DOUBLE-LABELED PROBE FOR MOLECULAR IMAGING AND USE THEREOF

The present invention relates to a compound or a pharmaceutically acceptable salt thereof having a chemical structure comprising: (A) at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; and (C) at least one dye moiety; wherein said compound has a molecular weight of not more than 5 kDa. Further, the invention refers to a method for producing such compound and to the in vivo and in vitro uses thereof. 1. A compound or a pharmaceutically acceptable salt thereof having a chemical structure comprising:(A) at least one motif specifically binding to cell membranes of neoplastic cells;(B) at least one chelator moiety of radiometals; and(C) at least one dye moiety;wherein said compound has a molecular weight of not more than 5 kDa.2. The compound according to claim 1 , wherein said compound has the following molecular structure:(A)-(B)-(C),{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein (A), (B) and (C) are defined as in .'}3. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein said compound has the following molecular structure:(A)-(B)-(C),{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein (A), (B) and (C) are defined as in , wherein (B) and (C) and (A) and (B) are conjugated with another via a spacer molecule.'}4. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein said compound has the following molecular structure:(A)-(B)-(C),wherein the “—” is a bond via a spacer molecule or a direct bond.5. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein said compound has the following molecular structure:(A)-x-(B)-y-(C),wherein x and y represent independently from another each a spacer molecule.6. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the motif specifically binding to cell membranes of neoplastic cells (A) is a motif ...

Labeled inhibitors of prostate specific membrane antigen (PSMA) as agents for the treatment of prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).

Use of labeled inhibitors of prostate specific membrane antigen (PSMA), as agents for the treatment of prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).

Double-Labeled Probe for Molecular Imaging and Use Thereof

The present invention relates to a compound or a pharmaceutically acceptable salt thereof having a chemical structure comprising: (A) at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; and (C) at least one dye moiety; wherein said compound has a molecular weight of not more than 5 kDa. Further, the invention refers to a method for producing such compound and to the in vivo and in vitro uses thereof. 1. A compound or a pharmaceutically acceptable salt thereof having a chemical structure comprising:(A) at least one motif specifically binding to cell membranes of neoplastic cells;(B) at least one chelator moiety of radiometals; and(C) at least one dye moiety;wherein said compound has a molecular weight of not more than 5 kDa.2. The compound according to claim 1 , wherein said compound has the following molecular structure:{'br': None, '(A)-(B)-(C),'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein (A), (B) and (C) are defined as in .'}3. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein said compound has the following molecular structure:{'br': None, '(A)-(B)-(C),'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein (A), (B) and (C) are defined as in , wherein (B) and (C) and (A) and (B) are conjugated with another via a spacer molecule.'}4. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein said compound has the following molecular structure:{'br': None, '(A)-(B)-(C),'}wherein the “-” is a bond via a spacer molecule or a direct bond.5. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein said compound has the following molecular structure:{'br': None, '(A)-x-(B)-y-(C),'}wherein x and y represent independently from another each a spacer molecule.6. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the motif specifically ...

Vehicle comprising a battery drive and a method for operating a vehicle of this type

Electrically driven passenger transport vehicles are supplied with energy by an external electric supply network. If the external energy supply fails, vehicles of this type require special auxiliary devices that do not rely on the supply network, for example rely on auxiliary vehicles, in order to move said vehicles again. A vehicle can move independently during a failure of the external energy supply, by switching the electric drive of said vehicle to a battery drive.

Vehicle Comprising a Battery Drive and a Method for Operating a Vehicle of this Type

Electrically driven passenger transport vehicles are supplied with energy by an external electric supply network. If the external energy supply fails, vehicles of this type require special auxiliary devices that do not rely on the supply network, for example rely on auxiliary vehicles, in order to move said vehicles again. A vehicle can move independently during a failure of the external energy supply, by switching the electric drive of said vehicle to a battery drive.

ANALYTICAL PROCESS FOR PREDICTING THE THERAPEUTIC EFFECT OF BH3 MIMETICS

The present invention relates to an analytical in vitro process for predicting the therapeutic effectiveness of at least one pharmaceutical compound in the treatment of leukemia and/or lymphoma, the process analysing the transmembrane potential of mitochondria in cells isolated from a patient by quantification of fluorescence emitted from a dye indicating induction of apoptosis.

18F-tagged inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer.

PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) LIGANDS WITH IMPROVED TISSUE SPECIFICITY

The present invention relates to a compound of formula (1), and to a complex comprising said compound and a radionuclide, and to the respective pharmaceutical composition, the compound having the following structure or a pharmaceutically acceptable salt or solvate thereof, wherein R1is H or —CH3, preferably H, wherein R2, R3and R4are independently of each other, selected from the group consisting of —CO2H, —SO2H, —SO3H, —OSO3H, —PO2H, —PO3H and —OPO3H2, Q1is selected from the group consisting of alkylaryl, arylalkyl, aryl, alkylheteroaryl, heteroarylalkyl and heteroaryl, Q2is selected from the group consisting of aryl, alkylaryl, arylalkyl, cycloalkyl, heterocycloalkyl, heteroaryl, heteroarylalkyl and alkylheteroaryl, A is a chelator residue derived from a chelator selected from the group consisting of 1,4,7,10-tetraazacyclododecane-N,N′,N″,N′″-tetraacetic acid (=DOTA), N,N″-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N″-diacetic acid, 1,4,7-triazacyclononane-1,4,7-triacetic ...

Double-labeled probe for molecular imaging and use thereof

The present invention relates to a compound or a pharmaceutically acceptable salt thereof having a chemical structure comprising: (A) at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; and (C) at least one dye moiety; wherein said compound has a molecular weight of not more than 5 kDa. Further, the invention refers to a method for producing such compound and to the in vivo and in vitro uses thereof.

Vehicle comprising a battery drive and a method for operating a vehicle of this type

Electrically driven passenger transport vehicles are supplied with energy by an external electric supply network. If the external energy supply fails, vehicles of this type require special auxiliary devices that do not rely on the supply network, for example rely on auxiliary vehicles, in order to move said vehicles again. A vehicle can move independently during a failure of the external energy supply, by switching the electric drive of said vehicle to a battery drive.

Monitoring Neuronal Signals

A monitoring device for monitoring an individual under investigation comprises a recording device for recording a neuronal signal from the individual, and a calculating device for calculating a parameter representing a quantitative measure of an anaesthesia or coma condition of the individual and being derived from the neuronal signal, wherein the calculating device is adapted for calculating a complexity parameter representing the quantitative measure of the anaesthesia or coma condition, and the calculating device includes a buffer circuit for storing at least one time series of the neuronal signal and an analysis circuit for subjecting the time series to a recurrence quantification analysis (RQA) providing the complexity parameter. Furthermore, a method includes estimating a parameter representing a quantitative measure of an anaesthesia or coma condition of an individual.

Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).

Analytical process for predicting the therapeutic effect of BH3 mimetics

The present invention relates to an analytical in vitro process for predicting the therapeutic effectiveness of at least one pharmaceutical compound in the treatment of leukemia and/or lymphoma, the process analysing the transmembrane potential of mitochondria in cells isolated from a patient by quantification of fluorescence emitted from a dye indicating induction of apoptosis.

18F—tagged inhibitors of prostate specific membrane antigen (PSMA) and their use as imaging agents for prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers and imaging agents for various disease states of prostate cancer.

Double-labeled probe for molecular imaging and use thereof

The present invention relates to a compound or a pharmaceutically acceptable salt thereof having a chemical structure comprising: (A) at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; and (C) at least one dye moiety; wherein said compound has a molecular weight of not more than 5 kDa. Further, the invention refers to a method for producing such compound and to the in vivo and in vitro uses thereof.

Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).

Labeled inhibitors of prostate specific membrane antigen (PSMA) as agents for the treatment of prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).

18F-TAGGED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer.

LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib). 114-. (canceled)16. The compound of claim 15 , wherein Chelator is a radical of:1,4,7,10-tetraazacyclododecane-N,N′,N″,N′″-tetraacetic acid (DOTA);N,N″-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N″-diacetic acid (HBED-CC);1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA);2-(4,7-bis(carboxymethyl)-1,4,7-triazonan-1-yl)pentanedioic acid (NODAGA);2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)pentanedioic acid (DOTAGA);1,4,7-triazacyclononane phosphinic acid (TRAP);1,4,7-triazacyclononane-1-[methyl(2-carboxyethyl)phosphinic acid]-4,7-bis[methyl(2-hydroxymethyl)phosphinic acid] (NOPO);3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-triene-3,6,9-triacetic acid (PCTA);N′-{5-[Acetyl(hydroxy)amino]pentyl}-N-[5-({4-[(5-aminopentyl)(hydroxy)amino]-4-oxobutanoyl}amino)pentyl]-N-hydroxysuccinamide (DFO);diethylenetriaminepentaacetic acid (DTPA);trans-cyclohexyl-diethylenetriaminepentaacetic acid (CHX-DTPA);1-oxa-4,7,10-triazacyclododecane-4,7,10-triacetic acid (oxo-Do3A);p-isothiocyanatobenzyl-DTPA (SCN-Bz-DTPA);1-(p-isothiocyanatobenzyI)-3-methyl-DTPA (1B3M);2-(p-isothiocyanatobenzyI)-4-methyl-DTPA (1M3B); or1-(2)-methyl-4-isocyanatobenzyl-DTPA (MX-DTPA).18. A radiolabeled compound of .19. A radiolabeled compound of .20. A metal complex comprising a radionuclide and a compound of .21. The metal complex of claim 20 , wherein the radionuclide is selected from Zr claim 20 , Sc claim 20 , In claim 20 , Y claim 20 , Ga claim 20 , Lu claim 20 , Tc claim 20 , Cu claim 20 , Cu claim 20 , Gd claim 20 , Gd claim 20 , Gd claim 20 , Bi claim 20 , or Ac.22. A pharmaceutical composition comprising the compound of or a pharmaceutically acceptable ...

