CN114728177B - 作为Kv1.3钾Shaker通道阻滞剂的芳基杂二环化合物 - Google Patents

作为Kv1.3钾Shaker通道阻滞剂的芳基杂二环化合物 Download PDF

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CN114728177B
CN114728177B CN202080084476.1A CN202080084476A CN114728177B CN 114728177 B CN114728177 B CN 114728177B CN 202080084476 A CN202080084476 A CN 202080084476A CN 114728177 B CN114728177 B CN 114728177B
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pharmaceutically acceptable
compound
acceptable salt
alkyl
certain embodiments
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CN114728177A (zh
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F·焦尔达内托
M·O·詹森
V·乔吉尼
R·J·斯诺
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DE Shaw Research LLC
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/12—Heterocyclic 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
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

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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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
CN202080084476.1A 2019-10-07 2020-10-06 作为Kv1.3钾Shaker通道阻滞剂的芳基杂二环化合物 Active CN114728177B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962911642P 2019-10-07 2019-10-07
US62/911642 2019-10-07
PCT/US2020/054348 WO2021071803A1 (en) 2019-10-07 2020-10-06 Aryl heterobicyclic compounds as kv1.3 potassium shaker channel blockers

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CN114728177A CN114728177A (zh) 2022-07-08
CN114728177B true CN114728177B (zh) 2025-06-24

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Country Link
US (1) US20230040182A1 (https=)
EP (1) EP4041408A4 (https=)
JP (1) JP7780439B2 (https=)
KR (1) KR20220079575A (https=)
CN (1) CN114728177B (https=)
AU (1) AU2020363354A1 (https=)
BR (1) BR112022006250A2 (https=)
CA (1) CA3156981C (https=)
IL (1) IL291867A (https=)
MX (1) MX2022004144A (https=)
WO (1) WO2021071803A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2023003841A (es) 2020-10-06 2023-06-23 De Shaw Res Llc Compuestos lactámicos como bloqueadores del canal agitador de potasio kv1.3.
CN114437070A (zh) * 2022-01-19 2022-05-06 广西-东盟食品检验检测中心 一种他达拉非新型衍生物的制备方法
WO2024088343A1 (zh) * 2022-10-28 2024-05-02 上海深势唯思科技有限责任公司 一种芳基杂环类Kv1.3抑制剂及其制备方法和用途
TW202521512A (zh) 2023-07-31 2025-06-01 美商美國禮來大藥廠 Kv1.3鉀shaker通道阻斷劑之固體形式及其使用方法
WO2026021011A1 (zh) * 2024-07-26 2026-01-29 浙江海正药业股份有限公司 芳基三环类衍生物及其制备方法和用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102333782A (zh) * 2008-12-12 2012-01-25 雅培卫生保健产品有限责任公司 作为Kv1.3钾通道阻断剂的螺氮杂环庚烷-噁唑烷酮
CN107548396A (zh) * 2015-03-13 2018-01-05 4Sc股份公司 Kv1.3抑制剂及其医学应用

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Publication number Priority date Publication date Assignee Title
WO2001007052A1 (en) * 1999-07-21 2001-02-01 Boehringer Ingelheim Pharmaceuticals, Inc. Small molecules useful in the treatment of inflammatory disease
US6348486B1 (en) * 2000-10-17 2002-02-19 American Home Products Corporation Methods for modulating bladder function
US6939968B2 (en) * 2002-12-23 2005-09-06 Bristol-Myers Squibb Company Atropisomers of 3-substituted-4-arylquinolin-2-one derivatives
WO2005030729A1 (en) * 2003-09-23 2005-04-07 Merck & Co., Inc. Isoquinoline potassium channel inhibitors
CN100530013C (zh) * 2005-03-04 2009-08-19 松下电器产业株式会社 电子设备控制装置及其控制方法
US7538110B2 (en) * 2005-10-27 2009-05-26 Adolor Corporation Opioid antagonists
US8124636B2 (en) * 2008-04-30 2012-02-28 Hoffmann-La Roche Inc. Imidazolidinone derivatives as 11B-HSD1 inhibitors
WO2011073273A1 (en) * 2009-12-16 2011-06-23 Evotec Ag Benzoxazine aryl sulfonamide derivatives as kv1.3 modulators
US20120065210A1 (en) * 2010-09-15 2012-03-15 Xin-Jie Chu Substituted hexahydropyrrolo[1,2-c]imidazolones

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102333782A (zh) * 2008-12-12 2012-01-25 雅培卫生保健产品有限责任公司 作为Kv1.3钾通道阻断剂的螺氮杂环庚烷-噁唑烷酮
CN107548396A (zh) * 2015-03-13 2018-01-05 4Sc股份公司 Kv1.3抑制剂及其医学应用

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Publication number Publication date
EP4041408A1 (en) 2022-08-17
CA3156981C (en) 2025-06-17
IL291867A (en) 2022-06-01
WO2021071803A1 (en) 2021-04-15
AU2020363354A1 (en) 2022-04-21
JP2022550641A (ja) 2022-12-02
JP7780439B2 (ja) 2025-12-04
KR20220079575A (ko) 2022-06-13
CA3156981A1 (en) 2021-04-15
US20230040182A1 (en) 2023-02-09
EP4041408A4 (en) 2023-10-18
MX2022004144A (es) 2022-06-14
BR112022006250A2 (pt) 2022-06-21
CN114728177A (zh) 2022-07-08

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