公开(公告)号：US10538487B2

公开(公告)日：2020-01-21

申请号：US15551264

申请日：2016-02-16

申请人： THE UNIVERSITY OF QUEENSLAND ,  THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, AND THE OTHER MEMBERS OF THE BOARD OF THE COLLEGE OF THE HOLY AND UNDIVIDED TRINITY OF QUEEN ELIZABETH NEAR DUBLIN

发明人： Luke O'Neill ,  Rebecca Coll ,  Matthew Cooper ,  Avril Robertson ,  Kate Schroder

IPC分类号： C07C311/56 ,  C07D307/18 ,  C07D307/64 ,  C07D407/12 ,  C07D493/04 ,  C07D405/12 ,  C07D333/34 ,  C07D277/36 ,  C07D249/12 ,  C07D249/04 ,  C07D231/18 ,  C07D403/12 ,  C07C311/60 ,  C07D333/52 ,  C07D249/06 ,  C07D413/12 ,  C07D495/04 ,  C07D401/12 ,  C07D241/24 ,  C07D307/68 ,  C07D271/12 ,  C07D311/16 ,  C07D317/62 ,  C07D487/04 ,  C07D215/36 ,  C07D217/02 ,  C07D241/42 ,  C07D498/04 ,  C07D307/82 ,  C07D333/62 ,  C07D217/24 ,  C07D207/38 ,  C07D261/18 ,  C07D213/71 ,  C07D221/18 ,  C07D309/08 ,  A61P1/00 ,  C07D417/12 ,  C07D495/06 ,  C07D311/60 ,  A61P35/00 ,  A61P3/00 ,  C07D235/02 ,  C07D311/18 ,  A61P17/00 ,  A61P5/00 ,  C07D401/06 ,  A61P37/00 ,  A61P25/00 ,  C07D217/22 ,  C07D241/44

摘要： The present invention provides for certain sulfonyl ureas and related compounds which have advantageous properties and show useful activity in the inhibition of activation of the NLRP3 inflammasome. Such compounds are useful in the treatment of a wide range of disorders in which the inflammation process, or more specifically the NLRP3 inflammasome, have been implicated as being a key factor.

公开(公告)号：US11840543B2

公开(公告)日：2023-12-12

申请号：US16614776

申请日：2017-05-24

申请人： The University of Queensland ,  THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, AND THE OTHER MEMBERS OF BOARD, OF THE COLLEGE OF THE HOLY AND UNDIVIDED TRINITY OF QUEEN ELIZABETH NEAR DUBLIN

发明人： Luke O'Neill ,  Rebecca Coll ,  Matthew Cooper ,  Avril Robertson ,  Kate Schroder ,  Angus Murray MacLeod ,  David John Miller

IPC分类号： C07C311/60 ,  C07D495/04 ,  C07D207/38 ,  C07D217/24 ,  C07D241/24 ,  C07D249/04 ,  C07D261/18 ,  C07D271/12 ,  C07D307/68 ,  C07D413/12

CPC分类号： C07D495/04 ,  C07C311/60 ,  C07D207/38 ,  C07D217/24 ,  C07D241/24 ,  C07D249/04 ,  C07D261/18 ,  C07D271/12 ,  C07D307/68 ,  C07D413/12

摘要： The present invention relates to compounds of formula (I): wherein Q is O or S; R1 is a cyclic group substituted with at least one group X, wherein R1 may optionally be further substituted; X is any group comprising a carbonyl group; and R2 is a cyclic group substituted at the α-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the dual action of NLRP3 inhibition and the stimulation of insulin secretion.

