ES2518316T3 - Compuestos heterocíclicos, métodos de fabricación de los mismos y su uso en terapia - Google Patents
Compuestos heterocíclicos, métodos de fabricación de los mismos y su uso en terapia Download PDFInfo
- Publication number
- ES2518316T3 ES2518316T3 ES03796699.1T ES03796699T ES2518316T3 ES 2518316 T3 ES2518316 T3 ES 2518316T3 ES 03796699 T ES03796699 T ES 03796699T ES 2518316 T3 ES2518316 T3 ES 2518316T3
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- Spain
- Prior art keywords
- group
- formula
- alkyl
- independently
- case
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 150000002391 heterocyclic compounds Chemical class 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 title 1
- 238000002560 therapeutic procedure Methods 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 abstract 1
- 125000004005 formimidoyl group Chemical group [H]\N=C(/[H])* 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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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
- C07D213/73—Unsubstituted amino or imino radicals
-
- 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
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
- Apparatus For Disinfection Or Sterilisation (AREA)
Abstract
Compuesto de fórmula IA:**Fórmula** en el que, independientemente para cada caso, L es un alquenilo C2; A es un anillo arilo monocíclico de 6 miembros, un anillo heteroarilo bicíclico de 8 ó 9 miembros, o un anillo arilo bicíclico de miembros; en el que el anillo heteroarilo contiene 1-4 heteroátomos seleccionados entre N, S y O; y en el que los anillos arilo y heteroarilo están opcionalmente substituidos con uno o más grupos seleccionados 15 entre alquilo C1-4, CH2OH, OR'', SR'', CN, N(R'')2, CH2N(R'')2, NO2, CF3, CO2R'', CON(R'')2, COR'', NR''C(O)R'', F, Cl, Br, I y -S(O)rCF3, en los que R'' es H, alquilo o alcarilo; R1 es, independientemente para casa caso, H, alquilo, cicloalquilo, arilo o alcarilo; R2 es**Fórmula** en el que el grupo B adyacente al grupo D se selecciona del grupo que consiste en: C(R1)2 y C>=O; D se selecciona, independientemente para cada caso, del grupo que consiste en: C(R1)2, NR1, C>=O,**Fórmula** siempre que los dos grupos D sean diferentes, y en el que para D, B se selecciona del grupo que consiste en un enlace, C(R1)2 y C>=O; J es NR1, CH2, CH2CH2 u O; Q es N o CH; r es 0, 1 ó 2; R1 es tal como se ha definido previamente; b es un número entero de 0 a 4; a es 0; y n es un número entero de 0 a 4; o una sal farmacéuticamente aceptable del mismo.
Description
Claims (1)
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imagen1 imagen2 imagen3 imagen4 imagen5
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US43140602P | 2002-12-06 | 2002-12-06 | |
| US431406P | 2002-12-06 | ||
| US46558303P | 2003-04-25 | 2003-04-25 | |
| US465583P | 2003-04-25 | ||
| PCT/US2003/038706 WO2004052890A1 (en) | 2002-12-06 | 2003-12-05 | Heterocyclic compounds, methods of making them and their use in therapy |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2518316T3 true ES2518316T3 (es) | 2014-11-05 |
Family
ID=32511562
