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公开(公告)号：US11980606B2
公开(公告)日：2024-05-14
申请号：US17094495
申请日：2020-11-10
发明人： Mohit Trikha , Nancy Levin , Ann Maclaren
IPC分类号： A61K39/00 , A61K31/407 , A61K31/495 , A61K39/395 , A61N5/10 , C07K16/22 , C07K16/28
CPC分类号： A61K31/407 , A61K31/495 , A61K39/3955 , A61K39/39558 , A61N5/10 , C07K16/22 , C07K16/2896 , A61K2039/545 , A61N2005/1098 , C07K2317/21 , C07K2317/24 , C07K2317/73 , A61K31/407 , A61K2300/00 , A61K39/3955 , A61K2300/00 , A61K31/495 , A61K2300/00
摘要： The present disclosure relates to treatment of central nervous system (CNS) cancers (e.g., malignant glioma, glioblastoma, or CNS-multiple myeloma) using marizomib. The disclosure further relates to uses of synergistic combinations of marizomib with additional therapeutic agents such as bevacizumab, daratumumab, temozolomide, pomalidomide, and radiotherapy.
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公开(公告)号：US20220235063A1
公开(公告)日：2022-07-28
申请号：US17459531
申请日：2021-08-27
发明人： Robert MANSFIELD
IPC分类号： C07D491/048 , C07D491/02 , A61P35/00
摘要： The present invention relates to polymorphic forms of marizomib (e.g., Morphic Form I). The morphic forms can be used alone and in pharmaceutical compositions for the treatment of disease.
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公开(公告)号：US20210169851A1
公开(公告)日：2021-06-10
申请号：US17094495
申请日：2020-11-10
发明人： Mohit Trikha , Nancy Levin , Ann MacLaren
IPC分类号： A61K31/407 , A61K39/395 , A61K31/495 , A61N5/10 , C07K16/22 , C07K16/28
摘要： The present disclosure relates to treatment of central nervous system (CNS) cancers (e.g., malignant glioma, glioblastoma, or CNS-multiple myeloma) using marizomib. The disclosure further relates to uses of synergistic combinations of marizomib with additional therapeutic agents such as bevacizumab, daratumumab, temozolomide, pomalidomide, and radiotherapy.
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公开(公告)号：US10894036B2
公开(公告)日：2021-01-19
申请号：US15611614
申请日：2017-06-01
发明人： Mohit Trikha , Ann MacLaren , Nancy Levin
IPC分类号： A61K31/495 , A61K31/407 , A61K39/395 , C07K16/22 , C07K16/28 , A61N5/10 , A61K39/00
摘要： The present disclosure relates to treatment of central nervous system (CNS) cancers (e.g., malignant glioma, glioblastoma, or CNS-multiple myeloma) using marizomib. The disclosure further relates to uses of synergistic combinations of marizomib with additional therapeutic agents such as bevacizumab, daratumumab, temozolomide, pomalidomide, and radiotherapy.
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公开(公告)号：US10703760B2
公开(公告)日：2020-07-07
申请号：US16325837
申请日：2017-08-18
发明人： Robert Mansfield
IPC分类号： A61K31/407 , A61P35/00 , C07D491/04 , C07D491/048 , C07D491/02
摘要： The present invention relates to polymorphic forms of marizomib (e.g., Morphic Form I). The morphic forms can be used alone and in pharmaceutical compositions for the treatment of disease.
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6.发明申请公开(公告)号：US20200085789A1
公开(公告)日：2020-03-19
申请号：US16493155
申请日：2018-03-07
发明人： Mohit TRIKHA , Nancy LEVIN , Benjamin WINOGRAD
IPC分类号： A61K31/407 , A61K31/4015 , A61N5/10 , A61P25/00 , A61P35/00 , C07K16/22 , A61N1/36
摘要： The present disclosure is related to dosage strategies for the treatment of CNS cancers with proteasome inhibitors (e.g., marizomib). For instance, the disclosure is related to strategies in which a proteasome inhibitor (e.g., marizomib) is administered at the same or higher dosage even after a subject has experienced a CNS-related adverse event.
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公开(公告)号：US10259823B2
公开(公告)日：2019-04-16
申请号：US15416758
申请日：2017-01-26
发明人： Marcus F. Boehm , Esther Martinborough , Manisha Moorjani , Junko Tamiya , Liming Huang , Adam R. Yeager , Enugurthi Brahmachary , Thomas Fowler , Andrew Novak , Premji Meghani , Michael Knaggs
IPC分类号： C07D213/24 , C07D495/04 , A61K31/506 , C07D403/12 , C07D401/04 , C07D403/04 , C07D239/26 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D271/06 , C07D231/12 , C07D233/64 , C07D243/08 , C07D403/10 , C07D413/14 , C07D417/04 , C07D471/04 , A61K31/155 , A61K31/415 , A61K31/4164 , A61K31/4245 , A61K31/4453 , A61K31/4985 , A61K31/505 , A61K31/551 , C07D237/04 , C07D401/12 , C07D403/14 , C07D413/10
摘要： Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
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公开(公告)号：US20170216392A1
公开(公告)日：2017-08-03
申请号：US15263637
申请日：2016-09-13
发明人： Marcus F. Boehm , Esther Martinborough , Manisha Moorjani , Junko Tamiya , Liming Huang , Adam R. Yeager , Enugurthi Brahmachary , Thomas Fowler , Andrew Novak , Premji Meghani , Michael Knaggs
IPC分类号： A61K38/05 , A61K31/506
CPC分类号： A61K38/05 , A61K31/155 , A61K31/4985 , A61K31/506 , A61K31/7004 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/14 , C07D409/10 , C07D409/12 , C07D409/14 , C07D471/08 , C07K5/06139 , A61K2300/00
摘要： Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36), GLP-1(9-36), and oxyntomodulin, or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, R1, R2, R3, R4, R5, n, p and q are as defined herein.
