AR094214A1 - Inhibidores de la quinasa que regula la señal de la apoptosis - Google Patents

Inhibidores de la quinasa que regula la señal de la apoptosis

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Publication number
AR094214A1
AR094214A1 ARP130104949A ARP130104949A AR094214A1 AR 094214 A1 AR094214 A1 AR 094214A1 AR P130104949 A ARP130104949 A AR P130104949A AR P130104949 A ARP130104949 A AR P130104949A AR 094214 A1 AR094214 A1 AR 094214A1
Authority
AR
Argentina
Prior art keywords
alkyl
diseases
hydrogen
cycloalkyl
substituted
Prior art date
Application number
ARP130104949A
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English (en)
Inventor
Notte Gregory
Original Assignee
Gilead Sciences Inc
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 Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of AR094214A1 publication Critical patent/AR094214A1/es

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    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/14Heterocyclic 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
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  • Engineering & Computer Science (AREA)
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  • General Chemical & Material Sciences (AREA)
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  • Cardiology (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Estos compuestos presentan actividad de inhibición sobre la quinasa que regula la señal de la apoptosis (ASK1), por lo que son útiles para tratar las afecciones que están mediadas por la ASK1, lo que abarca los trastornos autoinmunes, las enfermedades inflamatorias, las enfermedades cardiovasculares, la diabetes, la nefropatía diabética, las enfermedades cardiorrenales, que abarcan las enfermedades en los riñones, las enfermedades fibróticas, las enfermedades respiratorias, la EPOC, la fibrosis pulmonar idiopática, las lesiones agudas en los pulmones, las enfermedades hepáticas agudas o crónicas y las enfermedades neurodegenerativas. Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1), donde R¹ es un alquilo C₁₋₃ o un cicloalquilo C₃₋₆, donde el alquilo o el cicloalquilo pueden estar sustituidos con entre uno y tres átomos halógenos; R² es hidrógeno o un alquilo C₁₋₆, donde el alquilo puede estar sustituido con un halógeno; R³ es hidrógeno o un alquilo C₁₋₃; R⁴ es hidrógeno o un alquilo C₁₋₃; R⁵ es hidrógeno, un alquilo C₁₋₃, ORᵃ o NHRᵃ; R⁶ es hidrógeno, un alquilo C₁₋₃, un haloalquilo C₁₋₃ o un cicloalquilo C₃₋₆, donde el cicloalquilo puede estar sustituido con un alquilo C₁₋₃, con un haloalquilo C₁₋₃ o con 1 ó 2 átomos halógenos; Rᵃ y Rᵇ son independientemente hidrógeno o un alquilo C₁₋₃, o Rᵃ y Rᵇ pueden combinarse con el átomo de nitrógeno al que están unidos para formar un anillo heterocíclico de seis miembros, que puede comprender un átomo de oxígeno o de nitrógeno; o una sal o un estereoisómero farmacéuticamente aceptable de dicho compuesto.
ARP130104949A 2012-12-21 2013-12-20 Inhibidores de la quinasa que regula la señal de la apoptosis AR094214A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261740777P 2012-12-21 2012-12-21

Publications (1)

Publication Number Publication Date
AR094214A1 true AR094214A1 (es) 2015-07-15

Family

ID=49943575

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ARP130104949A AR094214A1 (es) 2012-12-21 2013-12-20 Inhibidores de la quinasa que regula la señal de la apoptosis

Country Status (29)

Country Link
US (4) US9051313B2 (es)
EP (2) EP2935258B1 (es)
JP (2) JP6086633B2 (es)
KR (1) KR101712758B1 (es)
CN (1) CN104918936B (es)
AR (1) AR094214A1 (es)
AU (2) AU2013361140B2 (es)
BR (1) BR112015014567A2 (es)
CA (1) CA2896060C (es)
CY (1) CY1118574T1 (es)
DK (1) DK2935258T3 (es)
EA (1) EA027645B1 (es)
ES (1) ES2612979T3 (es)
HK (1) HK1214247A1 (es)
HR (1) HRP20170112T8 (es)
HU (1) HUE032988T2 (es)
IL (2) IL239322A (es)
LT (1) LT2935258T (es)
MX (1) MX2015008090A (es)
NZ (1) NZ709248A (es)
PL (1) PL2935258T3 (es)
PT (1) PT2935258T (es)
RS (1) RS55676B1 (es)
SG (1) SG11201504865YA (es)
SI (1) SI2935258T1 (es)
SM (1) SMT201700051B (es)
TW (1) TWI622589B (es)
UY (1) UY35212A (es)
WO (1) WO2014100541A1 (es)

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NZ720660A (en) 2013-12-20 2018-01-26 Gilead Sciences Inc Apoptosis signal-regulating kinase inhibitors
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IL255799B (en) 2018-11-29
EA201591018A1 (ru) 2016-01-29
NZ709248A (en) 2016-04-29
CN104918936B (zh) 2018-04-27
SMT201700051B (it) 2017-03-08
CY1118574T1 (el) 2017-07-12
DK2935258T3 (en) 2017-02-13
KR101712758B1 (ko) 2017-03-06
KR20150095903A (ko) 2015-08-21
HUE032988T2 (hu) 2017-11-28
AU2016247182A1 (en) 2016-11-10
PT2935258T (pt) 2017-02-09
EA027645B1 (ru) 2017-08-31
BR112015014567A2 (pt) 2017-07-11
HRP20170112T8 (hr) 2017-06-16
AU2016247182B2 (en) 2017-12-21
ES2612979T3 (es) 2017-05-19
US20140179663A1 (en) 2014-06-26
IL255799A (en) 2018-01-31
US20180303844A1 (en) 2018-10-25
RS55676B1 (sr) 2017-06-30
JP2016503801A (ja) 2016-02-08
UY35212A (es) 2014-06-30
EP2935258A1 (en) 2015-10-28
LT2935258T (lt) 2017-02-10
AU2013361140B2 (en) 2016-11-03
SI2935258T1 (sl) 2017-02-28
US20150246910A1 (en) 2015-09-03
US20170173031A1 (en) 2017-06-22
IL239322A (en) 2017-12-31
US9051313B2 (en) 2015-06-09
CA2896060C (en) 2017-03-21
MX2015008090A (es) 2016-04-11
PL2935258T3 (pl) 2017-06-30
TW201441221A (zh) 2014-11-01
US10307427B2 (en) 2019-06-04
US9943521B2 (en) 2018-04-17
EP3150597A1 (en) 2017-04-05
SG11201504865YA (en) 2015-07-30
IL239322A0 (en) 2015-07-30
AU2013361140A1 (en) 2015-07-09
WO2014100541A1 (en) 2014-06-26
JP6086633B2 (ja) 2017-03-01
JP2016222721A (ja) 2016-12-28
HK1214247A1 (zh) 2016-07-22
EP2935258B1 (en) 2016-11-02
CA2896060A1 (en) 2014-06-26
CN104918936A (zh) 2015-09-16
HRP20170112T1 (hr) 2017-03-24
TWI622589B (zh) 2018-05-01

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