公开(公告)号：US06734208B2

公开(公告)日：2004-05-11

申请号：US10170971

申请日：2002-06-13

Applicant: David J. Grainger ,  James C. Metcalfe ,  Sudhakar Kasina

Inventor： David J. Grainger ,  James C. Metcalfe ,  Sudhakar Kasina

IPC: A61K3138

CPC classification number: A61K31/275 ,  A61K31/381 ,  C07D333/38 ,  G01N33/74 ,  G01N2333/495 ,  G01N2333/71 ,  G01N2800/108 ,  G01N2800/323

Abstract: The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compounds that elevate TGF-beta levels, as well as pharmaceutical compositions comprising compounds that elevate TGF-beta levels, and methods for detecting diseases associated with endothelial cell activation.

Abstract translation: 本发明提供了治疗具有或具有与TGF-β缺乏相关的指征的哺乳动物的方法，包括施用一种或多种有效提高TGF-β水平的试剂。 本发明还提供了提高TGF-β水平的新化合物，以及包含提高TGF-β水平的化合物的药物组合物，以及用于检测与内皮细胞活化相关的疾病的方法。

公开(公告)号：US06410587B1

公开(公告)日：2002-06-25

申请号：US09567558

申请日：2000-05-05

Applicant: David J. Grainger ,  James C. Metcalfe ,  Sudhakar Kasina

Inventor： David J. Grainger ,  James C. Metcalfe ,  Sudhakar Kasina

IPC: A61K3138

CPC classification number: A61K31/275 ,  A61K31/381 ,  C07D333/38 ,  G01N33/74 ,  G01N2333/495 ,  G01N2333/71 ,  G01N2800/108 ,  G01N2800/323

Abstract: The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compounds that elevate TGF-beta levels, as well as pharmaceutical compositions comprising compounds that elevate TGF-beta levels, and methods for detecting diseases associated with endothelial cell activation.

Abstract translation: 本发明提供了治疗具有或具有与TGF-β缺乏相关的指征的哺乳动物的方法，包括施用一种或多种有效提高TGF-β水平的试剂。 本发明还提供了提高TGF-β水平的新化合物，以及包含提高TGF-β水平的化合物的药物组合物，以及用于检测与内皮细胞活化相关的疾病的方法。

公开(公告)号：US06177551B1

公开(公告)日：2001-01-23

申请号：US09310900

申请日：1999-05-12

Applicant: Sudhakar Kasina

Inventor： Sudhakar Kasina

IPC: C07F938

CPC classification number: C07F13/005 ,  A61K51/04 ,  A61K51/0478 ,  A61K51/0482 ,  A61K51/0489 ,  A61K51/0497 ,  A61K51/087 ,  A61K51/088 ,  C07B2200/05 ,  C07C229/16 ,  C07C323/34 ,  C07D257/10 ,  C07D265/32 ,  C07D285/00 ,  C07D333/36 ,  C07D495/04 ,  C07D495/14 ,  C07F9/3817 ,  C07F9/6524 ,  C07F9/655345 ,  C07F9/6561

Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.

公开(公告)号：US6117911A

公开(公告)日：2000-09-12

申请号：US057323

申请日：1998-04-09

Applicant: David J. Grainger ,  James C. Metcalfe ,  Sudhakar Kasina

Inventor： David J. Grainger ,  James C. Metcalfe ,  Sudhakar Kasina

IPC: A61K31/381 ,  C07D333/38 ,  G01N33/74 ,  A61K31/135 ,  C07C213/00

CPC classification number: A61K31/275 ,  A61K31/381 ,  C07D333/38 ,  G01N33/74 ,  G01N2333/495 ,  G01N2333/71 ,  G01N2800/108 ,  G01N2800/323

Abstract: The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compounds that elevate TGF-beta levels, as well as pharmaceutical compositions comprising compounds that elevate TGF-beta levels, and methods for detecting diseases associated with endothelial cell activation.

