AR105848A1 - Derivados heterocíclicos antibacterianos - Google Patents

Derivados heterocíclicos antibacterianos

Info

Publication number
AR105848A1
AR105848A1 ARP160102629A ARP160102629A AR105848A1 AR 105848 A1 AR105848 A1 AR 105848A1 AR P160102629 A ARP160102629 A AR P160102629A AR P160102629 A ARP160102629 A AR P160102629A AR 105848 A1 AR105848 A1 AR 105848A1
Authority
AR
Argentina
Prior art keywords
4alkyl
cycloprop
phosphonooxy
carbonyloxymethyl
phenyl
Prior art date
Application number
ARP160102629A
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 AR105848A1 publication Critical patent/AR105848A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/423Oxazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58Benzoxazoles; Hydrogenated benzoxazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/68Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicación 1: Un compuesto de la fórmula (1) donde: V representa O ó S; R² y R³ representan, de manera independiente, hidrógeno o flúor; y M es uno de los grupos de fórmula (2) y (3), donde en el grupo de fórmula (2): A representa un enlace o -CºC-; R¹A representa hidrógeno, o halógeno; R²A representa hidrógeno, o halógeno; y R³A representa C₁₋₃alcoxi; hidroxi-C₁₋₄alquilo; o RNA¹RNA²N-C₁₋₃alquilo, donde RNA¹ y RNA² representan, de manera independiente, hidrógeno o C₁₋₃alquilo; o RNA¹ y RNA² junto con el nitrógeno al cual están unidos forman un anillo saturado de 4 a 6 miembros que opcionalmente contiene un átomo de anillo de oxígeno, donde dicho anillo está no sustituido, o monosustituido con flúor; y donde en el grupo de fórmula (3): R¹B representa hidroxi-C₁₋₄alquilo; 1-(3-hidroxiazetidina)-1-carboniloximetilo; 1-hidroximetil-cicloprop-1-ilo, o un grupo que es uno de sus profármacos, donde dicho grupo es 1-((fosfonooxi)metilo)-cicloprop-1-ilo, 1-[(di(C₁₋₄alquiloamino)-C₁₋₃alquilo-carboniloximetil]-cicloprop-1-ilo, 1-{[(2-(fosfonooxi-C₁₋₄alquilo)-fenilo)-C₁₋₄alquilo]-carboniloximetil}-cicloprop-1-ilo, 1-{[2-(fosfonooxi-C₁₋₄alquilo)-fenilo]-carboniloximetil}-cicloprop-1-ilo, o 1-{[(2-fosfonooxi-fenilo)-C₁₋₄alquilo]-carboniloximetil}-cicloprop-1-ilo; trans-2-hidroximetil-cicloprop-1-ilo, o un grupo que es uno de sus profármacos donde dicho grupo es trans-2-(fosfonooximetilo)-cicloprop-1-ilo, trans-2-[(diC₁₋₄alquiloamino)-C₁₋₃alquilo-carboniloximetil]-cicloprop-1-ilo, trans-2-{[(2-(fosfonooxi-C₁₋₄alquilo)-fenilo)-C₁₋₄alquilo]-carboniloximetil}-cicloprop-1-ilo, trans-2-{[2-(fosfonooxi-C₁₋₄alquilo)-fenilo]-carboniloximetil}-cicloprop-1-ilo, o trans-2-{[(2-fosfonooxi-fenilo)-C₁₋₄alquilo]-carboniloximetil}-cicloprop-1-ilo; 2-flúor-2-hidroximetil-cicloprop-1-ilo, o un grupo que es uno de sus profármacos, donde dicho grupo es 2-flúor-2-(fosfonooximetilo)-cicloprop-1-ilo, 2-flúor-2-[(diC₁₋₄alquiloamino)-C₁₋₃alquilo-carboniloximetil]-cicloprop-1-ilo, 2-flúor-2-{[(2-(fosfonooxi-C₁₋₄alquilo)-fenilo)-C₁₋₄alquilo]-carboniloximetil}-cicloprop-1-ilo, 2-flúor-2-{[2-(fosfonooxi-C₁₋₄alquilo)-fenilo]-carboniloximetil}-cicloprop-1-ilo, o 2-flúor-2-{[(2-fosfonooxi-fenilo)-C₁₋₄alquilo]-carboniloximetil}-cicloprop-1-ilo; 3-hidroxi-oxetan-3-ilo; trans-2-(1,2-dihidroxietilo)cicloprop-1-ilo; trans-(cis-3,4-dihidroxi)-ciclopent-1-ilo; RNB¹RNB²N-C₁₋₃alquilo, donde RNB¹ y RNB² representan, de manera independiente, hidrógeno o C₁₋₃alquilo; 1-(RNB³RNB⁴N)-cicloprop-1-ilo, donde RNB³ y RNB⁴ representan, de manera independiente, hidrógeno o C₁₋₃alquilo, o RNB³ representa hidrógeno y RNB⁴, (fosfonooxi)metoxi-carbonilo; azetidin-3-ilo, donde dicho azetidin-3-ilo está no sustituido, o mono- o di-sustituido, donde, si se presenta, un sustituyente se une en la posición 1 de dicho grupo azetidin-3-ilo, donde dicho sustituyente es seleccionado de C₁₋₃alquilo, C₃₋₄cicloalquilo, oxetan-3-ilo, w-flúor-C₂alquilo, o w-hidroxi-C₂₋₄alquilo; y/o un sustituyente es flúor unido en la posición 3 de dicho grupo azetidin-3-ilo; R¹ representa hidrógeno, o R¹ representa -PO₃H₂, -SO₃H, fosfonooximetilo, o el grupo L representado por la fórmula (4), donde R⁴ representa C₁₋₄alquiloaminoC₁₋₄alquilo, diC₁₋₄alquiloaminoC₁₋₄alquilo, fosfonooxiC₁₋₄alquilo, fosfonooximetoxi, 2-(fosfonooxi-C₁₋₄alquilo)-fenilo, [2-(fosfonooxi-C₁₋₄alquilo)-fenilo]-C₁₋₄alquilo, o (2-(fosfonooxi)-fenilo)-C₁₋₄alquilo; o una de sus sales farmacéuticamente aceptables.
ARP160102629A 2015-08-31 2016-08-29 Derivados heterocíclicos antibacterianos AR105848A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP2015069837 2015-08-31

