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AR095601A1 - Diazilhidrazinas que contienen boro - Google Patents

Diazilhidrazinas que contienen boro

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Publication number
AR095601A1
AR095601A1 ARP140101226A ARP140101226A AR095601A1 AR 095601 A1 AR095601 A1 AR 095601A1 AR P140101226 A ARP140101226 A AR P140101226A AR P140101226 A ARP140101226 A AR P140101226A AR 095601 A1 AR095601 A1 AR 095601A1
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Argentina
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group
optionally substituted
alkyl
hydrogen
hydroxy
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ARP140101226A
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Intrexon Corp
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    • 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
    • C07F5/025Boronic and borinic acid compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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
    • C07F5/027Organoboranes and organoborohydrides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/0803Compounds with Si-C or Si-Si linkages
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N55/00Biocides, pest repellants or attractants, or plant growth regulators, containing organic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen and sulfur
    • A01N55/08Biocides, pest repellants or attractants, or plant growth regulators, containing organic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen and sulfur containing boron
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/69Boron compounds
    • 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
    • C07F5/04Esters of boric acids

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)

Abstract

Es útil para aplicaciones tales como la terapia génica, el tratamiento de enfermedades, la producción a gran escala de proteínas y anticuerpos, los ensayos de cribado basados en células, la genómica funcional, la proteómica, la metabolómica y la regulación de los rasgos en organismos transgénicos, donde el control de gen los niveles de expresión es deseable. Reivindicación 1: Un compuesto que tiene la fórmula (1), donde: R¹ y R² se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno, alquilo opcionalmente sustituido y haloalquilo; o R¹ y R² tomados en conjunto con el átomo de carbono al cual están unidos forman un cicloalquilo de 4 a 8 miembros; R³ se selecciona del grupo que consiste de hidrógeno, alquilo opcionalmente sustituido, haloalquilo, cicloalquilo opcionalmente sustituido, alquenilo opcionalmente sustituido, arilo opcionalmente sustituido y heteroarilo opcionalmente sustituido; R⁴ se selecciona del grupo que consiste de los restos del grupo de fórmulas (2); X¹ se selecciona del grupo que consiste de -O- y -N(R⁸ᵃ)-; Y¹ es -(CR⁹ᵃR⁹ᵇ)ₘ-; Z¹ se selecciona del grupo que consiste de -O- y -N(R⁸ᵇ)- o Z¹ está ausente; R⁶ᵃ se selecciona del grupo que consiste de hidroxi, alquilo y alcoxi; o R⁶ᵃ forma un aducto de hidroxi ácido o un aducto de amino ácido; R⁷ᵃ y R⁷ᵇ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno, halo, nitro, ciano, hidroxi, amino, alquilo opcionalmente sustituido, haloalquilo, hidroxialquilo, alcoxi y alquiltio; R⁷ᵃ y R⁷ᵇ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno, halo, nitro, ciano, hidroxi, amino, alquilo opcionalmente