The present invention relates to the field of organic chemistry, in particular to the synthesis of iodinated contrast agents. More in particular, the invention relates to a sustainable process for the synthesis of iopamidol which allows to improve the purity profile of the product and avoids the use of potentially hazardous reagents and solvents.
C07C 231/12 - Préparation d'amides d'acides carboxyliques par des réactions n'impliquant pas la formation de groupes carboxamide
C07C 231/14 - Préparation d'amides d'acides carboxyliques par formation de groupes carboxamide combinée avec des réactions n'impliquant pas les groupes carboxamide
C07C 237/46 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle aromatique à six chaînons non condensé du squelette carboné ayant des atomes de carbone de groupes carboxamide, des groupes amino et au moins trois atomes de brome ou d'iode liés à des atomes de carbone du même cycle aromatique à six chaînons non condensé
C07C 235/48 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des atomes d'oxygène ayant des atomes de carbone de groupes carboxamide liés à des atomes de carbone de cycles aromatiques à six chaînons et des atomes d'oxygène, liés par des liaisons simples, liés au même squelette carboné avec des atomes de carbone de groupes carboxamide et des atomes d'oxygène, liés par des liaisons simples, liés à des atomes de carbone du même cycle aromatique à six chaînons non condensé ayant l'atome d'azote d'au moins un des groupes carboxamide lié à un atome de carbone acyclique d'un radical hydrocarboné substitué par des atomes d'oxygène liés par des liaisons simples
The present invention relates to the field of optical imaging. More particularly, it relates to compounds of the cyanine family with near-infrared emission characterized by improved physico-chemical and biological properties and to conjugates with biological ligands thereof. The invention also relates to the use of these compounds as optical diagnostic agents in imaging or therapy of solid tumors, to the methods for their preparation and to the compositions comprising them.
C07D 403/10 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne carbonée contenant des cycles aromatiques
C07D 403/14 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
C09B 23/01 - Colorants méthiniques ou polyméthiniques, p. ex. du type cyanine caractérisés par la chaîne méthinique
09 - Appareils et instruments scientifiques et électriques
10 - Appareils et instruments médicaux
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Recorded medical computer software for the centralized collection, storage, management, visualization, communication and reporting of data coming from medical imaging devices to be used in association with medical imaging procedures; recorded medical computer software for creating and distributing injection protocols for medical imaging devices to be used in association with medical imaging procedures; downloadable medical computer software for the centralized collection, storage, management, visualization, communication and reporting of data coming from medical imaging devices to be used in association with medical imaging procedures; downloadable medical computer software for creating and distributing injection protocols for medical imaging devices to be used in association with medical imaging procedures; software as a medical device [SaMD], recorded, for the centralized collection, storage, management, visualization, communication and reporting of data coming from medical imaging devices to be used in association with medical imaging procedures; software as a medical device [SaMD], downloadable, for the centralized collection, storage, management, visualization, communication and reporting of data coming from medical imaging devices to be used in association with medical imaging procedures; software as a medical device [SaMD], recorded, for creating and distributing injection protocols for medical imaging devices to be used in association with medical imaging procedures; Software as a medical device [SaMD], downloadable, for creating and distributing injection protocols for medical imaging devices to be used in association with medical imaging procedures. Contrast delivery products, namely, contrast injectors, syringes, tubing, hand-held controls for delivering contrast media to patients during medical procedures. Design and development of software for use in the medical field; installation of software, maintenance of software, and updating of software for use in the medical field; software as a service (saas) services featuring medical computer software for the centralized collection, storage, management, visualization, communication and reporting of data coming from medical imaging devices to be used in association with medical imaging procedures; software as a service (saas) services featuring medical computer software for creating and distributing injection protocols for medical imaging devices to be used in association with medical imaging procedures.
5.
PROCESS FOR THE PREPARATION OF 2,4,6-TRIIODOISOPHTHALIC BISAMIDES
The present invention relates to a novel process for the preparation of 2,4,6-triiodoisophthalic bisamide derivatives, which are useful intermediates in the preparation of non-ionic X-ray contrast agents, starting from the corresponding acyl chloride intermediates which are amidated in a mixture of specific hydrotropic solvents in the presence of a low amount of water. In addition, the invention relates to the use of such hydrotropic solvents in the preparation of said 2,4,6-triiodoisophthalic bisamide intermediates to produce non-ionic X-ray contrast agents.
C07C 237/32 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle aromatique à six chaînons non condensé du squelette carboné ayant l'atome d'azote du groupe carboxamide lié à un atome de carbone acyclique d'un radical hydrocarboné substitué par des atomes d'oxygène
6.
PROCESS FOR MANUFACTURING A MIXTURE COMPRISING A DIMERIC MACROCYCLE INTERMEDIATE OF A GADOLINIUM COMPLEX
The present invention relates to a process for the manufacturing of a mixture comprising the intermediate 1-[bis[2-hydroxy-3-[4,7,10-tris[2-(1,1-dimethylethoxy)-2-oxoethyl]-1,4,7,10-tetraazacyclododec-1-yl]propyl]amino]-1-deoxy-D-glucitol. Such intermediate is useful for the synthesis of the dimeric gadolinium complex [μ-[1-[bis[2-(hydroxy-κO)-3-[4,7,10-tris[(carboxy-κO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-κN1,κN4,κN7,κN10]propyl]amino]-1-deoxy-D-glucitolate(6-)]]digadolinium complex, which can be employed as a contrast agent in the field of diagnostic imaging, and in particular of Magnetic Resonance Imaging (MRI).
3636366-polyhydroxylketone with hydroxylamine or ions thereof, or with ammonia or ions thereof, and by subsequently electrolyzing the solution obtained in the previous step.
The invention relates to a process for the preparation of the gadolinium dimeric contrast agent [p-[1-[bis[2-(hydroxy-KO)-3-[4,7,10-tris[(carboxy-KO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-K/V1,K/V4,K/V7,K/V10]propyl]amino]-1-deoxy-D-glucitolato(6-)]]di-gadolinium complex. Such process includes preparation steps carried out one-pot and without isolation of the obtained intermediates. The gadolinium dimeric contrast agent can be for use in diagnostic imaging, in particular in Magnetic resonance Imaging (MRI).
The present invention relates to the industrial preparation of non-ionic X-ray contrast agents. In particular, it relates to a process for the synthesis of lopamidol using a reactive extrusion process in continuous which enable an efficient conversion of the relevant key intermediates, preferably in the absence of any solvent. The invention further relates to the preparation of radiographic X-rays contrast agents or key intermediates thereof by exploiting the technology of reactive extrusion.
C07C 231/02 - Préparation d'amides d'acides carboxyliques à partir d'acides carboxyliques ou à partir de leurs esters, anhydrides ou halogénures par réaction avec de l'ammoniac ou des amines
C07C 231/12 - Préparation d'amides d'acides carboxyliques par des réactions n'impliquant pas la formation de groupes carboxamide
C07C 231/14 - Préparation d'amides d'acides carboxyliques par formation de groupes carboxamide combinée avec des réactions n'impliquant pas les groupes carboxamide
C07C 237/46 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle aromatique à six chaînons non condensé du squelette carboné ayant des atomes de carbone de groupes carboxamide, des groupes amino et au moins trois atomes de brome ou d'iode liés à des atomes de carbone du même cycle aromatique à six chaînons non condensé
09 - Appareils et instruments scientifiques et électriques
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Image processing software for increasing the image
enhancement in contrast-enhanced images during medical
examinations. Software as a service (SAAS) services featuring image
processing software for increasing the image enhancement in
contrast-enhanced images during medical examinations.
