JP5468899B2 - Fabiインヒビターとしてのアクリルアミド誘導体 - Google Patents

Fabiインヒビターとしてのアクリルアミド誘導体 Download PDF

Info

Publication number
JP5468899B2
JP5468899B2 JP2009519767A JP2009519767A JP5468899B2 JP 5468899 B2 JP5468899 B2 JP 5468899B2 JP 2009519767 A JP2009519767 A JP 2009519767A JP 2009519767 A JP2009519767 A JP 2009519767A JP 5468899 B2 JP5468899 B2 JP 5468899B2
Authority
JP
Japan
Prior art keywords
methyl
compound
acrylamide
pyrido
tetrahydro
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.)
Expired - Fee Related
Application number
JP2009519767A
Other languages
English (en)
Japanese (ja)
Other versions
JP2010501474A5 (enExample
JP2010501474A (ja
Inventor
ハインツ, ダブリュー. ポールズ,
ジェイラール ラムナウス,
ピーター サンプソン,
アンドラス トロ,
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.)
Affinium Pharmaceuticals Inc
Original Assignee
Affinium Pharmaceuticals Inc
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 Affinium Pharmaceuticals Inc filed Critical Affinium Pharmaceuticals Inc
Publication of JP2010501474A publication Critical patent/JP2010501474A/ja
Publication of JP2010501474A5 publication Critical patent/JP2010501474A5/ja
Application granted granted Critical
Publication of JP5468899B2 publication Critical patent/JP5468899B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/90Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
    • 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
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Plant Pathology (AREA)
  • Zoology (AREA)
  • Pest Control & Pesticides (AREA)
  • Environmental Sciences (AREA)
  • Agronomy & Crop Science (AREA)
  • Dentistry (AREA)
  • Wood Science & Technology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Apparatus For Disinfection Or Sterilisation (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
JP2009519767A 2006-07-20 2007-07-19 Fabiインヒビターとしてのアクリルアミド誘導体 Expired - Fee Related JP5468899B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US83205806P 2006-07-20 2006-07-20
US60/832,058 2006-07-20
PCT/CA2007/001277 WO2008009122A1 (en) 2006-07-20 2007-07-19 Acrylamide derivatives as fab i inhibitors

Publications (3)

Publication Number Publication Date
JP2010501474A JP2010501474A (ja) 2010-01-21
JP2010501474A5 JP2010501474A5 (enExample) 2013-09-12
JP5468899B2 true JP5468899B2 (ja) 2014-04-09

Family

ID=38956481

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2009519767A Expired - Fee Related JP5468899B2 (ja) 2006-07-20 2007-07-19 Fabiインヒビターとしてのアクリルアミド誘導体

Country Status (6)

