AR041568A1 - Derivados de oxazolidinonas biciclicas (3.1.0) con actividad antimicrobiana - Google Patents
Derivados de oxazolidinonas biciclicas (3.1.0) con actividad antimicrobianaInfo
- Publication number
- AR041568A1 AR041568A1 ARP030103679A ARP030103679A AR041568A1 AR 041568 A1 AR041568 A1 AR 041568A1 AR P030103679 A ARP030103679 A AR P030103679A AR P030103679 A ARP030103679 A AR P030103679A AR 041568 A1 AR041568 A1 AR 041568A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- het1
- nhc
- aryl
- nr10r11
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- 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
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- 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
- 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
- C07D491/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Ophthalmology & Optometry (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente proporciona ciertos derivados de oxazolidinonas bicíclicas [3.1.0], o sales o profármacos farmacéuticamente aceptables de éstas que tengan actividad antimicrobiana, composiciones farmacéuticas que los contiene, métodos para su uso y métodos para preparar estos compuestos. Reivindicación 1: Un compuesto de fórmula (1), en donde: A es una estructura de fórmula de (2) a (5), en donde la línea punteada del grupo de fórmula (2) representa un doble enlace opcional; n es 0 ó 1; X es N ó CH; Y es N, O ó S; Z es NHC(=O)R1, NHC(=S)R1, CONHR1, NHC(=NCN)R1, NH-het1, O-het1, S-het1 o het2; R1 es H, NH2, NH-alquilo C1-4, alquilo C1-4, alquenilo C2-4, (CH2)mC(=O)-alquilo C1-4, O-alquilo C1-4, S-alquilo C1-4, (CH2)m-cicloalquilo C3-6, CH=CH-arilo, CH=CH-het1, CH2C(=O)arilo o CH2C(=O)-het1; R2 y R3 son independientemente H o F; R4 y R5 son independientemente H, Cl, F, CH3, NH2 u OH; R6 y R7 son independientemente H, F, OH, alquilo C1-4 o heterocicloalquilo C1-4; R8 es H, F, OH, CN, NR10R11, alquilo C1-4, cicloalquilo C3-6, heteroalquilo C1-4, arilo, het1, O-alquilo C1-4, alquilo (C1-4)-OR10, alquilo(C1-4)-NR10R11, O(C=O)-alquilo C1-4, C(=O)-alquilo C1-4, C(=O)OH, C(=O)NR10OR11, C(=NO-alquilo (C1-4)H, C(=NO-alquilo C1-4)alquilo C1-4, C(=O)het1, C(=NO-alquilo C1-4)het1, (CH2)mC(=O)NR10R11, NR10CONR10R11, NR10C(=O)-alquilo C1-4, NR10C(=O)-cicloalquilo C3-6, NR10C(=O)OH, NR10C(=O)H o O-alquilo(C1-4)CONR10R11, siempre que, cuando Y sea O o S, R8 esté presente, además, en donde cada R10 y R11 sean independientemente H, alquilo C1-4, cicloalquilo C3-6, arilo, het1, C(=O)arilo, C(=O)het1, SO2-alquilo C1-4 o SO2NH2; het1 sea un anillo heterocíclico de cinco (5) o seis (6) miembros C-ligado, que contenga de 1 a 4 heteroátomos seleccionados del grupo integrado por oxígeno, azufre y nitrógeno; het2 es un anillo heterocíclico de cinco (5) o seis (6) miembros N- o C-ligado, que contiene de 1 a 4 heteroátomos seleccionados del grupo integrado por oxígeno, azufre y nitrógeno; cada m es independientemente 0, 1 ó 2; y sus sales farmacéuticamente aceptables; con las siguientes condiciones adicionales: cuando Z es NHC(=O)R1 o NHC(=S)R1; n es 1; A es la estructura de fórmula (2); R2, R3, R6 y R7 son H; X es N; Y es N; R8 no sea C(=O)het1; y cuando Z es NHC(=O)R1 o NHC(=S)R1; n es 1; A es la estructura de fórmula (2); R2, R3, R6 y R7 son H; X es N; Y es N; y R8 es NR10R11 o alquilo(C1-4)-NR10R11, R10 y R11 no sean het1, arilo, C(=O)arilo o C(=O)het1.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41773502P | 2002-10-09 | 2002-10-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR041568A1 true AR041568A1 (es) | 2005-05-18 |