公开(公告)号：US6015897A

公开(公告)日：2000-01-18

申请号：US645211

申请日：1996-05-13

Applicant: Louis J. Theodore ,  Sudhakar Kasina ,  John M. Reno ,  Linda M. Gustavson

Inventor： Louis J. Theodore ,  Sudhakar Kasina ,  John M. Reno ,  Linda M. Gustavson

IPC: A61K47/48 ,  A61K48/00 ,  A61K51/10 ,  C07K14/765 ,  C07K16/30 ,  C12N15/87 ,  C07D257/02

CPC classification number: B82Y5/00 ,  A61K47/48146 ,  A61K47/48569 ,  A61K47/48746 ,  A61K48/00 ,  A61K51/1093 ,  C07K14/765 ,  C07K16/30 ,  C12N15/87 ,  A61K2039/505 ,  C07K2317/77

Abstract: Methods, compounds, compositions and kits that relate to pretargeted delivery of diagnostic and therapeutic agents are disclosed. Biotinamido-N-methylglycyl-seryl-O-succinamido-benzyl DOTA is disclosed.

Abstract translation: 公开了与诊断和治疗剂的预靶向递送相关的方法，化合物，组合物和试剂盒。 公开了生物素酰氨基-N-甲基甘氨酰 - 丝氨酰基-O-琥珀酰氨基 - 苄基DOTA。

公开(公告)号：US5556982A

公开(公告)日：1996-09-17

申请号：US90609

申请日：1993-07-12

Applicant: Alan R. Fritzberg ,  Sudhakar Kasina ,  Linda M. Gustavson

Inventor： Alan R. Fritzberg ,  Sudhakar Kasina ,  Linda M. Gustavson

IPC: A61K47/48 ,  A61K51/04 ,  A61K51/10 ,  A61K51/12 ,  C07B59/00 ,  C07C227/08 ,  C07C271/22 ,  C07C323/60 ,  C07D285/00 ,  C07D495/04 ,  C07F13/00 ,  C07K14/36 ,  C07K14/465 ,  C07D235/02 ,  A61K49/00 ,  C07C69/62 ,  C07C229/14 ,  A61K43/00

CPC classification number: C07D285/00 ,  A61K47/48746 ,  A61K47/48753 ,  A61K51/0478 ,  A61K51/0495 ,  A61K51/0497 ,  A61K51/10 ,  A61K51/1045 ,  A61K51/1048 ,  A61K51/1066 ,  A61K51/1093 ,  A61K51/12 ,  B82Y5/00 ,  C07B59/004 ,  C07B59/008 ,  C07C227/08 ,  C07C271/22 ,  C07C323/60 ,  C07D495/04 ,  C07F13/005 ,  C07K14/36 ,  C07K14/465 ,  A61K2123/00

Abstract: Protein, ligand and anti-ligand conjugated chelated metal radionuclides are provided for use in vivo. Intermediates are provided for preparing the compositions efficiently.

Abstract translation: 提供蛋白质，配体和抗配体缀合的螯合金属放射性核素用于体内。 提供中间体有效地制备组合物。

公开(公告)号：US5202109A

公开(公告)日：1993-04-13

申请号：US643578

申请日：1991-01-31

Applicant: Alan R. Fritzberg ,  Jean-Luc E. Vanderheyden ,  Sudhakar Kasina ,  Jeffrey N. Fitzner

Inventor： Alan R. Fritzberg ,  Jean-Luc E. Vanderheyden ,  Sudhakar Kasina ,  Jeffrey N. Fitzner

IPC: A61K51/04 ,  C07F9/38 ,  C07F13/00

CPC classification number: C07F9/3873 ,  A61K51/0497 ,  C07F13/005 ,  A61K2121/00 ,  A61K2123/00

Abstract: The present invention provides conjugates formed from calcified tissues targeting agents and radiolabeled compounds. One such conjugate comprises a chelate and a targeting agent that is capable of associating with calcified tissue, wherein the chelate contains at least one nitrogen atom or at least one sulfur atom or combinations thereof as the donor atoms.Another aspect of the invention provides method for using the conjugates for diagnostic and therapeutic purposes, including those related to bone cancer.

