AR105875A1 - Derivados de 2-oxo-1,2-dihidropiridina como inhibidores de bromodominio - Google Patents

Derivados de 2-oxo-1,2-dihidropiridina como inhibidores de bromodominio

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Publication number
AR105875A1
AR105875A1 ARP160102662A ARP160102662A AR105875A1 AR 105875 A1 AR105875 A1 AR 105875A1 AR P160102662 A ARP160102662 A AR P160102662A AR P160102662 A ARP160102662 A AR P160102662A AR 105875 A1 AR105875 A1 AR 105875A1
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alkyl
substituted
nr11r12
halo
groups
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ARP160102662A
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GLAXOSMITHKLINE INTELLECTUAL PROPERTY (Nº 2) LTD
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Publication of AR105875A1 publication Critical patent/AR105875A1/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
    • A61K31/435Heterocyclic 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
    • A61K31/4412Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • 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
    • A61K31/455Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D471/02Heterocyclic 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 two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La presente se refiere a compuestos de fórmula (1) y sales de los mismos, a composiciones farmacéuticas que contienen tales compuestos y a su uso en terapia. Reivindicación 1: Un compuesto de formula (1) o una sal del mismo en la que: R¹ es -alquilo C₁₋₃ o ciclopropilo; R² es H o -alquil C₀₋₃-cicloalquilo C₃₋₇, donde el grupo cicloalquilo no está sustituido o está sustituido con uno, dos o tres grupos R⁵ que pueden ser iguales o distintos; R³ es -H, -alquilo C₁₋₄, ciclopropilo o -(CH₂)ₚOR¹⁰; R⁴ es a) fenilo (que puede estar no sustituido o sustituido con uno, dos o tres grupos R⁷ que pueden ser iguales o distintos); b) un grupo heteroarilo de 5 ó 6 miembros (que puede estar no sustituido o sustituido con -alquilo C₁₋₃, -O-alquilo C₁₋₃, o halo); c) un grupo heteroarilo de 9 a 11 miembros (que puede estar no sustituido o sustituido con uno, dos o tres grupos, que pueden ser iguales o distintos, seleccionados de -alquil C₁₋₃-R⁸, -OCH₃, -O-alquil C₂₋₃-R⁸, halo, oxo, -O-CF₃ y -CN); o d) -(CH₂)ₙ-fenilo; p es 1 ó 2; n es 1 ó 2; R⁵ es halo, fenilo, -alquil C₁₋₆-R⁸, -CO₂H, -OCH₃, -O-alquil C₂₋₆-R⁸, -CN, -OH o -NHR⁶; R⁶ es -H, -C(O)OC(CH₃)₃, -alquilo C₁₋₆, -cicloalquilo C₃₋₇, un grupo heterociclilo de 4 a 7 miembros, o -alquil C₂₋₃-O-alquilo C₁₋₃ donde los grupos -alquilo C₁₋₆ y -cicloalquilo C₃₋₇ pueden estar opcionalmente sustituidos con uno, dos o tres fluoro; R⁷ es -NR¹¹R¹², -alquilo C₁₋₃, halo, -CO₂R¹⁰, -CH₂OH, -CH(R¹¹)OR¹⁰, -C(O)alquilo C₁₋₃, -CH(R¹⁰)NR¹¹R¹², -CN, -CHF₂, -CF₃, -OH, -OCHF₂, -OCF₃, -OCH₃, -O-alquil C₂₋₆-R⁹, -alquil C₁₋₆-R⁹ o -O-piperidinilo; R⁸ es -H, -OR¹⁰, -CO₂C(CH₃)₃ o -NR¹¹R¹²; R⁹ es -H, -OR¹⁰ o -NR¹¹R¹²; R¹⁰ es -H o -alquilo C₁₋₃; R¹¹ y R¹² están cada uno seleccionado independientemente de -H, -alquilo C₁₋₃ y -alquil C₁₋₃NR¹³R¹⁴; o R¹¹ y R¹² pueden unirse junto con el nitrógeno al que están unidos para formar un grupo heterociclilo de 4 a 7 miembros, opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente de -alquilo C₁₋₃, -OH y F; y R¹³ y R¹⁴ están cada uno seleccionado independientemente de -H, -alquilo C₁₋₃ y -C(O)CH₃.
ARP160102662A 2015-09-02 2016-08-31 Derivados de 2-oxo-1,2-dihidropiridina como inhibidores de bromodominio AR105875A1 (es)

Applications Claiming Priority (1)

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US201562213137P 2015-09-02 2015-09-02

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AR105875A1 true AR105875A1 (es) 2017-11-15

