KR101720885B1 - (e)-n-메틸-n-((3-메틸벤조푸란-2-일)메틸)-3-(7-옥소-5,6,7,8-테트라히드로-1,8-나프티리딘-3-일)아크릴아미드의전구약물 유도체 - Google Patents

(e)-n-메틸-n-((3-메틸벤조푸란-2-일)메틸)-3-(7-옥소-5,6,7,8-테트라히드로-1,8-나프티리딘-3-일)아크릴아미드의전구약물 유도체 Download PDF

Info

Publication number
KR101720885B1
KR101720885B1 KR1020157001113A KR20157001113A KR101720885B1 KR 101720885 B1 KR101720885 B1 KR 101720885B1 KR 1020157001113 A KR1020157001113 A KR 1020157001113A KR 20157001113 A KR20157001113 A KR 20157001113A KR 101720885 B1 KR101720885 B1 KR 101720885B1
Authority
KR
South Korea
Prior art keywords
compound
methyl
rti
administration
alkyl
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
KR1020157001113A
Other languages
English (en)
Korean (ko)
Other versions
KR20150023779A (ko
Inventor
존 제이. 파트리지
존 콜루치
이브 개류
미셸 테리엔
로버트 잠보니
배리 하프킨
앤소니 마르파트
헬미 자데인
Original Assignee
데비오팜 인터네셔날 에스 에이
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 데비오팜 인터네셔날 에스 에이 filed Critical 데비오팜 인터네셔날 에스 에이
Publication of KR20150023779A publication Critical patent/KR20150023779A/ko
Application granted granted Critical
Publication of KR101720885B1 publication Critical patent/KR101720885B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • C07F9/582
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/58Pyridine rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/60Quinoline or hydrogenated quinoline ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/662Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020157001113A 2012-06-19 2013-06-19 (e)-n-메틸-n-((3-메틸벤조푸란-2-일)메틸)-3-(7-옥소-5,6,7,8-테트라히드로-1,8-나프티리딘-3-일)아크릴아미드의전구약물 유도체 Active KR101720885B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261661559P 2012-06-19 2012-06-19
US61/661,559 2012-06-19
PCT/IB2013/001780 WO2013190384A1 (en) 2012-06-19 2013-06-19 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

Publications (2)

Publication Number Publication Date
KR20150023779A KR20150023779A (ko) 2015-03-05
KR101720885B1 true KR101720885B1 (ko) 2017-03-28

Family

ID=49768192

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020157001113A Active KR101720885B1 (ko) 2012-06-19 2013-06-19 (e)-n-메틸-n-((3-메틸벤조푸란-2-일)메틸)-3-(7-옥소-5,6,7,8-테트라히드로-1,8-나프티리딘-3-일)아크릴아미드의전구약물 유도체

Country Status (34)

