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PE20181495A1 - 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

Info

Publication number
PE20181495A1
PE20181495A1 PE2018001100A PE2018001100A PE20181495A1 PE 20181495 A1 PE20181495 A1 PE 20181495A1 PE 2018001100 A PE2018001100 A PE 2018001100A PE 2018001100 A PE2018001100 A PE 2018001100A PE 20181495 A1 PE20181495 A1 PE 20181495A1
Authority
PE
Peru
Prior art keywords
formula
diamine
hydroxycloalkylamine
hydroxialkylamine
voltage
Prior art date
Application number
PE2018001100A
Other languages
English (en)
Inventor
Thomas J Greshock
James Mulhearn
Junying Zheng
Ronald M Kim
Ting Zhang
Anthony J Roecker
Walter Won
Philippe Nantermet
Rajan Anand
Gang Zhou
Deping Wang
Liangqin Guo
Original Assignee
Merck Sharp & Dohme
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of PE20181495A1 publication Critical patent/PE20181495A1/es

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    • 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
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/433—Thidiazoles
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic 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
    • C07D277/32—Heterocyclic 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
    • C07D277/38—Nitrogen atoms
    • C07D277/50—Nitrogen atoms bound to hetero atoms
    • C07D277/52—Nitrogen atoms bound to hetero atoms to sulfur atoms, e.g. sulfonamides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (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)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Cephalosporin Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Referido a compuestos de formula A, o una sal de este, en la que R1 es -Cl, Br, o alquilo lineal, ramificado o ciclico de hasta 3 atomos de carbono; R2 es un resto de la formula (a), en la que uno de R3a y R3b es -H y el otro es -H, F, CH3; o un resto de la formula (b); E es un resto de la formula E1, en la que R6 es H o un alquilo lineal, ramificado o ciclico de hasta 6 atomos de carbono; y B es un resto de la formula (c), en donde se une a nitrogeno en uno de R7A, R7B, o R7C por medio de -CH2- , o se une a nitrogeno directamente en uno de R7C; m es 0, 1 o 2; R7D es -H, alquilo lineal, ramificado, o ciclico de hasta 5 atomos de carbono, entre otros. Estos compuestos de diamina-arilsulfonamida sustituidos con hidroxialquilamina e hidroxicicloalquilamina tienen propiedades para inhibir los canales de iones Na v 1.7 encontrados en neuronas perifericas y simpaticas. Tambien se refiere a formulaciones farmaceuticas que comprenden los compuestos de formula A o sus sales, y procedimientos de tratamiento de trastornos de dolor, tos, y picazon usando las mismas.
PE2018001100A 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 PE20181495A1 (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
PE20181495A1 true PE20181495A1 (es) 2018-09-18

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PE2018001100A PE20181495A1 (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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CO2018006137A2 (es) 2018-07-10
AU2016370554A1 (en) 2018-06-14
US10221167B2 (en) 2019-03-05
EA201891313A1 (ru) 2018-11-30
SV2018005708A (es) 2018-12-14
AR106987A1 (es) 2018-03-07
KR20180095598A (ko) 2018-08-27
NI201800067A (es) 2018-07-24
CA3008611A1 (en) 2017-06-22
EP3390374B1 (en) 2020-08-26
DOP2018000150A (es) 2018-07-31
TN2018000195A1 (en) 2019-10-04
AU2016370554B2 (en) 2018-11-29
ZA201803591B (en) 2019-04-24
IL260052A (en) 2018-07-31
JP6572392B2 (ja) 2019-09-11
BR112018012327A2 (pt) 2018-12-04
EP3390374A1 (en) 2018-10-24
CN108699015A (zh) 2018-10-23
SG11201804936UA (en) 2018-07-30
WO2017106226A1 (en) 2017-06-22
MX2018007450A (es) 2018-11-14
CR20180322A (es) 2018-08-21
CL2018001640A1 (es) 2018-08-03
ECSP18052850A (es) 2018-12-31
HK1255027A1 (zh) 2019-08-02
US20170174674A1 (en) 2017-06-22
US20190233406A1 (en) 2019-08-01
TW201726637A (zh) 2017-08-01
PH12018501288A1 (en) 2019-01-28
JP2019502681A (ja) 2019-01-31

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