CAS: 54-92-2; N'-Isopropylisonicotinohydrazide

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CAS号4813-04-1 1(Or 2)-(isopro... | CAS号54-85-3 异烟肼 | CAS号75-30-9 2-碘代丙烷 | CAS号75-26-3 2-溴丙烷

异烟肼置于sodium Cyanoborohydride,溶剂黄146体系中,用 甲醇,正己烷 作为反应溶剂,化学反应 30.0H,反应生成 异丙烟肼
参考文献:Discovery Of A Novel Series Of Indolyl Hydrazide Derivatives As Diacylglycerol Acyltransferase‐1 Inhibitors
标题:Discovery Of A Novel Series Of Indolyl Hydrazide Derivatives As Diacylglycerol Acyltransferase‐1 Inhibitors
摘要:研究人员合成了一系列新型酰肼衍生物,作为潜在的二酰基甘油酰基转移酶(dgat)抑制剂.其中,化合物 8U 和 8V 具有选择性和强效的 Dgat-1 抑制活性.此外,化合物 8U 还能剂量依赖性地抑制 Hepg2 细胞株中甘油三酯的合成.此外,用化合物 8U 进行口服脂质耐受性试验显示,与用车辆处理的对照组动物相比,血浆甘油三酯水平显著下降,这表明急性脂质挑战后甘油三酯的吸收延迟.
DOI:10.1002/bkcs.10123

专利信息

专利号:US-4310535-A
优先权日:1976-11-30
标题:Combination of drugs and a method for the selective control of the immune reactions evoked in a host by the administration of antigens
发明人：PIERPAOLI WALTER
权利人:PIERPAOLI WALTER
摘要:The invention concerns a new composition or combination of drugs effective to selectively control the immune reactions which are evoked in a host by the administration of antigens. It comprises active components capable of simultaneously blocking the alpha -adrenergic receptors of the cells for catecholamine, blocking the dopaminergic receptors of the cells and increasing the synthesis of serotonin. Preferred drug combinations according to the invention contain in association phentolamine, haloperidol, L-5-hydroxy-tryptophane and possibly dopamine.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人：MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:US-2008214827-A1
优先权日:2004-02-03
标 题:Synthesis of Cyanoimino-Benzoimidazoles
发明人：GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
权利人:EURO CELTIQUE SA
摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

专利号:US-5519131-A
优先权日:1991-04-15
标题:Synthesis of pyridooxazinyl-indoles
发明人：EFFLAND RICHARD C; DAVIS LARRY; OLSEN GORDON E
权利人:HOECHST MARION ROUSSEL INC
摘要:This application relates to a process for the preparation of indolylpyridooxazines of the formula wherein R1, R2 and R3 are as defined in the specification which comprises cyclizing compound of the formula in the presence of a strong base such as sodium hydride or potassium t-butoxide.

专利号:US-7749985-B2
优先权日:2006-09-15
标 题 :Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
发明人：GALLOP MARK A; XU FENG; PHAN THU; DILIP USHA; PENG GE
权利人:XENOPORT INC
摘要:Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of making acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of using acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, and pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs 3-aminopropylphosphinic acid and analogs thereof for treating diseases or disorders such as mild cognitive impairment, cognitive impairment associated with Alzheimer's disease Alzheimer's disease, depression, anxiety, and epilepsy are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, which are suitable for oral administration and sustained release oral dosage forms are also disclosed.

专利号:EP-3103803-B1
优先权日:2008-10-27
标 题 :Intermediates for the synthesis of mtor kinase inhibitors