Country Link
US (2) US8901105B2 (enExample)
EP (1) EP2861608B8 (enExample)
JP (2) JP6085026B2 (enExample)
KR (1) KR101720885B1 (enExample)
CN (1) CN104684922B (enExample)
AU (1) AU2013279021C1 (enExample)
BR (2) BR122021020778B1 (enExample)
CA (1) CA2875916C (enExample)
CL (1) CL2014003472A1 (enExample)
CY (1) CY1122006T1 (enExample)
DK (1) DK2861608T3 (enExample)
EA (1) EA028136B1 (enExample)
ES (1) ES2731474T3 (enExample)
HR (1) HRP20190980T1 (enExample)
HU (1) HUE043836T2 (enExample)
IL (1) IL236066A (enExample)
IN (1) IN2014KN02915A (enExample)
LT (1) LT2861608T (enExample)
MA (1) MA37625B1 (enExample)
ME (1) ME03392B (enExample)
MX (1) MX356695B (enExample)
MY (1) MY170437A (enExample)
NZ (1) NZ702695A (enExample)
PH (1) PH12014502823B1 (enExample)
PL (1) PL2861608T3 (enExample)
PT (1) PT2861608T (enExample)
RS (1) RS58898B1 (enExample)
SG (1) SG11201408100YA (enExample)
SI (1) SI2861608T1 (enExample)
SM (1) SMT201900411T1 (enExample)
TN (1) TN2014000506A1 (enExample)
TR (1) TR201909016T4 (enExample)
UA (1) UA113215C2 (enExample)
WO (1) WO2013190384A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008009122A1 (en) 2006-07-20 2008-01-24 Affinium Pharmaceuticals, Inc. Acrylamide derivatives as fab i inhibitors
NZ702695A (en) 2012-06-19 2015-10-30 Debiopharm Int 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
ES2842443T3 (es) * 2016-02-26 2021-07-14 Debiopharm Int Sa Medicamento para el tratamiento de infecciones del pie diabético
WO2018048882A1 (en) 2016-09-06 2018-03-15 The Research Foundation For The State University Of New York Positron imaging tomography imaging agent composition and method for bacterial infection
JP6633777B2 (ja) 2017-08-24 2020-01-22 ノヴォ ノルディスク アー/エス Glp−1組成物及びその使用
US11691967B2 (en) 2018-03-12 2023-07-04 The Board Of Trustees Of The University Of Illinois Antibiotics effective for gram-negative pathogens
AU2019380568B2 (en) * 2018-11-12 2024-08-15 Debiopharm International S.A. Antibiotic compounds, methods of manufacturing the same, pharmaceutical compositions containing the same and uses thereof
US10723741B1 (en) 2018-12-21 2020-07-28 Acurx Pharmaceuticals, Llc DNA polymerase IIIC inhibitors and use thereof
IL285204B2 (en) 2019-02-14 2025-02-01 Debiopharm Int Sa Formulation of apavicin, method for its preparation
EP3982975A1 (en) * 2019-06-14 2022-04-20 Debiopharm International SA Afabicin for use for treating bacterial infections involving biofilm
BR112022012020A2 (pt) 2019-12-19 2022-09-20 Debiopharm Int Sa Novos compostos e seu uso
AU2021208601B2 (en) 2020-02-18 2025-06-05 Novo Nordisk A/S Glp-1 compositions and uses thereof
BR112023027268A2 (pt) 2021-06-23 2024-04-30 Debiopharm Int Sa Compostos inovadores e seu uso
WO2025078209A1 (en) 2023-10-09 2025-04-17 Debiopharm International S.A. Antibiotic compounds for treating bacterial infections

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008098374A1 (en) 2007-02-16 2008-08-21 Affinium Pharmaceuticals, Inc. Salts, prodrugs and polymorphs of fab i inhibitors

Family Cites Families (143)