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES03796699.1T Expired - Lifetime ES2518316T3 (es) | 2002-12-06 | 2003-12-05 | Compuestos heterocíclicos, métodos de fabricación de los mismos y su uso en terapia |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US7790709B2 (es) |
| EP (1) | EP1575951B1 (es) |
| JP (2) | JP4859460B2 (es) |
| AU (1) | AU2003298937A1 (es) |
| CA (1) | CA2508792C (es) |
| CY (1) | CY1115606T1 (es) |
| DK (1) | DK1575951T3 (es) |
| ES (1) | ES2518316T3 (es) |
| PT (1) | PT1575951E (es) |
| SI (1) | SI1575951T1 (es) |
| WO (1) | WO2004052890A1 (es) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ECSP003699A (es) * | 1999-10-08 | 2002-04-23 | Smithkline Beecham Corp | Inhibidores de fab i |
| DE60230934D1 (de) * | 2001-04-06 | 2009-03-05 | Affinium Pharm Inc | Fab-i-inhibitoren |
| EP1575951B1 (en) | 2002-12-06 | 2014-06-25 | Debiopharm International SA | Heterocyclic compounds, methods of making them and their use in therapy |
| WO2004082586A2 (en) * | 2003-03-17 | 2004-09-30 | Affinium Pharmaceuticals, Inc. | Phamaceutical compositions comprising inhibitors of fab i and further antibiotics |
| US8450307B2 (en) * | 2004-06-04 | 2013-05-28 | Affinium Pharmaceuticals, Inc. | Therapeutic agents, and methods of making and using the same |
| US7973060B2 (en) | 2005-10-13 | 2011-07-05 | Crystalgenomics, Inc. | Fab I inhibitor and process for preparing same |
| CA2632476A1 (en) * | 2005-12-05 | 2007-06-14 | Affinium Pharmaceuticals, Inc. | Heterocyclylacrylamide compounds as fabi inhibitors and antibacterial agents |
| EP2687533B1 (en) * | 2006-07-20 | 2017-07-19 | Debiopharm International SA | Acrylamide derivatives as FAB I inhibitors |
| AU2007287430B2 (en) | 2006-08-23 | 2011-07-21 | Kudos Pharmaceuticals Limited | 2-methylmorpholine pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mTOR inhibitors |
| WO2008098374A1 (en) * | 2007-02-16 | 2008-08-21 | Affinium Pharmaceuticals, Inc. | Salts, prodrugs and polymorphs of fab i inhibitors |
| BRPI0914912A2 (pt) | 2008-06-20 | 2017-06-20 | Astrazeneca Ab | processo para a preparação de um composto, e de um inibidor de mtor quinase, sal de fumarato, composição farmacêutica, uso de um sal de fumarato, e, métodos para produzir um efeito inibitório mtor, e para produzir um efeito anti-câncer em um animal de sangue quente |
| EP2376453B1 (en) * | 2008-12-11 | 2019-11-20 | VIIV Healthcare Company | Intermediates for carbamoylpyridone hiv integrase inhibitors |
| WO2011061214A1 (en) | 2009-11-18 | 2011-05-26 | Fab Pharma Sas | Novel heterocyclic acrylamides and their use as pharmaceuticals |
| US9115149B2 (en) | 2011-09-19 | 2015-08-25 | Vitas Pharma Research Private Limited | Heterocyclic compounds as inhibitors of fatty acid biosysnthesis for bacterial infections |
| KR101720885B1 (ko) | 2012-06-19 | 2017-03-28 | 데비오팜 인터네셔날 에스 에이 | (e)-n-메틸-n-((3-메틸벤조푸란-2-일)메틸)-3-(7-옥소-5,6,7,8-테트라히드로-1,8-나프티리딘-3-일)아크릴아미드의전구약물 유도체 |
| WO2014072930A2 (en) * | 2012-11-09 | 2014-05-15 | Aurigene Discovery Technologies Limited | Fused pyridine derivatives as antibacterial agents |
| RS61312B1 (sr) | 2016-02-26 | 2021-02-26 | Debiopharm Int Sa | Lek za lečenje infekcija dijabetskog stopala |
| TWI903299B (zh) | 2018-03-08 | 2025-11-01 | 美商英塞特公司 | 作為PI3K-γ抑制劑之胺基吡嗪二醇化合物 |
