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PE20010635A1 - Inhibidores de fab i utiles para el tratamiento de infecciones bacterianas - Google Patents

Inhibidores de fab i utiles para el tratamiento de infecciones bacterianas

Info

Publication number
PE20010635A1
PE20010635A1 PE2000001060A PE0010602000A PE20010635A1 PE 20010635 A1 PE20010635 A1 PE 20010635A1 PE 2000001060 A PE2000001060 A PE 2000001060A PE 0010602000 A PE0010602000 A PE 0010602000A PE 20010635 A1 PE20010635 A1 PE 20010635A1
Authority
PE
Peru
Prior art keywords
alkyl
methyl
treatment
link
bacterial infections
Prior art date
Application number
PE2000001060A
Other languages
English (en)
Inventor
H Miller William
N Uzinskas Irene
A Newlander Kenneth
A Seefeld Mark
E Dewolf Walter
R Jakas Dalia
Original Assignee
Smithkline Beecham Corp
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 Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of PE20010635A1 publication Critical patent/PE20010635A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Indole Compounds (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE EL BICICLO SUSTITUIDO CON X ES UN GRUPO a, b, c, ENTRE OTROS; R1, R4, R6 SON H, ALQUILO C1-C4; R2 ES H, ALQUILO C1-C4, CICLOALQUILO C3-C6; R3 ES UN ARIL, PIRIDINA, PIRIMIDINA SUSTITUIDO CON X E Y, ENTRE OTROS; R5 ES CH2 CUANDO EL ENLACE AL CUAL ESTA UNIDO ES ENLACE DOBLE; O ES H, ALQUILO C1-4 CUANDO EL ENLACE AL CUAL ESTA UNIDO ES UN ENLACE SIMPLE; R7 ES H, ALQUILO C1-C6, ALQUILO C0-C6-Ar; Y ES H, ALQUILO C1-C4; N(R`)2, NHCOR', NHCH2C(O)R', ENTRE OTROS; X ES H, ALQUILO C1-C4, CH2OH, OR', SR', CN, N(R')2, ENTRE OTROS; W ES S, O; Q ES H, ALQUILO C1-C4; M ES CH2, O; L ES CH2, CO; E ES O, NR'; R' ES H, ALQUILO C1-C6, ALQUILO C0-C6-Ar; r ES 0-2. SON COMPUESTOS PREFERIDOS (E)-3-(6-AMINOPIRIDIN-3-IL)-N-METIL-N-(1-METIL-1H-INDOL-2-ILMETIL)ACRILAMIDA, (E)-3-(4-AMINOFENIL)-N-METIL-N-(1-METIL-1H-INDOL-2-ILMETIL)ACRILAMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. EL COMPUESTO I INHIBE A LA FAB-I, FAB-K Y PUEDE SER UTIL PARA EL TRATAMIENTO DE INFECCIONES BACTERIANAS
PE2000001060A 1999-10-08 2000-10-06 Inhibidores de fab i utiles para el tratamiento de infecciones bacterianas PE20010635A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US15870499P 1999-10-08 1999-10-08

Publications (1)

Publication Number Publication Date
PE20010635A1 true PE20010635A1 (es) 2001-08-15

Family

ID=22569335

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000001060A PE20010635A1 (es) 1999-10-08 2000-10-06 Inhibidores de fab i utiles para el tratamiento de infecciones bacterianas

Country Status (25)

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US (5) US6846819B1 (es)
EP (1) EP1226138B1 (es)
JP (1) JP4803935B2 (es)
KR (1) KR100823382B1 (es)
CN (1) CN1197860C (es)
AR (1) AR025976A1 (es)
AT (1) ATE285821T1 (es)
AU (1) AU773218B2 (es)
BR (1) BRPI0014470B1 (es)
CA (1) CA2387016C (es)
CZ (1) CZ302015B6 (es)
DE (1) DE60017180T2 (es)
EC (1) ECSP003699A (es)
ES (1) ES2231275T3 (es)
HK (1) HK1049656A1 (es)
HU (1) HU230030B1 (es)
IL (2) IL148820A0 (es)
NO (1) NO322708B1 (es)
NZ (1) NZ517706A (es)
PE (1) PE20010635A1 (es)
PL (1) PL201627B1 (es)
TW (1) TW534909B (es)
UY (1) UY26380A1 (es)
WO (1) WO2001027103A1 (es)
ZA (1) ZA200202631B (es)

