专利号:US-8535689-B2 优先权日:2007-10-01 标题 :Identification of bacterial autoinducer and use in treating bacterial pathogenicity 发明人:BASSLER BONNIE; SEMMELHACK MARTIN; HIGGINS DOUGLAS A; BOLITHO MEGAN EILEEN; KRAML KRISTINA M; NG WAI-LEUNG 权利人:BASSLER BONNIE; SEMMELHACK MARTIN; HIGGINS DOUGLAS A; BOLITHO MEGAN EILEEN; KRAML KRISTINA M; NG WAI-LEUNG; UNIV PRINCETON 摘要:A bacterial autoinducer, CAI-1, was purified and its structure identified. Methods for synthesis of the autoinducer and its analogues were elucidated. Methods of using the autoinducer or its analogues for treating bacterial pathogenicity and bio film formation are described. Methods for prevention and treatment of cholera are described. Synthetic (S)-3-hydroxytridecan-4-one functions as well as natural CAI-1 in repressing production of the virulence factor toxin co-regulated pilus (TCP). Strategies are described to manipulate bacterial quorum sensing in the clinical arena.
专利号:US-8030496-B2 优先权日:2005-02-17 标 题:Intermediate compound for synthesis of viridiofungin a derivative 发明人:KATO TATSUYA; KIMURA NOBUAKI; MIZUTANI AKEMI; MAKINO TOSHIHIKO; KAWASAKI KENICHI; FUKUDA HIROSHI; KOMIYAMA SUSUMU; TSUKUDA TAKUO 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:A method whereby a compound having HCV replication inhibitory activity and desired optical activity can be synthesized selectively and at high yield in a small number of steps by using a compound having a specific chiral auxiliary as a starting compound is provided. n A compound represented by the formula (1-8): n n n n n n n n n n n n wherein Y represents a group represented by the following formula: n n n n n n n n n n n n n n n n Q represents a protected carbonyl group; D represents —(CH 2 ) m —R′, etc.; and n represents an integer of 0 to 10.
专利号:US-6749778-B2 优先权日:2001-03-15 标题:Process for the synthesis of organomagnesium compounds using catalysts 发明人:BOGDANOVIC BORISLAV; SCHWICKARDI MANFRED 权利人:STUDIENGESELLSCHAFT KOHLE MBH 摘要:A process for the preparation of organomagnesium compounds from organic halides and magnesium metal in the presence of transition metal catalysts using an activity-enhancing main group metal component. The latter is a compound of a metal of Periodic Table groups 1, 2 or 13 in which elements of Periodic Table groups 14-17 or hydrogen are bonded to the metal. Some of these additional components may also be formed in situ.
专利号:US-2023151034-A1 优先权日:2020-03-17 标题:Peptidomimetic n5-methyl-n2-(nonanoyl-l-leucyl)-l-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds as inhibitors of norovirus and coronavirus replication 发明人:JACOBSON IRINA C; LEE SAM SK; PIZARRO NOVOA JUAN CARLOS 权利人:COCRYSTAL PHARMA INC 摘要:Peptidomimetic N5-methyl-N2-(nonanoyl-L-leucyl)-L-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds for use in methods of inhibiting the replication of noroviruses and coronaviruses in a biological sample or patient, for use in reducing the amount of noroviruses or coronaviruses in a biological sample or patient, and for use in treating norovirus and coronavirus in a patient, comprising administering to said biological sample or patient a safe and effective amount of a compound represented by formulae I or II, or a pharmaceutically acceptable salt thereof. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. page 99 to page 271; examples 1 to 3; compounds A1 to A104 and B1 to B66; tables A to E).
专利号:US-5936132-A 优先权日:1994-03-11 标题 :Alkene intermediates and synthesis thereof 发明人:MATSUMOTO MASAKATSU 摘要:A chemiluminescent 1,2-dioxetane derivative having a formula (I): ##STR1## wherein R 1 and R 4 each represent, individually, hydrogen, an alkyl group, an alkoxyl group, a hydroxyl group, or --OS;(R 9 R 10 R 11 ) in which R 9 , R 10 and R 11 each represent an alkyl group; R 2 , R 3 , R 5 and R 6 each represent, individually, hydrogen or an alkyl group, provided that R 2 , R 3 , R 5 and R 6 each cannot be hydrogen at the same time, and that R 2 and R 3 , and R 5 and R 6 , each taken together, can form a cycloalkyl group; R 7 represents an alkyl group; R 8 represents hydrogen, an alkoxyl group, a phosphate salt group, or --OSi(R 9 R 10 R 11 ); intermediates for synthesizing the above 1,2-dioxetane derivative; and methods of producing the intermediates are provided.
专利号:US-9663429-B2 优先权日:2013-11-20 标题 :Vitamin D analogues of pharmaceutical interest 发明人:PEREZ FERNANDEZ ROMAN; SEOANE RUZO SAMUEL; MOURIÑO MOSQUERA ANTONIO; MAESTRO SAAVEDRA MIGUEL; CASTELAO FERNANDEZ JOSE ESTEBAN; GOGOI PRANJAL 权利人:UNIV SANTIAGO COMPOSTELA; UNIV DA CORUÑA; SERVIZO GALEGO DE SAUDE (SERGAS); UNIV CORUNA 摘要:The present invention relates to compounds of pharmaceutical interest. More particularly, it relates to compounds of formula (I), to processes for obtaining thereof, to the intermediates of their synthesis and processes for obtaining the latter. The compounds of formula (I) have a certain affinity with the vitamin D receptor, they are active in a similar order to 1,25α-dihydroxyvitamin D 3 (1,25D), with the advantage of producing less or no hypercalcemia.
摘要:Oshima, K., Science of Synthesis, (2004) 7, 590. 摘要:Koutentis, P. A., Science of Synthesis, (2004) 13, 321. 摘要:Seela, F.; Ramzaeva, N.; Rosemeyer, H., Science of Synthesis, (2004) 16, 1075. 摘要:Braverman, S.; Cherkinsky, M.; Birsa, M. L., Science of Synthesis, (2005) 18, 78. 摘要:Braverman, S.; Cherkinsky, M.; Birsa, M. L., Science of Synthesis, (2005) 18, 182.