| US11691967B2 (en) | 2018-03-12 | 2023-07-04 | The Board Of Trustees Of The University Of Illinois | Antibiotics effective for gram-negative pathogens |
| WO2020010003A1 (en) | 2018-07-02 | 2020-01-09 | Incyte Corporation | AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS |
| MY203711A (en) | 2019-02-14 | 2024-07-15 | Debiopharm Int Sa | Afabicin formulation, method for making the same and uses thereof |
| JP7418475B2 (ja) | 2019-06-14 | 2024-01-19 | デバイオファーム インターナショナル エス.エー. | バイオフィルムが関与する細菌感染症を治療するための医薬及びその使用 |
Family Cites Families (121)
| 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 |
| US5614551A (en) * | 1994-01-24 | 1997-03-25 | The Johns Hopkins University | Inhibitors of fatty acid synthesis as antimicrobial agents |
| US6176842B1 (en) * | 1995-03-08 | 2001-01-23 | Ekos Corporation | Ultrasound assembly for use with light activated drugs |
| US5989832A (en) | 1995-04-21 | 1999-11-23 | Microcide Pharmaceuticals, Inc. | Method for screening for non-tetracycline efflux pump inhibitors |
| DE69626389T2 (de) | 1995-05-11 | 2003-10-09 | Biochemie Ges.M.B.H., Kundl | Antibakterielle cephalosporinverbindungen |
| US6057291A (en) * | 1995-06-02 | 2000-05-02 | University Of British Columbia | Antimicrobial cationic peptides |
| JP3180350B2 (ja) | 1996-02-29 | 2001-06-25 | 藤沢薬品工業株式会社 | β―ラクタム系抗生物質含有錠剤およびその製造法 |
| US6239154B1 (en) | 1996-03-08 | 2001-05-29 | Adolor Corporation | Kappa agonist compounds pharmaceutical formulations and method of prevention and treatment of pruritus therewith |
| US6367985B1 (en) | 1996-03-12 | 2002-04-09 | Intellectual Property Company | Optical connector using large diameter alignment features |
| US6451816B1 (en) * | 1997-06-20 | 2002-09-17 | Klinge Pharma Gmbh | Use of pyridyl alkane, pyridyl alkene and/or pyridyl alkine acid amides in the treatment of tumors or for immunosuppression |
| US6503881B2 (en) * | 1996-08-21 | 2003-01-07 | Micrologix Biotech Inc. | Compositions and methods for treating infections using cationic peptides alone or in combination with antibiotics |
| US6995254B1 (en) * | 1996-08-28 | 2006-02-07 | Affinium Pharmaceuticals, Inc. | Polynucleotide encoding the enoyl-acyl carrier protein reductase of Staphylococcus aureus, FAB I |
| BR9712072A (pt) | 1996-09-20 | 1999-08-24 | Meiji Seika Kaisha | Subst-ncia cristalina de defditoren pivoxil e a produ-Æo da mesma |
| US6521408B1 (en) * | 1997-09-25 | 2003-02-18 | National Institute Of Agrobiological Sciences | Method for assessing a function of a gene |
| DE19641437A1 (de) | 1996-10-08 | 1998-04-09 | Basf Ag | 1,3-Bis-(N-lactamyl)propane und deren pharmazeutische und kosmetische Verwendung |
| DE19652239A1 (de) * | 1996-12-16 | 1998-06-18 | Bayer Ag | Verwendung von 7-(2-Oxa-5,8-diazabicyclo[4.3.0]non-8-yl)-chinolon- und -naphthyridoncarbonsäure-Derivaten zur Therapie von Helicobacter-pylori-Infektionen und den damit assoziierten gastroduodenalen Erkrankungen |
| SI9600371B (sl) | 1996-12-18 | 2005-04-30 | LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d. | Etilidenski derivati tricikličnih karbapenemov |
| AU6870098A (en) | 1997-03-31 | 1998-10-22 | Du Pont Merck Pharmaceutical Company, The | Indazoles of cyclic ureas useful as hiv protease inhibitors |
