1,5-二溴戊烷置于盐酸,氨,Sodium Ethanolate体系中,用 苯 用作溶剂,化学反应 126.0H,反应生成喷他脒 参考文献:Analogs Of 1,5-Bis(4-Amidinophenoxy)Pentane (Pentamidine) In The Treatment Of Experimental Pneumocystis Carinii Pneumonia 标题:Analogs Of 1,5-Bis(4-Amidinophenoxy)Pentane (Pentamidine) In The Treatment Of Experimental Pneumocystis Carinii Pneumonia 摘要:A Series Of 33 Analogues Of The Anti-Pneumocystis Carinii Drug 1,5-Bis(4-Amidinophenoxy)Pentane (Pentamidine) Was Synthesized For Screening Against A Rat Model Of P. Carinii Pneumonia (Pcp). Twenty-Five Of The Compounds Showed Efficacy Against Pcp When Compared To A Saline-Treated Control Group. Two Compounds,1,4-Bis(4-Amidinophenoxy)Butane (Butamidine,6) And 1,3-Bis(4-Amidino-2-Methoxyphenoxy)Propane (Damp,16),Were Statistically More Effective Than The Parent Drug In Treating Pcp In The Rat Model Of Infection. In Addition To Their Activity Against Pcp,The Compounds Were Also Evaluated For Antitrypsin Activity,Ability To Inhibit Thymidylate Synthetase,Affinity For Dna,And Toxicity. No Correlation Was Observed Between The Tested Molecular Interactions Of The Diamidines And Their Effectiveness Against Pcp. Doi:10.1021/jm00166A026
专利信息
专利号:US-6818633-B2 优先权日:2001-06-29 标题:Antiviral compounds and methods for synthesis and therapy 发明人:BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN 权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING 摘要:Novel compounds are provided having formula (I)whereR1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
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-10308663-B2 优先权日:2015-06-16 标题:Inhibitors of PTP4A3 for the treatment of cancer 发明人:LAZO JOHN S; SHARLOW ELIZABETH R; MCQUEENEY KELLEY E; WIPF PETER; SALAMOUN JOSEPH M 权利人:LAZO JOHN S; SHARLOW ELIZABETH R; MCQUEENEY KELLEY E; WIPF PETER; SALAMOUN JOSEPH M; UNIV VIRGINIA PATENT FOUNDATION; UNIV OF PITTSBURGH —OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION 摘要:The invention provides protein tyrosine phosphatase inhibitor compounds, Their pharmaceutical compositions, uses, and methods of use, such as in the treatment of various cancers, and process for making the compounds. Also disclosed is an improved synthesis of protein tyrosine phosphatase inhibitor and precursor compound thienopyridone (5).
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.
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.
1: Al-Shaikhly T, Al-Obaydi S, Craig TJ, Henao MP. Sulfonamide allergy label and the risk of opportunistic infections in solid organ transplant recipients - A retrospective matched cohort study. Transpl Infect Dis. 2024 Aug 13:e14355. doi: 10.1111/tid.14355. Epub ahead of print. 11(7):004615. doi: 10.12890/2024_004615. 4: Knapp K, Klasinc R, Koren A, Siller M, Dingelmaier-Hovorka R, Drach M, Sanchez J, Chromy D, Kranawetter M, Grimm C, Bergthaler A, Kubicek S, Stockinger H, Stary G. Combination of compound screening with an animal model identifies pentamidine to prevent Chlamydia trachomatis infection. Cell Rep Med. 2024 Jul 16;5(7):101643. doi: 10.1016/j.xcrm.2024.101643. Epub 2024 Jul 8.
合成参考文献
参考文献:10.1007/s11095-005-9042-6 摘要:Duvvuri S, Gaurav Janoria K, Mitra AK. Effect of polymer blending on the release of ganciclovir from PLGA microspheres. Pharm Res. 2006 Jan;23(1):215–23. doi: 10.1007/s11095-005-9042-6. 参考文献:10.1016/j.bmc.2011.06.023 摘要:Bello ML, Chiaradia LD, Dias LR, Pacheco LK, Stumpf TR, Mascarello A, Steindel M, Yunes RA, Castro HC, Nunes RJ, Rodrigues CR. Trimethoxy-chalcone derivatives inhibit growth of Leishmania braziliensis: synthesis, biological evaluation, molecular modeling and structure-activity relationship (SAR). Bioorg Med Chem. 2011 Aug 15;19(16):5046–52. doi: 10.1016/j.bmc.2011.06.023. 参考文献:10.1001/archdermatol.2011.162-a 摘要:Gee SN, Rothschild B, Click J, Sheth V, Saavedra A, Hsu MY. Tender ulceronecrotic nodules in a patient with leukemia. Cutaneous acanthamebiasis. Arch Dermatol. 2011 Jul;147(7):857–62. doi: 10.1001/archdermatol.2011.162-a. 参考文献:10.1007/s00424-011-0995-5 摘要:López-Izquierdo A, Aréchiga-Figueroa IA, Moreno-Galindo EG, Ponce-Balbuena D, Rodríguez-Martínez M, Ferrer-Villada T, Rodríguez-Menchaca AA, van der Heyden MAG, Sánchez-Chapula JA. Mechanisms for Kir channel inhibition by quinacrine: acute pore block of Kir2.x channels and interference in PIP2 interaction with Kir2.x and Kir6.2 channels. Pflügers Archiv - European Journal of Physiology. 2011 Jul 22;462(4):505. doi: 10.1007/s00424-011-0995-5.