09 - Appareils et instruments scientifiques et électriques
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
(1) Image processing software for increasing the image enhancement in contrast-enhanced images during medical examinations. (1) Software as a service (SAAS) services featuring image processing software for increasing the image enhancement in contrast-enhanced images during medical examinations.
The present invention relates to the RRR/SSS pair of enantiomers of the of Gd(PCTA-tris-glutamic acid), the single enantiomers of the pair, the pharmaceutically acceptable salts thereof, their amide derivatives, and compositions comprising at least 50% of these compounds.
C07F 5/00 - Composés contenant des éléments des groupes 3 ou 13 du tableau périodique
13.
TRAINING OF A MACHINE LEARNING MODEL FOR USE IN MEDICAL IMAGING APPLICATIONS BASED ON COMBINATIONS OF INCOMPLETE SAMPLE SETS AND SAMPLE IMAGES SIMULATED THEREFROM
A solution is proposed for training a machine learning model (305) for use in medical imaging applications. A corresponding method (400) comprises providing (403-410) incomplete sample sets for each imaging procedure, each comprising a sample target image (or more) for a sample target-dose of a contrast agent and a sample baseline image (or more). A sample source image (or more) is simulated (411- 445; 450-456) from each of the incomplete sample sets (or a part thereof) to mimic the contrast agent at a sample source-dose lower than the sample target-dose. One or more complete sample sets are generated (446; 457) for each imaging procedure by combining the incomplete sample sets with the sample source images that have been simulated from other incomplete sample sets. The machine learning model (305) is then trained (458-473) using the complete sample sets. In addition, a method of using the machine learning model in a medical imaging application is proposed. A computer programs (300) and a computer program products for implementing the method (400) are proposed. Moreover, a computing system (130) for performing the method (400) is proposed. A corresponding medical method is further proposed.
The invention relates to a process for the manufacturing of a solution of a dimeric C gadolinium complex, such as [μ-[1-[bis[2-(hydroxy-xO)-3-[4,7,10-tris[(carboxy-xO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-κN1,κN4, κN7,κN10]propyl]amino]-1-deoxy-D-glucitolate(6-)]]digadoliniumcomplex, which is useful in the field of diagnostic imaging and of contrast agents in Magnetic Resonance Imaging (MRI), comprising the steps of precipitating a portion of free gadolinium metal ions by means of a precipitating agent. The invention further relates to a process for isolating the dimeric gadolinium complex from said solution, and to the solution and the isolated dimeric gadolinium complex obtainable by such processes.
A solution is proposed relating to medical imaging applications. Particularly, a method (600) for imaging a body-part of a patient comprises simulating (624-630) corresponding operative simulation images from an operative baseline image and operative administration images, which operative administration images have been acquired with administration of a contrast agent at an operative administration-dose: the operative simulation images mimic administration of the contrast agent at a higher dose. For this purpose, a machine learning model (420) is used that has been trained to optimize a capability thereof to mimic a corresponding increase of the contrast agent from a sample source-dose to a sample target-dose: the sample source-dose is different from the operative administration-dose. Corresponding computer program (500) and computer program product for implementing the imaging method (600) are proposed. Moreover, a computing system (115) for performing the imaging method (600) and an imaging system (105) comprising the computing system (115) and a scanner (110) are proposed. A medical method based on the same imaging method (600) is further proposed.
G16H 30/40 - TIC spécialement adaptées au maniement ou au traitement d’images médicales pour le traitement d’images médicales, p. ex. l’édition
A61B 6/00 - Appareils ou dispositifs pour le diagnostic par radiationsAppareils ou dispositifs pour le diagnostic par radiations combinés avec un équipement de thérapie par radiations
G06T 5/50 - Amélioration ou restauration d'image utilisant plusieurs images, p. ex. moyenne ou soustraction
G06T 5/92 - Modification de la plage dynamique d'images ou de parties d'images basée sur les propriétés globales des images
16.
TRAINING A MACHINE LEARNING MODEL FOR SIMULATING IMAGES AT HIGHER DOSE OF CONTRAST AGENT IN MEDICAL IMAGING APPLICATIONS
A solution is proposed for training a machine learning model (420) for use in medical imaging applications. A corresponding method (700) comprises providing (703-743: 759-763) sample sets, each comprising a sample baseline image, a sample target image (acquired from a corresponding body-part of a subject to which a contrast agent at a certain dose has been administered) and a sample source dose (corresponding to a different dose of the contrast agent). The machine learning model (420) is trained (744-758) so as to optimize its capability of generating each sample target image from the corresponding sample baseline image and sample source image. One or more of the sample sets are incomplete, missing their sample source images. Each incomplete sample set is completed (704-742: 759-763) by simulating the sample source image from at least the sample baseline image and the sample target image of the sample set. A computer programs (500) and a computer program products for implementing the method (700) are proposed. Moreover, a computing system (130) for performing the method (700) is proposed.
The invention is related to a process for preparing a iodinating X-rays contrast agent. More specifically, it relates to a process for the preparation of N,N′-bis-(2,3-dihydroxypropyl)-5-hydroxy-2,4,6-triiodo-1,3-benzenedicarboxaniide (I) by electrochemical iodination of N,N′-(2,3-dihydroxypropyl)-5-hydroxy-1,3-benzenedicarboxamide (II) with molecular iodine (I2) which is in situ electrochemically generated from a source of iodide ions (I−). The iodide ions (I−) are obtained by the dissolution of hydrogen iodide (HI) or an alkali metal iodide in the reaction medium or produced during the reaction of N,N′-(2,3-dihydroxypropyl)-5-hydroxy-1,3-benzenedicarboxamide with I2. The invention also relates to the use of the intermediate compound of formula (I), obtained through the above electrochemical iodination of compound (II), in the preparation of N,N′-bis[2,3-dihydroxypropyl]-5(hydroxyacetyl)methylamino]-2,4,6-triiodo-1,3-benzenedicarboxamide (iomeprol).
C07C 231/12 - Préparation d'amides d'acides carboxyliques par des réactions n'impliquant pas la formation de groupes carboxamide
C07C 237/46 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle aromatique à six chaînons non condensé du squelette carboné ayant des atomes de carbone de groupes carboxamide, des groupes amino et au moins trois atomes de brome ou d'iode liés à des atomes de carbone du même cycle aromatique à six chaînons non condensé
C25B 3/07 - Composés contenant au moins un atome d’oxygène
C25B 3/09 - Composés contenant au moins un atome d’azote
C25B 3/11 - Composés contenant au moins un atome d’halogènes
C25B 15/08 - Alimentation ou vidange des réactifs ou des électrolytesRégénération des électrolytes
The invention relates to a process for the preparation of dimeric contrast agents for use in Magnetic resonance Imaging (MRI), in particular [μ-[1-[bis[2-(hydroxy-κO)-3-[4,7,10-tris[(carboxy-κO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-κN1,κN4,κN7,κN10]propyl]amino]-1-deoxy-D-glucitolate(6-)]]di-gadolinium complex, which includes preparation steps carried out one-pot (without isolation of the obtained intermediate) and precipitation of at least part of free gadolinium metal ions in excess.
The present invention is related to the synthesis of 4-hydroxymethyl-2-oxazolidinone (serinol carbamate, SC), which can be subsequently hydrolyzed to 2-amino-1,3-propanediol (serinol), by reacting glycerol and urea: (I) In general, glycerol is heated with urea and a catalyst, with or without a solvent, to give mainly 4-hydroxymethyl-2-oxazolidinone (serinol carbamate, SC), which is hydrolyzed in the next step to 2-amino-1,3-propanediol (serinol). Alternatively, glycerol 1,2-carbonate can be used instead of glycerol. Serinol obtained by the process of the invention may be used in the synthesis of Iopamidol.
