ME03392B - Prolek derivati (e)-n-meтil-n-( (з-метi lbenzofuran-2-il)meтil)-3-(7 -okso-5 ,6, 7,8-тетrанidr0-1,8-nafтiridin-3-il)akrilamida - Google Patents

Prolek derivati (e)-n-meтil-n-( (з-метi lbenzofuran-2-il)meтil)-3-(7 -okso-5 ,6, 7,8-тетrанidr0-1,8-nafтiridin-3-il)akrilamida

Info

Publication number
ME03392B
ME03392B MEP-2019-159A MEP2019159A ME03392B ME 03392 B ME03392 B ME 03392B ME P2019159 A MEP2019159 A ME P2019159A ME 03392 B ME03392 B ME 03392B
Authority
ME
Montenegro
Prior art keywords
methyl
tetranidro
prolek
naftyridin
methylbenzofuran
Prior art date
Application number
MEP-2019-159A
Other languages
German (de)
English (en)
French (fr)
Inventor
John J Partridge
John Colucci
Yves Gareau
Michel Therien
Robert Zamboni
Barry Hafkin
Anthony Marfat
Helmi Zaghdane
Original Assignee
Debiopharm Int Sa
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 Debiopharm Int Sa filed Critical Debiopharm Int Sa
Publication of ME03392B publication Critical patent/ME03392B/me

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic 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
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/58—Pyridine rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/60—Quinoline or hydrogenated quinoline 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
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus 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)
MEP-2019-159A 2012-06-19 2013-06-19 Prolek derivati (e)-n-meтil-n-( (з-метi lbenzofuran-2-il)meтil)-3-(7 -okso-5 ,6, 7,8-тетrанidr0-1,8-nafтiridin-3-il)akrilamida ME03392B (me)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261661559P 2012-06-19 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
EP13806968.7A EP2861608B8 (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 (1)

Publication Number Publication Date
ME03392B true ME03392B (me) 2020-01-20

Family

ID=49768192

Family Applications (1)

Application Number Title Priority Date Filing Date
MEP-2019-159A ME03392B (me) 2012-06-19 2013-06-19 Prolek derivati (e)-n-meтil-n-( (з-метi lbenzofuran-2-il)meтil)-3-(7 -okso-5 ,6, 7,8-тетrанidr0-1,8-nafтiridin-3-il)akrilamida

Country Status (34)

Country Link
US (2) US8901105B2 (me)
EP (1) EP2861608B8 (me)
JP (2) JP6085026B2 (me)
KR (1) KR101720885B1 (me)
CN (1) CN104684922B (me)
AU (1) AU2013279021C1 (me)
BR (2) BR112014031635B1 (me)
CA (1) CA2875916C (me)
CL (1) CL2014003472A1 (me)
CY (1) CY1122006T1 (me)
DK (1) DK2861608T3 (me)
EA (1) EA028136B1 (me)
ES (1) ES2731474T3 (me)
HR (1) HRP20190980T1 (me)
HU (1) HUE043836T2 (me)
IL (1) IL236066A (me)
IN (1) IN2014KN02915A (me)
LT (1) LT2861608T (me)
MA (1) MA37625B1 (me)
ME (1) ME03392B (me)
MX (1) MX356695B (me)
MY (1) MY170437A (me)
NZ (1) NZ702695A (me)
PH (1) PH12014502823A1 (me)
PL (1) PL2861608T3 (me)
PT (1) PT2861608T (me)
RS (1) RS58898B1 (me)
SG (1) SG11201408100YA (me)
SI (1) SI2861608T1 (me)
SM (1) SMT201900411T1 (me)
TN (1) TN2014000506A1 (me)
TR (1) TR201909016T4 (me)
UA (1) UA113215C2 (me)
WO (1) WO2013190384A1 (me)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2054422B1 (en) 2006-07-20 2017-06-14 Debiopharm International SA Acrylamide derivatives as fab i inhibitors
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
DK3419628T3 (da) 2016-02-26 2021-01-11 Debiopharm Int Sa Medikament til behandling af diabetiske fodinfektioner
US11857352B2 (en) 2016-09-06 2024-01-02 The Research Foundation For The State University Of New York Positron imaging tomography imaging agent composition and method for bacterial infection
BR112020002804A2 (pt) 2017-08-24 2020-07-28 Novo Nordisk A/S composição farmacêutica líquida, e, kit
US11691967B2 (en) 2018-03-12 2023-07-04 The Board Of Trustees Of The University Of Illinois Antibiotics effective for gram-negative pathogens
LT3880675T (lt) * 2018-11-12 2024-12-27 Debiopharm International Sa Antibiotikų junginiai, jų gamybos būdas, farmacinės kompozicijos, kurių sudėtyje jie yra, ir jų panaudojimas
US10723741B1 (en) 2018-12-21 2020-07-28 Acurx Pharmaceuticals, Llc DNA polymerase IIIC inhibitors and use thereof
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
KR102932904B1 (ko) 2019-12-19 2026-02-27 데비오팜 인터네셔날 에스 에이 새로운 화합물 및 그 용도
IL294521A (en) 2020-02-18 2022-09-01 Novo Nordisk As glp-1 compounds and their uses
WO2022268890A1 (en) 2021-06-23 2022-12-29 Debiopharm International S.A. Novel compounds and their use
EP4791392A1 (en) 2023-10-09 2026-08-19 Debiopharm International SA Antibiotic compounds for treating bacterial infections

