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1.
ACS Med Chem Lett ; 15(9): 1430-1432, 2024 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-39291000

RESUMO

The rapid advancement of targeted therapeutics has significantly improved treatment precision and efficacy in oncology and metabolic disorders. This article integrates key developments in four areas: highly selective PPAR modulators for metabolic and inflammatory diseases; CRISPR-engineered T-cell receptor therapies targeting the KRAS G12D mutation in cancer; strategies to enhance antitumor immunity through glutamine metabolism modulation in the tumor microenvironment; and a novel system for analyzing coformulated biologics. These innovations highlight the integration of metabolic modulation, immune system engineering, and advanced biologic formulation, paving the way for more effective and personalized therapeutic approaches.

2.
ACS Med Chem Lett ; 15(9): 1437-1439, 2024 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-39291007

RESUMO

Recent advancements in medical research have focused on the utilization of entheogens, particularly psilocybin and its related compounds, as therapeutic agents in mitigating cognitive decline and enhancing psychological resilience in patients undergoing anesthesia and sedation. This Patent Highlight integrates findings from three patent applications, each contributing unique insights into the potential applications of these substances in medical settings. The article examines the therapeutic mechanisms, proposed treatment methods, and potential clinical outcomes, offering an overview of this innovative approach to postoperative care.

3.
ACS Med Chem Lett ; 15(9): 1443-1445, 2024 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-39291015

RESUMO

This article explores groundbreaking advancements in psychedelic research, highlighting the development of novel lysergic acid derivatives with modified LSD-like actions and innovative dosing methods based on ABCF1 gene expression for psilocybin. It also examines new strategies for treating binge eating disorder using psychedelics and techniques for neuroenhancement to enhance emotional responses. These developments offer fresh insights into the therapeutic potential of psychedelics, underscoring their significance in personalized medicine and mental health treatment. The article delves into the implications of these novel approaches, signaling a transformative phase in the application of psychedelics in clinical settings.

4.
ACS Med Chem Lett ; 15(9): 1440-1442, 2024 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-39291014

RESUMO

The landscape of therapeutic innovation is rapidly evolving, with significant advances in cancer treatment, obesity management, and the modulation of protein interactions in neurodegenerative disorders. This Patent Highlight explores the scientific breakthroughs described in four recent patents covering novel therapeutic compounds, advanced methods for identifying E3 ligase substrates, and developing new strategies for combating obesity and its related metabolic disorders. These innovations, focusing on specific molecular targets and pathways, promise more effective and personalized treatment options, addressing unmet needs in oncology, neurology, and metabolic health.

5.
ACS Med Chem Lett ; 15(9): 1446-1448, 2024 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-39291030

RESUMO

The continuous evolution of cancer therapy has driven the exploration of novel strategies to improve treatment specificity and efficacy while minimizing adverse effects. This article examines two innovative approaches that offer new directions in targeting cancer cells. The first approach focuses on developing antibodies that specifically bind to peptide/major histocompatibility complex (MHC) complexes, enhancing the precision and effectiveness of immunotherapy. The second approach introduces quinazoline compounds that target and inhibit critical tyrosine kinases in cancer progression. Together, these advancements represent promising strides in the quest to develop more effective and precise cancer therapies, offering promising new avenues for treating resistant and aggressive forms of cancer.

6.
ACS Med Chem Lett ; 15(9): 1427-1429, 2024 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-39291034

RESUMO

Recent advancements in pharmaceutical and gene therapy research have led to the development of novel compounds and delivery systems that target critical areas of unmet medical needs, including drug-resistant bacterial infections, cancer, and genetic diseases. This Patent Highlight reviews the key findings from three recent patents that describe innovations in tricyclic quinolone compounds and adeno-associated virus (AAV) vectors for gene editing. These innovations demonstrate significant progress in the treatment of antibiotic-resistant bacterial infections, BCL6-dependent cancers, and the efficient delivery of CRISPR-based gene editing tools.

7.
ACS Med Chem Lett ; 15(8): 1196-1198, 2024 Aug 08.
Artigo em Inglês | MEDLINE | ID: mdl-39140043

RESUMO

This Patent Highlight presents a detailed analysis of three novel classes of compounds designed to inhibit multiple forms of the K-Ras protein, as described in three patent applications. These patents cover macrocyclic compounds, peptidomimetics, and pyridopyrimidine inhibitors. This work explores each invention's design, mechanism of action, relevance to cancer treatment, and results from assays demonstrating the efficacy of these compounds. The findings highlight the significant potential of these compounds in inhibiting tumor growth and inducing apoptosis in cancer cells, offering promising therapeutic options for K-Ras-driven cancers.

