CAS: 66635-93-6; (R)-Ketorolac

该化合物是一种主要用于其止痛至严重疼痛的止炎性非类固醇抗炎药物(NSAID),主要用于治疗中度至重度疼痛,其特点是能够抑制酶环氧基酶(COX),该酶在合成丙烯菊酯,炎症和疼痛信号的化合物方面起着关键作用.该物质通常以其种族形式施用,但(+)抗炎药物是一种具有重大止痛效应的积极形式.(+)-Ketorolac因其迅速开始行动而闻名,经常用于手术后环境.它存在于各种配方中,包括口服片和可注射的形式.该药物一般受到良好的调适,但可产生副作用,包括胃肠问题,肾损伤和潜在的心血管风险,特别是长期用途.由于其能性能,建议短期使用,因此其开处方仅限于与具体临床风险相关的治疗.

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CAS号98-88-4 苯甲酰氯

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    📜5-Benzoyl-1,2-Dihydro-3H-Pyrrolo[1,2-A]Pyrrole-1-Carboxylic Acid Butyl Ester置于sodium Hydroxide,Phosphate Buffer,Lipase B From Candida Antarctica体系中,用 水 作为反应溶剂,化学反应 0.5H,反应生成 (R)-酮咯酸
    参考文献:Enzymatic Kinetic Resolution Of Ketorolac
    标题:Enzymatic Kinetic Resolution Of Ketorolac
    摘要:Ketorolac Was Resolved Into Each Enantiomer By Interesterification Using Lipase B From Candida Antarctica. The Acid Reacted With Various Alcohols And The Ester And Acid Were Resolved Up To > 99% E.E. When Reacted With octanol,Which Was The Best Result. To Increase Reactivity And Enantioselectivity,The Experimental Conditions Were Adjusted By Varying Temperature,Solvent,Alcohols And Reaction Time. (C) 2001 Published By Elsevier Science Ltd.
    DOI:10.1016/s0957-4166(01)00332-9

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    专利信息


    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:WO-2017100796-A1
    优先权日:2015-12-11
    标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
    权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.

    专利号:US-2017283878-A1
    优先权日:2015-12-11
    标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
    权利人:ACADEMIA SINICA
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

    专利号:US-10975069-B2
    优先权日:2014-04-01
    标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof
    发明人:HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN
    权利人:UNIV WASHINGTON
    摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.

    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.

    专利号:US-11628186-B2
    优先权日:2017-02-24
    标题 :Method and composition for the reduction of viral replication, duration and spread of the COVID-19 and the flu
    发明人:MARTIN ALAIN
    权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
    摘要:A method for stimulating the synthesis of nasal nitric oxide and nasal and lung surfactants to inhibit the docking and adhesion of viruses to cellular receptors, including ACE2, to reduce viral replication, duration, spread and severity of infections, and also to inhibit lung fibrosis, increase the synthesis of serotonin to reduce coughing and mouth breathing, reduce the cytokine storm produced by LI-6 caused by viruses such as COVID-19 and flu in patients susceptible to these infections, including patients with hypoxemia, asthma, chronic obstructive pulmonary disease, cystic fibrosis, diabetics, interstitial lung disease, pulmonary fibrosis, allergic rhinitis, sinusitis, smokers, sleep apnea and lung cancer, which includes: contacting mammalian cells with a therapeutically effective amount of a composition, said composition including the following constituents: sodium pyruvate; a phosphate; a salt of calcium; and a salt of magnesium.

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    合成参考文献


    参考文献:10.2147/opth.s7633
    摘要:Reddy R, Kim SJ. Critical appraisal of ophthalmic ketorolac in treatment of pain and inflammation following cataract surgery. Clin Ophthalmol. 2011;5():751–8.
    参考文献:10.4103/0972-124x.82274
    摘要:Hungund S, Thakkar R. Effect of pretreatment with ketorolac tromethamine on operative pain during periodontal surgery: A case-control study. J Indian Soc Periodontol. 2011 Jan;15(1):55–8.
    参考文献:10.1155/2011/982410
    摘要:van Philips LAM. Toxic Anterior Segment Syndrome after Foldable Artiflex Iris-Fixated Phakic Intraocular Lens Implantation. Journal of Ophthalmology. 2011;2011():1–5. doi: 10.1155/2011/982410.
    参考文献:10.3797/scipharm.1010-04
    摘要:Bhowmik M, Das S, Chattopadhyay D, Ghosh LK. Study of thermo-sensitive in-situ gels for ocular delivery. Sci Pharm. 2011 Apr;79(2):351–8.
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