sustituido, haloalquilo, hidroxialquilo, alcoxi y alquiltio; R⁸ᵃ y R⁸ᵇ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno y alquilo; R⁹ᵃ y R⁹ᵇ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno y alquilo; m es 1, 2, 3 ó 4; X² se selecciona del grupo que consiste de -O- y -N(R⁸ᶜ)-; Y² es -(CR⁹ᶜR⁹ᵈ)ₙ-; Z² se selecciona del grupo que consiste de -O- y -N(R⁸ᵈ)- o Z² está ausente; R⁶ᵇ se selecciona del grupo que consiste de hidroxi, alquilo y alcoxi; o R⁶ᵇ forma un aducto de hidroxi ácido o un aducto de amino ácido; R⁷ᶜ y R⁷ᵈ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno, halo, nitro, ciano, hidroxi, amino, alquilo opcionalmente sustituido, haloalquilo, hidroxialquilo, alcoxi y alquiltio; R⁸ᶜ y R⁸ᵈ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno y alquilo; R⁹ᶜ y R⁹ᵈ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno y alquilo; n es 1, 2, 3 ó 4; X se selecciona del grupo que consiste de -O- y -N(R⁸ᵉ)-; R⁶ᶜ se selecciona del grupo que consiste de hidroxi, alquilo y alcoxi; o R⁶ᶜ forma un aducto de hidroxi ácido o un aducto de amino ácido; R⁷ᵉ y R⁷ᶠ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno, halo, nitro, ciano, hidroxi, amino, alquilo opcionalmente sustituido, haloalquilo, hidroxialquilo, alcoxi y alquiltio; R⁸ᵉ se selecciona del grupo que consiste de hidrógeno y alquilo; R⁶ᵈ se selecciona del grupo que consiste de hidroxi, alquilo y alcoxi; o R⁶ᵈ forma un aducto de hidroxi ácido o un aducto de amino ácido; R⁶ᶠ se selecciona del grupo que consiste de hidrógeno, alquilo, amino e hidroxi; X⁵ se selecciona del grupo que consiste de -O- y -N(R⁸ᵏ)-; R⁷ᵍ y R⁷ʰ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno, halo, nitro, ciano, hidroxi, amino, alquilo opcionalmente sustituido, haloalquilo, hidroxialquilo, alcoxi y alquiltio; R⁸ᵏ se selecciona del grupo que consiste de hidrógeno y alquilo; X⁶ se selecciona del grupo que consiste de -O- y -N(R⁸ˡ)-; X⁷ se selecciona del grupo que consiste de -O- y -N(R⁸ⁿ)-; R⁸ˡ se selecciona del grupo que consiste de hidrógeno y alquilo; R⁸ᵐ se selecciona del grupo que consiste de hidrógeno y alquilo; R⁸ⁿ se selecciona del grupo que consiste de hidrógeno y alquilo; R¹⁰ᵃ se selecciona del grupo que consiste de hidrógeno y -(CR¹¹ᵃR¹¹ᵇ)ₒ-B(R¹²ᵃ)(R¹²ᵇ); y R¹⁰ᵇ, R¹⁰ᶜ, y R¹⁰ᵈ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno, halo, nitro, ciano, hidroxi, amino, -N(H)CHO, -N(H)CN, alquilo opcionalmente sustituido, haloalquilo, alcoxialquilo, hidroxialquilo, arilalquilo, cicloalquilo opcionalmente sustituido, alquenilo opcionalmente sustituido, alquinilo opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterociclo opcionalmente sustituido, alcoxi, ariloxi, arilalquiloxi, alquiltio, heteroalquilo, carboxamido, sulfonamido, -COR¹⁶, -SO₂R¹⁷, -N(R¹⁸)COR¹⁹, -N(R¹⁸)SO₂R²⁰ o N(R¹⁸)C=N(R²¹)-amino; o R¹⁰ᵇ se selecciona del grupo que consiste de hidrógeno, halo, nitro, ciano, hidroxi, -N(H)CHO, -N(H)CN, amino, alquilo opcionalmente sustituido, haloalquilo, hidroxialquilo, arilalquilo, cicloalquilo opcionalmente sustituido, alquenilo opcionalmente sustituido, alquinilo opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterociclo opcionalmente sustituido, alcoxi, ariloxi, arilalquiloxi, alquiltio, heteroalquilo, carboxamido, sulfonamido, -COR¹⁶, -SO₂R¹⁷, -N(R¹⁸)COR¹⁹, -N(R¹⁸)SO₂R²⁰ o -N(R¹⁸)C=N(R²¹)-amino; o R¹⁰ᶜ y R¹⁰ᵈ tomados en conjunto con dos átomos de carbono adyacentes forman un grupo cicloalquilo