The present invention is related to the synthesis of 4-hydroxymethyl-2-oxazolidinone (serinol carbamate, SC), which can be subsequently hydrolyzed to 2-amino-1,3-propanediol (serinol), by reacting glycerol and urea: (I) In general, glycerol is heated with urea and a catalyst, with or without a solvent, to give mainly 4-hydroxymethyl-2-oxazolidinone (serinol carbamate, SC), which is hydrolyzed in the next step to 2-amino-1,3-propanediol (serinol). Alternatively, glycerol 1,2-carbonate can be used instead of glycerol. Serinol obtained by the process of the invention may be used in the synthesis of Iopamidol.
C07C 213/02 - Préparation de composés contenant des groupes amino et hydroxy, amino et hydroxy éthérifiés ou amino et hydroxy estérifiés liés au même squelette carboné par des réactions impliquant la formation de groupes amino à partir de composés contenant des groupes hydroxy ou des groupes hydroxy éthérifiés ou estérifiés
C07C 231/02 - Préparation d'amides d'acides carboxyliques à partir d'acides carboxyliques ou à partir de leurs esters, anhydrides ou halogénures par réaction avec de l'ammoniac ou des amines
C07C 231/12 - Préparation d'amides d'acides carboxyliques par des réactions n'impliquant pas la formation de groupes carboxamide
C07D 263/24 - Atomes d'oxygène liés en position 2 avec des radicaux hydrocarbonés, substitués par des atomes d'oxygène, liés aux autres atomes de carbone du cycle
The present invention relates to a process for the preparation of Cyclen. in its turn widely employed in the manufacturing of a variety of macrocyclic gadolinium complexes for use as MRI contrast agents. The said process comprises an efficient coupling of glyoxal with triethylene tetramine and the subsequent reduction of the obtained intermediate derivative with an aluminium based reducing agent. The process is particularly advantageous for the industrial scale as it avoids the use and/or formation of hazardous compounds and further provides for Cyclen manufacturing in high yields and purity.
09 - Appareils et instruments scientifiques et électriques
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Image processing software for increasing the image enhancement in contrast-enhanced images during medical examinations. Software as a service (SAAS) services featuring image processing software for increasing the image enhancement in contrast-enhanced images during medical examinations.
22.
CATHETERIZATION WITH AUTOMATIC INSERTION AND ROTATION OF NEEDLE AND RELEASE OF FUNCTIONAL ELEMENT
FONDAZIONE ISTITUTO ITALIANO DI TECNOLOGIA (Italie)
Inventeur(s)
Acemoglu, Alperen
Koskinopoulou, Maria
De Mattos, Leonardo Serra
Abrégé
A solution is proposed for accessing a target region (103) within a body-part (106) of a patient. A corresponding catheterization device (400;500a;500b) has a support element (142) for a functional element (115;118) being a needle (118) or a catheter (115) mounted thereon. A curved guide (405) arranged on a slide (141) is used to guide the support element (142). An actuator (148) translates the slide (141) for causing the needle (118) to penetrate the body-part (106). A further actuator (410) rotates the support element (142) for reducing an angle between the needle (118) and the body-part (106) in response to a reaching of the target region (103). A still further actuator (154;254) releases the functional element (115;118) from the support element (142) in response to a completion of its rotation. A robotic system (600) comprising the catheterization device (400;500a;500b) is also proposed. Moreover, a corresponding method (900) for controlling the catheterization device (400;500a;500b) is proposed. A computer program and a corresponding computer program product for implementing the method (900) are further proposed. A method for inserting the catheter into the target region is also proposed.
The present invention relates to a method for precipitating the gadolinium complex of formula (I) from a solution comprising such gadolinium complex by means of mixing a first solution comprising the complex with a second solution, as well as to a method for isolating the precipitated gadolinium complex of formula (I) from a mixture comprising the precipitate; the gadolinium complex of formula (I) can be used as a contrast agent for magnetic resonance imaging (MRI).
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
C07D 403/12 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07F 5/00 - Composés contenant des éléments des groupes 3 ou 13 du tableau périodique
The present invention relates to the field of optical imaging. More particularly, it relates to compounds of the cyanine family with near-infrared emission characterized by improved physico-chemical and biological properties and to conjugates with biological ligands thereof. The invention also relates to the use of these compounds as optical diagnostic agents in imaging or therapy of solid tumors, to the methods for their preparation and to the compositions comprising them.
C07D 403/10 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne carbonée contenant des cycles aromatiques
C07D 403/14 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
C09B 23/01 - Colorants méthiniques ou polyméthiniques, p. ex. du type cyanine caractérisés par la chaîne méthinique
The present invention relates to the field of optical imaging. More particularly, it relates to fluorescent probes targeting carbonic anhydrase nine (CA-IX) comprising near-infrared (NIR) dyes of the cyanine. The invention also relates to the methods for preparing these compounds, to pharmaceutical compositions and kits incorporating them and to methods of use them as optical diagnostic agents in imaging or therapy of diseases such as solid tumors with hypoxic tissues involving cells expressing CA-IX. The compounds have formula (I).
C09B 23/01 - Colorants méthiniques ou polyméthiniques, p. ex. du type cyanine caractérisés par la chaîne méthinique
C09B 23/08 - Colorants méthiniques ou polyméthiniques, p. ex. du type cyanine caractérisés par la chaîne méthinique contenant un nombre impair de groupes CH plus de trois groupes CH, p. ex. polycarbocyanines
G01N 33/533 - Production de composés immunochimiques marqués avec un marqueur fluorescent
G01N 33/58 - 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
G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer
G01N 33/573 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour enzymes ou isoenzymes
The present invention relates to the field of optical imaging. More particularly, it relates to fluorescent probes targeting carbonic anhydrase nine (CA-IX) comprising near-infrared (NIR) dyes of the cyanine. The invention also relates to the methods for preparing these compounds, to pharmaceutical compositions and kits incorporating them and to methods of use them as optical diagnostic agents in imaging or therapy of diseases such as solid tumors with hypoxic tissues involving cells expressing CA-IX.
C09B 23/01 - Colorants méthiniques ou polyméthiniques, p. ex. du type cyanine caractérisés par la chaîne méthinique
C09B 23/08 - Colorants méthiniques ou polyméthiniques, p. ex. du type cyanine caractérisés par la chaîne méthinique contenant un nombre impair de groupes CH plus de trois groupes CH, p. ex. polycarbocyanines
G01N 33/533 - Production de composés immunochimiques marqués avec un marqueur fluorescent
G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer
G01N 33/58 - 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
G01N 33/573 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour enzymes ou isoenzymes
27.
1,4-BIS-(2-HYDROXY-BENZYL)-1,4,7-TRIAZACYCLONONANE DERIVATIVES AND SIMILAR COMPOUNDS AS LIGANDS IN IRON(III) COMPLEXES FOR USE AS MRI CONTRAST AGENTS
UNIVERSITÀ DEGLI STUDI DEL PIEMONTE ORIENTALE (Italie)
Inventeur(s)
Botta, Mauro
Tei, Lorenzo
Carniato, Fabio
Baranyai, Zsolt
Boccalon, Mariangela
Abrégé
The invention relates to the novel compounds of formula (I) as well as ions, stereoisomers, tautomers, hydrates, solvates, pharmaceutically acceptable salts thereof, or mixtures of the same. The compounds of formula (I) are ligands that are able to chelate Fe(III) ions, thereby generating Fe(III) complexes, which are particularly suitable in diagnostic imaging, for example as contrast agents for magnetic resonance imaging (MRI), due to their high relaxivity, thermodynamic stability, kinetic inertness and redox stability.
