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AR094122A1 - Compuestos triciclicos moduladores de la actividad de cftr - Google Patents

Compuestos triciclicos moduladores de la actividad de cftr

Info

Publication number
AR094122A1
AR094122A1 ARP130104861A ARP130104861A AR094122A1 AR 094122 A1 AR094122 A1 AR 094122A1 AR P130104861 A ARP130104861 A AR P130104861A AR P130104861 A ARP130104861 A AR P130104861A AR 094122 A1 AR094122 A1 AR 094122A1
Authority
AR
Argentina
Prior art keywords
alkyl
amino
alkoxy
halo
r6oc
Prior art date
Application number
ARP130104861A
Other languages
English (en)
Inventor
Ahmed Mahbub
Ashall-Kelly Alexander
Gueritz Louisa
Mkenna Jeffrey
Mkenna Joseph
Mutton Simon
Parmar Rakesh
Shepherd Jon
Wright Paul
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=50030372&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR094122(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR094122A1 publication Critical patent/AR094122A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/22Heterocyclic 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 four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Además se proporciona una combinación de agentes farmacológicamente activos y una composición farmacéutica para uso en el tratamiento de diarrea y enfermedades renales poliquísticas. Reivindicación 1: Un compuesto de la fórmula (1) o una sal farmacéuticamente aceptable del mismo, en donde R¹ representa fenilo, cicloalquenilo C₄₋₇ o Het¹, tal grupo R¹ puede ser no sustituido o sustituido en uno o dos átomos de carbono por sustituyentes Rᵃ, y puede sustituirse adicionalmente en un átomo de nitrógeno por un sustituyente Rᵃ¹; cada Rᵃ independientemente representa alquilo C₁₋₄, halo, halo-alquilo C₁₋₄, ciano, hidroxi-alquilo C₁₋₄, alcoxilo C₁₋₄, halo-alcoxilo C₁₋₄, alcoxi C₁₋₄alquilo C₁₋₄, R⁶OC(O)-, o R⁶OC(O)alquilo C₁₋₄-; Rᵃ¹ representa alquilo C₁₋₄, hidroxi-alquilo C₁₋₄, alcoxi C₁₋₄alquilo C₁₋₄, alquil C₁₋₄amino-alquil C₁₋₄-, di[alquil C₁₋₄]amino-alquil C₁₋₄-, aril-alquil C₁₋₄ o R⁶OC(O)alquilo C₁₋₄-; R² representa alquilo C₁₋₆, cicloalquilo C₃₋₇, cicloalquenilo C₄₋₇, fenilo, furanilo, tiazolilo o tienilo, tal R² puede ser no sustituido o sustituido en de uno a tres átomos de carbono con sustituyentes Rᵇ; cada Rᵇ independientemente representa alquilo C₁₋₄, halo, halo-alquilo C₁₋₄, ciano, alquil C₁₋₄amino-alquilo C₁₋₄-, di[alquil C₁₋₄]amino-alquilo C₁₋₄-, (R⁶)₂NC(O)alquilo C₁₋₄- o R⁶OC(O)alquilo C₁₋₄-; X representa S, Z representa CHR⁴ᵃ y n representa 1; o X representa CHR⁴ᵇ, Z representa NR⁵ y n representa 1 ó 2; o X representa CHR⁴ᵇ, Z representa CHR⁴ᵃ y n representa 0, 1 ó 2; o X representa C(=CH₂), CF₂ o C(CH₃)₂, Z representa CHR⁴ᵃ y n representa 0 ó 1; cada R³ independientemente representa metilo o etilo; cuando X representa S, R⁴ representa hidrógeno, alquilo C₁₋₄, halo-alquilo C₁₋₄, hidroxi-alquilo C₁₋₄, alcoxi C₁₋₄alquilo C₁₋₄-, amino-alquilo C₁₋₄-, alquil C₁₋₄amino-alquilo C₁₋₄-, di[alquil C₁₋₄]amino-alquilo C₁₋₄-, fenilo, Het¹-alquilo C₁₋₄-, Het²-alquilo C₁₋₄-, alquil C₁₋₄-S(O)₂NH-alquilo C₁₋₄-, o R⁷C(O)NH-alquilo C₁₋₄-; cuando X representa CHR⁴ᵇ, cada R⁴ independientemente representa hidrógeno, hidroxilo, alquilo C₁₋₄, alcoxilo C₁₋₄, halo-alquilo C₁₋₄, hidroxi-alquilo C₁₋₄, alcoxi C₁₋₄alquilo C₁₋₄-, amino-alquilo C₁₋₄-, alquil C₁₋₄amino-alquilo C₁₋₄-, di[alquil C₁₋₄]amino-alquilo C₁₋₄-, amino, alquil C₁₋₄amino-, di[alquil C₁₋₄]amino- ,fenilo, Het¹-alquilo C₁₋₄-, Het²-alquilo C₁₋₄-, alquil C₁₋₄-S(O)₂NH-alquilo C₁₋₄-, o R⁷C(O)NH-alquilo C₁₋₄-; R⁴ᵃ representa hidrógeno, alquilo C₁₋₄, hidroxi-alquilo C₁₋₄, halo-alquilo C₁₋₄, amino-alquilo C₁₋₄-, alquil C₁₋₄amino-alquilo C₁₋₄-, di[alquil C₁₋₄]amino-alquilo C₁₋₄-, Het¹-alquilo C₁₋₄-, Het²-alquilo C₁₋₄-, o R⁶OC(O)-; R⁴ᵇ representa hidrógeno o metilo; R⁵ representa hidrógeno o alquilo C₁₋₄; R⁶ representa hidrógeno o alquilo C₁₋₄; R⁷ representa alquilo C₁₋₂, alcoxilo C₁₋₂, alcoxi C₁₋₂-alquilo C₁₋₂ o fenilo; Het¹ representa un anillo de heteroarilo de 5 ó 6 miembros que comprende a) un átomo de oxígeno o azufre y opcionalmente uno o dos átomos de nitrógeno; o b) de uno a cuatro átomos de nitrógeno; y Het² representa un anillo heterocíclico de 4 a 7 miembros que comprende a) 1 ó 2 heteroátomos seleccionados a partir de N, O y S; o b) -C(O)- y 1 ó 2 heteroátomos seleccionados a partir de N y O.
ARP130104861A 2012-12-19 2013-12-19 Compuestos triciclicos moduladores de la actividad de cftr AR094122A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261739335P 2012-12-19 2012-12-19
US201361906141P 2013-11-19 2013-11-19