8.
ACS Med Chem Lett ; 15(8): 1193-1195, 2024 Aug 08.
Artigo em Inglês | MEDLINE | ID: mdl-39140059

RESUMO

The inhibition of phosphoinositide 3-kinases (PI3Ks) is a promising approach in cancer therapy due to their critical role in cellular growth, proliferation, and survival. This Patent Highlight explores the mechanism of action of novel PI3K inhibitors, emphasizing their efficacy in targeting various PI3K isoforms. The work integrates neuroprotective and anti-inflammatory strategies from related patents, highlighting their potential to enhance the therapeutic profile of these inhibitors. It also considers advanced diagnostic methods for monitoring treatment efficacy and safety, underscoring the need for a comprehensive approach to cancer treatment.

9.
ACS Med Chem Lett ; 15(8): 1199-1200, 2024 Aug 08.
Artigo em Inglês | MEDLINE | ID: mdl-39140060

RESUMO

Recently, the inhibition of diacylglyceride O-acyltransferase 2 (DGAT2) has emerged as a promising strategy for managing various metabolic disorders. This article discusses the latest developments in synthesizing and applying pyrazolopyridine and triazolopyridine derivatives as DGAT2 inhibitors. These compounds have demonstrated significant efficacy in preclinical models, showing potential to treat conditions such as hepatic steatosis, nonalcoholic steatohepatitis (NASH), type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, and cardiorenal diseases. The mechanism of action, significant findings from in vitro and in vivo studies, and the potential therapeutic benefits of these novel DGAT2 inhibitors are detailed, highlighting their role in reducing triacylglycerol (TG) synthesis and improving lipid metabolism.

10.
ACS Med Chem Lett ; 15(8): 1188-1190, 2024 Aug 08.
Artigo em Inglês | MEDLINE | ID: mdl-39140056

RESUMO

Ketamine, originally developed as an anesthetic, has shown significant potential for treating depression, chronic pain, and other conditions. However, its conventional formulations often result in side effects such as hallucinations and dizziness due to rapid spikes in blood concentration. This article explores recent patents that optimize ketamine delivery and efficacy: subcutaneous injectable compositions, ketamine conjugates with various molecules, and dual-release formulations combining ketamine with aspirin. These innovations promise to improve ketamine-based treatments' pharmacokinetic profiles, therapeutic outcomes, and safety.

11.
ACS Med Chem Lett ; 15(7): 1004-1006, 2024 Jul 11.
Artigo em Inglês | MEDLINE | ID: mdl-39015280

RESUMO

Advancements in targeted protein degradation (TPD) technologies are spearheading a new era in precision oncology, offering unprecedented avenues for tackling key oncogenic drivers such as Cyclin-dependent kinase 2 (CDK2). As a pivotal regulator of the cell cycle, CDK2's aberrant activity is closely linked with cancer progression, making it a prime target for therapeutic intervention. This Patent Highlight delves into the innovative TPD strategies aimed at CDK2 degradation, illustrating their potential to disrupt cancer cell proliferation and reshape the therapeutic landscape significantly. By extending the focus to other critical proteins within cancer biology, the discussion emphasizes TPD technologies' versatility and transformative potential in delivering targeted, efficacious cancer therapies.

12.
ACS Med Chem Lett ; 15(7): 1001-1003, 2024 Jul 11.
Artigo em Inglês | MEDLINE | ID: mdl-39015281

RESUMO

This Highlight explores significant advancements in neuropharmacology and neurotechnology, emphasizing their transformative impact on treating psychological and neurological disorders. This publication covers recent patents that introduce novel tryptamine derivatives, entactogenic mindstate inducers, and psychoplastogens aimed at promoting neuronal growth. It discusses advanced brain monitoring and stimulation systems integrated with AI to optimize treatment protocols. These innovations represent substantial progress in crafting unique therapeutic approaches and diagnostic tools, heralding a new era of personalized and effective treatment strategies for complex mental health and neurological conditions.

13.
ACS Med Chem Lett ; 15(7): 998-1000, 2024 Jul 11.
Artigo em Inglês | MEDLINE | ID: mdl-39015286

RESUMO

The continuous pursuit of novel therapeutic approaches to modulate biological processes and combat diseases such as cancer has led to significant advancements in protein degradation. This Patent Highlight reviews three recent patents introducing innovative compositions and methods to enhance enzyme activity and target protein degradation. These patents present groundbreaking advancements in the development of glutarimide-containing compounds and Protein-Protein Interaction Targeted Chimeras (PPI-TACs) aimed at improving therapeutic interventions' efficacy, selectivity, and stability.

14.
ACS Med Chem Lett ; 15(7): 1007-1009, 2024 Jul 11.
Artigo em Inglês | MEDLINE | ID: mdl-39015285

RESUMO

This Highlight explores three innovative clinical frameworks from recent patents, each introducing unique neuro-pharmaceutical compounds with potential therapeutic applications in cognitive and neurological health. This paper outlines their mechanisms, therapeutic benefits, and integrated clinical trial designs to prove efficacy and safety, demonstrating how these diverse approaches converge on advancing neurological treatment paradigms.