公开(公告)号：US11845715B2

公开(公告)日：2023-12-19

申请号：US17405989

申请日：2021-08-18

申请人： THE UNIVERSITY OF QUEENSLAND ,  THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, AND THE OTHER MEMBERS OF BOARD, OF THE COLLEGE OF THE HOLY AND UNDIVIDED TRINITY OF QUEEN ELIZABETH NEAR DUBLIN

发明人： Luke O'Neill ,  Rebecca Coll ,  Matthew Cooper ,  Avril Robertson ,  Kate Schroder

IPC分类号： C07C311/56 ,  A61P17/00 ,  C07D403/12 ,  C07D249/12 ,  C07D249/04 ,  C07D241/42 ,  A61P25/00 ,  A61P37/00 ,  C07D495/04 ,  C07D241/44 ,  C07D277/36 ,  C07D307/68 ,  C07D487/04 ,  C07D215/36 ,  C07D249/06 ,  C07D311/16 ,  C07D401/06 ,  C07D401/12 ,  A61P3/00 ,  C07C311/60 ,  C07D213/71 ,  C07D217/22 ,  C07D221/18 ,  C07D317/62 ,  C07D333/34 ,  A61P1/00 ,  A61P35/00 ,  C07D217/02 ,  C07D241/24 ,  C07D271/12 ,  C07D413/12 ,  C07D417/12 ,  A61P5/00 ,  C07D307/18 ,  C07D307/64 ,  C07D311/60 ,  C07D333/52 ,  C07D333/62 ,  C07D405/12 ,  C07D495/06 ,  C07D217/24 ,  C07D235/02 ,  C07D311/18 ,  C07D407/12 ,  C07D231/18 ,  C07D307/82 ,  C07D309/08 ,  C07D493/04 ,  C07D207/38 ,  C07D261/18 ,  C07D498/04

CPC分类号： C07C311/56 ,  A61P1/00 ,  A61P3/00 ,  A61P5/00 ,  A61P17/00 ,  A61P25/00 ,  A61P35/00 ,  A61P37/00 ,  C07C311/60 ,  C07D207/38 ,  C07D213/71 ,  C07D215/36 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D221/18 ,  C07D231/18 ,  C07D235/02 ,  C07D241/24 ,  C07D241/42 ,  C07D241/44 ,  C07D249/04 ,  C07D249/06 ,  C07D249/12 ,  C07D261/18 ,  C07D271/12 ,  C07D277/36 ,  C07D307/18 ,  C07D307/64 ,  C07D307/68 ,  C07D307/82 ,  C07D309/08 ,  C07D311/16 ,  C07D311/18 ,  C07D311/60 ,  C07D317/62 ,  C07D333/34 ,  C07D333/52 ,  C07D333/62 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D493/04 ,  C07D495/04 ,  C07D495/06 ,  C07D498/04 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2603/10

摘要： The present invention provides for certain sulfonyl ureas and related compounds which have advantageous properties and show useful activity in the inhibition of activation of the NLRP3 inflammasome. Such compounds are useful in the treatment of a wide range of disorders in which the inflammation process, or more specifically the NLRP3 inflammasome, have been implicated as being a key factor.

公开(公告)号：US20220112159A1

公开(公告)日：2022-04-14

申请号：US17405989

申请日：2021-08-18

申请人： THE UNIVERSITY OF QUEENSLAND ,  THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, AND THE OTHER MEMBERS OF BOARD, OF THE COLLEGE OF THE HOL

发明人： Luke O'NEILL ,  Rebecca Coll ,  Matthew Cooper ,  Avril Robertson ,  Kate Schroder

IPC分类号： C07C311/56 ,  A61P17/00 ,  C07D403/12 ,  C07D249/12 ,  C07D249/04 ,  C07D241/42 ,  A61P25/00 ,  A61P37/00 ,  C07D495/04 ,  C07D241/44 ,  C07D277/36 ,  C07D307/68 ,  C07D487/04 ,  C07D215/36 ,  C07D249/06 ,  C07D311/16 ,  C07D401/06 ,  C07D401/12 ,  A61P3/00 ,  C07C311/60 ,  C07D207/38 ,  C07D213/71 ,  C07D217/22 ,  C07D221/18 ,  C07D317/62 ,  C07D333/34 ,  A61P1/00 ,  A61P35/00 ,  C07D217/02 ,  C07D241/24 ,  C07D271/12 ,  C07D413/12 ,  C07D417/12 ,  A61P5/00 ,  C07D261/18 ,  C07D307/18 ,  C07D307/64 ,  C07D311/60 ,  C07D333/52 ,  C07D333/62 ,  C07D405/12 ,  C07D495/06 ,  C07D217/24 ,  C07D235/02 ,  C07D311/18 ,  C07D407/12 ,  C07D231/18 ,  C07D307/82 ,  C07D309/08 ,  C07D493/04 ,  C07D498/04

摘要： The present invention provides for certain sulfonyl ureas and related compounds which have advantageous properties and show useful activity in the inhibition of activation of the NLRP3 inflammasome. Such compounds are useful in the treatment of a wide range of disorders in which the inflammation process, or more specifically the NLRP3 inflammasome, have been implicated as being a key factor.

