CAS: 4499-40-5; 1,3-Dimethyl-2-Oxopurin-6-Olate,2-Hydroxyethyl(Trimethyl)Azanium

该化合物是主要用作气喘和慢性阻塞性肺病(COPD)等呼吸状况治疗支气管的药物化合物;是一种Xanthine衍生物,其结构上与咖啡因和顺眼线有关,其作用是放松气道的光滑肌肉,从而方便呼吸; 已知的有机磷素具有增强呼吸功能和改善空气流的能力; 该化合物一般是口服的,并且可以使用各种配方,包括药片和糖浆; 其药理效应归因于其抑制磷酸酯酶的能力,导致循环氨酸盐含量增加,从而推动溴化.尽管一般都受到良好的刺激,但潜在的副作用可能包括胃肠紊乱,...

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    专利号:US-2008300418-A1
    优先权日:2004-11-08
    标 题:Synthesis of Cardiolipin Analogues and Uses Thereof
    发明人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN
    权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN
    摘要:The invention provides novel synthetic methodologies for preparing cardiolipin, migrated caridiolipin (1,2-positional isomer of cardiolipin) and their analogues having varying fatty acids and/or alkyl chains with varying length and degrees of saturation/unsaturation. The method comprises (a) reacting an optically pure 1,2-O-dialkyl-sn-glycerol or 1,2-O-dialkyl-sn-glycerol with one or more phosphoramidite reagent(s), wherein a phosphite triester is produced; (b) coupling the product of (a) with glycerol, wherein a protected cardiolipin is produced; and (c) deprotecting the protected cardiolipin, such that cardiolipin is prepared. The cardiolipins and analogues thereof, prepared by the present methods, can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs, antisense nucleotides or diagnostic agents. Such liposomes can be used to treat diseases or can be used in diagnostic and/or analytical assays.

    专利号:US-2006078560-A1
    优先权日:2003-06-23
    标 题 :Method of inducing apoptosis and inhibiting cardiolipin synthesis
    发明人:JAMIL HARIS; AHMAD MOGHIS U; AHMAD IMRAN
    权利人:NEOPHARM INC
    摘要:The present invention provides a method for inducing apoptosis within a cell by exposing the cell to an inhibitor of cardiolipin synthesis under conditions sufficient to induce apoptosis within the cell. The method can be used to investigate or treat disorders such as cancer, obesity, and cardiovascular disorders. The invention also provides a pharmaceutical composition including an inhibitor of cardiolipin synthesis and a liposomal carrier.

    专利号:US-2008286351-A1
    优先权日:2004-06-29
    标 题:Pegylated Cardiolipin Analogs, Methods of Synthesis, and Uses Thereof
    发明人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN
    权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN
    摘要:The invention provides synthetic methods for PEGylated cardiolipins with varying linkers. The methods can be employed to prepare PEGylated cardiolipin with different fatty acid and/or alkyl chain length with or without unsaturation. The PEGylated cardiolipin, prepared by the present methods, can be incorporated into liposomes that can also include active agents such as hydrophilic or hydrophobic drugs for the treatment of human and animal diseases. In addition, the PEGylated cardiolipin can be incorporated into liposomes that include compounds for therapeutic and diagnostic imaging. The use of such liposomes with PEGylated cardiolipin prolongs the period of liposomal circulation without disrupting the lipid bilayer.

    专利号:US-2005266068-A1
    优先权日:2002-05-24
    标题 :Cardiolipin molecules and methods of synthesis
    发明人:AHMAD MOGHIS U; UKKALAM MURALI K; AHMAD IMRAN
    权利人:NEOPHARM INC
    摘要:The invention provides new synthetic routes for cardiolipin with different fatty acids and/or alkyl chains with varying chain length and also with or without unsaturation, particularly a short-chain cardiolipin. The methods comprise reacting a 1,2-O-sn-diacyl/1,2-O-sn-dialkyl glycerol or a 2-O-protected glycerol, with a phosphoramidite reagent or a phosphate triester to produce a protected cardiolipin, which is deprotected to prepare the short chain cardiolipin. The reaction schemes can be used to generate new variants of cardiolipin. The cardiolipin prepared by the present methods can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs. Such liposomes can be used to treat diseases or in diagnostic and/or analytical assays. Liposomes can also include ligands for targeting a particular cell type or specific tissue.

    专利号:US-8697730-B2
    优先权日:2007-10-26
    标题 :5-lipoxygenase activating protein (FLAP) inhibitor
    发明人:REWOLINSKI MELISSA VIRGINIA; SCHAAB KEVIN MURRAY; KING CHRISTOPHER DAVID; STOCK NICHOLAS SIMON
    权利人:REWOLINSKI MELISSA VIRGINIA; SCHAAB KEVIN MURRAY; KING CHRISTOPHER DAVID; STOCK NICHOLAS SIMON; PANMIRA PHARMACEUTICALS LLC
    摘要:Described herein are methods for the synthesis of 3-[5-(pyridin-2-ylmethoxy)-3-(2-methyl-2-propylthio)-1-[4-(2-methoxypyridin-5-yl)benzyl]-indol-2-yl]-2,2-dimethyl-propionic acid, pharmaceutically acceptable salts, pharmaceutically acceptable solvates thereof. Also described are pharmaceutical compositions suitable for oral administration to a mammal that include, as well as methods of using such oral pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.

    专利号:US-4778805-A
    优先权日:1987-06-18
    标题:4,7-benzofurandione derivatives useful as inhibitors of leukotriene synthesis
    发明人:ADAMS JULIAN; GUINDON YVAN; BELANGER PATRICE C; BELLEY MICHEL L; ROKACH JOSHUA
    权利人:MERCK FROSST CANADA
    摘要:4,7-Benzofurandione derivatives of Formula I, pharmaceutical compositions, and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation, psoriasis and allergic conjunctivitis. The compounds are also useful as analgesics and as cytoprotective agents. Also disclosed are novel intermediates useful for the preparation of the 4,7-benzofurandiones of this invention. ##STR1##

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    主要参考文献


    1: Adikusuma W, Chou WH, Lin MR, Ting J, Irham LM, Perwitasari DA, Chang WP, Chang WC. Identification of Druggable Genes for Asthma by Integrated Genomic Network Analysis. Biomedicines. 2022 Jan 6;10(1):113. doi: 10.3390/biomedicines10010113.
    2: Hendeles L, Jenkins J, Temple R. Revised FDA labeling guideline for theophylline oral dosage forms. Pharmacotherapy. 1995 Jul-Aug;15(4):409-27. 12(9):1083-90. doi: 10.1016/0731-7085(94)00050-6. 80(5):240-3. 44(6):223-5. 29(5):533-9. doi: 10.1111/j.1365-2125.1990.tb03676.x.
    7: Samaan S, Fox R. The effect of smoking on theophylline kinetics in healthy and asthmatic elderly males. J Clin Pharmacol. 1989 May;29(5):448-50. doi: 10.1002/j.1552-4604.1989.tb03360.x. 16(6):452-8. doi: 10.1177/030006058801600607.

    合成参考文献


    摘要:Drugs in Japan, 6(278), 1982
    摘要:American Journal of Emergency Medicine., 3(408), 1985 []
    参考文献:10.2165/00044011-199816060-00004
    摘要:Claesson CB, Schmidt IK. Drug use in Swedish nursing homes. Clin Drug Investig. 1998;16(6):441–52. doi: 10.2165/00044011-199816060-00004.
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