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Pyrrolidines as Main Protease Inhibitors for Treating Viral Infections, in Particular, Coronavirus Infections
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-11-15 DOI: 10.1021/acsmedchemlett.4c0055310.1021/acsmedchemlett.4c00553
Ram W. Sabnis*, 
{"title":"Pyrrolidines as Main Protease Inhibitors for Treating Viral Infections, in Particular, Coronavirus Infections","authors":"Ram W. Sabnis*,&nbsp;","doi":"10.1021/acsmedchemlett.4c0055310.1021/acsmedchemlett.4c00553","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00553https://doi.org/10.1021/acsmedchemlett.4c00553","url":null,"abstract":"<p >Provided herein are novel pyrrolidines as main protease inhibitors, pharmaceutical compositions, use of such compounds in treating viral infections, in particular, coronavirus infections, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"15 12","pages":"2097–2098 2097–2098"},"PeriodicalIF":3.5,"publicationDate":"2024-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142850304","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Heteroaryl Glutarimides and Dihydrouracils as Cereblon Ligand Scaffolds for Molecular Glue Degrader Discovery.
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-11-15 eCollection Date: 2024-12-12 DOI: 10.1021/acsmedchemlett.4c00445
Yuebiao Zhou, Star L Garrigues, Elisia Villemure, Noriko Ishisoko, Huy Q Nguyen, Nikkia K Hamidi, Rebecca Vogt, Yong Wang, Robert A Blake, Joachim Rudolph, Christian Nilewski
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引用次数: 0
Pyrrolidines as Main Protease Inhibitors for Treating Viral Infections, in Particular, Coronavirus Infections.
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-11-15 eCollection Date: 2024-12-12 DOI: 10.1021/acsmedchemlett.4c00553
Ram W Sabnis
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引用次数: 0
Heteroaryl Glutarimides and Dihydrouracils as Cereblon Ligand Scaffolds for Molecular Glue Degrader Discovery
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-11-15 DOI: 10.1021/acsmedchemlett.4c0044510.1021/acsmedchemlett.4c00445
Yuebiao Zhou*, Star L. Garrigues, Elisia Villemure, Noriko Ishisoko, Huy Q. Nguyen, Nikkia K. Hamidi, Rebecca Vogt, Yong Wang, Robert A. Blake, Joachim Rudolph and Christian Nilewski*, 
{"title":"Heteroaryl Glutarimides and Dihydrouracils as Cereblon Ligand Scaffolds for Molecular Glue Degrader Discovery","authors":"Yuebiao Zhou*,&nbsp;Star L. Garrigues,&nbsp;Elisia Villemure,&nbsp;Noriko Ishisoko,&nbsp;Huy Q. Nguyen,&nbsp;Nikkia K. Hamidi,&nbsp;Rebecca Vogt,&nbsp;Yong Wang,&nbsp;Robert A. Blake,&nbsp;Joachim Rudolph and Christian Nilewski*,&nbsp;","doi":"10.1021/acsmedchemlett.4c0044510.1021/acsmedchemlett.4c00445","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00445https://doi.org/10.1021/acsmedchemlett.4c00445","url":null,"abstract":"<p >Stabilization of cereblon (CRBN)/neosubstrate complexes with molecular glues followed by degradation of those neosubstrates is an emerging strategy in drug discovery with compelling potential to target certain proteins that were previously considered to be undruggable. In this context, the discovery of novel CRBN ligands is an important area of ongoing research that holds promise to expand the scope of proteins that can be targeted through this mode of action. Herein, we describe the synthesis and evaluation of CRBN ligands featuring heteroaryl glutarimide and dihydrouracil scaffolds. We identified a subset of heteroaryl glutarimides exhibiting potent CRBN binding and increased chemical stability in cell culture media compared with traditional immunomodulatory drugs (IMiDs). This indicates that the scaffolds described herein could become useful starting points for the discovery of novel molecular glue degraders.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"15 12","pages":"2158–2163 2158–2163"},"PeriodicalIF":3.5,"publicationDate":"2024-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142850303","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Pyrrolidinone Urea Compounds as FPR2 Agonists for Treating Atherosclerosis and Heart Failure 作为 FPR2 激动剂治疗动脉粥样硬化和心力衰竭的新型吡咯烷酮尿素化合物
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-11-14 DOI: 10.1021/acsmedchemlett.4c0053610.1021/acsmedchemlett.4c00536
Ram W. Sabnis*, 
{"title":"Novel Pyrrolidinone Urea Compounds as FPR2 Agonists for Treating Atherosclerosis and Heart Failure","authors":"Ram W. Sabnis*,&nbsp;","doi":"10.1021/acsmedchemlett.4c0053610.1021/acsmedchemlett.4c00536","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00536https://doi.org/10.1021/acsmedchemlett.4c00536","url":null,"abstract":"<p >Provided herein are novel pyrrolidinone urea compounds as FPR2 agonists, pharmaceutical compositions, use of such compounds in treating atherosclerosis and heart failure, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"15 12","pages":"2093–2094 2093–2094"},"PeriodicalIF":3.5,"publicationDate":"2024-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142843283","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Aryl Hydrocarbon Receptor Agonists for Treating Psoriasis and Atopic Dermatitis.
