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1. US20200017537 - Lincosamide derivatives, preparation and use thereof as antimicrobial agent

Office
United States of America
Application Number 16491133
Application Date 09.03.2018
Publication Number 20200017537
Publication Date 16.01.2020
Grant Number 10822366
Grant Date 03.11.2020
Publication Kind B2
IPC
C07H 15/18
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
15Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
18Acyclic radicals, substituted by carbocyclic rings
CPC
C07H 15/18
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
15Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
18Acyclic radicals, substituted by carbocyclic rings
Applicants MIKROBIOLOGICKY USTAV AV CR, V. V. I.
MIKROBIOLOGYICKY USTAV AG CR, V. V. I.
Inventors Jiri Janata
Zdenek Kamenik
Stanislav Kadlcik
Lucie Najmanova
Radek Gazak
Agents Notaro, Michalos & Zaccaria P.C.
Priority Data 2017-137 10.03.2017 CZ
Title
(EN) Lincosamide derivatives, preparation and use thereof as antimicrobial agent
Abstract
(EN)

Lincosamides of general formula I, where R1 is selected from C2-C8 alkyl or C2-C8 alkenyl; R3 is selected from OH, O(C1-C4 alkyl), SH, S(C1-C4 alkyl) or halogen; R4 is H or C1-C3 alkyl; each of R21, R22, R23, R24, R25 is independently selected from the group consisting of H, OH, C1-C4 alkyl, C1-C4 alkenyl, C1-C4 alkynyl, halogen, O(C1-C4 alkyl), O(C1-C4 alkenyl), O(C1-C4 alkynyl), NH2, N(C1-C4 alkyl)2, N(C1-C4 alkenyl)2, N(C1-C4 alkynyl)2; and pharmaceutically acceptable salts thereof. A method of preparation thereof, in particular a biosynthetic method using newly discovered functions of celesticetin biosynthetic proteins Ccb1 and/or Ccb2. Lincosamides of general formula I are suitable for use as antibacterial and antiprotozoal substances.


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