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公开(公告)号：US08378134B2
公开(公告)日：2013-02-19
申请号：US12570705
申请日：2009-09-30
申请人： Brian James Grimmond , Michael Todd Luttrell , Jeannette Christine DePuy , Mary Elizabeth Spilker , Michael James Rishel
发明人： Brian James Grimmond , Michael Todd Luttrell , Jeannette Christine DePuy , Mary Elizabeth Spilker , Michael James Rishel
IPC分类号： C07F15/00 , C07D225/00
CPC分类号： A61K49/103 , C07C229/16 , C07C229/76
摘要： In one aspect, the present invention provides a contrast enhancement agent comprising an iron chelate having structure I wherein R1 is independently at each occurrence a hydroxy group, a C1-C3hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R2-R7 are independently at each occurrence hydrogen, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R1-R7 is a hydroxy group or a C1-C3hydroxyalkyl group; and wherein Q is a charge balancing counterion. Also provided is a metal chelating ligand having structure IX and medical formulations comprising the contrast enhancement I.
摘要翻译： 一方面，本发明提供一种对比度增强剂，其包含具有结构I的铁螯合物，其中R1在每次出现时独立地为羟基，C1-C3羟烷基或C1-C3烷基，b为0-4 ; R2-R7各自独立地为氢，C1-C3羟基烷基或C1-C3烷基，条件是R1-R7中的至少一个为羟基或C1-C3羟烷基; 并且其中Q是电荷平衡抗衡离子。 还提供了具有结构IX的金属螯合配体和包含对比度增强I的医学制剂。
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公开(公告)号：US20110076237A1
公开(公告)日：2011-03-31
申请号：US12570705
申请日：2009-09-30
申请人： Brian James Grimmond , Michael Todd Luttrell , Jeannette Christine DePuy , Mary Elizabeth Spilker , Michael James Rishel
发明人： Brian James Grimmond , Michael Todd Luttrell , Jeannette Christine DePuy , Mary Elizabeth Spilker , Michael James Rishel
IPC分类号： A61K49/10 , C07F15/02 , C07C229/02 , C07C229/36
CPC分类号： A61K49/103 , C07C229/16 , C07C229/76
摘要： In one aspect, the present invention provides a contrast enhancement agent comprising an iron chelate having structure I wherein R1 is independently at each occurrence a hydroxy group, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R2-R7 are independently at each occurrence hydrogen, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R1-R7 is a hydroxy group or a C1-C3 hydroxyalkyl group; and wherein Q is a charge balancing counterion. Also provided is a metal chelating ligand having structure IX and medical formulations comprising the contrast enhancement I.
摘要翻译： 一方面，本发明提供了一种对比度增强剂，其包含具有结构I的铁螯合物，其中R1在每次出现时独立地为羟基，C1-C3羟烷基或C1-C3烷基，b为0- 4; R2-R7各自独立地为氢，C1-C3羟基烷基或C1-C3烷基，条件是R1-R7中的至少一个为羟基或C1-C3羟烷基; 并且其中Q是电荷平衡抗衡离子。 还提供了具有结构IX的金属螯合配体和包含对比度增强I的医学制剂。
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公开(公告)号：US20110245512A1
公开(公告)日：2011-10-06
申请号：US12956629
申请日：2010-11-30
IPC分类号： C07F7/18 , C07F9/40 , C07F9/6596 , C07F9/6561 , C07F9/38
CPC分类号： A61K49/103 , C07F9/3808 , C07F9/4075 , C07F9/6552 , C07F9/65522 , C07F9/6596
摘要： In one aspect, the present invention provides a contrast enhancement agent comprising an iron chelate having structure I and salts thereof wherein R1 is independently at each occurrence a hydroxy group, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R2-R7 are independently at each occurrence hydrogen, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R1-R7 is a hydroxy group or a C1-C3 hydroxyalkyl group; and wherein Q is one or more charge balancing counterions. Also provided are a metal chelating ligand having structure IX and medical formulations comprising the contrast enhancement agent I.
摘要翻译： 一方面，本发明提供一种对比度增强剂，其包含具有结构I的铁螯合物及其盐，其中R1在每次出现时独立地为羟基，C1-C3羟烷基或C1-C3烷基，b 是0-4; R2-R7各自独立地为氢，C1-C3羟基烷基或C1-C3烷基，条件是R1-R7中的至少一个为羟基或C1-C3羟烷基; 并且其中Q是一个或多个电荷平衡抗衡离子。 还提供了具有结构IX的金属螯合配体和包含对比度增强剂I的医药制剂。
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公开(公告)号：US08722020B2
公开(公告)日：2014-05-13
申请号：US12956629
申请日：2010-11-30
IPC分类号： A61B5/055 , C07F9/48 , C07D319/08
CPC分类号： A61K49/103 , C07F9/3808 , C07F9/4075 , C07F9/6552 , C07F9/65522 , C07F9/6596
摘要： In one aspect, the present invention provides a contrast enhancement agent comprising an iron chelate having structure I and salts thereof wherein R1 is independently at each occurrence a hydroxy group, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R2-R7 are independently at each occurrence hydrogen, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R1-R7 is a hydroxy group or a C1-C3 hydroxyalkyl group; and wherein Q is one or more charge balancing counterions. Also provided are a metal chelating ligand having structure IX and medical formulations comprising the contrast enhancement agent I.
摘要翻译： 一方面，本发明提供一种对比度增强剂，其包含具有结构I的铁螯合物及其盐，其中R1在每次出现时独立地为羟基，C1-C3羟烷基或C1-C3烷基，b 是0-4; R2-R7各自独立地为氢，C1-C3羟基烷基或C1-C3烷基，条件是R1-R7中的至少一个为羟基或C1-C3羟烷基; 并且其中Q是一个或多个电荷平衡抗衡离子。 还提供了具有结构IX的金属螯合配体和包含对比度增强剂I的医药制剂。
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公开(公告)号：US20110077417A1
公开(公告)日：2011-03-31
申请号：US12614729
申请日：2009-11-09
IPC分类号： C07D319/08 , C07F15/02 , C07C69/003
CPC分类号： C07F7/1896 , C07D319/08 , C07F7/1804 , Y02P20/55
摘要： In one aspect, the present invention provides a protected ligand precursor having structure XXI wherein R8 is independently at each occurrence a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R9-R11 are independently at each occurrence hydrogen, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R8-R11 is a protected hydroxy group or a protected C1-C3 hydroxyalkyl group; and R12 and R13 are independently at each occurrence acid sensitive protecting groups.
摘要翻译： 一方面，本发明提供了具有结构XXI的受保护配体前体，其中R8在每次出现时独立地为保护的羟基，被保护的C 1 -C 3羟烷基或C 1 -C 3烷基，b为0-4; R 9 -R 11在每次出现时独立地为氢，被保护的C 1 -C 3羟基烷基或C 1 -C 3烷基，条件是R 8 -R 11中的至少一个为被保护的羟基或被保护的C 1 -C 3羟烷基 ; R12和R13各自独立地存在酸敏感的保护基。
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公开(公告)号：US20110077396A1
公开(公告)日：2011-03-31
申请号：US12785110
申请日：2010-05-21
IPC分类号： C07F15/02 , C07D319/08 , C07C229/36 , C07F7/18 , C07C215/20
CPC分类号： A61K49/103
摘要： In one aspect, the present invention provides a protected ligand precursor having structure XX wherein R8 is independently at each occurrence a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R9-R11 are independently at each occurrence hydrogen, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R8-R11 is a protected hydroxy group or a protected C1-C3 hydroxyalkyl group; and R12 and R13 are independently at each occurrence a protecting group is selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, and C2-C30 aromatic radicals.
摘要翻译： 一方面，本发明提供具有结构XX的保护配体前体，其中R8在每次出现时独立地为保护的羟基，受保护的C1-C3羟烷基或C1-C3烷基，b为0-4; R 9 -R 11在每次出现时独立地为氢，被保护的C 1 -C 3羟基烷基或C 1 -C 3烷基，条件是R 8 -R 11中的至少一个为被保护的羟基或被保护的C 1 -C 3羟烷基 ; 并且R 12和R 13在每次出现时独立地为保护基团，选自C 1 -C 30脂族基，C 3 -C 30环脂族基和C 2 -C 30芳族基。
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公开(公告)号：US08362281B2
公开(公告)日：2013-01-29
申请号：US12751286
申请日：2010-03-31
IPC分类号： C07D319/08 , C07F9/40
CPC分类号： C07F9/091 , C07F9/4006 , C07F9/65522 , Y02P20/55
摘要： In one aspect, the present invention provides a protected ligand precursor having structure XX wherein R8 is independently at each occurrence a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R9-R11 are independently at each occurrence hydrogen, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R8-R11 is a protected hydroxy group or a protected C1-C3 hydroxyalkyl group; and R12 and R13 are independently at each occurrence a protecting group is selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, and C2-C30 aromatic radicals.
摘要翻译： 一方面，本发明提供具有结构XX的保护配体前体，其中R8在每次出现时独立地为保护的羟基，受保护的C1-C3羟烷基或C1-C3烷基，b为0-4; R 9 -R 11在每次出现时独立地为氢，被保护的C 1 -C 3羟基烷基或C 1 -C 3烷基，条件是R 8 -R 11中的至少一个为保护的羟基或被保护的C 1 -C 3羟烷基 ; 并且R 12和R 13在每次出现时独立地为保护基团，选自C 1 -C 30脂族基，C 3 -C 30环脂族基和C 2 -C 30芳族基。
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公开(公告)号：US20110243858A1
公开(公告)日：2011-10-06
申请号：US13077746
申请日：2011-03-31
CPC分类号： A61K49/103
摘要： A method of diagnostic imaging is disclosed comprising administering a medical formulation to a subject, the formulation comprising a contrast enhancement agent having structure I and salts thereof wherein R1 is independently at each occurrence a hydroxy group, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R2-R7 are independently at each occurrence hydrogen, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R1-R7 is a hydroxy group or a C1-C3 hydroxyalkyl group; and wherein Q is one or more charge balancing counterions; and one or more pharmaceutically acceptable carriers and excipients. The subject is subjected to a diagnostic imaging technique such as magnetic resonance imaging. The technique may be used in a variety of diagnostic imaging regimes, such as imaging of circulatory systems, genitourinary systems, hepatobiliary systems, central nervous systems, tumors, and abscesses among others.
摘要翻译： 公开了一种诊断成像方法，其包括向受试者施用药物制剂，所述制剂包含具有结构I的对比增强剂及其盐，其中R1在每次出现时独立地为羟基，C1-C3羟烷基或C1 -C 3烷基，b为0-4; R2-R7各自独立地为氢，C1-C3羟基烷基或C1-C3烷基，条件是R1-R7中的至少一个为羟基或C1-C3羟烷基; 并且其中Q是一个或多个电荷平衡抗衡离子; 和一种或多种药学上可接受的载体和赋形剂。 对受试者进行诸如磁共振成像的诊断成像技术。 该技术可用于各种诊断成像方案，例如循环系统的成像，泌尿生殖系统，肝胆系统，中枢神经系统，肿瘤和脓肿等。
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公开(公告)号：US08765977B2
公开(公告)日：2014-07-01
申请号：US13077746
申请日：2011-03-31
IPC分类号： C07D319/08 , C07D309/30
CPC分类号： A61K49/103
摘要： A method of diagnostic imaging is disclosed comprising administering a medical formulation to a subject, the formulation comprising a contrast enhancement agent having structure I and salts thereof wherein R1 is independently at each occurrence a hydroxy group, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R2-R7 are independently at each occurrence hydrogen, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R1-R7 is a hydroxy group or a C1-C3 hydroxyalkyl group; and wherein Q is one or more charge balancing counterions; and one or more pharmaceutically acceptable carriers and excipients. The subject is subjected to a diagnostic imaging technique such as magnetic resonance imaging. The technique may be used in a variety of diagnostic imaging regimes, such as imaging of circulatory systems, genitourinary systems, hepatobiliary systems, central nervous systems, tumors, and abscesses among others.
摘要翻译： 公开了一种诊断成像方法，其包括向受试者施用药物制剂，所述制剂包含具有结构I的对比增强剂及其盐，其中R1在每次出现时独立地为羟基，C1-C3羟烷基或C1 -C 3烷基，b为0-4; R2-R7各自独立地为氢，C1-C3羟基烷基或C1-C3烷基，条件是R1-R7中的至少一个为羟基或C1-C3羟烷基; 并且其中Q是一个或多个电荷平衡抗衡离子; 和一种或多种药学上可接受的载体和赋形剂。 对受试者进行诸如磁共振成像的诊断成像技术。 该技术可用于各种诊断成像方案，例如循环系统的成像，泌尿生殖系统，肝胆系统，中枢神经系统，肿瘤和脓肿等。
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公开(公告)号：US20110245511A1
公开(公告)日：2011-10-06
申请号：US12751286
申请日：2010-03-31
CPC分类号： C07F9/091 , C07F9/4006 , C07F9/65522 , Y02P20/55
摘要： In one aspect, the present invention provides a protected ligand precursor having structure XX wherein R8 is independently at each occurrence a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R9-R11 are independently at each occurrence hydrogen, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R8-R11 is a protected hydroxy group or a protected C1-C3 hydroxyalkyl group; and R12 and R13 are independently at each occurrence a protecting group is selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, and C2-C30 aromatic radicals.
摘要翻译： 一方面，本发明提供具有结构XX的保护配体前体，其中R8在每次出现时独立地为保护的羟基，受保护的C1-C3羟烷基或C1-C3烷基，b为0-4; R 9 -R 11在每次出现时独立地为氢，被保护的C 1 -C 3羟基烷基或C 1 -C 3烷基，条件是R 8 -R 11中的至少一个为被保护的羟基或被保护的C 1 -C 3羟烷基 ; 并且R 12和R 13在每次出现时独立地为保护基团，选自C 1 -C 30脂族基，C 3 -C 30环脂族基和C 2 -C 30芳族基。
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