)m—, m is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O— or —(CO)—; L4 is —(CH2)p—, p is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O—, —NH—, —(CO)—, —NH(CO)—, or —(CO)—NH—; X is selected from N, C, O, S, or
and R2 is a nuclide chelating group. The present disclosure also provides a radiolabeled complex based on the structure of the compound. The compound and the radiolabeled complex have the characteristics of significantly prolonging the half-life in blood circulation, improving the uptake and enrichment in tumors and prolonging the retention time, and are suitable for nuclide therapy and imaging of tumors with high expression of FAP.
The present disclosure provides a truncated Evans Blue modified fibroblast activation protein inhibitor compound. The compound is formed by connecting truncated Evans Blue, a fibroblast activation protein inhibitor and a nuclide chelating group by means of connecting groups L1, L2, L3, L4 and X. The compound has the following structure shown in Formula (I), where R1 is a fibroblast activation protein inhibitor; L1 is lysine, glutamic acid, or a derivative structure thereof; L2 is —(CH2)n—, n is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O—, —NH—, —(CO)—, —NH(CO)—, or —(CO)—NH—; L3 is —(CH2)m—, m is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O— or —(CO)—; L4 is —(CH2)p—, p is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O—, —NH—, —(CO)—, —NH(CO)—, or —(CO)—NH—; X is selected from N, C, O, S, or
and R2 is a nuclide chelating group. The present disclosure also provides a radiolabeled complex based on the structure of the compound. The compound and the radiolabeled complex have the characteristics of significantly prolonging the half-life in blood circulation, improving the uptake and enrichment in tumors and prolonging the retention time, and are suitable for nuclide therapy and imaging of tumors with high expression of FAP.
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
C07D 401/14 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant au moins trois hétérocycles
9.
INTERMEDIATE USED FOR FAPI SYNTHESIS, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF
An intermediate used for Evans blue modification FAPI synthesis, a method for preparing the intermediate, and an application of the intermediate in the synthesis of an Evans blue modified FAPI.
C07K 5/078 - Dipeptides le premier amino-acide étant hétérocyclique, p. ex. Pro, His, Trp
C07K 1/08 - Procédés généraux de préparation de peptides utilisant des groupes protecteurs ou des agents d'activation utilisant des agents d'activation
10.
COMPOUNDS TARGETING SSTR2, PREPARATION METHOD THEREFOR, AND USE THEREOF
The present invention relates to the fields of nuclear medicine and molecular imaging. Provided are compounds targeting SSTR2, a preparation method therefor, and the use thereof. The structure of one of the compounds targeting SSTR2 is represented by following formula (I), and the structure of the compound targeting SSTR2 and capable of being labelled with a radionuclide is represented by following formula (II). Also provided in the present invention is a radionuclide-labeled compound targeting SSTR2, said compound being obtained by labeling the compound of formula (II) with a radionuclide. Further provided in the present invention are a preparation method for the compounds represented by formula (I) and formula (II), and the use of the compounds in preparation of drugs used for diagnosing and/or treating diseases characterized by over-expression of SSTR2.
A61K 51/00 - Préparations contenant des substances radioactives utilisées pour la thérapie ou pour l'examen in vivo
A61K 47/55 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p. ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique l’agent de modification étant aussi un agent pharmacologiquement ou thérapeutiquement actif, c.-à-d. le conjugué entier étant un co-médicament, p. ex. un dimère, un oligomère ou un polymère de composés pharmacologiquement ou thérapeutiquement actifs
Provided is a dual-targeting compound against FAP and integrin αvβ3. The targeting compound and a radionuclide marker thereof can synergistically target a FAP target and an integrin αvβ3 target in tumors, such that the number of and the utilization efficiency of effective receptors in tumors can be increased. Also provided are a radionuclide marker on the basis of the targeting compound, and a preparation method therefor and use thereof in the diagnosis or treatment of a disease characterized by excessive expression of fibroblast activation protein (FAP) and/or integrin αvβ3.
