公开(公告)号：US07186400B2

公开(公告)日：2007-03-06

申请号：US10484111

申请日：2002-07-10

Applicant: Giovanni Battista Giovenzana ,  Giovanni Palmisano ,  Massimo Sisti ,  Camilla Cavallotti ,  Silvio Aime ,  Luisella Calabi

Inventor： Giovanni Battista Giovenzana ,  Giovanni Palmisano ,  Massimo Sisti ,  Camilla Cavallotti ,  Silvio Aime ,  Luisella Calabi

IPC: A61B5/055

CPC classification number: C07D243/08 ,  A61K49/0002 ,  A61K49/101

Abstract: Compounds of general formula (I): in which: R1 is hydrogen, C1–C20 alkyl, C3–C10 cycloalkyl, C4–C20 cycloalkylalkyl, aryl, arylalkyl, or two R1, taken together, form a straight or cyclic C2–C10 alkylene group or an ortho disubstituted arylene; R2 is hydrogen, C1–C20 alkyl, C3–C10 cycloalkyl, C4–C20 cycloalkylalkyl, aryl or aryl alkyl optionally substituted with functional groups which allow conjugation with a suitable molecule able to interact with physiological systems; R3, R4 and R5 are hydrogen, C1–C20 alkyl, C3–C10 cycloalkyl, C4–C20 cycloalkylalkyl, aryl, arylalkyl; and their chelates with bi-trivalent ions of the metal elements having atomic number ranging between 20 and 31, 39, 42, 43, 44, 49, and between 57 and 83, and radioisotopes chosen among 203Pb 67Ga 68Ga 72As 111In 113In 90Y 97Ru 62Cu 64Cu 52Fe 52mMn 140La 175Yb 153Sm 166Ho 149Pm 177Lu 142Pr 159Gd 212Bi 47Sc 149Pm 67Cu, 111Ag, 199Au, 161Tb and 51Cr as well as the salts thereof with physiologically compatible bases or acids

公开(公告)号：US20080003632A1

公开(公告)日：2008-01-03

申请号：US10591965

申请日：2005-03-22

Applicant: Luisella Calabi ,  Lino Paleari ,  Luca Biondi ,  Mario Demiranda ,  Goffredo Alfieri ,  Stefano Ghelli

Inventor： Luisella Calabi ,  Lino Paleari ,  Luca Biondi ,  Mario Demiranda ,  Goffredo Alfieri ,  Stefano Ghelli

IPC: G01N33/483

CPC classification number: G01N24/08

Abstract: The present invention relates to a method for the in vitro quantitative determination of cellular uptake of exogenous or endogenous substances which method comprises applying MAS-NMR spectroscopy technique to an in vitro cellular sample, in combination with a shift agent. The said method is particularly advantageous as it find general applicability for a variety of substances and cell samples.

Abstract translation: 本发明涉及体外定量测定外源或内源物质的细胞摄取的方法，该方法包括将MAS-NMR光谱技术与转移剂组合应用于体外细胞样品。 所述方法是特别有利的，因为它找到了各种物质和细胞样品的普遍适用性。

公开(公告)号：US07893223B2

公开(公告)日：2011-02-22

申请号：US11165793

申请日：2005-06-24

Applicant: Giovanni Battista Giovenzana ,  Giovanni Palmisano ,  Massimo Sisti ,  Camilla Cavallotti ,  Silvio Aime ,  Luisella Calabi ,  Rolf Swenson ,  Ramalingam Kondareddiar ,  Luciano Lattuada ,  Pierfrancesco Morosini

Inventor： Giovanni Battista Giovenzana ,  Giovanni Palmisano ,  Massimo Sisti ,  Camilla Cavallotti ,  Silvio Aime ,  Luisella Calabi ,  Rolf Swenson ,  Ramalingam Kondareddiar ,  Luciano Lattuada ,  Pierfrancesco Morosini

IPC: C07F13/00

CPC classification number: C07C209/62 ,  A61K49/0002 ,  A61K49/085 ,  A61K49/106 ,  A61K49/122 ,  A61K49/14 ,  A61K51/088 ,  C07D243/08 ,  C07D243/14 ,  C07F9/301 ,  C07F9/3808 ,  C07F9/4816 ,  C07F9/645 ,  C07C211/50

Abstract: Compounds of general formula (I): with substituents as defined herein and their chelates with bi-trivalent ions of the metal elements of atomic numbers 20 to 31, 39, 42, 43, 44, 49, and 57 to 83, and radioisotopes chosen among 203Pb, 67Ga, 68Ga, 72As, 111In, 113In, 90Y, 97Ru, 62Cu, 64Cu, 52Fe, 52mMn, 140La, 175Yb, 153Sm, 166Ho, 149Pm, 177Lu, 142Pr, 159Gd, 212Bi, 47Sc, 149Pm, 67Cu, 111Ag, 199Au, 161Tb, 51Cr, 167Tm, 141Ce, 168Yb, 88Y, 165Dy, 166Dy, 97Ru, 103Ru, 186Re, 99mTc, 211Bi, 213Bi, 214Bi, 105Rh, 109Pd, 177mSn, 177Sn and 199Au, as well as the salts thereof with physiologically compatible bases or acids.

