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AR108864A1 - ANTIBACTERIAL AGENTS - Google Patents

ANTIBACTERIAL AGENTS

Info

Publication number
AR108864A1
AR108864A1 ARP170101736A ARP170101736A AR108864A1 AR 108864 A1 AR108864 A1 AR 108864A1 AR P170101736 A ARP170101736 A AR P170101736A AR P170101736 A ARP170101736 A AR P170101736A AR 108864 A1 AR108864 A1 AR 108864A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
optionally substituted
heterocycloalkyl
haloalkyl
Prior art date
Application number
ARP170101736A
Other languages
Spanish (es)
Inventor
Darin James Hildebrandt
Timothy Robert Kane
Timothy D Machajewski
Taylor Ann Joo Choi
Andrei W Konradi
Frederick Cohen
Original Assignee
Achaogen Inc
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 Achaogen Inc filed Critical Achaogen Inc
Publication of AR108864A1 publication Critical patent/AR108864A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D331/00—Heterocyclic compounds containing rings of less than five members, having one sulfur atom as the only ring hetero atom
    • C07D331/04—Four-membered rings
    • 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
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), o una sal aceptable farmacéuticamente, hidrato, solvato, profármaco, estereoisómero, o tautómero del mismo, donde: X es S(O)q o NR⁶; A es C₆₋₁₀ arilo, heteroarilo, C₃₋₇ cicloalquilo, C₄₋₇ cicloalquenilo, o heterocicloalquilo, donde el arilo, heteroarilo, cicloalquilo, cicloalquenilo, o heterocicloalquilo está sustituido opcionalmente con uno o más R⁷; B es -CºC=R³, -CºC-CºC-R³, -CºC-CH=CH-R³, C₁₋₄ alquilo, C₁₋₄ haloalquilo, -OR⁸, -S(O)ʳR⁸, halógeno, C₆₋₁₀ arilo, heteroarilo, o -SF₅, donde el arilo o heteroarilo está sustituido opcionalmente con R²; R¹ es H, C₁₋₄ alquilo, C₂₋₄ alquenilo, C₂₋₄ alquinilo, C₁₋₄ alcoxi, C₁₋₄ haloalquilo, C₁₋₄ haloalcoxi, -(CH₂)ₘ-C₃₋₇ cicloalquilo, -(CH₂)ₘ-heterocicloalquilo, -O(CH₂)ₘ-C₃₋₇ cicloalquilo, -O(CH₂)ₘ-heterocicloalquilo, halógeno, -S(O)ₚ-C₁₋₄ alquilo, -OH, -(CH₂)ₙNH₂, -(CH₂)ₙ-C₁₋₄ alquilamino, o -(CH₂)ₙ-C₁₋₄ dialquilamino; R² es C₁₋₄ alquilo, C₁₋₄ alcoxi, C₁₋₄ haloalquilo, C₁₋₄ haloalcoxi, halógeno, -OH, -NH₂, o -CN; R³ es H, C₁₋₄ alquilo, C₃₋₇ cicloalquilo, heterocicloalquilo, o heteroarilo, donde el alquilo está sustituido opcionalmente con uno o más R⁴, y donde el cicloalquilo, heterocicloalquilo, o heteroarilo está sustituido opcionalmente con uno o más R⁵; cada R⁴ es en forma independiente en cada caso -OH, -NH₂, C₁₋₄ alcoxi, C₁₋₄ alquilamino, o C₁₋₄ dialquilamino; cada R⁵ es en forma independiente en cada caso C₁₋₄ alquilo, C₁₋₄ haloalquilo, C₁₋₄ alcoxi, C₁₋₄ haloalcoxi, halógeno, C₁₋₄ hidroxialquilo, -C(O)H, -C(=O)C₁₋₄ alquilo, -OH, -NH₂, C₁₋₄ alquilamino, C₁₋₄ dialquilamino, o -S(O)ₚ-C₁₋₄ alquilo; R⁶ es H, C₁₋₄ alquilo, C₁₋₄ hidroxialquilo, -C(O)H, -C(O)C₁₋₄ alquilo, -S(O)ʳ-C₁₋₄ alquilo, o -C(O)OC₁₋₄ alquilo; cada R⁷ es en forma independiente en cada caso C₁₋₄ alquilo, C₁₋₄ alcoxi, C₁₋₄ haloalquilo, C₁₋₄ haloalcoxi, o halógeno; o dos R⁷ en átomos adyacentes junto con los átomos a los que están unidos forman un anillo C₆₋₁₀ arilo opcionalmente sustituido con uno o más R⁹; o dos R⁷ en átomos adyacentes junto con los átomos a los que están unidos forman un anillo heteroarilo opcionalmente sustituido con uno o más R⁹; o dos R⁷ en átomos adyacentes junto con los átomos a los que están unidos forman un anillo C₄₋₈ cicloalquilo opcionalmente sustituido con uno o más R⁹; o dos R⁷ en átomos adyacentes junto con los átomos a los que están unidos