Piperazine inhibitors of bacterial gyrase and topoisomerase iv

Michael Givskov; Tim Tolker-Nielsen; Tim Holm Jakobsen; Jens Bo Andersen; Sebastian Thordal Le Quement; Thomas Eiland Nielsen; Thomas Flagstad; Mette Terp Petersen; Jakob Felding

Piperazine inhibitors of bacterial gyrase and topoisomerase iv

Michael Givskov (Inventor), Tim Tolker-Nielsen (Inventor), Tim Holm Jakobsen (Inventor), Jens Bo Andersen (Inventor), Sebastian Thordal Le Quement (Inventor), Thomas Eiland Nielsen (Inventor), Thomas Flagstad (Inventor), Mette Terp Petersen (Inventor), Jakob Felding (Inventor)

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Abstract

This invention relates to a piperazine derivative having the formula (I), wherein R' is selected from -H, -COOH and -CONH2; Ft" is selected from -H, -COOH and -CONH2 with the proviso that when R' is -COOH or -CONH2 then R" is not -COOH or -CONH2, and when R" is -COOH or -CONH2 then R' is not -COOH or -CONH2; A is selected from -(CH2)3-, -(CH2)2CH(OH)-, -CH2-CH=CH- (cis and trans), (a); B is selected from -(CH2)n-, -(CH2)nO-, -(CH2)nS- and -(CH2)n-CH=CH- (cis and trans), (b); and wherein n = 1 -4; and Y is selected from C1-C7 alkyl (straight or branched), C5-C6 cycloalkyi optionally substituted with one or more halogens, thiophene or phenyl optionally substituted with one or more halogens or -C(hal)3 wherein "hal" denotes a halogen, or a pharmaceutically acceptable salt thereof.

Original language	English
IPC	C07D 409/ 14 A I
Patent number	WO2016138988
Filing date	02/03/2015
Country/Territory	International Bureau of the World Intellectual Property Organization (WIPO)
Priority date	02/03/2015
Priority number	EP20150157154
Publication status	Published - 9 Sept 2016

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title = "Piperazine inhibitors of bacterial gyrase and topoisomerase iv",

abstract = "This invention relates to a piperazine derivative having the formula (I), wherein R' is selected from -H, -COOH and -CONH2; Ft{"} is selected from -H, -COOH and -CONH2 with the proviso that when R' is -COOH or -CONH2 then R{"} is not -COOH or -CONH2, and when R{"} is -COOH or -CONH2 then R' is not -COOH or -CONH2; A is selected from -(CH2)3-, -(CH2)2CH(OH)-, -CH2-CH=CH- (cis and trans), (a); B is selected from -(CH2)n-, -(CH2)nO-, -(CH2)nS- and -(CH2)n-CH=CH- (cis and trans), (b); and wherein n = 1 -4; and Y is selected from C1-C7 alkyl (straight or branched), C5-C6 cycloalkyi optionally substituted with one or more halogens, thiophene or phenyl optionally substituted with one or more halogens or -C(hal)3 wherein {"}hal{"} denotes a halogen, or a pharmaceutically acceptable salt thereof.",

author = "Michael Givskov and Tim Tolker-Nielsen and Jakobsen, {Tim Holm} and Andersen, {Jens Bo} and Quement, {Sebastian Thordal Le} and Nielsen, {Thomas Eiland} and Thomas Flagstad and Petersen, {Mette Terp} and Jakob Felding",

year = "2016",

month = sep,

day = "9",

language = "English",

type = "Patent",

note = "WO2016138988; C07D 409/ 14 A I",

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TY - PAT

T1 - Piperazine inhibitors of bacterial gyrase and topoisomerase iv

AU - Givskov, Michael

AU - Tolker-Nielsen, Tim

AU - Jakobsen, Tim Holm

AU - Andersen, Jens Bo

AU - Quement, Sebastian Thordal Le

AU - Nielsen, Thomas Eiland

AU - Flagstad, Thomas

AU - Petersen, Mette Terp

AU - Felding, Jakob

PY - 2016/9/9

Y1 - 2016/9/9

N2 - This invention relates to a piperazine derivative having the formula (I), wherein R' is selected from -H, -COOH and -CONH2; Ft" is selected from -H, -COOH and -CONH2 with the proviso that when R' is -COOH or -CONH2 then R" is not -COOH or -CONH2, and when R" is -COOH or -CONH2 then R' is not -COOH or -CONH2; A is selected from -(CH2)3-, -(CH2)2CH(OH)-, -CH2-CH=CH- (cis and trans), (a); B is selected from -(CH2)n-, -(CH2)nO-, -(CH2)nS- and -(CH2)n-CH=CH- (cis and trans), (b); and wherein n = 1 -4; and Y is selected from C1-C7 alkyl (straight or branched), C5-C6 cycloalkyi optionally substituted with one or more halogens, thiophene or phenyl optionally substituted with one or more halogens or -C(hal)3 wherein "hal" denotes a halogen, or a pharmaceutically acceptable salt thereof.

AB - This invention relates to a piperazine derivative having the formula (I), wherein R' is selected from -H, -COOH and -CONH2; Ft" is selected from -H, -COOH and -CONH2 with the proviso that when R' is -COOH or -CONH2 then R" is not -COOH or -CONH2, and when R" is -COOH or -CONH2 then R' is not -COOH or -CONH2; A is selected from -(CH2)3-, -(CH2)2CH(OH)-, -CH2-CH=CH- (cis and trans), (a); B is selected from -(CH2)n-, -(CH2)nO-, -(CH2)nS- and -(CH2)n-CH=CH- (cis and trans), (b); and wherein n = 1 -4; and Y is selected from C1-C7 alkyl (straight or branched), C5-C6 cycloalkyi optionally substituted with one or more halogens, thiophene or phenyl optionally substituted with one or more halogens or -C(hal)3 wherein "hal" denotes a halogen, or a pharmaceutically acceptable salt thereof.

M3 - Patent

M1 - WO2016138988

Y2 - 2015/03/02

ER -

Piperazine inhibitors of bacterial gyrase and topoisomerase iv

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