Abstract translation: 通式（I）的化合物：具有如本文所定义的取代基及其与原子序数为20至31,39,42,43,44,49和57至83的金属元素的双三价离子的螯合物和选择的放射性同位素 在203Pb，67Ga，68Ga，72As，111In，113In，90Y，97Ru，62Cu，64Cu，52Fe，52mMn，140La，175Yb，153Sm，166Ho，149Pm，177Lu，142Pr，159Gd，212Bi，47Sc，149Pm，67Cu，111Ag ，199Au，161Tb，51Cr，167Tm，141Ce，168Yb，88Y，165Dy，166Dy，97Ru，103Ru，186Re，99mTc，211Bi，213Bi，214Bi，105Rh，109Pd，177mSn，177Sn和199Au， 生理相容的碱或酸。

公开(公告)号：US06403055B1

公开(公告)日：2002-06-11

申请号：US09612392

申请日：2000-07-07

Applicant: Luisella Calabi ,  Alessandro Maiocchi ,  Marco Lolli ,  Fabrizio Rebasti

Inventor： Luisella Calabi ,  Alessandro Maiocchi ,  Marco Lolli ,  Fabrizio Rebasti

IPC: A61B5055

CPC classification number: C07D209/20 ,  A61K49/06 ,  C07C229/26 ,  C07C229/36 ,  C07C229/76 ,  Y10S977/928 ,  Y10S977/93

Abstract: Compounds of formula (I): are used as their paramagnetic chelates as contrast agents in magnetic resonance imaging. These compounds have high affinity to plasma proteins and exhibit extremely high values of relaxivity in serum and are thus useful as blood pool contrast agents.

Abstract translation: 式（I）化合物在磁共振成像中用作对比剂作为它们的顺磁性螯合物。 这些化合物对血浆蛋白质具有高亲和力，并且在血清中表现出非常高的舒张度值，因此可用作血液池造影剂。

公开(公告)号：US20110082280A1

公开(公告)日：2011-04-07

申请号：US12949306

申请日：2010-11-18

Applicant: Giovanni Battista GIOVENZANA ,  Giovanni PALMISANO ,  Massimo SISTI ,  Camilla CAVALLOTTI ,  Silvio AIME ,  Luisella CALABI ,  Rolf SWENSON ,  Kondareddiar RAMALINGAM ,  Luciano LATTUADA ,  Pierfrancesco MOROSINI

Inventor： Giovanni Battista GIOVENZANA ,  Giovanni PALMISANO ,  Massimo SISTI ,  Camilla CAVALLOTTI ,  Silvio AIME ,  Luisella CALABI ,  Rolf SWENSON ,  Kondareddiar RAMALINGAM ,  Luciano LATTUADA ,  Pierfrancesco MOROSINI

IPC: C07K7/08 ,  C07D243/12 ,  C07K7/06 ,  C07D403/06 ,  C07D243/08

CPC classification number: C07C209/62 ,  A61K49/0002 ,  A61K49/085 ,  A61K49/106 ,  A61K49/122 ,  A61K49/14 ,  A61K51/088 ,  C07D243/08 ,  C07D243/14 ,  C07F9/301 ,  C07F9/3808 ,  C07F9/4816 ,  C07F9/645 ,  C07C211/50

Abstract: Methods of coupling targeting molecules to multidentate aza ligands of general formula (I): in which: R1 through R5 and FG are as defined in the specification are presented. The aza ligands and/or the resulting conjugates may be labeled with bi-trivalent ions of the metal elements having atomic number ranging between 20 and 31, 39, 42, 43, 44, 49, and between 57 and 83, and radioisotopes chosen among 203Pb, 67Ga, 68Ga, 72As, 111In, 113In, 90Y, 97Ru, 62Cu, 64Cu, 52Fe, 52mMn, 140La, 175Yb, 153Sm, 166Ho, 149Pm, 177Lu, 142Pr, 159Gd, 212Bi, 47Sc, 149Pm, 67Cu, 111Ag, 199Au, 161Tb, 51Cr, 167Tm, 141Ce, 168Yb, 88Y, 165Dy, 166Dy, 97Ru, 103Ru, 186Re, 188Re, 99mTc, 211Bi, 212Bi, 213Bi, 214Bi, 105Rh, 109Pd, 117mSn, 177Sn and 199Au.