* 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
AU702661B2 (en) 1994-06-29 1999-02-25 Smithkline Beecham Corporation Vitronectin receptor antagonists
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
PL193133B1 (pl) 1995-05-11 2007-01-31 Sandoz Ag Przeciwbakteryjna cefalosporyna, sposób jej wytwarzania i jej zastosowanie
US6057291A (en) 1995-06-02 2000-05-02 University Of British Columbia Antimicrobial cationic peptides
PT890359E (pt) 1996-02-29 2003-03-31 Fujisawa Pharmaceutical Co Comprimidos que contem antibiotico de beta-lactama e processo para a sua preparacao
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
JP3403206B2 (ja) 1996-09-20 2003-05-06 明治製菓株式会社 セフジトレン ピボキシル結晶性物質及びその製造法
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
CA2282593A1 (en) 1997-03-31 1998-10-08 Du Pont Pharmaceuticals Company Indazoles of cyclic ureas useful as hiv protease inhibitors
WO1998043667A1 (en) 1997-04-01 1998-10-08 Borody Thomas J Methods and compositions for treating inflammatory bowel disease
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
CN1268135A (zh) 1997-06-23 2000-09-27 吉富制药株式会社 螺杆菌属感染引起的疾病的预防/治疗剂
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
AU737018B2 (en) 1997-07-25 2001-08-09 Tsumura & Co. Pyridylacrylamide derivatives and nephritis remedies and TGF-beta inhibitors containing the same
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
JP2001503280A (ja) 1997-10-31 2001-03-13 ノバルティス アクチエンゲゼルシャフト グリフォセート耐性トランスジェニック植物
US6432444B1 (en) 1997-10-31 2002-08-13 New Horizons Diagnostics Corp Use of bacterial phage associated lysing enzymes for treating dermatological infections
CN1285823A (zh) 1997-11-07 2001-02-28 先灵公司 作为h3受体拮抗剂的苯基-烷基-咪唑
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
CA2316841C (en) 1998-01-07 2007-11-20 Meiji Seika Kaisha 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
JP3531648B2 (ja) 1998-08-04 2004-05-31 武田シェリング・プラウ アニマルヘルス株式会社 β−ラクタム抗生物質の安定化製剤
KR100595956B1 (ko) 1998-08-21 2006-07-03 센주 세이야꾸 가부시키가이샤 수성액 제약학적 조성물
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
US6395746B1 (en) 1998-09-30 2002-05-28 Alcon Manufacturing, Ltd. Methods of treating ophthalmic, otic and nasal infections and attendant inflammation
US6509327B1 (en) 1998-09-30 2003-01-21 Alcon Manufacturing, Ltd. Compositions and methods for treating otic, ophthalmic and nasal infections
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
CA2371816C (en) 1999-02-18 2010-04-27 The Regents Of The University Of California 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
US6267985B1 (en) 1999-06-30 2001-07-31 Lipocine Inc. Clear oil-containing pharmaceutical compositions
US6294192B1 (en) 1999-02-26 2001-09-25 Lipocine, Inc. Triglyceride-free compositions and methods for improved delivery of hydrophobic therapeutic agents
US6248363B1 (en) 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
WO2000052035A1 (en) 1999-03-03 2000-09-08 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
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
US6239113B1 (en) 1999-03-31 2001-05-29 Insite Vision, Incorporated Topical treatment or prevention of ocular infections
WO2000059941A1 (en) 1999-04-08 2000-10-12 The General Hospital Corporation 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
DE60012026T2 (de) 1999-08-26 2004-12-30 Ganeden Biotech, Inc., San Diego Verwendung von emu-öl als träger für fungizide, antibakterielle und antivirale arzneien
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
US6503955B1 (en) 1999-09-11 2003-01-07 The Procter & Gamble Company Pourable liquid vehicles
DK1142573T3 (da) 1999-09-17 2006-04-10 Daiichi Asubio Pharma Co Ltd Farmaceutiske præparater omfattende faropenem-natrium og en diaminacetatforbindelse til forbedring af absorption i mave-tarm-kanalen
US6500463B1 (en) 1999-10-01 2002-12-31 General Mills, Inc. Encapsulation of sensitive components into a matrix to obtain discrete shelf-stable particles
