公开(公告)号：US11834482B2

公开(公告)日：2023-12-05

申请号：US17518247

申请日：2021-11-03

申请人： FOG PHARMACEUTICALS, INC.

发明人： Gerard Hilinski ,  So Youn Shim ,  Matthew Reiser Patton ,  John Hanney McGee ,  Paula Cristina Ortet ,  Gregory L Verdine

IPC分类号： A61K38/03 ,  C07K4/00 ,  C07K14/47 ,  C07K7/08 ,  A61K38/00 ,  C07K16/28

CPC分类号： C07K14/4703 ,  A61K38/03 ,  C07K4/00 ,  C07K7/08 ,  A61K38/00 ,  C07K16/2818 ,  C07K16/2827

摘要： Among other things, the present disclosure provides technologies for modulating functions of beta-catenin. In some embodiments, the present disclosure provides stapled peptides that interact with beta-catenin. In some embodiments, provided stapled peptides interact with beta-catenin at an Axin-binding site of beta-catenin. In some embodiments, the present disclosure provides compounds, compositions and methods for preventing and/or treating conditions, disorders and diseases that are associated with beta-catenin.

公开(公告)号：US11712480B2

公开(公告)日：2023-08-01

申请号：US16321695

申请日：2017-07-31

申请人： PFIZER INC.

发明人： Russell George Dushin ,  Daniel P. Uccello ,  Jeremy Starr ,  Ye Che ,  Mark Flanagan ,  Jeffrey M. Casavant ,  Christopher John O'Donnell ,  Gary Frederick Filzen ,  Jennifer Young ,  Joseph A. Abramite ,  Lawrence N. Tumey ,  Ludivine Moine ,  Adam Matthew Gilbert ,  Lee R. Roberts

IPC分类号： A61K47/54 ,  A61K47/68 ,  C07K4/00 ,  C07K5/02 ,  C07K7/02 ,  A61K47/50 ,  C07K5/062

CPC分类号： A61K47/6855 ,  A61K47/50 ,  A61K47/545 ,  A61K47/6867 ,  C07K4/00 ,  C07K5/0205 ,  C07K5/06052 ,  C07K7/02

摘要： The present invention is directed to novel heteroaryl sulfone-based conjugation handles of the formula:




(wherein R1, R2, Het, D, E, X, Y, Z, m, n, p, q, r, s and t are as defined herein), methods for their preparation, their use in synthesizing antibody drug conjugates, and the resulting antibody drug conjugates made with components having heteroaryl sulfone-based conjugation handles.

公开(公告)号：US20190112333A1

公开(公告)日：2019-04-18

申请号：US16090102

申请日：2017-04-11

申请人： Arizona Board of Regents on behalf of the University of Arizona

发明人： Ruben Vardanyan ,  Victor Hruby

IPC分类号： C07K4/00

CPC分类号： C07K4/00 ,  A61K38/00 ,  C07D211/58

摘要： The present invention provides compounds that can modulate opioid receptors. Some compounds of the invention are modulators of μ- and/or δ-opioid receptors. Still other compounds of the invention are opioid receptor antagonists. Some compounds of the invention can modulate opioid receptors with a significantly less likelihood of developing addiction or abuse compared to conventional opioid ligands, such as morphine. In particular, compounds of the invention are of the formula: wherein Ar1 is H, optionally substituted aryl or optionally substituted heteroaryl; R1 is a heteroalkyl; R2 is alkyl; R3 is an oligopeptide or a moiety of the formula —R4—Y; R4 is alkylene; Y is optionally substituted heteroaryl, optionally substituted aryl or a moiety of the formula —C(═X2)—X3—R5; each of X1, X2 and X3 is independently O, NR6 or S; and each of R5 and R6 is independently H or alkyl.

公开(公告)号：US20180327351A1

公开(公告)日：2018-11-15

申请号：US15756692

申请日：2016-09-08

申请人： CEPHALON, INC.

