AR105889A1 - Compuestos antibacterianos 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona sustituidos - Google Patents

Compuestos antibacterianos 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona sustituidos

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Publication number
AR105889A1
AR105889A1 ARP160102671A ARP160102671A AR105889A1 AR 105889 A1 AR105889 A1 AR 105889A1 AR P160102671 A ARP160102671 A AR P160102671A AR P160102671 A ARP160102671 A AR P160102671A AR 105889 A1 AR105889 A1 AR 105889A1
Authority
AR
Argentina
Prior art keywords
alkyl
methyl
carbonyloxymethyl
hydroxy
cycloprop
Prior art date
Application number
ARP160102671A
Other languages
English (en)
Original Assignee
Actelion Pharmaceuticals Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Actelion Pharmaceuticals Ltd filed Critical Actelion Pharmaceuticals Ltd
Publication of AR105889A1 publication Critical patent/AR105889A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

La presente solicitud se refiere a compuestos antibacterianos, especialmente para bacterias gram negativas aeróbicas y anaeróbicas. Reivindicación 1: Un compuesto de fórmula (1) donde M es uno de los grupos de fórmula (2), (3) y (4), donde R¹A representa hidrógeno o flúor; R³A representa 3-fluoroazetidin-3-ilo, 3-fluoro-1-metil-azetidin-3-ilo, 1-acetil-3-hidroxiazetidin-3-ilo, 3-fluoro-1-(oxetan-3-il)azetidin-3-ilo, (3-fluoroazetidin-1-il)metilo, (3-hidroxiazetidin-1-il)metilo, (5-(hidroximetil)-2-oxooxazolidin-3-il)metilo, (4-hidroxi-3-fluoropiperidin-1-il)metilo, (4-amino-3-fluoropiperidin-1-il)metilo, (4-hidroxi-3,3-difluoropiperidin-1-il)metilo, (4-amino-3,3-difluoropiperidin-1-il)metilo, (6-amino-3-azabiciclo[3.1.0]hexan-3-il)metilo, (2-oxa-6-azaspiro[3.3]heptan-6-il)metilo, 2-morfolino-1-hidroxietilo, 2-(metilsulfonil)etoxi, (3-hidroxiazetidin-1-il)carboniloximetilo, (4-hidroxipiperidin-1-il)carboniloximetilo, (4-metilpiperazin-1-il)carboniloximetilo, N-(2-hidroxietil)-N-(metil)carbamoiloximetilo, 1-hidroxi-2-[(2-metoxietil)(metil)amino]etilo, azetidin-3-iloxicarbonilaminometil o (N-metilazetidin-3-il)oxicarbonilaminometilo; R¹B representa trans-2-(1,2-dihidroxietil)cicloprop-1-ilo, 1-(metilamino)cicloprop-1-ilo, 1-(dimetilamino)cicloprop-1-ilo, 2-(dimetilaminometil)cicloprop-1-ilo, 1-((3-hidroxiazetidinil)-1-carboniloximetil)cicloprop-1-ilo, 2-(morfolinometil)cicloprop-1-ilo, 1-((4-metilpiperazinil)-1-carboniloximetil)cicloprop-1-ilo, 4-fluoropirrolidin-2-ilo, (2-oxooxazolidin-3-il)metilo, 1-(3-hidroxiazetidina)-1-carboniloximetilo, (4-hidroxipiperidin-1-il)carboniloximetilo, 1-(4-metilpiperazina)-1-carboniloximetil o N-(metilazetidin-3-il)oxicarbonilaminometilo, o R¹B representa un grupo Q, Q siendo uno de los grupos de fórmula (5), (6) y (7), donde XA¹ representa H, metil-d, metil-d2, alquilo C₁₋₄, acetil, w-haloalquilo C₂₋₃, w-hidroxialquilo C₂₋₃, 2,3-dihidroxiprop-1-ilo, 3-hidroxi-2-(hidroximetil)prop-1-ilo, oxetan-3-ilo, tietan-3-ilo, 1,1-dioxidotietan-3-ilo, cicloalquilo C₃₋₆, 3-hidroxiciclobut-1-ilo, tetrahidropiran-4-ilo o cicloalquil C₃₋₆alquilo C₁₋₃, XA²¹ y XA²² cada uno representa de modo independiente H, alquilo C₁₋₄, haloalquilo C₁₋₃ o hidroxi-alquilo C₁₋₃, y XA³ representa H, alquilo C₁₋₃ o halógeno, siempre que si XA¹ representa oxetan-3-ilo, al menos uno de XA²¹, XA²² y XA³ no represente H; XB¹ representa H, alquilo C₁₋₄, w-hidroxialquilo C₂₋₃, cicloalquilo C₃₋₆, oxetan-3-ilo o tetrahidropiran-4-ilo, XB²¹ y XB²² cada uno representa de modo independiente H, alquilo C₁₋₄, haloalquilo C₁₋₃ o hidroxialquilo C₁₋₃, y XB⁴ representa H, halógeno, hidroxi o alquilo C₁₋₃; XC¹ representa H, alquilo C₁₋₄, cicloalquilo C₃₋₆, w-hidroxialquilo C₂₋₃, oxetan-3-ilo o tetrahidropiran-4-ilo, XC² representa H, alquilo C₁₋₄, haloalquilo C₁₋₃ o hidroxialquilo C₁₋₃, XC³ representa H, halógeno, hidroxi, alquilo C₁₋₄, haloalquilo C₁₋₃, hidroxialquilo C₁₋₃, y XC⁴ representa H, alquilo C₁₋₃, halógeno o hidroxi; R¹C representa hidrógeno o flúor; R³C representa un grupo Q tal como se definió con anterioridad; y R¹ representa H, PO₃H₂, SO₃H, fosfonooximetil o el grupo de fórmula (8), donde R² representa alquilamino C₁₋₄alquilo C₁₋₄, [dialquilamino C₁₋₄]alquilo C₁₋₄, fosfonooxi-alquilo C₁₋₄, fosfonooximetoxi, 2-(fosfonooxi-alquil C₁₋₄)-fenilo, (2-(fosfonooxi)-fenil)-alquil C₁₋₄ (especialmente 2-(2-(fosfonooxi)-fenil)-etil) o [2-(fosfonooxi-alquil C₁₋₄)-fenil]-alquilo C₁₋₄); o una sal de este compuesto.
ARP160102671A 2015-09-03 2016-09-01 Compuestos antibacterianos 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona sustituidos AR105889A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP2015070144 2015-09-03