Abstract translation: 本发明提供由钙化组织靶向剂和放射性标记化合物形成的缀合物。 一种这样的缀合物包括能够与钙化组织结合的螯合物和靶向剂，其中螯合物含有至少一个氮原子或至少一个硫原子或其组合作为供体原子。 本发明的另一方面提供了用于诊断和治疗目的的缀合物的方法，包括与骨癌相关的那些。

公开(公告)号：US20110269943A1

公开(公告)日：2011-11-03

申请号：US12825229

申请日：2010-06-28

Applicant: Sudhakar Kasina ,  John M. Reno ,  Alan R. Fritzberg ,  Jonathan Tait

Inventor： Sudhakar Kasina ,  John M. Reno ,  Alan R. Fritzberg ,  Jonathan Tait

IPC: C07K14/00

CPC classification number: C07K7/06 ,  A61K47/54 ,  A61K47/547 ,  A61K47/549 ,  A61K51/087 ,  A61K51/088 ,  A61K2123/00 ,  C07K1/13 ,  C07K14/4721

Abstract: Radiolabeled annexin and modified annexin conjugates useful for imaging vascular thrombi are described. Methods for making and using such radiolabeled annexin conjugates are also provided.

Abstract translation: 描述了可用于成像血管血栓的放射性标记的膜联蛋白和修饰的膜联蛋白缀合物。 还提供了制备和使用这种放射性标记的膜联蛋白缀合物的方法。

公开(公告)号：US07511070B2

公开(公告)日：2009-03-31

申请号：US11270185

申请日：2005-11-09

Applicant: David J. Grainger ,  James C. Metcalfe ,  Sudhakar Kasina

Inventor： David J. Grainger ,  James C. Metcalfe ,  Sudhakar Kasina

IPC: A61K31/135 ,  A61K31/40 ,  C07C213/00 ,  C07C207/00

CPC classification number: A61K31/275 ,  A61K31/381 ,  C07D333/38 ,  G01N33/74 ,  G01N2333/495 ,  G01N2333/71 ,  G01N2800/108 ,  G01N2800/323

Abstract: The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compounds that elevate TGF-beta levels, as well as pharmaceutical compositions comprising compounds that elevate TGF-beta levels, and methods for detecting diseases associated with endothelial cell activation.

公开(公告)号：US06359111B1

公开(公告)日：2002-03-19

申请号：US09321054

申请日：1999-05-27

Applicant: Damon L. Meyer ,  Sudhakar Kasina

Inventor： Damon L. Meyer ,  Sudhakar Kasina

IPC: A61K31381

CPC classification number: C07D489/00 ,  A61K49/0002 ,  A61K51/0497

Abstract: A compound comprising a ligand portion which has binding affinity for an opioid receptor, and a therapeutically or diagnostically effective group selected from radionuclide chelating agents, fluorochromes, toxins, drugs, polyboron moieties, proteins, biological response modifiers, chemical moieties capable of binding to other molecules of interest, and radioisotopes selected from therapeutically effective alpha and beta emitters, and diagnostically effective gamma emitters. The compound may be used in a method of treating cancer, and in a method of imaging opioid receptors either inside or outside of the central nervous system.

Abstract translation: 包含对阿片受体具有结合亲和力的配体部分的化合物和选自放射性核素螯合剂，荧光染料，毒素，药物，多硼骨部分，蛋白质，生物反应调节剂，能够结合其他物质的化学部分的治疗或诊断有效的基团 感兴趣的分子和选自治疗有效的α和β发射体的放射性同位素以及诊断上有效的γ发射体。 该化合物可用于治疗癌症的方法，以及用于在中枢神经系统内部或外部成像阿片受体的方法。