AR040399A1 - Derivados de metil oxazolidinonas y su uso como agentes antibacterianos - Google Patents
Derivados de metil oxazolidinonas y su uso como agentes antibacterianosInfo
- Publication number
- AR040399A1 AR040399A1 AR20030100689A ARP030100689A AR040399A1 AR 040399 A1 AR040399 A1 AR 040399A1 AR 20030100689 A AR20030100689 A AR 20030100689A AR P030100689 A ARP030100689 A AR P030100689A AR 040399 A1 AR040399 A1 AR 040399A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- group
- alkoxy
- alkoxycarbonyl
- Prior art date
Links
- 239000003242 anti bacterial agent Substances 0.000 title abstract 2
- IZXIZTKNFFYFOF-UHFFFAOYSA-N 2-Oxazolidone Chemical compound O=C1NCCO1 IZXIZTKNFFYFOF-UHFFFAOYSA-N 0.000 title 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 32
- 229910052739 hydrogen Inorganic materials 0.000 abstract 19
- 239000001257 hydrogen Substances 0.000 abstract 18
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 10
- 125000001424 substituent group Chemical group 0.000 abstract 10
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 9
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 7
- 125000005843 halogen group Chemical group 0.000 abstract 7
- -1 hydroxyimino Chemical group 0.000 abstract 7
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 abstract 7
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 6
- 125000004423 acyloxy group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000004758 (C1-C4) alkoxyimino group Chemical group 0.000 abstract 4
- 125000005236 alkanoylamino group Chemical group 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 125000001589 carboacyl group Chemical group 0.000 abstract 4
- 125000004043 oxo group Chemical group O=* 0.000 abstract 4
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004122 cyclic group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000003709 fluoroalkyl group Chemical group 0.000 abstract 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 238000006467 substitution reaction Methods 0.000 abstract 2
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 abstract 1
- 229910014033 C-OH Inorganic materials 0.000 abstract 1
- 229910014570 C—OH Inorganic materials 0.000 abstract 1
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 abstract 1
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 abstract 1
- 125000006350 alkyl thio alkyl group Chemical group 0.000 abstract 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000006340 pentafluoro ethyl group Chemical group FC(F)(F)C(F)(F)* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 102220315634 rs1196125127 Human genes 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- 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
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- 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
