EA024782B1 - Производные фторпиридинона, полезные в качестве антибактериальных агентов - Google Patents

Производные фторпиридинона, полезные в качестве антибактериальных агентов Download PDF

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Publication number
EA024782B1
EA024782B1 EA201391072A EA201391072A EA024782B1 EA 024782 B1 EA024782 B1 EA 024782B1 EA 201391072 A EA201391072 A EA 201391072A EA 201391072 A EA201391072 A EA 201391072A EA 024782 B1 EA024782 B1 EA 024782B1
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EA
Eurasian Patent Office
Prior art keywords
fluoro
methylsulfonyl
methyl
butanamide
mmol
Prior art date
Application number
EA201391072A
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English (en)
Russian (ru)
Other versions
EA201391072A1 (ru
Inventor
Мэттью Фрэнк Браун
Йе Че
Майкл Джозеф Мелник
Джастин Йэн Монтгомери
Марк Стефен Пламмер
Лорен Майкл Прайс
Юса Рейлли
Original Assignee
Пфайзер Инк.
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Application filed by Пфайзер Инк. filed Critical Пфайзер Инк.
Publication of EA201391072A1 publication Critical patent/EA201391072A1/ru
Publication of EA024782B1 publication Critical patent/EA024782B1/ru

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    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 to ring carbon atoms
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/64One oxygen atom attached in position 2 or 6
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 to ring carbon atoms
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/69Two or more oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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 linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links

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  • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
EA201391072A 2011-03-07 2012-02-22 Производные фторпиридинона, полезные в качестве антибактериальных агентов EA024782B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161449825P 2011-03-07 2011-03-07
PCT/IB2012/050812 WO2012120397A1 (en) 2011-03-07 2012-02-22 Fluoro-pyridinone derivatives useful as antibacterial agents

Publications (2)

Publication Number Publication Date
EA201391072A1 EA201391072A1 (ru) 2014-02-28
EA024782B1 true EA024782B1 (ru) 2016-10-31

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA201391072A EA024782B1 (ru) 2011-03-07 2012-02-22 Производные фторпиридинона, полезные в качестве антибактериальных агентов

Country Status (34)

Country Link
US (2) US8624034B2 (enExample)
EP (1) EP2683689B1 (enExample)
JP (1) JP5620020B2 (enExample)
KR (1) KR101593288B1 (enExample)
CN (2) CN103443079B (enExample)
AP (1) AP3336A (enExample)
AR (1) AR085615A1 (enExample)
AU (1) AU2012226473B8 (enExample)
BR (1) BR112013022536B1 (enExample)
CA (1) CA2828337C (enExample)
CL (1) CL2013002417A1 (enExample)
CO (1) CO6761338A2 (enExample)
CR (1) CR20130403A (enExample)
CU (1) CU20130117A7 (enExample)
DO (1) DOP2013000200A (enExample)
EA (1) EA024782B1 (enExample)
EC (1) ECSP13012928A (enExample)
ES (1) ES2626457T3 (enExample)
GE (1) GEP20156370B (enExample)
GT (1) GT201300213A (enExample)
HK (1) HK1209734A1 (enExample)
IL (1) IL228100A0 (enExample)
MA (1) MA34963B1 (enExample)
MX (1) MX341977B (enExample)
NI (1) NI201300077A (enExample)
PE (1) PE20140397A1 (enExample)
PH (1) PH12013501780A1 (enExample)
SG (1) SG192766A1 (enExample)
TN (1) TN2013000353A1 (enExample)
TW (1) TWI453197B (enExample)
UA (1) UA107423C2 (enExample)
UY (1) UY33936A (enExample)
WO (1) WO2012120397A1 (enExample)
ZA (1) ZA201306515B (enExample)