C07D 255/02 - Composés hétérocycliques contenant des cycles comportant trois atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par les groupes non condensés avec d'autres cycles
C07D 255/02 - Composés hétérocycliques contenant des cycles comportant trois atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par les groupes non condensés avec d'autres cycles
The invention relates to a process for preparing Gadoteridol of formula (I). In particular, the process comprises the use of propylene oxide in the alkylation step of the compound of formula (II), wherein propylene oxide is directly reacted with the compound of formula (II) without being isolated, and wherein propylene oxide is obtained on demand by decomposition of propylene carbonate in the presence of an alkaline or alkaline earth metal halide as catalyst.
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
09 - Appareils et instruments scientifiques et électriques
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Image processing software for increasing the image enhancement in contrast-enhanced images during medical examinations. Software as a service (SAAS) services featuring image processing software for increasing the image enhancement in contrast-enhanced images during medical examinations.
09 - Appareils et instruments scientifiques et électriques
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Image processing software for increasing the image enhancement in contrast-enhanced images during medical examinations. Software as a service (SAAS) services featuring image processing software for increasing the image enhancement in contrast-enhanced images during medical examinations.
09 - Appareils et instruments scientifiques et électriques
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Recorded image processing software for increasing the image enhancement in contrast-enhanced images during medical examinations; downloadable image processing software for increasing the image enhancement in contrast-enhanced images during medical examinations Software as a service (SAAS) services featuring image processing software for increasing the image enhancement in contrast-enhanced images during medical examinations
09 - Appareils et instruments scientifiques et électriques
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Recorded image processing software for increasing the image enhancement in contrast-enhanced images during medical examinations; downloadable image processing software for increasing the image enhancement in contrast-enhanced images during medical examinations Software as a service (SAAS) services featuring image processing software for increasing the image enhancement in contrast-enhanced images during medical examinations
35.
PROCESS FOR THE PREPARATION OF 2,4,6-TRIIODOPHENOL DERIVATIVES
C07C 231/12 - Préparation d'amides d'acides carboxyliques par des réactions n'impliquant pas la formation de groupes carboxamide
C07C 235/48 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des atomes d'oxygène ayant des atomes de carbone de groupes carboxamide liés à des atomes de carbone de cycles aromatiques à six chaînons et des atomes d'oxygène, liés par des liaisons simples, liés au même squelette carboné avec des atomes de carbone de groupes carboxamide et des atomes d'oxygène, liés par des liaisons simples, liés à des atomes de carbone du même cycle aromatique à six chaînons non condensé ayant l'atome d'azote d'au moins un des groupes carboxamide lié à un atome de carbone acyclique d'un radical hydrocarboné substitué par des atomes d'oxygène liés par des liaisons simples
The present invention relates to the field of optical imaging. More particularly, it relates to compounds of the cyanine family with near-infrared emission characterized by improved physico-chemical and biological properties and to conjugates with biological ligands thereof. The invention also relates to the use of these compounds as optical diagnostic agents in imaging or therapy of solid tumors, to the methods for their preparation and to the compositions comprising them. The compounds have formula (I), formula (I), wherein X is direct bond or —O—; Y is a group selected from linear or branched C1-C6 alkyl, C3-C7 cycloalkyl and heterocyclyl, substituted by at least two hydroxyl groups; R1 and R2 are each independently a linear or branched C1-C6 alkyl substituted by a group selected from —SO3H, —COOH, —CONH2 and —COO—C1-C6 alkyl; and R3 is hydrogen, —SO3H or a linear or branched C1-C6 alkyl substituted by —COOH or —CONH—Y, wherein Y is a group selected from linear or branched C1-C6 alkyl, C3-C7 cycloalkyl and heterocyclyl, substituted by at least two hydroxyl groups.
C07D 403/10 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne carbonée contenant des cycles aromatiques
C09B 23/01 - Colorants méthiniques ou polyméthiniques, p. ex. du type cyanine caractérisés par la chaîne méthinique
C07D 403/14 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
The invention relates to a process for the preparation of dimeric contrast agents for use in Magnetic resonance Imaging (MRI), in particular [μ-[1-[bis[2-(hydroxy-kO)-3-[4,7,10-tris[(carboxy-kO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-kN1,kN4,kN7,kN10]propyl]amino]-1-deoxy-D-glucitolato(6-)]]di-gadolinium complex, which includes preparation steps carried out one-pot and without isolation of the obtained intermediate.
The present invention provides new polypeptide derivatives binding to Human Epidermal Growth Factor Receptor 2 (HER2) and their conjugates thereof, and to their use as a diagnostic agent, particularly for early detection, patient stratification and treatment monitoring of forms of cancer characterized by over-expression of HER2.
C07K 14/71 - RécepteursAntigènes de surface cellulaireDéterminants de surface cellulaire pour des facteurs de croissanceRécepteursAntigènes de surface cellulaireDéterminants de surface cellulaire pour des régulateurs de croissance
The present invention relates to a novel process for the preparation of 2,4,6-triiodoisophthalic bisamide derivatives, which are useful intermediates in the preparation of non-ionic X-ray contrast agents, starting from the corresponding acyl chloride intermediates which are amidated in a mixture of specific hydrotropic solvents in the presence of a low amount of water. In addition, the invention relates to the use of such hydrotropic solvents in the preparation of said 2,4,6-triiodoisophthalic bisamide intermediates to produce non-ionic X-ray contrast agents.
C07C 237/32 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle aromatique à six chaînons non condensé du squelette carboné ayant l'atome d'azote du groupe carboxamide lié à un atome de carbone acyclique d'un radical hydrocarboné substitué par des atomes d'oxygène
C07C 231/02 - Préparation d'amides d'acides carboxyliques à partir d'acides carboxyliques ou à partir de leurs esters, anhydrides ou halogénures par réaction avec de l'ammoniac ou des amines
The invention relates to a process for the preparation of the gadolinium dimeric contrast agent [p-[l-[bis[2-(hydroxy-KO)-3-[4,7,10-tris[(carboxy-KO)methyl]-l,4,7,10- tetraazacyclododec-l-yl-K/V1,K/V4,K/V7,K/V10]propyl]amino]-l-deoxy-D-glucitolato(6-)]]di- gadolinium complex. Such process includes preparation steps carried out one-pot and without isolation of the obtained intermediates. The gadolinium dimeric contrast agent can be for use in diagnostic imaging, in particular in Magnetic resonance Imaging (MRI).
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
43.
PROCESS FOR MANUFACTURING A MIXTURE COMPRISING A DIMERIC MACROCYCLE INTERMEDIATE OF A GADOLINIUM COMPLEX
The present invention relates to a process for the manufacturing of a mixture comprising the intermediate 1-[bis[2-hydroxy-3-[4,7,10-tris[2-(1,1-dimethylethoxy)-2-oxoethyl]-1,4,7,10-tetraazacyclododec-1-yl]propyl]amino]-1-deoxy-D-glucitol. Such intermediate is useful for the synthesis of the dimeric gadolinium complex [μ-[1-[bis[2-(hydroxy-κO)-3-[4,7,10-tris[(carboxy-κO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-κN1,κN4,κN7,κN10]propyl]amino]-1-deoxy-D-glucitolate(6-)]]digadolinium complex, which can be employed as a contrast agent in the field of diagnostic imaging, and in particular of Magnetic Resonance Imaging (MRI).
