ES2687393T3 - Derivados del ácido hidroxámico de isoxazolina como inhibidores de LpxC - Google Patents

Derivados del ácido hidroxámico de isoxazolina como inhibidores de LpxC Download PDF

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Publication number
ES2687393T3
ES2687393T3 ES15721435.4T ES15721435T ES2687393T3 ES 2687393 T3 ES2687393 T3 ES 2687393T3 ES 15721435 T ES15721435 T ES 15721435T ES 2687393 T3 ES2687393 T3 ES 2687393T3
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ES
Spain
Prior art keywords
mmol
equiv
methyl
methylsulfonyl
dihydroisoxazol
Prior art date
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Application number
ES15721435.4T
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English (en)
Spanish (es)
Inventor
Jiping Fu
Subramanian Karur
Patrick Lee
Zachary Kevin Sweeney
Xianming Jin
Guillaume LAPOINTE
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Novartis AG
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Novartis AG
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Filing date
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Publication of ES2687393T3 publication Critical patent/ES2687393T3/es
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Classifications

    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/04—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • 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
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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 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
    • C07D413/02—Heterocyclic 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
    • C07D413/10—Heterocyclic 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
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/10—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 two hetero rings linked by a carbon chain containing aromatic rings
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (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)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
ES15721435.4T 2014-04-22 2015-04-22 Derivados del ácido hidroxámico de isoxazolina como inhibidores de LpxC Active ES2687393T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461982467P 2014-04-22 2014-04-22
US201461982467P 2014-04-22
PCT/US2015/027009 WO2015164458A1 (en) 2014-04-22 2015-04-22 Isoxazoline hydroxamic acid derivatives as lpxc inhibitors

Publications (1)

Publication Number Publication Date
ES2687393T3 true ES2687393T3 (es) 2018-10-25

Family

ID=53059459

Family Applications (1)

Application Number Title Priority Date Filing Date
ES15721435.4T Active ES2687393T3 (es) 2014-04-22 2015-04-22 Derivados del ácido hidroxámico de isoxazolina como inhibidores de LpxC

Country Status (6)

Country Link
US (2) US9637482B2 (OSRAM)
EP (1) EP3134401B1 (OSRAM)
JP (1) JP6514716B2 (OSRAM)
CN (1) CN106573924B (OSRAM)
ES (1) ES2687393T3 (OSRAM)
WO (1) WO2015164458A1 (OSRAM)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20180088456A (ko) * 2015-12-08 2018-08-03 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 항박테리아 화합물로서의 치환된 벤자지논
HUE050796T2 (hu) * 2016-06-14 2021-01-28 Novartis Ag (R)-4-(5-(ciklopropiletinil)izoxazol-3-il)-N-hidroxi-2-metil-2-(metilszulfonil)butánamid kristályos formája baktériumellenes szerként
RU2722594C1 (ru) * 2016-09-28 2020-06-02 Тон-А Ст Ко., Лтд. Производные тетрагидропиридина и их использование в качестве антибактериальных средств
CA3119957A1 (en) * 2018-11-21 2020-05-28 Taisho Pharmaceutical Co., Ltd. Novel imidazole derivative
CN113365978A (zh) * 2019-01-06 2021-09-07 普梭梅根公司 Htra抑制剂和caga抑制剂及其应用
WO2024067812A1 (zh) * 2022-09-28 2024-04-04 浙江海正药业股份有限公司 芳香乙炔类衍生物及其制备方法和用途
CN120569379A (zh) * 2023-01-19 2025-08-29 浙江海正药业股份有限公司 芳香乙炔类衍生物及其制备方法和用途

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2176255C (en) * 1993-11-26 1999-02-23 Edward F. Kleinman Isoxazoline compounds as antiinflammatory agents
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
WO2004043349A2 (en) * 2002-11-06 2004-05-27 Bristol-Myers Squibb Company Isoxazoline derivatives as inhibitors of matrix metalloproteinases and/or tnf-alpha converting enzyme
CA2512582C (en) 2003-01-08 2014-07-08 University Of Washington Antibacterial agents
CA2735929C (en) 2008-09-19 2013-12-17 Pfizer Inc. Hydroxamic acid derivatives useful as antibacterial agents
WO2011045703A2 (en) * 2009-10-13 2011-04-21 Pfizer Inc. C-linked hydroxamic acid derivatives useful as antibacterial agents
EP2512474B1 (en) 2009-12-16 2014-11-05 Pfizer Inc N-linked hydroxamic acid derivatives useful as antibacterial agents
EP2683689B1 (en) 2011-03-07 2017-04-12 Pfizer Inc Fluoro-pyridinone derivatives useful as antibacterial agents
JP2014510132A (ja) * 2011-04-08 2014-04-24 ファイザー・インク 抗菌剤として有用なイソオキサゾール誘導体
KR20120137094A (ko) * 2011-06-10 2012-12-20 현대자동차주식회사 차량용 소음기
WO2014160649A1 (en) 2013-03-29 2014-10-02 Novartis Ag Hydroxamic acid derivatives as lpxc inhibitors for the treatment of bacterial infections

Also Published As

Publication number Publication date
US20170029415A1 (en) 2017-02-02
CN106573924A (zh) 2017-04-19
JP2017513892A (ja) 2017-06-01
WO2015164458A1 (en) 2015-10-29
US20170174640A1 (en) 2017-06-22
CN106573924B (zh) 2019-06-25
US9637482B2 (en) 2017-05-02
JP6514716B2 (ja) 2019-05-15
EP3134401A1 (en) 2017-03-01
EP3134401B1 (en) 2018-06-13
US9718792B2 (en) 2017-08-01

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