AR120856A1 - Derivados de furoindazol - Google Patents

Derivados de furoindazol

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Publication number
AR120856A1
AR120856A1 ARP200103594A ARP200103594A AR120856A1 AR 120856 A1 AR120856 A1 AR 120856A1 AR P200103594 A ARP200103594 A AR P200103594A AR P200103594 A ARP200103594 A AR P200103594A AR 120856 A1 AR120856 A1 AR 120856A1
Authority
AR
Argentina
Prior art keywords
alkyl
phenyl
heteroaryl
haloalkyl
heterocycloalkyl
Prior art date
Application number
ARP200103594A
Other languages
English (en)
Inventor
Olaf Panknin
Frank Sacher
Nicole Schmidt
Gernot Langer
Katrin Nowak-Reppel
Reinhard Nubbemeyer
Sabine Pilari
Antje Rottmann
Ondozabal Hideki Miyatake
Holger Siebeneicher
Laak Antonius Ter
Hana Cernecka
Original Assignee
Bayer 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
Application filed by Bayer Ag filed Critical Bayer Ag
Publication of AR120856A1 publication Critical patent/AR120856A1/es

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    • 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles 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
    • A61K31/435Heterocyclic 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
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La presente cubre compuestos de furoindazol de fórmula general (1) en la cual R¹, R², R³, R⁴, R⁵, R⁶, R⁷ᵃ y R⁷ᵇ son como se define en la presente, métodos para preparar dichos compuestos, compuestos intermediarios útiles para preparar dichos compuestos, composiciones farmacéuticas que comprenden dichos compuestos y el uso de dichos compuestos para elaborar composiciones farmacéuticas para el tratamiento o la profilaxis de enfermedades, en particular de enfermedades autoinmunes tales como esclerosis múltiple, psoriasis, artritis psoriásica, artritis reumatoidea, espondilitis anquilosante, lupus eritematoso sistémico, uveítis autoinmune primaria y secundaria, trastornos inflamatorios como endometriosis, enfermedades oculares inflamatorias, enfermedades renales inflamatorias, enfermedades hepáticas inflamatorias como enfermedades hepáticas no alcohólicas, alcohólicas y de hígado graso tóxicas, enfermedades pulmonares como asma, fibrosis pulmonar idiopática, enfermedad pulmonar obstructiva crónica, y trastornos metabólicos y metabólico- endocrinos como síndrome metabólico, resistencia a la insulina, diabetes mellitus tipo I y tipo II, y trastornos de síndrome de ovario poliquístico (PCOS), trastornos de dolor neuropático e inflamatorio en humanos y animales. Reivindicación 1: Un compuesto de fórmula general (1) en la cual: R¹ representa hidrógeno, alquilo-C₁₋₄ o haloalquilo-C₁₋₄; R² representa hidrógeno, alquilo-C₁₋₄ o haloalquilo-C₁₋₄; o R¹ y R² junto con el átomo de carbono al cual están unidos forman un anillo cicloalquilo o heterocicloalquilo de 3 a 6 miembros; R³ representa cicloalquilo-C₃₋₆, heterocicloalquilo de 3 a 6 miembros, heterocicloalquilo fusionado con fenilo o heteroarilo, o heteroarilo, en donde dichos grupos están opcionalmente sustituidos, una o varias veces, independientemente entre sí, con R⁸, o R³ representa fenilo, que está opcionalmente sustituido, una o varias veces, independientemente entre sí, con R⁸, y adicionalmente R⁷ᵃ y R⁷ᵇ representan deuterio; R⁴ representa hidrógeno, alquilo-C₁₋₄, haloalquilo-C₁₋₄ o cicloalquilo-C₃₋₆; R⁵, R⁶ representan, independientemente entre sí, hidrógeno, alquilo-C₁₋₄, hidroxialquilo-C₂₋₄, (alcoxi-C₁₋₄)-(alquilo-C₂₋₄)-, cicloalquilo-C₃₋₆, haloalquilo-C₁₋₄, halocicloalquilo-C₃₋₆, heterocicloalquilo de 3 a 6 miembros, heteroespirocicloalquilo, fenilo, heteroarilo, heterocicloalquilo fusionado con fenilo o heteroarilo, heterocicloalquil-(alquilo-C₁₋₃) de 3 a 6 miembros, heteroespirocicloalquil-(alquilo-C₁₋₃), (heterocicloalquilo fusionado con fenilo o heteroaril)-(alquilo-C₁₋₃)-, fenil-(alquilo-C₁₋₃)- o heteroaril-(alquilo-C₁₋₃)-, en donde dichos grupos heterocicloalquilo de 3 a 6 miembros, heteroespirocicloalquilo, heterocicloalquilo fusionado con fenilo o heteroarilo, fenilo o heteroarilo están opcionalmente sustituidos, una o varias veces, independientemente entre sí, con R⁹, o R⁵ y R⁶ junto con el átomo de nitrógeno al cual están unidos forman un anillo heterocíclico de 3 a 6 miembros que contiene nitrógeno, que opcionalmente contiene un heteroátomo o grupo que contiene heteroátomo adicional seleccionado de O, NH y S, y que puede estar opcionalmente sustituido, una o varias veces, independientemente entre sí, con R⁹; R⁷ᵃ representa hidrógeno, deuterio o alquilo-C₁₋₄; R⁷ᵇ representa hidrógeno, deuterio o alquilo-C₁₋₄; R⁸ representa halógeno, ciano, alquilo-C₁₋₄, haloalquilo-C₁₋₄, alcoxi-C₁₋₃, haloalcoxi-C₁₋₃, cicloalquilo-C₃₋₆, cicloalquil-C₃₋₆-(alquilo-C₁₋₃)-, R¹³-(C=O)-, R¹⁰-O-(C=O)-, R¹¹-NH-(C=O)- o R¹²-(SO₂)-; R⁹ representa halógeno, ciano, alquilo-C₁₋₄, haloalquilo-C₁₋₄, H₂N-alquilo-C₁₋₄, alcoxi-C₁₋₃, haloalcoxi-C₁₋₃, cicloalquilo-C₃₋₆, R¹⁰-O-(C=O)-, oxo, heterocicloalquilo- de 5 a 6 miembros, heterocicloalquil-(alquilo-C₁₋₃)- de 5 a 6 miembros, fenilo o heteroarilo, en donde dicho grupo fenilo o heteroarilo está opcionalmente sustituido, una o varias veces, independientemente entre sí, con halógeno, alquilo-C₁₋₄, haloalquilo-C₁₋₄, alcoxi-C₁₋₃ o haloalcoxi-C₁₋₃; R¹⁰ representa hidrógeno, alquilo-C₁₋₄ o fenilo-CH₂-; R¹¹ representa hidrógeno, alquilo-C₁₋₄, o heterocicloalquil-(alquilo-C₁₋₃)- de 5 a 6 miembros; R¹² representa alquilo-C₁₋₄ o fenilo; R¹³ representa alquilo-C₁₋₄, haloalquilo-C₁₋₄, (alcoxi-C₁₋₄)-(alquilo-C₁₋₄)-, alquilo-C₁₋₄-(C=O)-, cicloalquilo-C₃₋₆ o fenilo, en donde dicho grupo cicloalquilo-C₃₋₆ está opcionalmente sustituido con alquilo-C₁₋₄ o hidroxi y dicho grupo fenilo está opcionalmente sustituido, una o varias veces, independientemente entre sí, con halógeno, alquilo-C₁₋₄, haloalquilo-C₁₋₄, alcoxi-C₁₋₃ o haloalcoxi-C₁₋₃; o un estereoisómero, un tautómero, un N-óxido, un hidrato, un solvato o una sal de dicho compuesto, o una mezcla de ellos.
ARP200103594A 2019-12-19 2020-12-21 Derivados de furoindazol AR120856A1 (es)

