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公开(公告)号：US20220378785A1
公开(公告)日：2022-12-01
申请号：US17562933
申请日：2021-12-27
IPC分类号： A61K31/505 , C07D239/48 , C07D239/42
摘要： Provided herein are formulations, processes, solid forms and methods of use relating to 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide.
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![Substituted pyrazino[2,3-b]pyrazines as mTOR kinase inhibitors](/abs-image/US/2022/04/05/US11292796B2/abs.jpg.150x150.jpg)
公开(公告)号：US11292796B2
公开(公告)日：2022-04-05
申请号：US16865512
申请日：2020-05-04
发明人： Jan Elsner , Roy L. Harris , Branden Gingsee Lee , Deborah Mortensen , Garrick K. Packard , Patrick Papa , Jason Parnes , Sophie Perrin-Ninkovic , Jennifer Riggs , John Sapienza , Graziella I. Shevlin , Lida Tehrani , Jingjing Zhao
IPC分类号： C07D487/04 , C07D498/14 , C07D241/20 , C07D471/04 , C07D471/14 , C07D487/10 , C07D487/14
摘要： Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof. Further provided herein are methods for preparing a compound of formula (I), the method comprising contacting a compound of formula (III) with a compound of the following formula: R1-Y, in a solvent, in the presence of a palladium catalyst, wherein said contacting occurs in the presence of a base, wherein R1-R4, Y, the palladium catalyst and the base are as defined herein.
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公开(公告)号：US20210114992A1
公开(公告)日：2021-04-22
申请号：US17136276
申请日：2020-12-29
发明人： Mercedes Delgado , Jan Elsner , Paul Erdman , Robert Hilgraf , Mark A. Nagy , Stephen Norris , David A. Paisner , Yoshitaka Satoh , Marianne Sloss , Jayashree Tikhe , Won Hyung Yoon
IPC分类号： C07D239/48 , A61K31/505 , C07D401/12 , C07D409/12 , C07D403/12 , C07D401/04 , C07D405/12
摘要： Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
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公开(公告)号：US10689351B2
公开(公告)日：2020-06-23
申请号：US16452691
申请日：2019-06-26
发明人： Hon-Wah Man , Mohit Atul Kothare
IPC分类号： C07D239/48 , C07B59/00
摘要： Provided herein are isotopologues of Compound A, which are enriched with isotopes such as, for example, deuterium. Pharmaceutical compositions comprising the isotope-enriched compounds, and methods of using such compounds are also provided.
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5.发明授权公开(公告)号：US10646493B2
公开(公告)日：2020-05-12
申请号：US16514749
申请日：2019-07-17
发明人： Matthew Alexander , Sogole Bahmanyar , John Frederick Boylan , Joshua Hansen , Dehua Huang , Robert Hubbard , Brandon Jeffy , Jim Leisten , Mehran Moghaddam , Raj K. Raheja , Heather Raymon , Kimberly Schwarz , Marianne Sloss , Eduardo Torres , Tam Minh Tran , Shuichan Xu , JingJing Zhao
IPC分类号： A61K31/52 , C07D473/32 , A61P35/00 , A61K31/5377
摘要： Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.
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公开(公告)号：US10391092B2
公开(公告)日：2019-08-27
申请号：US15907619
申请日：2018-02-28
发明人： Heather Raymon , Toshiya Tsuji , Rama K. Narla , Kristen Mae Hege
IPC分类号： A61K31/4985 , A61K31/501 , A61K31/5377 , A61K31/4166 , A61K31/506 , A61K45/06
摘要： Provided herein are methods for treating or preventing a cancer, comprising administering an effective amount of a Dihydropyrazino-Pyrazine Compound and an effective amount of an androgen receptor antagonist to a patient having a cancer.
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公开(公告)号：US10183019B2
公开(公告)日：2019-01-22
申请号：US15459111
申请日：2017-03-15
发明人： Heather Raymon , Kristen Mae Hege
IPC分类号： A61K31/4985 , A61K49/00 , C07D487/04 , C12Q1/6886
摘要： Provided herein are methods for treating or preventing glioblastoma multiforme (GBM) characterized by O6-methylguanine-DNA methyltransferase (MGMT) expression and/or promoter methylation status, comprising administering an effective amount of a Dihydropyrazino-Pyrazine Compound to a patient having glioblastoma multiforme (GBM) characterized by O6-methylguanine-DNA methyltransferase (MGMT) expression and/or promoter methylation status.
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公开(公告)号：US09980963B2
公开(公告)日：2018-05-29
申请号：US15299589
申请日：2016-10-21
IPC分类号： A61K31/50 , A61K31/495 , A61K31/4985 , C07D487/04 , C12Q1/68
CPC分类号： A61K31/4985 , C07D487/04 , C12Q1/6886
摘要： Provided herein are methods for treating or preventing chronic lymphocytic leukemia, comprising administering an effective amount of a Dihydropyrazino-Pyrazine Compound to a patient having chronic lymphocytic leukemia.
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![Pharmaceutical formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one](/abs-image/US/2017/11/28/US09827243B2/abs.jpg.150x150.jpg)
公开(公告)号：US09827243B2
公开(公告)日：2017-11-28
申请号：US15150577
申请日：2016-05-10
发明人： Matthew Michael Kreilein , Thomas Lee , Ying Li , Jean Xu , William Wei-Hwa Leong , Benjamin Cohen
IPC分类号： C07D487/04 , A61K31/4985 , C07D471/04 , A61K9/20 , A61K9/48
CPC分类号： A61K31/4985 , A61K9/2018 , A61K9/2054 , A61K9/4858 , C07D471/04 , C07D487/04
摘要： Provided herein are formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.
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![Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-B]pyrazin-2(1H)-one, a solid form thereof and methods of their use](/abs-image/US/2017/10/24/US09795603B2/abs.jpg.150x150.jpg)
公开(公告)号：US09795603B2
公开(公告)日：2017-10-24
申请号：US15427242
申请日：2017-02-08
发明人： Marie Georges Beauchamps , Antonio Christian Ferretti , Juan Antonio Gamboa , Kevin Klopfer , William Edward Konnecke , Matthew Michael Kreilein , Anil Menon , Amanda Nicole Miklos , John Fitzgerald Traverse
IPC分类号： A61K31/4985 , A61K9/28 , A61K9/20 , C07D487/04
CPC分类号： A61K31/4985 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K9/28 , A61K9/2866 , C07B59/00 , C07B2200/13 , C07D241/20 , C07D487/04
摘要： Provided herein are compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, solid forms, isotopologues and metabolites thereof, and methods of their use for the treatment of a disease, disorder, or condition.
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