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
A61P 9/10 - Médicaments pour le traitement des troubles du système cardiovasculaire des maladies ischémiques ou athéroscléreuses, p. ex. médicaments antiangineux, vasodilatateurs coronariens, médicaments pour le traitement de l'infarctus du myocarde, de la rétinopathie, de l'insuffisance cérébro-vasculaire, de l'artériosclérose rénale
A61P 17/02 - Médicaments pour le traitement des troubles dermatologiques pour traiter les blessures, les ulcères, les brûlures, les cicatrices, les cheloïdes, ou similaires
14.
Compound targeting prostate specific membrane antigen, and preparation method and application thereof
2 is a nuclide chelating group. The present disclosure also provides a radiolabeled complex based on the structure of the compound. The compound and the radiolabeled complex have appropriate blood circulation time, high uptake in tumors and long retention time, and are suitable for nuclide therapy and imaging of tumors with high expression of PSMA.
C07D 257/02 - Composés hétérocycliques contenant des cycles comportant quatre atomes d'azote comme uniques hétéro-atomes du cycle non condensés avec d'autres cycles
15.
Truncated Evans Blue modified fibroblast activation protein inhibitor, preparation method and application thereof
2— may be individually substituted or unsubstituted with —O—, —NH—, —(CO)—, —NH(CO)—, or —(CO)—NH—; X is selected from N, C, O, S, or
2 is a nuclide chelating group. The present disclosure also provides a radiolabeled complex based on the structure of the compound. The compound and the radiolabeled complex have the characteristics of significantly prolonging the half-life in blood circulation, improving the uptake and enrichment in tumors and prolonging the retention time, and are suitable for nuclide therapy and imaging of tumors with high expression of FAP.
C07D 401/14 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant au moins trois hétérocycles
16.
DUAL-TARGETING COMPOUND, AND PREPARATION METHOD THEREFOR AND USE THEREOF
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
A61P 9/10 - Médicaments pour le traitement des troubles du système cardiovasculaire des maladies ischémiques ou athéroscléreuses, p. ex. médicaments antiangineux, vasodilatateurs coronariens, médicaments pour le traitement de l'infarctus du myocarde, de la rétinopathie, de l'insuffisance cérébro-vasculaire, de l'artériosclérose rénale
A61P 17/02 - Médicaments pour le traitement des troubles dermatologiques pour traiter les blessures, les ulcères, les brûlures, les cicatrices, les cheloïdes, ou similaires
17.
COMPOUND TARGETING PROSTATE SPECIFIC MEMBRANE ANTIGEN, AND PREPARATION METHOD THEREFOR AND USE THEREOF
11n2mq222p222 is a nuclide chelating group. Further provided is a radioactive marker on the basis of the structure of the compound. The compound and the radioactive marker have a suitable blood circulation time and relatively high tumor assimilation and retention time, and are suitable for use in nuclide treatment and imaging of tumors with high expression of PSMA.
Provided is a compound targeting a prostate specific membrane antigen (PSMA). The compound has a structure as represented by formula (I), wherein R1 is a compound targeting a prostate specific membrane antigen; L1 is -(X)n-(CH 2)m-(Y)q-, wherein X and Y are independently selected from lysine, glutamic acid or a derivative structure containing lysine and glutamic acid, n is an integer from 0 to 12, m is an integer from 0 to 60, q is an integer from 0 to 12, and each CH2 can be individually replaced with -O-, -NH(CO)- or -(CO)-NH-; L2 is -(CH2)p-, wherein p is an integer from 0 to 30, each CH2 can be individually replaced with -O-, -NH(CO)-, or -(CO)-NH-; and R2 is a nuclide chelating group. Further provided is a radioactive marker on the basis of the structure of the compound. The compound and the radioactive marker have a suitable blood circulation time and relatively high tumor assimilation and retention time, and are suitable for use in nuclide treatment and imaging of tumors with high expression of PSMA.