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GEP20156370B (en) 2011-03-07 2015-09-25 Pfizer Fluoro-pyridinone derivatives useful as antibacterial agents
EP2694488B1 (en) 2011-04-08 2014-11-12 Pfizer Inc Isoxazole derivatives useful as antibacterial agents
EP2694481B1 (en) * 2011-04-08 2015-12-30 Pfizer Inc Imidazole, pyrazole, and triazole derivatives useful as antibacterial agents
AR097617A1 (es) 2013-09-13 2016-04-06 Actelion Pharmaceuticals Ltd Derivados antibacterianos del 2h-indazol
WO2015085238A1 (en) * 2013-12-05 2015-06-11 The Regents Of The University Of California, A California Corporation Inhibitors of lpxc
JP6407288B2 (ja) 2013-12-19 2018-10-17 イドーシア ファーマシューティカルズ リミテッドIdorsia Pharmaceuticals Ltd 抗菌性1h−インダゾール及び1h−インドール誘導体
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EP3134401B1 (en) 2014-04-22 2018-06-13 Novartis AG Isoxazoline hydroxamic acid derivatives as lpxc inhibitors
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JP6195684B2 (ja) 2014-06-03 2017-09-13 アクテリオン ファーマシューティカルズ リミテッドActelion Pharmaceuticals Ltd ピラゾール化合物及びt型カルシウムチャンネルブロッカーとしてのそれらの使用
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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
HRP20201524T1 (hr) 2016-06-14 2021-03-05 Novartis Ag Kristalni oblik (r)-4-(5-(ciklopropiletinil) izoksazol-3 -il)-n-hidroksi-2-metil-2-(metilsufonil) butanamid kao antibakterijsko sredstvo
LT3554490T (lt) 2016-12-16 2022-04-25 Idorsia Pharmaceuticals Ltd Farmacinis derinys, apimantis t tipo kalcio kanalo blokatorių
CA3050348A1 (en) 2017-02-06 2018-08-09 Idorsia Pharmaceuticals Ltd A novel process for the synthesis of 1-aryl-1-trifluoromethylcyclopropanes
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US11981696B2 (en) 2018-03-15 2024-05-14 Pfizer Inc. Fluoro-pyridinone phosphates and boronates useful as antibacterial agents
CN110699312B (zh) * 2019-11-28 2022-08-12 西北农林科技大学 一种猪种布鲁氏菌bi-1基因缺失菌株及其构建方法和应用

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GEP20156370B (en) 2011-03-07 2015-09-25 Pfizer Fluoro-pyridinone derivatives useful as antibacterial agents
EP2694488B1 (en) 2011-04-08 2014-11-12 Pfizer Inc Isoxazole derivatives useful as antibacterial agents
EP2694481B1 (en) 2011-04-08 2015-12-30 Pfizer Inc Imidazole, pyrazole, and triazole derivatives useful as antibacterial agents

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WO2007069020A2 (en) * 2005-12-15 2007-06-21 Vicuron Pharmaceuticals Inc. N-hydroxyamide derivatives possessing antibacterial activity
WO2010017060A1 (en) * 2008-08-04 2010-02-11 Schering Corporation Urea derivatives as antibacterial agents
WO2011073845A1 (en) * 2009-12-16 2011-06-23 Pfizer Inc. N-linked hydroxamic acid derivatives useful as antibacterial agents

Also Published As

Publication number Publication date
AU2012226473B8 (en) 2015-10-15
WO2012120397A1 (en) 2012-09-13
AR085615A1 (es) 2013-10-16
PH12013501780A1 (en) 2019-07-03
UY33936A (es) 2012-10-31
MX341977B (es) 2016-09-07
CL2013002417A1 (es) 2013-12-13
KR20130131459A (ko) 2013-12-03
AU2012226473B2 (en) 2015-06-11
US20140057919A1 (en) 2014-02-27
HK1191951A1 (en) 2014-08-08
SG192766A1 (en) 2013-09-30
AU2012226473A1 (en) 2013-09-05
TN2013000353A1 (fr) 2015-01-20
MX2013010276A (es) 2013-10-01
US20120232083A1 (en) 2012-09-13
IL228100A0 (en) 2013-09-30
GT201300213A (es) 2014-06-06
CN104529883A (zh) 2015-04-22
CR20130403A (es) 2013-09-18
CA2828337A1 (en) 2012-09-13
NI201300077A (es) 2014-01-07
EA201391072A1 (ru) 2014-02-28
HK1209734A1 (en) 2016-04-08
TW201249798A (en) 2012-12-16
CN103443079A (zh) 2013-12-11
CU20130117A7 (es) 2013-10-29
CO6761338A2 (es) 2013-09-30
JP5620020B2 (ja) 2014-11-05
ES2626457T3 (es) 2017-07-25
CN103443079B (zh) 2015-06-03
EP2683689A1 (en) 2014-01-15
MA34963B1 (fr) 2014-03-01
NZ614205A (en) 2014-06-27
EP2683689B1 (en) 2017-04-12
KR101593288B1 (ko) 2016-02-11
US8779148B2 (en) 2014-07-15
UA107423C2 (en) 2014-12-25
ECSP13012928A (es) 2013-11-29
TWI453197B (zh) 2014-09-21
AP2013007074A0 (en) 2013-08-31
PE20140397A1 (es) 2014-03-28
BR112013022536A2 (pt) 2016-11-29
DOP2013000200A (es) 2014-06-15
US8624034B2 (en) 2014-01-07
CA2828337C (en) 2016-05-03
AP3336A (en) 2015-07-31
ZA201306515B (en) 2014-05-28
GEP20156370B (en) 2015-09-25
BR112013022536B1 (pt) 2020-05-26
JP2014507464A (ja) 2014-03-27

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