| ATE389417T1 (de) | 1997-04-01 | 2008-04-15 | Borody Thomas J | Verfahren und zusammensetzungen zur behandlung entzündlicher darmerkrankungen |
| US6406880B1 (en) | 1997-05-02 | 2002-06-18 | Integrated Research Technology, Llc | Betaines as adjuvants to susceptibility testing and antimicrobial therapy |
| US6184363B1 (en) | 1997-06-13 | 2001-02-06 | Northwestern University | Inhibitors of β-lactamases and uses therefor |
| WO1998058928A1 (fr) | 1997-06-23 | 1998-12-30 | Yoshitomi Pharmaceutical Industries, Ltd. | Agent prophylactique ou therapeutique contre des maladies attribuables a une infection par des helicobacters |
| AUPO758297A0 (en) | 1997-06-27 | 1997-07-24 | Rowe, James Baber | Control of acidic gut syndrome |
| US6198000B1 (en) | 1997-07-07 | 2001-03-06 | Pfizer Inc. | Intermediates useful in the synthesis of quinoline antibiotics |
| EP1000935A4 (en) | 1997-07-25 | 2001-03-21 | Tsumura & Co | PYRIDYL ACRYLAMIDE DERIVATIVES AND DRUGS AGAINST NEPHRITIS AND INHIBITORS OF THE TRANSFORMING GROWTH FACTOR BETA CONTAINING THESE DERIVATIVES |
| HN1998000106A (es) | 1997-08-01 | 1999-01-08 | Pfizer Prod Inc | Composiciones parenterales de alatroflaxacino |
| HUP0003855A3 (en) | 1997-08-08 | 2001-11-28 | Procter & Gamble | Improved processes for making surfactants via adsorptive separation and products thereof |
| 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 |
| US6432444B1 (en) | 1997-10-31 | 2002-08-13 | New Horizons Diagnostics Corp | Use of bacterial phage associated lysing enzymes for treating dermatological infections |
| RU2224024C2 (ru) | 1997-10-31 | 2004-02-20 | Зингента Партисипейшнс Аг | Трансгенные растения |
| SE9704404D0 (sv) | 1997-11-28 | 1997-11-28 | Astra Ab | New compounds |
| GB9725244D0 (en) | 1997-11-29 | 1998-01-28 | Zeneca Ltd | Chemical compounds |
| DE19753298A1 (de) | 1997-12-01 | 1999-06-02 | Basf Ag | Verfahren zur Herstellung von festen Dosierungsformen |
| EP1051978B1 (en) | 1998-01-07 | 2012-08-22 | Meiji Seika Pharma Co., Ltd. | Crystallographically stable amorphous cephalosporin compositions and process for producing the same |
| US6184380B1 (en) | 1999-01-25 | 2001-02-06 | Pfizer Inc. | Process for preparing naphthyridones and intermediates |
| PA8466701A1 (es) * | 1998-01-21 | 2000-09-29 | Pfizer Prod Inc | Comprimido de mesilato de trovafloxacino |
| US6204279B1 (en) | 1998-06-03 | 2001-03-20 | Microcide Pharmaceuticals, Inc. | Peptidomimetic efflux pump inhibitors |
| US6503539B2 (en) * | 1998-02-27 | 2003-01-07 | Biora Bioex Ab | Matrix protein compositions for wound healing |
| US6350738B1 (en) | 1998-03-06 | 2002-02-26 | Brigham Young University | Steroid derived antibiotics |
| JP4405602B2 (ja) * | 1998-04-16 | 2010-01-27 | バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト | ヒストン脱アセチル化酵素阻害剤 |
| DE19820801A1 (de) | 1998-05-09 | 1999-11-25 | Gruenenthal Gmbh | Orale Arzneiformen mit reproduzierbarer Wirkstofffreisetzung von Gatifloxacin oder pharmazeutisch verwendbaren Salzen oder Hydraten |
| DE19821039A1 (de) | 1998-05-11 | 1999-11-18 | Bayer Ag | Verfahren zur Herstellung von (S,S)-Benzyl-2,8-diazabicyclo[4.3.0]nonan |
| US6399629B1 (en) * | 1998-06-01 | 2002-06-04 | Microcide Pharmaceuticals, Inc. | Efflux pump inhibitors |
