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AR109495A1 - INHIBITORS OF CELLULAR METABOLIC PROCESSES - Google Patents

INHIBITORS OF CELLULAR METABOLIC PROCESSES

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Publication number
AR109495A1
AR109495A1 ARP170102433A ARP170102433A AR109495A1 AR 109495 A1 AR109495 A1 AR 109495A1 AR P170102433 A ARP170102433 A AR P170102433A AR P170102433 A ARP170102433 A AR P170102433A AR 109495 A1 AR109495 A1 AR 109495A1
Authority
AR
Argentina
Prior art keywords
alkyl
heterocycle
aryl
nr1r2
members
Prior art date
Application number
ARP170102433A
Other languages
Spanish (es)
Inventor
Zhixiong Ye
Zhihua Sui
Zenon D Konteatis
Jeremy M Travins
Original Assignee
Agios Pharmaceuticals 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 Agios Pharmaceuticals Inc filed Critical Agios Pharmaceuticals Inc
Publication of AR109495A1 publication Critical patent/AR109495A1/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Reivindicación 1: Un compuesto caracterizado porque es de acuerdo con la fórmula (1), o una sal farmacéuticamente aceptable del mismo; donde RA se selecciona entre el grupo que consiste en H, C₁₋₆-alquilo, C₂₋₆-alquenilo, C₁₋₆-alcoxi, C₃₋₁₄-carbociclo, (C₃₋₁₄-carbociclo)-C₁₋₆-alquilo-, heterociclo o heterociclo-C₁₋₆-alquilo- de entre 3 y 14 miembros (donde entre 1 y 4 miembros del anillo heterociclo son heteroátomos seleccionados entre N, O, y S), (heterociclo de entre 3 y 14 miembros)oxi-, C₆₋₁₄-arilo, (C₆₋₁₄-aril)-C₁₋₆-alquilo-, C₆₋₁₄-ariloxi-, -(CH₂)₀₋₆NR¹(CH₂)₀₋₆C₍O₎R², NR¹R², C(O)NR¹R², NR¹C(NR²)NR¹R², NR¹C(NR²)(=NR¹), SR¹, -CN, y -OH; donde cada alquilo, alquenilo, alcoxi, arilo, y heterociclo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en R¹, OR¹, halo, -N=N-R¹, NR¹R², -(C₁₋₆-alquil)NR¹R², -C(O)OR¹, -C(O)NR¹R², -OC(O)R¹, -CN, -OP(O)(OR¹)₁₋₂, y oxo; RB se selecciona entre el grupo que consiste en H, C₂₋₆-alquenilo, y C₁₋₆-alquilo, donde RB está opcionalmente sustituido con uno o más R¹; RC, RD, y RE se seleccionan en forma independiente entre el grupo que consiste en C₃₋₁₄-carbociclo, C₆₋₁₄-arilo, y heterociclo de entre 3 y 14 miembros (donde entre 1 y 4 miembros del anillo heterociclo son heteroátomos seleccionados entre N, O, y S), donde RC, RD, y RE están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre el grupo que consiste en R¹, -OR¹, halo, -NR¹R², -(C₁₋₆-alquil)-NR¹R², -C(O)OR¹, -C(O)NR¹R², -NO₂, -CN, y oxo; y R¹ y R² se seleccionan en forma independiente entre el grupo que consiste en H, D (²H), -CN, -OH, C₁₋₆-alquilo, C₁₋₆-alcoxi, C₂₋₆-alquenilo, C₂₋₆-alquinilo, NH₂, -S(O)₀₋₂-(C₁₋₆-alquilo), -S(O)₀₋₂-(C₆₋₁₄-arilo), -C(O)(C₁₋₆-alquilo), -C(O)(C₃₋₁₄-carbociclo), -C₃₋₁₄-carbociclo, C₆₋₁₄-arilo, heterociclo o heterociclo(C₁₋₆-alquilo)- de entre 3 y 14 miembros (donde entre 1 y 4 miembros del anillo heterociclo son heteroátomos seleccionados entre N, O, y S), donde cada unidad alquilo, alcoxi, alquenilo, alquinilo, arilo, carbociclo, y heterociclo de R¹ y R² está opcionalmente sustituida con uno o más sustituyentes seleccionados entre el grupo que consiste en hidroxi, halo, -NH₂, -NHC(O)(OC₁₋₆-alquilo), -NO₂, -CN, oxo, -C(O)OH, -C(O)O(C₁₋₆-alquilo), -C₁₋₆-alquil(C₁₋₆-alcoxi), -C(O)NH₂, C₁₋₆-alquilo, -C(O)C₁₋₆-alquilo, -OC₁₋₆-alquilo, -Si(C₁₋₆-alquil)₃, C₆₋₁₄-arilo, -(C₁₋₆-alquil)(C₆₋₁₄-arilo), heterociclo