- C07D413/06—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 only aliphatic carbon 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (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)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Los compuestos son útiles como agentes antibacterianos; y procesos para su fabricación y composiciones farmacéuticas que los contienen. Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula (1), o una sal aceptable para uso farmacéutico, o un éster hidrolizable in vivo del mismo, donde -N-HET se selecciona entre las estructuras (Ia) a (If) del grupo de fórmulas (2), donde u y v son en forma independiente 0 ó 1; R1 es un grupo alquilo (C1-4); Q se selecciona entre Q1 a Q6, del grupo de fórmulas (3), donde R2 y R3 seleccionados en forma independiente entre H, F, Cl, CF3, OMe, SMe, Me y Et; donde B1 es O ó S; donde T se selecciona entre los grupos en (TA) a (TE) siguientes (donde AR1, AR2, AR2a, AR2b, AR3, AR3a, AR3b, AR4, AR4a, CY1 y CY2 tienen los valores definidos más adelante); (TA) T se selecciona entre los siguientes grupos: (TAa) AR1 ó AR3; ó (TAb) un grupo de fórmula (TAb1) a (TAb6) del grupo de fórmulas (4) donde R6 se selecciona (en forma independiente donde sea apropiado) entre hidrógeno, alquilo (C1-4), (C1-4)alcoxicarbonilo, alcanoílo (C1-4), carbamoílo y ciano; R4 y R5 se seleccionan en forma independiente entre hidrógeno, halo, trifluorometilo, ciano, azido, nitro, alcoxi (C1-4), (C1-4)alquil-S(O)q- (q es 0, 1 ó 2), alcanoílo (C1-4), (C1-4)alcoxicarbonilo, benciloxi-(C1-4)alquilo, (C2-4)alcanoilamino, hidroxiimino, (C1-4)alcoxiimino, -CONRcRv y -NRcRv donde cualquier grupo alquilo (C1-4) contenido en los valores precedentes para R4 y R5 es sustituido opcionalmente por hasta tres sustituyentes seleccionados en forma independiente entre hidroxi ó azido (con ninguno de tales sustituyentes en C1 de un grupo alcoxi, y excluyendo la disustitución geminal), oxo, trifluorometilo, ciano, nitro, alcoxi (C1-4), alcanoiloxi (C2-4), hidroxiimino, (C1-4)alcoxiimino, (C1-4)alquil-S(O)q- (q es 0, 1 ó 2), (C1-4)alquilSO2-NRv-, (C1-4)alcoxicarbonilo, -CONRcRv, y -NRcRv (no en C1 de un grupo alcoxi, y excluyendo la disustitución geminal); donde Rv es hidrógeno ó alquilo (C1-4) y Rc tiene los valores que se definen más adelante; R4 y R5 pueden ser seleccionados además en forma independiente entre alquilo (C1-4) {sustituido opcionalmente por hasta tres sustituyentes seleccionados en forma independiente entre hidroxi ó azido (con ambos de tales sustituyentes excluidos de la disustitución geminal), oxo, trifluorometilo, ciano, nitro, alcoxi (C1-4), alcanoiloxi (C2-4), hidroxiimino, (C1-4)alcoxiimino, (C1-4)alquil-S(O)q- (q es 0, 1 ó 2), (C1-4)alquil-SO2-NRv-, (C1-4)alcoxicarbonilo, -CONRcRv, y -NRcRv (excluyendo la disustitución geminal); donde Rv es hidrógeno ó alquilo (C1-4)}; Rc tiene los valores que se definen más adelante; y donde cualquier grupo alquilo (C1-4) contenido en los sustituyentes optativos inmediatamente precedentes (cuando R4 y R5 son en forma independiente alquilo (C1-4)) es a su vez sustituido opcionalmente por hasta tres sustituyentes seleccionados en forma independiente entre hidroxi (no en C1 de un grupo alcoxi, y excluyendo la disustitución geminal), oxo, trifluorometilo, ciano, nitro, alcoxi (C1-4), alcanoiloxi (C2-4), hidroxiimino, (C1-4)alcoxiimino, (C1-4)alquil-S(O)q- (q es 0, 1 ó 2), (C1-4)alquil-SO2-NRv-, (C1-4)alcoxicarbonilo, -CONRcRv, y -NRcRv (no en C1 de un grupo alcoxi, y excluyendo la disustitución geminal); donde Rv es hidrógeno ó alquilo (C1-4) y Rc es tiene los valores definidos más adelante; ó R4 se selecciona entre uno de los grupos en (TAba) a (TAbc) siguientes, ó (donde sea apropiado) uno de R4 y R5 se selecciona entre la lista precedente de valores de R4 y