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
A solution is proposed for training a machine learning model (420) for use in medical imaging applications. A corresponding method (700) comprises providing (703-743; 759-763) sample sets, each comprising a sample baseline image, a sample target image (acquired from a corresponding body -part of a subject to which a contrast agent at a certain dose has been administered) and a sample source dose (corresponding to a different dose of the contrast agent). The machine learning model (420) is trained (744-758) so as to optimize its capability of generating each sample target image from the corresponding sample baseline image and sample source image. One or more of the sample sets are incomplete, missing their sample source images. Each incomplete sample set is completed (704-742; 759-763) by simulating the sample source image from at least the sample baseline image and the sample target image of the sample set. A computer programs (500) and a computer program products for implementing the method (700) are proposed. Moreover, a computing system (130) for performing the method (700) is proposed.
A solution is proposed relating to medical imaging applications. Particularly, a method (600) for imaging a body-part of a patient comprises simulating (624-630) corresponding operative simulation images from an operative baseline image and operative administration images, which operative administration images have been acquired with administration of a contrast agent at an operative administration-dose; the operative simulation images mimic administration of the contrast agent at a higher dose. For this purpose, a machine learning model (420) is used that has been trained to optimize a capability thereof to mimic a corresponding increase of the contrast agent from a sample source-dose to a sample target-dose; the sample source-dose is different from the operative administration-dose. Corresponding computer program (500) and computer program product for implementing the imaging method (600) are proposed. Moreover, a computing system (115) for performing the imaging method (600) and an imaging system (105) comprising the computing system (115) and a scanner (110) are proposed. A medical method based on the same imaging method (600) is further proposed.
A61B 6/00 - Appareils ou dispositifs pour le diagnostic par radiationsAppareils ou dispositifs pour le diagnostic par radiations combinés avec un équipement de thérapie par radiations
G01R 33/56 - Amélioration ou correction de l'image, p. ex. par des techniques de soustraction ou d'établissement de moyenne
G05B 13/02 - Systèmes de commande adaptatifs, c.-à-d. systèmes se réglant eux-mêmes automatiquement pour obtenir un rendement optimal suivant un critère prédéterminé électriques
G16H 50/00 - TIC spécialement adaptées au diagnostic médical, à la simulation médicale ou à l’extraction de données médicalesTIC spécialement adaptées à la détection, au suivi ou à la modélisation d’épidémies ou de pandémies
A61K 49/04 - Préparations de contraste pour rayons X
A61K 49/06 - Préparations de contraste pour la résonance magnétique nucléaire [RMN]Préparations de contraste pour l'imagerie par résonance magnétique [IRM]
A61K 49/22 - Préparations pour échographiePréparations pour imagerie par ultrasons
47.
ELECTROCHEMICAL IODINATION OF N,N'-(2,3-DIHYDROXYPROPYL)-5-HYDROXY-1,3-BENZENEDICARBOXAMIDE
The invention is related to a process for preparing a iodinating X-rays contrast agent. More specifically, it relates to a process for the preparation of N,N'-bis-(2,3-dihydroxypropyl)-5-hydroxy-2,4,6-triiodo-1,3-benzenedicarboxamide (I) by electrochemical iodination of N,N'-(2,3-dihydroxypropyl)-5-hydroxy-1,3-benzenedicarboxamide (II) with molecular iodine (I2) which is in situ electrochemically generated from a source of iodide ions (I-). The iodide ions (I-) are obtained by the dissolution of hydrogen iodide (HI) or an alkali metal iodide in the reaction medium or produced during the reaction of N,N'-(2,3-dihydroxypropyl)-5-hydroxy-1,3-benzenedicarboxamide with I2. The invention also relates to the use of the intermediate compound of formula (I), obtained through the above electrochemical iodination of compound (II), in the preparation of N,N'-bis[2,3-dihydroxypropyl]-5(hydroxyacetyl)methylamino]-2,4,6-triiodo-1,3-benzenedicarboxamide (iomeprol).
C07C 231/12 - Préparation d'amides d'acides carboxyliques par des réactions n'impliquant pas la formation de groupes carboxamide
C07C 235/46 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des atomes d'oxygène ayant des atomes de carbone de groupes carboxamide liés à des atomes de carbone de cycles aromatiques à six chaînons et des atomes d'oxygène, liés par des liaisons simples, liés au même squelette carboné avec des atomes de carbone de groupes carboxamide et des atomes d'oxygène, liés par des liaisons simples, liés à des atomes de carbone du même cycle aromatique à six chaînons non condensé ayant les atomes d'azote des groupes carboxamide liés à des atomes d'hydrogène ou à des atomes de carbone acycliques
C07C 235/48 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des atomes d'oxygène ayant des atomes de carbone de groupes carboxamide liés à des atomes de carbone de cycles aromatiques à six chaînons et des atomes d'oxygène, liés par des liaisons simples, liés au même squelette carboné avec des atomes de carbone de groupes carboxamide et des atomes d'oxygène, liés par des liaisons simples, liés à des atomes de carbone du même cycle aromatique à six chaînons non condensé ayant l'atome d'azote d'au moins un des groupes carboxamide lié à un atome de carbone acyclique d'un radical hydrocarboné substitué par des atomes d'oxygène liés par des liaisons simples
C07C 237/46 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle aromatique à six chaînons non condensé du squelette carboné ayant des atomes de carbone de groupes carboxamide, des groupes amino et au moins trois atomes de brome ou d'iode liés à des atomes de carbone du même cycle aromatique à six chaînons non condensé
C25B 3/07 - Composés contenant au moins un atome d’oxygène
C25B 3/09 - Composés contenant au moins un atome d’azote
C25B 3/11 - Composés contenant au moins un atome d’halogènes
The present invention relates to an iron complex having the general formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to a pharmaceutical composition formulated for oral and/or parenteral administration, preferably intravenous, said pharmaceutical composition preferably being formulated as an aqueous solution comprising said complex or salt. The present invention further relates to said complex or a salt thereof or said pharmaceutical composition for use as a contrast agent for magnetic resonance imaging (MRI), as well as a method and a kit for in situ preparation of said complex or salt and said pharmaceutical composition.
The present invention relates to the calcium complex of (4RS)(4-carboxy-5,8,11-tris(carboxymethyl)-1-phenyl oxa-5,8,11-triazatridecan-13-oato(5-))pentahydrogen (BOPTA) in the form of a salt, to the process for its preparation and to a formulation comprising said salt.
C07C 229/22 - Composés contenant des groupes amino et carboxyle liés au même squelette carboné ayant des groupes amino et carboxyle liés à des atomes de carbone acycliques du même squelette carboné le squelette carboné étant acyclique et saturé le squelette carboné étant substitué de plus par des atomes d'oxygène
C07C 227/18 - Préparation de composés contenant des groupes amino et carboxyle liés au même squelette carboné à partir de composés contenant déjà des groupes amino et carboxyle ou leurs dérivés par des réactions impliquant des groupes amino ou carboxyle, p. ex. hydrolyse d'esters ou d'amides, par formation d'halogénures, de sels ou d'esters
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
51.
ANTI-HER2 POLYPEPTIDES DERIVATIVES AS NEW DIAGNOSTIC MOLECULAR PROBES
The present invention provides new polypeptide derivatives binding to Human Epidermal Growth Factor Receptor 2 (HER2) and their conjugates thereof, and to their use as a diagnostic agent, particularly for early detection, patient stratification and treatment monitoring of forms of cancer characterized by over-expression of HER2.
