AR125477A1 - Compuestos heterocíclicos capaces de activar sting - Google Patents

Compuestos heterocíclicos capaces de activar sting

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Publication number
AR125477A1
AR125477A1 ARP220101113A ARP220101113A AR125477A1 AR 125477 A1 AR125477 A1 AR 125477A1 AR P220101113 A ARP220101113 A AR P220101113A AR P220101113 A ARP220101113 A AR P220101113A AR 125477 A1 AR125477 A1 AR 125477A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
heterocyclyl containing
membered bicyclic
atom
Prior art date
Application number
ARP220101113A
Other languages
English (en)
Inventor
Sebastian Carotta
Georg Dahmann
Cdrickx Godbout
Sandra Ruth Handschuh
Herbert Nar
Thorsten Oost
Ulrich Reiser
Matthias Treu
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR125477A1 publication Critical patent/AR125477A1/es

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    • 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
    • C07D401/14Heterocyclic 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 three or more hetero 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
    • A61K31/435Heterocyclic 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • 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
    • 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
    • A61P37/08Antiallergic agents
    • 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • 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
    • C07D495/02Heterocyclic 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 two hetero rings
    • C07D495/10Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Compuestos heterocíclicos de la fórmula (1) capaces de activar STING (estimulador de genes de interferón). Reivindicación 1: Un compuesto caracterizado porque tienen la fórmula (1) en donde A es N o C, B es un grupo seleccionado del grupo que consiste en un heterociclilo monocíclico de 5 - 7 miembros que contiene 1 o 2 átomos de N, un heterociclilo bicíclico de 6 miembros que contiene 1 átomo de N, un heterociclilo bicíclico de 7 - 11 miembros que contiene 2 átomos de N, un heterociclilo bicíclico de 7 miembros que contiene 1 átomo de N y 1 átomo de O, un heterociclilo monocíclico de 6 miembros que contiene 1 átomo de N y 1 heteroátomo seleccionado del grupo que consiste en O y S, un heterociclilo bicíclico de 9 miembros que contiene 3 heteroátomos, 2 de los cuales son N y el otro es O, un heterociclilo bicíclico de 9 miembros que contiene 1 átomo de N y 1 átomo de S, un heterociclilo bicíclico de 10 miembros que contiene 3 átomos de N, 2 de los cuales están sustituidos con C₁₋₆ alquilo, fenilo, un heterociclilo bicíclico de 9 miembros que contiene 3 átomos de N, -C₁₋₄-alquileno-pirimidina, y -C₁₋₄-alquileno-O-C₁₋₃-alquilo; D es un grupo seleccionado del grupo que consiste en un heterociclilo bicíclico de 9 miembros que contiene 2 átomos de N, un heterociclilo bicíclico de 10 miembros que contiene 1 átomo de N, y benzodioxol; R¹ se selecciona del grupo que consiste en -H, -C₁₋₆-alquilo, -CF₃, -C₂₋₆- alquinilo, -O-C₁₋₆-alquilo y halógeno; R² se selecciona del grupo que consiste en -H, -C₁₋₆-alquilo, -C₁₋₆-alquilenoOH, -C(O)OH, -C(O)O-C₁₋₆-alquilo y -pirazolilo-C₁₋₆-alquilo; R³ es -H o -C₁₋₆-alquilo; R⁴ se selecciona del grupo que consiste en -H, -C₁₋₃-alquilo, -NH₂, -NHC₁₋₃- alquilo y N(C₁₋₃-alquilo)₂; R⁵ está ausente o se selecciona del grupo que consiste en -H, -C₁₋₆-alquilo, - S(O₂)-C₁₋₆-alquilo, -NH-S(O₂)-C₁₋₆-alquilo, =O, -C(O)-C₁₋₆-alquilo, -C(O)H, - C(O)OH, -C(O)NH₂, -C(O)O-C₁₋₆-alquilo, -NR⁵.¹R⁵.², -C₁₋₆-alquileno-C(O)OH, -S(O₂)- NH₂, -pirolidin-2-ona-1-ilo, -tetrazolilo, y un heteroarilo de 5 miembros con 1 o 2 heteroátomos seleccionados del grupo que consiste en N y O, sustituido con R⁵.³; R⁵.¹ se selecciona del grupo que consiste en -H, -C₁₋₆-alquilo, -C(O)-C₁₋₆-alquilo y -C₁₋₆-alquileno-O-C₁₋₆-alquilo; R⁵.² se selecciona del grupo que consiste en -H, -C₁₋₆-alquilo, -C(O)-C₁₋₆- alquilo, -C₁₋₆-alquileno-O-C₁₋₆-alquilo y -C₁₋₆-alqileno-R⁵.³; R⁵.³ se selecciona del grupo que consiste en -H, -C₁₋₆-alquilo y un heteroarilo de 6 miembros con 1 o 2 heteroátomos seleccionados de un grupo que consiste en N y O; R⁶ está ausente o se selecciona del grupo que consiste en -H, -C₁₋₆-alquilo, =O y -C(O)OH; o una sal de este. Reivindicación 15: Una composición farmacéutica caracterizada porque comprende al menos un compuesto de acuerdo con cualquiera de las reivindicaciones 1 a 11 o una sal aceptable desde el punto de vista farmacéutico de este y un portador aceptable desde el punto de vista farmacéutico.
ARP220101113A 2021-04-29 2022-04-28 Compuestos heterocíclicos capaces de activar sting AR125477A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP21171155 2021-04-29

