ZA956445B - Benzoxazolyl- and benzothiazolyloxazolidinones - Google Patents

Benzoxazolyl- and benzothiazolyloxazolidinones

Info

Publication number
ZA956445B
ZA956445B ZA956445A ZA956445A ZA956445B ZA 956445 B ZA956445 B ZA 956445B ZA 956445 A ZA956445 A ZA 956445A ZA 956445 A ZA956445 A ZA 956445A ZA 956445 B ZA956445 B ZA 956445B
Authority
ZA
South Africa
Prior art keywords
alkyl
substd
opt
alkoxy
acyl
Prior art date
Application number
ZA956445A
Other languages
English (en)
Inventor
Dieter Haebich
Bernd Riedl
Martin Rupprlt
Andreas Stolle
Hanno Wild
Rainer Endermann
Klaus Dieter Bremm
Hein-Peter Kroll
Harald Labischinski
Klaus Schaller
Hans-Otto Werling
Original Assignee
Bayer Ag
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 Bayer Ag filed Critical Bayer Ag
Publication of ZA956445B publication Critical patent/ZA956445B/xx

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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (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)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
ZA956445A 1994-08-03 1995-08-02 Benzoxazolyl- and benzothiazolyloxazolidinones ZA956445B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE4427475 1994-08-03
DE19514313A DE19514313A1 (de) 1994-08-03 1995-04-18 Benzoxazolyl- und Benzothiazolyloxazolidinone

Publications (1)

Publication Number Publication Date
ZA956445B true ZA956445B (en) 1996-03-22

Family

ID=25938925

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA956445A ZA956445B (en) 1994-08-03 1995-08-02 Benzoxazolyl- and benzothiazolyloxazolidinones

Country Status (30)

Country Link
US (1) US5529998A (fr)
EP (1) EP0697412B1 (fr)
JP (1) JPH0881463A (fr)
KR (1) KR960007585A (fr)
CN (1) CN1122803A (fr)
AT (1) ATE188698T1 (fr)
AU (1) AU698939B2 (fr)
BG (1) BG62404B1 (fr)
CA (1) CA2155092A1 (fr)
CO (1) CO4410392A1 (fr)
CZ (1) CZ198895A3 (fr)
DE (2) DE19514313A1 (fr)
DZ (1) DZ1920A1 (fr)
EE (1) EE9500049A (fr)
FI (1) FI953665L (fr)
HR (1) HRP950428A2 (fr)
HU (1) HUT75037A (fr)
IL (1) IL114784A (fr)
MA (1) MA23638A1 (fr)
NO (1) NO305701B1 (fr)
NZ (1) NZ272674A (fr)
PE (1) PE2796A1 (fr)
PL (1) PL309848A1 (fr)
RO (1) RO115263B1 (fr)
SK (1) SK97495A3 (fr)
SV (1) SV1995000045A (fr)
TN (1) TNSN95088A1 (fr)
TW (1) TW352386B (fr)
YU (1) YU51095A (fr)
ZA (1) ZA956445B (fr)