Country Link
US (2) US8318720B2 (enExample)
EP (2) EP2687533B1 (enExample)
JP (1) JP5468899B2 (enExample)
CA (1) CA2658506C (enExample)
IL (1) IL196590A (enExample)
WO (1) WO2008009122A1 (enExample)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ECSP003699A (es) 1999-10-08 2002-04-23 Smithkline Beecham Corp Inhibidores de fab i
DE60230934D1 (de) * 2001-04-06 2009-03-05 Affinium Pharm Inc Fab-i-inhibitoren
EP1575951B1 (en) 2002-12-06 2014-06-25 Debiopharm International SA Heterocyclic compounds, methods of making them and their use in therapy
US8450307B2 (en) 2004-06-04 2013-05-28 Affinium Pharmaceuticals, Inc. Therapeutic agents, and methods of making and using the same
EP2687533B1 (en) 2006-07-20 2017-07-19 Debiopharm International SA Acrylamide derivatives as FAB I inhibitors
WO2008098374A1 (en) 2007-02-16 2008-08-21 Affinium Pharmaceuticals, Inc. Salts, prodrugs and polymorphs of fab i inhibitors
FR2927331B1 (fr) * 2008-02-07 2011-05-20 Centre Nat Rech Scient Nouveaux derives anti-infectieux, leur procede de preparation, compositions pharmaceutiques les contenant et leurs utilisations en therapeutique.
US8394139B2 (en) * 2008-08-29 2013-03-12 Cook Medical Technologies Llc Barbed anchors for wire stent
BR112012003661A2 (pt) 2009-08-19 2017-04-25 Ambit Biosciences Corp "compostos de biarila e métodos de uso dos mesmos."
CA2779088A1 (en) * 2009-11-16 2011-05-19 Mellitech [1,5]-diazocin derivatives
WO2011061214A1 (en) 2009-11-18 2011-05-26 Fab Pharma Sas Novel heterocyclic acrylamides and their use as pharmaceuticals
EP2579863A4 (en) * 2010-06-11 2013-11-27 Affinium Pharm Inc COMPOUNDS FOR THE TREATMENT OF BOVINE MASTITIS
CA2816983A1 (en) 2010-11-05 2012-05-10 Senomyx, Inc. Compounds useful as modulators of trpm8
CN104039782A (zh) * 2011-08-10 2014-09-10 爱尔兰詹森研发公司 抗菌的高哌啶基取代的3,4二氢1h[1,8]萘啶酮类
BR112014002958B1 (pt) * 2011-08-10 2020-10-06 Janssen Sciences Ireland Uc 3,4-dihidro-1h-[1,8]naftiridinonas substituídas com piperidinila antibacterianas, composição farmacêutica compreendendo os referidos compostos, processos para preparação destes e uso
JO3611B1 (ar) 2011-08-10 2020-08-27 Janssen Sciences Ireland Uc سايكلو بنتا (سي (بيرول 4,3 ثاني هيدرو 1 hمستبدله [8,1] نافثيريدينونات مضادة للجراثيم
KR101720885B1 (ko) 2012-06-19 2017-03-28 데비오팜 인터네셔날 에스 에이 (e)-n-메틸-n-((3-메틸벤조푸란-2-일)메틸)-3-(7-옥소-5,6,7,8-테트라히드로-1,8-나프티리딘-3-일)아크릴아미드의전구약물 유도체
WO2014072930A2 (en) * 2012-11-09 2014-05-15 Aurigene Discovery Technologies Limited Fused pyridine derivatives as antibacterial agents
EP3344613B1 (en) * 2015-08-31 2020-03-04 Dong-A Socio Holdings Co., Ltd. Heteroaryl compounds and their use as therapeutic drugs
US10392371B2 (en) 2015-10-01 2019-08-27 Senomyx, Inc. Compounds useful as modulators of TRPM8
IL287136B2 (en) 2016-02-05 2023-09-01 Denali Therapeutics Inc Receptor inhibitors - interacting with protein kinase 1
RS61312B1 (sr) 2016-02-26 2021-02-26 Debiopharm Int Sa Lek za lečenje infekcija dijabetskog stopala
US10913730B2 (en) 2016-10-10 2021-02-09 Dong-A Socio Holdings Co., Ltd. Heteroaryl compounds and their use as Mer inhibitors
HUE058802T2 (hu) 2016-12-09 2022-09-28 Denali Therapeutics Inc RIPK1 inhibitorokként alkalmas vegyületek
CA3119390A1 (en) * 2018-11-12 2020-05-22 Debiopharm International S.A. Antibiotic compounds, methods of manufacturing the same, pharmaceutical compositions containing the same and uses thereof
MY203711A (en) 2019-02-14 2024-07-15 Debiopharm Int Sa Afabicin formulation, method for making the same and uses thereof
JP7418475B2 (ja) 2019-06-14 2024-01-19 デバイオファーム インターナショナル エス.エー. バイオフィルムが関与する細菌感染症を治療するための医薬及びその使用
MX2022007412A (es) * 2019-12-19 2022-09-19 Debiopharm Int Sa Compuestos novedosos y sus usos.
CN112552303B (zh) * 2020-12-14 2021-11-30 承德医学院 嘧啶酮并二氮杂卓类化合物及其盐、其制备方法及医药用途
WO2022187329A1 (en) * 2021-03-03 2022-09-09 The Board Of Trustees Of The University Of Illinois Fabi inhibitors for gram-negative pathogens
US11999750B2 (en) 2022-01-12 2024-06-04 Denali Therapeutics Inc. Crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydropyrido [3,2-B][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide
WO2025248051A1 (en) 2024-05-31 2025-12-04 Debiopharm International S.A. Acrylamide derivatives for the treatment of diseases associated with pathogenic bacteria in the gastrointestinal system

