AR121573A1 - Moduladores de nlrp3 - Google Patents

Moduladores de nlrp3

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Publication number
AR121573A1
AR121573A1 ARP210100650A ARP210100650A AR121573A1 AR 121573 A1 AR121573 A1 AR 121573A1 AR P210100650 A ARP210100650 A AR P210100650A AR P210100650 A ARP210100650 A AR P210100650A AR 121573 A1 AR121573 A1 AR 121573A1
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AR
Argentina
Prior art keywords
alkyl
hydrogen
haloalkyl
halogen
independently selected
Prior art date
Application number
ARP210100650A
Other languages
English (en)
Inventor
Raju Mohan
John Nuss
Jason Harris
Shendong Yuan
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Zomagen Biosciences Ltd
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Publication date
Application filed by Zomagen Biosciences Ltd filed Critical Zomagen Biosciences Ltd
Publication of AR121573A1 publication Critical patent/AR121573A1/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
    • C07D491/12Heterocyclic 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 three hetero rings
    • C07D491/18Bridged systems
    • 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/18Bridged 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • 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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/18Bridged 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
    • C07D495/12Heterocyclic 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 three hetero rings
    • C07D495/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/18Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Amplifiers (AREA)
  • Burglar Alarm Systems (AREA)

Abstract

Reivindicación 1: Un compuesto de la fórmula (1) o una sal o solvato farmacéuticamente aceptable de este, caracterizado por que: X¹ es O, S o N(R³); X² es -N(R⁴)- o -C(R⁴)₂-; X³ es -N(R⁵)- o -C(R⁵)₂-; Y¹ es O, S o N(R⁸); Y² es N o C(R⁹); Z¹ es O, S, N(R³), o -C(R¹⁷)=C(R¹⁷)-; Z² es N o C(R¹⁹); R¹ es un compuesto del grupo de fórmulas (2); R² es un compuesto del grupo de fórmulas (3); R³ es hidrógeno, -OR¹⁴, -CN, -NO₂ o -S(=O)₂R¹⁵; cada R⁴ se selecciona independientemente de hidrógeno, alquilo C₁₋₆, alquilo -C₁₋₆-OR⁷ y alquilo -C₁₋₆-N(R⁷)₂; cada R⁵ se selecciona independientemente de hidrógeno, alquilo C₁₋₆, alquilo -C₁₋₆-OR⁷ y alquilo -C₁₋₆-N(R⁷)₂; cada R⁶ se selecciona independientemente de alquilo C₁₋₆, alquilo -C₁₋₆-CO₂R¹⁸, haloalquilo C₁₋₆, alquilo -C₁₋₆-OR⁷ y alquilo C₁₋₆-N(R⁷)₂; cada R⁷ se selecciona de independientemente de hidrógeno y alquilo C₁₋₆; R⁸ es hidrógeno, alquilo C₁₋₆, alquilo -C₁₋₆-OR⁷, alquilo -C₁₋₆-N(R⁷)₂ o cicloalquilo C₃₋₆; R⁹ es hidrógeno, halógeno, alquilo C₁₋₆, haloalquilo C₁₋₆ y cicloalquilo C₃₋₆; R¹⁰ es hidrógeno, halógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, alquilo -C₁₋₆-OR⁷ o alquilo -C₁₋₆-N(R⁷)₂; R¹¹ y R¹² se seleccionan independientemente de hidrógeno, halógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, alquilo -C₁₋₆-OR⁷ y alquilo C₁₋₆-N(R⁷)₂; o R¹¹ y R¹² se combinan para formar un anillo cicloalquilo de 5 ó 6 miembros; R¹³ es hidrógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₅, heterocicloalquilo C₂₋₉, fenilo o heteroarilo C₂₋₉, donde el cicloalquilo C₃₋₅, heterocicloalquilo C₂₋₉, fenilo y heteroarilo C₂₋₉ están opcionalmente sustituidos con 1, 2, 3 ó 4 R¹⁶; R¹⁴ es hidrógeno o alquilo C₁₋₆; R¹⁵ es alquilo C₁₋₆; o cada R¹⁶ se selecciona independientemente de halógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, haloalcoxi C₁₋₆, cicloalquilo C₃₋₆, heterocicloalquilo C₂₋₉, arilo C₆₋₁₀, heteroarilo C₂₋₉, donde el cicloalquilo C₃₋₆, heterocicloalquilo C₂₋₉, arilo C₆₋₁₀ y el heteroarilo C₂₋₉ están opcionalmente sustituidos con 1, 2 ó 3 grupos seleccionados entre halógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆ y haloalcoxi C₁₋₆; cada R¹⁷ se selecciona independientemente de hidrógeno, halógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, alquilo -C₁₋₆-OR⁷ y alquilo -C₁₋₆-N(R⁷)₂; R¹⁸ es hidrógeno o alquilo C₁₋₆; R¹⁹ es hidrógeno, halógeno, -CN, alquilo C₁₋₆, haloalquilo C₁₋₆, alquilo -C₁₋₆-OR⁷ o alquilo -C₁₋₆-N(R⁷)₂; m es 0, 1 ó 2; n es 1, 2 ó 3; p es 0, 1 ó 2; q es 0, 1, 2, 3 ó 4; s es 1, 2 ó 3; y t es 1, 2 ó 3.
ARP210100650A 2020-03-16 2021-03-15 Moduladores de nlrp3 AR121573A1 (es)