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
WO1996000730A1 (en) 1994-06-29 1996-01-11 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
ATE233268T1 (de) 1995-05-11 2003-03-15 Biochemie Gmbh Antibakterielle cephalosporinverbindungen
US6057291A (en) 1995-06-02 2000-05-02 University Of British Columbia Antimicrobial cationic peptides
TW473393B (en) 1996-02-29 2002-01-21 Fujisawa Pharmaceutical Co Beta-lactam antibiotic-containing tablet and production thereof
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
DE19624659A1 (de) 1996-06-20 1998-01-08 Klinge Co Chem Pharm Fab Neue Pyridylalken- und Pyridylalkinsäureamide
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
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
SK284973B6 (sk) 1996-09-20 2006-03-02 Meiji Seika Kaisha Ltd. Kryštalická forma Cefditoren pivoxylu a spôsob jej výroby
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
JP2001518094A (ja) 1997-03-31 2001-10-09 デュポン ファーマシューティカルズ カンパニー Ｈｉｖプロテアーゼ阻害剤として有用なインダゾール−環式尿素
CA2285923C (en) 1997-04-01 2013-03-12 Thomas Julius Borody 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
KR20010014105A (ko) 1997-06-23 2001-02-26 가마쿠라 아키오 헬리코박터 감염에 기인한 질환의 예방 또는 치료제
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
WO1999005109A1 (en) 1997-07-25 1999-02-04 Tsumura & Co. PYRIDYLACRYLAMIDE DERIVATIVES AND NEPHRITIS REMEDIES AND TGF-β 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
PL197872B1 (pl) 1997-10-31 2008-05-30 Syngenta Participations Ag Roślina buraka cukrowego wyrażająca aktywność enzymu cp4/epsps oraz jej rośliny potomne, transgeniczne nasiona rośliny buraka cukrowego wyrażające aktywność enzymu cp4/epsps oraz sposób wytwarzania transgenicznych roślin
US6432444B1 (en) 1997-10-31 2002-08-13 New Horizons Diagnostics Corp Use of bacterial phage associated lysing enzymes for treating dermatological infections
CA2309121A1 (en) 1997-11-07 1999-05-20 Schering Corporation Phenyl-alkyl-imidazoles as h3 receptor antagonists
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
PT1051978E (pt) 1998-01-07 2012-11-20 Meiji Seika Pharma Co Ltd Composições de cefalosporina amorfa cristalograficamente estável e processo para a sua produção
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
JP4726296B2 (ja) 1998-02-27 2011-07-20 インスティチュート ストローマン アーゲー 創傷治癒のためのマトリックスタンパク質組成物
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
EP1101497B1 (en) 1998-08-04 2008-02-20 Takeda Schering-Plough Animal Health K.K. Stabilized oily preparations of tobicillin (beta-lactam antibiotic)
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
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
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
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
AR024158A1 (es) 1999-06-01 2002-09-04 Smithkline Beecham Corp Compuestos antibacterianos
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
WO2001013956A2 (en) 1999-08-26 2001-03-01 Ganeden Biotech, Inc. Use of emu oil 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
JP2003509350A (ja) 1999-09-11 2003-03-11 ザ、プロクター、エンド、ギャンブル、カンパニー 注加可能な液体賦形剤
ATE315395T1 (de) 1999-09-17 2006-02-15 Daiichi Asubio Pharma Co Ltd Pharmazeutische zusammensetzungen, die faropenem natrium und eine diamineacetat 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
US6762201B1 (en) 1999-10-08 2004-07-13 Affinium Pharmaceuticals, Inc. Fab I inhibitors
EP1225895B1 (en) 1999-10-08 2005-05-04 Affinium Pharmaceuticals, Inc. Fab i inhibitors
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
ES2231275T3 (es) 1999-10-08 2005-05-16 Affinium Pharmaceuticals, Inc. Inhibidores de fab i.
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
DE60025019T2 (de) 1999-10-29 2006-08-24 Nektar Therapeutics, San Carlos Trockenpulverzusammensetzungen mit verbesserter dispersivität
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
US6448449B2 (en) 2000-04-21 2002-09-10 Rhodia Chirex, Inc. Process for preparation of (R)-1- (aryloxy)propan-2-ol
AU2001282988B2 (en) 2000-07-26 2006-01-05 Atopic Pty Ltd 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
RU2276429C2 (ru) 2000-09-21 2006-05-10 Кембридж Семикондактор Лимитед Полупроводниковое устройство и способ формирования полупроводникового устройства
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
EP1332131A2 (en) 2000-11-07 2003-08-06 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
AU2002232558A1 (en) 2000-12-12 2002-06-24 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
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
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
US20050187264A1 (en) 2002-04-02 2005-08-25 Tomohisa Hattori Phosphodiesterase iv inhibitor containing pyridylacrylamide derivative
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
PT1575951E (pt) 2002-12-06 2014-09-15 Debiopharm Int Sa Compostos heterocíclicos, métodos para os preparar e sua utilização em terapia
EP1608377B1 (en) 2003-03-17 2008-10-01 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
US8450307B2 (en) 2004-06-04 2013-05-28 Affinium Pharmaceuticals, Inc. Therapeutic agents, and methods of making and using the same
US7449458B2 (en) 2005-01-19 2008-11-11 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
US20090156578A1 (en) 2005-12-05 2009-06-18 PAULS Henry 3-Heterocyclylacrylamide Compounds as Fab I Inhibitors and Antibacterial Agents
EP2054422B1 (en) 2006-07-20 2017-06-14 Debiopharm International SA Acrylamide derivatives as fab i inhibitors
WO2008064274A1 (en) 2006-11-21 2008-05-29 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
WO2009003136A1 (en) 2007-06-26 2008-12-31 Rigel Pharmaceuticals, Inc. Substituted pyrimidine-2, 4 -diamines for treating cell proliferative disorders
PT2445502T (pt) * 2009-06-25 2017-09-22 Alkermes Pharma Ireland Ltd Compostos heterocíclicos para o tratamento de distúrbios neurológicos e psicológicos
JP5732453B2 (ja) * 2009-06-25 2015-06-10 アルカーメス ファーマ アイルランド リミテッド Ｎｈ酸性化合物のプロドラッグ
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
CA2776849A1 (en) * 2009-11-18 2011-05-26 Fab Pharma S.A.S. 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
SG11201402409UA (en) 2011-12-02 2014-10-30 Aurigene Discovery Tech Ltd Substituted pyridine derivatives as fabi inhibitors
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