18F - TAGGED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) AND THEIR USE AS IMAGING AGENTS FOR PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers and imaging agents for various disease states of prostate cancer. 5. The precursor or the solvate of claim 1 , wherein Ris selected from the group consisting of: methyl claim 1 , 2-ethyl claim 1 , 3-propyl claim 1 , 2- claim 1 ,3- claim 1 ,4-phenyl claim 1 , 2- claim 1 ,3- claim 1 ,4-phenylmethyl claim 1 , and 2 claim 1 ,3- claim 1 ,4-phenylpropyl.6. The precursor or the solvate of claim 1 , wherein Ris selected from the group consisting of methyl claim 1 , isopropyl claim 1 , tert-butyl claim 1 , phenyl claim 1 , and 1-naphtyl.7. A pharmaceutical composition comprising the precursor or the solvate of claim 1 , and a pharmaceutically acceptable carrier.8. A method of imaging a prostate region in a patient comprising the steps of:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(i) administering to a patient a diagnostically effective amount of the precursor or the solvate of ,'}(ii) exposing the prostate region of the patient to a scanning device to detect the 18F-tag; and(iii) obtaining an image of the prostate region of the patient by the scanning device. This application is continuation of U.S. application Ser. No. 15/915,978, filed Mar. 8, 2018; which is a continuation of PCT/EP2016/001573, filed Sep. 19, 2016, which claims priority of EP 15002800.9, filed Sep. 30, 2015, EP 16164090.9, filed Apr. 6, 2016, and EP16182764.7, filed Aug. 4, 2016. The contents of the above-identified applications are incorporated herein by reference in their entirety.The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers and imaging agents and for the various disease states of prostate cancer.Prostate cancer (PCa) is the leading cancer in the US and European population. At least 1-2 million men in the western hemisphere suffer from prostate cancer and it is estimated that the disease will strike ...

LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib). 114-. (canceled)16. The compound of claim 15 , wherein the compound is lyophilized.17. The compound of claim 15 , further comprising a pharmaceutically acceptable carrier claim 15 , wherein the compound and the pharmaceutically acceptable carrier are lyophilized.18. The compound of claim 17 , wherein the pharmaceutically acceptable carrier is selected from mannitol claim 17 , lactose claim 17 , glucose claim 17 , and albumin.21. The compound of claim 20 , wherein the radionuclide is chosen from Zr claim 20 , Sc claim 20 , In claim 20 , Y claim 20 , Ga claim 20 , Lu claim 20 , Tc claim 20 , Cu claim 20 , Cu claim 20 , Gd claim 20 , Gd claim 20 , Gd claim 20 , Bi claim 20 , or Ac.22. The compound of claim 20 , wherein the radionuclide is chosen from Cu claim 20 , Cu claim 20 , Ga claim 20 , Lu claim 20 , or Ac.23. The compound of claim 20 , wherein the radionuclide is Ga.24. The compound of claim 20 , wherein the radionuclide is Lu.25. The compound of claim 20 , wherein the radionuclide is Ac.26. The compound of claim 20 , wherein the radionuclide is chosen from Cu or Cu.27. The compound of claim 21 , wherein the radionuclide is chosen from Cu claim 21 , Cu claim 21 , Ga claim 21 , Lu claim 21 , or Ac.28. The compound of claim 21 , wherein the radionuclide is Ga.29. The compound of claim 21 , wherein the radionuclide is Lu.30. The compound of claim 21 , wherein the radionuclide is Ac.31. The compound of claim 21 , wherein the radionuclide is chosen from Cu or Cu.33. The composition of claim 32 , wherein the radionuclide is chosen from Zr claim 32 , Sc claim 32 , In claim 32 , Y claim 32 , Ga claim 32 , Lu claim 32 , Tc claim 32 , Cu claim 32 , Cu claim 32 , Gd ...

LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) AS AGENTS FOR THE TREATMENT OF PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib). 114-. (canceled)16. A composition comprising:{'claim-ref': {'@idref': 'CLM-00015', 'claim 15'}, '(1) the compound and/or a salt thereof according to ; and'}(2) optionally a pharmaceutically acceptable carrier.17. The composition of claim 16 ,wherein the composition further comprises an excipient, andwherein the excipient is different from said pharmaceutically acceptable carrier.18. The composition of claim 16 , wherein the composition is a buffered solution.19. The composition of claim 16 , wherein the pharmaceutically acceptable carrier is selected from mannitol claim 16 , lactose claim 16 , glucose claim 16 , albumin claim 16 , or a combination thereof.21. A composition comprising:{'claim-ref': {'@idref': 'CLM-00020', 'claim 20'}, '(1) the compound and/or a salt thereof according to ; and'}(2) optionally a pharmaceutically acceptable carrier.22. The composition of claim 21 ,wherein the composition further comprises an excipient, andwherein the excipient is different from said pharmaceutically acceptable carrier.23. The composition of claim 21 , wherein the composition is a buffered solution.24. The composition of claim 21 , wherein the pharmaceutically acceptable carrier is selected from mannitol claim 21 , lactose claim 21 , glucose claim 21 , and albumin.26. A composition comprising:{'claim-ref': {'@idref': 'CLM-00025', 'claim 25'}, '(1) the compound and/or a salt thereof according to ; and'}(2) optionally a pharmaceutically acceptable carrier.27. The composition of claim 26 ,wherein the composition further comprises an excipient, andwherein the excipient is different from said pharmaceutically acceptable carrier.28. The composition of claim 26 , wherein ...

18F - TAGGED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) AND THEIR USE AS IMAGING AGENTS FOR PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers and imaging agents for various disease states of prostate cancer. 5. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable prodrug claim 1 , salt claim 1 , or ester thereof claim 1 , and a pharmaceutically acceptable carrier.6. The compound of claim 1 , for use in a method of imaging in a patient.7. The compound of claim 1 , for use in a method of diagnosing prostate cancer and/or metastasis thereof.8. The compound of claim 1 , for use in a method of treating prostate cancer and/or metastasis thereof.9. The pharmaceutical composition of claim 5 , for use in a method of imaging in a patient.10. The pharmaceutical composition of claim 5 , for use in a method of diagnosing prostate cancer and/or metastasis thereof.11. The pharmaceutical composition of claim 5 , for use in a method of treating prostate cancer and/or metastasis thereof. This application is a continuation of PCT/EP2016/001573, filed Sep. 19, 2016, which claims priority of EP 15002800.9, filed Sep. 30, 2015, EP 16164090.9, filed Apr. 6, 2016, and EP16182764.7, filed Aug. 4, 2016. The contents of the above-identified applications are incorporated herein by reference in their entirety.The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers and imaging agents and for the various disease states of prostate cancer.Prostate cancer (PCa) is the leading cancer in the US and European population. At least 1-2 million men in the western hemisphere suffer from prostate cancer and it is estimated that the disease will strike one in six men between the ages of 55 and 85. There are more than 300.000 new cases of prostate cancer diagnosed each year in USA. The mortality from the disease is second only to lung cancer. Currently anatomic methods, such as computed tomography (CT), magnetic ...

LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib). 4. A radiolabeled compound comprising the compound of .5. A metal complex comprising a radionuclide and a compound of .6. The metal complex of claim 5 , wherein the radionuclide is In claim 5 , Y claim 5 , Ga claim 5 , Lu claim 5 , Tc claim 5 , Cu claim 5 , Gd claim 5 , Gd claim 5 , Gd claim 5 , Bi claim 5 , Ac or Fe.7. A pharmaceutical composition comprising the compound of or a pharmaceutically acceptable salt claim 1 , or ester thereof claim 1 , and a pharmaceutically acceptable carrier.8. The compound of for use in a method of imaging in a patient.9. The compound of for use in a method of diagnosing prostate cancer and/or metastasis thereof.10. The compound of for use in a method of treating prostate cancer and/or metastasis thereof.11. A pharmaceutical composition comprising the metal complex of claim 5 , or a pharmaceutically acceptable salt claim 5 , or ester thereof claim 5 , and a pharmaceutically acceptable carrier.12. The metal complex of for use in a method of imaging in a patient.13. The metal complex of for use in a method of diagnosing prostate cancer and/or metastasis thereof.14. The metal complex of for use in a method of treating prostate cancer and/or metastasis thereof. This application is a continuation-in-part application of international patent application Serial No. PCT/EP2014/002808 filed Oct. 17, 2014, which published as PCT Publication No. WO 2015/055318 on Apr. 23, 2015, which claims benefit of European patent application Serial Nos. 13004991.9 filed Oct. 18, 2013 and 14175612.2 filed Jul. 3, 2014.The foregoing applications, and all documents cited therein or during their prosecution (“appln cited documents”) and all documents cited ...

LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib). 4. A radiolabeled compound comprising the compound of .5. A metal complex comprising a radionuclide and a compound of .6. The metal complex of claim 5 , wherein the radionuclide is In claim 5 , Y claim 5 , Ga claim 5 , Lu claim 5 , Tc claim 5 , Cu claim 5 , Gd claim 5 , Gd claim 5 , Gd claim 5 , Bi claim 5 , Ac or Fe.7. A pharmaceutical composition comprising the compound of or a pharmaceutically acceptable salt claim 1 , or ester thereof claim 1 , and a pharmaceutically acceptable carrier.8. The compound of for use in a method of imaging in a patient.9. The compound of for use in a method of diagnosing prostate cancer and/or metastasis thereof.10. The compound of for use in a method of treating prostate cancer and/or metastasis thereof.11. A pharmaceutical composition comprising the metal complex of claim 5 , or a pharmaceutically acceptable salt claim 5 , or ester thereof claim 5 , and a pharmaceutically acceptable carrier.12. The metal complex of for use in a method of imaging in a patient.13. The metal complex of for use in a method of diagnosing prostate cancer and/or metastasis thereof.14. The metal complex of for use in a method of treating prostate cancer and/or metastasis thereof. This application is a continuation-in-part application of international patent application Serial No. PCT/EP2014/002808 filed Oct. 17, 2014, which published as PCT Publication No. WO 2015/055318 on Apr. 23, 2015, which claims benefit of European patent application Serial Nos. 13004991.9 filed Oct. 18, 2013 and 14175612.2 filed Jul. 3, 2014.The foregoing applications, and all documents cited therein or during their prosecution (“appln cited documents”) and all documents cited ...

A double-labeled probe for molecular imaging and use thereof

The present invention relates to a compound of a pharmaceutically acceptable salt thereof of formula (I) wherein (A) is at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; (C) a dye moiety; x 1 is a spacer or a chemical single bond covalently connecting (A) to the rest of the molecule; x 2 is a spacer or a chemical single bond covalently connecting (C) to the rest of the molecule. The invention further relates to compositions comprising said compounds as well as a method for detecting neoplastic cells in a sample in vitro with the aid of the compounds or composition.

A double-labeled probe for molecular imaging and use thereof

The present invention relates to a compound or a pharmaceutically acceptable salt thereof having a chemical structure comprising: A compound or a pharmaceutically acceptable salt thereof of formula (I): (A)-x 1 -(B)-x 2 -(C), wherein (A) is at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; (C) a dye moiety; x 1 is a spacer covalently connecting (A) and (B); x 2 is a spacer or a chemical single bond connecting (B) and (C); wherein (C) has the formula wherein R 1 to R 4 , R 9 , a, b, Y and X 1 to X 4 have the meaning as indicated in the claims and description. The invention further relates to compositions comprising said compounds as well as a method for detecting neoplastic cells in a sample in vitro with the aid of the compounds or composition

LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib). 4. A radiolabeled compound comprising the compound of .5. A metal complex comprising a radionuclide and a compound of .6. The metal complex of claim 5 , wherein the radionuclide is In claim 5 , Y claim 5 , Ga claim 5 , Lu claim 5 , Tc claim 5 , Cu claim 5 , Gd claim 5 , Gd claim 5 , Gd claim 5 , Bi claim 5 , Ac or Fe.7. A pharmaceutical composition comprising the compound of or a pharmaceutically acceptable salt claim 1 , or ester thereof claim 1 , and a pharmaceutically acceptable carrier.8. The compound of for use in a method of imaging in a patient.9. The compound of for use in a method of diagnosing prostate cancer and/or metastasis thereof.10. The compound of for use in a method of treating prostate cancer and/or metastasis thereof.11. A pharmaceutical composition comprising the metal complex of claim 5 , or a pharmaceutically acceptable salt claim 5 , or ester thereof claim 5 , and a pharmaceutically acceptable carrier.12. The metal complex of for use in a method of imaging in a patient.13. The metal complex of for use in a method of diagnosing prostate cancer and/or metastasis thereof.14. The metal complex of for use in a method of treating prostate cancer and/or metastasis thereof. This application is a continuation-in-part application of international patent application Serial No. PCT/EP2014/002808 filed Oct. 17, 2014, which published as PCT Publication No. WO 2015/055318 on Apr. 23, 2015, which claims benefit of European patent application Serial Nos. 13004991.9 filed Oct. 18, 2013 and 14175612.2 filed Jul. 3, 2014.The foregoing applications, and all documents cited therein or during their prosecution (“appln cited documents”) and all documents cited ...