15.
ACS Med Chem Lett ; 15(6): 758-760, 2024 Jun 13.
Artigo em Inglês | MEDLINE | ID: mdl-38894902

RESUMO

Managing chronic inflammatory diseases and cancers has traditionally faced challenges due to the complexity of disease mechanisms and the often-insufficient specificity of treatments. This Patent Highlight showcases findings from three innovative patents that propose distinct yet complementary therapeutic strategies to modulate key cellular processes involved in inflammation and cancer progression. The first strategy involves proteolysis targeting chimeras (PROTACs) for the selective degradation of IRAK4, a kinase central to inflammatory signaling, the second employs lipid-binding protein complexes to modulate systemic inflammatory responses, and the third utilizes selective inhibitors targeting pathogenic epithelial stem cells to prevent the progression of metaplasia into dysplasia and cancer. Collectively, these approaches highlight a shift toward precision medicine, offering the potential for synergistic applications in clinical settings.

16.
ACS Med Chem Lett ; 15(6): 755-757, 2024 Jun 13.
Artigo em Inglês | MEDLINE | ID: mdl-38894903

RESUMO

This Patent Highlight explores advancements in pharmacology, focusing on the novel delivery and application of psychoactive substances. It highlights the development of transdermal formulations for psychoactive alkaloids, neuroenhancement techniques to augment emotional responses, and the intravenous infusion of psilocybin or psilocin for various therapeutic purposes. Additionally, it delves into the characterization and potential uses of crystalline forms of tryptamine derivatives. These innovations signify significant progress in drug delivery systems, neurostimulation methods, and the therapeutic use of psychedelic compounds, potentially revolutionizing the treatment of psychological and neurological disorders.

17.
ACS Med Chem Lett ; 15(6): 761-762, 2024 Jun 13.
Artigo em Inglês | MEDLINE | ID: mdl-38894916

RESUMO

In cancer therapy, the modulation of tumor suppressor proteins represents a critical frontier in developing innovative treatments. A promising direction in this field is the strategic upregulation of tumor suppressor proteins, a paradigm illustrated by the development of compounds designed to enhance the activity of the p53 protein. This protein, often called the "guardian of the genome", is crucial in preventing cancer development by inducing cell cycle arrest, apoptosis, and senescence in response to DNA damage and oncogenic stress. However, p53 function is compromised in many cancers, leading to unchecked cell proliferation and tumor progression. Addressing this challenge, a novel approach focuses on manipulating the p53/MDM2 signaling pathway to restore p53's tumor-suppressive functions.

18.
ACS Med Chem Lett ; 15(6): 752-754, 2024 Jun 13.
Artigo em Inglês | MEDLINE | ID: mdl-38894914

RESUMO

The therapeutic landscape is experiencing a significant transformation with the development of strategies focused on the lysosomal degradation of extracellular targets. This innovative approach holds promise for combating many diseases by targeting and degrading pathogenic extracellular molecules. Pioneering advancements in this field introduce the concept of utilizing bifunctional compounds for the selective degradation of extracellular proteins and molecules. This Patent Highlight delves into the scientific principles, technological innovations, and therapeutic potential of these strategies, emphasizing their critical role in reshaping the future of medical treatments and highlighting their potential impact across a diverse range of disease contexts.

19.
ACS Med Chem Lett ; 15(5): 576-578, 2024 May 09.
Artigo em Inglês | MEDLINE | ID: mdl-38746879

RESUMO

Targeted protein degradation (TPD) technologies represent a groundbreaking approach in cancer therapy, focusing on the selective degradation of oncogenic proteins such as BCL6 and SMARCA2. By leveraging the ubiquitin-proteasome system, TPD offers a novel strategy that surpasses traditional therapies' limitations, targeting the core mechanisms of oncogenesis. This article explores the significant advancements in TPD, detailing innovative strategies for the degradation of essential proteins implicated in cancer, and discusses the potential of these approaches to transform cancer treatment through precision medicine and personalized therapy.

20.
ACS Med Chem Lett ; 15(5): 573-575, 2024 May 09.
Artigo em Inglês | MEDLINE | ID: mdl-38746888

RESUMO

This Patent Highlight delves into the ground-breaking impact of Proteolysis Targeting Chimeras (PROTACs) on targeted protein degradation, offering novel strategies to eliminate pathogenic proteins. By exploring the cutting-edge development of compounds targeting IRAK-4 and CDK2, this work illuminates PROTACs' role in treating immune disorders and cancer. The analysis not only highlights the specificity and potential of PROTACs in transforming disease treatment but also addresses the challenges and future directions of this technology, emphasizing its broad applicability and the promise of more effective therapeutic strategies.

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