The present disclosure provides a truncated Evans Blue modified fibroblast activation protein inhibitor compound, the molecular structure of the compound having any one of the following structures shown in Formula (II-1) to Formula (II- 8): Ng H 0 3 HNYN = Hq 54"0 NH2 0 0 c) ilk OH N = 410, rit,..,../..,y1,...Ni--,\N....7,/ 0 * 14/ 0. __ ilk -141' HN \--/ 'S.. 0 ."*--k Hd -0 ofirN N 'A \0,0 0)\'µ:NLe. N 3 1 OH HO-e 0 Formula (II-3), 0 NQk HN -.)-- NJ 0 -- HS 0 IS' 0 NH2 0 0 / OH P- * N ilkai isiN trillis=N=Thr N \--./ 0 HN 0 Hd "0 ow-N- IN ,=\,0 OH 0 t.....,N HO-re 0 Formula (11-4), 2 Date Recue/Date Received 2023-12-12 Nc, H j_..N.A1 HN. HO 0 --F F 0 ...z_\ (r \ OH N 0-- ,----\ ,...,_/ Inv N Hd "0 0 t---i OFrN N0 N 3 ' OH 0 HO-? o Formula (II-5), NC, H 0 >ILI N FIN¨)\- \...+F 0- HO0 F . ¨ NH2 0 0 0 / = ,, ,-,, ....37 Nc..1....11,i1,,,....õ....õ,i,11õrr- õõ00õ.....0.0,,,õ0õ...õ...ANT--AN. _./..._,,, \ / N ,--1 OWN N'\00 I\,,k' ) ' 0 N 1..._,N OH H04 0 Formula (II-6), 3 Date Recue/Date Recall/ad 2023-12-12 pic, H 0 µ... 0 F F ¨. WA 0 NH2 0 0 i 01 OH " Nr- '\N,j-jo * N jAL\ . ¨ \ it, .-1L..õ----TA try r...../ NV IP /- HN 0 `S.g.1 HO' \'' 0 /--1 OirN N,\00 s.,;'N i g OH HO--e 0 Formula (II-7), or Nc, H HN--)0 ..... "..N 0 F F HO 0 -.... `S") NH2 0 0 c:o 410 OH l ,p1 ii. ik, orks".yiLi--\ ..../...1 ip N/ 0. iiii. N' HN \--)1 S%0 " Hd ' 0 P--1 OHrN rs(\00 OH HO4 0 Formula (II-8). 4 Date Recue/Date Received 2023-12-12
A61K 47/54 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p. ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique
A61K 47/62 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p. ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant une protéine, un peptide ou un acide polyaminé
C07D 401/14 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant au moins trois hétérocycles
20.
DUAL-TARGETING COMPOUND AND PREPARATION METHOD AND APPLICATION THEREOF
A dual-targeting compound, and a preparation method therefor and the use thereof, which relate to the fields of nuclear medicine and molecular imaging. A radionuclide-labeled dual-targeting compound, having a structure as shown in formula (I-1) or formula (I-2). The dual-targeting compound has a high affinity to both an FAP target and an integrin ?v?3 target, can synergistically target the FAP target and the integrin ?v?3 target in tumors, and exhibits a high uptake and a long retention time in tumors. Provided are a radionuclide-labeled dual-targeting compound based on the dual-targeting compound, and a preparation method therefor and the use thereof in the preparation of a drug for diagnosing and treating diseases characterized by overexpression of FAP and/or integrin ?v?3.
