Invention Grant
- Patent Title: Antibacterial 1H-indazole and 1H-indole derivatives
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Application No.: US15106790Application Date: 2014-12-18
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Publication No.: US09624206B2Publication Date: 2017-04-18
- Inventor: Gaelle Chapoux , Jean-Christophe Gauvin , Christian Hubschwerlen , Azely Mirre , Etienne Ochala , Jean-Luc Specklin , Jean-Philippe Surivet
- Applicant: ACTELION PHARMACEUTICALS LTD
- Applicant Address: CH Allschwil
- Assignee: ACTELION PHARMACEUTICALS LTD
- Current Assignee: ACTELION PHARMACEUTICALS LTD
- Current Assignee Address: CH Allschwil
- Agency: Arent Fox LLP
- Priority: EP13198338 20131219
- International Application: PCT/EP2014/078384 WO 20141218
- International Announcement: WO2015/091741 WO 20150625
- Main IPC: C07D409/06
- IPC: C07D409/06 ; C07D231/56 ; C07D209/08 ; C07D405/06 ; C07D403/12 ; C07D403/06

Abstract:
The invention relates to antibacterial compounds of formula I wherein X is N or CH; R1 is H or halogen; R2 is alkynyloxy or the group M; R3 is H or halogen; M is one of the groups MA and MB represented below wherein A is a bond, CH2CH2, CH═CH or C≡C; R1A is H or halogen; R2A is H, alkoxy or halogen; R3A is H, alkoxy, hydroxyalkoxy, alkoxyalkoxy, thioalkoxy, trifluoromethoxy, amino, hydroxyalkyl, 2-hydroxyacetamido, 1-aminocyclopropyl, 1-hydroxymethyl-cycloprop-1-yl, 1-((phosphonooxy)methyl)cyclopropyl, 1-(((dimethylglycyl)oxy)methyl)cyclopropyl, trans-2-hydroxymethyl-cycloprop-1-yl, 1,2-dihydroxyethyl, 3-hydroxyoxetan-3-yl, 3-(hydroxyalkyl)oxetan-3-yl, 3-aminooxetan-3-yl, 3-hydroxythietan-3-yl, morpholin-4-ylalkoxy, morpholin-4-yl-alkyl, oxazol-2-yl or [1,2,3]triazol-2-yl; and R1B is hydroxyalkyl, dihydroxyalkyl, aminoalkyl, 1-hydroxymethyl-cycloprop-1-yl, 1-aminomethyl-cycloprop-1-yl, trans-2-hydroxymethyl-cycloprop-1-yl, 3-hydroxyoxetan-3-yl, 3-hydroxythietan-3-yl, 1-(2-hydroxyacetyl)azetidin-3-yl, 1-(2-aminoacetyl)azetidin-3-yl, 1-glycylazetidin-3-yl, 1-(2-amino-2-methylpropanoyl)azetidin-3-yl, 3-(2-aminoacetamido)cyclopentyl, trans-(cis-3,4-dihydroxy)-cyclopent-1-yl or 3-hydroxymethylbicyclo[1,1,1]pentan-1-yl; and salts thereof.
Public/Granted literature
- US20170029411A1 ANTIBACTERIAL 1H-INDAZOLE AND 1H-INDOLE DERIVATIVES Public/Granted day:2017-02-02
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