AR110053A2 - 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
AR110053A2
AR110053A2 ARP170103138A ARP170103138A AR110053A2 AR 110053 A2 AR110053 A2 AR 110053A2 AR P170103138 A ARP170103138 A AR P170103138A AR P170103138 A ARP170103138 A AR P170103138A AR 110053 A2 AR110053 A2 AR 110053A2
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Argentina
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substituted
alkyl
heteroalkyl
arylalkyl
acyl
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ARP170103138A
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English (en)
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Senomyx Inc
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Publication of AR110053A2 publication Critical patent/AR110053A2/es

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C07D239/96—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/15—Six-membered 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
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/74—Chemical 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
    • G—PHYSICS
    • G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16B—BIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B15/00—ICT specially adapted for analysing two-dimensional or three-dimensional molecular structures, e.g. structural or functional relations or structure alignment
    • G16B15/20—Protein or domain folding
    • G—PHYSICS
    • G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16B—BIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B20/00—ICT specially adapted for functional genomics or proteomics, e.g. genotype-phenotype associations
    • G16B20/30—Detection of binding sites or motifs
    • G—PHYSICS
    • G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16B—BIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B20/00—ICT specially adapted for functional genomics or proteomics, e.g. genotype-phenotype associations
    • G16B20/50—Mutagenesis
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/72—Assays involving receptors, cell surface antigens or cell surface determinants for hormones
    • G01N2333/726—G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/04—Screening 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)
    • G—PHYSICS
    • G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16B—BIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B15/00—ICT specially adapted for analysing two-dimensional or three-dimensional molecular structures, e.g. structural or functional relations or structure alignment
    • G—PHYSICS
    • G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16B—BIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B20/00—ICT specially adapted for functional genomics or proteomics, e.g. genotype-phenotype associations

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  • Chemical & Material Sciences (AREA)
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  • Urology & Nephrology (AREA)
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Abstract

La presente incluye métodos para identificar modificadores de receptores quimiosensoriales y sus ligandos, por ejemplo, mediante la determinación de si una entidad de ensayo es adecuada para interactuar con uno o mas sitios de interacción dentro de los dominios Venus atrapamoscas de los receptores quimiosensoriales, y modificadores capaces de modular receptores quimiosensoriales y sus ligandos. La presente también incluye modificadores de receptores quimiosensoriales y sus ligandos que tienen la fórmula (1), sus subgéneros, y compuestos específicos. Más aún, la presente incluye composiciones ingeribles que comprenden los modificadores de receptores quimiosensoriales y sus ligandos y métodos de utilización de los modificadores de receptores quimiosensoriales y sus ligandos para mejorar el sabor dulce de una composición ingerible o para tratar una afección asociada con un receptor quimiosensorial. Además, la presente incluye procesos para preparar los modificadores de receptores quimiosensoriales y sus ligandos. Reivindicación 1: Un compuesto, excluído su uso terapéutico, que tiene la fórmula estructural (2), o un tautómero o sal del mismo, en donde: (D)ₙ-G es un compuesto de fórmula (3) ó (4); A es alquilo, alquilo sustituido, halo, -CN, -NO₂, -OR⁹, SR⁹, -NHOR⁹, -NR⁹R¹⁰ o -NOR⁹; B es -N- o -C(R¹²)-; 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; E es -NR¹⁷, -N- o -C(R¹⁸)-; Y forma un enlace simple con W o Z y un enlace doble con el otro de W o Z; W es -C(R²⁴)-, -S-, -N-, -N(R²⁵)- o -O-; Y es -C(R²⁶)- o -N-; Z es -C(R²⁷)-, -S-, -N-, -N(R²⁸)- o -O-; 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; 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; R²⁴ es hidrógeno, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, acilo, acilo sustituido, heteroalquilo, heteroalquilo sustituido, heteroarilo, heteroarilo sustituido, heteroarilalquilo, heteroarilalquilo sustituido, -CN, -NO₂, -OR²⁹ o -NR²⁹R³⁰; R²⁶ es hidrógeno, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, acilo, acilo sustituido, heteroalquilo, heteroalquilo sustituido, heteroarilo, heteroarilalquilo sustituido, halo, -CN, -NO₂, -OR³¹, -OCOR³¹, -NR³¹R³², -CONR³¹R³² o -CO₂R³¹; R²⁷ es hidrógeno, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, acilo, acilo sustituido, heteroalquilo, heteroalquilo sustituido, heteroarilo, heteroarilo sustituido, heteroarilalquilo, heteroarilalquilo sustituido, halo, -CN, -NO₂, -OR³³ o -NR³³R³⁴, o alternativamente R²⁴ y R²⁶ o R²⁶ y R²⁷ junto con los átomos a los cuales están unidos forman un anillo cicloalquilo, cicloalquilo sustituido, cicloheteroalquilo o cicloheteroalquilo sustituido; R²⁵ y R²⁸ 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; y R²⁹, R³⁰, R³¹, R³², R³³ y R³⁴ 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 R²⁹ y R³⁰, R³¹ y R³² o R³³ y R³⁴ junto con los átomos a los cuales están unidos forman un anillo cicloheteroalquilo o cicloheteroalquilo sustituido; y con las siguientes condiciones: cuando W es -O-, -S- o -NR²⁵, entonces Z es -C(R²⁷) o -N-; cuando Z es -O-, -S- o -NR²⁸, entonces W es -C(R²⁴) o -N-; y cuando B es -N-, A no es halo.
ARP170103138A 2007-06-08 2017-11-10 Modulación de receptores quimiosensoriales y ligandos relacionados con los mismos AR110053A2 (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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ARP170103141A AR110056A2 (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
ARP170103139A AR110054A2 (es) 2007-06-08 2017-11-10 Modulación de receptores quimiosensoriales y ligandos relacionados con los mismos
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ARP170103140A AR110055A2 (es) 2007-06-08 2017-11-10 Modulación de receptores quimiosensoriales y ligandos relacionados con los mismos
ARP170103139A AR110054A2 (es) 2007-06-08 2017-11-10 Modulación de receptores quimiosensoriales y ligandos relacionados con los mismos

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