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

Info

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
Authority
ES
Spain
Prior art keywords
mmol
equiv
methyl
methylsulfonyl
dihydroisoxazol
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.)
Active
Application number
ES15721435.4T
Other languages
English (en)
Spanish (es)
Inventor
Jiping Fu
Subramanian Karur
Patrick Lee
Zachary Kevin Sweeney
Xianming Jin
Guillaume LAPOINTE
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.)
Novartis AG
Original Assignee
Novartis AG
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 Novartis AG filed Critical Novartis AG
Application granted granted Critical
Publication of ES2687393T3 publication Critical patent/ES2687393T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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 (enExample)
EP (1) EP3134401B1 (enExample)
JP (1) JP6514716B2 (enExample)
CN (1) CN106573924B (enExample)
ES (1) ES2687393T3 (enExample)
WO (1) WO2015164458A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017098440A1 (en) * 2015-12-08 2017-06-15 Glaxosmithkline Intellectual Property Development Limited Substituted benzazinones as antibacterial compounds
SMT202000524T1 (it) 2016-06-14 2020-11-10 Novartis Ag Forma cristallina di (r)-4-(5-(ciclopropiletinil)isossazol-3-il)-n-idrossi-2-metil-2-(metilsolfonil)butanammide come agente antibatterico
AU2017337946B2 (en) * 2016-09-28 2020-05-07 Dong-A St Co., Ltd. Tetrahydropyridine derivatives and their use as antibacterial agents
BR112021009536A2 (pt) * 2018-11-21 2021-08-17 Taisho Pharmaceutical Co., Ltd. derivado de imidazol
EP3906226A4 (en) * 2019-01-06 2023-03-15 Psomagen, Inc. HTRA INHIBITORS AND CAGA INHIBITORS AND THEIR USE
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
WO2024153173A1 (zh) * 2023-01-19 2024-07-25 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
CZ283564B6 (cs) * 1993-11-26 1998-05-13 Pfizer Inc. 3-Aryl-2-isoxazolin-5-hydroxamové kyseliny a farmaceutické prostředky na jejich bázi
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
AU2003301903A1 (en) * 2002-11-06 2004-06-03 Bristol-Myers Squibb Company Isoxazoline derivatives as inhibitors of matrix metalloproteinases and/or tnf-alpha converting enzyme
ES2387803T3 (es) 2003-01-08 2012-10-02 Novartis Vaccines And Diagnostics, Inc. Agentes antibacterianos
US8722686B2 (en) 2008-09-19 2014-05-13 Pfizer Inc. Hydroxamic acid derivatives useful as antibacterial agents
CA2774250C (en) * 2009-10-13 2013-12-17 Pfizer Inc. C-linked hydroxamic acid derivatives useful as antibacterial agents
JP5793766B2 (ja) 2009-12-16 2015-10-14 ファイザー・インク 抗菌剤として有用なｎ−結合型ヒドロキサム酸誘導体
AP3336A (en) 2011-03-07 2015-07-31 Pfizer Fluoro-pyridinone derivatives useful as antibacterial agents
WO2012137094A1 (en) * 2011-04-08 2012-10-11 Pfizer Inc. Isoxazole derivatives useful as antibacterial agents
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
US9637482B2 (en) 2017-05-02
US20170029415A1 (en) 2017-02-02
EP3134401A1 (en) 2017-03-01
US9718792B2 (en) 2017-08-01
CN106573924A (zh) 2017-04-19
US20170174640A1 (en) 2017-06-22
JP6514716B2 (ja) 2019-05-15
WO2015164458A1 (en) 2015-10-29
CN106573924B (zh) 2019-06-25
JP2017513892A (ja) 2017-06-01
EP3134401B1 (en) 2018-06-13

Similar Documents

Publication Publication Date Title
ES2756300T3 (es) Compuestos de ácido isoxazol hidroxámico como inhibidores de LpxC
EP3134401B1 (en) Isoxazoline hydroxamic acid derivatives as lpxc inhibitors
CN113195053B (zh) 氨基酸化合物和使用方法
CN110312719B (zh) 作为jak家族激酶抑制剂的咪唑并吡咯并吡啶
CN105579444B (zh) 哌啶基吲哚衍生物和它们作为补体因子b抑制剂的用途
WO2014160649A1 (en) Hydroxamic acid derivatives as lpxc inhibitors for the treatment of bacterial infections
WO2019025467A1 (en) SELECTIVE INHIBITORS OF INFLAMMASOME NLRP3
TW201204346A (en) Novel hydroxamic acid derivative
CN112088001A (zh) Magl抑制剂
CN108884058B (zh) 大环广谱抗生素
WO2016198691A1 (en) Efflux-pump inhibitors and therapeutic uses thereof
AU2019383674A1 (en) Novel imidazole derivative
WO2015066413A1 (en) Oxazolidinone hydroxamic acid compounds for the treatment of bacterial infections
JP6487333B2 (ja) 抗生物質の活性を増強する活性を有するスピロイソオキサゾリン化合物
CN106800589B (zh) 一类环肽类化合物、其制备方法、药物组合物及用途
UA122084C2 (uk) Похідні піролідину як інгібітори катепсинової протеази s
Righi et al. New one-pot procedure for the synthesis of diprotected amino alcohols from unprotected vinyl aziridines
WO2023015236A2 (en) Composition and method for treatment of gram negative bacterial infection
HK40105259A (en) Diazepine derivatives useful in the treatment of clostridium difficile
HK40008443A (en) Imidazopyrrolopyridine as inhibitors of the jak family of kinases
HK40000284A (en) Macrocyclic broad spectrum antibiotics