AR109774A1 - Compuestos heterocíclicos y su uso en la prevención o el tratamiento de infecciones bacterianas - Google Patents

Compuestos heterocíclicos y su uso en la prevención o el tratamiento de infecciones bacterianas

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Publication number
AR109774A1
AR109774A1 ARP170102732A ARP170102732A AR109774A1 AR 109774 A1 AR109774 A1 AR 109774A1 AR P170102732 A ARP170102732 A AR P170102732A AR P170102732 A ARP170102732 A AR P170102732A AR 109774 A1 AR109774 A1 AR 109774A1
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AR
Argentina
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nq1q2
heterocycle
nq1c
nhq3
different
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ARP170102732A
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English (en)
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Mutabilis
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    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • A61K31/546—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine containing further heterocyclic rings, e.g. cephalothin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

Reivindicación 1: Un compuesto de la fórmula (1), donde R¹ representa un heterociclo de 5 miembros, opcionalmente sustituido con uno o varios T¹, saturado, parcialmente insaturado o aromático que comprende al menos un átomo de nitrógeno, estando ligado el heterociclo con la estructura por el átomo de nitrógeno, al menos uno de los átomos de nitrógeno puede estar cuaternizado; R² representa -SO₃H, -CFHCOOH o -CF₂COOH; T¹, igual o diferente, representa, de modo independiente, un átomo de flúor; =O; -C(O)Q¹; -(CH₂)ₘ-S(O)₂-NQ¹Q²; -(CH₂)ₘ-C(=NOQ¹)Q³; -(X)-(CH₂)ₚ-S(O)₂NQ¹Q²; -C(O)-(CH₂)ₙ-S(O)₂NQ¹Q²; -(CH₂)ₘ-O-(CH₂)ₚ-O-(CH₂)ₚ-NQ¹Q²; -(CH₂)ₘOQ¹; -(CH₂)ₘ-CN; -(CH₂)ₘ-OC(O)Q¹; -(CH₂)ₘ-C(O)OQ¹; -(CH₂)ₘ-OC(O)OQ¹; -(CH₂)ₘ-OC(O)NQ¹Q²; -(CH₂)ₘ-C(O)NQ¹Q²; -(CH₂)ₘ-C(O)ONQ¹Q²; -(CH₂)ₘ-C(O)NQ¹OQ²; -(CH₂)ₘ-C(O)NQ¹-NQ¹Q²; -(CH₂)ₘ-NQ¹C(O)Q²; -(CH₂)ₘ-NQ¹S(O)₂NQ¹Q²; -(CH₂)ₘ-NQ¹S(O)₂Q²; -(CH₂)ₘ-NQ¹C(O)OQ²; -(CH₂)ₘ-NQ¹C(O)NQ¹Q²; -(CH₂)ₘ-NQ¹Q²; -(CH₂)ₘ-NH-C(NHQ³)=NQ⁴; -(CH₂)ₘ-NH-CH=NQ³; -(CH₂)ₘ-C(NHQ³)=NQ⁴; -(X)-(CH₂)ₚOQ¹; -(X)-(CH₂)ₙ-CN; -(X)-(CH₂)ₚ-OC(O)Q¹; -(X)-(CH₂)ₙ-C(O)OQ¹; -(X)-(CH₂)ₚ-OC(O)OQ¹; -(X)-(CH₂)ₚ-OC(O)NQ¹Q²; -(X)-(CH₂)ₙ-C(O)NQ¹Q²; -(X)-(CH₂)ₙ-C(O)ONQ¹Q²; -(X)-(CH₂)ₙ-C(O)NQ¹OQ²; -(X)-(CH₂)ₙ-C(O)NQ¹-NQ¹Q²; -(X)-(CH₂)ₚ-NQ¹C(O)Q²; -(X)-(CH₂)ₚ-NQ¹S(O)₂NQ¹Q²; -(X)-(CH₂)ₚ-NQ¹S(O)₂Q²; -(X)-(CH₂)ₚ-NQ¹C(O)OQ²; -(X)-(CH₂)ₚ-NQ¹C(O)NQ¹Q²; -(X)-(CH₂)ₚ-NQ¹Q²; -(X)-(CH₂)ₚ-NH-C(NHQ³)=NQ⁴; -(X)-(CH₂)ₚ-NH-CH=NQ³; -(X)-(CH₂)ₙ-C(NHQ³)=NQ⁴; -C(O)-(CH₂)ₙOQ¹; -C(O)-(CH₂)ₙ-CN; -C(O)-(CH₂)ₙ-OC(O)Q¹; -C(O)-(CH₂)ₙ-C(O)OQ¹; -C(O)-(CH₂)ₙ-OC(O)OQ¹; -C(O)-(CH₂)ₙ-OC(O)NQ¹Q²; -C(O)-(CH₂)ₙ-C(O)NQ¹Q²; -C(O)-(CH₂)ₙ-C(O)ONQ¹Q²; -C(O)-(CH₂)ₙ-C(O)NQ¹OQ²; -C(O)-(CH₂)ₙ-C(O)NQ¹-NQ¹Q²; -C(O)-(CH₂)ₙ-NQ¹C(O)Q²; -C(O)-(CH₂)ₙ-NQ¹S(O)₂NQ¹Q²; -C(O)-(CH₂)ₙ-NQ¹S(O)₂Q²; -C(O)-(CH₂)ₙ-NQ¹C(O)OQ²; -C(O)-(CH₂)ₙ-NQ¹C(O)NQ¹Q²; -C(O)-(CH₂)ₙ-NQ¹Q²; -C(O)-(CH₂)ₙ-NH-C(NHQ³)=NQ⁴; -C(O)-(CH₂)ₙ-NH-CH=NQ³; -C(O)-(CH₂)ₙ-C(NHQ³)=NQ⁴ o T¹, igual o diferente, representa, de modo independiente, un heterociclo no sustituido o sustituido con uno o varios T², -(CH₂)ₘ-(heterociclo de 4, 5 ó 6 miembros saturado, parcial o totalmente insaturado o aromático); -(X)-(CH₂)ₘ-(heterociclo de 4, 5 ó 6 miembros saturado, parcial o totalmente insaturado o aromático); alquilo C₁₋₃; fluoroalquilo C₁₋₃; -(X)-alquilo C₁₋₃; -(X)-fluoroalquilo C₁₋₃; -(CH₂)ₘ-cicloalquilo C₃₋₆; -(X)-(CH₂)ₘ-cicloalquilo C₃₋₆; -(CH₂)ₘ-ciclofluoroalquilo C₃₋₆; -(X)-(CH₂)ₘ-ciclofluoroalquilo C₃₋₆; -C(O)-(CH₂)ₘ-(heterociclo de 4, 5 ó 6 miembros saturado, parcial o totalmente insaturado o aromático); -C(O)-alquilo C₁₋₃; -C(O)-fluoroalquilo C₁₋₃; -C(O)O-fluoroalquilo C₁₋₃; -C(O)-(CH₂)ₘ-cicloalquilo C₃₋₆; -C(O)-(CH₂)ₘ-cicloalquilo C₃₋₆; -C(O)-(CH₂)ₘ-ciclofluoroalquilo C₃₋₆; -C(O)-(CH₂)ₘ-ciclofluoroalquilo C₃₋₆; T², igual o diferente, representa, de modo independiente, -OH; -NH₂; -CONH₂; Q¹ y Q², iguales o diferentes, representan, de modo independiente, un átomo de hidrógeno; -(CH₂)ʳ-NHQ³; -(CH₂)ʳ-NH-C(NHQ³)=NQ⁴; -(CH₂)ʳ-NH-CH=NQ³; (CH₂)ₙ-C(NHQ³)=NQ⁴; -(CH₂)ʳ-OQ³; -(CH₂)ₙ-CONHQ³; o un alquilo C₁₋₃ no sustituido o sustituido con uno o varios T²; fluoroalquilo C₁₋₃; heterociclo saturado, parcial o totalmente insaturado o aromático-(CH₂)ₘ-(de 4, 5 ó 6 miembros que comprende al menos un átomo de nitrógeno); o Q¹, Q² y el átomo de nitrógeno al que están unidos, forman juntos un heterociclo no sustituido o sustituido con uno o varios T², saturado o parcialmente insaturado de 4, 5 ó 6 miembros que comprende 1, 2 ó 3 heteroátomos; Q³ y Q⁴, iguales o diferentes, representan, de modo independiente, un átomo de hidrógeno o alquilo C₁₋₃; m, igual o diferente, representa, de modo independiente, 0, 1, 2 ó 3; n, igual o diferente, representa, de modo independiente, 1, 2 ó 3; p, igual o diferente, representa, de modo independiente, 2 ó 3; r es 1, 2 ó 3 cuando el (CH₂)ʳ está directamente ligado con un átomo de carbono o 2 ó 3 de otro modo, con preferencia, r es 2 ó 3; X, igual o diferente, representa, de modo independiente, O; S; S(O); S(O)₂ o N(Q³); donde cualquier átomo de carbono presente dentro de un grupo seleccionado de alquilo, cicloalquilo, fluoroalquilo, ciclofluoroalquilo y heterociclo se puede oxidar para formar un grupo C=O; cualquier átomo de azufre presente dentro de un heterociclo se puede oxidar para formar un grupo S=O o un grupo S(O)₂; cualquier átomo de nitrógeno presente dentro de un heterociclo o presente dentro de un grupo donde está trisustituido, formando así un grupo amino terciario, se puede cuaternizar con un grupo metilo; y uno de sus racematos, enantiómeros, diastereoisómeros, isómeros geométricos o una de sus sales farmacéuticamente aceptables, a excepción de los compuestos de fórmula (2), (3) y (4).
ARP170102732A 2016-09-30 2017-09-29 Compuestos heterocíclicos y su uso en la prevención o el tratamiento de infecciones bacterianas AR109774A1 (es)

Applications Claiming Priority (1)

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EP16306261.5A EP3301094A1 (en) 2016-09-30 2016-09-30 Heterocyclic compounds and their use in preventing or treating bacterial infections

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US (1) US10722520B2 (es)
EP (3) EP3301094A1 (es)
JP (2) JP7089508B2 (es)
KR (1) KR20190065326A (es)
CN (2) CN109906226B (es)
AR (1) AR109774A1 (es)
AU (1) AU2017335222C1 (es)
BR (1) BR112019006371A2 (es)
CA (1) CA3038221A1 (es)
CL (1) CL2019000857A1 (es)
DK (1) DK3519411T3 (es)
ES (1) ES2927528T3 (es)
HR (1) HRP20220831T1 (es)
HU (1) HUE059938T2 (es)
IL (1) IL265676B (es)
LT (1) LT3519411T (es)
MX (1) MX2019003545A (es)
PL (1) PL3519411T3 (es)
PT (1) PT3519411T (es)
RS (1) RS63473B1 (es)
SI (1) SI3519411T1 (es)
TW (1) TWI801353B (es)
WO (1) WO2018060481A1 (es)
ZA (1) ZA201901963B (es)

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EP3301094A1 (en) * 2016-09-30 2018-04-04 Mutabilis Heterocyclic compounds and their use in preventing or treating bacterial infections
CA3120371A1 (en) 2018-11-20 2020-05-28 Nflection Therapeutics, Inc. Cyanoaryl-aniline compounds for treatment of dermal disorders
JP2024503893A (ja) * 2021-01-21 2024-01-29 エヌフレクション セラピューティクス インコーポレイテッド ピロロピリジン－アニリン化合物を調製するための方法

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JP6767392B2 (ja) * 2015-05-07 2020-10-14 ミュタビリスＭｕｔａｂｉｌｉｓ 複素環式化合物及び細菌感染の治療又は予防におけるその使用
EP3091018A1 (en) * 2015-05-07 2016-11-09 Mutabilis Heterocyclic compounds and their use in preventing or treating bacterial infections
EP3301094A1 (en) * 2016-09-30 2018-04-04 Mutabilis Heterocyclic compounds and their use in preventing or treating bacterial infections

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PL3519411T3 (pl) 2022-08-22
EP3301094A1 (en) 2018-04-04
SI3519411T1 (sl) 2022-08-31
HRP20220831T1 (hr) 2022-09-30
EP3519411B1 (en) 2022-06-22
PT3519411T (pt) 2022-08-25
CL2019000857A1 (es) 2019-08-09
RU2019109177A3 (es) 2020-11-30
AU2017335222A1 (en) 2019-04-11
JP2019530690A (ja) 2019-10-24
KR20190065326A (ko) 2019-06-11
DK3519411T3 (da) 2022-07-11
US20190224210A1 (en) 2019-07-25
HUE059938T2 (hu) 2023-01-28
US10722520B2 (en) 2020-07-28
EP4086255A1 (en) 2022-11-09
ZA201901963B (en) 2021-01-27
CN109906226A (zh) 2019-06-18
AU2017335222B2 (en) 2021-07-15
IL265676A (en) 2019-05-30
CA3038221A1 (en) 2018-04-05
CN113929680A (zh) 2022-01-14
RS63473B1 (sr) 2022-08-31
TW201815791A (zh) 2018-05-01
LT3519411T (lt) 2022-09-12
TWI801353B (zh) 2023-05-11
EP3519411A1 (en) 2019-08-07
JP7089508B2 (ja) 2022-06-22
AU2017335222A2 (en) 2019-05-09
JP2022097520A (ja) 2022-06-30
AU2017335222C1 (en) 2022-01-20
IL265676B (en) 2021-12-01
MX2019003545A (es) 2019-06-17
RU2019109177A (ru) 2020-09-30
WO2018060481A1 (en) 2018-04-05
BR112019006371A2 (pt) 2019-06-25
ES2927528T3 (es) 2022-11-08
CN109906226B (zh) 2021-11-02

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