Publications (1)

Publication Number Publication Date
AR105848A1 true AR105848A1 (es) 2017-11-15

Family

ID=56893949

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP160102629A AR105848A1 (es) 2015-08-31 2016-08-29 Derivados heterocíclicos antibacterianos

Country Status (10)

Country Link
US (1) US20180251434A1 (es)
EP (1) EP3344609A1 (es)
JP (1) JP2018527349A (es)
KR (1) KR20180043355A (es)
CN (1) CN107922361A (es)
AR (1) AR105848A1 (es)
CA (1) CA2989968A1 (es)
MA (1) MA43883A (es)
TW (1) TW201718529A (es)
WO (1) WO2017037039A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR099612A1 (es) 2014-03-04 2016-08-03 Actelion Pharmaceuticals Ltd Derivados antibacterianos de 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona
AR105646A1 (es) 2015-08-11 2017-10-25 Actelion Pharmaceuticals Ltd Agentes antibacterianos de 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona sustituida
AR105889A1 (es) 2015-09-03 2017-11-22 Actelion Pharmaceuticals Ltd Compuestos antibacterianos 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona sustituidos

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103717582B (zh) * 2011-04-08 2015-09-30 辉瑞大药厂 用作抗菌剂的异*唑衍生物
MX2013011432A (es) * 2011-04-08 2013-12-09 Pfizer Derivados de imidazol, pirazol, y triazol utiles como agentes antibacterianos.
AR097617A1 (es) * 2013-09-13 2016-04-06 Actelion Pharmaceuticals Ltd Derivados antibacterianos del 2h-indazol
US9624206B2 (en) * 2013-12-19 2017-04-18 Actelion Pharmaceuticals Ltd Antibacterial 1H-indazole and 1H-indole derivatives
AR099612A1 (es) * 2014-03-04 2016-08-03 Actelion Pharmaceuticals Ltd Derivados antibacterianos de 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona
BR112017010474A2 (pt) * 2014-11-19 2017-12-26 Actelion Pharmaceuticals Ltd derivados antibacterianos de benzotiazol

Also Published As

Publication number Publication date
MA43883A (fr) 2018-12-05
JP2018527349A (ja) 2018-09-20
EP3344609A1 (en) 2018-07-11
CN107922361A (zh) 2018-04-17
US20180251434A1 (en) 2018-09-06
CA2989968A1 (en) 2017-03-09
WO2017037039A1 (en) 2017-03-09
KR20180043355A (ko) 2018-04-27
TW201718529A (zh) 2017-06-01

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