JP2014518267A - 細菌感染症の治療のための架橋二環式化合物 - Google Patents

細菌感染症の治療のための架橋二環式化合物 Download PDF

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JP2014518267A
JP2014518267A JP2014518932A JP2014518932A JP2014518267A JP 2014518267 A JP2014518267 A JP 2014518267A JP 2014518932 A JP2014518932 A JP 2014518932A JP 2014518932 A JP2014518932 A JP 2014518932A JP 2014518267 A JP2014518267 A JP 2014518267A
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oxabicyclo
methyl
naphthyridin
ethyl
pyrido
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JP2014518267A5 (enExample
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保路 福田
イー．カエリン ジュニア デビッド
ビー．シングフ シェオ
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
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    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—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 sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • 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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • 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
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • 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
    • C07D493/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07D495/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D515/04—Ortho-condensed systems
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2014518932A 2011-06-27 2012-06-26 細菌感染症の治療のための架橋二環式化合物 Pending JP2014518267A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161501692P 2011-06-27 2011-06-27
US61/501,692 2011-06-27
PCT/US2012/044267 WO2013003383A1 (en) 2011-06-27 2012-06-26 Bridged bicyclic compounds for the treatment of bacterial infections

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JP2014518267A true JP2014518267A (ja) 2014-07-28
JP2014518267A5 JP2014518267A5 (enExample) 2015-08-06

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US (1) US20140243302A1 (enExample)
EP (1) EP2723737A1 (enExample)
JP (1) JP2014518267A (enExample)
AU (1) AU2012275499A1 (enExample)
CA (1) CA2840060A1 (enExample)
WO (1) WO2013003383A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015508069A (ja) * 2012-02-10 2015-03-16 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 ナフチリジン誘導体の製造方法
JP2019517546A (ja) * 2016-06-08 2019-06-24 アジェンデ・キミケ・リウニテ・アンジェリニ・フランチェスコ・ア・チ・エレ・ア・エフェ・ソシエタ・ペル・アチオニＡｚｉｅｎｄｅ Ｃｈｉｍｉｃｈｅ Ｒｉｕｎｉｔｅ Ａｎｇｅｌｉｎｉ Ｆｒａｎｃｅｓｃｏ Ａ．Ｃ．Ｒ．Ａ．Ｆ．Ｓｏｃｉｅｔａ Ｐｅｒ Ａｚｉｏｎｉ 新しい抗菌性化合物

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GB201111705D0 (en) 2011-07-07 2011-08-24 Takeda Pharmaceutical Compounds and their use
JO3115B1 (ar) 2011-08-22 2017-09-20 Takeda Pharmaceuticals Co مركبات بيريدازينون واستخدامها كمثبطات daao
JP6169492B2 (ja) 2011-11-15 2017-07-26 武田薬品工業株式会社 ジヒドロキシ芳香族へテロ環化合物
GB201222711D0 (en) 2012-12-17 2013-01-30 Takeda Pharmaceutical Novel compounds
JP6112724B2 (ja) * 2013-10-31 2017-04-12 日本化薬株式会社 １，５−ナフチリジン誘導体およびそれを有効成分として含んでなる殺虫剤
ES2669208T3 (es) 2014-01-06 2018-05-24 Bristol-Myers Squibb Company Derivados de pirrolidinilsulfona y su uso como moduladores de ROR gamma
EP3050888A1 (en) 2015-01-27 2016-08-03 Merck Sharp & Dohme Corp. Compounds for the treatment of bacterial infections
UY36851A (es) 2015-08-16 2017-03-31 Glaxosmithkline Ip Dev Ltd Compuestos para uso en aplicaciones antibacterianas
WO2017153235A1 (de) 2016-03-09 2017-09-14 Bayer Pharma Aktiengesellschaft Substituierte n-cyclo-3-aryl-1-naphthamide und ihre verwendung
WO2018047081A1 (en) 2016-09-09 2018-03-15 Novartis Ag Compounds and compositions as inhibitors of endosomal toll-like receptors
KR20200092332A (ko) * 2017-11-02 2020-08-03 칼리코 라이프 사이언시스 엘엘씨 통합된 스트레스 경로의 조절제
EP3807290B1 (en) 2018-06-15 2022-03-30 Bristol-Myers Squibb Company Tetrahydropyran-based thiodisaccharide mimics as galectin-3 inhibitors
CN108947940A (zh) * 2018-06-20 2018-12-07 天津全和诚科技有限责任公司 一种2-氧杂环丁烷衍生物的合成方法
EP3911641A1 (en) 2019-01-14 2021-11-24 Innate Tumor Immunity, Inc. Nlrp3 modulators
WO2020160151A1 (en) 2019-01-31 2020-08-06 Kyorin Pharmaceutical Co., Ltd. 15-pgdh inhibitors
CN116075512A (zh) 2020-06-11 2023-05-05 Chdi基金会股份有限公司 用于对亨廷顿蛋白成像的杂环化合物和显像剂
AU2021385752A1 (en) 2020-11-26 2023-06-29 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Fused tricyclic compound, preparation method therefor and application thereof in medicine
CN114957056A (zh) * 2021-02-20 2022-08-30 帕潘纳(北京)科技有限公司 制备3-甲基-2-氯-4-甲基磺酰基苯甲酸甲酯及其中间体的方法

