CAS: 18472-51-0; 1,1'-Hexamethylenebis[5-(P-Chlorophenyl)Biguanide] (2R,3S,4R,5R)-2,3,4,5,6-Pentahydroxyhexanoic Acid(1:2)

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:WO-2017137818-A1
优先权日:2016-02-12
标 题 :Synthesis and application of an antimicrobial active
发明人：K RAKESH RATNAM; SARVIYA SAMIR
权利人:SALICYLATES & CHEMICALS
摘要:The disclosure Synthesis & Application of a Novel Antimicrobial active provides a method of synthesis of organic complex starting from fatty acid with a free base bioactive molecule containing nitrogen atoms. The reaction is usually conducted in refluxing alcohol. The product is synthesized by a acid-base reaction whereby the acid molecule is capable of donating a proton, to the free base molecule resulting in the formation of the desired complex. These complexes are very effective antimicrobial active against a variety of bacteria, fungi, protozoa, helminths and viruses. The process is suitable for large-scale synthesis and involves simple and high-yielding techno feasible chemical transformations using low-cost commercially available raw materials. The complex has wide spread use in human personal care, industries and household applications, as the disclosed chemical has antimicrobial activity against gram positive, gram negative bacteria, yeast, mold, fungi.

专利号:US-8557979-B2
优先权日:2004-06-10
标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation
发明人：CHOI WOO-BAEG; KOWALIK EWA
权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC
摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

专利号:US-2007212419-A1
优先权日:2006-02-18
标 题 :Synthesis of biocompatible nanocomposite hydrogels as a local drug delivery system
发明人：BAKO JOZSEF; SZEPESI MARTA; VERES ADRIENN J; CSERHATI CSABA; BORBELY ZSUZSA M; HEGDUS CSABA; BORBELY JANOS
权利人:BAKO JOZSEF; SZEPESI MARTA; VERES ADRIENN J; CSERHATI CSABA; BORBELY ZSUZSA M; HEGDUS CSABA; BORBELY JANOS
摘要:Nanocomposite biocompatible hydrogels (NCHGs) may be synthesised as model systems for in situ cured local drug delivery devices for treatment of inter alia periodontal infections. The composite includes the following components: nanoparticles (NPs), a matrix gel, and chlorhexidine (CHX) or other antibacterial drug. The NPs were obtained by free radical initiated copolymerization of the monomers, 2-hydroxyethyl methacrylate (HEMA) and polyethyleneglycol dimethacrylate (PEGDMA), in aqueous solution. The same monomers were used to prepare crosslinked matrices by photopolymerization. NCHGs were obtained by mixing NPs, monomers, and drug in an aqueous solution then crosslinked by photopolymerization.

专利号:US-10933051-B2
优先权日:2017-06-09
标 题 :Carbapenem compounds and compositions for the treatment of bacterial infections
发明人：CHOI WOO-BAEG; TOMIOKA TAKASHI; JOO HYUNG-YEUL; TRUONG PHONG; MIN BRIAN
权利人:FOB SYNTHESIS INC
摘要:The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.

专利号:US-9987208-B2
优先权日:2013-04-04
标题 :Elastin synthesis/regeneration promoting agent
发明人：NISHIZAKI TOMOYUKI; TANAKA AKITO
权利人:NISHIZAKI BIOINFORMATION RES INSTITUTE
摘要:8-[2-(2-Pentyl-cyclopropylmethyl)-cyclopropyl]-octanoic acid (DCP-LA) has an action to promote synthesis and regeneration of elastin, and is useful as an agent for the prophylaxis or improvement of wrinkles, and an anti-aging drug.