专利号:US-6734309-B1 优先权日:2002-12-23 标题:Process for the synthesis of isonicotinic acid hydrazide 发明人:RAY SUBHASH CHANDRA; NANDI LAKSHMI NARAYAN; SINGH BALDEV; PRASAD HIRALAL; MAHARAJ SUMANT; SARKAR PRODYOT KUMAR; DUTTA PASHUPATI; ROY SHYAM KISHORE; YADAV SATYA NIKETAN; BANDYOPADHYAY ANUP KUMAR 权利人:COUNCIL SCIENT IND RES 摘要:The invention provides a process for the manufacture of isonicotinic acid hydrazide(INH) useful in the treatment of tuberculosis. The invention relates to the single step conversion of isonicotinamide by hydrazine hydrate to isonicotinic acid hydrazide (INH) of yield greater than 95% (w/w) and purity more than 99%.
专利号:US-8895747-B2 优先权日:2009-07-27 标 题 :Method and substances for preparation of N-substituted pyridinium compounds 发明人:HEINDL DIETER; MAERZ HERIBERT; SCHMIDT AXEL 权利人:HEINDL DIETER; MAERZ HERIBERT; SCHMIDT AXEL; ROCHE DIAGNOSTICS OPERATIONS 摘要:Methods for the synthesis of N-substituted pyridinium compounds by using an N-heteroaryl substituted pyridinium salt (Zincke salt) and reacting it with a nucleophilic amine are provided. Novel purine-substituted pyridyl compounds, which may be useful reagents in the above reaction, are also disclosed.
专利号:US-6730787-B1 优先权日:1998-12-04 标题 :2,4Dioxo-5-arylidenimino-1,3-pyrimidines 发明人:KRUTIKOV VIKTOR I; ASHKINAZI RIMMA I 权利人:VIROMAX LLC 摘要:The invention relates to medicine, and more specifically to pharmacology, and in particular to synthetic biologically active derivatives of pyrimidine, and it is designated mainly for use as antiviral, immune-stimulating, antichlamydial, antituberculous, psychodepressant, analgesic, and hepatoprotective remedies. Besides that, these compounds may be used for treating malignant neoplasms, and also in veterinary. The objective of the invention is obtaining new chemical substances possessing pronounced biological activity of wide range. The proposed objective is achieved by synthesis of 2,4-dioxo-5-arylidenimino-1,3-pyrimidines of the general formulawhere R is chosen out of group H, OH, alkoxyl, dialkylamino, benzo, dibenzo, or 3,4-dioxolano General method of producing the claimed compounds and example of synthesis, a list of 25 compounds synthesized and tested, results of identification, and data on wide comparative testing their biological properties and toxicity are presented.
专利号:US-2024335420-A1 优先权日:2021-08-02 标题:N-acylhydrazone compounds capable of inhibiting nav 1.7 and/or nav 1.8, processes for the preparation thereof, compositions, uses, methods for treatment using same and kits 发明人:BARREIRO GABRIELA; SANT'ANA DANILO PEREIRA DE; GAMBA LUIS EDUARDO REINA; FRAGA CARLOS ALBERTO MANSSOUR; BARREIRO ELIEZER JESUS DE LACERDA; LIMA LÃ?DIA MOREIRA 权利人:EUROFARMA LABORATORIOS S A; UNIV FEDERAL DO RIO DE JANEIRO UFRJ 摘要:N-Acylhydrazone compounds that are Nav 1.7 and/or Nav 1.8 inhibitors, including N-acylhydrazone compounds of Formula (I), wherein substituents R1 to R4 are independently selected from the groups defined in the specification, as well as to the processes for the preparation thereof, compositions comprising at least one of these compounds, uses, treatment methods for treating or preventing pain-related pathologies, and kits, useful in the fields of medicinal chemistry, organic synthesis, as well as in the treatment of pain-related disorders.
专利号:US-10738028-B2 优先权日:2016-05-11 标题:Spiro three-membered ring, spiro five-membered ring peptide deformylase inhibitor and use thereof in antibacteria and anti-tumor 发明人:HU WENHAO; LV FENGPING; TANG YANG; LI ZIYAN; CHEN CHEN; WEI JIANHAI; DONG SUZHEN; QIAN YU 权利人:RUDONG RUIEN PHARMACEUTICAL TECH CO LTD 摘要:Disclosed are the anti-bacterial activity and the anti-tumor activity of a class of new spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, are effective against many antibiotic-resistant Gram-positive strains by inhibiting the activity of the peptide deformylase required in the synthesis of bacterial proteins, and do not affect the synthetic process of the main proteins of the human body, thus selectively killing bacteria. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, can affect the energy balance of the cancer cells through inhibiting the peptide deformylase of the mitochondria in the cells, so that the mitochondrial membrane is depolarized, ATP is exhausted and cell apoptosis is promoted, and has good inhibitory activities on many cancer cell strains such as colorectal cancer, leukemia, lung cancer, gastric cancer, cervical cancer, breast cancer, prostatic cancer, liver cancer and osteosarcoma at relatively lower concentrations. The structure of exemplary invention spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitors are represented by one or more of:
专利号:CN-109293636-B 优先权日:2018-10-22 标 题 :One-pot synthesis of capsule coordination compound containing Schiff base structural unit, preparation method and application
1: Priebe JP, Mello RS, Nome F, Bortoluzzi AJ. Nicotinohydrazide. Acta Crystallogr Sect E Struct Rep Online. 2007 Dec 18;64(Pt 1):o302-3. doi: 10.1107/S160053680706655X. 2: Akkurt M, Khandar AA, Tahir MN, Yazdi SA, Afkhami FA. Dibromido{N'-[1-(pyridin-2-yl)ethyl-idene]picolinohydrazide-κ(2)N',O}cadmium. Acta Crystallogr Sect E Struct Rep Online. 2012 Jun 1;68(Pt 6):m842. doi: 10.1107/S1600536812023185. Epub 2012 May 31. 3: Zhang S, Wang Y, Xu H. A new naphthalimide-picolinohydrazide derived fluorescent "turn-on" probe for hypersensitive detection of Al3+ ions and applications of real water analysis and bio-imaging. Spectrochim Acta A Mol Biomol Spectrosc. 2022 Jul 5;275:121193. doi: 10.1016/j.saa.2022.121193. Epub 2022 Mar 24.
合成参考文献
摘要:Aggarwal, P.; Bebbington, M. W. P., Science of Synthesis Knowledge Updates, (2012) 2, 384. 摘要:A. Albert. Nature 177, 525 (1956).