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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (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
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
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 (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
WO2008009122A1 (en) 2006-07-20 2008-01-24 Affinium Pharmaceuticals, Inc. Acrylamide derivatives as fab i inhibitors
SMT201900411T1 (it) 2012-06-19 2019-09-09 Debiopharm Int Sa Derivati di profaramci di (e)-n-metil-n-((3-metilbenzofuran-2-il)metil -3-(7-osso-5,6,7,8-tetraidro-1,8-naftiridin-3-il)acrilammide
SMT202000719T1 (it) * 2016-02-26 2021-03-15 Debiopharm Int Sa Medicinale per il trattamento d’infezioni del piede diabetico
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
MX2020001525A (es) 2017-08-24 2020-03-20 Novo Nordisk As Composiciones de peptido similar al glucagon tipo 1 (glp-1) y sus usos.
WO2019177975A1 (en) * 2018-03-12 2019-09-19 The Board Of Trustees Of The University Of Illinois Antibiotics effective for gram-negative pathogens
DK3880675T3 (da) * 2018-11-12 2024-12-02 Debiopharm Int Sa Antibiotiske forbindelser, fremgangsmåder til fremstilling deraf, farmaceutiske sammensætninger indeholdende disse og anvendelser deraf
WO2020132174A1 (en) 2018-12-21 2020-06-25 Acurx Pharmaceuticals, Llc Dna polymerase iiic inhibitors and use thereof
HUE062061T2 (hu) * 2019-02-14 2023-09-28 Debiopharm Int Sa Afabicin készítmény, eljárás annak elõállítására
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
JP7669372B2 (ja) 2019-12-19 2025-04-28 デバイオファーム インターナショナル エス．エー． 新規な化合物及びその使用
IL294520A (en) 2020-02-18 2022-09-01 Novo Nordisk As Pharmaceutical formulations
AU2022300316A1 (en) 2021-06-23 2024-02-08 Debiopharm International S.A. Novel compounds and their use
WO2025078209A1 (en) 2023-10-09 2025-04-17 Debiopharm International S.A. 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
PL318199A1 (en) 1994-06-29 1997-05-26 Smithkline Beecham Corp Antagonists of vitronectin receptors
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
IL132532A (en) 1995-05-11 2003-06-24 Biochemie Gmbh Intermediates for the preparation of substituted cephalosporins
US6057291A (en) 1995-06-02 2000-05-02 University Of British Columbia Antimicrobial cationic peptides
PT1166651E (pt) 1996-02-29 2005-04-29 Fujisawa Pharmaceutical Co Granulos de desintegracao rapida de um edulcorante sintetico contendo acido silicico e/ou dioxido de silicio
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
NZ334883A (en) 1996-09-20 2000-09-29 Meiji Seika Kaisha A crystalline substance of cefditoren pivoxil which has desirable thermal storage stability and the production of the same
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
EP0973767A1 (en) 1997-03-31 2000-01-26 Dupont Pharmaceuticals Company Indazoles of cyclic ureas useful as hiv protease inhibitors
NZ500696A (en) 1997-04-01 2002-05-31 Borody Thomas J Methods and compositions for treating inflammatory bowel disease comprising mycobacterial agents, including macrolides
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
CA2294453A1 (en) 1997-06-23 1998-12-30 Fumihiro Hirayama Prophylactic or therapeutic agent for diseases attributable to infection with 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
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
EP0950109A1 (en) 1997-10-31 1999-10-20 Novartis AG Glyphosate resistant transgenic plants
US6432444B1 (en) 1997-10-31 2002-08-13 New Horizons Diagnostics Corp Use of bacterial phage associated lysing enzymes for treating dermatological infections
ES2188029T3 (es) 1997-11-07 2003-06-16 Schering Corp Fenil-alquil-imidazoles como antagonistas del receptor h3.
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
CN1151845C (zh) 1998-01-07 2004-06-02 明治制果株式会社 含有晶体学稳定的无定形头孢茵素的组合物及其制备方法
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
HK1041217A1 (zh) 1998-08-04 2002-07-05 藤泽药品工业株式会社 β-内酰胺抗生素的稳定化制剂
CA2307632C (en) 1998-08-21 2007-05-22 Senju Pharmaceutical Co., Ltd. Aqueous liquid pharmaceutical composition
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
JP4819223B2 (ja) 1999-02-18 2011-11-24 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 発光マーカーとして使用するためのフタルアミド−ランタニド錯体
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
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
US6461829B1 (en) 1999-03-03 2002-10-08 The Trustees Of Princeton University Bacterial transglycosylases: assays for monitoring the activity using Lipid II substrates 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
US6448054B1 (en) 1999-04-08 2002-09-10 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
ES2221624T3 (es) 1999-08-26 2005-01-01 Ganeden Biotech, Inc. Uso de aceite de emu como vehiculo para mediaciones antifungicas, antibacterianas y antiviricas.
