公开(公告)号：US09546144B2

公开(公告)日：2017-01-17

申请号：US14880862

申请日：2015-10-12

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

发明人： Peter Wipf ,  Joel S. Greenberger ,  Michael W. Epperly ,  Melissa M. Sprachman ,  Julie Pamela Goff

IPC分类号： A61K38/06 ,  A61K38/07 ,  C07D305/06 ,  C07D405/14 ,  C07D405/12 ,  C07K5/087 ,  C07K5/065 ,  C07D205/04 ,  C07K5/097

CPC分类号： C07D305/06 ,  C07D205/04 ,  C07D405/12 ,  C07D405/14 ,  C07K5/06078 ,  C07K5/0812 ,  C07K5/0823

摘要： A compound having the formula: wherein X is S, SO or SO2; one of R1, R2, and R3 is O and the others of R1, R2 and R3 are independently, the same or different, CH2, or CR13 wherein, R13 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)mOR15, wherein R15 is an alkyl group or an aryl group and m is an integer in the range of 1 to 10, and one of R5, R6, and R7 is O and the others of R5, R6 and R7 are independently, the same or different, CH2, or CR14 wherein, R14 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)nOR16, wherein R16 is an alkyl group or an aryl group and n is an integer in the range of 1 to 10; R4 and R8 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group, a C1-C3 alkoxy group, an aryloxy group, or —(CH2)qOR17, wherein R17 is an alkyl group or an aryl group and q is an integer in the range of 1 to 10, provided that R4 is not a C1-C3 alkoxy group or an aryloxy group when R1 or R3 is O and R8 is not a C1-C3 alkoxy group or an aryloxy group when R5 or R7 is O; R9, R10, R11 and R12 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, or an aryl group.

摘要翻译： 具有下式的化合物：其中X是S，SO或SO 2; R 1，R 2和R 3中的一个为O，R 1，R 2和R 3中的一个独立地为相同或不同的CH 2或CR 13，其中R 13为烷基，烯基，炔基，三烷基甲硅烷基 或 - （CH 2）m OR 15，其中R 15是烷基或芳基，m是1至10的整数，R 5，R 6和R 7中的一个是O，而其中R 5，R 6和 R7独立地相同或不同，CH2或CR14，其中R14是烷基，烯基，炔基，三烷基甲硅烷基或 - （CH2）nOR16，其中R16是烷基或芳基 n为1〜10的整数， R4和R8独立地相同或不同，为氢，烷基，烯基，炔基，芳基，杂芳基，C1-C3烷氧基，芳氧基或 - （CH2）qOR17 其中R 17为烷基或芳基，q为1〜10的整数，条件是当R 1或R 3为O时，R 4不为C 1 -C 3烷氧基或芳氧基，且R 8不为 当R 5或R 7为O时，C 1 -C 3烷氧基或芳氧基; R 9，R 10，R 11和R 12独立地为相同或不同的H，烷基，烯基，炔基或芳基。

公开(公告)号：US20190210969A1

公开(公告)日：2019-07-11

申请号：US16240595

申请日：2019-01-04

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

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

IPC分类号： C07D211/94 ,  C07K5/087 ,  C07F9/22 ,  A61K31/13 ,  C07D207/46 ,  A61K31/445 ,  C07D471/08

CPC分类号： C07D211/94 ,  A61K31/13 ,  A61K31/445 ,  C07D207/46 ,  C07D471/08 ,  C07F9/22 ,  C07K5/0812

摘要： Provided herein are compositions and related methods useful for prevention or mitigation of ionizing radiation-induced esophagitis. The compositions comprise compounds comprising a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent or mitigate esophageal damage caused by radiation.

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.

公开(公告)号：US09200035B2

公开(公告)日：2015-12-01

申请号：US14352891

申请日：2012-10-19

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

发明人： Peter Wipf ,  Joel S. Greenberger ,  Michael W. Epperly ,  Melissa M. Sprachman ,  Julie Pamela Goff

