公开(公告)号：US20230144767A1

公开(公告)日：2023-05-11

申请号：US18093704

申请日：2023-01-05

申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education

发明人： Peter Wipf ,  Marie-Celine Frantz

IPC分类号： C07K5/08 ,  A61K31/454 ,  C07D211/58 ,  C07D401/12 ,  A61K47/64 ,  C07D417/12 ,  C07C237/16 ,  C07D209/46 ,  C07D211/94 ,  C07D221/22 ,  C07D209/44 ,  C07D279/06 ,  C07D471/08

CPC分类号： C07K5/08 ,  A61K31/454 ,  C07D211/58 ,  C07D401/12 ,  A61K47/64 ,  C07D417/12 ,  C07C237/16 ,  C07D209/46 ,  C07D211/94 ,  C07D221/22 ,  C07D209/44 ,  C07D279/06 ,  C07D471/08

摘要： Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

公开(公告)号：US11214560B2

公开(公告)日：2022-01-04

申请号：US16612342

申请日：2018-05-10

申请人： UNIVERSITY OF PITTSBURGH—OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION

发明人： Donna M. Huryn ,  Peter Wipf ,  Matthew G. LaPorte

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  A61P35/00 ,  A61P31/18

摘要： The present technology is directed to methods of inhibiting or modulating p97 and compounds and compositions useful in such methods Diseases and conditions that can be treated with the compounds and compositions of the present technology include, but are not limited to, antibacterial infection, antiviral infection, cancer and neurodegenerative disorders susceptible to treatment by inhibition or modulation of p97.

公开(公告)号：US10968196B2

公开(公告)日：2021-04-06

申请号：US16599339

申请日：2019-10-11

申请人： University of Pittsburgh—Of the Commonwealth System of Higher Education

发明人： Peter Wipf ,  Chaemin Lim ,  Wei Qian ,  Bennett Van Houten

IPC分类号： A61K31/352 ,  C07D311/92 ,  A61K45/06 ,  A61P25/28 ,  A61P35/00 ,  C07D405/12

摘要： Compounds are provided that are useful in treating cancer and neurodegeneration. The compounds comprise a β-lapachone or β-lapachone derivative tricyclic ortho-naphthoguinone moiety linked to a mitochondria-targeting moiety, for example as defined with respect to Formula (I): or a pharmaceutically-acceptable salt thereof. Pharmaceutical compositions are provided comprising the composition. Methods of treatment of cancer and neurodegenerative disorders also are provided.

公开(公告)号：US10894782B2

公开(公告)日：2021-01-19

申请号：US16301080

申请日：2017-05-11

申请人： University of Pittsburgh—Of the Commonwealth System of Higher Education

发明人： Donna M. Huryn ,  Peter Wipf ,  Matthew G. LaPorte

IPC分类号： C07D401/04 ,  A61K31/4196 ,  A61K45/06 ,  A61K31/44 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention is directed to methods of inhibiting or modulating p97 and compounds and compositions useful in such methods. Diseases and conditions that can be treated with the compounds and compositions of the invention include, but are not limited to, cancer and neurodegenerative disorders susceptible to treatment by modulation or inhibition of p97.

公开(公告)号：US10882834B2

公开(公告)日：2021-01-05

申请号：US15023349

申请日：2014-09-18

申请人： University of Pittsburgh—of the Commonwealth System of Higher Education

发明人： Peter Wipf ,  Erin M. Skoda ,  Zhou Wang

IPC分类号： A61K31/495 ,  C07D295/185 ,  C07D295/192 ,  A61K45/06 ,  C07D295/26 ,  C07D213/70 ,  C07D333/16 ,  C07D261/08 ,  C07D317/54 ,  C07D413/12 ,  A61K31/4525 ,  A61K31/551 ,  A61K31/58 ,  A61K31/496

摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: R20—(Z)b—(Y)c—(R21)a—X—R22—R23 wherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, or NR10, wherein R10 is H or alkyl; R21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, alkatrienyl, substituted alkatrienyl; X is —C(=0)- or —S(=0)(=0)-; R22 is a moiety that includes at least one divalent amino radical; R23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; a is 0 or 1; b is 0 or 1; and c is 0 or 1; provided that if X is —C(=0)- then Y is not S.

公开(公告)号：US10751273B2

公开(公告)日：2020-08-25

申请号：US14956272

申请日：2015-12-01

申请人： University of Pittsburgh—of the Commonwealth System of Higher Education

发明人： Laura J. Niedernhofer ,  Paul D. Robbins ,  Peter Wipf

IPC分类号： A61K8/64 ,  A61K31/40 ,  A61K8/49 ,  A61Q19/08 ,  A61K31/445 ,  A61K31/454 ,  A61K31/54 ,  A61K31/541 ,  A61K31/4468 ,  A61K31/4545 ,  A61K38/06

摘要： The present invention relates to methods of inhibiting one or more signs of aging and/or degenerative disorder in a subject in need of such treatment, which comprise administering, to the subject, an effective amount of one or more of the compounds as set forth herein. “Inhibiting a sign of aging or degenerative disorder” means reducing the risk of occurrence, delaying the onset, slowing the progression, and/or reducing the severity and/or manifestation, of a sign of aging or degenerative disorder, and includes, but is not limited to, preventing the occurrence, development or progression of a sign of aging or degenerative disorder.