A61P 9/10 - Médicaments pour le traitement des troubles du système cardiovasculaire des maladies ischémiques ou athéroscléreuses, p. ex. médicaments antiangineux, vasodilatateurs coronariens, médicaments pour le traitement de l'infarctus du myocarde, de la rétinopathie, de l'insuffisance cérébro-vasculaire, de l'artériosclérose rénale
A61P 17/02 - Médicaments pour le traitement des troubles dermatologiques pour traiter les blessures, les ulcères, les brûlures, les cicatrices, les cheloïdes, ou similaires
C07K 1/04 - Procédés généraux de préparation de peptides sur des supports
C07K 7/64 - Peptides cycliques ne comportant que des liaisons peptidiques normales
21.
RGD DIMER COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention provides an RGD dimer compound, a preparation method therefor and use thereof, and relates to the fields of nuclear medicine and molecular imaging. The RGD dimer compound has a structure shown in Formula (I) or Formula (I-1). The present invention further provides a radionuclide labeled compound with the RGD dimer compound shown in Formula (I-1) as a ligand, a pharmaceutical composition containing or composed of the RGD dimer compound, and a kit containing or composed of the RGD dimer compound or the pharmaceutical composition. The present invention further provides use of the RGD dimer compound or the pharmaceutical composition in diagnosis or treatment of diseases characterized by over-expression of an integrin αvpβ. The RGD dimer compound and the radionuclide labeled compound of the present invention have higher tumor uptake and a longer retention time and are expected to be used in diagnosis or treatment of diseases characterized by over-expression of the integrin αvpβ.
The present invention relates to a dual-targeting compound capable of targeting fibroblast activation protein (FAP) and integrin avI33. The targeting compound of the present invention and a radionuclide marker thereof can synergistically target an FAP target and an integrin avp, target in tumors, such that the number and utilization efficiency of effective receptors in tumors can be improved. The present invention further provides a radionuclide marker based on the targeting compound, a preparation method therefor and use thereof in diagnosis or treatment of diseases characterized by overexpression of fibroblast activation protein (FAP) and/or integrin 433.
A61P 9/10 - Médicaments pour le traitement des troubles du système cardiovasculaire des maladies ischémiques ou athéroscléreuses, p. ex. médicaments antiangineux, vasodilatateurs coronariens, médicaments pour le traitement de l'infarctus du myocarde, de la rétinopathie, de l'insuffisance cérébro-vasculaire, de l'artériosclérose rénale
A61P 17/02 - Médicaments pour le traitement des troubles dermatologiques pour traiter les blessures, les ulcères, les brûlures, les cicatrices, les cheloïdes, ou similaires
C07K 1/04 - Procédés généraux de préparation de peptides sur des supports
C07K 7/64 - Peptides cycliques ne comportant que des liaisons peptidiques normales
23.
COMPOUND TARGETING SSTR2, PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention relates to the fields of nuclear medicine and molecular imaging. Provided are compounds targeting SSTR2, a preparation method therefor, and the use thereof. The structure of one of the compounds targeting SSTR2 is represented by following formula (I), and the structure of the compound targeting SSTR2 and capable of being labelled with a radionuclide is represented by following formula (II). Also provided in the present invention is a radionuclide-labeled compound targeting SSTR2, said compound being obtained by labeling the compound of formula (II) with a radionuclide. Further provided in the present invention are a preparation method for the compounds represented by formula (I) and formula (II), and the use of the compounds in preparation of drugs used for diagnosing and/or treating diseases characterized by over-expression of SSTR2.
The present invention provides an intermediate used for Evans blue modified FAPI synthesis, a method for preparing the intermediate, and an application of the intermediate in the synthesis of an Evans blue modified FAPI. The use of the intermediate provided by the present invention to synthesize Evans blue modified FAPI can improve the production efficiency and reduce the production cost, and the intermediate is suitable for industrial production.
C07K 1/08 - Procédés généraux de préparation de peptides utilisant des groupes protecteurs ou des agents d'activation utilisant des agents d'activation
C07K 5/078 - Dipeptides le premier amino-acide étant hétérocyclique, p. ex. Pro, His, Trp
brevets