R5, y el otro se selecciona entre uno de los grupos en (TAba) a (TAbc) siguientes: (TAba) un grupo de la fórmula (5) (Taba1) donde Z0 es hidrógeno ó alquilo (C1-4); X0 y Y0 se seleccionan en forma independiente entre hidrógeno, alquilo (C1-4), alcoxicarbonilo (C1-4), halo, ciano, nitro, (C1-4)alquil-S(O)q- (q es 0, 1 ó 2), RvRwNSO2-, trifluorometilo, pentafluoroetilo, (C1-4)alcanoílo y -CONRvRw [donde Rv es hidrógeno ó alquilo (C1-4); Rw es hidrógeno ó (alquilo C1-4)]; ó uno de X0 y Y0 se selecciona entre la lista precedente de valores de X0 y Y0, y el otro se selecciona entre fenilo, fenilcarbonilo, -S(O)q-fenilo (q es 0, 1 ó 2), N-(fenil)carbamoilo, fenilaminosulfonilo, AR2, (AR2)-CO-, (AR2)-S(O)q- (q es 0, 1 ó 2), N-(AR2)carbamoílo y (AR2)aminosulfonilo; donde cualquier grupo fenilo en (TAba) puede ser sustituido opcionalmente por hasta tres sustituyentes seleccionados en forma independiente entre alquilo (C1-4), ciano, trifluorometilo, nitro, halo y (C1-4)alquilsulfonilo; (TAbb) un acetileno de la fórmula -s-H ó -s-alquilo (C1-4); (TAbc)-X1-Y1-AR2, -X1-Y1-AR2a, -X1-Y1-AR2b, -X1-Y1-AR3, -X1-Y1-AR3a ó -X1-Y1-AR3b; donde X1 es un enlace directo ó -CH(OH)- y Y1 es -(CH2)m-, -(CH2)n-NH-(CH2)m-, -CO-(CH2)m-, -CONH-(CH2)m-, -C(=S)NH-(CH2)m- ó -C(=O)O-(CH2)m; ó donde X1 es -(CH2)n- ó -CH(Me)-(CH2)m- y Y1 es -(CH2)m-NH-(CH2)m-, -CO-(CH2)m-, -CONH-(CH2)m-, -C(=S)NH-(CH2)m-, -C(=O)O-(CH2)m- ó -S(O)q-(CH2)m-; ó donde X1 es-CH2O-, -CH2NH- ó -CH2N(alquilo (C1-4))- y Y1 es -CO-(CH2)m-, -CONH-(CH2)m- ó -C(=S)NH-(CH2)m-; y además Y1 es -SO2- cuando X1 es -CH2NH- ó -CH2N(alquilo (C1-4))-, y Y1 es -(CH2)m- cuando X1 es -CH2O- ó -CH2N(alquilo (C1-4))-; donde n es 1, 2 ó 3; m es 0, 1, 2 ó 3 y q es 0, 1 ó 2; y cuando Y1 es -(CH2)m-NH-(CH2)m- cada m se selecciona en forma independiente entre 0, 1, 2 ó 3; ó (TB) T se selecciona entre halo, formilo ó -NRv1Rw1; ó se selecciona entre los siguientes grupos: (TBa) R10CO-, R10S(O)q- (q es 0, 1 ó 2) ó R10CS- donde R10 se selecciona entre los siguientes grupos: (TBaa) CY1 ó CY2; (TBab) (C1-4)alcoxicarbonilo, trifluorometilo, -NRvRw, etenilo, 2-(C1-4)alquiletenilo, 2-cianoetenilo, 2-ciano-2-(alquil (C1-4))etenilo, 2-nitroetenilo, 2-nitro-2-(alquil (C1-4))etenilo, 2-((C1-4)alquilaminocarbonil)etenilo, 2-((C1-4)alcoxicarbonil)etenilo, 2-(AR1)etenilo ó 2-(AR2)etenilo; ó (TBac) alquilo (C1-4) {sustituido opcionalmente por uno o más grupos cada uno seleccionado en forma independiente entre hidroxi, alcoxi (C1-4), alcanoílo (C1-4), ciano, halo, trifluorometilo, (C1-4)alcoxicarbonilo, -NRvRw, (C1-6)alcanoilamino, (C1-4)alcoxicarbonilamino, N-(C1-4)alquil-N-(C1-6)alcanoilamino, (C1-4)alquil-S(O)q- (q es 0, 1 ó 2), CY1, CY2, AR1, (C1-4)alquil-S(O)pNH- ó (C1-4)alquil-S(O)p-(alquil (C1-4))N- (p es 1 ó 2)}; donde Rv es hidrógeno ó alquilo (C1-4); Rw es hidrógeno ó alquilo (C1-4); Rv1 es hidrógeno, alquilo (C1-4) ó cicloalquilo (C3-8); Rw1 es hidrógeno, alquilo (C1-4), cicloalquilo (C3-8), formilo, (C1-4)alquil-CO- ó (C1-4)alquil-S(O)q- (q es 1 ó 2); ó (TC) T se selecciona entre un grupo de fórmula (TC1) a (TC4) del grupo de fórmulas (6) donde en (TC1): >A3-B3- es >C(Rq)-CH(Rr)- ó >N-CH2- y G es -O-, -S-, -SO-, -SO2- ó >N(Rc); donde en (TC2): m1 es 0, 1 ó 2; >A3-B3- es >C=C(Rr)- ó >C(Rq)-CH(Rr)- ó >N-CH2- y G es -O-, -S-, -SO-, -SO2- ó >N(Rc); donde en (TC3): m1 es 0, 1 ó 2; >A3-B3- es >C(Rq)-CH(Rr)- (salvo cuando Rq y Rr son ambos juntos hidrógeno) ó >N-CH2- y G es -O-, -S-, -SO-, -SO2- ó >N(Rc); donde en (TC4): n1 es 1 ó 2; o1 es 1 ó 2 y n1 + o1 = 2 ó 3; >A3-B3- es >C=C(Rr)- ó >C(Rq)-CH(Rr)- ó >N-CH2- y G es -O-, -S-, -SO-, -SO2- ó >N(Rc); Rp es hidrógeno, alquilo (C1-4) (salvo cuando dicha sustitución es definida por >A3-B3-), hidroxi, alcoxi (C1-4) ó alcanoiloxi (C1-4); donde en (TC1), (TC2) y (TC4); m1, n1 y o1 tienen los valores definidos anteriormente en (TC) >A3-B3- es >N-CH2- y G es >C(R11)(R12), >C=O, >C-OH, >C-alcoxi (C1-4), >C=N-OH, >C=N-alcoxi (C1-4), >C=N-NH-alquilo (C1-4), >C=N-N(alquil (C1-4))2 (donde los últimos dos grupos alquilo (C1-4) precedentes en G están sustituidos opcionalmente por hidroxi) ó >C=N-N-CO-alcoxi (C1-4); donde > representa dos uniones simples; Rq es hidrógeno, hidroxi, halo, alquilo (C1-4) ó alcanoiloxi (C1-4); Rr es (en forma independiente donde sea apropiado) hidrógeno ó alquilo (C1-4); R11 es hidrógeno, alquilo (C1-4), fluoroalquilo (C1-4), (C1-4)alquil-tio-alquilo (C1-4) ó hidroxialquilo (C1-4) y R12 es -[C(Rr)(Rr)]m2-N(Rr)(Rc) donde m2 es 0, 1 ó 2; y, salvo por la sustitución del anillo definida por G, >A3-B3- y Rp, cada sistema de anillos puede ser a su vez opcionalmente sustituido en un átomo de carbono no adyacente a la unión en >A3- por hasta dos sustituyentes seleccionados en forma independiente entre alquilo (C1-4), fluoroalquilo (C1-4) (incluyendo trifluorometilo), (C1-4)alquiltio-alquilo (C1-4), hidroxialquilo (C1-4), amino, aminoalquilo (C1-4), (C1-4)alcanoilamino, (C1-4)alcanoilamino-alquilo (C1-4), carboxi, (C1-4)alcoxicarbonilo, ARc-oximetilo, ARc-tiometilo, oxo (=O) (salvo cuando G es >N-Rc y Rc es un grupo (Rc2) según se ha definido) ó seleccionados en forma independiente entre Rc (si tales sustituyentes no están ya definidos en la presente en (TC)); y además hidroxi ó halo (los dos últimos sustituyentes optativos solamente cuando G es -O- ó -S-); donde ARc se selecciona entre AR1, AR2, AR2a, AR2b, CY1 y CY2 según se define más adelante y Rc se selecciona entre los grupos (Rc1) a (Rc5) según se definen más adelante; ó (TD) T se selecciona entre los siguientes grupos: (TDa) un sistema de anillos espiro bicíclico de fórmula (TDa1) a (TDa9) del grupo de fórmulas (7) donde: (i) el grupo de unión A4 es un átomo de nitrógeno o un átomo de carbono sp3 ó sp2 (con el doble enlace, donde sea apropiado, orientado en cualquier dirección); y (ii) uno de los carbonos del anillo en las posiciones marcadas * y ** se reemplaza por uno de los siguientes grupos -NRc-, >CH-NHRc, >CH-NRc-alquilo (C1-4), >CH-CH2-NHRc, >CH-CH2- NRc-alquilo (C1-4) [donde un enlace con la cadena -CH2- central es opcionalmente mono o disustituido por alquilo (C1-4)]; con la salvedad de que las posiciones marcadas * no se reemplacen por -NH- en el anillo que contiene el enlace A4 cuando A4 es un átomo de nitrógeno ó un átomo de carbono sp2, y que las posiciones marcadas * no se reemplacen por -NH- en el anillo de tres miembros en (TDa1), (TDa4) y (TDa5); y (iii) el sistema de anillo
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US36095702P | 2002-02-28 | 2002-02-28 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR040399A1 true AR040399A1 (es) | 2005-04-06 |
Family
ID=27766248
