公开(公告)号：US11111253B2

公开(公告)日：2021-09-07

申请号：US16846089

申请日：2020-04-10

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

发明人： Donna M. Huryn ,  Peter Wipf ,  Jennifer Rubin Grandis ,  Matthew G. LaPorte ,  Paul A. Johnston ,  Mark E. Schurdak ,  Raffaele Colombo

IPC分类号： C07D513/04 ,  A61P35/00

摘要： Compounds that selectivity inhibit the STAT3 pathway and not the STAT1 pathway and exhibit anti-proliferative activity are disclosed. Also disclosed are methods of treatment of cancers that are characterized by overexpression of STAT3, which are safer that other therapies.

公开(公告)号：US20200339602A1

公开(公告)日：2020-10-29

申请号：US16846089

申请日：2020-04-10

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

发明人： Donna M. Huryn ,  Peter Wipf ,  Jennifer Rubin Grandis ,  Matthew G. LaPorte ,  Paul A. Johnston ,  Mark E. Schurdak ,  Raffaele Colombo

IPC分类号： C07D513/04 ,  A61P35/00

摘要： Compounds that selectivity inhibit the STAT3 pathway and not the STAT1 pathway and exhibit anti-proliferative activity are disclosed. Also disclosed are methods of treatment of cancers that are characterized by overexpression of STAT3, which are safer that other therapies.

公开(公告)号：US20200317730A1

公开(公告)日：2020-10-08

申请号：US16689930

申请日：2019-11-20

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

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：US10752629B2

公开(公告)日：2020-08-25

申请号：US16193269

申请日：2018-11-16

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

发明人： Peter Wipf ,  Stephen D. Meriney ,  Mary Liang

IPC分类号： C07D473/16 ,  A61K31/52 ,  A61K31/495 ,  A61P21/00 ,  A61K45/06 ,  A61K31/375 ,  A61K31/53 ,  C07D487/04

摘要： Embodiments of calcium channel agonists, as well as methods of making and using the calcium channel agonists, are disclosed. The disclosed calcium channel agonists and corresponding salt forms have a structure according to general formula I: wherein each bond depicted as “” is a single bond or a double bond as needed to satisfy valence requirements; Z1, Z2, Z3, Z4, and Z5 independently are nitrogen or carbon; R1 and R3 are alkyl; R2 is alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; and R4 is alkyl or hydroxyalkyl.

公开(公告)号：US20200216410A1

公开(公告)日：2020-07-09

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

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：US20200095220A1

公开(公告)日：2020-03-26

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： C07D311/92 ,  A61K45/06 ,  A61P25/28 ,  A61P35/00 ,  C07D405/12

摘要： Compounds, compositions and methods useful for treating cancer and neurodegeneration are provided. The compounds comprise a mitochondria-targeting moiety linked to β-lapachone or a β-lapachone derivative.

公开(公告)号：US10450289B2

公开(公告)日：2019-10-22

申请号：US15580416

申请日：2016-06-08

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

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

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

摘要： Provided herein are compounds having the general formula compositions, and methods useful for treating cancer and neurodegeneration. The compounds comprise a mitochondria-targeting moiety linked to β-lapachone or a β-lapachone derivative.

公开(公告)号：US20190142893A1

公开(公告)日：2019-05-16

申请号：US16098322

申请日：2017-05-05

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

发明人： Al-Walid A. Mohsen ,  Gerard Vockley ,  Yudong Wang ,  Peter Wipf

IPC分类号： A61K38/06 ,  A61P3/00 ,  A61P9/00 ,  A61P19/00 ,  A61K31/4468

摘要： A method is provided for treating a fatty acid oxidation metabolic condition, such as an inborn error of fatty acid oxidation or oxidative phosphorylation, and/or hypoglycemia, rhabdomyolysis, or cardiomyopathy in a patient. A mitochondrial-targeted electron, radical, or ROS-scavenging agent is administered to the patient in an amount effective to treat, mitigate or prevent any fatty acid oxidation metabolic condition, such as inborn errors of fatty acid oxidation or oxidative phosphorylation, and/or hypoglycemia, rhabdomyolysis, or cardiomyopathy in a patient.

公开(公告)号：US20190100535A1

公开(公告)日：2019-04-04

申请号：US15543573

申请日：2016-01-15

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

发明人： Donna M. Huryn ,  Peter Wipf ,  Jennifer Rubin Grandis ,  Matthew G. LaPorte ,  Paul A. Johnston ,  Mark E. Schurdak ,  Raffaele Colombo

IPC分类号： C07D513/04 ,  A61P35/00

摘要： Compounds that selectivity inhibit the STAT3 pathway and not the STAT1 pathway and exhibit anti-proliferative activity are disclosed. Also disclosed are methods of treatment of cancers that are characterized by overexpression of STAT3, which are safer that other therapies.

公开(公告)号：US20190022093A1

公开(公告)日：2019-01-24

申请号：US16139950

申请日：2018-09-24

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 ,  Serene Tai ,  Keita Takubo ,  John Milligan

IPC分类号： A61K31/504 ,  A61K31/4985 ,  A61K31/497 ,  A61K31/4439 ,  A61K31/401 ,  A61K31/407 ,  A61K31/167 ,  A61K31/122 ,  A61K31/47 ,  A61K9/00 ,  A61P35/00

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, cycloalkyl, substituted cycloalkyl, 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, cycloalkenediyl, substituted cycloalkenediyl, 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, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; a, b, c, and d independently are 0 or 1.