Publications (1)

Publication Number Publication Date
AR105889A1 true AR105889A1 (es) 2017-11-22

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ARP160102671A AR105889A1 (es) 2015-09-03 2016-09-01 Compuestos antibacterianos 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona sustituidos

Country Status (17)

Country Link
US (1) US10314823B2 (es)
EP (1) EP3344630B1 (es)
JP (1) JP2018526391A (es)
KR (1) KR20180049017A (es)
CN (1) CN108137596A (es)
AR (1) AR105889A1 (es)
AU (1) AU2016313794B2 (es)
BR (1) BR112018004343A2 (es)
CA (1) CA2994996A1 (es)
CL (1) CL2018000533A1 (es)
EA (1) EA201890626A1 (es)
HK (1) HK1256614A1 (es)
IL (1) IL257757A (es)
MX (1) MX2018002644A (es)
PH (1) PH12018500323A1 (es)
TW (1) TW201714885A (es)
WO (1) WO2017037221A1 (es)

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Also Published As

Publication number Publication date
BR112018004343A2 (pt) 2018-09-25
US20180250273A1 (en) 2018-09-06
AU2016313794A1 (en) 2018-04-19
AU2016313794B2 (en) 2020-06-04
MX2018002644A (es) 2018-06-20
TW201714885A (zh) 2017-05-01
HK1256614A1 (zh) 2019-09-27
EA201890626A1 (ru) 2018-09-28
KR20180049017A (ko) 2018-05-10
EP3344630A1 (en) 2018-07-11
WO2017037221A1 (en) 2017-03-09
CA2994996A1 (en) 2017-03-09
CL2018000533A1 (es) 2018-06-29
JP2018526391A (ja) 2018-09-13
PH12018500323A1 (en) 2018-08-13
EP3344630B1 (en) 2020-12-09
US10314823B2 (en) 2019-06-11
CN108137596A (zh) 2018-06-08
IL257757A (en) 2018-04-30

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