opcionalmente sustituido fusionado, heterociclo opcionalmente sustituido o heteroarilo opcionalmente sustituido; R¹¹ᵃ y R¹¹ᵇ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno y alquilo; R¹²ᵃ y R¹²ᵇ se seleccionan del grupo que consiste de hidroxi y alcoxi; o R¹²ᵃ y R¹²ᵇ tomados en conjunto forman una unión -O(CR¹³ᵃR¹³ᵇ)ₚO-; o -B(R¹²ᵃ)(R¹²ᵇ) forma un aducto de flúor; R¹³ᵃ y R¹³ᵇ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno y alquilo C₁₋₄; o es 0, 1, 2, 3, 4 ó 5; p es 2, 3 ó 4; R⁵ es un resto R⁴-3, R⁴-4, R⁴-8, R⁴-9 o R⁴-10 del grupo de fórmulas (2); o R⁵ se selecciona del grupo que consiste de los compuestos del grupo de fórmulas (3); X³ se selecciona del grupo que consiste de -O- y -N(R⁸ᶠ)-; Y³ es -(CR⁹ᵉR⁹ᶠ)q-; Z³ se selecciona del grupo que consiste de -O- y -N(R⁸ᵍ)- o Z³ está ausente; R⁶ᵉ se selecciona del grupo que consiste de hidroxi y alquilo; o R⁶ᵉ forma un aducto de hidroxi ácido o un aducto de amino ácido; R⁷ⁱ y R⁷ʲ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno, halo, nitro, ciano, hidroxi, amino, alquilo opcionalmente sustituido, haloalquilo, hidroxialquilo, alcoxi y alquiltio; R⁸ᶠ y R⁸ᵍ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno y alquilo; R⁹ᵉ y R⁹ᶠ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno y alquilo; q es 1, 2, 3 ó 4; X⁴ se selecciona del grupo que consiste de -O- y -N(R⁸ʰ)-; Y⁴ es -(CR⁹ᵍR⁹ʰ)ʳ-; Z⁴ se selecciona del grupo que consiste de -O- y -N(R⁸ⁱ)- o Z⁴ está ausente; R⁶ᵍ se selecciona del grupo que consiste de hidroxi y alquilo; o R⁶ᵍ forma un aducto de hidroxi ácido o un aducto de amino ácido; R⁷ᵏ y R⁷ˡ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno, halo, nitro, ciano, hidroxi, amino, alquilo opcionalmente sustituido, haloalquilo, hidroxialquilo, alcoxi y alquiltio; R⁸ʰ y R⁸ⁱ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno y alquilo; R⁹ᵍ y R⁹ʰ se seleccionan -cada uno en forma independiente- del grupo que consiste de hidrógeno y alquilo; r es 1, 2, 3 ó 4; R¹⁰ᵉ se selecciona del grupo que consiste de hidrógeno y -(CR¹¹ᶜR¹¹ᵈ)ₛ-B(R¹²ᶜ)(R¹²ᵈ); y R¹⁰ᶠ, R¹⁰ᵍ, y R¹⁰ʰ se seleccionan -de manera independiente- del grupo que consiste de hidrógeno, halo, nitro, ciano, hidroxi, amino, -N(H)CHO, -N(H)CN, alquilo opcionalmente sustituido, haloalquilo, hidroxialquilo, arilalquilo, cicloalquilo opcionalmente sustituido, alquenilo opcionalmente sustituido, alquinilo opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterociclo opcionalmente sustituido, alcoxi, ariloxi, arilalquiloxi, alquiltio, carboxamido, sulfonamido, -COR¹⁶, -SO₂R¹⁷, -N(R¹⁸)COR¹⁹, -N(R¹⁸)SO₂R²⁰ o -N(R¹⁸)C=N(R²¹)-amino; o R¹⁰ᶠ se selecciona del grupo que consiste de hidrógeno, halo, nitro, ciano, hidroxi, amino, -N(H)CHO, -N(H)CN, alqu
ARP140101226A 2013-03-15 2014-03-17 Diazilhidrazinas que contienen boro AR095601A1 (es)

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US (4) US9127024B2 (es)
EP (1) EP2970106B1 (es)
JP (1) JP6379173B2 (es)
KR (1) KR20150129034A (es)
CN (1) CN105283439B (es)
AR (1) AR095601A1 (es)
AU (2) AU2014227571B2 (es)
BR (1) BR112015022994A2 (es)
CA (1) CA2904436C (es)
DK (1) DK2970106T3 (es)
ES (1) ES2683329T3 (es)
IL (1) IL241119B (es)
MX (1) MX361717B (es)
NZ (1) NZ712167A (es)
PH (1) PH12015502099A1 (es)
RU (1) RU2637946C2 (es)
SG (1) SG11201506875YA (es)
TW (1) TWI636986B (es)
WO (1) WO2014144380A1 (es)
ZA (1) ZA201506985B (es)

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