ATE294578T1 (de) 1999-10-08 2005-05-15 Affinium Pharm Inc Fab i hemmer
PE20010635A1 (es) 1999-10-08 2001-08-15 Smithkline Beecham Corp Inhibidores de fab i utiles para el tratamiento de infecciones bacterianas
US6730684B1 (en) 1999-10-08 2004-05-04 Affinium Pharmaceuticals, Inc. Fab I inhibitors
JP4831907B2 (ja) 1999-10-08 2011-12-07 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
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
ES2225237T3 (es) 1999-10-19 2005-03-16 Sato Pharmaceutical Co. Ltd. Agentes antimicrobianos de tipo 4-oxoquinolizina que tienen cadenas principales de 2-piridona como estructura parcial.
US6951729B1 (en) 1999-10-27 2005-10-04 Affinium Pharmaceuticals, Inc. High throughput screening method for biological agents affecting fatty acid biosynthesis
EP1666028B1 (en) 1999-10-29 2010-03-24 Novartis AG Dry powder compositions having improved dispersivity
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.
US6514541B2 (en) 2000-03-28 2003-02-04 Council Of Scientific And Industrial Research Formulation comprising thymol useful in the treatment of drug resistant bacterial infections
EP1280753A1 (en) 2000-04-21 2003-02-05 Rhodia/Chirex, Inc. Process for preparation of r-1-(aryloxy)propan-2-ol
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
AU9006801A (en) 2000-09-21 2002-04-02 Cambridge Semiconductor Ltd Semiconductor device and method of forming a semiconductor device
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
AU2002227269A1 (en) 2000-11-07 2002-06-03 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
US20020107266A1 (en) 2000-12-12 2002-08-08 Marguerita Lim-Wilby 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
DK1560584T3 (da) * 2001-04-06 2009-05-18 Affinium Pharm Inc Fab I inhibitorer
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
JPWO2003086396A1 (ja) 2002-04-02 2005-08-18 株式会社ツムラ ピリジルアクリル酸アミド誘導体を含有するホスホジエステラーゼiv阻害剤
AU2003250475A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc 5,6-fused 3,4-dihydropyrimidine-2-one derivatives as matrix metalloproteinase inhibitors
AU2003298937A1 (en) 2002-12-06 2004-06-30 Affinium Pharmaceuticals, Inc. Heterocyclic compounds, methods of making them and their use in therapy
CA2519429C (en) 2003-03-17 2013-08-06 Affinium Pharmaceuticals, Inc. Pharmaceutical 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
DK1828167T3 (da) 2004-06-04 2014-10-20 Debiopharm Int Sa Acrylamidderivater som antibiotiske midler
NZ555947A (en) 2005-01-19 2010-11-26 Rigel Pharmaceuticals Inc Prodrugs of 2,4-pyrimidinediamine compounds and their uses
CN101415701A (zh) * 2005-12-05 2009-04-22 Affinium医药公司 作为fabi抑制剂的杂环丙烯酰胺化合物和抗菌剂
CA2632476A1 (en) 2005-12-05 2007-06-14 Affinium Pharmaceuticals, Inc. Heterocyclylacrylamide compounds as fabi inhibitors and antibacterial agents
WO2008009122A1 (en) 2006-07-20 2008-01-24 Affinium Pharmaceuticals, Inc. 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
WO2009003136A1 (en) 2007-06-26 2008-12-31 Rigel Pharmaceuticals, Inc. Substituted pyrimidine-2, 4 -diamines for treating cell proliferative disorders
HUE033442T2 (en) * 2009-06-25 2017-11-28 Alkermes Pharma Ireland Ltd Heterocyclic compounds for the treatment of neurological and psychological disorders
EP2445343B1 (en) * 2009-06-25 2021-08-04 Alkermes Pharma Ireland Limited Prodrugs of nh-acidic compounds
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
MX2012005759A (es) 2009-11-18 2012-10-03 Fab Pharma S A S Acrilamidas heterociclicas novedosas y su uso como farmacos.
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
MY165902A (en) 2011-12-02 2018-05-18 Aurigene Discovery Tech Ltd Substituted pyridine derivatives as fabi inhibitors
NZ702695A (en) 2012-06-19 2015-10-30 Debiopharm Int 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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008098374A1 (en) 2007-02-16 2008-08-21 Affinium Pharmaceuticals, Inc. Salts, prodrugs and polymorphs of fab i inhibitors

