CAS: 4419-39-0; Beclomethasone

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beclomethasone 17,21-dipropionate 9β,11β-epoxy-17α,21-dihydroxy-16β-methylpregna-1,4-diene-3,20-dione 22H27ClO4C22H27ClO4 beclomethasone-11,17,21-tripropionate beclomethasone 17-monopropionate

📜丙酸倍氯米松置于potassium Hydrogencarbonate体系中,用 甲醇 作为反应溶剂,化学反应 72.0H,反应生成 倍氯米松
参考文献:Efficient Interfacially Driven Vehiculization Of Corticosteroids By Pulmonary Surfactant
标题:Efficient Interfacially Driven Vehiculization Of Corticosteroids By Pulmonary Surfactant
摘要:Pulmonary Surfactant Is A Crucial System To Stabilize The Respiratory Air Liquid Interface. Furthermore,Pulmonary Surfactant Has Been Proposed As An Effective Method For Targeting Drugs To The Lungs. However,Few Studies Have Examined In Detail The Mechanisms Of Incorporation Of Drugs Into Surfactant,The Impact Of The Presence Of Drugs On Pulmonary Surfactant Performance At The Interface Under Physiologically Meaningful Conditions,Or The Ability Of Pulmonary Surfactant To Use The Air Liquid Interface To Vehiculise Drugs To Long Distances. This Study Focuses On The Ability Of Pulmonary Surfactant To Interfacially Vehiculize Corticosteroids Such As Beclomethasone Dipropionate (Bdp) Or Budesonide (Bud) As Model Drugs. The Main Objectives Have Been To (A) Characterize The Incorporation Of Corticosteroids Into Natural And Synthetic Surfactants,. (B) Evaluate Whether The Presence Of Corticosteroids Affects Surfactant Functionality,And (C) Determine Whether Surfactant Preparations Enable The Efficient Spreading And Distribution Of Bdp And Bud Along The Air Liquid Interface. We Have Compared The Performance Of A Purified Surfactant From Porcine Lungs And Two Clinical Surfactants: Poractant Alfa,A Natural Surfactant Of Animal Origin Extensively Used To Treat Premature Babies,And Chf5633,A New Synthetic Surfactant Preparation Currently Under Clinical Trials. Both,Natural And Clinical Surfactants Spontaneously Incorporated Corticosteroids Up To At Least 10% By Mass With Respect To Phospholipid Content. The Presence Of The Drugs Did Not Interfere With Their Ability.To Efficiently Adsorb Into Air Liquid Interfaces And Form Surface Active Films Able To Reach And Sustain Very Low Surface Tensions (<2 Mn/m) Under Compression Expansion Cycling Mimicking Breathing Dynamics. Furthermore,The Combination Of Clinical Surfactant With Corticosteroids Efficiently Promoted The Active Diffusion Of The Drug To Long Distances Along The Air Liquid Interface. This Effect Could Not Be Mimicked By Vehiculisation Of Corticosteroids In Liposomes Or In Micellar Emulsions Similar To The Formulations Currently In Use To Deliver Anti-Inflammatory Corticosteroids Through Inhalation.
DOI:10.1021/acs.Langmuir.7B01177

专利信息

专利号:US-8546532-B2
优先权日:2008-04-17
标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders
发明人：BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS
权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC
摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:US-11311505-B2
优先权日:2017-02-24
标 题:Synergistic compositions to stimulate the synthesis of human lung and sinus surfactants to decrease coughing, increase FEV-1/FVC ratios, decrease lung fibrosis, by increasing apoptosis of myofibroblasts
发明人：MARTIN ALAIN
权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
摘要:Methods for the treatment of patients with both Chronic Obstructive Pulmonary Disease (COPD) and pulmonary fibrosis, and of patients with idiopathic pulmonary fibrosis without COPD, by stimulating the synthesis of human and animal patient lung and sinus surfactants to increase lung functions, inhibiting fibrosis and reducing coughing and nasal erythema, include the following steps: A) analyzing and diagnosing a patient with a lung ailment selected from the group consisting of i) both COPD and pulmonary fibrosis; and ii) idiopathic pulmonary fibrosis without COPD; and, B) treating the patient to raise the patient's lung functions including FEV1/FVC ratio by contacting mammalian cells with a [therapeutically effective amount of a treatment] composition that includes: a) a pyruvate salt; b) a phosphate; c) a salt of calcium; and d) a salt of magnesium, in an aqueous carrier, containing no more than 2.2 grams of said pyruvate salt per liter.

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-10813893-B2
优先权日:2017-02-24
标 题:Compositions and methods for the treatment and prevention of chronic hypoxemia and dyspnea
发明人：MARTIN ALAIN
权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
摘要:The present invention has shown that not all salts of pyruvic acid enhance lung functions or enhance the synthesis of lung surfactants and that certain salts of pyruvic acid with the correct concentrations of calcium, phosphate and magnesium, are synergistic in their ability to enhance the synthesis of lung surfactants that will enhance lung alveoli functions, while decreasing coughing and lung tightness, and increasing oxygen saturation values to prevent hypoxemia. This patent demonstrates that the sodium pyruvate formula with calcium, phosphate and magnesium was superior over standard sodium pyruvate formula in saline alone in the removal of mucus, reduction of lung or sinus infections, and in reducing drug side effects and congestion. The use of this formula clearly demonstrated that it can be used to produce better efficacy in patients with hypoxemia, with lung and sinus diseases including, asthma, COPD, cystic fibrosis, interstitial lung disease, allergic rhinitis, sinusitis, Alzheimer's, disease, Parkinson's disease, brain trauma, nicotine addiction, sleep apnea, autism, migraine headaches, sleep disorders, lung and sinus infections, cancer therapy with cancer drugs, nicotine addiction, and medications that cause a decrease in lung surfactants.