AR020250A1 - COMPOUND OF ISOXAZOLINONA, PHARMACEUTICAL COMPOSITION THAT INCLUDES IT AND ITS USE TO PREPARE SUCH COMPOSITION - Google Patents
COMPOUND OF ISOXAZOLINONA, PHARMACEUTICAL COMPOSITION THAT INCLUDES IT AND ITS USE TO PREPARE SUCH COMPOSITIONInfo
- Publication number
- AR020250A1 AR020250A1 ARP990104229A ARP990104229A AR020250A1 AR 020250 A1 AR020250 A1 AR 020250A1 AR P990104229 A ARP990104229 A AR P990104229A AR P990104229 A ARP990104229 A AR P990104229A AR 020250 A1 AR020250 A1 AR 020250A1
- Authority
- AR
- Argentina
- Prior art keywords
- carbon atoms
- alkyl
- optionally substituted
- ring
- halo
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D261/12—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Los compuestos de isoxazolinonas de la formula 1, son efectivas como agentes antibacterianos o una sal farmacéuticamente aceptable del mismo, en donde : R1es: H, alquilo de 1 a 8 átomos de carbono opcionalmente sustituido con uno o más F, Cl, OH,alc oxi de 1 a 8 átomos de carbono, o aciloxi de 1 a 8 átomos decarbono, cicloalquilo de 1 a 6 átomos de carbono, o alcoxi de 1 a 8 átomos de carbono, L es oxígeno o azufre, A es: formula 2, formula 3 , una porcionheteroaromática de 5 miembros quetiene uno a tres heteroátomos seleccionados a partir del grupo que consiste de S, N O, en donde la porcion heteroaromáticade 5 miembros se une via un átomo de carbono y puede crear adicionalmente un anillo de benceno o naftilo, y en donde laporcion heter oaromática estáopcionalmente sustituido con uno a tres R8, una porcion heteroaromática de 6 miembros que tiene al menos un átomo de nitrogeno, en donde la porcionheteroaromática de 6 miembros puede tener adicionalmente un anillo debenceno o naftilo fusionado, y en donde la porcion heteroaromática está opcionalmentesustituida con con uno a tres R9, una beta-carbolin-3-ilo o indolizinilo unido vía el anillo de 6 miembros opcionalmente sustituido con uno a tres R9, deformula 4 yformula 5 en donde R2 y R3 son cada uno independientemente H, F, Cl, Br, alquilo de 1 a 6 átomos de carbono NO2, I, alcoxi de 1 a 6 átomos decarbono, OH, amino, ciano, o 1) R2 y R3 tomamos conjuntamente son -O(CH2)n-O, en donde R4, H, alquilo de 1 a2 átomos de carbon o, F, o OH, R5 es H, CF3,alquilo sustituido con uno o más halo, fenilo opcionalmente sustituido con uno o más halo, R5 y R6 tomados conjuntamente son un anillo de 5, 6 o 7 miembros dela formulas 6 y 7 en la cual D es S, O o NR86en donde R86 es H alq uilo de 1 a 6 átomos de carbono, o R5 y R6 tomados conjuntamente son -(CH2)k-, en donde R7,es un grupo de retiro de electrones. R6 y R7 en cada ocurrencia son los mismos o diferentes y son un grupo de retiro de electrones, H,CF3, alquilo de 1 a 3áto mos de carbono opcionalmente sustituido con un halo, fenilo, con la condicion de que al menos uno de R6 y R7 es un grupo de retiro de electrones, o R6 y R7The isoxazolinone compounds of the formula 1 are effective as antibacterial agents or a pharmaceutically acceptable salt thereof, wherein: R1 is: H, alkyl of 1 to 8 carbon atoms optionally substituted with one or more F, Cl, OH, alc oxy of 1 to 8 carbon atoms, or acyloxy of 1 to 8 carbon atoms, cycloalkyl of 1 to 6 carbon atoms, or alkoxy of 1 to 8 carbon atoms, L is oxygen or sulfur, A is: formula 2, formula 