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP960159A2 (en) * 1995-04-21 1997-08-31 Bayer Ag Benzocyclopentane oxazolidinones containing heteroatoms
GB9601666D0 (en) * 1996-01-27 1996-03-27 Zeneca Ltd Chemical compounds
DE19604223A1 (de) * 1996-02-06 1997-08-07 Bayer Ag Neue substituierte Oxazolidinone
HRP970049A2 (en) 1996-02-06 1998-04-30 Bayer Ag New heteroaryl oxazolidinones
GB9702213D0 (en) 1996-02-24 1997-03-26 Zeneca Ltd Chemical compounds
GB9609919D0 (en) 1996-05-11 1996-07-17 Zeneca Ltd Chemical compounds
GB9717804D0 (en) 1997-08-22 1997-10-29 Zeneca Ltd Chemical compounds
GB9717807D0 (en) * 1997-08-22 1997-10-29 Zeneca Ltd Chemical compounds
GB9725244D0 (en) 1997-11-29 1998-01-28 Zeneca Ltd Chemical compounds
WO1999037630A1 (fr) 1998-01-23 1999-07-29 Versicor, Inc. Banques combinatoires d'oxazolidinones, compositions a base de tels composes et procedes de preparation
KR20010052615A (ko) 1998-06-05 2001-06-25 다비드 에 질레스 옥사졸리디논 유도체, 이것의 제조 방법 및 이것을함유하는 약학 조성물
GB9815880D0 (en) 1998-07-21 1998-09-16 Pfizer Ltd Heterocycles
US6420349B1 (en) 1998-08-24 2002-07-16 Bristol-Myers Squibb Company Isoxazolinone antibacterial agents
AU1045300A (en) * 1998-11-17 2000-06-05 Bayer Aktiengesellschaft Novel heterocyclyl-substituted oxazolidone derivatives
EP1147422A1 (fr) 1999-01-27 2001-10-24 Pharmacia & Upjohn Company Dosages de modulateurs de l'activite du facteur d'elongation p
GB9928568D0 (en) 1999-12-03 2000-02-02 Zeneca Ltd Chemical compounds
US6514529B2 (en) 2000-03-22 2003-02-04 Pharmacia & Upjohn Company Oxazolidinone tablet formulation
MY127336A (en) 2000-03-22 2006-11-30 Upjohn Co Container for linezolid iv solution
GB0009803D0 (en) * 2000-04-25 2000-06-07 Astrazeneca Ab Chemical compounds
US6465456B2 (en) 2000-06-29 2002-10-15 Bristol-Myers Squibb Company Isoxazolinone antibacterial agents
JP2004501965A (ja) 2000-06-30 2004-01-22 ファルマシア・アンド・アップジョン・カンパニー 細菌感染を治療するための組成物および方法
MY138797A (en) * 2000-12-15 2009-07-31 Vertex Pharma Bacterial gyrase inhibitors and uses thereof
ATE319710T1 (de) 2000-12-21 2006-03-15 Pharmacia & Upjohn Co Llc Antimikrobielle chinolonderivate und ihre verwendung zur behandlung bakterieller infektionen
US7141588B2 (en) * 2002-02-25 2006-11-28 Pfizer, Inc. N-aryl-2-oxazolidinone-5-carboxamides and their derivatives
AR038536A1 (es) * 2002-02-25 2005-01-19 Upjohn Co N-aril-2-oxazolidinona-5- carboxamidas y sus derivados
WO2003084534A1 (fr) * 2002-03-29 2003-10-16 Pharmacia & Upjohn Company Llc Administration orale, parenterale ou intraveineuse d'oxazolidinones utilisees dans le traitement des infections du pied causees par le diabete
MXPA04012628A (es) * 2002-06-13 2005-03-23 Patricia Olivershaffer DERIVADOS Y COMPUESTOS RELACIONADOS DEL áCIDO 2-UREIDO-6-HETEROARIL-3H-BENZOIMIDAZOL-4-CARBOXILICO COMO INHIBIDORES DE GIRASA Y/O TOPOISOMERASA IV PARA EL TRATAMIENTO DE INFECCIONES BACTERIALES.
WO2004014897A1 (fr) * 2002-08-12 2004-02-19 Pharmacia & Upjohn Company Llc N-aryl-2-oxazolidinones et leurs derives
AU2002339721A1 (en) * 2002-09-20 2004-04-08 Lupin Limited Oxazolidinone derivatives, process for their preperation and their use as antimycobacterial agents
WO2004045616A1 (fr) * 2002-11-21 2004-06-03 Pharmacia & Upjohn Company Llc Derives de n-(4-(piperazine-1-yl)-phenyl-2-oxazolidinone-5-carboxamides et composes associes servant d'agents antibacteriens
US7582635B2 (en) * 2002-12-24 2009-09-01 Purdue Pharma, L.P. Therapeutic agents useful for treating pain
US8193352B2 (en) * 2003-01-31 2012-06-05 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US7569591B2 (en) * 2003-01-31 2009-08-04 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US7582641B2 (en) 2003-01-31 2009-09-01 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
AR042956A1 (es) 2003-01-31 2005-07-13 Vertex Pharma Inhibidores de girasa y usos de los mismos
US7618974B2 (en) * 2003-01-31 2009-11-17 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
EP1594494A1 (fr) * 2003-02-07 2005-11-16 Warner-Lambert Company LLC Derives d'oxazolidinone n-substitues par un noyau bicyclique, utilises comme agents antibacteriens
EP1594865A2 (fr) * 2003-02-07 2005-11-16 Warner-Lambert Company LLC Agents antibacteriens
US7012088B2 (en) * 2003-02-24 2006-03-14 Pharmacia & Upjohn Company Indolone oxazolidinones and derivatives thereof
US20040204463A1 (en) * 2003-04-01 2004-10-14 Harris Christina Renee N-aryl-2-oxazolidinone-5-carboxamides and their derivatives
BRPI0413838A (pt) * 2003-08-25 2006-10-24 Warner Lambert Co compostos de ariloxazolidinona antimicrobianos
US7304050B2 (en) * 2003-09-16 2007-12-04 Pfizer Inc. Antibacterial agents
US20060004090A1 (en) * 2004-07-01 2006-01-05 Roberts William J Forskolin compositions and methods for administration
WO2007088438A2 (fr) * 2006-02-01 2007-08-09 Pfizer Products Inc. Agents antibactériens
EP2181994B1 (fr) 2006-03-31 2014-05-28 Research Foundation Itsuu Laboratory Composés antimicrobiens
EP2479173A1 (fr) 2007-04-27 2012-07-25 Purdue Pharma LP Agents thérapeutiques utiles pour traiter la douleur
EP2604599A1 (fr) 2007-04-27 2013-06-19 Purdue Pharma LP Antagonistes de TRPV1 et utilisations de ceux-ci
US8530646B2 (en) * 2007-10-02 2013-09-10 Research Foundation Itsuu Laboratory Oxazolidinone derivative having 7-membered hetero ring
JP5404652B2 (ja) * 2008-02-22 2014-02-05 アクテリオン ファーマシューティカルズ リミテッド オキサゾリジノン誘導体
US8759362B2 (en) * 2008-10-24 2014-06-24 Purdue Pharma L.P. Bicycloheteroaryl compounds and their use as TRPV1 ligands
US8703962B2 (en) * 2008-10-24 2014-04-22 Purdue Pharma L.P. Monocyclic compounds and their use as TRPV1 ligands
JP6085829B2 (ja) 2011-01-14 2017-03-01 スペロ トリネム, インコーポレイテッド ピリミジンジャイレースおよびトポイソメラーゼiv阻害剤
RU2625305C2 (ru) 2011-01-14 2017-07-13 Сперо Тринем, Инк. Твердые формы ингибитора гиразы (r)-1-этил-3-[6-фтор-5[2-(1-гидрокси-1-метил-этил) пиримидин-5-ил]-7-(тетрагидрофуран-2-ил)-1н-бензимидазол-2-ил] мочевины
PT2663556E (pt) 2011-01-14 2014-11-27 Vertex Pharma Processo de fabrico de inibidores de girase e topoisomerase iv
EP2663558A1 (fr) 2011-01-14 2013-11-20 Vertex Pharmaceuticals Incorporated Formes solides de l'inhibiteur de gyrase, la (r)-1-éthyl-3-[5-[2-{1-hydroxy-1-méthyl-éthyl}pyrimidin-5-yl]-7-(tétrahydrofuran-2-yl}-1h-benzimidazol-2-yl]urée
WO2012177707A1 (fr) 2011-06-20 2012-12-27 Vertex Pharmaceuticals Incorporated Esters phosphoriques d'inhibiteurs de gyrases et de topoisomérases
US9273043B2 (en) 2011-06-22 2016-03-01 Purdue Pharma L.P. TRPV1 antagonists including dihydroxy substituent and uses thereof
AU2012293417A1 (en) 2011-08-10 2013-05-02 Purdue Pharma L.P. TRPV1 antagonists including dihydroxy substituent and uses thereof
WO2014014845A1 (fr) 2012-07-18 2014-01-23 Vertex Pharmaceuticals Incorporated Thérapie combinée comprenant de la 1-éthyl-3[5-[-2-{1-hydroxy-1-méthyl-éthyl}pyrimidin-5-yl]-7-(tétrahydrofuran-2-yl}-1h-benzimidazol-2-yl]urée et ses dérivés pour traiter des maladies mycobactériennes
US9018216B2 (en) 2012-07-18 2015-04-28 Vertex Pharmaceuticals Incorporated Solid forms of (R)-2-(5-(2-(3-ethylureido)-6-fluoro-7-(tetrahydrofuran-2-yl)-1H-benzo[d]imidazol-5-yl)pyrimidin-2-yl)propan-2-yl dihydrogen phosphate and salts thereof

