公开(公告)号：US20160304555A1

公开(公告)日：2016-10-20

申请号：US14917127

申请日：2012-08-21

Applicant: Eric WANG ,  Hartmuth C. KOLB ,  Anna Katrin INGS ,  Changhui LIU ,  Joseph C. WALSH ,  Gang CHEN ,  Anjana SINHA ,  Dhanalakshmi KASI ,  Chul YU ,  Umesh B. GANGADHARMATH ,  Wei ZHANG ,  Tieming ZHAO ,  Vani P. MOCHARLA

Inventor： Eric Wang ,  Hartmuth C. Kolb ,  Anna Katrin Szardenings ,  Changhui Liu ,  Joseph C. Walsh ,  Gang Chen ,  Anjana Sinha ,  Dhanalakshmi Kasi ,  Chul Yu ,  Umesh B. Gangadharmath ,  Wei Zhang ,  Tieming Zhao ,  Vani P. Mocharla

IPC: C07K5/02 ,  A61K51/04 ,  A61K51/08 ,  C07D249/06 ,  C07D249/04

CPC classification number: C07K5/0215 ,  A61K38/00 ,  A61K51/0453 ,  A61K51/088 ,  C07D207/16 ,  C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D233/78 ,  C07D233/96 ,  C07D239/60 ,  C07D249/04 ,  C07D249/06 ,  C07D251/30 ,  C07D263/34 ,  C07D277/56 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07K5/06026 ,  C07K5/06113

Abstract: Compounds for targeting and agents for imaging, Prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.

Abstract translation: 公开了靶向化合物和成像剂，前列腺特异性膜抗原（PSMA）。 还公开了合成化合物和成像剂的方法以及PSMA成像方法。 所公开的成像剂适用于PET和SPECT成像。

公开(公告)号：US20110182812A1

公开(公告)日：2011-07-28

申请号：US13035405

申请日：2011-02-25

Applicant: Anna Katrin Szardenings ,  Wei Zhang ,  Hartmuth C. Kolb ,  Daniel Kurt Cashion ,  Gang Chen ,  Dhanalakshmi Kasi ,  Changhui Liu ,  Anjana Sinha ,  Eric Wang ,  Chul Yu ,  Umesh B. Gangadharmath ,  Joseph C. Walsh

Inventor： Anna Katrin Szardenings ,  Wei Zhang ,  Hartmuth C. Kolb ,  Daniel Kurt Cashion ,  Gang Chen ,  Dhanalakshmi Kasi ,  Changhui Liu ,  Anjana Sinha ,  Eric Wang ,  Chul Yu ,  Umesh B. Gangadharmath ,  Joseph C. Walsh

IPC: A61K51/04 ,  C07D513/04 ,  C07D231/56 ,  C07D487/04 ,  C07D471/04 ,  C07D413/14 ,  C07D401/10 ,  C07D401/04 ,  A61K49/00 ,  A61P43/00 ,  A61P25/28

CPC classification number: C07D235/04 ,  A61K51/04 ,  C07B59/002 ,  C07D215/06 ,  C07D235/14 ,  C07D277/62 ,  C07D401/02 ,  C07D401/04 ,  C07D403/06 ,  C07D413/10 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

Abstract: Imaging agents of formulas (I)-(V) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formulas (I)-(V) capable of binding to tau proteins and β-amyloid peptides are presented herein. The invention also relates to methods of imaging Aβ and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formulas (I)-(V) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.

Abstract translation: 式（I） - （V）的成像剂和用于检测神经障碍的方法包括向需要的患者施用能够结合tau蛋白和＆amp;淀粉样蛋白肽的式（I） - （V）化合物。 本发明还涉及成像A＆bgr的方法; 和tau聚集体，其包括引入可检测量的包含放射性标记的式（I） - （V）化合物的药物制剂，并检测患者中与淀粉样蛋白沉积物和/或tau蛋白相关的标记化合物。 这些方法和组合使得临床前诊断和监测AD和其他神经障碍的进展。