3, a 5-membered heteroaromatic portion having one to three heteroatoms selected from the group consisting of S, NO, wherein the 5-member heteroaromatic portion is attached via a carbon atom and can additionally create a benzene or naphthyl ring, and wherein the oaromatic heteric portion is optionally substituted with one to three R8, a 6-membered heteroaromatic portion that has at least one nitrogen atom, where the 6-membered heteroaromatic portion may additionally have a must ring eno or fused naphthyl, and wherein the heteroaromatic portion is optionally substituted with one to three R9, a beta-carbolin-3-yl or indolizinyl attached via the 6-membered ring optionally substituted with one to three R9, deformulates 4 and formulates 5 into where R2 and R3 are each independently H, F, Cl, Br, alkyl of 1 to 6 carbon atoms NO2, I, alkoxy of 1 to 6 carbon atoms, OH, amino, cyano, or 1) R2 and R3 we take together are -O (CH2) nO, wherein R4, H, alkyl of 1 to 2 carbon atoms or, F, or OH, R5 is H, CF3, alkyl substituted with one or more halo, phenyl optionally substituted with one or more halo , R5 and R6 taken together are a ring of 5, 6 or 7 members of formulas 6 and 7 in which D is S, O or NR86 where R86 is H alkyl of 1 to 6 carbon atoms, or R5 and R6 taken together they are - (CH2) k-, where R7 is an electron removal group. R6 and R7 in each occurrence are the same or different and are an electron removal group, H, CF3, alkyl of 1 to 3 carbon atoms optionally substituted with a halo, phenyl, with the proviso that at least one of R6 and R7 is an electron removal group, or R6 and R7
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US9757498P | 1998-08-24 | 1998-08-24 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR020250A1 true AR020250A1 (en) | 2002-05-02 |
Family
ID=22264103
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP990104229A AR020250A1 (en) | 1998-08-24 | 1999-08-24 | COMPOUND OF ISOXAZOLINONA, PHARMACEUTICAL COMPOSITION THAT INCLUDES IT AND ITS USE TO PREPARE SUCH COMPOSITION |
Country Status (22)
Country | Link |
---|---|
EP (1) | EP1107756A4 (en) |
JP (1) | JP2002523369A (en) |
KR (1) | KR20010072945A (en) |
CN (1) | CN1314813A (en) |
AR (1) | AR020250A1 (en) |
AU (1) | AU748750B2 (en) |
BR (1) | BR9913225A (en) |
CA (1) | CA2341271A1 (en) |
CO (1) | CO5160266A1 (en) |
CZ (1) | CZ2001669A3 (en) |
HU (1) | HUP0103433A3 (en) |
ID (1) | ID27690A (en) |
IL (1) | IL141542A0 (en) |
NO (1) | NO20010916L (en) |
NZ (1) | NZ509867A (en) |
PE (1) | PE20001063A1 (en) |
PL (1) | PL346267A1 (en) |
TR (1) | TR200100672T2 (en) |
TW (1) | TW572757B (en) |
UY (1) | UY25677A1 (en) |
WO (1) | WO2000010566A1 (en) |
ZA (1) | ZA200101505B (en) |
Families Citing this family (27)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6465456B2 (en) * | 2000-06-29 | 2002-10-15 | Bristol-Myers Squibb Company | Isoxazolinone antibacterial agents |
JP2002020366A (en) * | 2000-07-05 | 2002-01-23 | Sumitomo Seika Chem Co Ltd | Method for producing alkylthiophenylacetic acid |
PE20020689A1 (en) | 2000-11-17 | 2002-08-03 | Upjohn Co | OXAZOLIDINONES WITH A HETEROCYCLE OF 6 OR 7 MEMBERS UNITED WITH ANNULAR LINK TO BENZENE |
PE20030044A1 (en) * | 2000-11-17 | 2003-02-09 | Upjohn Co | BICYCLE ISOXAZOLINONES OF FORMULA I |