发明人： Ralph LAUFER ,  Gregory R. OTT

IPC分类号： C07C271/22 ,  C07C229/42 ,  C07C237/20 ,  C07F9/09 ,  C07C305/12 ,  C07D263/18 ,  C07K4/00 ,  C07D223/16 ,  C07D207/09 ,  C07C233/36 ,  C07C233/05 ,  C07C311/51 ,  C07C233/47 ,  C07H13/04 ,  C07C233/54 ,  C07C271/28 ,  A61K31/198 ,  A61K31/325 ,  A61K31/196 ,  A61K31/661 ,  A61K31/255 ,  A61K31/421 ,  A61K38/03 ,  A61K31/216 ,  A61K31/24 ,  A61K31/55 ,  A61K31/40 ,  A61K31/165 ,  A61K31/18 ,  A61K31/7028

CPC分类号： C07C271/22 ,  A61K31/165 ,  A61K31/18 ,  A61K31/196 ,  A61K31/198 ,  A61K31/216 ,  A61K31/24 ,  A61K31/255 ,  A61K31/325 ,  A61K31/40 ,  A61K31/421 ,  A61K31/55 ,  A61K31/661 ,  A61K31/7028 ,  A61K38/03 ,  C07C229/42 ,  C07C233/05 ,  C07C233/36 ,  C07C233/47 ,  C07C233/51 ,  C07C233/54 ,  C07C237/20 ,  C07C271/28 ,  C07C305/12 ,  C07C311/51 ,  C07D207/08 ,  C07D207/09 ,  C07D223/12 ,  C07D223/16 ,  C07D263/18 ,  C07F9/09 ,  C07H13/04 ,  C07K4/00

摘要： The present disclosure relates to prodrugs of 7-chlorokynurenic acid. In certain embodiments, the prodrugs include those having the structure of any one of formula (I)-(VIII), wherein R1-R13, monomer 1, monomer 2, and linker are defined herein. Also provided are methods of preparing and using these prodrugs.

公开(公告)号：US20180078607A1

公开(公告)日：2018-03-22

申请号：US15707596

申请日：2017-09-18

申请人： The Regents of the University of Michigan ,  Vanderbilt University

发明人： Patrice E. Fort ,  Kevin Schey

IPC分类号： A61K38/16 ,  C07K4/00

CPC分类号： A61K38/16 ,  A61K9/0048 ,  A61K31/57 ,  C07K4/00

摘要： This invention relates to αA-crystallin protein modulating compounds (e.g., phosphomimetic peptides), compositions comprising such modulating compounds, and their use as therapeutics for the treatment and prevention of conditions involving neurodegeneration and neuroinflammation.

公开(公告)号：US20170258930A1

公开(公告)日：2017-09-14

申请号：US15506560

申请日：2015-08-27

申请人： The Regents of the University of California ,  CTX Technology Inc.

发明人： John A. Muraski ,  Samir Mitragotri ,  Sunny Kumar

IPC分类号： A61K48/00 ,  C07K4/00 ,  C07K7/04 ,  A61K38/04 ,  A61K49/00 ,  A61K47/48 ,  A61K38/16

CPC分类号： A61K38/04 ,  A61J3/04 ,  A61K47/64 ,  A61K2039/6031 ,  A61L15/44 ,  A61L17/10 ,  A61L26/0066 ,  A61L27/54 ,  A61L29/16 ,  A61L31/16 ,  A61L2300/25 ,  C07K4/00 ,  C07K7/04 ,  C07K7/08 ,  C07K19/00 ,  C07K2319/10 ,  C12N15/87 ,  C12N2810/859 ,  C08L77/00

摘要： The present disclosure provides peptides and peptide compositions, optionally in the from of a vaccine, which facilitate the delivery of an active agent or an active agent carrier wherein the compositions are capable of penetrating the stratum corneum (SC) and/or the cellular membranes of viable cells. Also provided are methods of employing the peptides and peptide compositions to deliver active agents; treat diseases or disorders; and inducing immune responses.

公开(公告)号：US09724378B2

公开(公告)日：2017-08-08

申请号：US14716275

申请日：2015-05-19

申请人： Samsung Electronics Co., Ltd.