Abstract translation: 将靶向分子与通式（I）的多齿氮杂配体偶联的方法：其中：R1至R5和FG如说明书中所定义。 氮杂配体和/或所得到的缀合物可以用原子序数在20,31,42,43,44,49和57和83之间的金属元素的二价离子标记，并且放射性同位素选自 203Pb，67Ga，68Ga，72As，111In，113In，90Y，97Ru，62Cu，64Cu，52Fe，52mMn，140La，175Yb，153Sm，166Ho，149Pm，177Lu，142Pr，159Gd，212Bi，47Sc，149Pm，67Cu，111Ag， 199Au，161Tb，51Cr，167Tm，141Ce，168Yb，88Y，165Dy，166Dy，97Ru，103Ru，186Re，188Re，99mTc，211Bi，212Bi，213Bi，214Bi，105Rh，109Pd，117mSn，177Sn和199Au。

公开(公告)号：US20060034773A1

公开(公告)日：2006-02-16

申请号：US11165793

申请日：2005-06-24

Applicant: Giovanni Giovenzana ,  Giovanni Palmisano ,  Massimo Sisti ,  Camilla Cavallotti ,  Silvio Aime ,  Luisella Calabi ,  Rolf Swenson ,  Ramalingam Kondareddiar ,  Luciano Lattuada ,  Pierfrancesco Morosini

Inventor： Giovanni Giovenzana ,  Giovanni Palmisano ,  Massimo Sisti ,  Camilla Cavallotti ,  Silvio Aime ,  Luisella Calabi ,  Rolf Swenson ,  Ramalingam Kondareddiar ,  Luciano Lattuada ,  Pierfrancesco Morosini

IPC: A61K49/10 ,  C07F9/22

CPC classification number: C07C209/62 ,  A61K49/0002 ,  A61K49/085 ,  A61K49/106 ,  A61K49/122 ,  A61K49/14 ,  A61K51/088 ,  C07D243/08 ,  C07D243/14 ,  C07F9/301 ,  C07F9/3808 ,  C07F9/4816 ,  C07F9/645 ,  C07C211/50

Abstract: Compounds of general formula (I): in which: R1 through R5 are as defined in the specification FG, which can be the same or different, are carboxy, —PO3H2 or —RP(O)OH groups, wherein R is hydrogen, or an optionally substituted group selected from C1-C20 alkyl, C3-C10 cycloalkyl, C4-C20 cycloalkylalkyl, aryl, arylalkyl, a group bearing an acidic moiety, and a group bearing an amino moiety, each of which may be further optionally substituted with functional groups which allow conjugation with a suitable molecule able to interact with physiological systems; and their chelates with bi-trivalent ions of the metal elements having atomic number ranging between 20 and 31, 39, 42, 43, 44, 49, and between 57 and 83, and radioisotopes chosen among 203Pb, 67Ga, 68Ga, 72As, 111In, 113In, 90Y, 97Ru, 62Cu, 64Cu, 52Fe, 52mMn, 140La, 175Yb, 153Sm, 166Ho, 149Pm, 177Lu, 142Pr, 159Gd, 212Bi, 47Sc, 149Pm, 67Cu, 111Ag, 199Au, 161Tb, 51Cr, 167Tm, 141Ce, 168Yb, 88Y, 165Dy, 166Dy, 97Ru, 103Ru, 186Re, 188Re, 99mTc, 211Bi, 212Bi, 213Bi, 214Bi, 105Rh, 109Pd, 117mSn, 177Sn and 199Au, as well as the salts thereof with physiologically compatible bases or acids.

公开(公告)号：US06509324B1

公开(公告)日：2003-01-21

申请号：US09913711

申请日：2001-09-24

Applicant: Maurizio Franzini ,  Andrea Beltrami ,  Luisella Calabi ,  Alessandro Maiocchi ,  Mario Virtuani ,  Pier Lucio Anelli ,  Kondareddiar Ramalingam ,  Ramachandran S. Ranganathan

Inventor： Maurizio Franzini ,  Andrea Beltrami ,  Luisella Calabi ,  Alessandro Maiocchi ,  Mario Virtuani ,  Pier Lucio Anelli ,  Kondareddiar Ramalingam ,  Ramachandran S. Ranganathan

IPC: C07F928

CPC classification number: A61K49/10 ,  A61K49/0438 ,  A61K49/085 ,  A61K49/103 ,  C07F9/3808 ,  C07F9/5728 ,  C07J51/00 ,  Y10S977/93

Abstract: Compounds able to chelate bi- and trivalent paramagnetic metal ions, their chelated complexes with these metal ions and physiologically compatible salts thereof and therein magnetic resonance imaging.

Abstract translation: 能够螯合双和三价顺磁性金属离子，它们与这些金属离子的螯合络合物及其生理相容的盐以及其中磁共振成像的化合物。

公开(公告)号：US06337064B1

公开(公告)日：2002-01-08

申请号：US09601576

申请日：2000-09-25

Applicant: Marino Brocchetta ,  Luisella Calabi ,  Daniela Palano ,  Lino Paleari ,  Fulvio Uggeri

Inventor： Marino Brocchetta ,  Luisella Calabi ,  Daniela Palano ,  Lino Paleari ,  Fulvio Uggeri

IPC: A61K4910

CPC classification number: C07C229/16 ,  A61K49/06 ,  C07C233/83 ,  C07C2603/24 ,  Y10S977/915

Abstract: Compounds of formula (I) both in the racemic and optically active forms, are used in MRI diagnostic imaging.

Abstract translation: 以外消旋和旋光形式的式（I）化合物用于MRI诊断成像。