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4705799A (en) 1983-06-07 1987-11-10 E. I. Du Pont De Nemours And Company Aminomethyl oxooxazolidinyl benzenes useful as antibacterial agents
GB8504871D0 (en) * 1985-02-26 1985-03-27 Ici Plc Heterocyclic compounds
US4921869A (en) 1987-10-09 1990-05-01 E. I. Du Pont De Nemours And Company Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives useful as antibacterial agents
US4801600A (en) 1987-10-09 1989-01-31 E. I. Du Pont De Nemours And Company Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives useful as antibacterial agents
US4965268A (en) 1987-10-09 1990-10-23 E. I. Du Pont De Nemours And Company Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives useful as antibacterial agents
CA1320730C (fr) 1987-10-16 1993-07-27 The Du Pont Merck Pharmaceutical Company Derives d'aminomethyloxooxazolidinylaroylbenzene, agents antibacteriens
US5254577A (en) 1988-07-29 1993-10-19 The Du Pont Merck Pharmaceutical Company Aminomethyloxooxazolidinyl arylbenzene derivatives useful as antibacterial agents
ATE112773T1 (de) * 1988-09-15 1994-10-15 Upjohn Co 5-indolinyl-5-beta-amidomethyloxazolidin-2-one, 3-(substituierte kondensierte)phenyl-5-beta amidomethyloxazolidin-2-one und 3-(nitrogen- substituierte)phenyl-5-beta-amidomethyloxazolid n-2-one.
JP2669579B2 (ja) * 1991-10-23 1997-10-29 エーザイ株式会社 オキサゾリドン誘導体
AU667198B2 (en) * 1991-11-01 1996-03-14 Pharmacia & Upjohn Company Substituted aryl- and heteroarylphenyloxazolidinones useful as antibacterial agents