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
AU770516B2 (en) 1999-09-11 2004-02-26 Procter & Gamble Company, The Polyoxyalkylene copolymers containing pourable liquid vehicles
CN1198611C (zh) 1999-09-17 2005-04-27 第一三得利制药株式会社 药物抗菌剂组合物
US6500463B1 (en) 1999-10-01 2002-12-31 General Mills, Inc. Encapsulation of sensitive components into a matrix to obtain discrete shelf-stable particles
AU773218B2 (en) 1999-10-08 2004-05-20 Debiopharm International Sa Fab I inhibitors
CO5251397A1 (es) 1999-10-08 2003-02-28 Smithkline Beecham Corp Inhibidores de fab i
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
US6762201B1 (en) 1999-10-08 2004-07-13 Affinium Pharmaceuticals, Inc. Fab I inhibitors
US6503908B1 (en) 1999-10-11 2003-01-07 Pfizer Inc Pharmaceutically active compounds
ATE277042T1 (de) 1999-10-19 2004-10-15 Sato Pharma Antimikrobielle 4-oxochinolizine mit 2- pyridongerüsten als teilstruktur
US6951729B1 (en) 1999-10-27 2005-10-04 Affinium Pharmaceuticals, Inc. High throughput screening method for biological agents affecting fatty acid biosynthesis
IL149085A0 (en) 1999-10-29 2002-11-10 Inhale Therapeutic Syst A dry powder composition containing a di or tripeptide
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
US6448449B2 (en) 2000-04-21 2002-09-10 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
ATE545958T1 (de) 2000-09-21 2012-03-15 Cambridge Semiconductor Ltd Halbleiterbauelement und dessen herstellungsverfahren
US6821746B2 (en) 2000-10-06 2004-11-23 Affinium Pharmaceuticals, Inc. Methods of screening for FabK antagonists and agonists
US7048926B2 (en) 2000-10-06 2006-05-23 Affinium Pharmaceuticals, Inc. Methods of agonizing and antagonizing FabK
EP1332131A2 (en) 2000-11-07 2003-08-06 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
EP1560584B1 (en) 2001-04-06 2009-01-14 Affinium Pharmaceuticals, Inc. Fab i inhibitors
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
RU2004131879A (ru) 2002-04-02 2005-04-20 Цумура Энд Ко (Jp) Ингибитор фосфодиэстеразы iv, содержащий пиридилакриламидное производное
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
ES2518316T3 (es) 2002-12-06 2014-11-05 Debiopharm International Sa Compuestos heterocíclicos, métodos de fabricación de los mismos y su uso en terapia
ATE409485T1 (de) 2003-03-17 2008-10-15 Affinium Pharm Inc Pharmazeutische zusammensetzungen inhibitoren von fab i und weitere antibiotika enthaltend
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
DE602006010979D1 (de) 2005-01-19 2010-01-21 Rigel Pharmaceuticals Inc Prodrugs aus 2,4-pyrimidindiamin-verbindungen und ihre verwendungen
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
WO2008009122A1 (en) 2006-07-20 2008-01-24 Affinium Pharmaceuticals, Inc. Acrylamide derivatives as fab i inhibitors
US8163902B2 (en) 2006-11-21 2012-04-24 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
EP3255045A1 (en) * 2007-02-16 2017-12-13 Debiopharm International SA 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
SMT201700430T1 (it) * 2009-06-25 2018-01-11 Alkermes Pharma Ireland Ltd Composti eterociclici per il trattamento di disturbi neurologici e psicologici
NZ597108A (en) * 2009-06-25 2014-04-30 Alkermes Pharma Ireland Ltd 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
WO2011061214A1 (en) 2009-11-18 2011-05-26 Fab Pharma Sas Novel heterocyclic acrylamides and their use as pharmaceuticals
WO2011156811A2 (en) 2010-06-11 2011-12-15 Affinium Pharmaceuticals, Inc. Compounds for 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
US9062002B2 (en) 2011-12-02 2015-06-23 Aurigene Discovery Technologies Limited Substituted pyridine derivatives as FabI inhibitors
SMT201900411T1 (it) 2012-06-19 2019-09-09 Debiopharm Int Sa Derivati di profaramci di (e)-n-metil-n-((3-metilbenzofuran-2-il)metil -3-(7-osso-5,6,7,8-tetraidro-1,8-naftiridin-3-il)acrilammide

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