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AR100126A1 - Activadores de herg policíclicos - Google Patents

Activadores de herg policíclicos

Info

Publication number
AR100126A1
AR100126A1 ARP150101163A ARP150101163A AR100126A1 AR 100126 A1 AR100126 A1 AR 100126A1 AR P150101163 A ARP150101163 A AR P150101163A AR P150101163 A ARP150101163 A AR P150101163A AR 100126 A1 AR100126 A1 AR 100126A1
Authority
AR
Argentina
Prior art keywords
alkyl
halogen
substituted
alkoxy
amino
Prior art date
Application number
ARP150101163A
Other languages
English (en)
Inventor
Raymond Bebernitz Gregory
Francis Day Robert
Cody Emma
Jayprakash Patel Tajesh
Qian Ming
Whitehead Lewis
Zabawa Thomas
Zecri Frdric
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of AR100126A1 publication Critical patent/AR100126A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
    • 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
    • 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
    • A61K31/428—Thiazoles condensed with carbocyclic 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans 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 carbon atoms of the hetero ring
    • C07D307/84—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D307/85—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • 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
    • 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
    • C07D417/14—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 three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Furan Compounds (AREA)

Abstract

Un método para la elaboración de los compuestos de la presente, y sus usos terapéuticos. La presente proporciona además una combinación de agentes farmacológicamente activos y una composición farmacéutica. Reivindicación 1: Un compuesto, o una sal del mismo, de la fórmula (1), en donde: R¹ se selecciona a partir de: CO₂H, o tetrazol; y R² se selecciona a partir de: H, halógeno, alquilo C₁₋₄ o alquilo C₁₋₄ sustituido por halógeno, o R¹ es H y R² es CO₂H o tetrazol; X se selecciona a partir de: H, halógeno, alquilo C₁₋₄, alcoxilo C₁₋₄, NR⁸R⁹, alquilo C₁₋₄ sustituido por halógeno, fenilo o un heteroarilo de 5 a 6 miembros que contiene de 1 a 3 heteroátomos, cada uno independientemente seleccionado a partir de O, N, o S, en donde el fenilo o heteroarilo están opcionalmente sustituidos con 1 a 2 sustituyentes, cada uno independientemente seleccionado a partir de halógeno, alquilo C₁₋₄, alcoxilo C₁₋₄, alquilo C₁₋₄ sustituido por halógeno, alquilo C₁₋₄ sustituido por hidroxilo, alquilo C₁₋₄ sustituido por alquilo C₁₋₄-amino, alquilo C₁₋₄ sustituido por dimetil-amino; R⁸ se selecciona a partir de: H, o alquilo C₁₋₄; R⁹ se selecciona a partir de: H, o alquilo C₁₋₄; R³ es un resto de fórmula (2) ó (3); en donde R³ᵃ se selecciona a partir de: H, alquilo C₁₋₄ o alquilo C₁₋₄ sustituido por halógeno; R³ᵇ se selecciona a partir de: H, alquilo C₁₋₄, o tomado junto con R³ᵃ forma un cicloalquilo saturado de 3 a 7 miembros o un heterociclo saturado de 3 a 7 miembros que contiene de 1 a 2 heteroátomos seleccionados a partir de O, S o N; R³ᶜ se selecciona a partir de: H o CH₃; R³ᵇ se selecciona a partir de: H o CH₃; R⁴ se selecciona a partir del grupo de fórmulas (4); en donde la línea punteada indica el punto de unión; R⁵ se selecciona a partir de: H o CH₃; R⁶ se selecciona independientemente a partir de: halógeno, nitrilo, alquilo C₁₋₄, alquilo C₁₋₄ sustituido por halógeno, alquilo C₁₋₄ sustituido por nitrilo, alcoxilo C₁₋₄, alcoxilo C₁₋₄ sustituido por halógeno, alcoxilo C₁₋₄ sustituido por nitrilo, alquileno C₁₋₄, N-acetilo, trifluoro-acetilo, tioalquilo C₁₋₄, tio sustituido por halógeno, tioalquilo C₁₋₄ sustituido por halógeno, cicloalquilo C₃₋₆, alquilo C₁₋₄ sustituido por metil-amino, alquilo C₁₋₄ sustituido por dimetil-amino, hidroxi-alquilo C₁₋₄ sustituido por halógeno, un heterociclo saturado de 4 a 6 miembros que contiene de 1 a 2 heteroátomos seleccionados a partir de O, S o N, o un heteroarilo de 5 a 6 miembros que contiene de 1 a 3 heteroátomos, cada uno independientemente seleccionado a partir de O, N, o S, en donde el heterociclo o heteroarilo están opcionalmente sustituidos con 1 a 2 sustituyentes, cada uno independientemente seleccionado a partir de alquilo C₁₋₄, halógeno, hidroxilo, amino, o alcoxilo C₁₋₄; R⁷ se selecciona a partir de: H o halógeno; n es 1, 2 ó 3; m es 0, 1 ó 2; o R³ᶜ y R⁴ tomados junto con la amina a la que R³ᶜ y R⁴ están unidos, forman un heterociclo de 4 a 7 miembros completamente saturado, en donde 1 a 2 de los átomos de carbono en el anillo son cada uno independientemente reemplazados opcionalmente con un átomo de nitrógeno (N) o de oxígeno (O), y el heterociclo está opcionalmente sustituido con 1 a 2 sustituyentes, cada uno independientemente seleccionado a partir de alcoxilo C₁₋₄, alquilo C₁₋₄, alquilo C₁₋₄ sustituido por halógeno, hidroxi-alquilo C₁₋₄, ciclopropilo u oxo; o una sal farmacéuticamente aceptable del mismo.
ARP150101163A 2014-04-17 2015-04-17 Activadores de herg policíclicos AR100126A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201461980932P 2014-04-17 2014-04-17