Families Citing this family (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CO5180550A1 (es) 1999-04-19 2002-07-30 Smithkline Beecham Corp Inhibidores de fab i
AR024158A1 (es) 1999-06-01 2002-09-04 Smithkline Beecham Corp Compuestos antibacterianos
ATE332130T1 (de) * 1999-10-08 2006-07-15 Affinium Pharm Inc Fab-i-hemmer
NZ517706A (en) * 1999-10-08 2004-01-30 Affinium Pharm Inc Fab I inhibitors
US6762201B1 (en) 1999-10-08 2004-07-13 Affinium Pharmaceuticals, Inc. Fab I inhibitors
US6730684B1 (en) 1999-10-08 2004-05-04 Affinium Pharmaceuticals, Inc. Fab I inhibitors
JP4272338B2 (ja) 2000-09-22 2009-06-03 バイエル アクチェンゲゼルシャフト ピリジン誘導体
US7048926B2 (en) 2000-10-06 2006-05-23 Affinium Pharmaceuticals, Inc. Methods of agonizing and antagonizing FabK
AU2000277557A1 (en) * 2000-10-06 2002-04-22 Smith Kline Beecham Corporation Methods of agonizing and antagonizing fabk
DE60230934D1 (de) * 2001-04-06 2009-03-05 Affinium Pharm Inc Fab-i-inhibitoren
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
WO2005066135A2 (en) 2003-12-29 2005-07-21 Sepracor Inc. Pyrrole and pyrazole daao inhibitors
SI1828167T1 (sl) * 2004-06-04 2014-12-31 Debiopharm International Sa Forum "Apres-Demain" Akrilamidni derivati kot anitibiotična sredstva
JP5474299B2 (ja) 2004-08-21 2014-04-16 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング チエノ［２，３−ｂ］チオフェンのモノマー、オリゴマーおよびポリマー
US7973060B2 (en) 2005-10-13 2011-07-05 Crystalgenomics, Inc. Fab I inhibitor and process for preparing same
EP1973902A2 (en) * 2005-12-05 2008-10-01 Affinium Pharmaceuticals, Inc. 3-heterocyclylacrylamide compounds as fabi inhibitors and antibacterial agents
JP5438975B2 (ja) 2006-01-06 2014-03-12 サノビオン ファーマシューティカルズ インク テトラロン系モノアミン再取り込み阻害剤
US20070203111A1 (en) 2006-01-06 2007-08-30 Sepracor Inc. Cycloalkylamines as monoamine reuptake inhibitors
WO2007086584A1 (ja) * 2006-01-30 2007-08-02 Meiji Seika Kaisha, Ltd. 新規ＦａｂＫおよびＦａｂＩ／Ｋ阻害剤
WO2007115185A2 (en) 2006-03-31 2007-10-11 Sepracor Inc. Preparation of chiral amides and amines
US7884124B2 (en) 2006-06-30 2011-02-08 Sepracor Inc. Fluoro-substituted inhibitors of D-amino acid oxidase
EP2687533B1 (en) * 2006-07-20 2017-07-19 Debiopharm International SA Acrylamide derivatives as FAB I inhibitors
US7902252B2 (en) 2007-01-18 2011-03-08 Sepracor, Inc. Inhibitors of D-amino acid oxidase
US8263613B2 (en) * 2007-02-16 2012-09-11 Affinium Pharmaceuticals, Inc. Salts, prodrugs and polymorphs of fab I inhibitors
RU2470011C2 (ru) 2007-05-31 2012-12-20 Сепракор Инк. Циклоалкиламины, содержащие в качестве заместителя фенил, как ингибиторы обратного захвата моноаминов
EP2014287A1 (de) * 2007-06-13 2009-01-14 Bayer Schering Pharma Aktiengesellschaft Verwendung von Zimtsäurederivaten als Modulatoren des EP2-Rezeptors
EP2286808A1 (en) * 2009-08-18 2011-02-23 Rheinische Friedrich-Wilhelms Universität Cytohesin inhibitors
WO2011061214A1 (en) 2009-11-18 2011-05-26 Fab Pharma Sas Novel heterocyclic acrylamides and their use as pharmaceuticals
US20130281442A1 (en) * 2010-06-11 2013-10-24 Barry Hafkin Compounds for Treatment of Bovine Mastitis
EP3470407B1 (en) 2010-11-05 2024-01-24 Firmenich Incorporated Compounds useful as modulators of trpm8