MARKED MEMBRANE-SPECIFIC PROSTATIC ANTIGEN (PSMA) INHIBITORS INCLUDING CARBOXYL GROUPS AND A MODIFIED BINDER REGION, IMAGING AGENTS, AND UNDERSTANDING PHARMACEUTICAL AGENTS

Esta referido a compuestos de Formula Ia o Ib, en donde: Z es -CO2H, -SO2H, -SO3H, -SO4H, -PO2H, -PO3H, -PO4H2; n es 0, 1; Y es arilo, alquilarilo, ciclopentilo, entre otros; m es 1, 2, 3, 4; X es naftilo, fenilo, bifenilo, entre otros; Quelante es DOTA, HBED-CC, NOTA, entre otros. Estos compuestos son radiofarmacos y se emplean en medicina nuclear como trazadores, agentes formadores de imagenes y para el tratamiento de diversos estados patologicos de cancer de prostata. It refers to compounds of Formula Ia or Ib, where: Z is -CO2H, -SO2H, -SO3H, -SO4H, -PO2H, -PO3H, -PO4H2; n is 0.1; Y is aryl, alkylaryl, cyclopentyl, among others; m is 1, 2, 3, 4; X is naphthyl, phenyl, biphenyl, among others; Chelator is DOTA, HBED-CC, NOTE, among others. These compounds are radiopharmaceuticals and are used in nuclear medicine as tracers, imaging agents, and for the treatment of various disease states of prostate cancer.

18f-tagged inhibitors of prostate specific membrane antigen (psma) and their use as imaging agents for prostate cancer

The present invention relates generally to the field of radiopharmaceuticals and their use in nuclear medicine as tracers and imaging agents for various disease states of prostate cancer. More particularly, the present invention discloses compounds comprising PMSA-targeting moiety, lipophilic and hydrophobic linkers, and an 18F tag, pharmaceutical compositions comprising same and uses therefor. The compounds of the present invention may have improved efficacy as tracers and imaging agents for various disease states of prostate cancer.

18f-tagged inhibitors of prostate specific membrane antigen (psma) and their use as imaging agents for prostate cancer

Vehicle comprising a battery drive and a method for operating a vehicle of this type

Elektrisch angetriebene Nahverkehrs- und Regionalverkehrs-Personentransportmittel werden in der Regel von externen elektrischen Versorgungsnetzen mit Energie versorgt. Falls diese externe Energieversorgung ausfällt, benötigen solche Fahrzeuge 1 spezielle fahrleitungsunabhängige Hilfseinrichtungen, wie z.B. Hilfsfahrzeuge, um diese Fahrzeuge 1 weiterbewegen zu können. Die vorliegende Erfindung offenbart nun ein Fahrzeug 1, welches bei Ausfall der externen Energieversorgung eigenständig bewegt werden kann, indem der elektrische Antrieb 3 des Fahrzeuges 1 auf einen Batteriebetrieb umgeschaltet wird.

A double-labeled probe for molecular imaging and use thereof

The present invention relates to a compound or a pharmaceutically acceptable salt thereof of formula (I) wherein (A) is at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; (C) a dye moiety; x

18f-tagged inhibitors of prostate specific membrane antigen (psma) and their use as imaging agents for prostate cancer

Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (la) or (Ib).

Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (la) or (lb).

Psma targeting urea-based ligands for prostate cancer radiotherapy and imaging

The present invention provides novel PSMA targeting urea-based ligands that binds to prostate‐specific membrane antigen (PSMA) which is expressed 8-to-12-fold higher in prostate cancer cells when compared to healthy tissue. The PSMA targeting urea-based ligands comprises a chelating agent that may comprise a metal and a halogen radioisotope of fluorine, iodine, bromine or astatine. The invention further relates to a method for providing the PSMA targeting urea-based ligands of the invention, to precursors of the PSMA targeting urea-based ligands and to the PSMA targeting urea-based ligands use in radiotherapy, imaging and theranostic.

Vehicle comprising a battery drive and a method for operating a vehicle of this type

Electrically driven local and regional means of passenger transport are as a rule supplied with energy by external electric supply networks. If said external energy supply fails, vehicles (1) of this type require special auxiliary devices that do not rely on aerial contact lines, e.g. auxiliary vehicles, in order to move said vehicles again (1). The invention relates to a vehicle (1), which can move independently during a failure of the external energy supply, by switching the electric drive (3) of said vehicle (1) to a battery drive.