o heterociclo(C₁₋₆-alquilo)- de entre 3 y 14 miembros (donde entre 1 y 4 miembros del anillo heterociclo son heteroátomos seleccionados entre N, O, y S), y -O(C₆₋₁₄-arilo), donde cada alquilo, arilo, y heterociclo en R¹ y R² está opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en hidroxi, -OC₁₋₆-alquilo, halo, -NH₂, -(C₁₋₆-alquil)NH₂, -C(O)OH, CN, y oxo.Claim 1: A compound characterized in that it is according to formula (1), or a pharmaceutically acceptable salt thereof; where RA is selected from the group consisting of H, C₁₋₆-alkyl, C₂₋₆-alkenyl, C₁₋₆-alkoxy, C₃₋₁₄-carbocycle, (C₃₋₁₄-carbocycle) -C₁₋₆-alkyl- , heterocycle or hetero-C₁₋₆-alkyl- of between 3 and 14 members (where between 1 and 4 members of the heterocycle ring are heteroatoms selected from N, O, and S), (heterocycle of between 3 and 14 members) oxy , C₆₋₁₄-aryl, (C₆₋₁₄-aryl) -C₁₋₆-alkyl-, C₆₋₁₄-aryloxy-, - (CH₂) ₀₋₆NR¹ (CH₂) ₀₋₆C₍O₎R², NR¹R², C (O) NR¹R², NR¹C (NR²) NR¹R², NR¹C (NR²) (= NR¹), SR¹, -CN, and -OH; wherein each alkyl, alkenyl, alkoxy, aryl, and heterocycle is optionally substituted with one or more substituents selected from the group consisting of R¹, OR¹, halo, -N = N-R¹, NR¹R², - (C₁₋₆-alkyl) NR¹R², -C (O) OR¹, -C (O) NR¹R², -OC (O) R¹, -CN, -OP (O) (OR¹) ₁₋₂, and oxo; RB is selected from the group consisting of H, C₂₋₆-alkenyl, and C₁₋₆-alkyl, where RB is optionally substituted with one or more R¹; RC, RD, and RE are independently selected from the group consisting of C₃₋₁₄-carbocycle, C₆₋₁₄-aryl, and heterocycle of between 3 and 14 members (where between 1 and 4 members of the heterocycle ring are selected heteroatoms between N, O, and S), where RC, RD, and RE are optionally substituted with one or more substituents selected from the group consisting of R¹, -OR¹, halo, -NR¹R², - (C₁₋₆-alkyl) - NR¹R², -C (O) OR¹, -C (O) NR¹R², -NO₂, -CN, and oxo; and R¹ and R² are independently selected from the group consisting of H, D (²H), -CN, -OH, C₁₋₆-alkyl, C₁₋₆-alkoxy, C₂₋₆-alkenyl, C₂₋₆- alkynyl, NH₂, -S (O) ₀₋₂- (C₁₋₆-alkyl), -S (O) ₀₋₂- (C₆₋₁₄-aryl), -C (O) (C₁₋₆-alkyl) , -C (O) (C₃₋₁₄-carbocycle), -C₃₋₁₄-carbocycle, C₆₋₁₄-aryl, heterocycle or heterocycle (C₁₋₆-alkyl) - from 3 to 14 members (where between 1 and 4 heterocycle ring members are heteroatoms selected from N, O, and S), where each alkyl, alkoxy, alkenyl, alkynyl, aryl, carbocycle, and heterocycle unit of R¹ and R² is optionally substituted with one or more substituents selected from the group that consists of hydroxy, halo, -NH₂, -NHC (O) (OC₁₋₆-alkyl), -NO₂, -CN, oxo, -C (O) OH, -C (O) O (C₁₋₆-alkyl) , -C₁₋₆-alkyl (C₁₋₆-alkoxy), -C (O) NH₂, C₁₋₆-alkyl, -C (O) C₁₋₆-alkyl, -OC₁₋₆-alkyl, -Si (C₁ ₋₆-al quil) ₃, C₆₋₁₄-aryl, - (C₁₋₆-alkyl) (C₆₋₁₄-aryl), heterocycle or heterocycle (C₁₋₆-alkyl) - of between 3 and 14 members (where between 1 and 4 members of the heterocycle ring are heteroatoms selected from N, O, and S), and -O (C₆₋₁₄-aryl), where each alkyl, aryl, and heterocycle in R¹ and R² is optionally substituted with one or more substituents selected from the group consisting of hydroxy, -OC₁₋₆-alkyl, halo, -NH₂, - (C₁₋₆-alkyl) NH₂, -C (O) OH, CN, and oxo.