Publications (1)

Publication Number Publication Date
AR094122A1 true AR094122A1 (es) 2015-07-08

Family

ID=50030372

Family Applications (1)

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ARP130104861A AR094122A1 (es) 2012-12-19 2013-12-19 Compuestos triciclicos moduladores de la actividad de cftr

Country Status (25)

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US (2) US9359381B2 (es)
EP (1) EP2935278B1 (es)
JP (1) JP6284546B2 (es)
KR (1) KR20150097660A (es)
CN (1) CN105143230B (es)
AP (1) AP2015008539A0 (es)
AR (1) AR094122A1 (es)
AU (1) AU2013365739A1 (es)
BR (1) BR112015014292A2 (es)
CA (1) CA2895660A1 (es)
CL (1) CL2015001730A1 (es)
CR (1) CR20150325A (es)
CU (1) CU20150066A7 (es)
EA (1) EA201591177A1 (es)
ES (1) ES2628369T3 (es)
HK (1) HK1209741A1 (es)
IL (1) IL239389A0 (es)
MX (1) MX2015007939A (es)
PE (1) PE20151055A1 (es)
PH (1) PH12015501386A1 (es)
SG (1) SG11201504594QA (es)
TN (1) TN2015000279A1 (es)
TW (1) TW201429974A (es)
UY (1) UY35211A (es)
WO (1) WO2014097148A1 (es)