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EP19217856 2019-12-19

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AR120856A1 true AR120856A1 (es) 2022-03-23

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US (1) US20230112499A1 (es)
EP (1) EP4077334A1 (es)
JP (1) JP2023508908A (es)
KR (1) KR20220118480A (es)
CN (1) CN115135656B (es)
AR (1) AR120856A1 (es)
AU (1) AU2020408908A1 (es)
BR (1) BR112022011237A2 (es)
CA (1) CA3164963A1 (es)
CL (1) CL2022001644A1 (es)
CO (1) CO2022008338A2 (es)
CR (1) CR20220291A (es)
DO (1) DOP2022000126A (es)
EC (1) ECSP22047527A (es)
GE (1) GEP20247585B (es)
IL (1) IL293968A (es)
JO (1) JOP20220156A1 (es)
MX (1) MX2022007685A (es)
PE (1) PE20221786A1 (es)
TW (1) TW202136271A (es)
WO (1) WO2021122415A1 (es)

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CN118638043A (zh) 2019-12-19 2024-09-13 阿尔维纳斯运营股份有限公司 用于雄激素受体的靶向降解的化合物和方法
EP4298102A1 (en) * 2021-02-23 2024-01-03 Bayer Aktiengesellschaft Furoindazole derivatives as gpr84 antagonists
WO2022194267A1 (zh) * 2021-03-18 2022-09-22 武汉人福创新药物研发中心有限公司 一种gpr84拮抗剂及其制备方法和用途
WO2022229061A1 (en) * 2021-04-29 2022-11-03 Bayer Aktiengesellschaft Furoindazole derivatives as antagonists or inhibitors of gpr84
WO2024083705A1 (en) 2022-10-18 2024-04-25 Bayer Aktiengesellschaft Furoindazole derivatives for the treatment of pain
WO2024140969A1 (zh) * 2022-12-30 2024-07-04 广州市联瑞制药有限公司 三环类化合物及其制备方法和应用

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CN115135656A (zh) 2022-09-30
CN115135656B (zh) 2024-06-14
KR20220118480A (ko) 2022-08-25
CL2022001644A1 (es) 2023-02-24
EP4077334A1 (en) 2022-10-26
WO2021122415A9 (en) 2022-06-30
GEP20247585B (en) 2024-01-25
ECSP22047527A (es) 2022-07-29
JP2023508908A (ja) 2023-03-06
CR20220291A (es) 2022-08-10
CA3164963A1 (en) 2021-06-24
US20230112499A1 (en) 2023-04-13
MX2022007685A (es) 2022-07-19
PE20221786A1 (es) 2022-11-22
DOP2022000126A (es) 2022-07-15
CO2022008338A2 (es) 2022-07-08
AU2020408908A1 (en) 2022-06-30
WO2021122415A1 (en) 2021-06-24
TW202136271A (zh) 2021-10-01
JOP20220156A1 (ar) 2023-01-30
BR112022011237A2 (pt) 2022-08-30
IL293968A (en) 2022-08-01

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