Family
ID=32094075
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030103679A AR041568A1 (es) | 2002-10-09 | 2003-10-09 | Derivados de oxazolidinonas biciclicas (3.1.0) con actividad antimicrobiana |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US6875784B2 (es) |
| EP (1) | EP1549641A1 (es) |
| JP (1) | JP2006508934A (es) |
| AR (1) | AR041568A1 (es) |
| AU (1) | AU2003278791A1 (es) |
| BR (1) | BR0315106A (es) |
| CA (1) | CA2501352A1 (es) |
| MX (1) | MXPA05003780A (es) |
| TW (1) | TW200410961A (es) |
| WO (1) | WO2004033451A1 (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1646630A1 (en) * | 2003-07-02 | 2006-04-19 | Merck & Co., Inc. | Oxazolidinone antibiotics and derivatives thereof |
| WO2005005398A2 (en) | 2003-07-02 | 2005-01-20 | Merck & Co., Inc. | Cyclopropyl group substituted oxazolidinone antibiotics and derivatives thereof |
| EP1944288A1 (en) * | 2007-01-09 | 2008-07-16 | Bayer Schering Pharma Aktiengesellschaft | Radiolabelling via fluorination of aziridines |
| BRPI0720884A2 (pt) * | 2007-01-09 | 2014-03-25 | Bayer Schering Pharma Ag | Radiorrotulação por meio de fluoração de aziridinas |
| PE20091682A1 (es) | 2007-12-20 | 2009-12-04 | Astrazeneca Ab | Compuestos de carbamoilo como inhibidores de dgat1 190 |
| WO2009090548A2 (en) * | 2008-01-17 | 2009-07-23 | Glenmark Pharmaceuticals, S.A. | 3-azabicyclo [3.1.0] hexane derivatives as vanilloid receptor ligands |
| KR20110092309A (ko) | 2008-11-20 | 2011-08-17 | 파나세아 바이오테크 리미티드 | 신규 항균제 |
| RU2012102094A (ru) | 2009-06-26 | 2013-08-10 | Панацеа Биотек Лтд. | Новые азабициклогексаны |
| WO2012042539A2 (en) | 2010-09-28 | 2012-04-05 | Panacea Biotec Ltd | Novel bicyclic compounds |
| CN110483522B (zh) | 2014-05-13 | 2022-05-03 | 豪夫迈·罗氏有限公司 | 氘化杂环化合物和其作为成像剂的用途 |
| US10550092B2 (en) | 2015-07-17 | 2020-02-04 | The Global Alliance For Tb Drug Development, Inc. | Substituted phenyloxazolidinones for antimicrobial therapy |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4183857A (en) | 1978-07-06 | 1980-01-15 | Shell Oil Company | 3-Benzyl-3-azabicyclo(3.1.0)hexane-2,4-dione |
| US4235871A (en) | 1978-02-24 | 1980-11-25 | Papahadjopoulos Demetrios P | Method of encapsulating biologically active materials in lipid vesicles |
| US4501728A (en) | 1983-01-06 | 1985-02-26 | Technology Unlimited, Inc. | Masking of liposomes from RES recognition |
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US4837028A (en) | 1986-12-24 | 1989-06-06 | Liposome Technology, Inc. | Liposomes with enhanced circulation time |
| US5011472A (en) | 1988-09-06 | 1991-04-30 | Brown University Research Foundation | Implantable delivery system for biological factors |
| US5023472A (en) * | 1988-09-09 | 1991-06-11 | Texas Instruments Incorporated | Capacitor-driven signal transmission circuit |
| SK283420B6 (sk) | 1992-05-08 | 2003-07-01 | Pharmacia & Upjohn Company | Antimikrobiálne oxazolidinóny obsahujúce substituované diazínové skupiny |
| MY115155A (en) | 1993-09-09 | 2003-04-30 | Upjohn Co | Substituted oxazine and thiazine oxazolidinone antimicrobials. |
