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公开(公告)号：US20240360084A1
公开(公告)日：2024-10-31
申请号：US18633495
申请日：2024-04-11
发明人： Xin JIANG , Melean VISNICK , Christopher F. BENDER , Gary BOLTON , Bradley CAPRATHE , Chitase LEE , Brian KORNBERG , Patrick O'BRIEN , Martha R. HOTEMA
IPC分类号： C07D231/54 , C07D235/02 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/04 , C07D409/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/14
CPC分类号： C07D231/54 , C07D235/02 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/04 , C07D409/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/14
摘要： Disclosed herein are compounds of the formula:
as well as analogs thereof, wherein the variables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used to modulate the activity of IL-17 and RORγ. Also provided are methods of administering compounds and composition provided herein to a patient in need thereof, for example, for the treatment or prevention of diseases or disorders associated with inflammation or for autoimmune disorders.-
公开(公告)号：US12122785B2
公开(公告)日：2024-10-22
申请号：US18160479
申请日：2023-01-27
发明人： Anjali Pandey , Gregory Dietsch , Bhaskar Chaudhuri , Seetharaman Manojveer , Mahesh Thakkar , Athisayamani Jeyaraj Duraiswamy , Sukesh Kalva
IPC分类号： A61K31/4162 , C07D231/54 , C07D471/04 , C07D471/14 , C07D487/04 , C07D491/052
CPC分类号： C07D491/052 , C07D471/04 , C07D471/14 , C07D487/04
摘要： Described herein are compounds of Formula (I) that are TYK2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of TYK2 activity.
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公开(公告)号：US11999718B2
公开(公告)日：2024-06-04
申请号：US18150955
申请日：2023-01-06
发明人： Soo Jin Lee , Sung Hwan Moon , Sooho Ban , Eunsil Lee , Eun Jung Shin , Yoo-Kyung Goh
IPC分类号： C07D401/14 , A61P1/16 , A61P11/00 , A61P35/00 , A61P39/06 , C07D231/54 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D495/04
CPC分类号： C07D401/14 , A61P1/16 , A61P11/00 , A61P35/00 , A61P39/06 , C07D231/54 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D495/04
摘要： The Present invention provides a novel pyrazole derivative compound represented by Chemical formula 1, a stereoisomer thereof, a solvate thereof, an isotopic variant thereof, a tautomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.
(In the above, A, B and R, and the like are the same as defined in the description of the invention.)-
公开(公告)号：US11981662B2
公开(公告)日：2024-05-14
申请号：US17964110
申请日：2022-10-12
IPC分类号： C07D403/12 , A61K31/416 , A61K31/4192 , A61K31/454 , A61K31/5377 , A61K45/06 , A61P35/00 , A61P35/02 , C07D231/54 , C07D405/14
CPC分类号： C07D403/12 , A61K31/416 , A61K31/4192 , A61K31/454 , A61K31/5377 , A61K45/06 , A61P35/00 , A61P35/02 , C07D231/54 , C07D405/14
摘要： The inventors have used a differential nuclear staining (DNS) assay to discover compounds with cytotoxic activity against the CEM cell line that has been determined to be highly sensitive to a variety of anti-cancer compounds. Compounds were synthesized based on a pyrazole backbone structure. Several newly synthesized compounds have been tested to identify the compounds with highest activity. One compound identified is the SSK-3 compound which has been tested on cancer cell lines and determined that it induced apoptosis via phosphatidylserine membrane exposure and activation of caspase 3 in the CEM lymphoma cell line.
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公开(公告)号：US11814338B2
公开(公告)日：2023-11-14
申请号：US17457808
申请日：2021-12-06
发明人： Eric Anderson , Gary L. Bolton , Bradley Caprathe , Xin Jiang , Chitase Lee , William H. Roark , Melean Visnick
IPC分类号： C07D231/54 , C07C255/47 , C07D239/70 , C07D401/04 , C07D403/04 , C07D417/04 , C07D487/04 , C07D413/04
CPC分类号： C07C255/47 , C07D231/54 , C07D239/70 , C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04 , C07D487/04
摘要： Disclosed herein are novel antioxidant inflammation modulators, including those of the formula:
wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.-
公开(公告)号：US11613548B2
公开(公告)日：2023-03-28
申请号：US17737872
申请日：2022-05-05
发明人： Anjali Pandey , Gregory Dietsch , Bhaskar Chaudhuri , Seetharaman Manojveer , Mahesh Thakkar , Athisayamani Jeyaraj Duraiswamy , Sukesh Kalva
IPC分类号： A61K31/4162 , C07D231/54 , C07D491/052 , C07D471/04 , C07D471/14 , C07D487/04
摘要： Described herein are compounds of Formula (XVII) that are TYK2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of Using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of TYK2 activity.
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公开(公告)号：US20230065034A1
公开(公告)日：2023-03-02
申请号：US17782615
申请日：2020-12-01
发明人： Neil J. ASHWEEK , John P. WILLIAMS , Lev Alexander ZEGELMAN , Christina Marie COSTA , Scott STIRN , Shawn BRANUM , Jackie LE , John Lloyd TUCKER , Brian M. COCHRAN , David KUCERA , Donald HETTINGER , Max A. MELLMER
IPC分类号： C07D487/04 , C07D233/20 , C07D231/54 , G01N33/74 , A61P5/00
摘要： Compounds are provided herein that antagonize corticotropin-releasing factor (CRF) receptors, in particular CRF receptor 1 (CRF1), as well as related preparations, compositions and methods for treating diseases and/or disorders that would benefit from the same such as congenital adrenal hyperplasia (CAH).
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公开(公告)号：US11352367B2
公开(公告)日：2022-06-07
申请号：US17045675
申请日：2019-04-05
发明人： Curtis Harwig , Jeremy D. Pettigrew , Jennifer Cross , Jeyaprakashnarayanan Seenisamy , Mahesh Narayan Keregadde , Karthikeyan Iyanar
IPC分类号： C07D493/10 , C07D231/54 , C07D401/08 , C07D403/08 , C07D417/08 , A61P29/00
摘要： Compounds of formula (I): wherein, R1, R2, R3, R4a, R4b and R5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.
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公开(公告)号：US20210253534A1
公开(公告)日：2021-08-19
申请号：US17236596
申请日：2021-04-21
申请人： NOVARTIS AG
发明人： Donatella CHIANELLI , Runyan LI , Valentina MOLTENI , John NELSON , Jason Thomas ROLAND , Paul Vincent RUCKER , David Charles TULLY , Xiaoyang WANG , Liladhar Murlidhar WAYKOLE , Yubo ZHANG , Bo ZHOU
IPC分类号： C07D231/54 , C07D471/04 , C07D491/052 , A61K31/416 , A61K31/4162 , A61K31/4439 , A61K31/4745 , C07D471/06
摘要： The present invention relates to compounds of Formula I, a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).
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公开(公告)号：US10927115B2
公开(公告)日：2021-02-23
申请号：US16550715
申请日：2019-08-26
申请人： Duke University
IPC分类号： A61K31/404 , A61K31/416 , C07D209/04 , C07D231/56 , C07D473/34 , C07D413/12 , C07D473/24 , C07D487/04 , C07D493/10 , C07D231/54 , C07D405/14 , G01N33/569 , G01N33/574
摘要： Substituted indazoles linked to a substituted adenine with a polyethylene glycol moiety selectively bind to Hsp90. The compounds include detection moieties such as fluorophores and are useful in methods and kits for selective detection of Hsp90 in a sample.
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