AR110055A2 - Modulación de receptores quimiosensoriales y ligandos relacionados con los mismos - Google Patents

Modulación de receptores quimiosensoriales y ligandos relacionados con los mismos

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Publication number
AR110055A2
AR110055A2 ARP170103140A ARP170103140A AR110055A2 AR 110055 A2 AR110055 A2 AR 110055A2 AR P170103140 A ARP170103140 A AR P170103140A AR P170103140 A ARP170103140 A AR P170103140A AR 110055 A2 AR110055 A2 AR 110055A2
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Argentina
Prior art keywords
substituted
alkyl
heteroalkyl
arylalkyl
acyl
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ARP170103140A
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English (en)
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Senomyx Inc
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Publication of AR110055A2 publication Critical patent/AR110055A2/es

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    • 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
    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/78Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/95Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/95Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C07D239/96Two oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/15Six-membered rings
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/74Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors
    • GPHYSICS
    • G16INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16BBIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B15/00ICT specially adapted for analysing two-dimensional or three-dimensional molecular structures, e.g. structural or functional relations or structure alignment
    • G16B15/20Protein or domain folding
    • GPHYSICS
    • G16INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16BBIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B20/00ICT specially adapted for functional genomics or proteomics, e.g. genotype-phenotype associations
    • G16B20/30Detection of binding sites or motifs
    • GPHYSICS
    • G16INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16BBIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B20/00ICT specially adapted for functional genomics or proteomics, e.g. genotype-phenotype associations
    • G16B20/50Mutagenesis
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/72Assays involving receptors, cell surface antigens or cell surface determinants for hormones
    • G01N2333/726G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00Screening for compounds of potential therapeutic value
    • G01N2500/04Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
    • GPHYSICS
    • G16INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16BBIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B15/00ICT specially adapted for analysing two-dimensional or three-dimensional molecular structures, e.g. structural or functional relations or structure alignment
    • GPHYSICS
    • G16INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16BBIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B20/00ICT specially adapted for functional genomics or proteomics, e.g. genotype-phenotype associations

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
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  • Veterinary Medicine (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
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  • Theoretical Computer Science (AREA)
  • Medical Informatics (AREA)
  • Evolutionary Biology (AREA)
  • Bioinformatics & Computational Biology (AREA)
  • Biophysics (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
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  • Proteomics, Peptides & Aminoacids (AREA)
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  • General Physics & Mathematics (AREA)
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Abstract