Family Cites Families (144)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3828068A (en) 1971-05-10 1974-08-06 Tenneco Chem ((substituted indazolyl)-n1-methyl)carbamates
US4154943A (en) 1977-12-29 1979-05-15 University Of Vermont Preparation of vincadifformine
FR2619111B1 (fr) 1987-08-07 1991-01-11 Synthelabo Derives de (piperidinyl-4)methyl-2 tetrahydro-1,2,3,4 9h-pyrido (3,4-b) indole, leur preparation et leur application en therapeutique
CA2020437A1 (en) 1989-07-05 1991-01-06 Yoshihide Fuse Cinnamamide derivative
DE4126662A1 (de) 1991-08-13 1993-02-18 Boehringer Mannheim Gmbh Neue 3,5-di-tert.butyl-4-hydroxyphenyl-derivate, verfahren zu ihrer herstellung und arzneimittel
HU210679B (en) 1991-11-21 1995-06-28 Richter Gedeon Vegyeszet Process for producing new tetrahydro-pyrido/3,4-b/indol derivatives and pharmaceutical compositions containing the same
FR2692575B1 (fr) 1992-06-23 1995-06-30 Sanofi Elf Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
US5416193A (en) 1993-04-30 1995-05-16 Pfizer Inc. Coupling reagent and method
MA23420A1 (fr) 1994-01-07 1995-10-01 Smithkline Beecham Corp Antagonistes bicycliques de fibrinogene.
US5614551A (en) 1994-01-24 1997-03-25 The Johns Hopkins University Inhibitors of fatty acid synthesis as antimicrobial agents
JPH10504808A (ja) 1994-06-29 1998-05-12 スミスクライン・ビーチャム・コーポレイション ビトロネクチン受容体拮抗物質
US6176842B1 (en) 1995-03-08 2001-01-23 Ekos Corporation Ultrasound assembly for use with light activated drugs
US5989832A (en) 1995-04-21 1999-11-23 Microcide Pharmaceuticals, Inc. Method for screening for non-tetracycline efflux pump inhibitors
DE69626389T2 (de) 1995-05-11 2003-10-09 Biochemie Ges.M.B.H., Kundl Antibakterielle cephalosporinverbindungen
US6057291A (en) 1995-06-02 2000-05-02 University Of British Columbia Antimicrobial cationic peptides
JP3180350B2 (ja) 1996-02-29 2001-06-25 藤沢薬品工業株式会社 β―ラクタム系抗生物質含有錠剤およびその製造法
US6239154B1 (en) 1996-03-08 2001-05-29 Adolor Corporation Kappa agonist compounds pharmaceutical formulations and method of prevention and treatment of pruritus therewith
US6367985B1 (en) 1996-03-12 2002-04-09 Intellectual Property Company Optical connector using large diameter alignment features
US6451816B1 (en) 1997-06-20 2002-09-17 Klinge Pharma Gmbh Use of pyridyl alkane, pyridyl alkene and/or pyridyl alkine acid amides in the treatment of tumors or for immunosuppression
DE19624659A1 (de) 1996-06-20 1998-01-08 Klinge Co Chem Pharm Fab Neue Pyridylalken- und Pyridylalkinsäureamide
US6503881B2 (en) 1996-08-21 2003-01-07 Micrologix Biotech Inc. Compositions and methods for treating infections using cationic peptides alone or in combination with antibiotics
US6995254B1 (en) 1996-08-28 2006-02-07 Affinium Pharmaceuticals, Inc. Polynucleotide encoding the enoyl-acyl carrier protein reductase of Staphylococcus aureus, FAB I
BR9712072A (pt) 1996-09-20 1999-08-24 Meiji Seika Kaisha Subst-ncia cristalina de defditoren pivoxil e a produ-Æo da mesma
US6521408B1 (en) 1997-09-25 2003-02-18 National Institute Of Agrobiological Sciences Method for assessing a function of a gene
DE19641437A1 (de) 1996-10-08 1998-04-09 Basf Ag 1,3-Bis-(N-lactamyl)propane und deren pharmazeutische und kosmetische Verwendung
DE19652239A1 (de) 1996-12-16 1998-06-18 Bayer Ag Verwendung von 7-(2-Oxa-5,8-diazabicyclo[4.3.0]non-8-yl)-chinolon- und -naphthyridoncarbonsäure-Derivaten zur Therapie von Helicobacter-pylori-Infektionen und den damit assoziierten gastroduodenalen Erkrankungen
SI9600371B (sl) 1996-12-18 2005-04-30 LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d. Etilidenski derivati tricikličnih karbapenemov