The invention relates to a process for the preparation of dimeric contrast agents foruse in Magnetic resonance Imaging (MRI), in particular [?-[1-[bis[2-(hydroxy-?O)-3-[4,7,10-tris[(carboxy-?O)methyl]-1,4,7,10-tetraazacyclododec-1-yl-?N1,?N4,?N7,?N10]propyl]amino]-1-deoxy-D-glucitolate(6-)]]di-gadolinium complex, whichincludes preparation steps carried out one-pot (without isolation of the obtainedintermediate) and precipitation of at least part of free gadolinium metal ions in excess.
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
C07F 5/00 - Composés contenant des éléments des groupes 3 ou 13 du tableau périodique
53.
PROCESS FOR THE MANUFACTURING OF A GADOLINIUM COMPLEX SOLUTION
The invention relates to a process for the manufacturing of a solution of a dimeric gadolinium complex, such as [?-[1-[bis[2-(hydroxy-?O)-3-[4,7,10-tris[(carboxy-?O)methyl]-1,4,7,10-tetraazacyclododec-1-yl-?N1,?N4,?N7,?N10]propyl]amino]-1-deoxy-D-glucitolate(6-)]]digadolinium complex, which is useful in the field of diagnostic imaging and of contrast agents in Magnetic Resonance Imaging (MRI), comprising the steps of precipitating a portion of free gadolinium metal ions by means of a precipitating agent. The invention further relates to a process for isolating the dimeric gadolinium complex from said solution, and to the solution and the isolated dimeric gadolinium complex obtainable by such processes.
C07D 403/12 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07F 3/00 - Composés contenant des éléments des groupes 2 ou 12 du tableau périodique
54.
PROCESS FOR THE MANUFACTURING OF A GADOLINIUM COMPLEX SOLUTION
The invention relates to a process for the manufacturing of a solution of a dimeric gadolinium complex, such as [μ-[1-[bis[2-(hydroxy-κO)-3-[4,7,10-tris[(carboxy-κO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-κN1,κN4,κN7,κN10]propyl]amino]-1-deoxy-D-glucitolate(6-)]]digadolinium complex, which is useful in the field of diagnostic imaging and of contrast agents in Magnetic Resonance Imaging (MRI), comprising the steps of precipitating a portion of free gadolinium metal ions by means of a precipitating agent. The invention further relates to a process for isolating the dimeric gadolinium complex from said solution, and to the solution and the isolated dimeric gadolinium complex obtainable by such processes.
C07F 3/00 - Composés contenant des éléments des groupes 2 ou 12 du tableau périodique
C07D 403/12 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
The invention relates to a process for the preparation of dimeric contrast agents foruse in Magnetic resonance Imaging (MRI), in particular [μ-[1-[bis[2-(hydroxy-κO)-3-[4,7,10-tris[(carboxy-κO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-κN1,κN4,κN7,κN10]propyl]amino]-1-deoxy-D-glucitolate(6-)]]di-gadolinium complex, whichincludes preparation steps carried out one-pot (without isolation of the obtainedintermediate) and precipitation of at least part of free gadolinium metal ions in excess.
C07F 5/00 - Composés contenant des éléments des groupes 3 ou 13 du tableau périodique
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
56.
PHARMACEUTICAL COMPOSITIONS OF GD-BASED CONTRAST AGENTS
The present invention relates to pharmaceutical compositions comprising an gadolinium-complex and a saturated macrocyclic tetraamine that find application in diagnostic imaging as diagnostic agents, in particular as contrast agents having improved tolerability, specifically in Magnetic Resonance Imaging (MRI), and to their preparation.
The present invention provides nucleic acid aptamers binding to the Carbonic Anhydrase IX (CA-IX) enzyme, derivatives and conjugates thereof and their use as diagnostic tools, particularly for the imaging of organs and tissues expressing CA-IX, or as therapeutic agents for prevention or treatment of CA-IX related diseases.
C12N 15/115 - Aptamères, c.-à-d. acides nucléiques liant spécifiquement une molécule cible avec une haute affinité sans s'y hybrider
C12Q 1/6886 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p. ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique pour le cancer
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
The present invention relates to a process for the preparation of Cyclen, in its turn widely employed in the manufacturing of a variety of macrocyclic gadolinium complexes for use as MRI contrast agents. The said process comprises an efficient coupling of glyoxal with triethylene tetramine and the subsequent reduction of the obtained intermediate derivative with an aluminium based reducing agent. The process is particularly advantageous for the industrial scale as it avoids the use and/or formation of hazardous compounds and further provides for Cyclen manufacturing in high yields and purity.
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
The present invention is related to the synthesis of 4-hydroxymethyl-2-oxazolidinone (serinol carbamate, SC), which can be subsequently hydrolyzed to 2-amino-1,3-propanediol (serinol), by reacting glycerol and urea: (I) In general, glycerol is heated with urea and a catalyst, with or without a solvent, to give mainly 4-hydroxymethyl-2-oxazolidinone (serinol carbamate, SC), which is hydrolyzed in the next step to 2-amino-1,3-propanediol (serinol). Alternatively, glycerol 1,2-carbonate can be used instead of glycerol. Serinol obtained by the process of the invention may be used in the synthesis of Iopamidol.
C07C 213/02 - Préparation de composés contenant des groupes amino et hydroxy, amino et hydroxy éthérifiés ou amino et hydroxy estérifiés liés au même squelette carboné par des réactions impliquant la formation de groupes amino à partir de composés contenant des groupes hydroxy ou des groupes hydroxy éthérifiés ou estérifiés
C07C 231/02 - Préparation d'amides d'acides carboxyliques à partir d'acides carboxyliques ou à partir de leurs esters, anhydrides ou halogénures par réaction avec de l'ammoniac ou des amines
C07C 231/12 - Préparation d'amides d'acides carboxyliques par des réactions n'impliquant pas la formation de groupes carboxamide
C07D 263/24 - Atomes d'oxygène liés en position 2 avec des radicaux hydrocarbonés, substitués par des atomes d'oxygène, liés aux autres atomes de carbone du cycle
C07C 215/10 - Composés contenant des groupes amino et hydroxy liés au même squelette carboné ayant des groupes hydroxy et des groupes amino liés à des atomes de carbone acycliques du même squelette carboné le squelette carboné étant saturé et acyclique avec un groupe amino et au moins deux groupes hydroxy liés au squelette carboné
C07C 237/30 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle aromatique à six chaînons non condensé du squelette carboné ayant l'atome d'azote du groupe carboxamide lié à des atomes d'hydrogène ou à des atomes de carbone acycliques
C07C 237/46 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle aromatique à six chaînons non condensé du squelette carboné ayant des atomes de carbone de groupes carboxamide, des groupes amino et au moins trois atomes de brome ou d'iode liés à des atomes de carbone du même cycle aromatique à six chaînons non condensé
The present invention relates to the field of optical imaging More particularly, it relates to compounds of the cyanine family characterized by improved physico-chemical and biological properties and to their conjugates with biological ligands thereof. The invention also relates to the use of these compounds as optical diagnostic agents in imaging or therapy of solid tumors, to the methods for their preparation and to the compositions comprising them.
C07D 403/14 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
C07D 403/06 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne carbonée ne contenant que des atomes de carbone aliphatiques
C09B 23/06 - Colorants méthiniques ou polyméthiniques, p. ex. du type cyanine caractérisés par la chaîne méthinique contenant un nombre impair de groupes CH trois groupes CH, p. ex. carbocyanines
C09B 23/08 - Colorants méthiniques ou polyméthiniques, p. ex. du type cyanine caractérisés par la chaîne méthinique contenant un nombre impair de groupes CH plus de trois groupes CH, p. ex. polycarbocyanines
The present invention relates to the field of optical imaging. More particularly, it relates to a class of monoalkylated cyanine dyes with red to near-infrared (650-900 nm) emission characterized by pH responsiveness and to conjugates with biological ligands thereof. The invention also relates to the use of these compounds as optical diagnostic agents in imaging or therapy of solid tumors, to the methods for their preparation and to the compositions comprising them. The monoalkylated cyanine dyes have general formula (I) wherein R1 and R3 are independently selected from the group consisting of hydrogen, -SO3H, - COOH and -CONH-Y; and R2 and R4 are hydrogen, or both R1 together with R2 and R3 together with R4, respectively and with the atoms to which they are bonded, form two aryl rings, optionally substituted with from 1 to 4 -SO3H groups; R5 is an alkyl optionally substituted by a group selected from -SO3H, - COOH and -CONH2.