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公开(公告)号：US09700543B2
公开(公告)日：2017-07-11
申请号：US14997364
申请日：2016-01-15
发明人： Marcus F. Boehm , Esther Martinborough , Manisha Moorjani , Junko Tamiya , Liming Huang , Thomas Fowler , Andrew Novak , Premji Meghani , Enugurthi Brahmachary , Adam Richard Yeager
IPC分类号： A61K31/4245 , A61K9/00 , A61K47/20 , A61K47/26 , A61K47/40 , A61K47/48 , A61K45/06 , A61K31/155 , A61K38/26 , C07C255/57 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D309/06 , C07D309/08 , C07D311/16 , C07C271/28 , C07D215/48 , C07D217/02 , C07C275/42 , C07D317/68 , C07D231/12 , C07D333/38 , C07D233/60 , C07C311/08 , C07C311/13 , C07C311/21 , C07D235/06 , C07C311/29 , C07D235/12 , C07D235/18 , C07C311/48 , C07D239/26 , C07D239/28 , C07C317/28 , C07C317/44 , C07D239/74 , C07D413/04 , C07D239/91 , C07D413/12 , C07D241/42 , C07D241/44 , C07D417/12 , C07C323/62 , C07C229/14 , C07D249/08 , C07D257/04 , C07C233/47 , C07C233/51 , C07D261/18 , C07C233/81 , C07C233/83 , C07C235/12 , C07D263/32 , C07C235/38 , C07D263/34 , C07C235/48 , C07D263/48 , C07D263/57 , C07C237/22 , C07C237/36 , C07C237/42 , C07D271/06 , C07D271/07 , C07D271/107 , C07D207/267 , C07D277/30 , C07D209/08 , C07D277/56 , C07D277/66 , C07D279/12 , C07D211/14 , C07D211/34 , C07D211/62 , C07D295/15 , C07D295/155 , C07D295/205 , C07D213/55 , C07D213/65 , C07D307/24 , C07D307/54 , C07D307/68 , C07D307/79 , C08B37/16 , C08L5/16 , B82Y5/00 , A61K31/235 , A61K31/341 , A61K31/4406 , A61K31/4465 , A61K31/495 , A61K31/505 , A61K31/5375 , A61K31/54 , C07D295/24 , A61K31/4439 , A61K31/4725
CPC分类号： A61K31/4245 , A61K9/0019 , A61K9/0095 , A61K31/155 , A61K31/235 , A61K31/341 , A61K31/4406 , A61K31/4439 , A61K31/4465 , A61K31/4725 , A61K31/495 , A61K31/505 , A61K31/5375 , A61K31/54 , A61K38/22 , A61K38/26 , A61K45/06 , A61K47/20 , A61K47/26 , A61K47/40 , A61K47/6951 , B82Y5/00 , C07C229/14 , C07C233/47 , C07C233/51 , C07C233/81 , C07C233/83 , C07C235/12 , C07C235/38 , C07C235/48 , C07C237/22 , C07C237/36 , C07C237/42 , C07C255/57 , C07C271/28 , C07C275/42 , C07C311/08 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/48 , C07C317/28 , C07C317/44 , C07C323/62 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/267 , C07D209/08 , C07D211/14 , C07D211/34 , C07D211/62 , C07D213/55 , C07D213/65 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D215/48 , C07D217/02 , C07D231/12 , C07D233/60 , C07D235/06 , C07D235/12 , C07D235/18 , C07D239/26 , C07D239/28 , C07D239/74 , C07D239/91 , C07D241/42 , C07D241/44 , C07D249/08 , C07D257/04 , C07D261/18 , C07D263/32 , C07D263/34 , C07D263/48 , C07D263/57 , C07D271/06 , C07D271/07 , C07D271/107 , C07D277/30 , C07D277/56 , C07D277/66 , C07D279/12 , C07D295/15 , C07D295/155 , C07D295/205 , C07D295/24 , C07D307/24 , C07D307/54 , C07D307/68 , C07D307/79 , C07D309/06 , C07D309/08 , C07D311/16 , C07D317/68 , C07D333/38 , C07D413/04 , C07D413/12 , C07D417/12 , C08B37/0015 , C08L5/16 , A61K2300/00
摘要： Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP(1-42), PTH(1-34), Glucagon(1-29), GLP-2(1-33), GLP-1(7-36), GLP-1(9-36), oxyntomodulin and exendin variants.
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公开(公告)号：US20210130768A1
公开(公告)日：2021-05-06
申请号：US17006334
申请日：2020-08-28
发明人： Kin Sing LAM , Ginger TSUENG
摘要： Growth medium are disclosed for use in fermenting a marine microorganism. The medium comprise Potassium, Calcium, Strontium, Borate and Fluoride at specific concentrations. Alternatively, the growth medium comprises cobalt at specified concentrations or comprises vitamin B12 at specified concentrations. Methods of producing certain desired compound by fermentation of a marine microorganism are also disclosed.
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