US6861433B2 (en) | 2000-12-15 | 2005-03-01 | Pharmacia & Upjohn Company | Oxazolidinone photoaffinity probes |
ES2256331T3 (en) | 2000-12-21 | 2006-07-16 | PHARMACIA & UPJOHN COMPANY LLC | ANTIMICROBIAL QUINOLINE DERIVATIVES AND USE OF THE SAME TO TREAT BACTERIAL INFECTIONS. |
ES2180456B1 (en) * | 2001-07-20 | 2004-05-01 | Laboratorios S.A.L.V.A.T., S.A. | SUBSTITUTED ISOXAZOLS AND ITS USE AS ANTIBIOTICS. |
WO2003031443A1 (en) | 2001-10-04 | 2003-04-17 | Morphochem Aktiengesellschaft für kombinatorische Chemie | Dual actions antibiotics comprising a oxazoldinone and a quinolone or naphthyridinone moiety |
EP1443930A1 (en) | 2001-10-25 | 2004-08-11 | AstraZeneca AB | Isoxazoline derivatives useful as antimicrobials |
US6875784B2 (en) | 2002-10-09 | 2005-04-05 | Pharmacia & Upjohn Company | Antimibicrobial [3.1.0.] bicyclic oxazolidinone derivatives |
US7105547B2 (en) | 2002-10-10 | 2006-09-12 | Pharmacia And Upjohn Company | Antimicrobial 1-aryl dihydropyridone compounds |
MXPA05007724A (en) * | 2003-02-07 | 2005-09-30 | Warner Lambert Co | Antibacterial agents. |
MXPA05011654A (en) | 2003-04-30 | 2005-12-15 | Morphochem Ag Komb Chemie | Use of oxazolidinone-quinoline hybrid antibiotics for the treatment of anthrax and other infections. |
EP2492264A3 (en) | 2003-06-03 | 2012-12-19 | Rib-X Pharmaceuticals, Inc. | Biaryl Heterocyclic Compounds And Methods Of Making And Using The Same |
JP2007525468A (en) * | 2003-06-03 | 2007-09-06 | リブ−エックス ファーマシューティカルズ,インコーポレイテッド | Sulfonamide compounds and methods for producing and using the same |
US8324398B2 (en) | 2003-06-03 | 2012-12-04 | Rib-X Pharmaceuticals, Inc. | Process for the synthesis of biaryl oxazolidinones |
US20070197541A1 (en) * | 2003-07-29 | 2007-08-23 | Oyelere Adegboyega K | Biaryl heterocyclic amines,amides, and sulfur-containing compounds and methods of making and using the same |
DE10340485B4 (en) * | 2003-09-03 | 2015-05-13 | Morphochem AG Aktiengesellschaft für kombinatorische Chemie | Process for the preparation of oxazolidinone-quinolone hybrids |
US7304050B2 (en) | 2003-09-16 | 2007-12-04 | Pfizer Inc. | Antibacterial agents |
TW200526649A (en) | 2003-12-17 | 2005-08-16 | Rib X Pharmaceuticals Inc | Halogenated biaryl heterocyclic compounds and methods of making and using the same |
US8158797B2 (en) | 2003-12-18 | 2012-04-17 | Morphochem Aktiengesellschaft Fur Kombinatorische Chemie | Oxazolidinone-quinolone hybrid antibiotics |
CN1898238A (en) | 2003-12-18 | 2007-01-17 | 莫弗凯姆联合化学股份公司 | Oxazolidinone-quinolone hybrid antibiotics |
WO2005082900A2 (en) * | 2004-01-28 | 2005-09-09 | Pharmacia & Upjohn Company Llc | Oxazolidinone amidoximes as antibacterial agents |
JP5534497B2 (en) | 2005-06-08 | 2014-07-02 | メリンタ セラピューティクス,インコーポレイテッド | Method for synthesizing triazoles |
AT503354B1 (en) * | 2006-02-22 | 2008-07-15 | Dsm Fine Chem Austria Gmbh | METHOD FOR THE PRODUCTION OF 3,4-DISUBSTITUTED PHENYL ACETIC ACIDS, AND NEW INTERMEDIATE COMPOUNDS |
JP4518066B2 (en) * | 2006-10-25 | 2010-08-04 | 宇部興産株式会社 | Dialkoxynitrile derivative and process for producing the same |
CN110423610B (en) * | 2019-08-29 | 2023-05-12 | 浙江理工大学 | Fluorescent probe for detecting two-photon mercury ions and preparation method and use method thereof |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE2045049A1 (en) * | 1970-09-11 | 1972-03-23 | Dr Karl Thomae GmbH, 7950 Biberach | New Nitrofurandenvate and processes for their production |
