专利号:WO-2021161084-A1 优先权日:2020-02-16 标题 :N-(4-fluorophenyl)-5-phenyl-[1,2,4] triazolo [1,5-a] pyridine-2-carboxamide derivatives and their synthesis thereof 发明人:NINGEGOWDA RAGHU; BANUPRAKASH GOVINDAPPA; CHANDRASHEKHARAPPA SANDEEP 权利人:NINGEGOWDA RAGHU; BANUPRAKASH GOVINDAPPA; CHANDRASHEKHARAPPA SANDEEP 摘要:The present invention relates to the development of novel N-(4-fluorophenyl)-5-phenyl- [1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives for their different pharmacological activities. It particularly relates to the development of N-(4-fluorophenyl)-5-phenyl- [1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives as antiviral, anticancer, antifungal, hypoglycemic, anti-tubercular, sedative, anti-type 2 diabetes activity. It specifically relates to the N-(4-fluorophenyl)-5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives for treatment of H37Rv and multidrug-resistant (MDR) strains of Mycobacterium tuberculosis (MTB). The present invention also relates to the process for synthesis of N-(4-fluorophenyl)- 5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives. The invention further relates to method for treatment of method for treatment of diseases such as tuberculosis, type 2 diabetes, bacterial, viral and fungal infections. Invention addresses the challenges in working with chemical processes and products by inventing novel reaction methodology that can maximize the desired products and minimize by-products, designing new synthetic schemes that can simplify operations in chemical productions and seeking nontoxic reagent that are inherently environmentally and ecologically benign. Synthesis of novel N-(4- fluorophenyl)-5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives is being employed to develop a novel synthetic methodology and their pharmacological applications. Novel series of N-(4-fluorophenyl)-5-phenyl-[1,2,4]triazolo[l,5-a]pyridine-2-carboxamide derivatives were designed synthesized evaluated for their in vitro anti-mycobacterial activity against H37Rv and multi-drug-resistant (MDR) strains of mycobacterium tuberculosis (MTB). All the synthesized compounds were characterized by spectroscopic methods like Mass, NMR and elemental analysis.
专利号:US-6441189-B1 优先权日:2000-03-31 标 题 :Process for the preparation of matrix metalloproteinase inhibitors 发明人:BAILEY ANNE E; HILL DAVID R; HSIAO CHI-NUNG W; KURUKULASURIYA RAVI; WITTENBERGER STEVE; MCDERMOTT TODD; MCLAUGHLIN MAUREEN A 权利人:ABBOTT LAB 摘要:The instant invention provides a process for the synthesis of matrix metalloproteinase inhibitors.
专利号:US-7115737-B2 优先权日:2003-05-05 标题:Solid phase synthesis of novel biaryl triazine library by suzuki cross coupling 发明人:CHANG YOUNG-TAE 权利人:UNIV NEW YORK 摘要:Two methods are used to produce diaryl trisubstituted triazines. In the first method, cyanuric chloride is first reacted with a 4-alkoxybenzylamine. The product of this reaction is then reacted with a resin-bound amine, such as 4-alkoxybenzylamine, to ensure that the final compound will be bound to a resin. The product of this reaction is then reacted with boronic acid to produce a trisubstituted diaryl triazine. In the second method, cyanuric chloride is reacted with a benzenealkanethiol. The product of this reaction is then reacted with a resin-bound amine, such as 4-alkoxybenzylamine, to ensure that the final compound will be bound to a resin. The product of this reaction is then reacted with m-CPBA to form a sulfone, which is then reacted with a 4-alkoxybenzylamine to form the desired trisubstituted biaryltriazine.
专利号:US-12150934-B2 优先权日:2016-11-30 标 题 :Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases 发明人:SIDDIQUI ARSHAD M; CIBLAT STEPHANE; CONSTANTINEAU-FORGET LEA; GRAND-MAITRE CHANTAL; GUO XIANGYU; SRIVASTAVA SANJAY; SHIPPS GERALD W; COOPER ALAN B; OZA VIBHA; KOSTURA MATTHEW W; LUTHER MICHAEL; LEVINE JEDD 权利人:BANTAM PHARMACEUTICAL LLC 摘要:Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X1, X2, Z1, Z2, the ring system denoted by “aâ€?, R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.
专利号:US-2010120784-A1 优先权日:2007-04-20 标题 :Novel heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:LACHANCE NICOLAS; LI CHUN SING; LECLERC JEAN-PHILPPE; RAMTOHUL YEEMAN K 权利人:LACHANCE NICOLAS; LI CHUN SING; LECLERC JEAN-PHILPPE; RAMTOHUL YEEMAN K 摘要:Heteroaromatic compounds of structural formula (I) or a pharmaceutically acceptable salt thereof, wherein W is a substituted heteroaryl, X and Y are each independently a bond, —O—, —S—, —S(O)—, —S(O) 2 —, —NR 6 —, —C(O)—, —C(CH 3 )(OH)— or —C(CH 3 )â•?CH—, u (I) is an integer from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) 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, Type 2 diabetes, insulin resistance, hyperglycemia, Metabolic Syndrome, neurological disease, cancer, and liver steatosis
专利号:WO-2023086799-A1 优先权日:2021-11-09 标 题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P 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.
摘要:Aggarwal, P.; Bebbington, M. W. P., Science of Synthesis Knowledge Updates, (2012) 2, 457. 摘要:Croft, R. A.; Bull, J. A., Science of Synthesis Knowledge Updates, (2018) 4, 419. 摘要:Vashchenko, B. V.; Grygorenko, O. O., Science of Synthesis Knowledge Updates, (2021) 3, 297. 摘要:Sloane, S. E.; Behlow, K. T.; Mills, M. D.; Clark, J. R., Science of Synthesis Knowledge Updates, (2022) 2, 397. 摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 95.