AR106987A1 - Compuestos de diamina-arilsulfonamida sustituidos con hidroxialquilamina e hidroxicicloalquilamina con actividad selectiva en canales de sodio activados por voltaje - Google Patents

Compuestos de diamina-arilsulfonamida sustituidos con hidroxialquilamina e hidroxicicloalquilamina con actividad selectiva en canales de sodio activados por voltaje

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Publication number
AR106987A1
AR106987A1 ARP160103829A ARP160103829A AR106987A1 AR 106987 A1 AR106987 A1 AR 106987A1 AR P160103829 A ARP160103829 A AR P160103829A AR P160103829 A ARP160103829 A AR P160103829A AR 106987 A1 AR106987 A1 AR 106987A1
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AR
Argentina
Prior art keywords
carbon atoms
branched
linear
cyclic alkyl
formula
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ARP160103829A
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English (en)
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Merck Sharp & Dohme
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Publication of AR106987A1 publication Critical patent/AR106987A1/es

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    • 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
    • C07D417/12Heterocyclic 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 chain containing hetero atoms as chain links
    • 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
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/081,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433Thidiazoles
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D277/38Nitrogen atoms
    • C07D277/50Nitrogen atoms bound to hetero atoms
    • C07D277/52Nitrogen atoms bound to hetero atoms to sulfur atoms, e.g. sulfonamides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Cephalosporin Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Reivindicación 1: Un compuesto, o una sal farmacéuticamente aceptable del mismo, que tiene la estructura de fórmula (1), en la que: R¹ es: -Cl, -Br, o alquilo lineal, ramificado o cíclico de hasta 3 átomos de carbono; R² es: (a) un resto de la fórmula (2), en la que, uno de R³ᵃ y R³ᵇ es -H y el otro es -H, -F, CH₃; o (b) un resto de la fórmula (3); y E es: (I) un resto de fórmula (4), en la que: R⁶ es -H o un alquilo lineal, ramificado o cíclico de hasta 6 átomos de carbono; y B es: (a) un resto de la fórmula (5), resto que se une a nitrógeno en uno de R⁷A, R⁷B, o R⁷C por medio de -CH₂-, o se une a nitrógeno directamente en uno de R⁷C, y en la que: m es 0, 1 ó 2; R⁷A y R⁷B son independientemente para cada aparición -H, o un alquilo lineal, ramificado o cíclico de hasta 3 átomos de carbono cuando no se selecciona para unirse al nitrógeno por medio de metileno; R⁷C cuando no se selecciona para unirse al nitrógeno directamente o por medio de metileno es independientemente para cada aparición (i) -H; (ii) alquilo lineal, ramificado o cíclico de hasta tres carbonos; y R⁷D es: (ai) -H; o (aii) un alquilo lineal, ramificado o cíclico de hasta 5 átomos de carbono; o (b) un resto de la fórmula (6), en la que: R⁷ʰ es -H o un alquilo lineal, ramificado o cíclico de hasta 3 átomos de carbono; y R⁷ᵍ y R⁷ᶠ se seleccionan como sigue: (i) R⁷ᵍ es un alquilo lineal de al menos 2, hasta 4 átomos de carbono, un alquilo ramificado de al menos 3 hasta 6 átomos de carbono o alquilo cíclico de hasta 6 átomos de carbono y R⁷ᶠ es un alquilo lineal de al menos 2 átomos de carbono hasta 4 átomos de carbono, o un alquilo ramificado o cíclico de hasta 6 átomos de carbono que está sustituido con -OH en un átomo de carbono del mismo que está unido en beta, o más lejos, al nitrógeno al que está unido; o (ii) R⁷ᶠ es -H o un alquilo lineal, ramificado o cíclico de hasta 6 átomos de carbono o y R⁷ᵍ es -(CH₂)₁₋₂-(HC(OH))-(CH₂)₁₋₂; (II) un resto de fórmula (7), en la que cada R⁸ es independientemente -H o alquilo lineal, ramificado o cíclico de hasta 6 átomos de carbono; o (III) un resto de fórmula (8), en la que: R⁹A es independientemente para cada aparición (i) -H; (ii) -OH; o (iii) un alquilo lineal, ramificado o cíclico de hasta 6 átomos de carbono que está opcionalmente sustituido en un átomo de carbono del mismo con un -OH; R¹⁰A es independientemente para cada aparición (i) -H; o (ii) alquilo lineal, ramificado o cíclico de hasta 6 átomos de carbono que está opcionalmente sustituido en un átomo de carbono del mismo con un -OH; R¹¹A es -H o un, alquilo de 2 ó 3 carbonos que está opcionalmente sustituido en un carbono b o g con un -OH, con la condición de que únicamente un sustituyente -OH esté presente entre todos de R⁹A, R¹⁰A y R¹¹A.
ARP160103829A 2015-12-18 2016-12-14 Compuestos de diamina-arilsulfonamida sustituidos con hidroxialquilamina e hidroxicicloalquilamina con actividad selectiva en canales de sodio activados por voltaje AR106987A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562269327P 2015-12-18 2015-12-18
US201662290235P 2016-02-02 2016-02-02
US201662420956P 2016-11-11 2016-11-11

Publications (1)

Publication Number Publication Date
AR106987A1 true AR106987A1 (es) 2018-03-07

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ARP160103829A AR106987A1 (es) 2015-12-18 2016-12-14 Compuestos de diamina-arilsulfonamida sustituidos con hidroxialquilamina e hidroxicicloalquilamina con actividad selectiva en canales de sodio activados por voltaje

Country Status (27)

Country Link
US (2) US10221167B2 (es)
EP (1) EP3390374B1 (es)
JP (1) JP6572392B2 (es)
KR (1) KR20180095598A (es)
CN (1) CN108699015A (es)
AR (1) AR106987A1 (es)
AU (1) AU2016370554B2 (es)
BR (1) BR112018012327A2 (es)
CA (1) CA3008611A1 (es)
CL (1) CL2018001640A1 (es)
CO (1) CO2018006137A2 (es)
CR (1) CR20180322A (es)
DO (1) DOP2018000150A (es)
EA (1) EA201891313A1 (es)
EC (1) ECSP18052850A (es)
HK (1) HK1255027A1 (es)
IL (1) IL260052A (es)
MX (1) MX2018007450A (es)
NI (1) NI201800067A (es)
PE (1) PE20181495A1 (es)
PH (1) PH12018501288A1 (es)
SG (1) SG11201804936UA (es)
SV (1) SV2018005708A (es)
TN (1) TN2018000195A1 (es)
TW (1) TW201726637A (es)
WO (1) WO2017106226A1 (es)
ZA (1) ZA201803591B (es)

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