CAS: 139481-59-7; 1-((2'-(2H-Tetrazol-5-yl)-[1,1'-Biphenyl]-4-yl)Methyl)-2-Ethoxy-1H-Benzo[d]Imidazole-7-Carboxylic Acid

上下游产品

CAS号139481-69-9 坎地沙坦甲酯 | CAS号856414-35-2 N-三苯甲基坎地沙坦乙酯 | CAS号139481-58-6 坎地沙坦乙酯 | CAS号21606-04-2 2-(甲氧羰基)-6-硝基苯甲酸 | CAS号73833-13-3 acid chloride o... | CAS号603-11-2 3-硝基邻苯二甲酸 | CAS号57113-90-3 2-(叔丁氧羰基氨基)-3-硝... | CAS号136304-78-4 3-氨基-2-[(2-氰基联苯... | CAS号139481-28-0 甲酯C4 | CAS号139481-72-4 三苯甲基坎地沙坦 | CAS号145040-37-5 坎地沙坦酯 | CAS号170791-09-0 三苯甲基坎地沙坦西来替昔酯

坎地沙坦酯置于双(对硝基苯基)磷酸酯体系中,用 二甲基亚砜,乙腈 用作溶剂,化学反应 0.03H,反应生成坎地沙坦
参考文献:Different Hydrolases Involved In Bioactivation Of Prodrug-Type Angiotensin Receptor Blockers: Carboxymethylenebutenolidase And Carboxylesterase 1
标题:Different Hydrolases Involved In Bioactivation Of Prodrug-Type Angiotensin Receptor Blockers: Carboxymethylenebutenolidase And Carboxylesterase 1
摘要:奥美沙坦酯(om)是一种前药类型的血管紧张素ii 1型受体阻断剂(arb).我们最近鉴定出羧甲基烯酮合成酶同源物(cmbl)是人类中负责om生物活化的酶.在本研究中,我们通过关注种间差异和组织特异性,比较了om与其他前药类型的arb,坎地沙坦环己酯(cc)和阿齐沙坦酯(am)的生物活化特性.在采用小鼠,大鼠,猴,狗和人的组织亚细胞组分的体外实验中,除了狗的肠道(几乎没有活性)外,所有测试物种的肝细胞,肠细胞和肾细胞中都观测到显著的om水解酶活性,而肺细胞中的活性相对较低.相比之下,肝微粒体表现出所有测试物种中各种组织亚细胞组分中的最高cc水解酶活性.通过western印迹分析采用组织亚细胞组分,用人cmbl和羧酸酯酶1(ces1)抗体染色的条带强度很好地反映了动物和人类中的om和am水解酶活性和cc水解酶活性.人重组的cmbl和ces1表现出显著的am和cc水解酶活性,而cc水解几乎不能通过重组的羧酸酯酶2(ces2)催化.总之,Om不仅在人类中通过肠道cmbl生物活化,而且在小鼠,大鼠和猴中也是如此,而cc通过肝ces1而非包括ces2在内的肠道酶生物活化.Am是cmbl的底物.
Doi:10.1124/dmd.113.053595

专利信息

专利号:US-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人：JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

专利号:US-2008214637-A1
优先权日:2004-11-11
标题 :Process for the Synthesis of Tetrazoles
发明人：ANTONCIC LJUBOMIR; LUDESCHER JOHANNES
权利人:LEK PHARMACEUTICALS
摘要:A process for the synthesis of tetrazol derivative has been developed which starts from a tetrazole derivative where acidic hydrogen atom has been replaced by a protecting group and the deprotection is performed with a catalytic amount of organic acid and can proceed in an aqueous solvent.

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-6271375-B1
优先权日:1997-06-30
标 题 :Ortho-metalation process for the synthesis of 2-substituted-1-(tetrazol-5-yl)benzenes
发明人：VILLA MARCO; ALLEGRINI PIETRO; ARRIGHI KATIUSCIA; PAIOCCHI MAURIZIO
权利人:ZAMBON SPA
摘要:A process of direct metalation of phenyltetrazoles useful for preparing compounds of formula (II) intermediates for the synthesis of angiotensin II antagonists is described.

专利号:US-8431712-B2
优先权日:2004-02-09
标 题 :Methods for the synthesis of pyridoxamine
发明人：KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT
权利人:KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT; NEPHROGENEX INC
摘要:The invention provides non-oxidative methods for the large scale manufacture of pyridoxamine (I) (4-aminomethyl-3-hydroxy-5-hydroxymethyl-2-methylpyridine): n nand salts thereof.n nThe invention also provides intermediate compounds for the synthesis of pyridoxamine, as well as compositions and methods for the treatment and/or prevention of conditions associated with the formation of post-Amadori advanced glycation end-products.

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人：GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.