Also Published As

Publication number Publication date
US5529998A (en) 1996-06-25
MA23638A1 (fr) 1996-04-01
CO4410392A1 (es) 1997-01-09
PE2796A1 (es) 1996-03-23
SV1995000045A (es) 1996-06-17
NO953045D0 (no) 1995-08-02
YU51095A (sh) 1998-07-10
HU9502295D0 (en) 1995-09-28
IL114784A0 (en) 1995-11-27
CN1122803A (zh) 1996-05-22
EP0697412A1 (fr) 1996-02-21
EP0697412B1 (fr) 2000-01-12
CZ198895A3 (en) 1996-02-14
FI953665A7 (fi) 1996-02-04
TNSN95088A1 (fr) 1996-02-06
BG62404B1 (bg) 1999-10-29
AU2723095A (en) 1996-02-15
HRP950428A2 (en) 1997-08-31
HUT75037A (en) 1997-03-28
IL114784A (en) 1999-10-28
SK97495A3 (en) 1996-06-05
BG99833A (bg) 1996-02-28
PL309848A1 (en) 1996-02-05
EE9500049A (et) 1996-02-15
ATE188698T1 (de) 2000-01-15
CA2155092A1 (fr) 1996-02-04
FI953665L (fi) 1996-02-04
DZ1920A1 (fr) 2002-02-17
NZ272674A (en) 1997-02-24
TW352386B (en) 1999-02-11
FI953665A0 (fi) 1995-08-01
NO953045L (no) 1996-02-05
AU698939B2 (en) 1998-11-12
JPH0881463A (ja) 1996-03-26
KR960007585A (ko) 1996-03-22
RO115263B1 (ro) 1999-12-30
NO305701B1 (no) 1999-07-12
DE19514313A1 (de) 1996-02-08
DE59507595D1 (de) 2000-02-17

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