公开(公告)号：US20160320402A1

公开(公告)日：2016-11-03

申请号：US15013102

申请日：2016-02-02

Applicant: STC.UNM ,  TORREY PINES INSTITUTE FOR MOLECULAR STUDIES

Inventor： Bruce S. Edwards ,  Larry A. Sklar ,  Clemencia Pinilla ,  Richard A. Houghten ,  Jon R. Appel ,  Marc A. Giulianotti ,  Jose Medina-Franco

IPC: G01N33/68 ,  A61K31/17 ,  A61K31/496 ,  C40B30/02 ,  G01N33/74

CPC classification number: G01N33/6845 ,  A61K31/17 ,  A61K31/496 ,  A61K38/00 ,  A61K45/06 ,  B01J2219/00585 ,  C07C275/28 ,  C07D241/08 ,  C07D403/14 ,  C07K1/047 ,  C40B30/02 ,  G01N33/74 ,  G01N2333/726 ,  A61K2300/00

Abstract: The present invention provides novel methods and assays for high-throughput screening of combinatorial libraries to identify FPR1 and/or FPR2 ligands (e.g., agonists and/or antagonists), preferably FPR1 agonists and/or FPR2 antagonists, by positional scanning deconvolution.The invention also provides novel FPR1 and FPR2 ligands (e.g, agonists and antagonists), related pharmaceutical compositions and methods of treating FPR1 and FPR2-related disorders.

Abstract translation: 本发明还提供新的FPR1和FPR2配体（例如激动剂和拮抗剂），相关的药物组合物和治疗FPR1和FPR2相关疾病的方法。

公开(公告)号：US20220213068A1

公开(公告)日：2022-07-07

申请号：US17567201

申请日：2022-01-03

Applicant: REGENTS OF THE UNIVERSITY OF MINNESOTA ,  TORREY PINES INSTITUTE FOR MOLECULAR STUDIES

Inventor： Carrie Haskell-Luevano ,  Skye Ross Doering ,  Marcello A. Giulianotti ,  Clemencia Pinilla ,  Radleigh G. Santos ,  Richard A. Houghten

IPC: C07D403/14 ,  A61P3/04 ,  A61K9/20 ,  A61K9/48

Abstract: The invention provides compounds having the general formula I: and salts thereof, wherein the variables R1, R2, R3 and R4 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

公开(公告)号：US20190367534A1

公开(公告)日：2019-12-05

申请号：US16540757

申请日：2019-08-14

Applicant: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. ,  TORREY PINES INSTITUTE FOR MOLECULAR STUDIES

Inventor： Said M. Sebti ,  Yangmei Li ,  Richard A. Houghten

IPC: C07D513/04 ,  A61P35/00

Abstract: Compositions and methods for inhibits the binding of GTP to oncogenic mutant KRas are disclosed. These compositions may be used in method to treat a subject with cancer. In particular, the compositions may be used to treat cancers involving overactive Ras signaling.

公开(公告)号：US20180297942A1

公开(公告)日：2018-10-18

申请号：US15766680

申请日：2016-11-04

Applicant: University of Florida Research Foundation, Inc. ,  Torrey Pines Institute for Molecular Studies

Inventor： Christopher R. Cogle ,  Amy M. Meacham ,  Peter P. Sayeski ,  Marcello A. Giulianotti ,  Richard A. Houghten ,  Gregory S. Welmaker

IPC: C07C311/18 ,  C07C311/05 ,  C07D279/02

Abstract: Cancer is a disease for which there remains a great unmet medical need, and therefore the discovery and development of new antineoplastic agents is critically important. The present invention relates in part to new therapeutic compounds with antineoplastic activity. Provided herein are polyamine sulfonamides such as compounds of Formula (I), or pharmaceutically acceptable salts thereof, which may be used in the treatment and/or prevention of diseases such as cancer. Also provided herein are pharmaceutical compositions and kits comprising the inventive compounds. Furthermore, the present invention provides methods of treating and/or preventing diseases (e.g., cancer) using compounds of Formula (I), or pharmaceutically acceptable salts thereof or pharmaceutical compositions thereof. Other methods provided include methods for inducing apoptosis of a cell, as well as methods for inhibiting alpha-enolase enzymatic activity in vivo and in vitro.

公开(公告)号：US10048272B2

公开(公告)日：2018-08-14

申请号：US15013102

申请日：2016-02-02

Applicant: STC.UNM ,  TORREY PINES INSTITUTE FOR MOLECULAR STUDIES

Inventor： Bruce S. Edwards ,  Larry A. Sklar ,  Clemencia Pinilla ,  Richard A. Houghten ,  Jon R. Appel ,  Marc A. Giulianotti ,  Jose Medina-Franco

IPC: A61K31/497 ,  A61K31/517 ,  A61K31/17 ,  G01N33/68 ,  C07D403/14 ,  A61K31/496 ,  A61K45/06 ,  C07C275/28 ,  C40B30/02 ,  G01N33/74 ,  A61K38/00 ,  C07D241/08 ,  C07K1/04

Abstract: The present invention provides novel methods and assays for high-throughput screening of combinatorial libraries to identify FPR1 and/or FPR2 ligands (e.g., agonists and/or antagonists), preferably FPR1 agonists and/or FPR2 antagonists, by positional scanning deconvolution.The invention also provides novel FPR1 and FPR2 ligands (e.g, agonists and antagonists), related pharmaceutical compositions and methods of treating FPR1 and FPR2-related disorders.