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US (2) US10428026B2 (es)
EP (1) EP3344615A1 (es)
JP (1) JP6532599B2 (es)
KR (1) KR102088157B1 (es)
CN (1) CN108137542B (es)
AR (1) AR105875A1 (es)
AU (1) AU2016315360B2 (es)
CA (1) CA2996245C (es)
CL (1) CL2018000565A1 (es)
CO (1) CO2018002211A2 (es)
CR (1) CR20180138A (es)
DO (1) DOP2018000062A (es)
EA (1) EA033679B1 (es)
HK (1) HK1249504A1 (es)
IL (1) IL257431B (es)
MA (1) MA43940A (es)
MX (1) MX2018002699A (es)
PE (1) PE20181273A1 (es)
PH (1) PH12018500446A1 (es)
TW (1) TWI724022B (es)
UY (1) UY36875A (es)
WO (1) WO2017037116A1 (es)

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MA43940A (fr) * 2015-09-02 2018-12-12 Glaxosmithkline Ip No 2 Ltd Dicarboxamide de pyridinone utilisé comme inhibiteur de bromodomaine
AU2016326864A1 (en) 2015-09-22 2018-03-22 Glaxosmithkline Intellectual Property (No.2) Limited Pyridinone dicarboxamide for use as bromodomain inhibitors
BR112018006545A2 (pt) 2015-10-05 2018-10-16 Glaxosmithkline Ip No 2 Ltd ?composto, composição farmacêutica, combinação, uso de um composto, e, método para tratamento de uma doença ou condição?
JP6954921B2 (ja) 2016-04-07 2021-10-27 グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited ブロモドメイン阻害薬としてのピリジル誘導体
RU2018142988A (ru) * 2016-05-24 2020-06-25 ГлаксоСмитКлайн Интеллекчуал Проперти (N2) Лимитед Производные пиридиндикарбоксамида в качестве ингибиторов бромодомена
JOP20190192A1 (ar) 2017-03-01 2019-08-08 Glaxosmithkline Ip No 2 Ltd مشتقات بيرازول بوصفها مثبطات برومودومين
GB201703282D0 (en) 2017-03-01 2017-04-12 Glaxosmithkline Intellectual Property (No 2) Ltd Compounds
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CN108484494B (zh) * 2018-06-15 2021-07-30 沈阳药科大学 2-氧代-1,2-二氢吡啶-4-甲酸类化合物
GB201814167D0 (en) 2018-08-31 2018-10-17 Glaxosmithkline Ip No 2 Ltd Compounds
BR112022026364A2 (pt) 2020-06-23 2023-01-17 Genentech Inc Composto macrocíclico, compostos, complexo, uso de um composto, composição farmacêutica, métodos para tratar câncer e para tratar uma condição fibrótica e invenção

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BR112018006545A2 (pt) 2015-10-05 2018-10-16 Glaxosmithkline Ip No 2 Ltd ?composto, composição farmacêutica, combinação, uso de um composto, e, método para tratamento de uma doença ou condição?
JP6954921B2 (ja) 2016-04-07 2021-10-27 グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited ブロモドメイン阻害薬としてのピリジル誘導体
RU2018142988A (ru) 2016-05-24 2020-06-25 ГлаксоСмитКлайн Интеллекчуал Проперти (N2) Лимитед Производные пиридиндикарбоксамида в качестве ингибиторов бромодомена

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DOP2018000062A (es) 2018-03-30
KR102088157B1 (ko) 2020-03-12
IL257431A (en) 2018-04-30
CN108137542B (zh) 2023-10-27
CR20180138A (es) 2018-07-16
US20180258044A1 (en) 2018-09-13
EA033679B1 (ru) 2019-11-15
TWI724022B (zh) 2021-04-11
EA201890331A1 (ru) 2018-08-31
US10428026B2 (en) 2019-10-01
KR20180043366A (ko) 2018-04-27
US20190359572A1 (en) 2019-11-28
AU2016315360B2 (en) 2019-09-12
BR112018003827A2 (pt) 2018-09-25
EP3344615A1 (en) 2018-07-11
JP6532599B2 (ja) 2019-06-19
WO2017037116A1 (en) 2017-03-09
HK1249504A1 (zh) 2018-11-02
CO2018002211A2 (es) 2018-05-21
UY36875A (es) 2017-03-31
CL2018000565A1 (es) 2018-07-06
CN108137542A (zh) 2018-06-08
MX2018002699A (es) 2018-04-13
PE20181273A1 (es) 2018-08-03
US10927080B2 (en) 2021-02-23
AU2016315360A1 (en) 2018-03-22
JP2018526383A (ja) 2018-09-13
CA2996245C (en) 2023-10-17
CA2996245A1 (en) 2017-03-09
IL257431B (en) 2021-04-29
PH12018500446A1 (en) 2018-09-10
MA43940A (fr) 2018-12-12
TW201718504A (zh) 2017-06-01

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