公开(公告)号：US11279733B2

公开(公告)日：2022-03-22

申请号：US16761067

申请日：2018-11-02

申请人： THE UNIVERSITY OF QUEENSLAND

发明人： Matthew Cooper ,  Mark Blaskovich ,  Alejandra Gallardo-Godoy ,  Karl Hansford ,  Alysha Elliott ,  Craig Muldoon ,  Bernd Becker

IPC分类号： A61K38/12 ,  C07K7/56 ,  C07K7/62 ,  A61P31/04 ,  A61K38/00 ,  A61K45/06

摘要： There is provided a range of novel compounds. These novel compounds may demonstrate abroad spectrum antibacterial and antifungal activity. These compounds may be active against the emerging polymyxin resistant bacteria. These compounds may also be useful when used in conjunction with other pharmaceutically active agents.

公开(公告)号：US20170204138A1

公开(公告)日：2017-07-20

申请号：US15117704

申请日：2014-02-10

申请人： THE UNIVERSITY OF QUEENSLAND

发明人： Matthew Cooper ,  Mark Blaskovich

IPC分类号： C07K5/11

CPC分类号： C07K5/1019 ,  A61K38/00 ,  C07K5/06086 ,  C07K5/0815 ,  C07K7/06 ,  C07K9/008

摘要： The invention concerns agents with antibacterial activity, their production and use in the treatment of bacterial infections in animals, including man. The agents are derivatives of vancomycin-type antibiotics, of structure X—W-L-V, wherein X is hydrogen, acetyl or a lipophilic membrane-insertive element, W is a basic peptide or basic amino acid; L is a linking group and V is a glycopeptide moiety which inhibits peptidoglycan biosynthesis in bacteria.

公开(公告)号：US11130731B2

公开(公告)日：2021-09-28

申请号：US16535002

申请日：2019-08-07

申请人： THE UNIVERSITY OF QUEENSLAND ,  THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, AND THE OTHER MEMBERS OF BOARD, OF THE COLLEGE OF THE HOLY AND UNDIVIDED TRINITY OF QUEEN ELIZABETH NEAR DUBLIN

发明人： Luke O'Neill ,  Rebecca Coll ,  Matthew Cooper ,  Avril Robertson ,  Kate Schroder

IPC分类号： C07C311/56 ,  A61P5/00 ,  C07D403/12 ,  A61P37/00 ,  A61P35/00 ,  A61P3/00 ,  A61P25/00 ,  A61P1/00 ,  C07D215/36 ,  C07D401/12 ,  C07D487/04 ,  C07D493/04 ,  A61P17/00 ,  C07D213/71 ,  C07D309/08 ,  C07D311/18 ,  C07D311/60 ,  C07D217/22 ,  C07D217/24 ,  C07D495/04 ,  C07D217/02 ,  C07D221/18 ,  C07D241/42 ,  C07D307/68 ,  C07D311/16 ,  C07D333/52 ,  C07D307/82 ,  C07D307/64 ,  C07D307/18 ,  C07D277/36 ,  C07D498/04 ,  C07D207/38 ,  C07D495/06 ,  C07D271/12 ,  C07D261/18 ,  C07D249/12 ,  C07D249/06 ,  C07D249/04 ,  C07D417/12 ,  C07D241/44 ,  C07D317/62 ,  C07D231/18 ,  C07D333/34 ,  C07D333/62 ,  C07C311/60 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12 ,  C07D241/24 ,  C07D235/02 ,  C07D401/06

摘要： The present invention provides for certain sulfonyl ureas and related compounds which have advantageous properties and show useful activity in the inhibition of activation of the NLRP3 inflammasome. Such compounds are useful in the treatment of a wide range of disorders in which the inflammation process, or more specifically the NLRP3 inflammasome, have been implicated as being a key factor.

