专利号:US-8906915-B2 优先权日:2009-12-17 标 题:Compounds, compositions, and methods for controlling biofilms 发明人:DE KEERSMAECKER SIGRID; DE VOS DIRK; ERMOLATEV DENIS; STEENACKERS HANS; VAN DER EYCKEN ERIK; VANDERLEYDEN JOZEF; SAVALIYA BHARAT S 权利人:DE KEERSMAECKER SIGRID; DE VOS DIRK; ERMOLATEV DENIS; STEENACKERS HANS; VAN DER EYCKEN ERIK; VANDERLEYDEN JOZEF; SAVALIYA BHARAT S; UNIV LEUVEN KATH 摘要:The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients. Methods for inhibiting or controlling microbial biofilm formation in a plant, a body part of a human or an animal, or a surface with which a human or an animal may come into contact are also disclosed.
专利号:US-11325903-B2 优先权日:2016-11-30 标 题:Substituted pyrazole compounds and methods of using them for treatment of hyperproliferative diseases 发明人:SIDDIQUI M ARSHAD; CIBLAT STEPHANE; DERY MARTIN; CONSTANTINEAU-FORGET LEA; GRAND-MAITRE CHANTAL; BRUNEAU-LATOUR NICOLAS; SHIPPS GERALD W; COOPER ALAN B; OZA VIBHA; KOSTURA MATTHEW J; LUTHER MICHAEL; LEVINE JEDD 权利人:BANTAM PHARMACEUTICAL LLC 摘要:Disclosed are compounds useful, for example, in 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 formulae (Ia), (Ib), (Ic), (Id) and (Ie), in which R 1 , L 1 , L 2 , Q, L 3 , R 3 , L 4 , R 4 , L 5 , and R 5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.
专利号:US-8691854-B2 优先权日:2005-07-01 标题:Chemical compounds and the uses thereof as a medicine 发明人:CHAIMBAULT CORINNE; DROUOT CYRILLE; JAMOT LAURE; PRUSS REBECCA; SIMON CELINE 权利人:CHAIMBAULT CORINNE; DROUOT CYRILLE; JAMOT LAURE; PRUSS REBECCA; SIMON CELINE; TROPHOS 摘要:The present invention relates to the field of pharmacy, especially the treatment of neurodegenerative diseases. The invention specifically relates to a family of chemical compounds for which a neuroprotective activity has been demonstrated. n Given that certain members of said family are novel compounds which have never been described, the invention relates to said novel products, the synthesis method thereof and certain novel intermediate synthesis products. n The present invention further relates to compositions comprising the compounds of said family, and the use of said compounds as medicaments, especially for the preparation of a medicament for the treatment of neurodegenerative diseases.
专利号:US-4968702-A 优先权日:1989-01-17 标 题 :Substituted quinolinecarboxylic acids 发明人:POLETTO JOHN F; POWELL DENNIS W; BOSCHELLI DIANE H 权利人:AMERICAN CYANAMID CO 摘要:Substituted quinolinecarboxylic acids useful in the treatment of arthritis by inhibiting the progressive joint deterioration characteristic of arthritic disease and for inducing immunosuppression are disclosed. Methods of synthesis and use of the novel compounds are also disclosed.
专利号:CN-103450177-A 优先权日:2012-05-29 标题 :Synthesis and preparation method of a class of metronidazole grafted thiazole hydrazone derivatives
专利号:CN-101735800-B 优先权日:2007-10-17 标 题 :A class of organic electron transport and/or hole blocking material and its synthesis method and application
参考标题:An Efficient Method For The Synthesis Of 2-Thiazoleacetic Acid N-Sulfonyl Amidines 作者:Vladimir G. Il'Kin,Vera S. Berseneva,Pavel а. Slepukhin,Vasiliy а. Bakulev |发布日期:2018.12 摘要:A Three-Step Method Was Designed And Developed On The Basis Of Retrosynthetic Analysis For The Synthesis Of Hybrid Molecules Containing A Thiazole Ring And An N-Sulfonyl Amidine Fragment, Connected By A Methylene Linker. The Mechanism Of The Last Step Involves The Formation Of Intermediate 1,2,3,4-Thiatriazoles And Their Transformation Into The Final Products As A Result Of The Elimination Of Molecular
合成参考文献
摘要:Ayad, T.; Pirat, J.-L.; Virieux, D., Science of Synthesis Knowledge Updates, (2022) 1, 343. 摘要:Tang, R.-Y., Science of Synthesis: Knowledge Updates, (2024) 1, 439.