US4000155A (en) * | 1975-12-11 | 1976-12-28 | Eli Lilly And Company | Herbicidal 2-methyl-4-phenyl-5-pyrazolinones[and isoxazolinones] |
ATE161833T1 (en) * | 1992-12-08 | 1998-01-15 | Upjohn Co | PHENYLOXAZOLIDINONE DERIVATIVES SUBSTITUTED BY A TROPONE GROUP AS AN ANTIBACTERIAL AGENT |
ES2185800T3 (en) * | 1995-09-15 | 2003-05-01 | Upjohn Co | ANTIBACTERIAL AGENTS BASED ON 5-AMIDOMETHYL, 3-ARYL BUTIROLACTONE ALPHA, BETA SATURATED AND UNSATURATED. |
GB9521508D0 (en) * | 1995-10-20 | 1995-12-20 | Zeneca Ltd | Chemical compounds |
ES2186916T3 (en) * | 1996-08-21 | 2003-05-16 | Upjohn Co | ISOXAZOLINE DERIVATIVES AS ANTIMICROBIAL AGENTS. |
-
1999
- 1999-08-19 TW TW88114208A patent/TW572757B/en active
- 1999-08-23 ID IDW20010439A patent/ID27690A/en unknown
- 1999-08-23 TR TR2001/00672T patent/TR200100672T2/en unknown
- 1999-08-23 CA CA002341271A patent/CA2341271A1/en not_active Abandoned
- 1999-08-23 EP EP99945157A patent/EP1107756A4/en not_active Withdrawn
- 1999-08-23 CZ CZ2001669A patent/CZ2001669A3/en unknown
- 1999-08-23 WO PCT/US1999/019265 patent/WO2000010566A1/en not_active Application Discontinuation
- 1999-08-23 NZ NZ509867A patent/NZ509867A/en unknown
- 1999-08-23 HU HU0103433A patent/HUP0103433A3/en unknown
- 1999-08-23 PL PL99346267A patent/PL346267A1/en not_active Application Discontinuation
- 1999-08-23 CN CN99809894A patent/CN1314813A/en active Pending
- 1999-08-23 CO CO99053191A patent/CO5160266A1/en unknown
- 1999-08-23 BR BR9913225-7A patent/BR9913225A/en not_active IP Right Cessation
- 1999-08-23 JP JP2000565887A patent/JP2002523369A/en active Pending
- 1999-08-23 IL IL14154299A patent/IL141542A0/en unknown
- 1999-08-23 AU AU57833/99A patent/AU748750B2/en not_active Ceased
- 1999-08-23 KR KR1020017002377A patent/KR20010072945A/en not_active Application Discontinuation
- 1999-08-24 AR ARP990104229A patent/AR020250A1/en not_active Application Discontinuation
- 1999-08-24 PE PE1999000853A patent/PE20001063A1/en not_active Application Discontinuation
- 1999-08-24 UY UY25677A patent/UY25677A1/en unknown
-
2001
- 2001-02-22 ZA ZA200101505A patent/ZA200101505B/en unknown
- 2001-02-23 NO NO20010916A patent/NO20010916L/en not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
AU748750B2 (en) | 2002-06-13 |
TR200100672T2 (en) | 2001-07-23 |
HUP0103433A3 (en) | 2002-08-28 |
CZ2001669A3 (en) | 2001-08-15 |
ID27690A (en) | 2001-04-19 |
CO5160266A1 (en) | 2002-05-30 |
EP1107756A4 (en) | 2003-02-26 |
CN1314813A (en) | 2001-09-26 |
WO2000010566A1 (en) | 2000-03-02 |
NO20010916D0 (en) | 2001-02-23 |
JP2002523369A (en) | 2002-07-30 |
PE20001063A1 (en) | 2000-12-24 |
AU5783399A (en) | 2000-03-14 |
BR9913225A (en) | 2001-05-22 |
EP1107756A1 (en) | 2001-06-20 |
TW572757B (en) | 2004-01-21 |
KR20010072945A (en) | 2001-07-31 |
PL346267A1 (en) | 2002-01-28 |
ZA200101505B (en) | 2002-02-22 |
NZ509867A (en) | 2003-08-29 |
NO20010916L (en) | 2001-04-10 |
IL141542A0 (en) | 2002-03-10 |
UY25677A1 (en) | 2001-08-27 |
CA2341271A1 (en) | 2000-03-02 |
HUP0103433A2 (en) | 2002-01-28 |
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Legal Events
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FA | Abandonment or withdrawal |