| US6428579B1 (en) | 1998-07-01 | 2002-08-06 | Brown University Research Foundation | Implantable prosthetic devices coated with bioactive molecules |
| US6423741B1 (en) | 1998-07-10 | 2002-07-23 | Council Of Scientific And Industrial Research | Anti-microbial composition and method for producing the same |
| GB9815567D0 (en) | 1998-07-18 | 1998-09-16 | Glaxo Group Ltd | Antiviral compound |
| PT1101497E (pt) | 1998-08-04 | 2008-04-23 | Schering Plough Animal Health | Preparações oleosas estabilizadas de tobicilina (antibiótico beta-lactâmico) |
| CN1133432C (zh) | 1998-08-21 | 2004-01-07 | 千寿制药株式会社 | 含水液体药物组合物 |
| US6461607B1 (en) | 1998-08-24 | 2002-10-08 | Ganeden Biotech, Inc. | Probiotic, lactic acid-producing bacteria and uses thereof |
| US6518487B1 (en) | 1998-09-23 | 2003-02-11 | Pioneer Hi-Bred International, Inc. | Cyclin D polynucleotides, polypeptides and uses thereof |
| 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 |
| AU768957B2 (en) | 1999-02-18 | 2004-01-08 | Regents Of The University Of California, The | Phthalamide-lanthanide complexes for use as luminescent markers |
| 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 |
| US6248363B1 (en) | 1999-11-23 | 2001-06-19 | Lipocine, Inc. | Solid carriers for improved delivery of active ingredients in 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 |
| AU4230900A (en) * | 1999-04-08 | 2000-10-23 | General Hospital Corporation, The | Purposeful movement of human migratory cells away from an agent source |
| CO5180550A1 (es) * | 1999-04-19 | 2002-07-30 | Smithkline Beecham Corp | Inhibidores de fab i |
| US6290946B1 (en) | 1999-05-13 | 2001-09-18 | Geltex Pharmaceuticals, Inc. | Anionic polymers as toxin binders and antibacterial agents |
| US6514535B2 (en) | 1999-05-21 | 2003-02-04 | Noveon Ip Holdings Corp. | Bioadhesive hydrogels with functionalized degradable crosslinks |
| AR024077A1 (es) * | 1999-05-25 | 2002-09-04 | Smithkline Beecham Corp | Compuestos antibacterianos |
| CO5370679A1 (es) | 1999-06-01 | 2004-02-27 | Smithkline Beecham Corp | Inhibidores fab 1 |
| US6239141B1 (en) * | 1999-06-04 | 2001-05-29 | Pfizer Inc. | Trovafloxacin oral suspensions |
| CO5180605A1 (es) * | 1999-06-23 | 2002-07-30 | Smithkline Beecham Corp | Compuestos de indol |
| CA2282066C (en) | 1999-06-29 | 2010-09-07 | Smithkline Beecham Corporation | Methods of use of quinolone compounds against atypical upper respiratory pathogenic bacteria |
| US6309663B1 (en) | 1999-08-17 | 2001-10-30 | Lipocine Inc. | Triglyceride-free compositions and methods for enhanced absorption of hydrophilic therapeutic agents |
| US6500459B1 (en) | 1999-07-21 | 2002-12-31 | Harinderpal Chhabra | Controlled onset and sustained release dosage forms and the preparation thereof |
| US6346391B1 (en) * | 1999-07-22 | 2002-02-12 | Trustees Of Tufts College | Methods of reducing microbial resistance to drugs |
| EP1212093B1 (en) | 1999-08-26 | 2004-07-07 | Ganeden Biotech, Inc. | Use of emu oil as a carrier for antifungal, antibacterial and antiviral medications |
| US6221859B1 (en) * | 1999-08-27 | 2001-04-24 | Merck & Co., Inc. | Carbapenem antibacterial compositions and methods of the treatment |