IPC分类号： A61K38/06 ,  A61K38/07 ,  C07K5/087 ,  C07D405/14 ,  C07D405/12 ,  C07D305/06 ,  C07K5/065 ,  C07D205/04

CPC分类号： C07D305/06 ,  C07D205/04 ,  C07D405/12 ,  C07D405/14 ,  C07K5/06078 ,  C07K5/0812 ,  C07K5/0823

摘要： A compound having the formula: wherein X is S, SO or SO2; one of R1, R2, and R3 is O and the others of R1, R2 and R3 are independently, the same or different, CH2, or CR13 wherein, R13 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)mOR15, wherein R15 is an alkyl group or an aryl group and m is an integer in the range of 1 to 10, and one of R5, R6, and R7 is O and the others of R5, R6 and R7 are independently, the same or different, CH2, or CR14 wherein, R14 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)nOR16, wherein R16 is an alkyl group or an aryl group and n is an integer in the range of 1 to 10; R4 and R8 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group, a C1-C3 alkoxy group, an aryloxy group, or —(CH2)qOR17, wherein R17 is an alkyl group or an aryl group and q is an integer in the range of 1 to 10, provided that R4 is not a C1-C3 alkoxy group or an aryloxy group when R1 or R3 is O and R8 is not a C1-C3 alkoxy group or an aryloxy group when R5 or R7 is O; R9, R10, R11 and R12 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, or an aryl group.

摘要翻译： 具有下式的化合物：其中X是S，SO或SO 2; R 1，R 2和R 3中的一个为O，R 1，R 2和R 3中的一个独立地为相同或不同的CH 2或CR 13，其中R 13为烷基，烯基，炔基，三烷基甲硅烷基 或 - （CH 2）m OR 15，其中R 15是烷基或芳基，m是1至10的整数，R 5，R 6和R 7中的一个是O，而其中R 5，R 6和 R7独立地相同或不同，CH2或CR14，其中R14是烷基，烯基，炔基，三烷基甲硅烷基或 - （CH2）nOR16，其中R16是烷基或芳基 n为1〜10的整数， R4和R8独立地相同或不同，为氢，烷基，烯基，炔基，芳基，杂芳基，C1-C3烷氧基，芳氧基或 - （CH2）qOR17 其中R 17为烷基或芳基，q为1〜10的整数，条件是当R 1或R 3为O时，R 4不为C 1 -C 3烷氧基或芳氧基，且R 8不为 当R 5或R 7为O时，C 1 -C 3烷氧基或芳氧基; R 9，R 10，R 11和R 12独立地为相同或不同的H，烷基，烯基，炔基或芳基。

公开(公告)号：US20160176836A1

公开(公告)日：2016-06-23

申请号：US14880862

申请日：2015-10-12

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

发明人： Peter Wipf ,  Joel S. Greenberger ,  Michael W. Epperly ,  Melissa M. Sprachman ,  Julie Pamela Goff

IPC分类号： C07D305/06 ,  C07K5/097 ,  C07D405/12

CPC分类号： C07D305/06 ,  C07D205/04 ,  C07D405/12 ,  C07D405/14 ,  C07K5/06078 ,  C07K5/0812 ,  C07K5/0823

摘要： A compound having the formula: wherein X is S, SO or SO2; one of R1, R2, and R3 is O and the others of R1, R2 and R3 are independently, the same or different, CH2, or CR13 wherein, R13 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)mOR15, wherein R15 is an alkyl group or an aryl group and m is an integer in the range of 1 to 10, and one of R5, R6, and R7 is O and the others of R5, R6 and R7 are independently, the same or different, CH2, or CR14 wherein, R14 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)nOR16, wherein R16 is an alkyl group or an aryl group and n is an integer in the range of 1 to 10; R4 and R8 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group, a C1-C3 alkoxy group, an aryloxy group, or —(CH2)qOR17, wherein R17 is an alkyl group or an aryl group and q is an integer in the range of 1 to 10, provided that R4 is not a C1-C3 alkoxy group or an aryloxy group when R1 or R3 is O and R8 is not a C1-C3 alkoxy group or an aryloxy group when R5 or R7 is O; R9, R10, R11 and R12 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, or an aryl group.

摘要翻译： 具有下式的化合物：其中X是S，SO或SO 2; R 1，R 2和R 3中的一个为O，R 1，R 2和R 3中的一个独立地为相同或不同的CH 2或CR 13，其中R 13为烷基，烯基，炔基，三烷基甲硅烷基 或 - （CH 2）m OR 15，其中R 15是烷基或芳基，m是1至10的整数，R 5，R 6和R 7中的一个是O，而其中R 5，R 6和 R7独立地相同或不同，CH2或CR14，其中R14是烷基，烯基，炔基，三烷基甲硅烷基或 - （CH2）nOR16，其中R16是烷基或芳基 n为1〜10的整数， R4和R8独立地相同或不同，为氢，烷基，烯基，炔基，芳基，杂芳基，C1-C3烷氧基，芳氧基或 - （CH2）qOR17 其中R 17为烷基或芳基，q为1〜10的整数，条件是当R 1或R 3为O时，R 4不为C 1 -C 3烷氧基或芳氧基，且R 8不为 当R 5或R 7为O时，C 1 -C 3烷氧基或芳氧基; R 9，R 10，R 11和R 12独立地为相同或不同的H，烷基，烯基，炔基或芳基。