Vehicle comprising a battery drive and a method for operating a vehicle of this type

Prostate specific membrane antigen (psma) ligands comprising an amylase cleavable linker

In particular, the present invention relates to a PSMA binding ligand comprising an oligosaccharide building block which comprises a bond being cleavable by alpha-amylase. Typically, this PSMA binding ligand further comprises a PSMA binding motif Q and a chelator residue A, wherein the PSMA binding motif Q and the chelator residue A are preferably linked via at least one linker A-L AQ -Q comprising the oligosaccharide building block, the PSMA binding ligand thus preferably having the structure (I) or a pharmaceutically acceptable salt or solvate thereof

Enhanced 18f-labeled inhibitors of the prostate-specific membrane antigen (psma) and its use as imaging agents for prostate cancer

La presente invención generalmente se refiere al campo de los radiofármacos y a su uso en medicina nuclear como trazadores y agentes de formación de imágenes para diversos estados de enfermedad del cáncer de próstata The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers and imaging agents for various stages of prostate cancer disease.

18f-tagged inhibitors of prostate specific membrane antigen (psma) and their use as imaging agents for prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers and imaging agents for various disease states of prostate cancer.

Inhibiteurs marqués par f18 de l'antigène membranaire spécifique de la prostate (psma) et leur utilisation comme agents d'imagerie pour le cancer de la prostate

La présente invention concerne de façon générale le domaine des produits radio-pharmaceutiques et leur utilisation en médecine nucléaire comme traceurs et agents d'imagerie pour le traitement de divers états pathologiques du cancer de la prostate.

Fahrzeug mit batteriefahrt und verfahren zum betrieb eines solchen fahrzeuges

Prostate specific membrane antigen (psma) ligands with improved renal clearance

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of PSMA-expressing cancers, especially prostate cancer, and metastases thereof. In particular, the present invention relates to a PSMA binding ligand or a pharmaceutically acceptable salt or solvate thereof comprising a PSMA binding motif Q and a chelator residue A linked via at least one linker LAQ, the linker comprising at least one N-alkylated, preferably N-methylated amino acid.

Prostate specific membrane antigen (psma) ligands

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of PSMA-expressing cancers, especially prostate cancer, and metastases thereof. In particular, the present invention relates to a PSMA binding ligand or a pharmaceutically acceptable salt or solvate thereof as well as to the use of said PSMA binding ligand, the PSMA binding ligand comprising a PSMA binding motif Q and a chelator residue A linked via at least one linker L AQ comprising at least one, optionally N-alkylated, neutral amino acid X i .

Dosage of psma-ligands for fluorescence based detection of cancerous tissue

The present invention relates to a use of a labeling compound having a chemical structure of formula (I): (A)-x1-(B)-x2-(C), wherein (A) is at least one motif specifically binding to cell membranes of cancer cells; (B) at least one chelator moiety; (C) a dye moiety; x1 is a spacer covalently connecting (A) and (B); x2 is a spacer or a chemical single bond connecting (B) and (C), or a pharmaceutically acceptable salt thereof, as a labeling agent for detecting cancerous tissue in a subject, said use comprising administration of a labeling dose of said labeling compound to said subject; and to compounds for use, and methods related thereto.

Prostate specific membrane antigen (psma) ligands

The present invention generally relates to the field of dye labelled, preferably fluorescent dye labelled, radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of PSMA-expressing cancers, especially prostate cancer, and metastases thereof as well as their use in preoperative PET Imaging and Fluorescence-Guided Surgery of cancers, especially prostate cancer, and metastases thereof. In particular, the present invention relates to a PSMA binding ligand or a pharmaceutically acceptable salt or solvate thereof comprising a PSMA binding motif Q and a chelator residue A and a dye group Z a linker L1 and a linker L2, the compound preferably having the structure Z-L2-A-L1-Q.

Prostate specific membrane antigen (psma) ligands

The present invention generally relates to the field of dye labelled, preferably fluorescent dye labelled, radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of PSMA-expressing cancers, especially prostate cancer, and metastases thereof as well as their use in preoperative PET Imaging and Fluorescence-Guided Surgery of cancers, especially prostate cancer, and metastases thereof.

Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer

分子イメージングのための二重標識プローブ及びその使用

【課題】改善された腫瘍対臓器比を有する、特定の化合物を提供する。【解決手段】式(I)：(A)-x1-(B)-x2-(C)(式中、(A)は、新生細胞の細胞膜に特異的に結合する少なくとも1つのモチーフであり；(B)は、少なくとも1つの放射性金属のキレート剤部分であり；(C)は、色素部分であり；x1は、(A)と(B)を共有結合的に結合するスペーサーであり；x2は、(B)と(C)を結合するスペーサー又は化学的単結合であり；ここで(C)は、式：JPEG2023145464000053.jpg2473で表される化合物又はその薬学的に許容される塩である。【選択図】なし

Σημασμενοι me 18f αναστολεις του ειδικου προστατικου αντιγονου της μεμβρανης (psma) και χρηση τους ως απεικονιστικα μεσα για τον καρκινο του προστατη

Η παρούσα εφεύρεση γενικά σχετίζεται με το πεδίο των ραδιοφαρμακευτικών προϊόντων και την χρήση τους στην πυρηνική ιατρική ως ιχνηθέτες και απεικονιστικά μέσα για διάφορες καταστάσεις νόσου του καρκίνου του προστάτη.

Prostataspesifisen membraaniantigeenin (psma) leimattuja estäjiä, niiden käyttö kuvantamisaineina ja farmaseuttisia aineita eturauhassyövän hoitoon

Double-labeled probe for molecular imaging and use thereof

The present invention relates to a compound or a pharmaceutically acceptable salt thereof having a chemical structure comprising: A compound or a pharmaceutically acceptable salt thereof of formula (I): (A)-x 1 -(B)-x 2 -(C), wherein (A) is at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; (C) a dye moiety; x 1 is a spacer covalently connecting (A) and (B); x 2 is a spacer or a chemical single bond connecting (B) and (C); wherein (C) has the formula wherein R 1 to R 4 , R 9 , a, b, Y and X 1 to X 4 have the meaning as indicated in the claims and description. The invention further relates to compositions comprising said compounds as well as a method for detecting neoplastic cells in a sample in vitro with the aid of the compounds or composition.

Verfahren zum Herstellen und Montieren eines Bauteils und Transportschutzhülle eines Bauteils

Označeni zaviralci za prostato specifičnega membranskega antigena (PSMA), njihova uporaba kot kontrastna sredstva in farmacevtska sredstva za zdravljenje raka prostate

Oznaczone inhibitory specyficznego dla prostaty antygenu błonowego (psma), ich zastosowanie jako środków obrazujących i środków farmaceutycznych do leczenia raka gruczołu krokowego

Označeni inhibitori prostata specifičnog membranskog antigena (psma), njihova upotreba kao sredstava za snimanje i farmaceutska sredstva za liječenje raka prostate

Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer.Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).

Obeleženi inhibitori membranskog antigena specifičnog za prostatu (psma), njihova upotreba kao agenasa za snimanje i farmaceutskih agenasa za lečenje karcinoma prostate

Žymėti prostatos specifinio membranos antigeno (psma) inhibitoriai, jų naudojimas kaip vizualizavimo medžiagų ir farmacinių medžiagų prostatos vėžiui gydyti

Mærkede hæmmere af prostataspecifikt membranantigen (psma), deres anvendelse som billeddannelsesmidler og farmaceutiske midler til behandling af prostatacancer

18f - tagged inhibitors of prostate specific membrane antigen (psma) and their use as imaging agents for prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers and imaging agents for various disease states of prostate cancer.

Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer.Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).

Improved 18f-tagged inhibitors of prostate specific membrane antigen (psma) and their use as imaging agents for prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers and imaging agents for various disease states of prostate cancer.

18F-tagged inhibitors of prostate specific membrane antigen (PSMA) and their use as imaging agents for prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers and imaging agents for various disease states of prostate cancer.

Analytical process for predicting the therapeutic effect of bh3 mimetics

The present invention relates to an analytical in vitro process for predicting the therapeutic effectiveness of at least one pharmaceutical compound in the treatment of leukemia and/or lymphoma, the process analysing the transmembrane potential of mitochondria in cells isolated from a patient by quantification of fluorescence emitted from a dye indicating induction of apoptosis.

Inhibidores marcados de antígeno prostático específico de membrana (psma), su uso como agentes formadores de imágenes y agentes farmacéuticos para el tratamiento de cáncer de próstata

La presente invención se refiere en general al campo de los radiofármacos y su uso en medicina nuclear como trazadores, agentes de imagen y para el tratamiento de diversos estados patológicos del cáncer de próstata. Por tanto, la presente invención se refiere a compuestos que están representados por las Fórmulas generales (Ia) o (Ib). (Traducción automática con Google Translate, sin valor legal)

Labeled inhibitors of prostate specific membrane antigen (psma) as agents for the treatment of prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).