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-7645754-B2 优先权日:2001-12-20 标题 :Pyrrolopyrimidine A2B selective antagonist compounds, their synthesis and use 发明人:CASTELHANO ARLINDO; MCKIBBEN BRYAN; STEINIG ARNO 权利人:OSI PHARM INC 摘要:The subject invention provides compounds having the structure: n n n n n n n n n n n n wherein,n R 1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O) R a ; R 2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O)R a , or R 1 , R 2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH 2 ) 2 OH or —CH 2 C(â•?O)OH; R 3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C 1 -C 15 )alkyl, (C 1 -C 15 )alkoxy, or —NR a R b ; R 4 is hydrogen or substituted or unsubstituted (C 1 -C 15 )alkyl; R 5 is —(CH 2 ) m OR 6 , —CHNOR 7 , —C(â•?O)NR 8 R 9 , —(CH 2 ) m C(â•?O)OR 10 , —(CH 2 ) k C(â•?O)NR 11 R 12 ;n wherein R 6 is a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R 7 is hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl; R 8 and R 9 are each independently hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl, (C 1 -C 30 )alkylamino, (C 1 -C 30 )alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R 8 , N, and R 9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R 10 is hydrogen or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R 11 , N and R 12 together form a 4-8 membered heterocyclic ring; R a and R b are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3,n nor a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A 2b adenosine receptor in a sbject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.
专利号:CN-109232343-A 优先权日:2018-10-24 标 题 :A method for copper-catalyzed synthesis of aromatic/alkane 2,2,2-trifluoroethyl selenide and its application in pesticides
专利号:US-3076033-A 优先权日:1949-12-17 标 题 :Synthesis of aldehydes 发明人:LESTER FRIEDMAN 权利人:JACOB T BASSECHES
专利号:CN-109232343-B 优先权日:2018-10-24 标 题:A method for copper-catalyzed synthesis of aromatic/alkane 2,2,2-trifluoroethyl selenide and its application in pesticides
专利号:US-7109220-B2 优先权日:2003-11-19 标 题:Amino substituted pyridinyl methanone compounds useful in treating kinase disorders 发明人:LIN RONGHUI; WETTER STEVEN K; LU YANHUA; CONNOLLY PETER J; EMANUEL STUART; GRUNINGER ROBERT H; MIDDLETON STEVEN A 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention provides amino substituted pyridinyl methanone compounds; pharmaceutical compositions comprising the compounds and methods of synthesis thereof. The compounds, which are cyclin dependent kinase (CDK) inhibitors, can be used to treat or ameliorate CDK mediated disorders. The invention thus also provides the therapeutic or prophylactic use of the compounds and/or pharmaceutical compositions to treat such disorders.
参考标题:Carbopalladation Of Nitriles: Synthesis Of 2,3-Diarylindenones And Polycyclic Aromatic Ketones By The Pd-Catalyzed Annulation Of Alkynes And Bicyclic Alkenes By 2-Iodoarenenitriles 作者:Alexandre A. Pletnev,Qingping Tian,Richard C. Larock |发布日期:2002.12.1 摘要:Represents One Of The First Examples Of The Addition Of An Organopalladium Moiety To The Carbon-Nitrogen Triple Bond Of A Nitrile. The Reaction Is Compatible With A Number Of Functional Groups. A Reaction Mechanism, As Well As A Model Accounting For The Electronic Effects Of Substituents On The Aromatic Ring Of The Nitrile, Is Proposed.
合成参考文献
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