Also Published As

Publication number Publication date
HRP20190980T1 (hr) 2019-08-23
IL236066A (en) 2016-12-29
EP2861608A4 (en) 2016-01-20
CA2875916C (en) 2017-04-25
IN2014KN02915A (me) 2015-05-08
PH12014502823B1 (en) 2015-02-02
SMT201900411T1 (it) 2019-09-09
AU2013279021A1 (en) 2015-01-22
MY170437A (en) 2019-07-31
CY1122006T1 (el) 2020-10-14
BR112014031635B1 (pt) 2022-01-11
EP2861608B8 (en) 2019-06-19
PT2861608T (pt) 2019-06-28
DK2861608T3 (da) 2019-06-24
SG11201408100YA (en) 2015-01-29
US20140051666A1 (en) 2014-02-20
EA201492127A1 (ru) 2015-06-30
BR122021020778B1 (pt) 2022-07-12
JP6085026B2 (ja) 2017-02-22
US8901105B2 (en) 2014-12-02
EP2861608A1 (en) 2015-04-22
KR20150023779A (ko) 2015-03-05
MA37625A1 (fr) 2016-09-30
WO2013190384A1 (en) 2013-12-27
TN2014000506A1 (en) 2016-03-30
PL2861608T3 (pl) 2019-09-30
SI2861608T1 (sl) 2019-08-30
CN104684922A (zh) 2015-06-03
JP2015521617A (ja) 2015-07-30
US20150065415A1 (en) 2015-03-05
RS58898B1 (sr) 2019-08-30
BR112014031635A2 (pt) 2017-06-27
CA2875916A1 (en) 2013-12-27
CL2014003472A1 (es) 2015-07-31
IL236066A0 (en) 2015-02-01
AU2013279021B2 (en) 2016-09-08
EA028136B1 (ru) 2017-10-31
CN104684922B (zh) 2016-10-26
MX2014015855A (es) 2015-03-05
MX356695B (es) 2018-06-11
KR101720885B1 (ko) 2017-03-28
LT2861608T (lt) 2019-07-10
US10035813B2 (en) 2018-07-31
PH12014502823A1 (en) 2015-02-02
AU2013279021C1 (en) 2017-03-16
HUE043836T2 (hu) 2019-09-30
UA113215C2 (xx) 2016-12-26
HK1208226A1 (en) 2016-02-26
ES2731474T3 (es) 2019-11-15
JP2017105758A (ja) 2017-06-15
TR201909016T4 (tr) 2019-07-22
MA37625B1 (fr) 2017-04-28
EP2861608B1 (en) 2019-04-24
NZ702695A (en) 2015-10-30