公开(公告)号：US10947271B2

公开(公告)日：2021-03-16

申请号：US15117704

申请日：2015-02-10

申请人： THE UNIVERSITY OF QUEENSLAND

发明人： Matthew Cooper ,  Mark Blaskovich

IPC分类号： C07K5/11 ,  C07K7/06 ,  C07K5/09 ,  C07K5/068 ,  C07K9/00 ,  A61K38/00

摘要： The invention concerns agents with antibacterial activity, their production and use in the treatment of bacterial infections in animals, including man. The agents are derivatives of vancomycin-type antibiotics, of structure X—W-L-V, wherein X is hydrogen, acetyl or a lipophilic membrane-insertive element, W is a basic peptide or basic amino acid; L is a linking group and V is a glycopeptide moiety which inhibits peptidoglycan biosynthesis in bacteria.

公开(公告)号：US11858922B2

公开(公告)日：2024-01-02

申请号：US15999424

申请日：2017-02-16

申请人： The University of Queensland ,  THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, AND THE OTHER MEMBERS OF BOARD, OF THE COLLEGE OF THE HOLY AND UNDIVIDED TRINITY OF QUEEN ELIZABETH NEAR DUBLIN

发明人： Luke O'Neill ,  Rebecca Coll ,  Matthew Cooper ,  Avril Robertson ,  Kate Schroder ,  Angus Murray Macleod ,  David John Miller

IPC分类号： C07D413/12 ,  A61K49/00 ,  C07C311/47 ,  C07D209/08 ,  C07D209/14 ,  C07D213/42 ,  C07D233/64 ,  C07D235/26 ,  C07D241/04 ,  C07D271/06 ,  C07D277/28 ,  C07D295/26 ,  C07D307/52 ,  C07D311/20 ,  C07D317/66 ,  C07D403/12 ,  C07D413/04

CPC分类号： C07D413/12 ,  A61K49/0004 ,  C07C311/47 ,  C07D209/08 ,  C07D209/14 ,  C07D213/42 ,  C07D233/64 ,  C07D235/26 ,  C07D241/04 ,  C07D271/06 ,  C07D277/28 ,  C07D295/26 ,  C07D307/52 ,  C07D311/20 ,  C07D317/66 ,  C07D403/12 ,  C07D413/04

摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, solvates and prodrugs thereof:




wherein Q is selected from O, S and Se; J is S or Se; W1 and W2, when present, are independently selected from N and C; R1 and R2 are independently selected from the group consisting of hydrogen, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, cycloalkenyl, amino, amido, alkylthio, acyl, arylalkyl and acylamido, all of which may be optionally substituted; and wherein at least one of W1 and W2 is present and is a nitrogen atom and when R1 or R2 are cyclic then the respective W1 or W2 may form part of the ring structure. The present invention also relates to pharmaceutical compositions including such compounds, to methods of treatment using such compounds, in particular in relation to NLRP3 inflammasome mediated disorders, and to associated diagnostic uses.

公开(公告)号：US20200207780A1

公开(公告)日：2020-07-02

申请号：US16614776

申请日：2017-05-24

申请人： The University of Queensland ,  THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, AND THE OTHER MEMBERS OF BOARD, OF THE COLLEGE OF THE HOL

发明人： Luke O'Neill ,  Rebecca Coll ,  Matthew Cooper ,  Avril Robertson ,  Kate Schroder ,  Angus Murray MacLeod ,  David John Miller

IPC分类号： C07D495/04 ,  C07C311/60 ,  C07D241/24 ,  C07D261/18 ,  C07D217/24 ,  C07D207/38 ,  C07D307/68 ,  C07D271/12 ,  C07D249/04 ,  C07D413/12

摘要： The present invention relates to compounds of formula (I): wherein Q is O or S; R1 is a cyclic group substituted with at least one group X, wherein R1 may optionally be further substituted; X is any group comprising a carbonyl group; and R2 is a cyclic group substituted at the α-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the dual action of NLRP3 inhibition and the stimulation of insulin secretion.