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WO2009147616A1 (en) * 2008-06-03 2009-12-10 Actelion Pharmaceuticals Ltd [4-(1-amino-ethyl) -cyclohexyl] -methyl-amine and [6-(1-amino-ethyl) -tetrahydro- pyran-3-yl] -methyl-amine derivatives as antibacterials
WO2010043714A1 (en) * 2008-10-17 2010-04-22 Glaxo Group Limited Tricyclic nitrogen compounds used as antibacterials
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WO2010116337A1 (en) * 2009-04-09 2010-10-14 Actelion Pharmaceuticals Ltd 2-hydroxyethyl-1h-quinolin-2-one derivatives and their azaisosteric analogues with antibacterial activity

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PT1230243E (pt) 1999-11-12 2009-06-12 Biogen Idec Inc Policicloalquilpurinas como antagonistas dos receptores da adenosina
JP4887297B2 (ja) * 2004-09-24 2012-02-29 アクテリオン ファーマシューティカルズ リミテッド 新規二環式抗生物質
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WO2008152603A1 (en) * 2007-06-15 2008-12-18 Actelion Pharmaceuticals Ltd 3-amino-6-(1-amino-ethyl)-tetrahydropyran derivatives
WO2009147616A1 (en) * 2008-06-03 2009-12-10 Actelion Pharmaceuticals Ltd [4-(1-amino-ethyl) -cyclohexyl] -methyl-amine and [6-(1-amino-ethyl) -tetrahydro- pyran-3-yl] -methyl-amine derivatives as antibacterials
WO2010043714A1 (en) * 2008-10-17 2010-04-22 Glaxo Group Limited Tricyclic nitrogen compounds used as antibacterials
WO2010055348A1 (en) * 2008-11-14 2010-05-20 Astrazeneca Ab [4- (1-amino-ethyl) -cyclohexyl] -methyl-amines as antibacterials
WO2010067332A1 (en) * 2008-12-12 2010-06-17 Actelion Pharmaceuticals Ltd 5-amino-2-(1-hydroxy-ethyl)-tetrahydropyran derivatives
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015508069A (ja) * 2012-02-10 2015-03-16 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 ナフチリジン誘導体の製造方法
JP2019517546A (ja) * 2016-06-08 2019-06-24 アジェンデ・キミケ・リウニテ・アンジェリニ・フランチェスコ・ア・チ・エレ・ア・エフェ・ソシエタ・ペル・アチオニＡｚｉｅｎｄｅ Ｃｈｉｍｉｃｈｅ Ｒｉｕｎｉｔｅ Ａｎｇｅｌｉｎｉ Ｆｒａｎｃｅｓｃｏ Ａ．Ｃ．Ｒ．Ａ．Ｆ．Ｓｏｃｉｅｔａ Ｐｅｒ Ａｚｉｏｎｉ 新しい抗菌性化合物

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EP2723737A1 (en) 2014-04-30
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US20140243302A1 (en) 2014-08-28
AU2012275499A1 (en) 2013-12-19

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