公开(公告)号：US09365597B2

公开(公告)日：2016-06-14

申请号：US13675208

申请日：2012-11-13

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

发明人： Jeffrey Atkinson ,  Jeffrey Stuart ,  Valarian E. Kagan ,  Detcho A. Stoyanovsky ,  Michael W. Epperly ,  Joel S. Greenberger ,  Hülya Bayîr

IPC分类号： C07F9/6506 ,  C07D233/64 ,  C07D233/60

CPC分类号： C07F9/6506 ,  C07D233/60 ,  C07D233/64

摘要： The present application is directed to novel imidazole-substituted fatty acids that have been functionalized with an alkyl triphenylphosphonium group, compositions comprising these compounds and their use as inhibitors of cytochrome c peroxidase, in particular for the treatment and prevention of apoptosis.

摘要翻译： 本申请涉及已经用烷基三苯基鏻基团官能化的新型咪唑取代的脂肪酸，包含这些化合物的组合物及其作为细胞色素c过氧化物酶抑制剂的用途，特别是用于治疗和预防凋亡。

公开(公告)号：US10251860B2

公开(公告)日：2019-04-09

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： A61P19/00 ,  A61P19/10 ,  A61K31/337 ,  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.

公开(公告)号：US20140256654A1

公开(公告)日：2014-09-11

申请号：US14352891

申请日：2012-10-19

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

发明人： Peter Wipf ,  Joel S. Greenberger ,  Michael W. Epperly ,  Melissa M. Sprachman ,  Julie Pamela Goff

IPC分类号： C07K5/087 ,  C07D205/04 ,  C07D405/12 ,  C07D305/06

CPC分类号： C07D305/06 ,  C07D205/04 ,  C07D405/12 ,  C07D405/14 ,  C07K5/06078 ,  C07K5/0812 ,  C07K5/0823

摘要： A compound having the formula: wherein X is S, SO or SO2; one of R1, R2, and R3 is O and the others of R1, R2 and R3 are independently, the same or different, CH2, or CR13 wherein, R13 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)mOR15, wherein R15 is an alkyl group or an aryl group and m is an integer in the range of 1 to 10, and one of R5, R6, and R7 is O and the others of R5, R6 and R7 are independently, the same or different, CH2, or CR14 wherein, R14 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)nOR16, wherein R16 is an alkyl group or an aryl group and n is an integer in the range of 1 to 10; R4 and R8 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group, a C1-C3 alkoxy group, an aryloxy group, or —(CH2)qOR17, wherein R17 is an alkyl group or an aryl group and q is an integer in the range of 1 to 10, provided that R4 is not a C1-C3 alkoxy group or an aryloxy group when R1 or R3 is O and R8 is not a C1-C3 alkoxy group or an aryloxy group when R5 or R7 is O; R9, R10, R11 and R12 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, or an aryl group.

摘要翻译： 具有下式的化合物：其中X是S，SO或SO 2; R 1，R 2和R 3中的一个为O，R 1，R 2和R 3中的一个独立地为相同或不同的CH 2或CR 13，其中R 13为烷基，烯基，炔基，三烷基甲硅烷基 或 - （CH 2）m OR 15，其中R 15是烷基或芳基，m是1至10的整数，R 5，R 6和R 7中的一个是O，而其中R 5，R 6和 R7独立地相同或不同，CH2或CR14，其中R14是烷基，烯基，炔基，三烷基甲硅烷基或 - （CH2）nOR16，其中R16是烷基或芳基 n为1〜10的整数， R4和R8独立地相同或不同，为氢，烷基，烯基，炔基，芳基，杂芳基，C1-C3烷氧基，芳氧基或 - （CH2）qOR17 其中R 17为烷基或芳基，q为1〜10的整数，条件是当R 1或R 3为O时，R 4不为C 1 -C 3烷氧基或芳氧基，且R 8不为 当R 5或R 7为O时，C 1 -C 3烷氧基或芳氧基; R 9，R 10，R 11和R 12独立地为相同或不同的H，烷基，烯基，炔基或芳基。