EP1401830A2 - Agents antibacteriens - Google Patents

Agents antibacteriens

Info

Publication number
EP1401830A2
EP1401830A2 EP02730582A EP02730582A EP1401830A2 EP 1401830 A2 EP1401830 A2 EP 1401830A2 EP 02730582 A EP02730582 A EP 02730582A EP 02730582 A EP02730582 A EP 02730582A EP 1401830 A2 EP1401830 A2 EP 1401830A2
Authority
EP
European Patent Office
Prior art keywords
fluoro
cyclopropyl
dione
quinazoline
methyl
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP02730582A
Other languages
German (de)
English (en)
Inventor
Edmund Lee Pfizer Global R&D ELLSWORTH
Howard Daniel H. Pfizer Global R&D SHOWALTER
Sharon Anne Pfizer Global R&D POWELL
Joseph Peter Pfizer Global R&D SANCHEZ
James Alan Kerschen
Michael Andrew Pfizer Global R&D STIER
Tuan Phong Pfizer Global R&D TRAN
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Warner Lambert Co LLC
Original Assignee
Warner Lambert Co LLC
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 Warner Lambert Co LLC filed Critical Warner Lambert Co LLC
Publication of EP1401830A2 publication Critical patent/EP1401830A2/fr
Withdrawn legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • 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
    • C07D487/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