AU6870098A (en) 1997-03-31 1998-10-22 Du Pont Merck Pharmaceutical Company, The Indazoles of cyclic ureas useful as hiv protease inhibitors
ATE389417T1 (de) 1997-04-01 2008-04-15 Borody Thomas J Verfahren und zusammensetzungen zur behandlung entzündlicher darmerkrankungen
US6406880B1 (en) 1997-05-02 2002-06-18 Integrated Research Technology, Llc Betaines as adjuvants to susceptibility testing and antimicrobial therapy
US6184363B1 (en) 1997-06-13 2001-02-06 Northwestern University Inhibitors of β-lactamases and uses therefor
US6207679B1 (en) 1997-06-19 2001-03-27 Sepracor, Inc. Antimicrobial agents uses and compositions related thereto
WO1998058928A1 (fr) 1997-06-23 1998-12-30 Yoshitomi Pharmaceutical Industries, Ltd. Agent prophylactique ou therapeutique contre des maladies attribuables a une infection par des helicobacters
AUPO758297A0 (en) 1997-06-27 1997-07-24 Rowe, James Baber Control of acidic gut syndrome
US6198000B1 (en) 1997-07-07 2001-03-06 Pfizer Inc. Intermediates useful in the synthesis of quinoline antibiotics
EP1000935A4 (en) 1997-07-25 2001-03-21 Tsumura & Co PYRIDYL ACRYLAMIDE DERIVATIVES AND DRUGS AGAINST NEPHRITIS AND INHIBITORS OF THE TRANSFORMING GROWTH FACTOR BETA CONTAINING THESE DERIVATIVES
HN1998000106A (es) 1997-08-01 1999-01-08 Pfizer Prod Inc Composiciones parenterales de alatroflaxacino
US5932743A (en) 1997-08-21 1999-08-03 American Home Products Corporation Methods for the solid phase synthesis of substituted indole compounds
GB9717804D0 (en) 1997-08-22 1997-10-29 Zeneca Ltd Chemical compounds
RU2224024C2 (ru) 1997-10-31 2004-02-20 Зингента Партисипейшнс Аг Трансгенные растения
US6432444B1 (en) 1997-10-31 2002-08-13 New Horizons Diagnostics Corp Use of bacterial phage associated lysing enzymes for treating dermatological infections
ATE231841T1 (de) 1997-11-07 2003-02-15 Schering Corp Phenyl-alkyl imidazole als h3 rezeptor antagonisten
SE9704404D0 (sv) 1997-11-28 1997-11-28 Astra Ab New compounds
GB9725244D0 (en) 1997-11-29 1998-01-28 Zeneca Ltd Chemical compounds
DE19753298A1 (de) 1997-12-01 1999-06-02 Basf Ag Verfahren zur Herstellung von festen Dosierungsformen
EP1051978B1 (en) 1998-01-07 2012-08-22 Meiji Seika Pharma Co., Ltd. Crystallographically stable amorphous cephalosporin compositions and process for producing the same
US6184380B1 (en) 1999-01-25 2001-02-06 Pfizer Inc. Process for preparing naphthyridones and intermediates
US6248343B1 (en) 1998-01-20 2001-06-19 Ethicon, Inc. Therapeutic antimicrobial compositions
PA8466701A1 (es) 1998-01-21 2000-09-29 Pfizer Prod Inc Comprimido de mesilato de trovafloxacino
US6204279B1 (en) 1998-06-03 2001-03-20 Microcide Pharmaceuticals, Inc. Peptidomimetic efflux pump inhibitors
US6503539B2 (en) 1998-02-27 2003-01-07 Biora Bioex Ab Matrix protein compositions for wound healing
US6350738B1 (en) 1998-03-06 2002-02-26 Brigham Young University Steroid derived antibiotics
US6369049B1 (en) 1998-04-30 2002-04-09 Eli Lilly And Company Treatment of mastitis
DE19820801A1 (de) 1998-05-09 1999-11-25 Gruenenthal Gmbh Orale Arzneiformen mit reproduzierbarer Wirkstofffreisetzung von Gatifloxacin oder pharmazeutisch verwendbaren Salzen oder Hydraten
DE19821039A1 (de) 1998-05-11 1999-11-18 Bayer Ag Verfahren zur Herstellung von (S,S)-Benzyl-2,8-diazabicyclo[4.3.0]nonan
US6399629B1 (en) 1998-06-01 2002-06-04 Microcide Pharmaceuticals, Inc. Efflux pump inhibitors
US6428579B1 (en) 1998-07-01 2002-08-06 Brown University Research Foundation Implantable prosthetic devices coated with bioactive molecules
US6423741B1 (en) 1998-07-10 2002-07-23 Council Of Scientific And Industrial Research Anti-microbial composition and method for producing the same