公开(公告)号：US20180200250A1

公开(公告)日：2018-07-19

申请号：US15744399

申请日：2016-07-13

Applicant: UNIVERSITY OF SOUTH FLORIDA ,  TORREY PINES INSTITUTE FOR MOLECULAR STUDIES

Inventor： ROBERT JOSEPH DESCHENES ,  MARCELLO ANGELO GIULIANOTTI ,  RICHARD ALLEN HOUGHTEN ,  DAVID ALLEN MITCHELL ,  LAURA DAWN HAMEL

IPC: A61K31/496 ,  A61P35/02

CPC classification number: A61K31/496 ,  A61P35/02 ,  C07D241/04

Abstract: Embodiments of the present disclosure include compositions and pharmaceutical compositions that include protein acyl transferases (PAT) inhibitors, methods of treating a condition or disease, methods of treating autopalmitoylation activity, and the like.

公开(公告)号：US09994536B2

公开(公告)日：2018-06-12

申请号：US15306824

申请日：2015-05-01

Applicant: TORREY PINES INSTITUTE FOR MOLECULAR STUDIES

Inventor： Madepalli K. Lakshmana ,  Adel Nefzi ,  Richard Houghten ,  Dmitriy Minond

IPC: C07D277/42

CPC classification number: C07D277/42 ,  C07D417/12 ,  C07D417/14

Abstract: Embodiments of the present disclosure provide for compositions including a compound, pharmaceutical compositions including the compound, methods of treatment of a disease or related condition (e.g., neurological disease on condition), methods of treatment using compositions or pharmaceutical compositions, and the like.

公开(公告)号：US09969746B2

公开(公告)日：2018-05-15

申请号：US15102066

申请日：2014-12-05

Applicant: THE UNIVERSITY OF BATH ,  THE TORREY PINES INSTITUTE FOR MOLECULAR STUDIES ,  SRI INTERNATIONAL

Inventor： John Lewis ,  Stephen Husbands ,  Lawrence Toll

IPC: C07D489/08 ,  C07D489/02

CPC classification number: C07D489/08 ,  C07D489/02

Abstract: The present invention relates to opioid compounds, especially to C14 esters and ethers of naltrexone and analogs thereof. The present invention also relates to compositions, methods and medical uses that employ such compounds. More specifically, the present invention pertains to compounds of formula: and to their use in the treatment of diseases and disorders including pain, hyperalgesia, addiction, substance abuse disorders, stress, anorexia, anxiety, depression, cough, asthma, hypertension, gastrointestinal motility disorder, water retention, cognitive disorders, and locomotor disorders.

公开(公告)号：US20180118761A1

公开(公告)日：2018-05-03

申请号：US15568931

申请日：2016-04-25

Applicant: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. ,  TORREY PINES INSTITUTE FOR MOLECULAR STUDIES

Inventor： Said M. Sebti ,  Yangmei Li ,  Richard A. Houghten

IPC: C07D513/04 ,  A61P35/00

Abstract: Compositions and methods for inhibits the binding of GTP to oncogenic mutant KRas are disclosed. These compositions may be used in method to treat a subject with cancer. In particular, the compositions may be used to treat cancers involving overactive Ras signaling.

公开(公告)号：US20160304529A1

公开(公告)日：2016-10-20

申请号：US15102066

申请日：2014-12-05

Applicant: THE UNIVERSITY OF BATH ,  THE TORREY PINES INSTITUTE FOR MOLECULAR STUDIES ,  SRI INTERNATIONAL

Inventor： John LEWIS ,  Stephen HUSBANDS ,  Lawrence TOLL

IPC: C07D489/08

CPC classification number: C07D489/08 ,  C07D489/02

Abstract: The present invention relates to opioid compounds, especially to C14 esters and ethers of naltrexone and analogues thereof. The present invention also relates to compositions, methods and medical uses that employ such compounds. More specifically, the present invention pertains to compounds of formula: and to their use in the treatment of diseases and disorders including pain, hyperalgesia, addiction, substance abuse disorders, stress, anorexia, anxiety, depression, cough, asthma, hypertension, gastrointestinal motility disorder, water retention, cognitive disorders, and locomotor disorders.

Abstract translation: 本发明涉及阿片类化合物，特别涉及纳曲酮及其类似物的C14酯和醚。 本发明还涉及使用这些化合物的组合物，方法和医疗用途。 更具体地，本发明涉及式的化合物及其在治疗疾病和病症中的用途，包括疼痛，痛觉过敏，成瘾，物质滥用障碍，压力，厌食，焦虑，抑郁，咳嗽，哮喘，高血压，胃肠蠕动 障碍，保水，认知障碍和运动障碍。