公开(公告)号：US20100239496A1

公开(公告)日：2010-09-23

申请号：US12661777

申请日：2010-03-23

Applicant: Umesh B. Gangadharmath ,  Hartmuth C. Kolb ,  Peter J.H. Scott ,  Joseph C. Walsh ,  Wei Zhang ,  Anna Katrin Szardenings ,  Anjana Sinha ,  Gang Chen ,  Eric Wang ,  Vani P. Mocharia ,  Chul Yu ,  Changhui Liu ,  Daniel Kurt Cashion ,  Dhanalakshmi Kasi

Inventor： Umesh B. Gangadharmath ,  Hartmuth C. Kolb ,  Peter J.H. Scott ,  Joseph C. Walsh ,  Wei Zhang ,  Anna Katrin Szardenings ,  Anjana Sinha ,  Gang Chen ,  Eric Wang ,  Vani P. Mocharia ,  Chul Yu ,  Changhui Liu ,  Daniel Kurt Cashion ,  Dhanalakshmi Kasi

IPC: A61K51/04 ,  C07D401/04 ,  C07D215/06 ,  C07D413/10 ,  C07D235/18 ,  C07D405/04 ,  C07D409/04 ,  C07D413/14 ,  C07D497/04 ,  C12Q1/02

CPC classification number: A61K51/0455 ,  A61K51/04 ,  A61K51/0453 ,  A61K51/0459 ,  A61K51/0463 ,  C07B59/002 ,  C07D215/06 ,  C07D235/14 ,  C07D277/62 ,  C07D401/04 ,  C07D403/06 ,  C07D413/10 ,  C07D413/14 ,  C07D487/04

Abstract: Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formula (I) capable of binding to tau proteins and β-amyloid peptides are presented herein. The invention also relates to methods of imaging Aβ and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.

Abstract translation: 式（I）的成像剂和用于检测神经障碍的方法包括向需要的患者施用能够结合tau蛋白和β-淀粉样蛋白肽的式（I）化合物。 本发明还涉及成像A＆bgr的方法; 和tau聚集体，其包括引入可检测量的包含放射性标记的式（I）化合物的药物制剂，并检测患者中与淀粉样蛋白沉积物和/或tau蛋白相关的标记化合物。 这些方法和组合使得临床前诊断和监测AD和其他神经障碍的进展。

公开(公告)号：US10011632B2

公开(公告)日：2018-07-03

申请号：US14917127

申请日：2012-08-21

Applicant: Eric Wang ,  Hartmuth C. Kolb ,  Anna Katrin Szardenings ,  Changhui Liu ,  Joseph C. Walsh ,  Gang Chen ,  Anjana Sinha ,  Dhanalakshmi Kasi ,  Chul Yu ,  Umesh B. Gangadharmath ,  Wei Zhang ,  Tieming Zhao ,  Vani P. Mocharla

Inventor： Eric Wang ,  Hartmuth C. Kolb ,  Anna Katrin Szardenings ,  Changhui Liu ,  Joseph C. Walsh ,  Gang Chen ,  Anjana Sinha ,  Dhanalakshmi Kasi ,  Chul Yu ,  Umesh B. Gangadharmath ,  Wei Zhang ,  Tieming Zhao ,  Vani P. Mocharla

IPC: C07K5/02 ,  A61K51/04 ,  C07D249/06 ,  C07D249/04 ,  A61K51/08 ,  C07K5/062 ,  C07K5/072 ,  C07D403/12 ,  C07D213/81 ,  C07D213/82 ,  C07D233/78 ,  C07D233/96 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D239/60 ,  C07D251/30 ,  C07D263/34 ,  C07D207/16 ,  C07D277/56 ,  C07D209/48 ,  A61K38/00

CPC classification number: C07K5/0215 ,  A61K38/00 ,  A61K51/0402 ,  A61K51/0453 ,  A61K51/0497 ,  A61K51/088 ,  C07D207/16 ,  C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D233/78 ,  C07D233/96 ,  C07D239/60 ,  C07D249/04 ,  C07D249/06 ,  C07D251/30 ,  C07D263/34 ,  C07D277/56 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07K5/06026 ,  C07K5/06113

Abstract: Compounds for targeting and agents for imaging, Prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.

