公开(公告)号：US20240325321A1

公开(公告)日：2024-10-03

申请号：US18281737

申请日：2022-03-11

Applicant: Arizona Board of Regents on Behalf of the University of Arizona

Inventor： Jun Wang ,  Yanmei Hu ,  Chunlong Ma ,  Naoya Kitamura

IPC: A61K31/137 ,  A61K31/166 ,  A61K31/18 ,  A61K31/40 ,  A61K31/4045 ,  A61K31/415 ,  A61K31/416 ,  A61K31/417 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4406 ,  A61K31/4412 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4965 ,  A61K31/513 ,  A61K31/538 ,  A61K31/69 ,  A61P31/14

CPC classification number: A61K31/137 ,  A61K31/166 ,  A61K31/18 ,  A61K31/40 ,  A61K31/4045 ,  A61K31/415 ,  A61K31/416 ,  A61K31/417 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4406 ,  A61K31/4412 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4965 ,  A61K31/513 ,  A61K31/538 ,  A61K31/69 ,  A61P31/14

Abstract: This invention is in the field of medicinal chemistry and relates to a new class of small-molecules having a N-methyl-1-(naphthalen-1-yl)ethan-1-amine (or similar) structure (e.g.: Formula I) which function as inhibitors of the SARS-CoV-2 papain-like protease (PLpro), which function as therapeutics for the treatment of viral infection characterized with PLpro protease activity and/or expression (e.g., COVID-19), and which function as therapeutics for the treatment of other conditions characterized with PLpro protease activity and/or expression.

公开(公告)号：US20230192674A1

公开(公告)日：2023-06-22

申请号：US17924863

申请日：2021-05-12

Applicant: Arizona Board of Regents on Behalf of the University of Arizona

Inventor： Jun Wang ,  Rajesh Khanna

IPC: C07D409/14 ,  C07D405/14 ,  C07D401/14 ,  C07D417/14 ,  C07D413/14 ,  A61P25/02 ,  A61K45/06

CPC classification number: C07D409/14 ,  C07D405/14 ,  C07D401/14 ,  C07D417/14 ,  C07D413/14 ,  A61P25/02 ,  A61K45/06

Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a piperazine or piperidine structure which function as inhibitors of the CaV3.2 voltage gated calcium channel activity (e.g., depolarization-induced calcium influx), and their use as therapeutics for the treatment and/or prevention of CaV3.2 related pain e g., HIV-associated peripheral sensory neuropathy, chemotherapy-induced peripheral neuropathy (CIPN), spinal nerve ligation (SNL) induced neuropathy) and related conditions.

公开(公告)号：US20220332683A1

公开(公告)日：2022-10-20

申请号：US17724125

申请日：2022-04-19

Applicant: Arizona Board of Regents on Behalf of the University of Arizona

Inventor： Jun Wang

IPC: C07D207/273 ,  C07D207/46 ,  A61K31/16 ,  A61P11/00 ,  A61P31/14 ,  C07D209/02 ,  A61K9/00

Abstract: This invention is in the field of medicinal chemistry and relates to a new class of small-molecules having a pyrrolidinone-acetamide (or similar) structure (e.g., Formula I) which function as inhibitors of the SARS-CoV-2 papain-like protease (PLpro), which function as inhibitors of the SARS-CoV-2 related viral 3CL protease (MPpro), which function as therapeutics for the treatment of viral infection characterized with PLPpro and/or Mpro protease activity and/or expression (e.g., COVID-19), and which function as therapeutics for the treatment of other conditions characterized with PLPpro and/or Mpro protease activity and/or expression.

公开(公告)号：US20230148179A1

公开(公告)日：2023-05-11

申请号：US17917789

申请日：2021-04-07

Applicant: Arizona Board of Regents on Behalf of the University of Arizona

Inventor： Jun Wang ,  Chunlong Ma

IPC: C07K5/083 ,  A61K45/06 ,  C07K5/062 ,  C07K5/065 ,  C07K5/087 ,  A61K38/05 ,  A61K38/06 ,  A61P31/14 ,  C07C323/41 ,  A61K31/27

CPC classification number: C07K5/081 ,  A61K45/06 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/0812 ,  C07K5/06034 ,  C07K5/0808 ,  A61K38/05 ,  A61K38/06 ,  A61P31/14 ,  C07C323/41 ,  A61K31/27

Abstract: This invention is in the field of medicinal pharmacology. In particular, the present invention relates to pharmaceutical agents which function as inhibitors of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) viral replication and/or SARS-CoV-2 related viral 3CL protease (Mpro) activity. The invention further relates to methods of treating and/or ameliorating symptoms related to conditions caused by the SARS-CoV-2 virus (e.g., COVID-19), comprising administering to a subject (e.g., a human patient) a composition comprising one or more pharmaceutical agents which function as inhibitors of SARS-CoV-2 viral replication and/or inhibitors of SARS-CoV-2 related Mpro activity.

公开(公告)号：US20220306627A1

公开(公告)日：2022-09-29

申请号：US17705984

申请日：2022-03-28

Applicant: Arizona Board of Regents on Behalf of the University of Arizona

Inventor： Jun Wang ,  Naoya Kitamura

IPC: C07D471/04

Abstract: This invention is in the field of medicinal chemistry and relates to a new class of small-molecules having a pyrazolopyridine (or similar) structure (e.g., Formula I) which function as inhibitors of the viral protein 2C protein activity and/or expression, and which function as therapeutics for the treatment of viral infection characterized with viral protein 2C activity and/or expression (e.g., non-polio enterovirus infection) (e.g., enterovirus D68 (EV-D68) infection, enterovirus A71 (EV-A71) infection, and coxsackievirus B3 (CVB3) infection.

公开(公告)号：US11866407B2

公开(公告)日：2024-01-09

申请号：US17724125

申请日：2022-04-19

Applicant: Arizona Board of Regents on Behalf of the University of Arizona

Inventor： Jun Wang

IPC: C07D207/273 ,  C07D207/46 ,  A61K31/16 ,  A61P11/00 ,  A61K9/00 ,  C07D209/02 ,  A61P31/14

CPC classification number: C07D207/273 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0053 ,  A61K31/16 ,  A61P11/00 ,  A61P31/14 ,  C07D207/46 ,  C07D209/02

Abstract: This invention is in the field of medicinal chemistry and relates to a new class of small-molecules having a pyrrolidinone-acetamide (or similar) structure (e.g.,




Formula I) which function as inhibitors of the SARS-CoV-2 papain-like protease (PLpro), which function as inhibitors of the SARS-CoV-2 related viral 3CL protease (MPpro), which function as therapeutics for the treatment of viral infection characterized with PLPpro and/or Mpro protease activity and/or expression (e.g., COVID-19), and which function as therapeutics for the treatment of other conditions characterized with PLPpro and/or Mpro protease activity and/or expression.

公开(公告)号：US20230365544A1

公开(公告)日：2023-11-16

申请号：US18069030

申请日：2022-12-20

Applicant: Arizona Board of Regents on Behalf of the University of Arizona

Inventor： Jun Wang ,  Rajesh Khanna

IPC: C07D409/14 ,  C07D405/12 ,  C07D409/06 ,  C07D401/12 ,  C07D401/14 ,  A61K45/06

CPC classification number: C07D409/14 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/06

Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a piperazine or piperidine structure which function as either inhibitors of pan-T-type calcium channel activity (e.g., CaV3.1 voltage gated calcium channel activity) (e.g., CaV3.2 voltage gated calcium channel activity) (e.g., CaV3.3 voltage gated calcium channel activity) (e.g., depolarization-induced calcium influx) or specific inhibitors of CaV3.2 voltage gated calcium channel activity, and their use as therapeutics for the treatment and/or prevention of pan-T-type calcium channel related pain (e.g., CaV3.1 related pain) (e.g., CaV3.2 related pain) (e.g., CaV3.3 related pain) (e.g., HIV-associated peripheral sensory neuropathy, chemotherapy-induced peripheral neuropathy (CIPN), spinal nerve ligation (SNL) induced neuropathy) (e.g., tonic, neuropathic, and/or inflammatory pain) and related conditions.

公开(公告)号：US20210244721A1

公开(公告)日：2021-08-12

申请号：US17162670

申请日：2021-01-29

Applicant: Arizona Board of Regents on Behalf of the University of Arizona

Inventor： Jun Wang ,  Rami Ghassan Musharrafieh ,  Chunlong Ma ,  Jiantao Zhang ,  Yanmei Hu

IPC: A61K31/47 ,  A61P31/14 ,  A61K31/4709 ,  A61K31/4748 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/496

Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a quinoline (or similar) structure which function as antagonists of androgen receptor activity, and their use as therapeutics for the treatment of cancer (e.g., castration-resistant prostate cancer) and other conditions characterized with androgen receptor activity and/or androgen receptor expression.

公开(公告)号：US20240083885A1

公开(公告)日：2024-03-14

申请号：US18265335

申请日：2021-11-29

Applicant: Arizona Board of Regents on Behalf of the University of Arizona

Inventor： Jun Wang ,  Naoya Kitamura ,  Chunlong Ma

IPC: C07D405/12 ,  A61K31/4706 ,  A61K31/573 ,  A61K31/706 ,  A61K45/06 ,  C07D401/12 ,  C07D405/14 ,  C07D413/12

CPC classification number: C07D405/12 ,  A61K31/4706 ,  A61K31/573 ,  A61K31/706 ,  A61K45/06 ,  C07D401/12 ,  C07D405/14 ,  C07D413/12

Abstract: This invention is in the field of medicinal chemistry and relates to a new class of small-molecules having a methyl-acetamido-propanamide structure (e.g., Formula I) which function as inhibitors of the SARS-CoV-2 main protease (Mpro), which function as therapeutics for the treatment of viral infection characterized with Mpro protease activity and/or expression (e.g., COVID-19), and which function as therapeutics for the treatment of other conditions characterized with Mpro protease activity and/or expression.

公开(公告)号：US11834451B2

公开(公告)日：2023-12-05

申请号：US17705984

申请日：2022-03-28

Applicant: Arizona Board of Regents on Behalf of the University of Arizona

Inventor： Jun Wang ,  Naoya Kitamura

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: This invention is in the field of medicinal chemistry and relates to a new class of small-molecules having a pyrazolopyridine (or similar) structure (e.g.,




Formula I) which function as inhibitors of the viral protein 2C protein activity and/or expression, and which function as therapeutics for the treatment of viral infection characterized with viral protein 2C activity and/or expression (e.g., non-polio enterovirus infection) (e.g., enterovirus D68 (EV-D68) infection, enterovirus A71 (EV-A71) infection, and coxsackievirus B3 (CVB3) infection.