AR088729A1 (es) * 2011-03-29 2014-07-02 Actelion Pharmaceuticals Ltd Derivados de 3-ureidoisoquinolin-8-ilo y una composicion farmaceutica
CN102675311A (zh) * 2011-06-14 2012-09-19 苏春华 一种氟代丙烯酰胺的衍生物
JP6294822B2 (ja) 2011-08-10 2018-03-14 ヤンセン・サイエンシズ・アイルランド・ユーシー 抗菌性ピペリジニル置換３，４−ジヒドロ−１ｈ−［１，８］−ナフチリジノン類
US9394295B2 (en) 2011-08-10 2016-07-19 Janssen Sciences Ireland Uc Antibacterial homopiperidinyl substituted 3,4-dihydro-1H-[1,8]naphthyridinones
JO3611B1 (ar) 2011-08-10 2020-08-27 Janssen Sciences Ireland Uc سايكلو بنتا (سي (بيرول 4,3 ثاني هيدرو 1 hمستبدله [8,1] نافثيريدينونات مضادة للجراثيم
CA2849057C (en) * 2011-09-19 2021-05-11 Vitas Pharma Research Pvt Ltd Heterocyclic compounds as inhibitors of fatty acid biosynthesis for bacterial infections
EP2785715A1 (en) 2011-12-02 2014-10-08 Aurigene Discovery Technologies Limited Substituted pyridine derivatives as fabi inhibitors
US9062075B2 (en) 2011-12-02 2015-06-23 Aurigene Discovery Technologies Limited Tetrahydropyridine derivatives as FabI inhibitors
RS58898B1 (sr) 2012-06-19 2019-08-30 Debiopharm Int Sa Prolek derivati (e)-n-metil-n-((3-metilbenzofuran-2-il)metil)-3-(7-okso-5,6,7,8-tetrahidro-1,8-naftiridin-3-il)akrilamida
KR102323876B1 (ko) 2012-08-10 2021-11-09 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 신규한 항균성 화합물
CN104981466B (zh) 2012-08-10 2019-06-14 爱尔兰詹森科学公司 抗细菌化合物
WO2014072930A2 (en) * 2012-11-09 2014-05-15 Aurigene Discovery Technologies Limited Fused pyridine derivatives as antibacterial agents
EP3004099B1 (en) 2013-06-04 2023-04-19 Aurigene Oncology Limited Tetrahydropyridine derivatives as fabi inhibitors
BR112016022785B8 (pt) 2014-04-04 2020-09-15 Iomet Pharma Ltd composto inibidor de triptofano-2,3-dioxigenase (tdo) e/ou indoleamina-2,3-dioxigenase (ido), composição farmacêutica, e, uso de composto inibidor de triptofano-2,3-dioxigenase (tdo) e/ou indoleamina-2,3dioxigenase (ido) ou de um sal farmaceuticamente aceitável do mesmo para fabricação de um medicamento
EP3356356B1 (en) 2015-10-01 2021-05-26 Firmenich Incorporated Compounds useful as modulators of trpm8
CN105669519B (zh) * 2016-01-04 2018-01-05 北方民族大学 吲哚类化合物、制备方法及其作为抗耐药菌药物的应用
PT3419628T (pt) 2016-02-26 2021-01-05 Debiopharm Int Sa Medicamento para o tratamento de infeções do pé diabético
US10858319B2 (en) 2016-10-03 2020-12-08 Iomet Pharma Ltd. Indole derivatives for use in medicine
AU2018388404B2 (en) 2017-12-22 2023-11-02 HiberCell Inc. Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
US11691967B2 (en) 2018-03-12 2023-07-04 The Board Of Trustees Of The University Of Illinois Antibiotics effective for gram-negative pathogens
PL3880675T3 (pl) 2018-11-12 2025-02-10 Debiopharm International Sa Związki antybiotykowe, sposoby ich wytwarzania, kompozycje farmaceutyczne zawierające te związki oraz ich zastosowanie
CA3129508A1 (en) 2019-02-14 2020-08-20 Debiopharm International S.A. Solid formulations of afabicin with histidine
CN113939306B (zh) 2019-06-14 2024-07-19 德彪药业国际股份公司 用于治疗涉及生物膜的细菌感染的药物及其用途
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
CN115151541B (zh) 2019-12-19 2024-06-25 德彪药业国际股份公司 新型化合物及其用途