Publications (1)

Publication Number Publication Date
AR125477A1 true AR125477A1 (es) 2023-07-19

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US (2) US12065427B2 (es)
EP (1) EP4330250A1 (es)
JP (1) JP2024514361A (es)
KR (1) KR20240004646A (es)
CN (2) CN118546123A (es)
AR (1) AR125477A1 (es)
AU (1) AU2022265323C1 (es)
BR (1) BR112023017873A2 (es)
CA (1) CA3214127A1 (es)
CL (1) CL2023002959A1 (es)
CO (1) CO2023014672A2 (es)
CR (1) CR20230509A (es)
DO (1) DOP2023000234A (es)
EC (1) ECSP23069018A (es)
IL (1) IL307977A (es)
MX (1) MX2023012800A (es)
PE (1) PE20240069A1 (es)
TW (1) TW202309031A (es)
WO (1) WO2022229341A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024089155A1 (en) * 2022-10-28 2024-05-02 Boehringer Ingelheim International Gmbh Heterocyclic compounds as sting antagonists
WO2024209363A1 (en) 2023-04-06 2024-10-10 Pfizer Inc. Substituted indazole propionic acid derivative compounds and uses thereof as ampk activators

Family Cites Families (13)

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AR090151A1 (es) 2012-03-07 2014-10-22 Lilly Co Eli Compuestos inhibidores de raf
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
TWI848953B (zh) 2018-06-09 2024-07-21 德商百靈佳殷格翰國際股份有限公司 針對癌症治療之多特異性結合蛋白
EP3817820A1 (en) 2018-07-03 2021-05-12 IFM Due, Inc. Compounds and compositions for treating conditions associated with sting activity
TW202028183A (zh) 2018-10-10 2020-08-01 大陸商江蘇豪森藥業集團有限公司 含氮雜芳類衍生物調節劑、其製備方法和應用
SG11202103573YA (en) 2018-10-11 2021-05-28 Ono Pharmaceutical Co STING Agonistic Compound
CN113563313B (zh) * 2019-01-31 2022-11-04 成都先导药物开发股份有限公司 一种免疫调节剂
CN112521394A (zh) * 2019-09-19 2021-03-19 中国药科大学 杂环酰胺类化合物、其可药用的盐及其制备方法和用途
CA3155569A1 (en) * 2019-09-25 2021-04-01 Pfizer Inc. Polyheterocyclic modulators of sting (stimulator of interferon genes)
TW202128756A (zh) 2019-10-02 2021-08-01 德商百靈佳殷格翰國際股份有限公司 用於癌症治療之多重專一性結合蛋白
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CN114761394B (zh) 2020-01-16 2024-03-29 浙江海正药业股份有限公司 吡啶或嘧啶类衍生物及其制备方法和用途
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CN118546123A (zh) 2024-08-27
EP4330250A1 (en) 2024-03-06
US12065427B2 (en) 2024-08-20
US20240270718A1 (en) 2024-08-15
BR112023017873A2 (pt) 2023-12-12
CR20230509A (es) 2023-12-07
CA3214127A1 (en) 2022-11-03
AU2022265323C1 (en) 2024-09-12
DOP2023000234A (es) 2023-11-30
KR20240004646A (ko) 2024-01-11
AU2022265323A1 (en) 2023-09-14
MX2023012800A (es) 2023-11-08
WO2022229341A1 (en) 2022-11-03
AU2022265323B2 (en) 2024-05-16
ECSP23069018A (es) 2023-10-31
PE20240069A1 (es) 2024-01-11
TW202309031A (zh) 2023-03-01
CN117255784A (zh) 2023-12-19
CL2023002959A1 (es) 2024-03-01
JP2024514361A (ja) 2024-04-01
IL307977A (en) 2023-12-01
CO2023014672A2 (es) 2023-11-10
US20220388986A1 (en) 2022-12-08

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