CL2012000042A1 - Compuestos derivados de imidazo[1,2-a]pirazin-7-il; composición farmacéutica que comprende a uno de los compuestos; y uso de uno de los compuestos en la preparación de un medicamento útil para tratar una enfermedad relacionada con el género plasmodium en un sujeto. - Google Patents

Compuestos derivados de imidazo[1,2-a]pirazin-7-il; composición farmacéutica que comprende a uno de los compuestos; y uso de uno de los compuestos en la preparación de un medicamento útil para tratar una enfermedad relacionada con el género plasmodium en un sujeto.

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Publication number
CL2012000042A1
CL2012000042A1 CL2012000042A CL2012000042A CL2012000042A1 CL 2012000042 A1 CL2012000042 A1 CL 2012000042A1 CL 2012000042 A CL2012000042 A CL 2012000042A CL 2012000042 A CL2012000042 A CL 2012000042A CL 2012000042 A1 CL2012000042 A1 CL 2012000042A1
Authority
CL
Chile
Prior art keywords
compounds
alkylocl
alkyl
hydrogen
imidazo
Prior art date
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CL2012000042A
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English (en)
Inventor
K Chatterjee Arnab
Nagle Advait
Wu Tao
Tully David
L Kuhen Kelli
Original Assignee
Novartis Ag
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42727573&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CL2012000042(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of CL2012000042A1 publication Critical patent/CL2012000042A1/es

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    • 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
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/69Boron compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
    • 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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/022Boron compounds without C-boron linkages
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

COMPUESTOS DERIVADOS DE IMIDAZO[1 ,2-AJPIRAZIN-7-II REPRESENTADO POR LA FORMULA LA: EN DONDE RA SE SELECCIONA A PARTIR DE -X3NR7R8, -X30R8, -X35(0)0-2R8, -X3C(0)NR7R8 Y BENCILO OPCIONA!MENTE SUSTITUIDO COMO SE DESCRIBE EN LAS REIVINDICACIONES; R2 SE SELECCIONA ENTRE HIDRÓGENO, ALQUILOCL-6, AMINO, CICLOALQUILC3-8-ALQUILOCO-4, ARIL-C6-10-ALQUILOCO-4, ALQUILOCL -6 HALO-SUSTITUIDO, ALQUILOCL -6 HIDROXI-SUSTITUIDO Y HETEROCICLIL-ALQUILOCO-4; DEFINIDO EN LAS REIVINDICACIONES; EN DONDE DICHO ARILOC6-1 O O HETEROCICLO DE R2 ESTÁ OPCIONALMENTE SUSTITUIDO; O R2 Y R3 JUNTO CON EL ÁTOMO DE CARBONO AL CUAL R2 Y R3 ESTÁN UNIDOS FORMAN UN CICLOALQUILOC3-8; O R2 Y R13 JUNTO CON LOS ÁTOMOS A LOS CUALES P2 Y R13 ESTÁN UNIDOS FORMAN UN ANILLO HETEROCÍCLICO MONO O FUSIONADO COMO SE DEFINE EN LAS REIVINDICACIONES; R4 Y R5 SE SELECCIONA ENTRE HIDRÓGENO Y ALQUILOCL-6; O P4 Y RS JUNTO CON EL ÁTOMO DE CARBONO AL CUAL R4 Y P5 ESTÁN UNIDOS FORMAN UN CICLOALQUILOC3-8; P6 SE SELECCIONA ENTRE ARILOC6-10, CICLOALQUILOC3-8 Y UN ANILLO HETEROCÍCLICO MONO O FUSIONADO DEFINIDO EN LAS REIVINDICACIONES; R9, RIO, Y RL 1, SE SELECCIONA ENTRE HIDRÓGENO Y ALQUILO CI-6; R12 SE SELECCIONA ENTRE HIDRÓGENO Y ALQUILO C1-6; O RL 1 Y R12 COMBINADOS PARA FORMAR UN C(0); O UNA SAL FARMACÉUTICAMENTE ACEPTABLE DEL MISMO, EL RESTO DE LOS RADICALES SE DEFINEN COMO EN EL CAPÍTULO REIVINDICATORIO. ADICIONALMENTE, LA INVENCIÓN RECLAMA COMPOSICIONES FARMACÉUTICAS QUE COMPRENDEN DICHOS COMPUESTOS Y USOS PARA TRATAR O PREVENIR EL PALUDISMO.
CL2012000042A 2009-07-09 2012-01-06 Compuestos derivados de imidazo[1,2-a]pirazin-7-il; composición farmacéutica que comprende a uno de los compuestos; y uso de uno de los compuestos en la preparación de un medicamento útil para tratar una enfermedad relacionada con el género plasmodium en un sujeto. CL2012000042A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US22443309P 2009-07-09 2009-07-09

Publications (1)

Publication Number Publication Date
CL2012000042A1 true CL2012000042A1 (es) 2012-12-21

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ID=42727573

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Application Number Title Priority Date Filing Date
CL2012000042A CL2012000042A1 (es) 2009-07-09 2012-01-06 Compuestos derivados de imidazo[1,2-a]pirazin-7-il; composición farmacéutica que comprende a uno de los compuestos; y uso de uno de los compuestos en la preparación de un medicamento útil para tratar una enfermedad relacionada con el género plasmodium en un sujeto.

Country Status (38)

Country Link
US (3) US8557801B2 (es)
EP (2) EP2737927B1 (es)
JP (1) JP5432376B2 (es)
KR (1) KR101378666B1 (es)
CN (1) CN102471341B (es)
AR (1) AR077463A1 (es)
AU (1) AU2010271247B2 (es)
BR (1) BR112012000413B1 (es)
CA (1) CA2767664C (es)
CL (1) CL2012000042A1 (es)
CO (1) CO6491060A2 (es)
CR (1) CR20120008A (es)
CU (1) CU24155B1 (es)
DK (1) DK2451814T3 (es)
EA (1) EA019655B1 (es)
EC (1) ECSP12011585A (es)
ES (2) ES2477940T3 (es)
GT (1) GT201200004A (es)
HK (1) HK1164304A1 (es)
HN (1) HN2012000023A (es)
HR (1) HRP20140641T1 (es)
IL (1) IL217384A (es)
JO (1) JO3156B1 (es)
MA (1) MA33419B1 (es)
MX (1) MX2012000389A (es)
MY (1) MY157238A (es)
NZ (1) NZ597275A (es)
PE (1) PE20130399A1 (es)
PL (1) PL2451814T3 (es)
PT (1) PT2451814E (es)
SG (1) SG176938A1 (es)
SI (1) SI2451814T1 (es)
SM (1) SMT201400096B (es)
TN (1) TN2011000647A1 (es)
TW (1) TWI421252B (es)
UA (1) UA103930C2 (es)
UY (1) UY32776A (es)
WO (1) WO2011006143A2 (es)

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