发明人： Jae Il Lee ,  Hye Yoon Kang ,  Dongkyu Shin ,  Jung Min Kim ,  Jungmin Lee

IPC分类号： C07K4/00 ,  A61K38/03 ,  C12N9/64 ,  A61K38/48 ,  C07K16/28 ,  A61K39/395 ,  A61K38/00

CPC分类号： A61K38/03 ,  A61K38/00 ,  A61K38/482 ,  A61K39/3955 ,  C07K4/00 ,  C07K16/2863 ,  C07K2318/20 ,  C07K2319/00 ,  C07K2319/01 ,  C07K2319/035 ,  C07K2319/33 ,  C07K2319/50 ,  C07K2319/70 ,  C12N9/6467 ,  C12Y304/21079

摘要： A fusion protein including granzyme B, a cell penetrating peptide, a cleavage site, and a targeting moiety, a composition for cell membrane penetration comprising the fusion protein, and an anticancer composition comprising the fusion protein.

公开(公告)号：US09260476B2

公开(公告)日：2016-02-16

申请号：US14073069

申请日：2013-11-06

申请人： The Research Foundation for The State University of New York

发明人： Matthew David Disney

IPC分类号： C07K4/00 ,  C07K5/08 ,  C07K14/00 ,  C07K7/06 ,  C07K7/08 ,  C07K9/00 ,  G01N33/53

CPC分类号： C07K4/00 ,  C07K5/08 ,  C07K7/06 ,  C07K7/08 ,  C07K9/001 ,  C07K14/00 ,  C07K14/001 ,  C07K14/003 ,  G01N33/5308

摘要： Disclosed are RNA targeting compounds, methods for using the subject RNA targeting compounds to treat myotonic dystrophy and other diseases are also disclosed.

摘要翻译： 公开了RNA靶向化合物，还公开了使用目标RNA靶向化合物治疗强直性营养不良的其它疾病的方法。

公开(公告)号：US20160031952A1

公开(公告)日：2016-02-04

申请号：US14775272

申请日：2014-03-13

申请人： UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR COMMERCIALIZATION

发明人： Valerie DAGGETT ,  Gene HOPPING

IPC分类号： C07K14/435 ,  C07K7/08 ,  G01N33/68 ,  C07K7/06

CPC分类号： C07K14/435 ,  A61K38/00 ,  A61K38/03 ,  A61K38/10 ,  A61K38/16 ,  C07K4/00 ,  C07K7/06 ,  C07K7/08 ,  C07K14/00 ,  C07K14/4711 ,  G01N33/6893 ,  G01N33/6896 ,  G01N2800/2821 ,  G01N2800/2828 ,  G01N2800/709

摘要： Isolated polypeptides that possess an a-sheet structure are disclosed that can be used to treat or diagnose amyloid diseases.

摘要翻译： 公开了具有一片结构的分离的多肽，其可用于治疗或诊断淀粉样蛋白病。

公开(公告)号：US20140187477A1

公开(公告)日：2014-07-03

申请号：US14197016

申请日：2014-03-04

申请人： The United Sates of America, as Represented by the Secretary, Department of Health and Human Service ,  Integratech Proteomics, LLC

发明人： Tanya Sandrock ,  Robert Craigie

IPC分类号： C07K7/08

CPC分类号： C07K4/00 ,  A61K38/00 ,  A61K38/03 ,  A61K38/10 ,  A61K39/00 ,  C07K1/00 ,  C07K7/02 ,  C07K7/08 ,  C12Q1/68 ,  C12Q1/70 ,  C40B30/04 ,  G01N33/573 ,  G01N2333/15 ,  G01N2500/02

摘要： Described herein are compositions and methods for inhibiting HIV integrase activity. Also described are methods of identifying agents that inhibit HIV integrase for use in treating or preventing HIV. Also disclosed are methods of identifying agents that inhibit HIV viral mutants that are resistant to integrase inhibitors.

摘要翻译： 本文描述了用于抑制HIV整合酶活性的组合物和方法。 还描述了鉴定抑制HIV整合酶用于治疗或预防HIV的药剂的方法。 还公开了鉴定抑制对整合酶抑制剂有抗性的HIV病毒突变体的药剂的方法。