AR064148A1 - Derivados de quinolina antibacterial - Google Patents

Derivados de quinolina antibacterial

Info

Publication number
AR064148A1
AR064148A1 ARP070105441A ARP070105441A AR064148A1 AR 064148 A1 AR064148 A1 AR 064148A1 AR P070105441 A ARP070105441 A AR P070105441A AR P070105441 A ARP070105441 A AR P070105441A AR 064148 A1 AR064148 A1 AR 064148A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
mono
het
optionally substituted
Prior art date
Application number
ARP070105441A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38048032&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR064148(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR064148A1 publication Critical patent/AR064148A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • A61P31/06Antibacterial agents for tuberculosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • C07D215/227Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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 only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged 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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Los compuestos reivindicados son utiles para el tratamiento de una infeccion bacteriana. Incluso, se reivindica una composicion que comprende un vehículo farmacéuticamente aceptable y, como ingrediente activo, una cantidad terapéuticamente efectiva de los compuestos reivindicados, el uso de los compuestos o composiciones reivindicadas para la preparacion de un medicamento para el tratamiento de una infeccion bacteriana y un proceso para preparar los compuestos reivindicados. Reivindicacion 1: Un compuesto de formula (1a) o (1b) que incluye cualquier forma estereoquímicamente isomérica del mismo, en donde p es un numero entero igual a 1, 2, 3 o 4; q es un numero entero igual a cero, 1, 2, 3 o 4; R1 es hidrogeno, ciano, formilo, carboxilo, halo, alquilo, alquenilo C2-6, alquinilo C2-6, haloalquilo, hidroxi, alquiloxi, alquiltio, alquiltioalquilo, -C=N-OR11, amino, mono o di(alquil)amino, aminoalquilo, mono o di(alquil)aminoalquilo, alquilcarboniloaminoalquilo, aminocarbonilo, mono o di(alquil)aminocarbonilo, arilalquilo, arilcarbonilo, R5aR4aNalquilo, di(aril)alquilo, arilo, R5aR4aN-, R5aR4aN-C(=O)-, o Het; R2 es hidrogeno, alquiloxi, arilo, ariloxi, hidroxi, mercapto, alquiloxialquiloxi, alquiltio, mono o di(alquilo)amino, pirrolidino o un radical de formula (2) en donde Y es CH2, O, S, NH o N-alquilo; R3 es alquilo, arilalquilo, aril-O-alquilo, aril-alquil-O-alquilo, arilo, aril-arilo, Het, Het-alquilo, Het-O-alquilo, Het-alquil-O-alquilo o un radical de formula (3); R4 es H o alquilo; R5 es -C(=NH)-NH2; arilalquilo; Het-alquilo; mono o dialquilaminoalquilo; biciclo[2.2.2]heptilo; het; o arilo; o R4 y R5 junto con el átomo de nitrogeno al que se encuentran unidos, forman un radical seleccionado del grupo que comprende azetidinilo; 2,3-dihidroisoindol-1-ilo; tiazolidin-3-ilo; 1 2,3,6-tetrahidropiridilo; hexahidro-1H-azepinilo; hexahidro-1H-1,4-diazepinilo; hexahidro-1,4-oxazepinilo; 1 ,2,3,4-tetrahidroisoquinolin-2-ilo; 2,5- diazabiciclo[2.2.1]heptilo; 1,1-dioxido-tiomorfolinilo; cada radical opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes, cada sustituyente seleccionado en forma independiente de alquilo, haloalquilo, alquilcarbonilo, halo, arilalquilo, hidroxi, alquiloxi, amino, mono o dialquilamino, mono o dialquilaminoalquilo, alquiltio, alquiloxialquilo, alquiltioalquilo, arilo, piperidinilo opcionalmente sustituido con alquilo, pirrolidinilo opcionalmente sustituido con arilalquilo, piridilo o pirimidinilo; o R4 y R5 junto con el átomo de nitrogeno al que se encuentran unidos, forman un radical seleccionado del grupo que comprende piperidinilo o piperazinilo, cada uno sustituido con arilo, alquilcarbonilo, piperidinilo o pirrolidinilo opcionalmente sustituido con arilalquilo; R4a y R5a junto con el átomo de nitrogeno al que se encuentran unidos, forman un radical seleccionado del grupo que comprende pirrolidino, piperidino, piperazino, morfolino, 4-tiomorfolino, 2,3- dihidroisoindol-1-ilo, tiazolidin-3-ilo, 1,2,3,6-tetrahidropiridilo, hexahidro-1H-azepinilo, hexahidro-1H-1,4-diazepinilo, hexahidro-1,4-oxazepinilo, 1,2,3,4-tetrahidroisoquinolin-2-ilo, pirrolinilo, pirrolilo, imidazolidinilo, pirazolidinilo, 2- imidazolinilo, 2-pirazolinilo, imidazolilo, pirazolilo, triazolilo, piridinilo, piridazinilo, pirimidinilo, pirazinilo y triazinilo, cada radical opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes, cada sustituyente seleccionado en forma independiente de alquilo, haloalquilo, halo, arilalquilo, hidroxi, alquiloxi, amino, mono o dialquiloamino, alquiltio, alquiltioalquilo, arilo, piridilo o pirimidinilo; R6 es arilo1 o Het; R7 es hidrogeno, halo, alquilo, arilo o Het; R8 es hidrogeno o alquilo; R9 es oxo; o R8 y R9 forman juntos el radical -CH=CH-N=; R11 es hidrogeno o alquilo; arilo es un homociclo seleccionado de fenilo, naftilo, acenaftilo o tetrahidronaftilo, cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes, cada sustituyente seleccionado en forma independiente de hidroxi, halo, ciano, nitro, amino, mono o dialquiloamino, alquilo, alquenilo C2-6 opcionalmente sustituido con fenilo, haloalquilo, alquiloxi, haloalquiloxi, carboxilo, alquiloxicarbonilo, aminocarbonilo, morfolinilo o mono o dialquilaminocarbonilo; arilo1 es un homociclo seleccionado de fenilo, naftilo, acenaftilo o tetrahidronaftilo, cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes, cada sustituyente seleccionado en forma independiente de hidroxi, halo, ciano, nitro, amino, mono o dialquilamino, alquilo, haloalquilo, alquiloxi, alquiltio, haloalquiloxi, carboxilo, alquiloxicarbonilo, aminocarbonilo, morfolinilo, Het o mono o dialquilaminocarbonilo; Het es un heterociclo monocíclico seleccionado de N-fenoxipiperidinilo, piperidinilo, piperazina, pirrolilo, pirazolilo, imidazolilo, furanilo, tienilo, oxazolilo, isoxazolilo, tiazolilo, isotiazolilo, piridinilo, pirimidinilo, pirazinilo o piridazinilo; o un heterociclo bicíclico seleccionado de quinolinilo, quinoxalinilo, indolilo, bencimidazolilo, benzoxazolilo, bencisoxazolilo, benzotiazolilo, bencisotiazolilo, benzofuranilo, benzotienilo, 2,3-dihidrobenzo[1,4]dioxinilo o benzo[1,3]dioxolilo; cada heterociclo monocíclico y bicíclico opcionalmente sustituido con 1, 2 o 3 sustituyentes, cada sustituyente seleccionado en forma independiente de halo, hidroxi, alquilo o alquiloxi; con la condicion que R5 no sea bencilo; un N-oxido del mismo, una sal farmacéuticamente aceptable del mismo o un solvato del mismo.
ARP070105441A 2006-12-06 2007-12-05 Derivados de quinolina antibacterial AR064148A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP06125545 2006-12-06