Publications (1)

Publication Number Publication Date
AR100126A1 true AR100126A1 (es) 2016-09-14

Family

ID=53008919

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP150101163A AR100126A1 (es) 2014-04-17 2015-04-17 Activadores de herg policíclicos

Country Status (15)

Country Link
US (2) US9255093B2 (es)
EP (1) EP3131893B1 (es)
JP (1) JP6518692B2 (es)
KR (1) KR20160142887A (es)
CN (1) CN106604918B (es)
AR (1) AR100126A1 (es)
AU (1) AU2015247575C1 (es)
BR (1) BR112016023991A2 (es)
CA (1) CA2945539A1 (es)
EA (1) EA030824B1 (es)
ES (1) ES2787625T3 (es)
MX (1) MX2016013561A (es)
TW (1) TW201602089A (es)
UY (1) UY36084A (es)
WO (1) WO2015161052A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019087162A1 (en) * 2017-11-06 2019-05-09 Novartis Ag Polycyclic herg activators
WO2019087163A1 (en) * 2017-11-06 2019-05-09 Novartis Ag Polycyclic herg activators
CN110642818B (zh) * 2019-11-11 2023-05-30 云南师范大学 一种制备苯并呋喃-2-甲酰胺类化合物的方法
CN120053458A (zh) * 2025-04-28 2025-05-30 昆明医科大学 一种Ribociclib合并NS1643组合物及其应用

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE671060A (es) * 1965-10-19 1966-04-19
US4455427A (en) * 1981-07-01 1984-06-19 The Upjohn Company Pyridyl-substituted-benzofurans
AU2001296013A1 (en) 2000-11-01 2002-05-15 Shionogi And Co., Ltd. Pgd2 receptor antagonistic pharmaceutical compositions
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
WO2005023237A1 (en) * 2003-09-04 2005-03-17 Poseidon Pharmaceuticals A/S Erg channel openers for the treatment of cardiac arrhythmias
WO2007062028A2 (en) * 2005-11-21 2007-05-31 Tap Pharmaceutical Products, Inc. Treatment of qt interval prolongation and diseases associated therewith
TWI464148B (zh) * 2006-03-16 2014-12-11 Evotec Us Inc 作為ｐ２ｘ7調節劑之雙環雜芳基化合物與其用途
US20120329865A1 (en) * 2009-12-31 2012-12-27 Huayun Deng MOLECULES RELATED hERG ION CHANNELS AND THE USE THEREOF

Also Published As

Publication number Publication date
CN106604918A (zh) 2017-04-26
ES2787625T3 (es) 2020-10-16
AU2015247575A1 (en) 2016-10-27
BR112016023991A2 (pt) 2017-08-15
CN106604918B (zh) 2019-09-27
WO2015161052A1 (en) 2015-10-22
TW201602089A (zh) 2016-01-16
MX2016013561A (es) 2017-01-23
UY36084A (es) 2015-11-30
AU2015247575B2 (en) 2018-01-25
JP6518692B2 (ja) 2019-05-22
US9255093B2 (en) 2016-02-09
JP2017511355A (ja) 2017-04-20
EA201692090A1 (ru) 2017-03-31
EA030824B1 (ru) 2018-10-31
KR20160142887A (ko) 2016-12-13
CA2945539A1 (en) 2015-10-22
EP3131893B1 (en) 2020-02-12
US20160108025A1 (en) 2016-04-21
US20150299181A1 (en) 2015-10-22
AU2015247575C1 (en) 2019-04-11
EP3131893A1 (en) 2017-02-22

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