6-溴-3-吡嗪胺置于sodium Hydroxide,Palladium On Activated Charcoal体系中,化学反应生成 哒嗪-3-胺 参考文献:Pyridazine Derivatives. Ii.1 An Improved Synthesis Of 3-Aminopyridazine 标题:Pyridazine Derivatives. Ii.1 An Improved Synthesis Of 3-Aminopyridazine 摘要: DOI:10.1021/ja01641A043
专利信息
专利号:WO-2025128848-A1 优先权日:2023-12-12 标题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).
专利号:WO-9740052-A1 优先权日:1996-04-22 标题 :Propagylglycine derivatives, preparation and utilisation thereof as synthesis intermediates 发明人:CARDINAUD ISABELLE; CHEKROUN ISAAC; ROSSEY GUY; CREMER GERARD; GOBERVILLE PASCALE; HOORNAERT CHRISTIAN 权利人:SYNTHELABO; CARDINAUD ISABELLE; CHEKROUN ISAAC; ROSSEY GUY; CREMER GERARD; GOBERVILLE PASCALE; HOORNAERT CHRISTIAN 摘要:Compounds of formula (I) wherein R2 is -CH2C=CH or -CH2C=C-Het where Het is a 2-aminopyridyl, 2-aminopyrimidyl, 6-aminopyridazinyl, imidazol-4-yl group, R3 and R4 each represent hydrogen, (C1-C4)alkyl, (C1-C4)alkoxycarbonyl, ArCH2CO2- or ArSO2- where Ar is an aryl group, or a group (a) where R7 is hydrogen or -COR, R being straight or branched (C1-C7) alkyl, -(CH2)nOCH3 or -CH2O(C2H4O)nCH3 (n is 1, 2 or 3) and A is chosen among the phenyl, pyrimidyl, pyridinyl, thienyl, thiazolyl and furyl groups, R6 represents either a straight or branched (C1-C4) alkoxy group, or a benzyloxy group or a group (b) where R12 is a hydrogen atom or a carboxylic or (C1-C4)alkoxycarbonyl group and R13 is a straight or branched (C1-C4)alkyl group. They constitute synthesis intermediates.
专利号:US-7019094-B2 优先权日:2002-05-31 标 题:Intermediate products, methods for their preparation and use thereof 发明人:WESTMAN JACOB; LUNDIN RONNY 权利人:BIOTAGE AB 摘要:Novel solid supported intermediate products of the general formula n ncoupled to a solid polymeric support through one or both of the R 1 groups or through the R 4 group which are suitable for synthesis of heterocyclic compounds are disclosed. Methods for preparing such intermediate products are also disclosed and also the use of the intermediate products in simple and fast methods on solid phase for synthesis of heterocycles.
专利号:WO-2011047481-A1 优先权日:2009-10-23 标题 :Novel spiro compounds useful as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:FORTIN REJEAN; LACHANCE NICOLAS; LI CHUN SING; TRANMER GEOFFREY 权利人:MERCK FROSST CANADA LTD; FORTIN REJEAN; LACHANCE NICOLAS; LI CHUN SING; TRANMER GEOFFREY 摘要:Heteroaromatic compounds of structural formula I are selective inhibitors of stearoyl- coenzyme. A delta-9 desaturase (SCDl) relative to other known stearoyl-coenzyme. A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. Formula (I).
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:
摘要:Graham, J. S.; Stanway-Gordon, H. A.; Waring, M. J., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 438. 参考文献:10.1385/jmn:24:1:001 摘要:Refolo LM, Fillit HM. Drug discovery for Alzheimer's disease: the end of the beginning. J Mol Neurosci. 2004;24(1):1–8. doi: 10.1385/jmn:24:1:001. 参考文献:10.1385/jmn:24:1:115 摘要:Craft JM, Van Eldik LJ, Zasadzki M, Hu W, Watterson DM. Aminopyridazines attenuate hippocampus-dependent behavioral deficits induced by human β-amyloid in a murine model of neuroinflammation. Journal of Molecular Neuroscience. 2004 Aug;24(1):115–22. doi: 10.1385/jmn:24:1:115.