Publications (1)

Publication Number Publication Date
AR064148A1 true AR064148A1 (es) 2009-03-18

Family

ID=38048032

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070105441A AR064148A1 (es) 2006-12-06 2007-12-05 Derivados de quinolina antibacterial

Country Status (34)

Country Link
US (1) US20100063026A1 (es)
EP (1) EP2099761B1 (es)
JP (1) JP5466013B2 (es)
KR (1) KR101553600B1 (es)
CN (1) CN101547906B (es)
AP (1) AP2477A (es)
AR (1) AR064148A1 (es)
AT (1) ATE486061T1 (es)
AU (1) AU2007328892B2 (es)
BR (1) BRPI0719915A2 (es)
CA (1) CA2668558C (es)
CL (1) CL2007003518A1 (es)
CY (1) CY1112027T1 (es)
DE (1) DE602007010182D1 (es)
DK (1) DK2099761T3 (es)
EA (1) EA016760B1 (es)
ES (1) ES2354755T3 (es)
HK (1) HK1137437A1 (es)
HR (1) HRP20110024T1 (es)
IL (1) IL199082A (es)
JO (1) JO2683B1 (es)
ME (1) ME01230B (es)
MX (1) MX2009005906A (es)
MY (1) MY145940A (es)
NO (1) NO341984B1 (es)
NZ (1) NZ576862A (es)
PL (1) PL2099761T3 (es)
PT (1) PT2099761E (es)
RS (1) RS51582B (es)
SI (1) SI2099761T1 (es)
TW (1) TWI487526B (es)
UA (1) UA101307C2 (es)
WO (1) WO2008068272A2 (es)
ZA (1) ZA200903949B (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO2970B1 (en) * 2006-12-06 2016-03-15 جانسين فارماسوتيكا ان. في Quinoline antibacterial derivatives
MX355050B (es) 2012-04-27 2018-04-02 Janssen Pharmaceutica Nv Derivados de quinolina antibacterianos.
CN104254528B (zh) 2012-04-27 2017-06-06 詹森药业有限公司 抗菌的喹啉衍生物
AU2023235233A1 (en) 2022-03-14 2024-09-12 Slap Pharmaceuticals Llc Multicyclic compounds