C09B 23/08 - Colorants méthiniques ou polyméthiniques, p. ex. du type cyanine caractérisés par la chaîne méthinique contenant un nombre impair de groupes CH plus de trois groupes CH, p. ex. polycarbocyanines
C09B 23/01 - Colorants méthiniques ou polyméthiniques, p. ex. du type cyanine caractérisés par la chaîne méthinique
G01N 33/52 - Utilisation de composés ou de compositions pour des recherches colorimétriques, spectrophotométriques ou fluorométriques, p. ex. utilisation de bandes de papier indicateur
G01N 33/84 - 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 composés inorganiques ou le pH
The invention relates to a process for preparing Gadoteridol of formula (I).In particular, the process comprises the use of propylene oxide in the alkylation step of the compound of formula (II), wherein propylene oxide is directly reacted with the compound of formula (II) without being isolated, and wherein propylene oxide is obtained on demand by decomposition of propylene carbonate in the presence of an alkaline or alkaline earth metal halide as catalyst.
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
The present invention refers to pharmaceutical compositions comprising a macrocyclic gadolinium complex and a water-soluble polyarylene additive useful in diagnostic imaging as diagnostic agents, in particular as contrast agents, specifically in Magnetic Resonance Imaging (MRI).
A61K 47/20 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant du soufre, p. ex. sulfoxyde de diméthyle [DMSO], docusate, laurylsulfate de sodium ou acides aminosulfoniques
66.
METHOD FOR LABELING OF SENSITIVE AND THERMOSENSITIVE TARGETING BIOMOLECULES WITH TECHNETIUM BASED COMPOUNDS
The present invention relates to a labeling procedure for the incorporation, in mild reaction conditions, of sensitive and thermosensitive targeting molecules into a [99mTc(N)(PNP)]-based compound suitable for a kit formulation.
The invention relates to a process for the preparation of dimeric contrast agents for use in Magnetic resonance Imaging (MRI), in particular [?-[1-[bis[2-(hydroxy-kO)-3- [4,7,10-tris[(carboxy-kO)methyl]-1,4,7,10-tetraazacyclododec-1-yl- kN1,kN4,kN7,kN10]propyl]amino]-1-deoxy-D-glucitolato(6-)]]di-gadolinium complex, which includes preparation steps carried out one-pot and without isolation of the obtained intermediate.
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
The invention relates to a process for the preparation of dimeric contrast agents for use in Magnetic resonance Imaging (MRI), in particular [μ-[1-[bis[2-(hydroxy-kO)-3- [4,7,10-tris[(carboxy-kO)methyl]-1,4,7,10-tetraazacyclododec-1-yl- kN1,kN4,kN7,kN10]propyl]amino]-1-deoxy-D-glucitolato(6-)]]di-gadolinium complex, which includes preparation steps carried out one-pot and without isolation of the obtained intermediate.
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
A chelating compound of formula (I) or a pharmaceutically acceptable salt thereof and its complexes with metals or radioisotopes thereof. The invention further relates to the preparation of such ligand and complexes as well as to their use as diagnostic or therapeutic agents.
The present invention relates to the field of optical imaging. More particularly, it relates to compounds of the cyanine family with near- infrared emission characterized by improved physico-chemical and biological properties and to conjugates with biological ligands thereof. The invention also relates to the use of these compounds as optical diagnostic agents in imaging or therapy of solid tumors, to the methods for their preparation and to the compositions comprising them. The compounds have formula (I), formula (I), wherein X is direct bond or -O-; Y is a group selected from linear or branched C1-C6 alkyl, C3-C7 cycloalkyl and heterocyclyl, substituted by at least two hydroxyl groups; R1 and R2 are each independently a linear or branched C1-C6 alkyl substituted by a group selected from -SO3H, -COOH, -CONH2 and - COO-C1-C6 alkyl; and R3 is hydrogen, -SO3H or a linear or branched C1-C6 alkyl substituted by -COOH or -CONH-Y, wherein Y is a group selected from linear or branched C1-C6 alkyl, C3-C7 cycloalkyl and heterocyclyl, substituted by at least two hydroxyl groups.
The present invention relates to the field of optical imaging. More particularly, it relates to compounds of the cyanine family with near- infrared emission characterized by improved physico-chemical and biological properties and to conjugates with biological ligands thereof. The invention also relates to the use of these compounds as optical diagnostic agents in imaging or therapy of solid tumors, to the methods for their preparation and to the compositions comprising them. The compounds have formula (I), formula (I), wherein X is direct bond or -O-; Y is a group selected from linear or branched C1-C6 alkyl, C3-C7 cycloalkyl and heterocyclyl, substituted by at least two hydroxyl groups; R1 and R2 are each independently a linear or branched C1-C6 alkyl substituted by a group selected from -SO3H, -COOH, -CONH2 and - COO-C1-C6 alkyl; and R3 is hydrogen, -SO3H or a linear or branched C1-C6 alkyl substituted by -COOH or -CONH-Y, wherein Y is a group selected from linear or branched C1-C6 alkyl, C3-C7 cycloalkyl and heterocyclyl, substituted by at least two hydroxyl groups.
G01N 33/533 - Production de composés immunochimiques marqués avec un marqueur fluorescent
G01N 33/58 - 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
78.
Gene signatures for the prediction of prostate cancer recurrence
Disclosed are gene signatures and methods for predicting the recurrence of prostate cancer in prostatectomized subjects. Other objectives of the invention are assay devices and kits for determining the expression levels of specific gene sets correlated to prostate cancer recurrence.
C12Q 1/6886 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p. ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique pour le cancer
79.
ICAM-1 aptamers, diagnostic and therapeutic uses thereof
The present invention provides nucleic acid aptamers binding to the Intercellular Adhesion Molecule-1 (ICAM-1), derivatives and conjugates thereof and their use as diagnostic tools, particularly for the imaging of organs and tissues expressing ICAM-1, or as therapeutic agents for prevention or treatment of ICAM-1-related diseases.
C12N 15/115 - Aptamères, c.-à-d. acides nucléiques liant spécifiquement une molécule cible avec une haute affinité sans s'y hybrider
C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques
The present invention relates to on the use of exogenous agents having a pool of mobile proton(s) in CEST-MR imaging to generate Chemical Exchange Rotation Transfer-based CEST contrast, and to a ratiometric-based CEST-MR procedure that comprises using these exogenous agents to set-up CERT-based concentration-independent CEST MR imaging, and as responsive agents to set-up CERT-based concentration independent responsiveness.
G01R 33/56 - Amélioration ou correction de l'image, p. ex. par des techniques de soustraction ou d'établissement de moyenne
A61B 5/055 - Détection, mesure ou enregistrement pour établir un diagnostic au moyen de courants électriques ou de champs magnétiquesMesure utilisant des micro-ondes ou des ondes radio faisant intervenir la résonance magnétique nucléaire [RMN] ou électronique [RME], p. ex. formation d'images par résonance magnétique
The present invention relates to an iron complex having the general formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to a pharmaceutical composition formulated for oral and/or parenteral administration, preferably intravenous, said pharmaceutical composition preferably being formulated as an aqueous solution comprising said complex or salt. The present invention further relates to said complex or a salt thereof or said pharmaceutical composition for use as a contrast agent for magnetic resonance imaging (MRI), as well as a method and a kit for in situ preparation of said complex or salt and said pharmaceutical composition.