GB9815567D0 (en) 1998-07-18 1998-09-16 Glaxo Group Ltd Antiviral compound
PT1101497E (pt) 1998-08-04 2008-04-23 Schering Plough Animal Health Preparações oleosas estabilizadas de tobicilina (antibiótico beta-lactâmico)
CN1133432C (zh) 1998-08-21 2004-01-07 千寿制药株式会社 含水液体药物组合物
US6461607B1 (en) 1998-08-24 2002-10-08 Ganeden Biotech, Inc. Probiotic, lactic acid-producing bacteria and uses thereof
US6518487B1 (en) 1998-09-23 2003-02-11 Pioneer Hi-Bred International, Inc. Cyclin D polynucleotides, polypeptides and uses thereof
US6509327B1 (en) 1998-09-30 2003-01-21 Alcon Manufacturing, Ltd. Compositions and methods for treating otic, ophthalmic and nasal infections
US6395746B1 (en) 1998-09-30 2002-05-28 Alcon Manufacturing, Ltd. Methods of treating ophthalmic, otic and nasal infections and attendant inflammation
DE19851104C2 (de) 1998-11-06 2003-04-03 Huhtamaki Forchheim Verfahren zum Herstellen eines mehrschichtigen Verbundes
TW526202B (en) 1998-11-27 2003-04-01 Shionogi & Amp Co Broad spectrum cephem having benzo[4,5-b]pyridium methyl group of antibiotic activity
AU768957B2 (en) 1999-02-18 2004-01-08 Regents Of The University Of California, The Phthalamide-lanthanide complexes for use as luminescent markers
US6235728B1 (en) 1999-02-19 2001-05-22 Bristol-Myers Squibb Company Water-soluble prodrugs of azole compounds
US6248363B1 (en) 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
US6294192B1 (en) 1999-02-26 2001-09-25 Lipocine, Inc. Triglyceride-free compositions and methods for improved delivery of hydrophobic therapeutic agents
US6267985B1 (en) 1999-06-30 2001-07-31 Lipocine Inc. Clear oil-containing pharmaceutical compositions
AU3615200A (en) 1999-03-03 2000-09-21 Princeton University Bacterial transglycosylases: assays for monitoring the activity using lipid ii substrate analogs and methods for discovering new antibiotics
US6495161B1 (en) 1999-03-09 2002-12-17 Vivorx, Inc. Cytoprotective biocompatible containment systems for biologically active materials and methods of making same
US6239113B1 (en) 1999-03-31 2001-05-29 Insite Vision, Incorporated Topical treatment or prevention of ocular infections
US6224579B1 (en) 1999-03-31 2001-05-01 The Trustees Of Columbia University In The City Of New York Triclosan and silver compound containing medical devices
AU4230900A (en) 1999-04-08 2000-10-23 General Hospital Corporation, The Purposeful movement of human migratory cells away from an agent source
CO5180550A1 (es) 1999-04-19 2002-07-30 Smithkline Beecham Corp Inhibidores de fab i
US6290946B1 (en) 1999-05-13 2001-09-18 Geltex Pharmaceuticals, Inc. Anionic polymers as toxin binders and antibacterial agents
US6514535B2 (en) 1999-05-21 2003-02-04 Noveon Ip Holdings Corp. Bioadhesive hydrogels with functionalized degradable crosslinks
AR024077A1 (es) 1999-05-25 2002-09-04 Smithkline Beecham Corp Compuestos antibacterianos
CO5370679A1 (es) 1999-06-01 2004-02-27 Smithkline Beecham Corp Inhibidores fab 1
US6239141B1 (en) 1999-06-04 2001-05-29 Pfizer Inc. Trovafloxacin oral suspensions
CO5180605A1 (es) 1999-06-23 2002-07-30 Smithkline Beecham Corp Compuestos de indol
CA2282066C (en) 1999-06-29 2010-09-07 Smithkline Beecham Corporation Methods of use of quinolone compounds against atypical upper respiratory pathogenic bacteria
US6309663B1 (en) 1999-08-17 2001-10-30 Lipocine Inc. Triglyceride-free compositions and methods for enhanced absorption of hydrophilic therapeutic agents
US6500459B1 (en) 1999-07-21 2002-12-31 Harinderpal Chhabra Controlled onset and sustained release dosage forms and the preparation thereof
