CN114555601B - 新颖的四唑类 - Google Patents

新颖的四唑类 Download PDF

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Publication number
CN114555601B
CN114555601B CN202080071658.5A CN202080071658A CN114555601B CN 114555601 B CN114555601 B CN 114555601B CN 202080071658 A CN202080071658 A CN 202080071658A CN 114555601 B CN114555601 B CN 114555601B
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China
Prior art keywords
compound
diseases
trpa1
compounds
salt
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CN202080071658.5A
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English (en)
Chinese (zh)
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CN114555601A (zh
Inventor
M·T·弗莱克
F·P·C·宾德尔
G·达曼
J·P·海恩
U·F·莱塞尔
J·威尔瓦赫
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Boehringer Ingelheim International GmbH
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Boehringer Ingelheim International GmbH
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Publication of CN114555601A publication Critical patent/CN114555601A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28—Oxygen atom
    • C07D473/30—Oxygen atom attached in position 6, e.g. hypoxanthine
    • 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
    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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 two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN202080071658.5A 2019-10-15 2020-10-14 新颖的四唑类 Active CN114555601B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP19203174.8 2019-10-15
EP19203174 2019-10-15
PCT/EP2020/078856 WO2021074198A1 (en) 2019-10-15 2020-10-14 Novel tetrazoles

Publications (2)

Publication Number Publication Date
CN114555601A CN114555601A (zh) 2022-05-27
CN114555601B true CN114555601B (zh) 2024-04-02

Family

ID=68289875

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080071658.5A Active CN114555601B (zh) 2019-10-15 2020-10-14 新颖的四唑类

Country Status (5)

Country Link
US (1) US12497401B2 (enExample)
EP (1) EP4045053B1 (enExample)
JP (1) JP7612682B2 (enExample)
CN (1) CN114555601B (enExample)
WO (1) WO2021074198A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7612682B2 (ja) * 2019-10-15 2025-01-14 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規なテトラゾール
JP7565457B2 (ja) 2021-04-14 2024-10-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ＴＲＰＡ１阻害剤としての３Ｈ，４Ｈ－チエノ－［２，３－ｄ］ピリミジン－４－オン誘導体
IT202100015098A1 (it) * 2021-06-09 2022-12-09 Flonext S R L Composto antagonista del canale trpa1 per uso in patologie degenerative della retina
WO2025167992A1 (zh) * 2024-02-08 2025-08-14 宜昌人福药业有限责任公司 一种非选择性阳离子通道trpa1拮抗剂及其用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015155306A1 (en) * 2014-04-11 2015-10-15 Almirall, S.A. New trpa1 antagonists
WO2017060488A1 (en) * 2015-10-09 2017-04-13 Almirall, S.A. New trpa1 antagonists

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU5982296A (en) 1995-06-07 1996-12-30 G.D. Searle & Co. Method to treat cardiofibrosis with a combination of an angi otensin ii antagonist and spironolactone
US7754709B2 (en) 2003-06-10 2010-07-13 Solvay Pharmaceuticals Bv Tetracyclic thiophenepyrimidinone compounds as inhibitors of 17β hydroxysteroid dehydrogenase compounds
PE20120834A1 (es) 2009-03-23 2012-07-25 Glenmark Pharmaceuticals Sa Derivados de furopirimidindiona como moduladores de trpa1
KR101591153B1 (ko) 2010-12-20 2016-02-02 그렌마크 파머수티칼스 에스. 아. Trpa1 길항제로서의 2-아미노-4-아릴티아졸 화합물
RU2014100744A (ru) 2011-06-13 2015-07-20 Гленмарк Фармасьютикалс С.А. Лечение респираторных нарушений с помощью trpa1 антагонистов
EP3180345B1 (en) 2014-08-11 2018-10-10 Hydra Biosciences, Inc. Thieno- and furo[2,3-d]pyrimidine-2,4[1h,3h]-dione derivatives as trpc5 modulators for the treatment of neuropsychiatric disorders
WO2016081649A1 (en) 2014-11-18 2016-05-26 Emory University Thieno[2,3-d]pyrimidin-4-one derivatives as nmdar modulators and uses related thereto
WO2016133888A1 (en) 2015-02-16 2016-08-25 Biota Pharmaceuticals, Inc. Compounds for treating respiratory syncytial virus infections
WO2019015583A1 (en) 2017-07-17 2019-01-24 Nanjing Ruijie Pharmatech Co., Ltd. NOVEL COMPOUNDS AND THEIR USES AS ACC INHIBITORS
PH12022550846A1 (en) 2019-10-15 2023-03-27 Boehringer Ingelheim Pharma Thienopyrimidones as trpa1 inhibitors
JP7612682B2 (ja) * 2019-10-15 2025-01-14 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規なテトラゾール
MX2022004565A (es) 2019-10-15 2022-05-06 Boehringer Ingelheim Int Tienopirimidonas como inhibidores de trpa1.
KR20230087531A (ko) 2020-10-14 2023-06-16 베링거 인겔하임 인터내셔날 게엠베하 Trpa1 억제제로서 테트라졸 유도체
IL301717B2 (en) 2020-10-14 2026-05-01 Boehringer Ingelheim Int History of tetrazoles as TRPA1 inhibitors
JP7565457B2 (ja) 2021-04-14 2024-10-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ＴＲＰＡ１阻害剤としての３Ｈ，４Ｈ－チエノ－［２，３－ｄ］ピリミジン－４－オン誘導体

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015155306A1 (en) * 2014-04-11 2015-10-15 Almirall, S.A. New trpa1 antagonists
WO2017060488A1 (en) * 2015-10-09 2017-04-13 Almirall, S.A. New trpa1 antagonists

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity;Laurie B. Schenkel等;Journal of Medicinal Chemistry;第59卷;2794-2809 *

Also Published As

Publication number Publication date
US20240101561A1 (en) 2024-03-28
EP4045053A1 (en) 2022-08-24
EP4045053B1 (en) 2023-12-06
JP7612682B2 (ja) 2025-01-14
JP2022552520A (ja) 2022-12-16
WO2021074198A1 (en) 2021-04-22
CN114555601A (zh) 2022-05-27
US12497401B2 (en) 2025-12-16

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