公开(公告)号：US20190211019A1

公开(公告)日：2019-07-11

申请号：US16246745

申请日：2019-01-14

申请人： Duquesne University of the Holy Ghost

发明人： Aleem Gangjee

IPC分类号： C07D487/04 ,  A61K31/519 ,  C07D239/70 ,  A61K31/517

CPC分类号： C07D487/04 ,  A61K31/517 ,  A61K31/519 ,  C07D239/70

摘要： The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.

公开(公告)号：US20170015672A1

公开(公告)日：2017-01-19

申请号：US15280724

申请日：2016-09-29

申请人： DUQUESNE UNIVERSITY OF THE HOLY GHOST ,  WAYNE STATE UNIVERSITY

发明人： ALEEM GANGJEE ,  LARRY H. MATHERLY

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： Pyrrolo[2,3-d]pyrimidine derivatives, and pharmaceutical acceptable salts thereof, useful in therapeutically treating patients with cancer are disclosed. These compounds selectively target folate receptors (FR) of cancerous tumor cells and inhibit purine synthesis and hence, DNA synthesis.

摘要翻译： 公开了可用于治疗癌症患者的吡咯并[2,3-d]嘧啶衍生物及其药学上可接受的盐。 这些化合物选择性靶向癌性肿瘤细胞的叶酸受体（FR），并抑制嘌呤合成，从而抑制DNA合成。

公开(公告)号：US20160097754A1

公开(公告)日：2016-04-07

申请号：US14503711

申请日：2014-10-01

申请人： Duquesne University of The Holy Ghost

发明人： Partha BASU ,  Igor PIMKOV ,  Kristine DEIBLER

IPC分类号： G01N33/20 ,  G01N21/76 ,  C07D495/14

CPC分类号： G01N33/20 ,  C07D495/14 ,  G01N21/643 ,  G01N2021/6439

摘要： The invention relates to non-fluorescent or low-fluorescent compounds for contact with mercury ions to produce fluorescent compounds as a detector for mercury. The fluorescence produced by the contact of the non-fluorescent or low-fluorescent compounds with mercury ions has an intensity greater than the intensity produced by the contact of the non-fluorescent or low-fluorescent compounds with other metals. The fluorescent compounds may be used as sensors/detectors for mercury ions in various samples. Methods for detecting and calculating the concentration of mercury ions in samples are also disclosed.

摘要翻译： 本发明涉及用于与汞离子接触以产生荧光化合物作为汞检测器的非荧光或低荧光化合物。 通过非荧光或低荧光化合物与汞离子的接触产生的荧光的强度大于非荧光或低荧光化合物与其它金属接触产生的强度。 荧光化合物可用作各种样品中汞离子的传感器/检测器。 还公开了检测和计算样品中汞离子浓度的方法。

公开(公告)号：US09266889B2

公开(公告)日：2016-02-23

申请号：US14581314

申请日：2014-12-23

申请人： DUQUESNE UNIVERSITY OF THE HOLY GHOST

发明人： Partha Basu ,  Igor Pimkov

IPC分类号： C07D475/04 ,  C07D495/04 ,  C07D409/04 ,  C07D487/04 ,  C07D495/14

CPC分类号： C07D475/04 ,  C07D409/04 ,  C07D487/04 ,  C07D495/04 ,  C07D495/14

摘要： The present invention relates to substituted pterin compounds, their synthesis and use. In particular, the present invention relates to a new precursor compound and its analogs for synthesizing a new substituted pterin compound and its analogs. These new compounds are particularly suitable for treating molybdenum cofactor deficiency.

公开(公告)号：US10654792B2

公开(公告)日：2020-05-19

申请号：US15383635

申请日：2016-12-19

申请人： DUQUESNE UNIVERSITY OF THE HOLY GHOST

发明人： Suravi Chakrabarty ,  Darlene Monlish ,  Patrick Flaherty ,  Jane E. Cavanaugh ,  Sneha Potdar

IPC分类号： C07C227/10 ,  C07C229/58

摘要： The invention generally relates to compounds having structure I: wherein x represents alkyl, aryl or het-aryl, each of y independently represents hydrogen or halogen and z represents hydrogen or alkyl. Further, said compounds are inhibitors of MEK 1, 2 and 5. Furthermore, the invention includes methods of making said compounds, compositions including said compounds and uses for inhibiting MEK 1, 2 and 5.

