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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.
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2.发明申请HIGH-AFFINITY SMALL MOLECULE FORMYLPEPTIDE RECEPTOR LIGANDS FROM SCREENING OF COMBINATORIAL MIXTURE-BASED LIBRARIES 审中-公开从组合混合型图书馆筛选出的高亲和力小分子甲基化受体配体公开(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。
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公开(公告)号：US11014876B2
公开(公告)日：2021-05-25
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 , A61K31/18 , A61K45/06
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.
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4.发明授权High-affinity small molecule formylpeptide receptor ligands from screening of combinatorial mixture-based libraries 有权高亲和力小分子甲酰肽受体配体筛选组合基于混合物的文库公开(公告)号：US09310364B1
公开(公告)日：2016-04-12
申请号：US14174564
申请日：2014-02-06
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: A61K38/00 , A61K31/17 , C07D241/08 , C40B30/02 , G01N33/566 , C07D403/14 , A61K31/496 , A61K45/06 , C07C275/28 , C07K1/04
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: 本发明提供了用于通过位置扫描反卷积来组合文库以鉴定FPR1和/或FPR2配体（例如激动剂和/或拮抗剂），优选FPR1激动剂和/或FPR2拮抗剂的高通量筛选的新方法和测定法。 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。
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公开(公告)号：US09233159B2
公开(公告)日：2016-01-12
申请号：US14354092
申请日：2012-10-24
Inventor： Andrea Leone-Bay , Richard A. Houghten , Joseph J. Guarneri , Grayson W. Stowell
IPC: A61K38/04 , A61K38/07 , A61K38/08 , A61K9/14 , C07K5/10 , C07K7/06 , A61K47/22 , 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.
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。
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Patent Agency Ranking
公开(公告)号：US20140302151A1
公开(公告)日：2014-10-09
申请号：US14354092
申请日：2012-10-24
Inventor： Andrea Leone-Bay , Richard A. Houghten , Joseph J. Guarneri , Grayson W. Stowell
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。
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公开(公告)号：US11932628B2
公开(公告)日：2024-03-19
申请号：US17567201
申请日：2022-01-03
Inventor： Carrie Haskell-Luevano , Skye Ross Doering , Marcello A. Giulianotti , Clemencia Pinilla , Radleigh G. Santos , Richard A. Houghten
IPC: C07D403/14 , A61K9/20 , A61K9/48 , A61P3/04
CPC classification number: C07D403/14 , A61K9/2013 , A61K9/2027 , A61K9/2054 , A61K9/2059 , A61K9/485 , A61K9/4858 , A61K9/4866 , A61P3/04
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：US10258664B2
公开(公告)日：2019-04-16
申请号：US15439813
申请日：2017-02-22
Inventor： Andrea Leone-Bay , Richard A. Houghten , Joseph J. Guarneri , Grayson W. Stowell
IPC: A61K38/07 , A61K38/08 , A61K9/14 , A61K38/04 , A61K9/00 , A61K31/495 , A61K31/198 , A61K31/401 , A61K31/405 , A61K47/22 , C07K5/10 , C07K7/06 , C07K5/107
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.
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公开(公告)号：US20170342107A1
公开(公告)日：2017-11-30
申请号：US15605213
申请日：2017-05-25
Inventor： Carrie Haskell-Luevano , Skye Ross Doering , Jon R. Appel , Marc A. Giulianotti , Richard A. Houghten , Clemencia Pinilla , Radleigh G. Santos
CPC classification number: C07K5/1027 , A61K38/00
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.
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公开(公告)号：US20220213068A1
公开(公告)日：2022-07-07
申请号：US17567201
申请日：2022-01-03
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.
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