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
AR20030100689A AR040399A1 (es) | 2002-02-28 | 2003-02-28 | Derivados de metil oxazolidinonas y su uso como agentes antibacterianos |
Country Status (20)
Country | Link |
---|---|
US (1) | US7473699B2 (es) |
EP (1) | EP1497286A1 (es) |
JP (1) | JP2005524661A (es) |
KR (1) | KR20040087329A (es) |
CN (1) | CN1649866A (es) |
AR (1) | AR040399A1 (es) |
AU (1) | AU2003207340A1 (es) |
BR (1) | BR0308056A (es) |
CA (1) | CA2477344A1 (es) |
CO (1) | CO5601011A2 (es) |
IL (1) | IL163688A0 (es) |
IS (1) | IS7427A (es) |
MX (1) | MXPA04008312A (es) |
NO (1) | NO20043950L (es) |
NZ (1) | NZ535592A (es) |
PL (1) | PL372191A1 (es) |
RU (1) | RU2004129276A (es) |
TW (1) | TW200304821A (es) |
WO (1) | WO2003072575A1 (es) |
ZA (1) | ZA200406812B (es) |
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KR101739923B1 (ko) | 2009-02-03 | 2017-05-25 | 머크 샤프 앤드 돔 코포레이션 | R)-3-(4-(2-(2-메틸테트라졸-5-일)피리딘-5-일)-3-플루오로페닐)-5-히드록시메틸 옥사졸리딘-2-온 디히드로겐 포스페이트의 결정형 |
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2003
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- 2003-02-25 MX MXPA04008312A patent/MXPA04008312A/es unknown
- 2003-02-25 RU RU2004129276/04A patent/RU2004129276A/ru not_active Application Discontinuation
- 2003-02-25 CN CNA038091712A patent/CN1649866A/zh active Pending
- 2003-02-25 JP JP2003571281A patent/JP2005524661A/ja active Pending
- 2003-02-25 PL PL03372191A patent/PL372191A1/xx not_active Application Discontinuation
- 2003-02-25 US US10/506,020 patent/US7473699B2/en not_active Expired - Fee Related
- 2003-02-25 AU AU2003207340A patent/AU2003207340A1/en not_active Abandoned
- 2003-02-25 IL IL16368803A patent/IL163688A0/xx unknown
- 2003-02-25 BR BR0308056-0A patent/BR0308056A/pt not_active IP Right Cessation
- 2003-02-25 KR KR10-2004-7013454A patent/KR20040087329A/ko not_active Application Discontinuation
- 2003-02-25 EP EP03704812A patent/EP1497286A1/en not_active Withdrawn
- 2003-02-25 NZ NZ535592A patent/NZ535592A/en unknown
- 2003-02-25 WO PCT/GB2003/000785 patent/WO2003072575A1/en active Application Filing
- 2003-02-27 TW TW092104245A patent/TW200304821A/zh unknown
- 2003-02-28 AR AR20030100689A patent/AR040399A1/es unknown
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2004
- 2004-08-25 CO CO04083221A patent/CO5601011A2/es not_active Application Discontinuation
- 2004-08-26 ZA ZA200406812A patent/ZA200406812B/en unknown
- 2004-08-27 IS IS7427A patent/IS7427A/is unknown
- 2004-09-21 NO NO20043950A patent/NO20043950L/no not_active Application Discontinuation
Also Published As
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CO5601011A2 (es) | 2006-01-31 |
WO2003072575A1 (en) | 2003-09-04 |
NO20043950L (no) | 2004-10-13 |
IS7427A (is) | 2004-08-27 |
BR0308056A (pt) | 2004-12-07 |
KR20040087329A (ko) | 2004-10-13 |
MXPA04008312A (es) | 2004-11-26 |
PL372191A1 (en) | 2005-07-11 |
ZA200406812B (en) | 2005-09-12 |
US20050119292A1 (en) | 2005-06-02 |
EP1497286A1 (en) | 2005-01-19 |
CA2477344A1 (en) | 2003-09-04 |
JP2005524661A (ja) | 2005-08-18 |
IL163688A0 (en) | 2005-12-18 |
US7473699B2 (en) | 2009-01-06 |
CN1649866A (zh) | 2005-08-03 |
RU2004129276A (ru) | 2005-06-10 |
AU2003207340A1 (en) | 2003-09-09 |
NZ535592A (en) | 2006-07-28 |
TW200304821A (en) | 2003-10-16 |
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