forman un anillo heterocicloalquilo opcionalmente sustituido con uno o más R⁹; R⁸ es C₁₋₄ alquilo, C₂₋₄ alquenilo, C₂₋₄ alquinilo, C₁₋₄ haloalquilo, o C₃₋₆ cicloalquilo, donde el alquilo, alquenilo, o alquinilo está sustituido opcionalmente con uno o más sustituyentes seleccionados entre el grupo que consiste en C₃₋₇ cicloalquilo y heterocicloalquilo; cada R⁹ es en forma independiente en cada caso C₁₋₄ alquilo, C₁₋₄ alcoxi, C₁₋₄ haloalquilo, C₁₋₄ haloalcoxi, o halógeno; cada R’ es C₁₋₄ alquilo; o es 1 ó 2; s es 0, 1, ó 2; cada q, p, y r es en forma independiente en cada caso 0, 1, ó 2; y cada m y n es en forma independiente en cada caso 0, 1, 2, ó 3.Claim 1: A compound characterized in that it is of formula (1), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein: X is S (O) q or NR⁶; A is C₆₋₁₀ aryl, heteroaryl, C₃₋₇ cycloalkyl, C₄₋₇ cycloalkenyl, or heterocycloalkyl, where aryl, heteroaryl, cycloalkyl, cycloalkenyl, or heterocycloalkyl is optionally substituted with one or more R⁷; B is -CºC = R³, -CºC-CºC-R³, -CºC-CH = CH-R³, C₁₋₄ alkyl, C₁₋₄ haloalkyl, -OR⁸, -S (O) ʳR⁸, halogen, C₆₋₁₀ aryl, heteroaryl, or -SF₅, where the aryl or heteroaryl is optionally substituted with R²; R¹ is H, C₁₋₄ alkyl, C₂₋₄ alkenyl, C₂₋₄ alkynyl, C₁₋₄ alkoxy, C₁₋₄ haloalkyl, C₁₋₄ haloalkoxy, - (CH₂) ₘ-C₃₋₇ cycloalkyl, - (CH₂) ₘ -heterocycloalkyl, -O (CH₂) ₘ-C₃₋₇ cycloalkyl, -O (CH₂) ₘ-heterocycloalkyl, halogen, -S (O) ₚ-C₁₋₄ alkyl, -OH, - (CH₂) ₙNH₂, - (CH₂ ) ₙ-C₁₋₄ alkylamino, or - (CH₂) ₙ-C₁₋₄ dialkylamino; R² is C₁₋₄ alkyl, C₁₋₄ alkoxy, C₁₋₄ haloalkyl, C₁₋₄ haloalkoxy, halogen, -OH, -NH₂, or -CN; R³ is H, C₁₋₄ alkyl, C₃₋₇ cycloalkyl, heterocycloalkyl, or heteroaryl, where the alkyl is optionally substituted with one or more R⁴, and where the cycloalkyl, heterocycloalkyl, or heteroaryl is optionally substituted with one or more R⁵; each R⁴ is independently in each case -OH, -NH₂, C₁₋₄ alkoxy, C₁₋₄ alkylamino, or C₁₋₄ dialkylamino; each R⁵ is independently in each case C₁₋₄ alkyl, C₁₋₄ haloalkyl, C₁₋₄ alkoxy, C₁₋₄ haloalkoxy, halogen, C₁₋₄ hydroxyalkyl, -C (O) H, -C (= O) C₁ ₋₄ alkyl, -OH, -NH₂, C₁₋₄ alkylamino, C₁₋₄ dialkylamino, or -S (O) ₚ-C₁₋₄ alkyl; R⁶ is H, C₁₋₄ alkyl, C₁₋₄ hydroxyalkyl, -C (O) H, -C (O) C₁₋₄ alkyl, -S (O) ʳ-C₁₋₄ alkyl, or -C (O) OC₁ ₋₄ alkyl; each R⁷ is independently in each case C₁₋₄ alkyl, C₁₋₄ alkoxy, C₁₋₄ haloalkyl, C₁₋₄ haloalkoxy, or halogen; or two R⁷ in adjacent atoms together with the atoms to which they are attached form a C₆₋₁₀ aryl ring optionally substituted with one or more R⁹; or two R⁷ in adjacent atoms together with the atoms to which they are attached form a heteroaryl ring optionally substituted with one or more R⁹; or two R⁷ in adjacent atoms together with the atoms to which they are attached form a C₄₋₈ cycloalkyl ring optionally substituted with one or more R⁹; or two R⁷ in adjacent atoms together with the atoms to which they are attached form a heterocycloalkyl ring optionally substituted with one or more R⁹; R⁸ is C₁₋₄ alkyl, C₂₋₄ alkenyl, C₂₋₄ alkynyl, C₁₋₄ haloalkyl, or C₃₋₆ cycloalkyl, where the alkyl, alkenyl, or alkynyl is optionally substituted with one or more substituents selected from the group consisting in C₃₋₇ cycloalkyl and heterocycloalkyl; each R⁹ is independently in each case C₁₋₄ alkyl, C₁₋₄ alkoxy, C₁₋₄ haloalkyl, C₁₋₄ haloalkoxy, or halogen; each R ’is C₁₋₄ alkyl; or is 1 or 2; s is 0, 1, or 2; each q, p, and r is independently in each case 0, 1, or 2; and each m and n is independently in each case 0, 1, 2, or 3.