公开(公告)号：US20120302755A1

公开(公告)日：2012-11-29

申请号：US13477095

申请日：2012-05-22

Applicant: Anna Katrin Szardenings ,  Hartmuth C. Kolb ,  Joseph C. Walsh ,  Gang Chen ,  Umesh B. Gangadharmath ,  Dhanalakshmi Kasi ,  Changhui Liu ,  Anjana Sinha ,  Eric Wang ,  Chul Yu ,  Wei Zhang ,  Kai Chen ,  Vani P. Mocharla ,  Peter J.H. Scott

Inventor： Anna Katrin Szardenings ,  Hartmuth C. Kolb ,  Joseph C. Walsh ,  Gang Chen ,  Umesh B. Gangadharmath ,  Dhanalakshmi Kasi ,  Changhui Liu ,  Anjana Sinha ,  Eric Wang ,  Chul Yu ,  Wei Zhang ,  Kai Chen ,  Vani P. Mocharla ,  Peter J.H. Scott

IPC: C07D471/04 ,  C07D471/14

CPC classification number: A61K51/0455 ,  A61K51/0446 ,  C07B59/002 ,  C07D471/04 ,  C07D471/14

Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled carbazoles and derivatives thereof and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.

Abstract translation: 本文公开了在哺乳动物中诊断阿尔茨海默病或倾向于其的化合物和方法，所述方法包括向哺乳动物施用诊断有效量的放射性标记的化合物，其中所述化合物选自放射性标记的咔唑及其衍生物，以及 三唑衍生物，允许化合物分布到脑组织中并对脑组织进行成像，其中与正常对照水平的结合相比，化合物与脑组织的结合增加表明哺乳动物患有或处于危险中 发展为阿尔茨海默病。

公开(公告)号：US09023318B2

公开(公告)日：2015-05-05

申请号：US13849646

申请日：2013-03-25

Applicant: Gang Chen ,  Umesh B. Gangadharmath ,  Dhanalakshmi Kasi ,  Harmuth C. Kolb ,  Changhui Liu ,  Anjana Sinha ,  Anna Katrin Szardenings ,  Joseph C. Walsh ,  Eric Wang ,  Chul Yu ,  Wei Zhang ,  Klaus Kopka ,  Guenter Haufe ,  Michael Schaefers ,  Verena Hugenberg ,  Stefan Wagner ,  Sven Hermann ,  Hans-Joerg Breyholz ,  Andreas Faust

Inventor： Gang Chen ,  Umesh B. Gangadharmath ,  Dhanalakshmi Kasi ,  Harmuth C. Kolb ,  Changhui Liu ,  Anjana Sinha ,  Anna Katrin Szardenings ,  Joseph C. Walsh ,  Eric Wang ,  Chul Yu ,  Wei Zhang ,  Klaus Kopka ,  Guenter Haufe ,  Michael Schaefers ,  Verena Hugenberg ,  Stefan Wagner ,  Sven Hermann ,  Hans-Joerg Breyholz ,  Andreas Faust

IPC: A61K51/00 ,  A61M36/14 ,  C07D403/14 ,  C07D405/14 ,  C07D249/04 ,  C07D309/12 ,  C07D213/42

CPC classification number: C07D403/14 ,  C07D213/42 ,  C07D249/04 ,  C07D309/12 ,  C07D405/14

Abstract: Novel compounds and pharmaceutical compositions having MMP inhibitory activity are disclosed, which have been found to be particularly useful in the prevention, treatment and diagnostic imaging of diseases associated with an unpaired activity of MMP, amongst others MMP-2, MMP-8, MMP-9 and/or MMP-13 to name a few. The compounds of the present invention are useful for the prevention, the treatment and the in vivo diagnostic imaging of a range of disease states (inflammatory, malignant and degenerative diseases) where specific matrix metalloproteinases are known to be involved.

Abstract translation: 已经公开了具有MMP抑制活性的新型化合物和药物组合物，其已经被发现特别可用于预防，治疗和诊断成像与MMP的非配对活性相关的疾病，其中MMP-2，MMP-8，MMP- 9和/或MMP-13等等。 本发明的化合物可用于预防，治疗和体内诊断成像的一系列疾病状态（炎性，恶性和退行性疾病），其中已知特定的基质金属蛋白酶涉及。