Definitions

  • This invention relates to antibacterial agents having a quinazolindione core structure, processes for their preparation, and methods for their use.
  • Antibiotic resistance is a worldwide problem with catastrophic potential.
  • a Task Force co-chaired by the United States Centers for Disease Control (CDC), Food and Drug Administration (FDA), and National Institutes of Health (NIH) recently addressed this important issue, observing that drug resistant pathogens are a growing menace to all people, regardless of race, age, gender, or socioeconomic background.
  • the Task Force noted that a number of microbes responsible for infections in humans are rapidly developing resistance to existing drugs. For example, according to the Task Force, in the United States alone, up to 30 percent of the Staphylococcus pneumoniae infections (skin, bone, lung, and bloodstream infections) are no longer susceptible to penicillin in some areas. Up to 11 percent of S. pneumoniae are resistant to third generation cephalosporin antibiotics. Significantly, resistance of S. pneumoniae to the fluoroquinolones, a newer class of potent antibiotics, has also been reported.
  • the fluoroquinolones are bacterial inhibitors that apparently exert their effect by inhibiting bacterial DNA gyrase and topoisomerase IV.
  • antibiotic resistance particularly fluoroquinolone resistance
  • fluoroquinolone resistance can be fatal for some individuals.
  • a 62-year-old woman diagnosed with food poisoning from ciprofloxacin-resistant Salmonella died after undergoing antibiotic treatment using that drug.
  • R 2 is H
  • R3, R4, and R independently are H, OH,
  • R a and R b taken together with the nitrogen to which they are attached form a 4, 5, 6, 7, or 8 membered ring having from 0 to 3 heteroatoms selected from N, O, and S, wherein said ring is optionally substituted by one or more substituents;
  • R j and Rg taken together with the atoms to which they are attached form a
  • R5 is hydrogen, C]-C7 alkyl and substituted alkyl
  • R f and R g are defined as for R a and R b above; aryl or fused aryl, heterocyclic or fused heterocyclic, heteroaryl or fused heteroaryl, bicyclic heterocyclic or spiro heterocyclic, wherein fused aryl, fused heterocyclic, fused heteroaryl, bicyclic heterocyclic, or spiro heterocyclic can be substituted; and wherein J and K independently are C or N, provided that when J or K is N, R4 or R 6 is absent at that position.
  • the invention also provides a compound of Formula II:
  • R 2 is H
  • R3, R4, and Rg independently are H, OH,
  • R a and Rb taken together with the nitrogen to which they are attached form a 4, 5, 6, 7, or 8 membered ring having from 0 to 3 heteroatoms selected from N, O, and S, wherein said ring is optionally substituted by one or more substituents;
  • Rl and Rg taken together with the atoms to which they are attached to form a 5, 6, 7, or 8 membered ring having from 0 to 3 heteroatoms selected from N, O, and S, wherein said ring is optionally substituted by one or more substituents;
  • R5 is hydrogen
  • CN NR f Rg, wherein Rf and R g are defined as for R a and R b above; aryl or fused aryl, heterocyclic or fused heterocyclic, heteroaryl or fused heteroaryl, or bicyclic heterocyclic or spiro heterocyclic; wherein fused aryl, fused heterocyclic, fused heteroaryl, bicyclic heterocyclic, or spiro heterocyclic can be substituted.
  • the present invention also provides a compound of Formula III:
  • Rl is H
  • R c is ⁇ C1-C7 alkyl and substituted alkyl
  • R a and R b are each independently H, C -C7 alkyl and substituted alkyl
  • R c is C1-C7 alkyl and substituted alkyl
  • R a and R b taken together with the nitrogen to which they are attached form a 4, 5, 6, 7, or 8 membered ring having from 0 to 3 heteroatoms selected from N, O, and S, wherein said ring is optionally substituted by one or more substituents;
  • R5 is hydrogen,
  • CN NR f R g , wherein R f and R g are defined as for R a and R b above; aryl or fused aryl, heterocyclic or fused heterocyclic, heteroaryl or fused heteroaryl, or bicyclic heterocyclic or spiro heterocyclic, wherein fused aryl, fused heterocyclic, fused heteroaryl, bicyclic heterocyclic, or spiro heterocyclic can be substituted.
  • the present invention also provides a compound of Formula IV:
  • R 2 is H
  • R3 and Rg independently are H, OH,
  • R f and R g are defined as for R a and R b above; aryl or fused aryl, heterocyclic or fused heterocyclic, heteroaryl or fused heteroaryl, bicyclic heterocyclic or spiro heterocyclic, wherein fused aryl, fused heterocyclic, fused heteroaryl, bicyclic heterocyclic, or spiro heterocyclic can be substituted.
  • the present invention also provides a compound of Formula V:
  • R is H
  • R 3 is H, OH,
  • R a and R b are each independently H, C1 -C7 alkyl and substituted alkyl, C 2 -C7 alkenyl and substituted alkenyl,
  • R f and R g are defined as for R a and R above; aryl or fused aryl, heterocyclic or fused heterocyclic, heteroaryl or fused heteroaryl, bicyclic heterocyclic or spiro heterocyclic, wherein fused aryl, fused heterocyclic, fused heteroaryl, bicyclic heterocyclic, or spiro heterocyclic can be substituted.