| US6174878B1 (en) * | 1999-08-31 | 2001-01-16 | Alcon Laboratories, Inc. | Topical use of kappa opioid agonists to treat otic pain |
| CN1373674A (zh) | 1999-09-11 | 2002-10-09 | 宝洁公司 | 易流动液体载体 |
| DE60025503T2 (de) | 1999-09-17 | 2006-09-07 | Daiichi Asubio Pharma Co., Ltd. | Pharmazeutische Zusammensetzungen, die Faropenem-Natrium und eine Diaminoacetat Verbindung zur Verbesserung der Magen-Darm-Trakt Absorption enthalten |
| US6500463B1 (en) | 1999-10-01 | 2002-12-31 | General Mills, Inc. | Encapsulation of sensitive components into a matrix to obtain discrete shelf-stable particles |
| ECSP003699A (es) * | 1999-10-08 | 2002-04-23 | Smithkline Beecham Corp | Inhibidores de fab i |
| DE60019954T2 (de) * | 1999-10-08 | 2006-02-23 | Affinium Pharmaceuticals, Inc., Toronto | Fab i hemmer |
| 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 |
| DE60029235T2 (de) * | 1999-10-08 | 2007-06-14 | Affinium Pharmaceuticals, Inc., Toronto | Fab-i-hemmer |
| CA2323008C (en) * | 1999-10-11 | 2005-07-12 | Pfizer Inc. | Pharmaceutically active compounds |
| EP1227096B1 (en) | 1999-10-19 | 2004-09-22 | Sato Pharmaceutical Co. Ltd. | 4-oxoquinolizine antimicrobials having 2-pyridone skeletons as the partial structure |
| US6951729B1 (en) * | 1999-10-27 | 2005-10-04 | Affinium Pharmaceuticals, Inc. | High throughput screening method for biological agents affecting fatty acid biosynthesis |
| CN1188111C (zh) * | 1999-10-29 | 2005-02-09 | 耐科塔医药公司 | 分散性得到改进的干粉组合物 |
| US6531291B1 (en) * | 1999-11-10 | 2003-03-11 | The Trustees Of Columbia University In The City Of New York | Antimicrobial activity of gemfibrozil and related compounds and derivatives and metabolites thereof |
| US6514986B2 (en) | 2000-11-22 | 2003-02-04 | Wockhardt Limited | Chiral fluoroquinolone arginine salt forms |
| US6372752B1 (en) * | 2000-02-07 | 2002-04-16 | Genzyme Corporation | Inha inhibitors and methods of use thereof |
| AU2000255628A1 (en) | 2000-03-28 | 2001-10-08 | Council Of Scientific And Industrial Research | Formulation comprising thymol useful in the treatment of drug resistant bacterial infections |
| JP2003531184A (ja) | 2000-04-21 | 2003-10-21 | ローディア/カイレックス・インコーポレイテッド | (r)−1−(アリールオキシ)プロパン−2−オールの製造方法 |
| WO2002007682A1 (en) * | 2000-07-26 | 2002-01-31 | Vyden John K | Methods for treating atopic disorders |
| DE10037029A1 (de) | 2000-07-27 | 2002-02-28 | Kugelstrahlzentrum Aachen Gmbh | Verfahren und Vorrichtung zum Umformen von Strukturbauteilen |
| US6288239B1 (en) * | 2000-09-19 | 2001-09-11 | Board Of Trustees Operating Michigan State University | 5-trityloxymethyl-oxazolidinones and process for the preparation thereof |
| US7048926B2 (en) * | 2000-10-06 | 2006-05-23 | Affinium Pharmaceuticals, Inc. | Methods of agonizing and antagonizing FabK |
| US6821746B2 (en) | 2000-10-06 | 2004-11-23 | Affinium Pharmaceuticals, Inc. | Methods of screening for FabK antagonists and agonists |
| US6388070B1 (en) * | 2001-01-05 | 2002-05-14 | Orchid Chemicals & Pharmaceuticals Ltd. | Thioester derivatives of thiazolyl acetic acid and their use in the preparation of cephalosporin compounds |
| US6495158B1 (en) | 2001-01-19 | 2002-12-17 | Lec Tec Corporation | Acne patch |
| PA8539401A1 (es) * | 2001-02-14 | 2002-10-28 | Warner Lambert Co | Quinazolinas como inhibidores de mmp-13 |