公开(公告)号：US20130217887A1

公开(公告)日：2013-08-22

申请号：US13849646

申请日：2013-03-25

Applicant: Gang Chen ,  Umesh B. Gangadharmath ,  Dhanalakshmi Kasi ,  Harmuth C. Kolb ,  Changhui Liu ,  Anjana Sinha ,  Anna Katrin Szardenings ,  Joseph C. Walsh ,  Eric Wang ,  Chul Yu ,  Wei Zhang ,  Klaus Kopka ,  Guenter Haufe ,  Michael Schaefers ,  Verena Hugenberg ,  Stefan Wagner ,  Sven Hermann ,  Hans-Joerg Breyholz ,  Andreas Faust

Inventor： Gang Chen ,  Umesh B. Gangadharmath ,  Dhanalakshmi Kasi ,  Harmuth C. Kolb ,  Changhui Liu ,  Anjana Sinha ,  Anna Katrin Szardenings ,  Joseph C. Walsh ,  Eric Wang ,  Chul Yu ,  Wei Zhang ,  Klaus Kopka ,  Guenter Haufe ,  Michael Schaefers ,  Verena Hugenberg ,  Stefan Wagner ,  Sven Hermann ,  Hans-Joerg Breyholz ,  Andreas Faust

IPC: C07D403/14 ,  C07D249/04 ,  C07D405/14

CPC classification number: C07D403/14 ,  C07D213/42 ,  C07D249/04 ,  C07D309/12 ,  C07D405/14

Abstract: Novel compounds and pharmaceutical compositions having MMP inhibitory activity are disclosed, which have been found to be particularly useful in the prevention, treatment and diagnostic imaging of diseases associated with an unpaired activity of MMP, amongst others MMP-2, MMP-8, MMP-9 and/or MMP-13 to name a few. The compounds of the present invention are useful for the prevention, the treatment and the in vivo diagnostic imaging of a range of disease states (inflammatory, malignant and degenerative diseases) where specific matrix metalloproteinases are known to be involved.

Abstract translation: 已经公开了具有MMP抑制活性的新型化合物和药物组合物，其已经被发现特别可用于预防，治疗和诊断成像与MMP的非配对活性相关的疾病，其中MMP-2，MMP-8，MMP- 9和/或MMP-13等等。 本发明的化合物可用于预防，治疗和体内诊断成像的一系列疾病状态（炎性，恶性和退行性疾病），其中已知特定的基质金属蛋白酶涉及。

公开(公告)号：US08491869B2

公开(公告)日：2013-07-23

申请号：US12661777

申请日：2010-03-23

Applicant: Umesh B. Gangadharmath ,  Hartmuth C. Kolb ,  Peter J. H. Scott ,  Joseph C. Walsh ,  Wei Zhang ,  Anna Katrin Szardenings ,  Anjana Sinha ,  Gang Chen ,  Eric Wang ,  Vani P. Mocharia ,  Chul Yu ,  Changhui Liu ,  Daniel Kurt Cashion ,  Dhanalakshmi Kasi

Inventor： Umesh B. Gangadharmath ,  Hartmuth C. Kolb ,  Peter J. H. Scott ,  Joseph C. Walsh ,  Wei Zhang ,  Anna Katrin Szardenings ,  Anjana Sinha ,  Gang Chen ,  Eric Wang ,  Vani P. Mocharia ,  Chul Yu ,  Changhui Liu ,  Daniel Kurt Cashion ,  Dhanalakshmi Kasi

IPC: A61K51/00 ,  A61M36/14

CPC classification number: A61K51/0455 ,  A61K51/04 ,  A61K51/0453 ,  A61K51/0459 ,  A61K51/0463 ,  C07B59/002 ,  C07D215/06 ,  C07D235/14 ,  C07D277/62 ,  C07D401/04 ,  C07D403/06 ,  C07D413/10 ,  C07D413/14 ,  C07D487/04

Abstract: Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering ti a patient in need compounds of formula (I) capable of binding to tau proteins and β-amyloid peptides are presented herein. The invention also relates to methods of imaging Aβ and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.

Abstract translation: 式（I）的成像剂和用于检测神经障碍的方法包括给予需要能够结合tau蛋白和β-淀粉样肽的式（I）化合物的化合物。 本发明还涉及成像Abeta和tau聚集体的方法，包括引入可检测量的包含放射性标记的式（I）化合物的药物制剂，并检测患者中与淀粉样蛋白沉积物和/或tau蛋白相关的标记化合物。 这些方法和组合使得临床前诊断和监测AD和其他神经障碍的进展。