公开(公告)号：US10544110B2

公开(公告)日：2020-01-28

申请号：US15961475

申请日：2018-04-24

申请人： University of Pittsburgh-Of the Commonwealth System of Higher Education

发明人： Peter Wipf ,  James K. Johnson ,  Erin M. Skoda ,  Joel B. Nelson ,  Zhou Wang

IPC分类号： C07D261/08 ,  C07D451/00 ,  C07D413/12 ,  A61K31/454 ,  C07D295/185 ,  A61K31/495 ,  A61K31/496 ,  A61K31/42 ,  A61K31/46 ,  A61K31/4166 ,  A61K45/06 ,  A61K31/58

摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I: R20—(Z)b—(Y)c—(R21)a—(X)d—R22—R23 wherein R20 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, S(═O), —S(═O)(═O)—, or NR10, wherein R10 is H or alkyl; R21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl alkadienyl, substituted alkadienyl, alkatrienyl, substituted alkatrienyl; X is —C(═O)—, —S(═O)(═O)—, or —N(H)C(═O)—; R22 includes at least one divalent amino radical; R23 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; a, b, c, and d independently are 0 or 1.

公开(公告)号：US10172795B2

公开(公告)日：2019-01-08

申请号：US14651840

申请日：2013-12-12

申请人： University of Pittsburgh—Of The Commonwealth System of Higher Education

发明人： Xiang Gao ,  Song Li ,  Peter Wipf ,  Michael Wayne Epperly ,  Joel S. Greenberger

IPC分类号： A61K31/45 ,  A61K9/107 ,  A61K9/127 ,  A61K31/337 ,  A61K31/704

摘要： A method of creating a formulation for a compound includes determining a compound interactive agent comprising at least one group that interacts with the compound, creating a carrier agent by conjugating at least one compound interactive domain comprising the at least one group that interacts with the compound with at least one hydrophilic domain, and combining the compound and the carrier agent to create the formulation. Creating the carrier agent may further include conjugating the at least one compound interactive domain with at least one hydrophobic domain so that the at least one compound interactive domain is positioned between the at least one hydrophilic domain and the at least one hydrophobic domain.

公开(公告)号：US20180319778A1

公开(公告)日：2018-11-08

申请号：US15769987

申请日：2016-10-20

申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education ,  National Institute of Health, A Component of the U.S Department of Health and Human Services ,  The Regents of the University of California

发明人： Donna M. HURYN ,  Peter Wipf ,  Matthew G. LaPorte ,  Raffaele Colombo ,  Marina Kovaliov ,  Chaemin Lim ,  Celeste Natalie Alverez ,  Zhizhou Yue ,  Lalith Palitha Samankumara ,  Alexander Julian Chatterley ,  Yongzhao Yan ,  Mary Liang ,  Neal J. Green ,  Eric T. Baldwin ,  William J. Moore ,  Michelle Arkin ,  R. Jeffrey Neilz ,  Kean-Hooi Ang ,  Cliffford Bryant ,  Stacie Bulfer

IPC分类号： C07D405/14 ,  C07D401/14 ,  C07D401/10 ,  C07D413/14 ,  C07D417/14 ,  A61P25/28 ,  A61P35/00

CPC分类号： C07D405/14 ,  A61K31/404 ,  A61K31/454 ,  A61K31/496 ,  A61P25/28 ,  A61P35/00 ,  C07D401/10 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention is directed to methods of inhibiting p97 and compounds and compositions useful in such methods. Diseases and conditions the can be treated with the compounds and compositions of the invention include, but are not limited to, cancer and neurodegenerative disorders susceptible to treatment by inhibition of p97.

公开(公告)号：US20180185322A1

公开(公告)日：2018-07-05

申请号：US15906856

申请日：2018-02-27

申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education ,  The Brigham and Women's Hospital, Inc.

发明人： Michael W. Epperly ,  Joel S. Greenberger ,  Peter Wipf ,  Julianne Glowacki

IPC分类号： A61K31/337 ,  A61P19/00

CPC分类号： A61K31/337 ,  A61P19/00 ,  C07D305/06

摘要： Disclosed herein are embodiments of a method of accelerating bone healing in a subject in need thereof, comprising administering to the subject a compound disclosed here. The method may further comprise selecting or identifying a subject that has bone damage, or is a risk of developing bone damage. The compound may be administered after bone damage has occurred, or it may be administered prophylactically. The compound may be administered to a subject that has not and/or will not be exposed to radiation. In other embodiments, the subject has been and/or will be exposed to radiation.