| DE60230934D1 (de) * | 2001-04-06 | 2009-03-05 | Affinium Pharm Inc | Fab-i-inhibitoren |
| US6503906B1 (en) | 2002-02-21 | 2003-01-07 | Ren-Jin Lee | Method for optimizing ciprofloxacin treatment of anthrax-exposed patients according to the patient's characteristics |
| MXPA04009580A (es) * | 2002-04-02 | 2005-05-27 | Tsumura & Co | Inhibidor de fosfodiesterasa iv que contiene un derivado de piridilacrilamida. |
| EP1575951B1 (en) | 2002-12-06 | 2014-06-25 | Debiopharm International SA | Heterocyclic compounds, methods of making them and their use in therapy |
| WO2004082586A2 (en) * | 2003-03-17 | 2004-09-30 | Affinium Pharmaceuticals, Inc. | Phamaceutical compositions comprising inhibitors of fab i and further antibiotics |
| CA2632476A1 (en) * | 2005-12-05 | 2007-06-14 | Affinium Pharmaceuticals, Inc. | Heterocyclylacrylamide compounds as fabi inhibitors and antibacterial agents |
| EP2687533B1 (en) | 2006-07-20 | 2017-07-19 | Debiopharm International SA | Acrylamide derivatives as FAB I inhibitors |
| WO2008098374A1 (en) * | 2007-02-16 | 2008-08-21 | Affinium Pharmaceuticals, Inc. | Salts, prodrugs and polymorphs of fab i inhibitors |
| CA2757954A1 (en) | 2009-04-08 | 2010-10-14 | C & D Zodiac, Inc. | Vehicle seat tubing having variable wall thickness |
| JP6013846B2 (ja) | 2011-10-06 | 2016-10-25 | リコー電子デバイス株式会社 | スイッチングレギュレータ及び電子機器 |
| US8975502B1 (en) | 2012-05-15 | 2015-03-10 | Rodulfo Delgado | Guitar with body-mounted tuning system |
| US8973902B2 (en) | 2012-12-21 | 2015-03-10 | Comeup Industries Inc. | Power winch horizontal-pull clutch device |
-
2003
- 2003-12-05 EP EP03796699.1A patent/EP1575951B1/en not_active Expired - Lifetime
- 2003-12-05 DK DK03796699.1T patent/DK1575951T3/da active
- 2003-12-05 AU AU2003298937A patent/AU2003298937A1/en not_active Abandoned
- 2003-12-05 WO PCT/US2003/038706 patent/WO2004052890A1/en not_active Ceased
- 2003-12-05 US US10/537,747 patent/US7790709B2/en not_active Expired - Lifetime
- 2003-12-05 ES ES03796699.1T patent/ES2518316T3/es not_active Expired - Lifetime
- 2003-12-05 SI SI200332388T patent/SI1575951T1/sl unknown
- 2003-12-05 PT PT37966991T patent/PT1575951E/pt unknown
- 2003-12-05 CA CA2508792A patent/CA2508792C/en not_active Expired - Fee Related
- 2003-12-05 JP JP2005508475A patent/JP4859460B2/ja not_active Expired - Fee Related
-
2010
- 2010-07-27 US US12/844,403 patent/US20110124633A1/en not_active Abandoned
-
2011
- 2011-06-30 JP JP2011145487A patent/JP2012006927A/ja active Pending
-
2014
- 2014-09-25 CY CY20141100786T patent/CY1115606T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20110124633A1 (en) | 2011-05-26 |
| AU2003298937A1 (en) | 2004-06-30 |
| EP1575951A1 (en) | 2005-09-21 |
| CY1115606T1 (el) | 2017-01-04 |
| CA2508792C (en) | 2013-02-05 |
| SI1575951T1 (sl) | 2014-10-30 |
| EP1575951B1 (en) | 2014-06-25 |
| CA2508792A1 (en) | 2004-06-24 |
| WO2004052890A1 (en) | 2004-06-24 |
| JP2012006927A (ja) | 2012-01-12 |
| JP2006513262A (ja) | 2006-04-20 |
| PT1575951E (pt) | 2014-09-15 |
| JP4859460B2 (ja) | 2012-01-25 |
| US20060183908A1 (en) | 2006-08-17 |
| DK1575951T3 (da) | 2014-09-15 |
| US7790709B2 (en) | 2010-09-07 |
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