  • the invention also provides a compound of formula VI:
  • R3, R4, and Rg independently are H,
  • R a and R b are each independently H, C -C7 alkyl and substituted alkyl
  • R c is C -C7 alkyl and substituted alkyl
  • R and R e are independantly H, C1-C7 alkyl and substituted alkyl,
  • R a and Rb taken together with the nitrogen to which they are attached form a 5, 6, 7, or 8 membered ring having from 0 to
  • the invention also provides a compound of formula VII:
  • Rl is H, C1-C7 alkyl and substituted alkyl
  • R is H
  • R3, and R4 independently are H,
  • R a and R are each independently H, C1-C7 alkyl and substituted alkyl
  • the invention also provides a compound of formula VIII:
  • R3 and R4 independently are H
  • Rd and R e are independantly H, C -C7 alkyl and substituted alkyl, C2-C7 alkenyl and substituted alkenyl,
  • R a and R taken together with the nitrogen to which they are attached form a 4, 6, 7, or 8 membered ring having from 0 to 3 heteroatoms selected from N, O, and S, wherein said ring is optionally substituted by one or more substituents; ydrogen,
  • R f and R g are defined as for R a and R b above; aryl or fused aryl, heterocyclic or fused heterocyclic, heteroaryl or fused heteroaryl, bicyclic heterocyclic or spiro heterocyclic, wherein fused aryl, fused heterocyclic, fused heteroaryl, bicyclic heterocyclic, or spiro heterocyclic can be substituted;
  • X and Y each independently are O, CH 2 , CH(C 1 -C 7 alkyl), C(C C 7 alkyl) 2 ,
  • R j and Rkindependently are H, C1-C7 alkyl and substituted alkyl
  • R j and R k taken together with the nitrogen to which they are attached form a 3- to 7-membered ring containing from 1 to 3 heteroatoms selected from N, O, and S, said ring being unsubstituted or substituted with 1, 2, 3, or 4 substituent groups.
  • the invention also provides a compound of formula IX:
  • R3, R4, and Rg independently are H,
  • R a and R b are each independently H, C1-C7 alkyl and substituted alkyl
  • R c is C -C7 alkyl and substituted alkyl
  • R and R e are independantly H, C1-C7 alkyl and substituted alkyl,
  • R a and R b taken together with the nitrogen to which they are attached form a 4, 5, 6, 7, or 8 membered ring having from 0 to 3 heteroatoms selected from N, O, and S, wherein said ring is optionally substituted by one or more substituents; Rg taken together with the atoms to which they are attached form a
  • V is N, CH, or C, provided that when Z is N or CH, "- -" is absent and when Z is C, "— " is a double bond;
  • z is O, 1, 2, or 3;
  • V is O, S, NH 2 , NHR", wherein R" is C1-C7 alkyl and substituted alkyl;
  • the invention also provides a compound which is 7-(6-amino-3-aza-bicyclo[3.1.0]hex-3-yl) -6-fluoro-3H-l- methylcyclopropyl-lH-quinazoline-2, 4-dione (l ⁇ , 5 ⁇ , 6 ⁇ ) hydrochloride, l-Cyclopropyl-6-fluoro-8-methyl-7-[(R)-3-((S)-l-methylaminoethyl)- pyrrolidin-l-yl]-lH-quinazolinedione,
  • the invention also provides a compound of the invention which is:
  • the invention also provides a pharmaceutical composition comprising a compound of one of the above-mentioned Formulas admixed with a carrier, diluent, or excipient.
  • the invention also provides a method of treating a bacterial infection in a mammal comprising administering to the mammal in need thereof an antibacterial effective amount of a compound of one of the above-mentioned Formulas.
  • the invention also provides a method of inhibiting a bacterial topoisomerase in a mammal comprising administering to the mammal in need thereof an effective amount of a compound of one of the above-mentioned Formulas.
  • the invention also provides a method of inhibiting a bacterial DNA gyrase in a mammal comprising administering to the mammal in need thereof an effective amount of a compound of one of the above-mentioned Formulas.
  • the invention also provides a method of inhibiting a bacterial topoisomerase IV in a mammal comprising administering to the mammal in need thereof an effective amount of a compound of one of the above-mentioned Formulas.
  • the invention also provides a method of inhibiting a quinolone-resistant bacteria in a mammal comprising administering to the mammal an effective amount of a compound of one of the above-mentioned Formulas.
  • the invention also provides a method of inhibiting a quinolone resistant bacterial DNA gyrase in a mammal comprising administering to the mammal an effective amount of a compound of any of Formulas I- VIII.
  • a method of inhibiting a quinolone resistant bacterial topoisomerase in a mammal comprising administering to the mammal an effective amount of a compound of any of Formulas I- VIII.
  • the invention also provides a process for preparing a compound of formula DC, wherein Ri, R , R 3 , R ⁇ R 6 , J, K, V, V, z, and R' are as defined above and R.y is halo, comprising: (a) coupling compound IXA wherein M is n-Bu 3 Sn with compound IXB wherein R 5 - is halo in the presence of Pd° to provide the R5-coupled product IXC;