Family Cites Families (122)

* 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
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
CA2248179C (en) 1996-02-29 2007-09-18 Fujisawa Pharmaceutical Co., Ltd. .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
US6451816B1 (en) 1997-06-20 2002-09-17 Klinge Pharma Gmbh Use of pyridyl alkane, pyridyl alkene and/or pyridyl alkine acid amides in the treatment of tumors or for immunosuppression
DE19624659A1 (de) * 1996-06-20 1998-01-08 Klinge Co Chem Pharm Fab Neue Pyridylalken- und Pyridylalkinsäureamide
US6503881B2 (en) 1996-08-21 2003-01-07 Micrologix Biotech Inc. Compositions and methods for treating infections using cationic peptides alone or in combination with antibiotics
US6995254B1 (en) 1996-08-28 2006-02-07 Affinium Pharmaceuticals, Inc. Polynucleotide encoding the enoyl-acyl carrier protein reductase of Staphylococcus aureus, FAB I
BR9712072A (pt) 1996-09-20 1999-08-24 Meiji Seika Kaisha Subst-ncia cristalina de defditoren pivoxil e a produ-Æo da mesma
US6521408B1 (en) 1997-09-25 2003-02-18 National Institute Of Agrobiological Sciences Method for assessing a function of a gene
DE19641437A1 (de) 1996-10-08 1998-04-09 Basf Ag 1,3-Bis-(N-lactamyl)propane und deren pharmazeutische und kosmetische Verwendung
DE19652239A1 (de) 1996-12-16 1998-06-18 Bayer Ag Verwendung von 7-(2-Oxa-5,8-diazabicyclo[4.3.0]non-8-yl)-chinolon- und -naphthyridoncarbonsäure-Derivaten zur Therapie von Helicobacter-pylori-Infektionen und den damit assoziierten gastroduodenalen Erkrankungen
SI9600371B (sl) 1996-12-18 2005-04-30 LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d. Etilidenski derivati tricikličnih karbapenemov
WO1998043969A1 (en) 1997-03-31 1998-10-08 Dupont Pharmaceuticals Company Indazoles of cyclic ureas useful as hiv protease inhibitors
US6277836B1 (en) 1997-04-01 2001-08-21 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
SK88599A3 (en) 1997-10-31 2000-03-13 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
EP1028948B1 (en) * 1997-11-07 2003-01-29 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
IL137004A0 (en) 1998-01-07 2001-06-14 Meiji Seika Kaisha 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
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
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
ATE332692T1 (de) 1998-08-21 2006-08-15 Kyorin Seiyaku Kk Wässerige flüssige zubereitungen
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
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
US6267985B1 (en) 1999-06-30 2001-07-31 Lipocine Inc. Clear oil-containing pharmaceutical compositions
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
EP1159293A1 (en) 1999-03-03 2001-12-05 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
JP2003502282A (ja) 1999-04-08 2003-01-21 ザ ゼネラル ホスピタル コーポレーション ヒト転移性細胞の作用因子源から離れた意図された移動
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
CO5190665A1 (es) * 1999-06-23 2002-08-29 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
AU6925500A (en) * 1999-08-23 2001-03-19 Smithkline Beecham Corporation Fatty acid synthase inhibitors
EP1212093B1 (en) 1999-08-26 2004-07-07 Ganeden Biotech, Inc. Use of emu oil as a carrier for antifungal, antibacterial and antiviral medications
US6221859B1 (en) 1999-08-27 2001-04-24 Merck & Co., Inc. Carbapenem antibacterial compositions and methods of the treatment
US6174878B1 (en) 1999-08-31 2001-01-16 Alcon Laboratories, Inc. Topical use of kappa opioid agonists to treat otic pain
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
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
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
ATE332130T1 (de) 1999-10-08 2006-07-15 Affinium Pharm Inc Fab-i-hemmer
NZ517706A (en) 1999-10-08 2004-01-30 Affinium Pharm Inc Fab I inhibitors
US6503908B1 (en) 1999-10-11 2003-01-07 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
AU775565B2 (en) 1999-10-29 2004-08-05 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
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
WO2001081286A1 (en) 2000-04-21 2001-11-01 Rhodia/Chirex, Inc. Process for preparation of r-1-(aryloxy)propan-2-ol
US20050043321A1 (en) 2000-07-26 2005-02-24 Vyden John K. Method for treating atopic disorders
US6288239B1 (en) 2000-09-19 2001-09-11 Board Of Trustees Operating Michigan State University 5-trityloxymethyl-oxazolidinones and process for the preparation thereof
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
WO2002048097A1 (en) 2000-12-12 2002-06-20 Corvas International, Inc. Compounds, compositions and methods for treatment of parasitic infections
US6388070B1 (en) 2001-01-05 2002-05-14 Orchid Chemicals & Pharmaceuticals Ltd. Thioester derivatives of thiazolyl acetic acid and their use in the preparation of cephalosporin compounds
US6495158B1 (en) 2001-01-19 2002-12-17 Lec Tec Corporation Acne patch
DE60230934D1 (de) 2001-04-06 2009-03-05 Affinium Pharm Inc Fab-i-inhibitoren
US6573941B1 (en) * 2002-04-22 2003-06-03 Thomson Licensing Sa Low bit rate compression format conversion for improved resolution
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
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
SI1828167T1 (sl) 2004-06-04 2014-12-31 Debiopharm International Sa Forum "Apres-Demain" Akrilamidni derivati kot anitibiotična sredstva
EP1973902A2 (en) 2005-12-05 2008-10-01 Affinium Pharmaceuticals, Inc. 3-heterocyclylacrylamide compounds as fabi inhibitors and antibacterial agents
EP2687533B1 (en) 2006-07-20 2017-07-19 Debiopharm International SA Acrylamide derivatives as FAB I inhibitors
US8263613B2 (en) 2007-02-16 2012-09-11 Affinium Pharmaceuticals, Inc. Salts, prodrugs and polymorphs of fab I inhibitors

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