US6346391B1 (en) 1999-07-22 2002-02-12 Trustees Of Tufts College Methods of reducing microbial resistance to drugs
EP1212093B1 (en) 1999-08-26 2004-07-07 Ganeden Biotech, Inc. Use of emu oil as a carrier for antifungal, antibacterial and antiviral medications
US6221859B1 (en) 1999-08-27 2001-04-24 Merck & Co., Inc. Carbapenem antibacterial compositions and methods of the treatment
US6174878B1 (en) 1999-08-31 2001-01-16 Alcon Laboratories, Inc. Topical use of kappa opioid agonists to treat otic pain
US6428444B1 (en) * 1999-09-06 2002-08-06 Toyota Jidosha Kabushiki Kaisha Apparatus for controlling a vehicle and a method of controlling the vehicle
CN1373674A (zh) 1999-09-11 2002-10-09 宝洁公司 易流动液体载体
DE60025503T2 (de) 1999-09-17 2006-09-07 Daiichi Asubio Pharma Co., Ltd. Pharmazeutische Zusammensetzungen, die Faropenem-Natrium und eine Diaminoacetat Verbindung zur Verbesserung der Magen-Darm-Trakt Absorption enthalten
US6500463B1 (en) 1999-10-01 2002-12-31 General Mills, Inc. Encapsulation of sensitive components into a matrix to obtain discrete shelf-stable particles
DE60029235T2 (de) 1999-10-08 2007-06-14 Affinium Pharmaceuticals, Inc., Toronto Fab-i-hemmer
US6730684B1 (en) 1999-10-08 2004-05-04 Affinium Pharmaceuticals, Inc. Fab I inhibitors
DE60019954T2 (de) 1999-10-08 2006-02-23 Affinium Pharmaceuticals, Inc., Toronto Fab i hemmer
ECSP003699A (es) 1999-10-08 2002-04-23 Smithkline Beecham Corp Inhibidores de fab i
US6762201B1 (en) 1999-10-08 2004-07-13 Affinium Pharmaceuticals, Inc. Fab I inhibitors
CA2323008C (en) 1999-10-11 2005-07-12 Pfizer Inc. Pharmaceutically active compounds
EP1227096B1 (en) 1999-10-19 2004-09-22 Sato Pharmaceutical Co. Ltd. 4-oxoquinolizine antimicrobials having 2-pyridone skeletons as the partial structure
US6951729B1 (en) 1999-10-27 2005-10-04 Affinium Pharmaceuticals, Inc. High throughput screening method for biological agents affecting fatty acid biosynthesis
CN1188111C (zh) 1999-10-29 2005-02-09 耐科塔医药公司 分散性得到改进的干粉组合物
US6531291B1 (en) 1999-11-10 2003-03-11 The Trustees Of Columbia University In The City Of New York Antimicrobial activity of gemfibrozil and related compounds and derivatives and metabolites thereof
US6514986B2 (en) 2000-11-22 2003-02-04 Wockhardt Limited Chiral fluoroquinolone arginine salt forms
US6656703B1 (en) 1999-12-29 2003-12-02 Millennium Pharamaceuticals, Inc. High throughput screen for inhibitors of fatty acid biosynthesis in bacteria
US6372752B1 (en) 2000-02-07 2002-04-16 Genzyme Corporation Inha inhibitors and methods of use thereof
ES2179729B1 (es) 2000-03-23 2003-12-16 Dreiman Lab Farmaceuticos S A Forma farmaceutica solida de administracion oral dispersable en agua, que comprende rifampicina, isoniazida y piridoxina hidrocloruro, procedimiento para su obtencion y forma de presentacion de dicha forma farmaceutica.
AU2000255628A1 (en) 2000-03-28 2001-10-08 Council Of Scientific And Industrial Research Formulation comprising thymol useful in the treatment of drug resistant bacterial infections
JP2003531184A (ja) 2000-04-21 2003-10-21 ローディア/カイレックス・インコーポレイテッド (r)−1−(アリールオキシ)プロパン−2−オールの製造方法
WO2002007682A1 (en) 2000-07-26 2002-01-31 Vyden John K Methods for treating atopic disorders
DE10037029A1 (de) 2000-07-27 2002-02-28 Kugelstrahlzentrum Aachen Gmbh Verfahren und Vorrichtung zum Umformen von Strukturbauteilen
US6288239B1 (en) 2000-09-19 2001-09-11 Board Of Trustees Operating Michigan State University 5-trityloxymethyl-oxazolidinones and process for the preparation thereof
US7048926B2 (en) 2000-10-06 2006-05-23 Affinium Pharmaceuticals, Inc. Methods of agonizing and antagonizing FabK