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-11-14 eCollection Date: 2024-12-12 DOI: 10.1021/acsmedchemlett.4c00537
Ram W Sabnis
{"title":"Novel Aryl Hydrocarbon Receptor Agonists for Treating Psoriasis and Atopic Dermatitis.","authors":"Ram W Sabnis","doi":"10.1021/acsmedchemlett.4c00537","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00537","url":null,"abstract":"<p><p>Provided herein are novel aryl hydrocarbon receptor agonists, pharmaceutical compositions, use of such compounds in treating immune-mediated diseases, in particular psoriasis and atopic dermatitis, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"15 12","pages":"2095-2096"},"PeriodicalIF":3.5,"publicationDate":"2024-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11647673/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142845284","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel GIPR Antagonists for Treating Obesity and Type 2 Diabetes Mellitus.
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-11-14 eCollection Date: 2024-12-12 DOI: 10.1021/acsmedchemlett.4c00535
Ram W Sabnis
{"title":"Novel GIPR Antagonists for Treating Obesity and Type 2 Diabetes Mellitus.","authors":"Ram W Sabnis","doi":"10.1021/acsmedchemlett.4c00535","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00535","url":null,"abstract":"<p><p>Provided herein are novel GIPR antagonists, pharmaceutical compositions, use of such compounds in treating obesity and type 2 diabetes mellitus and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"15 12","pages":"2091-2092"},"PeriodicalIF":3.5,"publicationDate":"2024-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11647710/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142845285","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Aryl Hydrocarbon Receptor Agonists for Treating Psoriasis and Atopic Dermatitis
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-11-14 DOI: 10.1021/acsmedchemlett.4c0053710.1021/acsmedchemlett.4c00537
Ram W. Sabnis*, 
{"title":"Novel Aryl Hydrocarbon Receptor Agonists for Treating Psoriasis and Atopic Dermatitis","authors":"Ram W. Sabnis*,&nbsp;","doi":"10.1021/acsmedchemlett.4c0053710.1021/acsmedchemlett.4c00537","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00537https://doi.org/10.1021/acsmedchemlett.4c00537","url":null,"abstract":"<p >Provided herein are novel aryl hydrocarbon receptor agonists, pharmaceutical compositions, use of such compounds in treating immune-mediated diseases, in particular psoriasis and atopic dermatitis, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"15 12","pages":"2095–2096 2095–2096"},"PeriodicalIF":3.5,"publicationDate":"2024-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142849900","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Pyrrolidinone Urea Compounds as FPR2 Agonists for Treating Atherosclerosis and Heart Failure.
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-11-14 eCollection Date: 2024-12-12 DOI: 10.1021/acsmedchemlett.4c00536
Ram W Sabnis
{"title":"Novel Pyrrolidinone Urea Compounds as FPR2 Agonists for Treating Atherosclerosis and Heart Failure.","authors":"Ram W Sabnis","doi":"10.1021/acsmedchemlett.4c00536","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00536","url":null,"abstract":"<p><p>Provided herein are novel pyrrolidinone urea compounds as FPR2 agonists, pharmaceutical compositions, use of such compounds in treating atherosclerosis and heart failure, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"15 12","pages":"2093-2094"},"PeriodicalIF":3.5,"publicationDate":"2024-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11647672/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142845286","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel GIPR Antagonists for Treating Obesity and Type 2 Diabetes Mellitus
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-11-14 DOI: 10.1021/acsmedchemlett.4c0053510.1021/acsmedchemlett.4c00535
Ram W. Sabnis*, 
{"title":"Novel GIPR Antagonists for Treating Obesity and Type 2 Diabetes Mellitus","authors":"Ram W. Sabnis*,&nbsp;","doi":"10.1021/acsmedchemlett.4c0053510.1021/acsmedchemlett.4c00535","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00535https://doi.org/10.1021/acsmedchemlett.4c00535","url":null,"abstract":"<p >Provided herein are novel GIPR antagonists, pharmaceutical compositions, use of such compounds in treating obesity and type 2 diabetes mellitus and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"15 12","pages":"2091–2092 2091–2092"},"PeriodicalIF":3.5,"publicationDate":"2024-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142849899","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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