Oteseconazole was approved by the US FDA in April 2022. It is the first approved selective and orally bioavailable CYP51 inhibitor for the treatment of patients with recurrent Vulvovaginal ...candidiasis. Herein, we describe its dosage, administration, chemical structure, physical properties, synthesis, mechanism of action, and pharmacokinetics.
Atopic dermatitis is epidermal hyperplasia, skin barrier dysfunction, and the aberrant activation of immune cells. Janus kinase (JAK) is a family of cytoplasmic nonreceptor tyrosine kinases that ...consists of four members, such as JAK1, JAK2, JAK3, and TYK2. The JAK signaling pathway plays a critical role in a wide range of autoimmune and inflammatory diseases, including atopic dermatitis. Abrocitinib is an orally bioavailable and selective JAK1 inhibitor, and it was approved in January, 2022, for the treatment of atopic dermatitis. The chemical structure and physical properties of abrocitinib, its synthesis, mechanism of action, and pharmacokinetic profile are summarized.
COVID-19 is a contagious disease. Paxlovid, a combination of Nirmatrelvir and Ritonavir, was granted emergency use authorization by the United States Food and Drug Administration (FDA) for the ...treatment of COVID-19 on December 22, 2021. These are peptidomimetic coronavirus main protease inhibitors. Nirmatrelvir is a proline derivative. The present patent describes similar proline- like compounds, their preparation, use, pharmaceutical composition, and treatment.
Myelofibrosis is one kind of bone marrow blood cancer that gives mainly bone marrow scarring. JAK families include JAK1, JAK2, JAK3, and tyrosine kinase 2 (TYK2) and they control hematopoiesis and ...immune cell function. JAK-STAT pathways have the critical roles in the pathogenesis of a variety of autoimmune and inflammatory diseases such as myelofibrosis. The 8 JAK inhibitors are approved by the US FDA for the treatment of various diseases. Abrocitinib, baricitinib, oclacitinib, ruxolitinib, tofacitinib, upadacitinib, fedratinib, and pactrinib with their IC50 values against JAK1, JAK2, JAK3, and TYK2 are included. All approved JAK inhibitors with structural similarities and dissimilarities are summarized. The development story of pacritinib and new design route to overcome intellectual property-related issues by connecting the A ring and C ring to form the macrocyclic compounds like 16 without compromising the binding modes in the hinge region are discussed. By using the powerful ring-closing metathesis (RCM), they designed and synthesized and delivered FDA approved pacritinib. In this short perspective, the chemical structure, physicochemical properties, mechanism of action, drug-interactions, adverse events, and pharmacokinetic profile of pacritinib are summarized. Detailed step by step synthesis of pacritinib is provided. Pacritinib is an orally bioavailable and isoform selective JAK-2 inhibitor for the treatment of patients with myelofibrosis. Detailed metabolism pathway with proper explanation is discussed.
This patent describes the synthesis of compounds, methods, and compositions for preventing, treating, and/or curing Covid-19, human coronavirus, and enterovirus infections. Some peptidomimetic ...compounds are very potent and could be a game changer in new treatment therapy for COVID-19.
This application describes the synthesis of new 1,4-dihydropyrido2,3-bpyrazine-2,3-dione derivatives and methods of using these compounds as KRAS covalent inhibitors. This class of compounds is ...useful for treating cancer and other diseases associated with KRAS activity.
Diaminopyrimidine compounds having the following general structure (I), compositions comprising an effective amount of a diaminopyrimidine compound, and methods for treating or preventing fibrotic ...liver disorders or other diseases associated with the JNK pathway are discussed in this patent study.
The present disclosure relates to p38α mitogen-activated protein kinase inhibitors, pharmaceutical compositions thereof, and the use of the p38α mitogen-activated protein kinase inhibitors and ...pharmaceutical compositions thereof for treating various diseases such as cancer, rheumatoid arthritis, amyotrophic lateral sclerosis, cystic fibrosis, cardiovascular disease, multiple sclerosis, inflammatory bowel disease, chronic obstructive pulmonary disease (COPD), asthma, COVID-19, acute respiratory distress syndrome (ARDS), and acute lung injury (ALI).