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US202062990363P 2020-03-16 2020-03-16

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AR121573A1 true AR121573A1 (es) 2022-06-15

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US (3) US11603375B2 (es)
EP (1) EP4121059A4 (es)
JP (1) JP2023518044A (es)
KR (1) KR20220154165A (es)
CN (1) CN115605209A (es)
AR (1) AR121573A1 (es)
AU (1) AU2021237477A1 (es)
BR (1) BR112022018480A2 (es)
CA (1) CA3175729A1 (es)
CL (1) CL2022002531A1 (es)
CO (1) CO2022014499A2 (es)
IL (1) IL296488A (es)
MX (1) MX2022011576A (es)
TW (1) TW202200584A (es)
WO (1) WO2021188450A1 (es)

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AR121573A1 (es) 2020-03-16 2022-06-15 Zomagen Biosciences Ltd Moduladores de nlrp3
CN117279903A (zh) * 2021-02-10 2023-12-22 杭州英创医药科技有限公司 作为nlrp3抑制剂的化合物

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3578547T3 (pl) 2015-02-16 2021-12-20 The University Of Queensland Pochodne sulfonylomocznika i związki pokrewne oraz ich zastosowanie
US11858922B2 (en) 2016-02-16 2024-01-02 The University Of Queensland Sulfonylureas and related compounds and use of same
MA44734A (fr) 2016-04-18 2021-05-19 Novartis Ag Composés et compositions destinés au traitement d'états associés à une activité de nlrp
EP3571187B1 (en) * 2017-01-23 2023-11-22 Genentech, Inc. Chemical compounds as inhibitors of interleukin-1 activity
JP7072586B2 (ja) * 2017-05-24 2022-05-20 ザ ユニバーシティ オブ クィーンズランド 新規な化合物及び使用
PL3661925T3 (pl) * 2017-07-07 2022-02-28 Inflazome Limited Nowe związki sulfonamidowo karboksyamidowe
US11542255B2 (en) 2017-08-15 2023-01-03 Inflazome Limited Sulfonylureas and sulfonylthioureas as NLRP3 inhibitors
KR20200041919A (ko) 2017-08-15 2020-04-22 인플라좀 리미티드 Nlrp3 저해제로서의 설포닐유레아 및 설포닐티오유레아
CN111417622A (zh) 2017-10-17 2020-07-14 诺华炎症研究公司 用于治疗与nlrp活性相关的病症的磺胺类及其组合物
GB201721185D0 (en) * 2017-12-18 2018-01-31 Nodthera Ltd Sulphonyl urea derivatives
CN112513048A (zh) * 2018-07-20 2021-03-16 豪夫迈·罗氏有限公司 作为白细胞介素-1活性抑制剂的磺酰亚胺酰胺类化合物
WO2020086732A1 (en) 2018-10-24 2020-04-30 Novartis Inflammasome Research, Inc. Compounds and compositions for treating conditions associated with nlrp activity
JP2022541254A (ja) 2019-07-17 2022-09-22 ズーマゲン バイオサイエンシーズ エルティーディー 多発性硬化症(MS)の治療のためのNLPR3モジュレーターとしてのN-((1,2,3,5,6,7-ヘキサヒドロ-s-インダセン-4-イル)カルバモイル)-4,5,6,7-テトラヒドロベンゾフラン-2-スルホンアミド誘導体および関連化合物
US20220259170A1 (en) 2019-07-17 2022-08-18 Zomagen Biosciences Ltd Nlrp3 modulators
AR121573A1 (es) 2020-03-16 2022-06-15 Zomagen Biosciences Ltd Moduladores de nlrp3

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US20240101571A1 (en) 2024-03-28
EP4121059A1 (en) 2023-01-25
MX2022011576A (es) 2022-10-18
WO2021188450A1 (en) 2021-09-23
IL296488A (en) 2022-11-01
KR20220154165A (ko) 2022-11-21
CL2022002531A1 (es) 2023-03-31
CO2022014499A2 (es) 2023-02-16
EP4121059A4 (en) 2023-12-13
CA3175729A1 (en) 2021-09-23
AU2021237477A1 (en) 2022-10-13
JP2023518044A (ja) 2023-04-27
CN115605209A (zh) 2023-01-13
US20210292336A1 (en) 2021-09-23
BR112022018480A2 (pt) 2022-11-29
US11603375B2 (en) 2023-03-14
TW202200584A (zh) 2022-01-01
US20230183258A1 (en) 2023-06-15

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