CAS: 224452-66-8; (3Ar,4R,5R,7S,8S,9R,9As,12R)-8-Hydroxy-4,7,9,12-Tetramethyl-5-((3-(((3-Exo)-8-Methyl-8-Azabicyclo[3.2.1]Octan-3-yl)Thio)Prop-1-En-2-yl)Oxy)-7-Vinyloctahydro-4,9A-Propanocyclopenta[8]Annulen-3(3Ah)-One

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CAS号848130-83-6 8-Methyl-8-azab... | CAS号60924-38-1 截短侧耳素-22-甲磺酸酯

专利信息

专利号:US-12221452-B2
优先权日:2017-10-04
标题:Synthesis of cantharidin
发明人：DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
权利人:VERRICA PHARMACEUTICALS INC
摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

专利号:US-11447742-B2
优先权日:2016-02-09
标题 :Compositions and methods for activation and overexpression of secondary metabolites in microorganisms
发明人：HAMILL DAKOTA BENJAMIN; COTTER JAKE J
权利人:PROSPECTIVE RES INC
摘要:Methods and compositions herein provide non-naturally occurring γ-butyrolactones (GBLs) in racemic mixtures that increase efficiency and effectiveness of screening for production of antibiotics, and enhance yields and express silent pathways. Non-naturally occurring GBLs were synthesized and found to stimulate antibiotic production in several different streptomycete strains. Antibiotic production by Streptomyces coelicolor was induced by a racemic mixture of non-cognate stereoisomers of VB-D, seven of which are non-naturally occurring. Further, novel A-factor-type GBL analogs stimulated antibiotic production in S. coelicolor . Synthesis in response to the treatment with the non-cognates GBL was observed for known compounds including undecylprodigiosin, desferrioxamine and streptorubin B, as was synthesis of a compound of unknown structure. A group of 37 additional microbial strains was screened by principal component analysis to determine optimal concentrations of each of a panel of four non-cognate synthetic GBLs for addition to cultures with optimal stimulation of secondary metabolites, and large scale fermentations were analyzed and product enhancement by the GBLs was observed.

专利号:US-10472663-B2
优先权日:2015-01-21
标 题:Procedure for the rapid determination of bacterial susceptibility to antibiotics that inhibit protein synthesis
发明人：FERNÃ?NDEZ GARCÃ?A JOSÉ LUIS; GOSÃ?LVEZ BERENGUER JAIME; BOU ARÉVALO GERMÃ?N; TAMAYO NOVAS MARIA; SANTISO BRANDARIZ REBECA; OTERO FARIÑA FÃ?TIMA MARÃ?A
权利人:ABM TECH LLC
摘要:The present invention relates to a method for the rapid evaluation of bacterial susceptibility or non-susceptibility of bacteria to antibiotics that inhibit protein synthesis. The rationale is to identify bacterial responses that depend or are influenced by protein synthesis. If this response is prevented or reduced by the antibiotic that inhibits the protein synthesis, the bacteria are susceptible to this antibiotic. Otherwise, if the response keeps similar despite the incubation with the antibiotic, the bacteria are not susceptible or resistant to this antibiotic. These responses could be determined at the DNA lev-el, cell wall level, morphological level or any other experimental approach, including metabolic, bio-chemical, physiological or genetic processes.

专利号:US-8461188-B2
优先权日:2011-10-20
标题 :Therapeutic combination of daptomycin and protein synthesis inhibitor antibiotic, and methods of use
发明人：BARTIZAL KENNETH F; LOCKE JEFFREY B; SHAW KAREN JOY; PROKOCIMER PHILIPPE G
权利人:TRIUS THERAPEUTICS INC
摘要:A therapeutic combination comprises an antibacterially effective amount of daptomycin, and an amount of protein synthesis inhibitor antibiotic effective to prevent the development of daptomycin non-susceptibility in bacteria. Related combination therapies and methods are also included.

专利号:US-10947203-B2
优先权日:2016-03-25
标题 :1,4,5-substituted 1,2,3-triazole analogues as antagonists of the pregnane X receptor
发明人：CHEN TAOSHENG; LIN WENWEI; WANG YUEMING
权利人:ST JUDE CHILDRENS RES HOSPITAL; ST JUDE CHILDRENS RSEARCH HOSPITAL
摘要:In an aspect, the invention relates to 1,4,5-substituted 1,2,3-triazole and 1,2,4,5-substituted imidazoles having a structure represented by a formula: n nwhich are modulators the pregnane X receptor (“PXRâ€?); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of modulating an adverse drug reaction in a mammal using the compounds and pharmaceutical compositions; methods of treatment of a disorder of uncontrolled cellular proliferation, such as a cancer, using the compounds and pharmaceutical compositions; methods of modulating pregnane X receptor activity in a mammal using the compounds and pharmaceutical compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

专利号:US-9879050-B2
优先权日:2013-08-30
标 题 :Substituted urea depsipeptide analogs as activators of the CLPP endopeptidase
发明人：LEE RICHARD E; ZHAO YING; GRIFFITH ELIZABETH; ZHENG ZHONG; SINGH AMAN P
权利人:ST JUDE CHILDREN'S RES HOSPITAL
摘要:In one aspect, the invention relates to substituted urea depsipeptide analogs, derivatives thereof, and related compounds, which are useful as activators the ClpP endopeptidease; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating infectious disease using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.