US6821746B2 (en) 2000-10-06 2004-11-23 Affinium Pharmaceuticals, Inc. Methods of screening for FabK antagonists and agonists
HUP0400651A2 (hu) 2000-11-07 2004-06-28 Bristol-Myers Squibb Company Szerin proteáz inhibitorokként alkalmazható savszármazékok és ezeket tartalmazó gyógyszerkészítmények
WO2002048097A1 (en) 2000-12-12 2002-06-20 Corvas International, Inc. Compounds, compositions and methods for treatment of parasitic infections
US6388070B1 (en) 2001-01-05 2002-05-14 Orchid Chemicals & Pharmaceuticals Ltd. Thioester derivatives of thiazolyl acetic acid and their use in the preparation of cephalosporin compounds
US6495158B1 (en) 2001-01-19 2002-12-17 Lec Tec Corporation Acne patch
PA8539401A1 (es) 2001-02-14 2002-10-28 Warner Lambert Co Quinazolinas como inhibidores de mmp-13
DE60230934D1 (de) * 2001-04-06 2009-03-05 Affinium Pharm Inc Fab-i-inhibitoren
US6503906B1 (en) 2002-02-21 2003-01-07 Ren-Jin Lee Method for optimizing ciprofloxacin treatment of anthrax-exposed patients according to the patient's characteristics
MXPA04009580A (es) 2002-04-02 2005-05-27 Tsumura & Co Inhibidor de fosfodiesterasa iv que contiene un derivado de piridilacrilamida.
WO2004014869A2 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc 5,6-fused 3,4-dihydropyrimidine-2-one derivatives as matrix metalloproteinase inhibitors
EP1575951B1 (en) * 2002-12-06 2014-06-25 Debiopharm International SA Heterocyclic compounds, methods of making them and their use in therapy
WO2004082586A2 (en) 2003-03-17 2004-09-30 Affinium Pharmaceuticals, Inc. Phamaceutical compositions comprising inhibitors of fab i and further antibiotics
US7745625B2 (en) 2004-03-15 2010-06-29 Bristol-Myers Squibb Company Prodrugs of piperazine and substituted piperidine antiviral agents
US8450307B2 (en) 2004-06-04 2013-05-28 Affinium Pharmaceuticals, Inc. Therapeutic agents, and methods of making and using the same
CN101115761B (zh) 2005-01-19 2012-07-18 里格尔药品股份有限公司 2,4-嘧啶二胺化合物的前药及其应用
CA2632476A1 (en) 2005-12-05 2007-06-14 Affinium Pharmaceuticals, Inc. Heterocyclylacrylamide compounds as fabi inhibitors and antibacterial agents
EP2687533B1 (en) 2006-07-20 2017-07-19 Debiopharm International SA Acrylamide derivatives as FAB I inhibitors
EP2420505A1 (en) 2006-11-21 2012-02-22 Rigel Pharmaceuticals, Inc. Prodrug salts of 2, 4- pyrimidinediamine compounds and their uses
WO2008098374A1 (en) 2007-02-16 2008-08-21 Affinium Pharmaceuticals, Inc. Salts, prodrugs and polymorphs of fab i inhibitors
US20090012045A1 (en) 2007-06-26 2009-01-08 Rigel Pharmaceuticals, Inc. Methods of Treating Cell Proliferative Disorders
CA2757954A1 (en) 2009-04-08 2010-10-14 C & D Zodiac, Inc. Vehicle seat tubing having variable wall thickness
UA108077C2 (xx) 2009-07-02 2015-03-25 Синтез динатрієвої солі n4-(2,2-диметил-4-$(дигідрофосфонокси)метил]-3-оксо-5-піридо$1,4]оксазин-6-іл)-5-фтор-n2-(3,4,5-триметоксифеніл)-2,4-піримідиндіаміну
WO2011061214A1 (en) 2009-11-18 2011-05-26 Fab Pharma Sas Novel heterocyclic acrylamides and their use as pharmaceuticals
EP2579863A4 (en) 2010-06-11 2013-11-27 Affinium Pharm Inc COMPOUNDS FOR THE TREATMENT OF BOVINE MASTITIS
CN102675311A (zh) 2011-06-14 2012-09-19 苏春华 一种氟代丙烯酰胺的衍生物
JP6013846B2 (ja) 2011-10-06 2016-10-25 リコー電子デバイス株式会社 スイッチングレギュレータ及び電子機器
US8975502B1 (en) 2012-05-15 2015-03-10 Rodulfo Delgado Guitar with body-mounted tuning system
KR101720885B1 (ko) 2012-06-19 2017-03-28 데비오팜 인터네셔날 에스 에이 (e)-n-메틸-n-((3-메틸벤조푸란-2-일)메틸)-3-(7-옥소-5,6,7,8-테트라히드로-1,8-나프티리딘-3-일)아크릴아미드의전구약물 유도체
US8973902B2 (en) 2012-12-21 2015-03-10 Comeup Industries Inc. Power winch horizontal-pull clutch device