ARP170102433A 2016-08-31 2017-08-31 INHIBITORS OF CELLULAR METABOLIC PROCESSES AR109495A1 (en)

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PCT/CN2016/097524 WO2018039972A1 (en) 2016-08-31 2016-08-31 Inhibitors of cellular metabolic processes

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AR109495A1 true AR109495A1 (en) 2018-12-12

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MX2022006281A (en) 2019-11-25 2022-06-08 Amgen Inc HETEROCYCLIC COMPOUNDS AS DELTA-5 DESATURASE INHIBITORS AND METHODS OF USE.
WO2021139775A1 (en) * 2020-01-10 2021-07-15 江苏先声药业有限公司 Pyridone compound and application
US20230257359A1 (en) * 2020-06-10 2023-08-17 Ideaya Biosciences, Inc. 4-arylquinazoline derivatives as methionine adenosyltransferase 2a inhibitors
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WO2021252678A1 (en) * 2020-06-10 2021-12-16 Ideaya Biosciences, Inc. Heteroaryl alkylene substituted 2-oxoquinazoline derivatives as methionine adenosyltransferase 2a inhibitors
WO2021252681A1 (en) * 2020-06-10 2021-12-16 Ideaya Biosciences, Inc. Quinolinone derivatives as methionine adenosyltransferase 2a inhibitors
WO2021254529A1 (en) * 2020-07-14 2021-12-23 江苏先声药业有限公司 Bicyclic compound
CN113999232B (en) * 2020-07-28 2025-01-07 南京正大天晴制药有限公司 MAT2A inhibitors
CN116568677A (en) 2020-07-31 2023-08-08 探戈医药股份有限公司 Piperidin-1-yl-N-pyridin-3-yl-2-oxoacetamide derivatives useful in the treatment of MTAP deficiency and/or MTA accumulation cancers
AR123228A1 (en) * 2020-08-12 2022-11-09 Servier Pharmaceuticals Llc SOLID STATE FORMS OF AN ORGANIC COMPOUND
CN116782903A (en) * 2020-10-15 2023-09-19 南京再明医药有限公司 Substituted pyridone compounds and uses thereof
TW202237610A (en) * 2020-11-25 2022-10-01 法商施維雅藥廠 New organic compounds
US20240124454A1 (en) 2020-12-31 2024-04-18 Nanjing Zaiming Pharmaceutical Co., Ltd. Tricyclic compound and use thereof
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CN116283994B (en) * 2021-12-20 2025-01-07 艾立康药业股份有限公司 Heterocyclic compounds as MAT2A inhibitors
US20250145628A1 (en) * 2022-02-15 2025-05-08 Novo Nordisk A/S Pyrazolopyrimidines, compositions comprising them and uses thereof
WO2023185811A1 (en) 2022-03-29 2023-10-05 首药控股(北京)股份有限公司 Novel heterocyclic compound
CN120865217A (en) 2022-06-27 2025-10-31 石药集团中奇制药技术(石家庄)有限公司 Tricyclic compounds and uses thereof
CN116425721B (en) * 2022-12-19 2024-02-02 艾立康药业股份有限公司 Bicyclic compounds as MAT2A inhibitors
WO2024153244A1 (en) * 2023-01-20 2024-07-25 南京再明医药有限公司 Nitrogen-containing compound
WO2025166215A1 (en) 2024-02-02 2025-08-07 Ideaya Biosciences, Inc. Triheterocyclic guanidino compounds as prmt5 inhibitors
WO2025166260A1 (en) 2024-02-02 2025-08-07 Ideaya Biosciences, Inc. Amide substituted tricyclic guanidino compounds as prmt5 inhibitors
WO2025166229A1 (en) 2024-02-02 2025-08-07 Ideaya Biosciences, Inc. Tricyclic amidino compounds as prmt5 inhibitors
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