Also Published As

Publication number Publication date
AU2013279021B2 (en) 2016-09-08
SMT201900411T1 (it) 2019-09-09
CY1122006T1 (el) 2020-10-14
US10035813B2 (en) 2018-07-31
ME03392B (me) 2020-01-20
SI2861608T1 (sl) 2019-08-30
JP6085026B2 (ja) 2017-02-22
DK2861608T3 (da) 2019-06-24
BR122021020778B1 (pt) 2022-07-12
LT2861608T (lt) 2019-07-10
CA2875916C (en) 2017-04-25
MX356695B (es) 2018-06-11
EP2861608B8 (en) 2019-06-19
MY170437A (en) 2019-07-31
EA201492127A1 (ru) 2015-06-30
IL236066A0 (en) 2015-02-01
AU2013279021A1 (en) 2015-01-22
EP2861608A1 (en) 2015-04-22
BR112014031635A2 (pt) 2017-06-27
UA113215C2 (xx) 2016-12-26
IL236066A (en) 2016-12-29
AU2013279021C1 (en) 2017-03-16
TN2014000506A1 (en) 2016-03-30
PH12014502823A1 (en) 2015-02-02
MA37625A1 (fr) 2016-09-30
HUE043836T2 (hu) 2019-09-30
EP2861608B1 (en) 2019-04-24
TR201909016T4 (tr) 2019-07-22
CN104684922B (zh) 2016-10-26
CL2014003472A1 (es) 2015-07-31
US20140051666A1 (en) 2014-02-20
PL2861608T3 (pl) 2019-09-30
CN104684922A (zh) 2015-06-03
SG11201408100YA (en) 2015-01-29
KR20150023779A (ko) 2015-03-05
MX2014015855A (es) 2015-03-05
PT2861608T (pt) 2019-06-28
JP2015521617A (ja) 2015-07-30
MA37625B1 (fr) 2017-04-28
US8901105B2 (en) 2014-12-02
RS58898B1 (sr) 2019-08-30
HRP20190980T1 (hr) 2019-08-23
IN2014KN02915A (enExample) 2015-05-08
EP2861608A4 (en) 2016-01-20
CA2875916A1 (en) 2013-12-27
BR112014031635B1 (pt) 2022-01-11
PH12014502823B1 (en) 2015-02-02
HK1208226A1 (en) 2016-02-26
WO2013190384A1 (en) 2013-12-27
NZ702695A (en) 2015-10-30
US20150065415A1 (en) 2015-03-05
JP2017105758A (ja) 2017-06-15
ES2731474T3 (es) 2019-11-15
EA028136B1 (ru) 2017-10-31

Similar Documents

Publication Publication Date Title
KR101720885B1 (ko) (e)-n-메틸-n-((3-메틸벤조푸란-2-일)메틸)-3-(7-옥소-5,6,7,8-테트라히드로-1,8-나프티리딘-3-일)아크릴아미드의전구약물 유도체
US8263613B2 (en) Salts, prodrugs and polymorphs of fab I inhibitors
CN107922418A (zh) 抗微生物化合物及制备和使用所述化合物的方法
US11780841B2 (en) 3,6-methano-1H-pyrrolo[3,2-b]pyridine and 3,6-methano-1H-pyrrolo[3,2-c]pyridine compounds and medicaments using same
CN112739338A (zh) β-内酰胺化合物与丙磺舒的组合及其用途
JP2022506957A (ja) 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
KR20000067306A (ko) 퀴놀론이 치환된 옥사졸리디논 유도체 및 그의 제조 방법과 항균제로서의 용도
JP2004137185A (ja) チオフェン骨格を有する抗菌剤
AU2006263884A1 (en) Quinoline derivatives as antibacterial agents
US12503476B2 (en) Ring-fused 2-pyridone compounds, methods for preparation thereof and their use in the treatment and/or prevention of a disease involving gram-positive bacteria
HK1208226B (en) 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
EP4104902A1 (en) Compound and drug containing same
WO2025078209A1 (en) Antibiotic compounds for treating bacterial infections
JP2017105714A (ja) 多剤排出ポンプ阻害剤
EA046887B1 (ru) Антибиотические соединения, способы их получения, фармацевтические композиции, содержащие их, и их применение
HK40051087A (en) Combinations of beta-lactam compounds and probenecid and uses thereof
WO2005030752A1 (ja) 8−シアノキノロンカルボン酸誘導体

Legal Events

Date Code Title Description
A201 Request for examination
PA0105 International application

Patent event date: 20150115

Patent event code: PA01051R01D

Comment text: International Patent Application

PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20150115

Comment text: Request for Examination of Application

PG1501 Laying open of application
E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20160609

Patent event code: PE09021S01D

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20170117

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20170322

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20170322

End annual number: 3

Start annual number: 1

PG1601 Publication of registration
FPAY Annual fee payment

Payment date: 20200312

Year of fee payment: 4

PR1001 Payment of annual fee

Payment date: 20200312

Start annual number: 4

End annual number: 4

PR1001 Payment of annual fee

Payment date: 20210316

Start annual number: 5

End annual number: 5

PR1001 Payment of annual fee

Payment date: 20230307

Start annual number: 7

End annual number: 7

PR1001 Payment of annual fee

Payment date: 20240307

Start annual number: 8

End annual number: 8