The present invention relates to the RRR/SSS pair of enantiomers of the of Gd(PCTA-tris-glutaric acid), the single enantiomers of the pair, the pharmaceutically acceptable salts thereof, their amide derivatives, and compositions comprising at least 50% of these compounds.
A61B 5/055 - Détection, mesure ou enregistrement pour établir un diagnostic au moyen de courants électriques ou de champs magnétiquesMesure utilisant des micro-ondes ou des ondes radio faisant intervenir la résonance magnétique nucléaire [RMN] ou électronique [RME], p. ex. formation d'images par résonance magnétique
The present invention provides new polypeptide derivatives binding to Human Epidermal Growth Factor Receptor 2 (HER2) and their conjugates thereof, and to their use as a diagnostic agent, particularly for early detection, patient stratification and treatment monitoring of forms of cancer characterized by over-expression of HER2.
The present invention relates to the calcium complex of (4RS)(4-carboxy-5,8,11- tris(carboxymethyl)-1-phenyl-2-oxa-5,8,11-triazatridecan-13-oato(5-))pentahydrogen (BOPTA) in the form of a salt, to the process for its preparation and to a formulation comprising said salt.
C07C 227/18 - Préparation de composés contenant des groupes amino et carboxyle liés au même squelette carboné à partir de composés contenant déjà des groupes amino et carboxyle ou leurs dérivés par des réactions impliquant des groupes amino ou carboxyle, p. ex. hydrolyse d'esters ou d'amides, par formation d'halogénures, de sels ou d'esters
C07C 229/36 - Composés contenant des groupes amino et carboxyle liés au même squelette carboné ayant des groupes amino et carboxyle liés à des atomes de carbone acycliques du même squelette carboné le squelette carboné contenant des cycles aromatiques à six chaînons avec au moins un groupe amino et un groupe carboxyle liés au même atome de carbone du squelette carboné
85.
ANTI-HER2 POLYPEPTIDES DERIVATIVES AS NEW DIAGNOSTIC MOLECULAR PROBES
The present invention provides new polypeptide derivatives binding to Human Epidermal Growth Factor Receptor 2 (HER2) and their conjugates thereof, and to their use as a diagnostic agent, particularly for early detection, patient stratification and treatment monitoring of forms of cancer characterized by over-expression of HER2.
The present invention provides new polypeptide derivatives binding to Human Epidermal Growth Factor Receptor 2 (HER2) and their conjugates thereof, and to their use as a diagnostic agent, particularly for early detection, patient stratification and treatment monitoring of forms of cancer characterized by over-expression of HER2.
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
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
89.
PHARMACEUTICAL COMPOSITIONS OF GD-BASED CONTRAST AGENTS
The present invention relates to pharmaceutical compositions comprising an gadolinium-complex and a saturated macrocyclic tetraamine that find application in diagnostic imaging as diagnostic agents, in particular as contrast agents having improved tolerability, specifically in Magnetic Resonance Imaging (MRI), and to their preparation.
The present invention provides nucleic acid aptamers binding to the Carbonic Anhydrase IX (CA-IX) enzyme, derivatives and conjugates thereof and their use as diagnostic tools, particularly for the imaging of organs and tissues expressing CA-IX, or as therapeutic agents for preventionor treatment of CA-IX related diseases.
C12N 15/115 - Aptamères, c.-à-d. acides nucléiques liant spécifiquement une molécule cible avec une haute affinité sans s'y hybrider
C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques
The present invention relates to new class of dimeric macrocycles capable of chelating paramagnetic metal ions, their chelated complexes with metal ions and the use thereof as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.
A61B 5/055 - Détection, mesure ou enregistrement pour établir un diagnostic au moyen de courants électriques ou de champs magnétiquesMesure utilisant des micro-ondes ou des ondes radio faisant intervenir la résonance magnétique nucléaire [RMN] ou électronique [RME], p. ex. formation d'images par résonance magnétique
C07D 403/12 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
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
The present invention relates to the RRR/SSS pair of enantiomers of the of Gd(PCTA-tris-glutaric acid), the single enantiomers of the pair, the pharmaceutically acceptable salts thereof, their amide derivatives, and compositions comprising at least 50% of these compounds.
A61B 5/055 - Détection, mesure ou enregistrement pour établir un diagnostic au moyen de courants électriques ou de champs magnétiquesMesure utilisant des micro-ondes ou des ondes radio faisant intervenir la résonance magnétique nucléaire [RMN] ou électronique [RME], p. ex. formation d'images par résonance magnétique
The present invention relates to the field of optical imaging. More particularly, it relates to compounds of the cyanine family characterized by improved physico-chemical and biological properties and to their conjugates with biological ligands thereof. The invention also relates to the use of these compounds as optical diagnostic agents in imaging or therapy of solid tumors, to the methods for their preparation and to the compositions comprising them.
C07D 209/14 - Radicaux substitués par des atomes d'azote ne faisant pas partie d'un radical nitro
C07K 7/52 - Peptides cycliques contenant au moins une liaison peptidique anormale ne comportant que des liaisons peptidiques normales dans le cycle
C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
The present invention relates to the field of optical imaging. More particularly, it relates to compounds of the cyanine family characterized by improved physico-chemical and biological properties and to their conjugates with biological ligands thereof. The invention also relates to the use of these compounds as optical diagnostic agents in imaging or therapy of solid tumors, to the methods for their preparation and to the compositions comprising them.
A61K 39/00 - Préparations médicinales contenant des antigènes ou des anticorps
C07K 7/52 - Peptides cycliques contenant au moins une liaison peptidique anormale ne comportant que des liaisons peptidiques normales dans le cycle
C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
C07D 209/14 - Radicaux substitués par des atomes d'azote ne faisant pas partie d'un radical nitro
C07D 403/12 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07D 417/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
The present invention relates to new class of dimeric macrocycles capable of chelating paramagnetic metal ions, their chelated complexes with metal ions and the use thereof as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.
A61B 5/055 - Détection, mesure ou enregistrement pour établir un diagnostic au moyen de courants électriques ou de champs magnétiquesMesure utilisant des micro-ondes ou des ondes radio faisant intervenir la résonance magnétique nucléaire [RMN] ou électronique [RME], p. ex. formation d'images par résonance magnétique
C07D 403/12 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
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
The present invention relates to new class of functionalized macrocycles capable of chelating paramagnetic metal ions, their chelated complexes with metal ions and the use thereof as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.
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
C07D 401/06 - 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 deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
The present invention discloses a solid-phase process for the preparation of a Near Infra-Red (NIR) fluorescent probe characterized by an aza-bicycloalkane based cyclic peptide labelled with a Cy5.5 dye moiety and used in the guided surgery of tumors and pathologic regions.
The present invention refers to pharmaceutical compositions comprising a macrocyclic gadolinium complex and a water-soluble polyarylene additive useful in diagnostic imaging as diagnostic agents, in particular as contrast agents, specifically in Magnetic Resonance Imaging (MRI).
A chelating compound of formula (I) or a pharmaceutically acceptable salt thereof and its complexes with metals or radioisotopes thereof. The invention further relates to the preparation of such ligand and complexes as well as to their use as diagnostic or therapeutic agents.
C07D 417/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