Similar Documents

Publication Publication Date Title
CY2024012I1 (el) Παραγωγα 2.2-διφθοροπροπιοναμιδιου απο μεθυλικη βαρδοξολονη, πολυμορφικες μορφες και μεθοδοι χρησης αυτων
HUE056365T2 (hu) 2-(2,4,5-Helyettesített-anilino)pirimidin származékok
SMT201600198B (it) Derivati di 1,2,4-triazina-4-ammina
SMT201700052B (it) 2-(azaindol-2-il)benzimidazoli come inibitori di pad4
HUE058009T2 (hu) 1,3-Tiazol-2-il szubsztituált benzamid-származékok
BR302012005339S1 (pt) "configuração aplicada em pote".
BR112014031635A2 (pt) derivados de pró-fármaco de (e)-n-metil-n-( (3-metilbenzofuran-2-il) metil)-3-(7-oxo-5,6,7,8-tetraidro- 1, 8- naftirindin-3-il) acrilamida
LT3527263T (lt) Bipirazolo dariniai, kaip jak inhibitoriai
LT3371190T (lt) Heterocikliniai junginiai, kaip pi3k-gama inhibitoriai
DK3054936T5 (da) 4-((2-hydroxy-3-methoxybenzyl)amino) benzensulfonamid derivater som 12-lipoxygenase inhibitorer
ME03036B (me) 2-amin0-6-fluoro-n-( 5-fluoro-4-( 4-( 4-( oksetan -3-il)piperrazin -1-karbonil)piperidin-1-il)piridin-3-il )pirazol0[1,5alfa] pirimidin-3-karboksamid kao inhibitor atr kinaze
EP2762476A4 (en) 1,2,4-triazine-6-carboxamide derivative
DK3003038T3 (da) 2h-1,2,3-triazolderivater som inhibitorer af fibrose
EP2935214A4 (en) 1,4-pyridone COMPOUNDS
BR302012004626S1 (pt) "configuração aplicada em leitora para dispositivo móvel."
EP2945634A4 (en) N- (SUBSTITUTED) 5-FLUORO-4-IMINO-3-METHYL-2-OXO-3,4-DIHYDROPYRIMIDIN-1 (2H) CARBOXYLATE DERIVATIVES
EP2858501A4 (en) TRKA KINASE INHIBITORS, COMPOSITIONS AND METHOD THEREFOR
EP2863748A4 (en) 1,2,4-triazine-6-CARBOXAMIDKINASEINHIBITOREN
DK2938194T3 (da) N-(substituerede)-5-fluor-4-imino-3-methyl-2-oxo-3,4-dihydropyrimidin-1 (2h)-carboxylatderivater
DK3638680T3 (da) Heteroaromatiske forbindelser som vanininhibitorer
BR302012004997S1 (pt) "configuração aplicada em farol para motoneta"
DK3319970T3 (da) Pyrido-oxazinonderivater som tnap-hæmmere
ME02908B (me) Supstituisani 2-alkil-1-okso-n-fenil-3-heteroaril-1,2,3,4-tetrahidroizohinolin-4-karboksamidi za antimalarijske terapije
DK2851075T3 (da) Præparat, der indeholder 6,7-umættet -7-carbamoylmorphinanderivat
DK3237407T3 (da) 3,5-diaminopyrazolkinasehæmmere