JP2009518399A - Ｆａｂｉ阻害剤および抗菌剤としてのヘテロ環アクリルアミド化合物 - Google Patents

Ｆａｂｉ阻害剤および抗菌剤としてのヘテロ環アクリルアミド化合物 Download PDF

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JP2009518399A
JP2009518399A JP2008544384A JP2008544384A JP2009518399A JP 2009518399 A JP2009518399 A JP 2009518399A JP 2008544384 A JP2008544384 A JP 2008544384A JP 2008544384 A JP2008544384 A JP 2008544384A JP 2009518399 A JP2009518399 A JP 2009518399A
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Prior art keywords
methyl
acrylamide
oxo
naphthyridin
pyrido
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Japanese (ja)
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JP2009518399A5 (cg-RX-API-DMAC10.html
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ヘンリー ポールズ，
ジャッド， エム． バーマン，
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Affinium Pharmaceuticals Inc
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Affinium Pharmaceuticals Inc
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Publication of JP2009518399A5 publication Critical patent/JP2009518399A5/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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 three or more hetero 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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61P31/02—Local antiseptics
    • 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
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/20—Spiro-condensed 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2008544384A 2005-12-05 2006-12-01 Ｆａｂｉ阻害剤および抗菌剤としてのヘテロ環アクリルアミド化合物 Pending JP2009518399A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US74251405P 2005-12-05 2005-12-05
US75402405P 2005-12-23 2005-12-23
PCT/US2006/045903 WO2007067416A2 (en) 2005-12-05 2006-12-01 Heterocyclylacrylamide compounds as fabi inhibitors and antibacterial agents

Publications (2)

Publication Number Publication Date
JP2009518399A true JP2009518399A (ja) 2009-05-07
JP2009518399A5 JP2009518399A5 (cg-RX-API-DMAC10.html) 2010-01-14

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JP2008544384A Pending JP2009518399A (ja) 2005-12-05 2006-12-01 Ｆａｂｉ阻害剤および抗菌剤としてのヘテロ環アクリルアミド化合物

Country Status (7)

Country Link
US (1) US20090156578A1 (cg-RX-API-DMAC10.html)
EP (1) EP1973902A2 (cg-RX-API-DMAC10.html)
JP (1) JP2009518399A (cg-RX-API-DMAC10.html)
KR (1) KR20080075027A (cg-RX-API-DMAC10.html)
CA (1) CA2632476A1 (cg-RX-API-DMAC10.html)
IL (1) IL191987A0 (cg-RX-API-DMAC10.html)
WO (1) WO2007067416A2 (cg-RX-API-DMAC10.html)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010501474A (ja) * 2006-07-20 2010-01-21 アフィニウム ファーマシューティカルズ， インク． Ｆａｂｉインヒビターとしてのアクリルアミド誘導体
JP2022506957A (ja) * 2018-11-12 2022-01-17 デバイオファーム インターナショナル エス．エー． 抗生物質化合物、それを製造する方法、それを含む医薬組成物及びその使用
JP2023507400A (ja) * 2019-12-19 2023-02-22 デバイオファーム インターナショナル エス．エー． 新規な化合物及びその使用

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ES2231275T3 (es) 1999-10-08 2005-05-16 Affinium Pharmaceuticals, Inc. Inhibidores de fab i.
JP4387804B2 (ja) * 2001-04-06 2009-12-24 アフィニアム・ファーマシューティカルズ・インコーポレイテッド ＦａｂＩ阻害剤
PT1575951E (pt) * 2002-12-06 2014-09-15 Debiopharm Int Sa Compostos heterocíclicos, métodos para os preparar e sua utilização em terapia
US8450307B2 (en) * 2004-06-04 2013-05-28 Affinium Pharmaceuticals, Inc. Therapeutic agents, and methods of making and using the same
WO2008098374A1 (en) * 2007-02-16 2008-08-21 Affinium Pharmaceuticals, Inc. Salts, prodrugs and polymorphs of fab i inhibitors
JP5270943B2 (ja) * 2008-03-28 2013-08-21 大阪瓦斯株式会社 フルオレン誘導体およびこのフルオレン誘導体を用いたアミノ基含有フルオレン誘導体の製造方法
KR20120059558A (ko) 2009-08-19 2012-06-08 암비트 바이오사이언시즈 코포레이션 바이아릴 화합물 및 이의 사용 방법
CA2776849A1 (en) 2009-11-18 2011-05-26 Fab Pharma S.A.S. Novel heterocyclic acrylamides and their use as pharmaceuticals
EP2758376A4 (en) * 2011-09-19 2015-04-29 Vitas Pharma Res Private Ltd HETEROCYCLIC COMPOUNDS AS INHIBITORS OF FATTY ACID BIOSYNTHESIS FOR BACTERIAL INFECTIONS
EP2861608B8 (en) 2012-06-19 2019-06-19 Debiopharm International SA Prodrug derivatives of (e)-n-methyl-n-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide
US9815850B2 (en) 2016-02-05 2017-11-14 Denali Therapeutics Inc. Compounds, compositions and methods
DK3419628T3 (da) 2016-02-26 2021-01-11 Debiopharm Int Sa Medikament til behandling af diabetiske fodinfektioner
LT3552017T (lt) 2016-12-09 2022-05-10 Denali Therapeutics Inc. Junginiai, naudotini kaip ripk1 inhibitoriai
US11691967B2 (en) 2018-03-12 2023-07-04 The Board Of Trustees Of The University Of Illinois Antibiotics effective for gram-negative pathogens
ES2944535T3 (es) 2019-02-14 2023-06-22 Debiopharm Int Sa Formulación de afabicina, método para preparar la misma
UA129222C2 (uk) 2019-06-14 2025-02-12 Дебіофарм Інтернешнл С.А. Лікарський засіб і його застосування для лікування бактеріальних інфекцій, пов'язаних з біоплівкою
WO2022187329A1 (en) * 2021-03-03 2022-09-09 The Board Of Trustees Of The University Of Illinois Fabi inhibitors for gram-negative pathogens
WO2022268890A1 (en) 2021-06-23 2022-12-29 Debiopharm International S.A. Novel compounds and their use
CN113861137B (zh) * 2021-09-26 2023-08-15 重庆医科大学 酮与alpha氯代酮一步反应合成呋喃类化合物的方法
EP4463229A1 (en) 2022-01-12 2024-11-20 Denali Therapeutics Inc. Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2, 3,4,5- tetrahydropyrido [3,2-b] [l,4]oxazepin-3-yl)-4h-l,2,4-triazole-3-carboxamide
EP4768485A1 (en) * 2023-10-07 2026-07-01 Guangzhou Baiyunshan Pharmaceutical Holdings Co., Ltd. Baiyunshan Pharmaceutical General Factory FABI ENZYME INHIBITOR AND ITS USES
EP4791392A1 (en) 2023-10-09 2026-08-19 Debiopharm International SA Antibiotic compounds for treating bacterial infections

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