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0936866A4 (en) * 1996-10-28 2001-04-11 Dept Of The Army Us Government COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATING ANTIBIOTIC RESIST INFECTIONS
JP4484703B2 (ja) * 2002-07-25 2010-06-16 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ キノリン誘導体およびミコバクテリア抑制剤としてのそれらの使用
EA011277B1 (ru) * 2004-01-23 2009-02-27 Янссен Фармацевтика Н.В. Производные хинолина и их применение в качестве ингибиторов микобактерий
WO2005075428A1 (en) * 2004-01-29 2005-08-18 Janssen Pharmaceutica N.V. Quinoline derivatives for use as mycobacterial inhibitors
KR20130024969A (ko) * 2004-05-28 2013-03-08 얀센 파마슈티카 엔.브이. 약물 내성 마이코박테리아 질환 치료를 위한 치환된 퀴놀린 유도체의 용도
EE05394B1 (et) * 2004-12-24 2011-04-15 Janssen Pharmaceutica N.V. Kinoliinihendid kasutamiseks latentse tuberkuloosi ravis
EE05697B1 (et) * 2005-06-08 2014-02-17 Janssen Pharmaceutica N.V. Kinoliini derivaadid kui antibakteriaalsed toimeained
JO2752B1 (en) * 2005-06-28 2014-03-15 شركة جانسين فارماسوتيكا ان. في Quinoline derivatives acting as antibacterial agents
RS55601B1 (sr) * 2005-06-28 2017-06-30 Janssen Pharmaceutica Nv Derivati kvinolina kao antibakterijski agensi
JO2837B1 (en) * 2005-08-03 2014-09-15 جانسن فارمسيتكا ان في Quinoline derivatives acting as antibacterial agents
JO2952B1 (en) * 2005-08-03 2016-03-15 جانسين فارماسوتيكا ان. في Quinoline derivatives acting as antibacterial agents
JO2855B1 (en) * 2005-08-03 2015-03-15 شركة جانسين فارماسوتيكا ان. في Quinoline derivatives acting as antibacterial agents

Also Published As

Publication number Publication date
KR20090102778A (ko) 2009-09-30
IL199082A (en) 2014-04-30
JO2683B1 (en) 2013-03-03
CL2007003518A1 (es) 2008-07-11
AU2007328892A1 (en) 2008-06-12
MY145940A (en) 2012-05-31
EP2099761A2 (en) 2009-09-16
HRP20110024T1 (hr) 2011-04-30
TWI487526B (zh) 2015-06-11
EA200970537A1 (ru) 2009-10-30
ES2354755T3 (es) 2011-03-17
DK2099761T3 (da) 2011-02-07
PT2099761E (pt) 2011-01-18
NO341984B1 (no) 2018-03-05
EA016760B1 (ru) 2012-07-30
WO2008068272A2 (en) 2008-06-12
CN101547906A (zh) 2009-09-30
HK1137437A1 (en) 2010-07-30
SI2099761T1 (sl) 2011-02-28
TW200831095A (en) 2008-08-01
WO2008068272A3 (en) 2008-07-24
CY1112027T1 (el) 2015-11-04
MX2009005906A (es) 2009-06-16
AU2007328892B2 (en) 2013-05-16
CA2668558A1 (en) 2008-06-12
UA101307C2 (ru) 2013-03-25
ME01230B (me) 2013-03-20
KR101553600B1 (ko) 2015-09-16
DE602007010182D1 (de) 2010-12-09
ZA200903949B (en) 2010-08-25
NZ576862A (en) 2012-01-12
PL2099761T3 (pl) 2011-04-29
JP5466013B2 (ja) 2014-04-09
EP2099761B1 (en) 2010-10-27
NO20092541L (no) 2009-09-02
RS51582B (en) 2011-08-31
AP2009004873A0 (en) 2009-06-30
BRPI0719915A2 (pt) 2014-03-04
AP2477A (en) 2012-09-27
CN101547906B (zh) 2014-08-06
JP2010511672A (ja) 2010-04-15
US20100063026A1 (en) 2010-03-11
CA2668558C (en) 2016-06-07
ATE486061T1 (de) 2010-11-15

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