| KR960004339A (ko) | 1994-07-02 | 1996-02-23 | 임성기 | 신규한 퀴놀린계 화합물 및 그 의 제조방법 |
| KR100389773B1 (ko) | 1995-02-02 | 2003-10-23 | 다이이찌 세이야꾸 가부시기가이샤 | 헤테로사이클릭화합물 |
| US6124334A (en) * | 1995-02-03 | 2000-09-26 | Pharmacia & Upjohn Company | Hetero-aromatic ring substituted phenyloxazolidinone antimicrobials |
| US6255304B1 (en) * | 1997-05-30 | 2001-07-03 | Pharmacia & Upjohn Company | Oxazolidinone antibacterial agents having a thiocarbonyl functionality |
| JP2002501530A (ja) | 1997-05-30 | 2002-01-15 | ファルマシア・アンド・アップジョン・カンパニー | チオカルボニル官能基を有するオキサゾリジノン抗菌剤 |
| CA2315735A1 (en) | 1998-02-13 | 1999-08-19 | Michael R. Barbachyn | Substituted aminophenyl isoxazoline derivatives useful as antimicrobials |
| CN1311787A (zh) | 1998-06-05 | 2001-09-05 | 阿斯特拉曾尼卡有限公司 | 噁唑烷酮衍生物、其制备方法以及含有它们的药物组合物 |
| TW572757B (en) | 1998-08-24 | 2004-01-21 | Bristol Myers Squibb Co | Novel isoxazolinone antibacterial agents |
| GB9821938D0 (en) | 1998-10-09 | 1998-12-02 | Zeneca Ltd | Chemical compounds |
| CN1221548C (zh) | 1999-12-21 | 2005-10-05 | 法玛西雅厄普约翰美国公司 | 含有砜亚氨基官能团的噁唑烷酮 |
| US6451345B1 (en) * | 2000-01-20 | 2002-09-17 | Eurand Pharmaceuticals Ltd. | Functional coating of linezolid microcapsules for taste-masking and associated formulation for oral administration |
| US6642238B2 (en) * | 2000-02-10 | 2003-11-04 | Pharmacia And Upjohn Company | Oxazolidinone thioamides with piperazine amide substituents |
| GB0009803D0 (en) | 2000-04-25 | 2000-06-07 | Astrazeneca Ab | Chemical compounds |
| PE20020044A1 (es) * | 2000-06-16 | 2002-01-30 | Upjohn Co | Tiazina oxazolidinona |
| PL363960A1 (en) | 2000-07-17 | 2004-11-29 | Ranbaxy Laboratories Limited | Oxazolidinone derivatives as antimicrobials |
| WO2002032857A1 (en) | 2000-10-17 | 2002-04-25 | Pharmacia & Upjohn Company | Methods of producing oxazolidinone compounds |
| ES2256331T3 (es) * | 2000-12-21 | 2006-07-16 | PHARMACIA & UPJOHN COMPANY LLC | Derivados de quinolina antimicrobianos y uso de los mismos para tratar infecciones bacterianas. |
| ATE304536T1 (de) | 2001-04-17 | 2005-09-15 | Merck & Co Inc | Bicyclo(3,1,0)hexan als strukturelement enthaltende oxazolidinon-antibiotika und deren derivate |
| MXPA05001199A (es) * | 2002-07-29 | 2005-05-16 | Ranbaxy Lab Ltd | Derivados de oxazolidinona como antimicrobianos. |
-
2003
- 2003-10-02 US US10/677,451 patent/US6875784B2/en not_active Expired - Fee Related
- 2003-10-03 EP EP03770310A patent/EP1549641A1/en not_active Withdrawn
- 2003-10-03 CA CA002501352A patent/CA2501352A1/en not_active Abandoned
- 2003-10-03 WO PCT/US2003/028560 patent/WO2004033451A1/en active Application Filing
- 2003-10-03 MX MXPA05003780A patent/MXPA05003780A/es unknown
- 2003-10-03 BR BR0315106-9A patent/BR0315106A/pt not_active IP Right Cessation
- 2003-10-03 AU AU2003278791A patent/AU2003278791A1/en not_active Abandoned
- 2003-10-03 JP JP2004543288A patent/JP2006508934A/ja not_active Withdrawn
- 2003-10-09 TW TW092128102A patent/TW200410961A/zh unknown
- 2003-10-09 AR ARP030103679A patent/AR041568A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BR0315106A (pt) | 2005-08-09 |
| JP2006508934A (ja) | 2006-03-16 |
| MXPA05003780A (es) | 2005-06-08 |
| US6875784B2 (en) | 2005-04-05 |
| TW200410961A (en) | 2004-07-01 |
| AU2003278791A1 (en) | 2004-05-04 |
| WO2004033451A1 (en) | 2004-04-22 |
| CA2501352A1 (en) | 2004-04-22 |
| US20040127530A1 (en) | 2004-07-01 |