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Communicable Diseases (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

L'invention concerne des composés représentés par la formule (I) dans laquelle R1-R6, J et K ont n'importe lesquelles des valeurs définies dans le descriptif, ainsi que leurs sels pharmaceutiquement acceptables, qui sont utilisés comme agents antibactériens. Par ailleurs, l'invention concerne des compositions pharmaceutiques contenant un ou plusieurs des composés de la formule (I), des procédés de préparation des composés de formule (I), ainsi que des intermédiaires utilisés pour préparer les composés de formule (I).
EP02730582A 2001-06-19 2002-05-13 Agents antibacteriens Withdrawn EP1401830A2 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US29924901P 2001-06-19 2001-06-19
US299249P 2001-06-19
PCT/IB2002/001768 WO2002102793A2 (fr) 2001-06-19 2002-05-13 Agents antibacteriens

Publications (1)

Publication Number Publication Date
EP1401830A2 true EP1401830A2 (fr) 2004-03-31

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Application Number Title Priority Date Filing Date
EP02730582A Withdrawn EP1401830A2 (fr) 2001-06-19 2002-05-13 Agents antibacteriens

Country Status (13)

Country Link
EP (1) EP1401830A2 (fr)
JP (1) JP2005501021A (fr)
AU (1) AU2002302894A1 (fr)
BR (1) BR0210028A (fr)
CA (1) CA2446963A1 (fr)
DO (1) DOP2002000422A (fr)
GT (1) GT200200104A (fr)
HN (1) HN2002000150A (fr)
MX (1) MXPA03009894A (fr)
PA (1) PA8548401A1 (fr)
PE (1) PE20030272A1 (fr)
SV (1) SV2003001089A (fr)
WO (1) WO2002102793A2 (fr)

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ES2991427T3 (es) 2018-05-04 2024-12-03 Incyte Corp Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas
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US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2021007269A1 (fr) 2019-07-09 2021-01-14 Incyte Corporation Hétérocycles bicycliques en tant qu'inhibiteurs de fgfr
WO2021067374A1 (fr) 2019-10-01 2021-04-08 Incyte Corporation Hétérocycles bicycliques en tant qu'inhibiteurs de fgfr
GEAP202415945A (en) 2019-10-14 2024-04-25 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (fr) 2019-10-16 2021-04-22 Incyte Corporation Hétérocycles bicycliques en tant qu'inhibiteurs de fgfr
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
CA3163875A1 (fr) 2019-12-04 2021-06-10 Incyte Corporation Heterocycles tricycliques en tant qu'inhibiteurs de fgfr
WO2021146424A1 (fr) 2020-01-15 2021-07-22 Incyte Corporation Hétérocycles bicycliques en tant qu'inhibiteurs de fgfr
CN115734785A (zh) 2020-04-14 2023-03-03 桑诺维恩药品公司 (S)-(4,5-二氢-7H-噻吩并[2,3-c]吡喃-7-基)-N-甲基甲胺用于治疗神经和精神方面的病症
EP4323405A1 (fr) 2021-04-12 2024-02-21 Incyte Corporation Polythérapie comprenant un inhibiteur de fgfr et un agent de ciblage de nectine-4
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PA8548401A1 (es) 2003-05-14
AU2002302894A1 (en) 2003-01-02
HN2002000150A (es) 2002-09-13
MXPA03009894A (es) 2004-02-17
CA2446963A1 (fr) 2002-12-27
PE20030272A1 (es) 2003-03-21
GT200200104A (es) 2003-02-11
WO2002102793A3 (fr) 2003-04-10
BR0210028A (pt) 2004-06-22
WO2002102793A2 (fr) 2002-12-27
DOP2002000422A (es) 2002-12-30
JP2005501021A (ja) 2005-01-13
SV2003001089A (es) 2003-03-18

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