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：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：US20150150980A1

公开(公告)日：2015-06-04

申请号：US14622660

申请日：2015-02-13

Applicant: MannKind Corporation ,  Torrey Pines Institute for Molecular Studies

Inventor： Andrea Leone-Bay ,  Richard A. Houghten ,  Joseph J. Guarneri ,  Grayson W. Stowell

IPC: A61K47/22 ,  C07K7/06 ,  A61K9/00 ,  C07K5/107

CPC classification number: A61K38/08 ,  A61K9/0075 ,  A61K9/14 ,  A61K31/198 ,  A61K31/401 ,  A61K31/405 ,  A61K31/495 ,  A61K38/04 ,  A61K38/07 ,  A61K47/22 ,  C07K5/10 ,  C07K5/1016 ,  C07K7/06 ,  A61K2300/00

Abstract: Methods and compositions for treating pain are disclosed. The compositions are based on dry powders comprising microparticles of diketopiperazines and an analgesic active agent. The analgesic in the compositions comprises one or more peptide analgesics or derivatives thereof, which are administered to a subject using a pulmonary inhalation drug delivery system comprising a dry powder inhaler and the analgesic composition. The present compositions produce fewer side effects associated with current opioid therapy.

Abstract translation: 公开了治疗疼痛的方法和组合物。 所述组合物基于包含二酮哌嗪的微粒和止痛活性剂的干燥粉末。 组合物中的镇痛剂包含一种或多种肽止痛剂或其衍生物，其使用包含干粉吸入器和镇痛组合物的肺吸入药物递送系统施用于受试者。 本发明组合物产生与当前阿片样物质治疗相关的较少副作用。

公开(公告)号：US11352370B2

公开(公告)日：2022-06-07

申请号：US16927517

申请日：2020-07-13

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: C07D221/16 ,  C07D401/04 ,  C07D401/14 ,  A61K31/429 ,  A61P35/00 ,  C07D513/04

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：US20210115063A1

公开(公告)日：2021-04-22

申请号：US16927517

申请日：2020-07-13

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 ,  A61K31/429 ,  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：US10899793B2

公开(公告)日：2021-01-26

申请号：US15605213

申请日：2017-05-25

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

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

IPC: C07K5/10 ,  A61K38/00 ,  A61K38/07 ,  C07K14/575

Abstract: Certain embodiments of the invention provide a compound of formula (I): R1—C(═O)—W—X—Y—Z—N(R2)2  (I) or a salt thereof, wherein R1, R2, W, X, Y and Z are as defined herein, as well as methods of use thereof.

公开(公告)号：US10711014B2

公开(公告)日：2020-07-14

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: A61K31/429 ,  A61K35/00 ,  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：US10421764B2

公开(公告)日：2019-09-24

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: C07D221/16 ,  C07D401/04 ,  C07D401/14 ,  C07D513/04 ,  A61K31/429 ,  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：US09610351B2

公开(公告)日：2017-04-04

申请号：US14622660

申请日：2015-02-13

Applicant: MannKind Corporation ,  Torrey Pines Institute for Molecular Studies

Inventor： Andrea Leone-Bay ,  Richard A. Houghten ,  Joseph J. Guarneri ,  Grayson W. Stowell

IPC: A61K38/07 ,  A61K38/08 ,  A61K9/14 ,  C07K5/10 ,  C07K7/06 ,  A61K47/22 ,  A61K38/04 ,  A61K9/00 ,  A61K31/495 ,  A61K31/198 ,  A61K31/401 ,  A61K31/405 ,  C07K5/107

CPC classification number: A61K38/08 ,  A61K9/0075 ,  A61K9/14 ,  A61K31/198 ,  A61K31/401 ,  A61K31/405 ,  A61K31/495 ,  A61K38/04 ,  A61K38/07 ,  A61K47/22 ,  C07K5/10 ,  C07K5/1016 ,  C07K7/06 ,  A61K2300/00

Abstract: Methods and compositions for treating pain are disclosed. The compositions are based on dry powders comprising microparticles of diketopiperazines and an analgesic active agent. The analgesic in the compositions comprises one or more peptide analgesics or derivatives thereof, which are administered to a subject using a pulmonary inhalation drug delivery system comprising a dry powder inhaler and the analgesic composition. The present compositions produce fewer side effects associated with current opioid therapy.