| EP1549641A1 (en) | 2005-07-06 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2528451T3 (es) | Inhibidores de esfingosina cinasa | |
| CO5601039A2 (es) | Oxazolidinonas de indolona y derivados de las mismas | |
| PE20070218A1 (es) | COMPUESTOS DE CICLOALQUILO AMINO-HIDANTOINA Y USO DE ESTOS PARA LA MODULACION DE ß-SECRETASA | |
| RU2009105826A (ru) | 2,4-ди(ариламино)питимидин-5-карбоксамидные соединения в качестве ингибиторов jak-киназ | |
| AR041568A1 (es) | Derivados de oxazolidinonas biciclicas (3.1.0) con actividad antimicrobiana | |
| AR039222A1 (es) | Derivados de quinolina e isoquinolina, un metodo para su preparacion y su uso como inhibidores de la inflamacion | |
| AR035513A1 (es) | Derivados de tetrahidropiridina, proceso para prepararlos, composiciones farmaceuticas que los contienen, y uso de dichos compuestos en la preparacion de medicamentos | |
| AR054035A1 (es) | Derivados benzodioxano y benzodioxolano y uso de los mismos | |
| PE20090060A1 (es) | ANALOGOS DE IMIDAZOLOPIRIMIDINA Y SU USO COMO INHIBIDORES DE PI3 CINASA Y mTOR | |
| AR053120A1 (es) | Aminopiridinas como inhibidores de beta secretasa | |
| CO5640152A2 (es) | Composiciones farmaceuticas para inhibidores de la proteasa del virus de la hepatitis c | |
| CO5690588A2 (es) | Derivados de 4-tetrazolilo-4 fenilpiperidina para el trata- miento del dolor | |
| AR069510A1 (es) | Arilo y heteroarilo imidazo[1,5-a]pirazinas fusionadas como inhibidores de la fosfodiesterasa 10 | |
| PE20070189A1 (es) | COMPUESTO DE AMINO-5-HETEROARILO (5 MIEMBROS) IMIDAZOLONA Y SU USO PARA MODULACION DE LA ß-SECRETASA | |
| AR025276A1 (es) | El uso de un compuesto que es un derivado de 2-amino-1,3-tiazol, un compuesto que es un derivado de 2-amino-1,3-tiazol, un procedimiento para producirlo y una composicion farmaceutica que lo comprende | |
| AR030230A1 (es) | Derivados de acilfenilurea, procedimiento para su preparacion y su empleo en la preparacion de medicamentos | |
| AR035260A1 (es) | Derivados de piperidina amino sustituidas, composiciones farmaceuticas y el uso de dichos derivados para la preparacion de medicamentos como inhibidores de la gama secretasa, y para el tratamiento de la enfermedad de alzheimer | |
| AR034292A1 (es) | Compuesto de piperazina azoindoloxoacetica sustituido, formulacion farmaceutica que lo comprende y su uso para preparar dicha formulacion | |
| PE20090042A1 (es) | Analogos de ciclopamina | |
| AR049346A1 (es) | 3-amino-1-arilpropil-indoles como inhibidores de reabsorcion de monoaminas | |
| AR033379A1 (es) | Compuestos de difenilurea, procedimiento para su preparacion y composiciones farmaceuticas que los contienen | |
| AR041941A1 (es) | Derivado de 1-aminociclohexano sustituidos en la posicion 4 utilizado como receptor orl1 | |
| AR038401A1 (es) | Derivados de indazol substituidos como agentes terapeuticos | |
| AR034203A1 (es) | Derivados de 1-aril- o 1-alquilsulfonilbenzazol como ligandos de 5-hidroxitriptamina-6, un metodo para su preparacion, composicion farmaceutica y el uso de los mismos para la fabricacion de un medicamento | |
| AR035759A1 (es) | Compuestos acilurea antagonistas de la funcion mpc-1, un procedimiento para su preparacion, composicion farmaceutica y el uso de dichos compuestos para la preparacion de medicamentos |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |