公开(公告)号：US20150218156A1

公开(公告)日：2015-08-06

申请号：US14420236

申请日：2013-08-08

Applicant: THE JOHNS HOPKINS UNIVERSITY

Inventor： Takashi Tsukamoto ,  Barbara Stauch Slusher ,  Dana V. Ferraris ,  Camilo Rojas ,  Niyada Hin ,  Bridget Duvall

IPC: C07D471/04 ,  A61K31/53 ,  C07D409/06 ,  C07D403/06 ,  A61K31/5377 ,  C07D401/06 ,  C07D253/06 ,  A61K31/198

CPC classification number: C07D471/04 ,  A61K31/198 ,  A61K31/53 ,  A61K31/5377 ,  C07D253/06 ,  C07D253/075 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06 ,  A61K2300/00

Abstract: D-amino acid oxidase (DAAO) inhibitors and methods of their use, either alone or in combination with D-serine or D-alanine, to facilitate allosteric activation of NMDA receptor-mediated neurotransmission and methods of their use as therapeutic agents for treating a subject afflicted with one or more cognitive-disorders, such as schizophrenia, including subjects suffering from negative symptoms and cognitive impairments, post-traumatic stress disorder (PTSD), or pain, are disclosed.

Abstract translation: D-氨基酸氧化酶（DAAO）抑制剂及其使用方法，单独或与D-丝氨酸或D-丙氨酸组合，以促进NMDA受体介导的神经传递的变构激活及其用作治疗剂的方法 公开了患有一种或多种认知障碍（例如精神分裂症）的受试者，包括患有负面症状和认知障碍的受试者，创伤后应激障碍（PTSD）或疼痛。

公开(公告)号：US20240115574A1

公开(公告)日：2024-04-11

申请号：US18446244

申请日：2023-08-08

Applicant: The Johns Hopkins University

Inventor： Norman Haughey ,  Barbara Slusher ,  Camilo Rojas

IPC: A61K31/519 ,  A61K31/4178 ,  A61K31/5025 ,  A61P31/18

CPC classification number: A61K31/519 ,  A61K31/4178 ,  A61K31/5025 ,  A61P31/18

Abstract: Methods for treating a Human Immunodeficiency Virus (HIV) infection comprising administering to a subject in need of treatment thereof an effective amount of a small molecule nSMase2 inhibitor.

公开(公告)号：US20130116293A1

公开(公告)日：2013-05-09

申请号：US13672102

申请日：2012-11-08

Applicant: THE JOHNS HOPKINS UNIVERSITY

Inventor： Barbara S. Slusher ,  Jesse Alt ,  Camilo Rojas ,  Takashi Tsukamoto

IPC: G01N21/64 ,  A61K31/407 ,  A61K31/423

CPC classification number: G01N21/6428 ,  A61K31/198 ,  A61K31/407 ,  A61K31/423 ,  A61K2300/00

Abstract: Described herein are high-throughput methods of monitoring D-serine levels in plasma. The assay involves the use of strong cation solid phase extraction (SPE) to isolate D-serine from plasma, followed by quantitation of D-serine using the D-amino acid oxidase-(DAAO-) catalyzed reaction. Also described are methods of screening for compounds that act as DAAO inhibitors.

Abstract translation: 本文描述了监测血浆中D-丝氨酸水平的高通量方法。 该测定包括使用强阳离子固相萃取（SPE）从血浆中分离D-丝氨酸，然后使用D-氨基酸氧化酶（DAAO））催化的反应定量D-丝氨酸。 还描述了筛选起作为DAAO抑制剂的化合物的方法。

公开(公告)号：US12195450B2

公开(公告)日：2025-01-14

申请号：US17422670

申请日：2020-01-29

Applicant: The Johns Hopkins University

Inventor： Takashi Tsukamoto ,  Niyada Hin ,  Ondrej Stepanek ,  Barbara Slusher ,  Camilo Rojas ,  Ajit G. Thomas

IPC: C07D409/04 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/4439 ,  A61P25/00 ,  A61P25/28 ,  C07D233/64 ,  C07D235/18 ,  C07D401/04 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04

Abstract: Small molecule inhibitors of neutral sphingomyelinase 2 (nSMase2) and their use for treating neurodegenerative diseases, such as, neurodegenerative diseases associated with high levels of ceramide, including, but not limited to Alzheimer's disease (AD), HIV-associated neurocognitive disorder (HAND), multiple sclerosis (MS), and amyotrophic lateral sclerosis (ALS), and, in other aspects, for treating cancer or HIV-1, are provided.

公开(公告)号：US20240002395A1

公开(公告)日：2024-01-04

申请号：US18255767

申请日：2021-11-30

Applicant: The Johns Hopkins University

Inventor： Takashi Tsukamoto ,  Barbara Slusher ,  Nlyada Hin ,  Camilo Rojas ,  Xinzhong Dong ,  Yun Guan ,  Ilyas Abdul-Quddoos Berhane

IPC: C07D495/04 ,  C07D491/048 ,  A61K45/06 ,  A61P25/00

CPC classification number: C07D495/04 ,  C07D491/048 ,  A61K45/06 ,  A61P25/00

Abstract: Positive allosteric modulators (PAMs) of Mas-related G protein-coupled receptor X1 (MRGPRX1) and their use for treating neuropathic pain is disclosed.

公开(公告)号：US11759466B2

公开(公告)日：2023-09-19

申请号：US16977309

申请日：2019-03-01

Applicant: The Johns Hopkins University

Inventor： Norman Haughey ,  Barbara Slusher ,  Camilo Rojas

IPC: A61K31/51 ,  A61P31/18 ,  A61K31/519 ,  A61K31/4178 ,  A61K31/5025

CPC classification number: A61K31/519 ,  A61K31/4178 ,  A61K31/5025 ,  A61P31/18

Abstract: Methods for treating a Human Immunodeficiency Virus (HIV) infection comprising administering to a subject in need of treatment thereof an effective amount of a small molecule nSMase2 inhibitor.

公开(公告)号：US20220119374A1

公开(公告)日：2022-04-21

申请号：US17422670

申请日：2020-01-29

Applicant: The Johns Hopkins University

Inventor： Takashi Tsukamoto ,  Niyada Hin ,  Ondrej Stepanek ,  Barbara Slusher ,  Camilo Rojas ,  Ajit G. Thomas

IPC: C07D409/04 ,  C07D233/64 ,  C07D409/14 ,  C07D405/14

Abstract: Small molecule inhibitors of neutral sphingomyelinase 2 (nSMase2) and their use for treating neurodegenerative diseases, such as, neurodegenerative diseases associated with high levels of ceramide, including, but not limited to Alzheimer's disease (AD), HIV-associated neurocognitive disorder (HAND), multiple sclerosis (MS), and amyotrophic lateral sclerosis (ALS), and, in other aspects, for treating cancer or HIV-1, are provided.

公开(公告)号：US20210000833A1

公开(公告)日：2021-01-07

申请号：US16977309

申请日：2019-03-01

Applicant: The Johns Hopkins University

Inventor： Norman Haughey ,  Barbara Slusher ,  Camilo Rojas

IPC: A61K31/519 ,  A61K31/5025 ,  A61K31/4178 ,  A61P31/18

Abstract: Methods for treating a Human Immunodeficiency Virus (HIV) infection comprising administering to a subject in need of treatment thereof an effective amount of a small molecule nSMase2 inhibitor.

公开(公告)号：US11766423B2

公开(公告)日：2023-09-26

申请号：US16977305

申请日：2019-03-01

Applicant: THE JOHNS HOPKINS UNIVERSITY ,  THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES, OFFICE OF TECHNOLOGY TRANSFER, NATIONAL INSTITUTES OF HEALTH

Inventor： Barbara Slusher ,  Camilo Rojas ,  Ajit G. Thomas ,  Norman Haughey ,  Marc Ferrer ,  Xin Hu

IPC: A61K31/4178 ,  A61P25/28

CPC classification number: A61K31/4178 ,  A61P25/28

Abstract: Methods for treating one or more diseases associated with neutral sphingomyelinase 2 (nSMase2) in a subject in need of treatment thereof, the method comprising administering to the subject a therapeutically effective amount of 2,6-dimethoxy-4-(5-phenyl-4-thiophen-2-yl-1H-imidazol-2-yl)-phenol (DPTIP) or a pharmaceutically acceptable salt thereof, are disclosed.

公开(公告)号：US11427590B2

公开(公告)日：2022-08-30

申请号：US16475433

申请日：2018-01-05

Applicant: The Johns Hopkins University ,  Institute of Organic Chemistry and Biochemistry AS CR V.V.I.

Inventor： Barbara Slusher ,  Camilo Rojas ,  Ajit G. Thomas ,  Radim Nencka ,  Michal Sala ,  Hubert Hrebabecky ,  Norman Haughey

IPC: A61P25/28 ,  A61P25/00 ,  A61P35/00 ,  C07D487/04

Abstract: Small molecule inhibitors of neutral sphingomyelinase 2 (nSMase2) and their use for treating neurodegenerative diseases, such as, neurodegenerative diseases associated with high levels of ceramide, including, but not limited to Alzheimer's disease (AD), HIV-associated neurocognitive disorder (HAND), multiple sclerosis (MS), and amyotrophic lateral sclerosis (ALS), and, in other aspects, for treating cancer, are provided.