公开(公告)号：US10208051B2

公开(公告)日：2019-02-19

申请号：US15875231

申请日：2018-01-19

申请人： Duquesne University of the Holy Ghost

发明人： Aleem Gangjee

IPC分类号： C07D487/04 ,  C07D239/70 ,  A61K31/517 ,  A61K31/519

摘要： The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.

公开(公告)号：US09908846B2

公开(公告)日：2018-03-06

申请号：US14626984

申请日：2015-02-20

申请人： DUQUESNE UNIVERSITY OF THE HOLY GHOST

发明人： Fraser Fergusson Fleming ,  Jesus Armando Lujan-Montelongo

IPC分类号： C07C317/28 ,  C07C303/36 ,  C07C315/00 ,  C07C317/30

CPC分类号： C07C317/28 ,  C07C303/36 ,  C07C315/00 ,  C07C317/30 ,  C07C2601/14

摘要： This invention relates to novel isonitriles, including arylsulfonyl isonitriles, and methods for their synthesis. The isonitriles include a conjugated ring system. The structure is designed with the flexibility to have multiple substitution patterns. The isonitriles may be used in applications including, but not limited to, pharmaceutical compositions.

公开(公告)号：US09896455B2

公开(公告)日：2018-02-20

申请号：US15242928

申请日：2016-08-22

申请人： Duquesne University of the Holy Ghost

发明人： Aleem Gangjee

IPC分类号： C07D487/04 ,  C07D239/70 ,  A61K31/517 ,  A61K31/519

CPC分类号： C07D487/04 ,  A61K31/517 ,  A61K31/519 ,  C07D239/70

摘要： The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.

公开(公告)号：US09556112B2

公开(公告)日：2017-01-31

申请号：US14081426

申请日：2013-11-15

申请人： DUQUESNE UNIVERSITY OF THE HOLY GHOST

发明人： Suravi Chakrabarty ,  Darlene Monlish ,  Patrick Flaherty ,  Jane E. Cavanaugh ,  Sneha Potdar

IPC分类号： C07C229/58

CPC分类号： C07C227/10 ,  C07C229/58

摘要： The invention generally relates to compounds having structure I: wherein x represents alkyl, aryl or het-aryl, each of y independently represents hydrogen or halogen and z represents hydrogen or alkyl. Further, said compounds are inhibitors of MEK 1, 2 and 5. Furthermore, the invention includes methods of making said compounds, compositions including said compounds and uses for inhibiting MEK 1, 2 and 5.

摘要翻译： 本发明一般涉及具有结构I的化合物：其中x代表烷基，芳基或苯基 - 芳基，y各自独立地表示氢或卤素，z代表氢或烷基。 此外，所述化合物是MEK 1,2和5的抑制剂。此外，本发明包括制备所述化合物，包含所述化合物的组合物和用于抑制MEK 1,2和5的方法。

公开(公告)号：US20160229857A1

公开(公告)日：2016-08-11

申请号：US14617332

申请日：2015-02-09

申请人： Duquesne University of The Holy Ghost

发明人： ALEEM GANGJEE ,  LARRY H. MATHERLY

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： Pyrrolo[2,3-d]pyrimidine derivatives, and pharmaceutical acceptable salts thereof, useful in therapeutically treating patients with cancer are disclosed. These compounds selectively target folate receptors (FR) of cancerous tumor cells and inhibit purine synthesis and hence, DNA synthesis.

摘要翻译： 公开了可用于治疗癌症患者的吡咯并[2,3-d]嘧啶衍生物及其药学上可接受的盐。 这些化合物选择性靶向癌性肿瘤细胞的叶酸受体（FR），并抑制嘌呤合成，从而抑制DNA合成。