ARP170101736A 2016-06-23 2017-06-22 ANTIBACTERIAL AGENTS AR108864A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201662353910P 2016-06-23 2016-06-23

Publications (1)

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AR108864A1 true AR108864A1 (en) 2018-10-03

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AR (1) AR108864A1 (en)
TW (1) TW201803847A (en)
WO (1) WO2017223349A1 (en)

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WO2016201288A1 (en) 2015-06-12 2016-12-15 Brown University Novel antibacterial compounds and methods of making and using same
CN108358887B (en) * 2018-03-20 2020-12-22 富乐马鸿凯（大连）医药有限公司 Synthesis of optically pure sulfur-containing quaternary heterocyclic drug intermediate
CN110283745B (en) * 2019-06-27 2021-05-11 浙江工业大学 Hospital Acinetobacter FK2 and Its Application in Degrading Organic Pollutants
US11555010B2 (en) 2019-07-25 2023-01-17 Brown University Diamide antimicrobial agents
CN110563611B (en) * 2019-09-19 2021-02-02 中国医学科学院医药生物技术研究所 A kind of hydroxamic acid derivative and its preparation method and application
CN113604408B (en) * 2021-09-06 2023-08-22 浙江树人学院（浙江树人大学） Acinetobacter mordistus HYY-1 and application thereof in degrading organic pollutants
CN116730870B (en) * 2023-08-08 2023-10-13 中国医学科学院医药生物技术研究所 Hydroxamic acid compounds or pharmaceutically acceptable salts thereof, uses and preparation methods thereof

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TW201803847A (en) 2018-02-01

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