Also Published As

Publication number Publication date
EP2687533A3 (en) 2014-04-16
US20100130470A1 (en) 2010-05-27
JP2010501474A (ja) 2010-01-21
IL196590A (en) 2017-03-30
US8895545B2 (en) 2014-11-25
CA2658506A1 (en) 2008-01-24
WO2008009122A1 (en) 2008-01-24
IL196590A0 (en) 2009-11-18
US20130237523A1 (en) 2013-09-12
EP2054422A4 (en) 2012-10-03
EP2687533A2 (en) 2014-01-22
EP2054422B1 (en) 2017-06-14
EP2687533B1 (en) 2017-07-19
EP2054422A1 (en) 2009-05-06
US8318720B2 (en) 2012-11-27
CA2658506C (en) 2016-01-26

Similar Documents

Publication Publication Date Title
JP5468899B2 (ja) Fabiインヒビターとしてのアクリルアミド誘導体
JP5087406B2 (ja) 治療薬ならびにその製造方法および使用方法
JP2012006927A (ja) ヘテロ環化合物、その製造方法および治療におけるその使用
JP4880448B2 (ja) 複数の抗生物質を含む組成物、及びそれを用いる方法
JP2009518399A (ja) 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
CN101415701A (zh) 作为fabi抑制剂的杂环丙烯酰胺化合物和抗菌剂
EA043636B1 (ru) АНТИБАКТЕРИАЛЬНЫЕ 3,4-ДИГИДРО-1Н-[1,8]НАФТИРИДИНОНЫ, ЗАМЕЩЕННЫЕ ЦИКЛОПЕНТА[с]ПИРРОЛОМ

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20100715

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20100715

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20130415

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20130422

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20130515

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20130522

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20130617

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20130624

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130716

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20130716

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20140107

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20140130

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees