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    • 2. 发明申请
    • HETERODIMERS OF GLUTAMIC ACID
    • 谷氨酸的交联剂
    • US20080193381A1
    • 2008-08-14
    • US11936659
    • 2007-11-07
    • John W. BabichCraig N. ZimmermanKevin P. Maresca
    • John W. BabichCraig N. ZimmermanKevin P. Maresca
    • A61K49/00C07D213/04C07C275/04A61K31/17A61P35/00A61K31/444C07F13/00
    • C07C275/16A61K39/385C07B59/001C07C275/24C07C275/30C07C311/19C07D213/38
    • Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR′R′, Q is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R′ is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
    • 式(Ia)的化合物,其中R是C 6 -C 12取代或未取代的芳基,C 6 -C 12 取代或未取代的杂芳基,C 1 -C 6 - 取代或未取代的烷基或-NR'R',Q是C(O),O,NR C(O)2(CH 2)p Y是C(O),O,NR',S,S(O )C 2(O)2(CH 2)n Z Z是H或C 1 -C 3 烷基,R'是H,C(O),S(O)2,C(O)2,C 6 C 12 -C 12取代或未取代的芳基,C 6 -C 12 - 取代或未取代的杂芳基或C 1 当被取代时,芳基,杂芳基和烷基被卤素取代,取代或未取代的烷基,C 6 -C 12 具有诊断和治疗性质的杂芳基,-NR'R'或COOZ,例如前列腺癌的治疗和治疗以及与NAALADase抑制相关的其它疾病。 放射性标记可以通过各种通过碳或杂原子连接在X氨基酸侧链附着的假基团并入结构中。
    • 4. 发明申请
    • Heterodimers of Glutamic Acid
    • 谷氨酸的异二聚体
    • US20120269726A1
    • 2012-10-25
    • US13271549
    • 2011-10-12
    • John W. BabichCraig N. ZimmermanKevin P. Maresca
    • John W. BabichCraig N. ZimmermanKevin P. Maresca
    • A61K51/04A61P25/00G01N33/573A61P25/18A61P29/00A61P25/04A61K39/385A61P35/00
    • C07C275/16A61K39/385C07B59/001C07C275/24C07C275/30C07C311/19C07D213/38
    • Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR′R′, Q is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R′ is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C1-C12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
    • 式(Ia)化合物,其中R是C 6 -C 12取代或未取代的芳基,C 6 -C 12取代或未取代的杂芳基,C 1 -C 6取代或未取代的烷基或-NR'R',Q是C(O) ,NR',S,S(O)2,C(O)2(CH 2)p Y是C(O),O,NR',S,S(O)2,C(O) Z是H或C1-C4烷基,R'是H,C(O),S(O)2,C(O)2,C6-C12取代或未取代的芳基,C6-C12取代或未取代的杂芳基或 C 1 -C 6取代或未取代的烷基,当被取代时,芳基,杂芳基和烷基被卤素,C 1 -C 12杂芳基,-NR'R'或COOZ取代,其具有诊断和治疗性质,例如前列腺癌的治疗和治疗 和其他与NAALADase抑制有关的疾病。 放射性标记可以通过各种通过碳或杂原子连接在X氨基酸侧链附着的假基团并入结构中。
    • 5. 发明申请
    • HETERODIMERS OF GLUTAMIC ACID
    • 谷氨酸的交联剂
    • US20120208988A1
    • 2012-08-16
    • US13294677
    • 2011-11-11
    • John W. BabichCraig N. ZimmermanKevin P. Maresca
    • John W. BabichCraig N. ZimmermanKevin P. Maresca
    • C07F13/00C07C311/19C07C275/24C07D401/12C07C275/16
    • C07C275/16A61K39/385C07B59/001C07C275/24C07C275/30C07C311/19C07D213/38
    • Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR′R′, Q is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R′ is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
    • 式(Ia)化合物,其中R是C 6 -C 12取代或未取代的芳基,C 6 -C 12取代或未取代的杂芳基,C 1 -C 6取代或未取代的烷基或-NR'R',Q是C(O) ,NR',S,S(O)2,C(O)2(CH 2)p Y是C(O),O,NR',S,S(O)2,C(O) Z是H或C1-C4烷基,R'是H,C(O),S(O)2,C(O)2,C6-C12取代或未取代的芳基,C6-C12取代或未取代的杂芳基或 C 1 -C 6取代或未取代的烷基,当被取代时,芳基,杂芳基和烷基被卤素,C 6 -C 12杂芳基,-NR'R'或COOZ取代,其具有诊断和治疗性质,例如前列腺癌的治疗和治疗 和其他与NAALADase抑制有关的疾病。 放射性标记可以通过各种通过碳或杂原子连接在X氨基酸侧链附着的假基团并入结构中。
    • 7. 发明授权
    • Technetium-dipyridine complexes, and methods of use thereof
    • 锝 - 二吡啶络合物及其使用方法
    • US07381399B2
    • 2008-06-03
    • US10386403
    • 2003-03-11
    • John W. BabichKevin P. Maresca
    • John W. BabichKevin P. Maresca
    • A61K51/00A61M36/14
    • C07D213/38C07F13/005
    • One aspect of the invention relates to novel complexes of technetium (Tc) with various heteroaromatic ligands, e.g., pyridyl and imidazolyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to novel pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the technetium complexes are also described. Another aspect of the invention relates to novel pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.
    • 本发明的一个方面涉及锝(Tc)与各种杂芳族配体如吡啶基和咪唑基配体的新型复合物,以及它们在放射性药物中用于各种临床诊断和治疗应用的用途。 本发明的另一方面涉及形成上述配合物的一部分的新型吡啶基配体。 还描述了制备锝络合物的方法。 本发明的另一方面涉及基于通过固相合成方法与小肽缀合的衍生化赖氨酸,丙氨酸和双氨基酸的新型吡啶基配体。 另外,本发明涉及使用本发明复合物成像哺乳动物区域的方法。