公开(公告)号：US11040973B2

公开(公告)日：2021-06-22

申请号：US16499133

申请日：2018-03-29

Applicant: Purdue Research Foundation

Inventor： Herman O. Sintim ,  Neetu Dayal ,  Clement Opoku-Temeng

IPC: C07D471/02 ,  A61K31/4745 ,  C07D471/14 ,  C07D209/08 ,  C07D231/56 ,  C07D401/14 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D491/147 ,  C07D495/14 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

Abstract: The present invention generally relates to compounds as a dual kinase-demethylase inhibitor useful for the treatment of diseases mediated by a kinase and/or a histone demethylase, such as inflammation, cancer, viral and bacterial infections, neurological and immunological disorders. Pharmaceutical compositions and methods for treating those diseases are within the scope of this invention.

公开(公告)号：US20200308173A1

公开(公告)日：2020-10-01

申请号：US16499133

申请日：2018-03-29

Applicant: Purdue Research Foundation

Inventor： Herman O. Sintim ,  Neetu Dayal ,  Clement Opoku-Temeng

IPC: C07D471/14 ,  C07D491/147 ,  C07D471/04 ,  C07D495/14 ,  C07D417/12 ,  C07D209/08 ,  C07D231/56 ,  C07D401/14 ,  C07D413/14 ,  C07D519/00 ,  C07D513/04 ,  C07D498/04

Abstract: The present invention generally relates to compounds as a dual kinase-demethylase inhibitor useful for the treatment of diseases mediated by a kinase and/or a histone demethylase, such as inflammation, cancer, viral and bacterial infections, neurological and immunological disorders. Pharmaceutical compositions and methods for treating those diseases are within the scope of this invention.

公开(公告)号：US20250002501A1

公开(公告)日：2025-01-02

申请号：US18885251

申请日：2024-09-13

Applicant: Purdue Research Foundation

Inventor： Herman O. Sintim ,  George Naclerio ,  Caroline Karanja

IPC: C07D495/04

Abstract: Cyclic nucleotides, both mono- and di-nucleotides, play diverse roles in the prokaryotes and eukaryotes. Described are compounds, which inhibit phosphodiesterases that inhibit cyclic mononucleotide or dinucleotides and/or both mononucleotide and dinucleotide. These compounds have potential diverse applications as antiviral, antibacterial, anti-inflammatory and anticancer agents, including cancer immunotherapy. Pharmaceutical compositions and methods for treating those kinase related diseases are within the scope of this invention.

公开(公告)号：US11891391B2

公开(公告)日：2024-02-06

申请号：US17243629

申请日：2021-04-29

Applicant: PURDUE RESEARCH FOUNDATION

Inventor： Herman O. Sintim ,  Neetu Dayal ,  Clement Opoku-Temeng

IPC: C07D471/06 ,  A61K31/437 ,  C07D471/14 ,  C07D209/08 ,  C07D231/56 ,  C07D401/14 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D491/147 ,  C07D495/14 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

CPC classification number: C07D471/14 ,  C07D209/08 ,  C07D231/56 ,  C07D401/14 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D491/147 ,  C07D495/14 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00 ,  C07B2200/05

Abstract: The present invention generally relates to compounds as a dual kinase-demethylase inhibitor useful for the treatment of diseases mediated by a kinase and/or a histone demethylase, such as inflammation, cancer, viral and bacterial infections, neurological and immunological disorders. Pharmaceutical compositions and methods for treating those diseases are within the scope of this invention.

公开(公告)号：US20230312562A1

公开(公告)日：2023-10-05

申请号：US18012564

申请日：2021-07-01

Applicant: Purdue Research Foundation

Inventor： Herman O. Sintim ,  Neetu Dayal

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: The present invention generally relates to tetrahydro-3H-pyrazolo-[4,3-f]-quinolone and tetrahydro-3H-pyrrolo-[3,2-f]quinoline-containing compounds as a tubulin polymerization inhibitor for the treatment of various cancers, and methods of uses thereof. Pharmaceutical compositions and the methods for treating those kinase related diseases are within the scope of this invention.

公开(公告)号：US20230183246A1

公开(公告)日：2023-06-15

申请号：US17926379

申请日：2021-05-13

Applicant: Purdue Research Foundation

Inventor： David Harley Thompson ,  Herman O. Sintim ,  Qingqing Qi ,  Shruti Biyani

IPC: C07D487/04 ,  C07D401/06 ,  C07D471/04 ,  B01J31/24

CPC classification number: C07D487/04 ,  C07D401/06 ,  C07D471/04 ,  B01J31/2404 ,  B01J2531/824 ,  B01J2231/32

Abstract: The present disclosure relates to a telescoped continuous flow Sonogashira coupling synthesis for some lead compounds to support in vivo studies and pre-clinical evaluation. The application of high throughput tools combined with the telescoped continuous synthesis method can enable an efficient and safe synthesis of compounds of interest involving hazardous coupling reagents such as HATU, while minimizing by-product formation.

公开(公告)号：US11022604B2

公开(公告)日：2021-06-01

申请号：US16555486

申请日：2019-08-29

Applicant: Purdue Research Foundation

Inventor： Marxa L. Figueiredo ,  Charles Samuel Umbaugh ,  Herman O. Sintim ,  Adriana Diaz-Quinones

IPC: G01N33/50 ,  G01N33/574 ,  G16B15/30 ,  G16C20/60 ,  G16C20/50 ,  A61K31/497

Abstract: An in silico screening method generated compounds that are against laminin receptor 37LR and their anti-cancer functions in prostate cancer cell lines are disclosed herein. A group of derivatives based on the hit compound from the in silico screening are synthesized and tested with improved IC50 value that can have relevant clinical use for prostate cancer or osteoarthritis.

公开(公告)号：US20200064334A1

公开(公告)日：2020-02-27

申请号：US16555486

申请日：2019-08-29

Applicant: Purdue Research Foundation

Inventor： Marxa L. Figueiredo ,  Charles Samuel Umbaugh ,  Herman O. Sintim ,  Adriana Diaz-Quinones

IPC: G01N33/50 ,  G01N33/574 ,  A61K31/497 ,  G16C20/60 ,  G16C20/50 ,  G16B15/30

Abstract: An in silico screening method generated compounds that are against laminin receptor 37LR and their anti-cancer functions in prostate cancer cell lines are disclosed herein. A group of derivatives based on the hit compound from the in silico screening are synthesized and tested with improved IC50 value that can have relevant clinical use for prostate cancer or osteoarthritis.

公开(公告)号：US20190065669A1

公开(公告)日：2019-02-28

申请号：US16113718

申请日：2018-08-27

Applicant: Purdue Research Foundation

Inventor： Marxa L. Figueiredo ,  Charles Samuel Umbaugh ,  Herman O. Sintim ,  Adriana Diaz-Quinones

IPC: G06F19/16 ,  C40B30/02 ,  A61K31/497 ,  A61P35/00 ,  A61P19/02

CPC classification number: G16B15/00 ,  A61K31/497 ,  A61P19/02 ,  A61P35/00 ,  G16B15/30 ,  G16B35/00 ,  G16C20/50 ,  G16C20/60 ,  G16C20/64

Abstract: An in silico screening method generated compounds that are against laminin receptor 37 LR and their anti-cancer functions in prostate cancer cell lines are disclosed herein. A group of derivatives based on the hit compound from the in silico screening are synthesized and tested with improved IC50 value that can have relevant clinical use for prostate cancer or osteoarthritis.