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US9056867B2 (en) 2011-09-16 2015-06-16 Novartis Ag N-substituted heterocyclyl carboxamides
EP2935278B1 (en) 2012-12-19 2017-03-15 Novartis AG Tricyclic compounds for inhibiting the cftr channel
KR20150095925A (ko) 2012-12-19 2015-08-21 노파르티스 아게 Cftr 억제제로서의 트리시클릭 화합물
CN106715536B (zh) * 2014-09-19 2021-06-01 莫门蒂夫性能材料股份有限公司 用于受控的硅氧烷交联的铂(ii)二烯配合物
US9624233B2 (en) * 2015-04-23 2017-04-18 Trevi Therapeutics, Inc. Compounds for treating pruritic conditions
CN106478558B (zh) * 2016-10-17 2019-03-29 天津雅奥科技发展有限公司 一种4-羟甲基-二氢-呋喃-2(3h)-酮的合成方法
US12319686B2 (en) 2019-01-17 2025-06-03 Hoffmann-La Roche Inc. Process for the preparation of tetrahydropyridopyrimidines
CN114007623A (zh) * 2019-06-12 2022-02-01 加利福尼亚大学董事会 治疗胆汁酸性腹泻的方法
AU2022265718A1 (en) 2021-04-29 2023-11-02 Novartis Ag Deubiquitinase-targeting chimeras and related methods
CN117654560B (zh) * 2023-12-01 2024-06-04 安徽泽升科技股份有限公司 一种通过氧化氨基连续化制备硝基化合物的方法

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CA2382528A1 (en) 1999-08-25 2001-03-01 Banyu Pharmaceutical Co., Ltd. Novel isoindole derivatives
JP2002255967A (ja) 2001-02-27 2002-09-11 Banyu Pharmaceut Co Ltd イソインドール誘導体を有効成分とする糖尿病の治療剤、糖尿病の慢性合併症の予防剤又は肥満の治療剤。
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US20110015137A1 (en) * 2007-07-05 2011-01-20 Trustees Of Boston University Reca inhibitors and their uses as microbial inhibitors or potentiators of antibiotic activity
AU2008345225A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
IN2012DN00719A (es) * 2009-08-10 2015-06-19 Univ California
USRE48842E1 (en) * 2011-05-27 2021-12-07 The Regents Of The University Of California Pyrimido-pyrrolo-oxazine-dione compound inhibitors of the cystic fibrosis transmembrane conductance regulator protein and uses therefor
EP2935278B1 (en) 2012-12-19 2017-03-15 Novartis AG Tricyclic compounds for inhibiting the cftr channel
KR20150095925A (ko) 2012-12-19 2015-08-21 노파르티스 아게 Cftr 억제제로서의 트리시클릭 화합물

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Publication number Publication date
HK1209741A1 (en) 2016-04-08
US9359381B2 (en) 2016-06-07
KR20150097660A (ko) 2015-08-26
IL239389A0 (en) 2015-07-30
ES2628369T3 (es) 2017-08-02
WO2014097148A9 (en) 2015-02-19
TW201429974A (zh) 2014-08-01
EP2935278B1 (en) 2017-03-15
CN105143230A (zh) 2015-12-09
CL2015001730A1 (es) 2015-08-28
AU2013365739A1 (en) 2015-07-09
EP2935278A1 (en) 2015-10-28
TN2015000279A1 (en) 2016-10-03
CN105143230B (zh) 2017-06-09
CA2895660A1 (en) 2014-06-26
EA201591177A1 (ru) 2015-11-30
UY35211A (es) 2014-07-31
CR20150325A (es) 2015-08-10
JP2016509579A (ja) 2016-03-31
PH12015501386A1 (en) 2015-09-02
BR112015014292A2 (pt) 2017-07-11
US20140171417A1 (en) 2014-06-19
PE20151055A1 (es) 2015-08-05
SG11201504594QA (en) 2015-07-30
AP2015008539A0 (en) 2015-06-30
MX2015007939A (es) 2016-03-11
JP6284546B2 (ja) 2018-02-28
CU20150066A7 (es) 2015-11-27
US20150336986A1 (en) 2015-11-26
WO2014097148A1 (en) 2014-06-26

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