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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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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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28Oxygen atom
    • C07D473/30Oxygen atom attached in position 6, e.g. hypoxanthine
    • 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
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • A61K31/53Heterocyclic 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
    • 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
    • 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
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (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)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (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 2019-10-15
EP19203174.8 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 (https=)
EP (1) EP4045053B1 (https=)
JP (1) JP7612682B2 (https=)
CN (1) CN114555601B (https=)
WO (1) WO2021074198A1 (https=)

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
AU2022257269A1 (en) 2021-04-14 2023-08-17 Boehringer Ingelheim International Gmbh 3H,4H-THIENO[2,3-d]PYRIMIDIN-4-ONE DERIVATIVES AS TRPA1 INHIBITORS
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)

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Publication number Priority date Publication date Assignee Title
WO1996040256A1 (en) 1995-06-07 1996-12-19 G.D. Searle & Co. Method to treat cardiofibrosis with a combination of an angiotensin 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
EP2411395B1 (en) 2009-03-23 2013-05-29 Glenmark Pharmaceuticals S.A. Furopyrimidinedione derivatives as trpa1 modulators
PE20140234A1 (es) 2010-12-20 2014-03-08 Glenmark Phamaceuticals S A Compuestos de 2-amino-4-ariltiazol como antagonistas de trpa1
CA2836856A1 (en) 2011-06-13 2012-12-20 Glenmark Pharmaceuticals, S.A. Treatment of respiratory disorders using trpa1 antagonists
JP6573968B2 (ja) 2014-08-11 2019-09-11 ハイドラ バイオサイエンシズ インコーポレイテッドHydra Biosciences,Inc. TRPC5調節因子としての、精神神経障害の処置のためのチエノおよびフロ[2,3−d]ピリミジン−2,4[1H,3H]−ジオン誘導体
US12006328B2 (en) 2014-11-18 2024-06-11 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
CN111201234A (zh) 2017-07-17 2020-05-26 南京瑞捷医药科技有限公司 新型化合物及其作为acc抑制剂的用途
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
CA3153115A1 (en) 2019-10-15 2021-04-22 Boehringer Ingelheim International Gmbh Thienopyrimidones as trpa1 inhibitors
JP7376706B2 (ja) 2019-10-15 2023-11-08 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阻害剤としてのチエノピリミドン
CN116348471B (zh) 2020-10-14 2025-10-31 勃林格殷格翰国际有限公司 作为trpa1抑制剂的四唑衍生物
AU2021363101A1 (en) 2020-10-14 2023-03-23 Boehringer Ingelheim International Gmbh Tetrazole derivatives as TRPA1 inhibitors
AU2022257269A1 (en) 2021-04-14 2023-08-17 Boehringer Ingelheim International Gmbh 3H,4H-THIENO[2,3-d]PYRIMIDIN-4-ONE DERIVATIVES AS TRPA1 INHIBITORS

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

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