Reivindicación 1: Un compuesto, excluyendo su uso terapéutico, que tiene la fórmula estructural (1), o un tautómero o sal del mismo, en donde: A es alquilo, alquilo sustituido, halo, -CN, -NO₂, -OR⁹, SR⁹, -NHOR⁹, -NR⁹R¹⁰ o -NOR⁹; B es -N- o -C(R¹²)-; (D)ₙ-G es un resto de fórmula (2) ó (3); E es -NR¹⁷, -N- o -C(R¹⁸)-; H es -C(R³⁵)- o -N-; I es -C(R³⁶) o -N-; J es -C(R³⁷)- o -N-; K es -C(R³⁸)- o -N-; R⁹, R¹⁰, R¹³, R¹⁴ y R¹⁸ son independientemente hidrógeno, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, acilo, acilo sustituido, heteroalquilo, heteroalquilo sustituido, heteroarilo, heteroarilo sustituido, heteroarilalquilo o heteroarilalquilo sustituido; o alternativamente, R⁹ y R¹⁰ o R¹³ y R¹⁴, junto con los átomos a los cuales están unidos, forman un anillo cicloheteroalquilo o cicloheteroalquilo sustituido; R¹² es hidrógeno, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, acilo, acilo sustituido, heteroalquilo, heteroalquilo sustituido, heteroarilo, heteroarilo sustituido, heteroarilalquilo, heteroarilalquilo sustituido, -NR¹³R¹⁴, CN, -OR¹³, -CO₂R¹³ o -CONR¹³R¹⁴; R¹⁷ es hidrógeno, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, acilo, acilo sustituido, heteroalquilo, heteroalquilo sustituido, heteroarilo, heteroarilo sustituido, heteroarilalquilo o heteroarilalquilo sustituido; R³⁵ es hidrógeno, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, acilo, acilo sustituido, halo, cicloalquenilo, cicloalquenilo sustituido, heteroalquilo, heteroalquilo sustituido, heteroarilo, heteroarilo sustituido, heteroarilalquilo, heteroarilalquilo sustituido, -CN, -NO₂, -OR³⁹, -NR³⁹R⁴⁰, -CONR³⁹R⁴⁰ o -CO₂R³⁹; R³⁶ es hidrógeno, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, acilo, acilo sustituido, halo, cicloalquenilo, cicloalquenilo sustituido, heteroalquilo, heteroalquilo sustituido, heteroarilo, heteroarilo sustituido, heteroarilalquilo, heteroarilalquilo sustituido, -CN, -NO₂, -OR⁴¹, NR⁴¹R⁴², -CONR⁴¹R⁴² o -CO₂R⁴¹; R³⁷ es hidrógeno, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, acilo, acilo sustituido, halo, cicloalquenilo, cicloalquenilo sustituido, heteroalquilo, heteroalquilo sustituido, heteroarilo, heteroarilo sustituido, heteroarilalquilo, heteroarilalquilo sustituido, -CN, -NO₂, -OR⁴³, -NR⁴³R⁴⁴, -CONR⁴³R⁴⁴ o -CO₂R⁴³; R³⁸ es hidrógeno, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, acilo, acilo sustituido, halo, cicloalquenilo, cicloalquenilo sustituido, heteroalquilo, heteroalquilo sustituido, heteroarilo, heteroarilo sustituido, heteroarilalquilo, heteroarilalquilo sustituido, -CN, -NO₂, -OR⁴⁵, -NR⁴⁵R⁴⁶, -CONR⁴⁵R⁴⁶, -COR⁴⁵ o -CO₂R⁴⁵; o alternativamente R³⁶ y R³⁷ o R³⁷ y R³⁸, tomados junto con el átomo al cual están unidos, forman un anillo cicloalquilo, cicloalquilo sustituido, cicloheteroalquilo, o cicloheteroalquilo sustituido; R³⁹, R⁴⁰, R⁴¹, R⁴², R⁴³, R⁴⁴, R⁴⁵ y R⁴⁶ son independientemente hidrógeno, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, acilo, acilo sustituido, heteroalquilo, heteroalquilo sustituido, heteroarilo, heteroarilo sustituido, heteroarilalquilo o heteroarilalquilo sustituido, o alternativamente R³⁹ y R⁴⁰, R⁴¹ y R⁴², R⁴³ y R⁴⁴ o R⁴⁵ y R⁴⁶, junto con los átomos a los cuales están unidos, forman un anillo cicloheteroalquilo o cicloheteroalquilo sustituido; con la condición de que, como máximo, dos de H, I, J y K sean -N-.
ARP170103140A 2007-06-08 2017-11-10 Modulación de receptores quimiosensoriales y ligandos relacionados con los mismos AR110055A2 (es)

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US11/760,592 US9603848B2 (en) 2007-06-08 2007-06-08 Modulation of chemosensory receptors and ligands associated therewith

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ARP170103139A AR110054A2 (es) 2007-06-08 2017-11-10 Modulación de receptores quimiosensoriales y ligandos relacionados con los mismos
ARP170103140A AR110055A2 (es) 2007-06-08 2017-11-10 Modulación de receptores quimiosensoriales y ligandos relacionados con los mismos
ARP170103138A AR110053A2 (es) 2007-06-08 2017-11-10 Modulación de receptores quimiosensoriales y ligandos relacionados con los mismos
ARP170103141A AR110056A2 (es) 2007-06-08 2017-11-10 Modulación de receptores quimiosensoriales y ligandos relacionados con los mismos

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ARP170103141A AR110056A2 (es) 2007-06-08 2017-11-10 Modulación de receptores quimiosensoriales y ligandos relacionados con los mismos

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