JP2022520410A - ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤 - Google Patents

４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤 Download PDF

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JP2022520410A
JP2022520410A JP2021547248A JP2021547248A JP2022520410A JP 2022520410 A JP2022520410 A JP 2022520410A JP 2021547248 A JP2021547248 A JP 2021547248A JP 2021547248 A JP2021547248 A JP 2021547248A JP 2022520410 A JP2022520410 A JP 2022520410A
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amount
crystal form
corneal
formulation
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JP2022520410A5 (https=
Inventor
ポール ブロック，ジョセフ
マヘシュワリ，チンメイ
メドリー，キンタス
宗人 茂木
モンテッチ－パルメール，ミケラ
モランディ，グレゴリー
マッツ，マイケル
スタシ，カリオピ
ステファン タオラー，クリストファー
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ノバルティス アーゲー
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Publication of JP2022520410A publication Critical patent/JP2022520410A/ja
Publication of JP2022520410A5 publication Critical patent/JP2022520410A5/ja
Priority to JP2024128919A priority Critical patent/JP2024161426A/ja
Priority to JP2025148623A priority patent/JP2026004320A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Ophthalmology & Optometry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2021547248A 2019-02-15 2020-02-13 ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤 Pending JP2022520410A (ja)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2024128919A JP2024161426A (ja) 2019-02-15 2024-08-05 ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤
JP2025148623A JP2026004320A (ja) 2019-02-15 2025-09-08 ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962806697P 2019-02-15 2019-02-15
US62/806,697 2019-02-15
PCT/IB2020/051212 WO2020165840A1 (en) 2019-02-15 2020-02-13 Crystalline forms of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile and formulations thereof

Related Child Applications (1)

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JP2024128919A Division JP2024161426A (ja) 2019-02-15 2024-08-05 ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤

Publications (2)

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JP2022520410A true JP2022520410A (ja) 2022-03-30
JP2022520410A5 JP2022520410A5 (https=) 2023-02-16

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Family Applications (3)

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JP2021547248A Pending JP2022520410A (ja) 2019-02-15 2020-02-13 ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤
JP2024128919A Pending JP2024161426A (ja) 2019-02-15 2024-08-05 ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤
JP2025148623A Pending JP2026004320A (ja) 2019-02-15 2025-09-08 ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤

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JP2024128919A Pending JP2024161426A (ja) 2019-02-15 2024-08-05 ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤
JP2025148623A Pending JP2026004320A (ja) 2019-02-15 2025-09-08 ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤

Country Status (5)

Country Link
US (1) US12600702B2 (https=)
EP (2) EP4431497A1 (https=)
JP (3) JP2022520410A (https=)
CN (1) CN113423696A (https=)
WO (1) WO2020165840A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022520832A (ja) * 2019-02-15 2022-04-01 ノバルティス アーゲー 眼表面疼痛を治療する方法
JP2023536938A (ja) * 2020-08-06 2023-08-30 ノバルティス アーゲー ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022105792A1 (zh) * 2020-11-17 2022-05-27 苏州晶云药物科技股份有限公司 一种喹唑啉酮衍生物的新晶型及其制备方法

Citations (1)

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JP2012515150A (ja) * 2009-01-13 2012-07-05 ノバルティス アーゲー バニロイドアンタゴニストとして有用なキナゾリノン誘導体

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US3931319A (en) 1974-10-29 1976-01-06 Millmaster Onyx Corporation Capped polymers
US4027020A (en) 1974-10-29 1977-05-31 Millmaster Onyx Corporation Randomly terminated capped polymers
US4407791A (en) 1981-09-28 1983-10-04 Alcon Laboratories, Inc. Ophthalmic solutions
US4525346A (en) 1981-09-28 1985-06-25 Alcon Laboratories, Inc. Aqueous antimicrobial ophthalmic solutions
US4836986A (en) 1984-09-28 1989-06-06 Bausch & Lomb Incorporated Disinfecting and preserving systems and methods of use
US5037647A (en) 1988-09-15 1991-08-06 Alcon Laboratories, Inc. Aqueous antimicrobial opthalmic solutions comprised of quaternary ammonium compound, citric acid, citrate and sodium chloride
US5145643A (en) 1990-01-05 1992-09-08 Allergan, Inc. Nonoxidative ophthalmic compositions and methods for preserving and using same
US5300287A (en) 1992-11-04 1994-04-05 Alcon Laboratories, Inc. Polymeric antimicrobials and their use in pharmaceutical compositions
GB0412769D0 (en) 2004-06-08 2004-07-07 Novartis Ag Organic compounds
EP3470059B1 (en) * 2015-01-26 2020-04-01 Bausch & Lomb Incorporated Ophthalmic suspension composition
WO2022029656A1 (en) * 2020-08-06 2022-02-10 Novartis Ag Crystalline forms of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile and formulations thereof

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
JP2012515150A (ja) * 2009-01-13 2012-07-05 ノバルティス アーゲー バニロイドアンタゴニストとして有用なキナゾリノン誘導体

Non-Patent Citations (4)

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Title
塩路雄作, 固形製剤の製造技術, vol. 普及版, JPN6011023134, 27 January 2003 (2003-01-27), pages 9 - 12, ISSN: 0005426131 *
平山令明, 有機化合物結晶作製ハンドブック, JPN6014035600, 2008, pages 17 - 23, ISSN: 0005426128 *
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高田則幸: "創薬段階における原薬Formスクリーニングと選択", PHARM STAGE, vol. 6, no. 10, JPN6009053755, 15 January 2007 (2007-01-15), pages 20 - 25, ISSN: 0005426129 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022520832A (ja) * 2019-02-15 2022-04-01 ノバルティス アーゲー 眼表面疼痛を治療する方法
JP7571037B2 (ja) 2019-02-15 2024-10-22 ボシュ ＋ ロム アイルランド リミテッド 眼表面疼痛を治療する方法
JP2023536938A (ja) * 2020-08-06 2023-08-30 ノバルティス アーゲー ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤

Also Published As

Publication number Publication date
JP2026004320A (ja) 2026-01-14
EP3924345A1 (en) 2021-12-22
US12600702B2 (en) 2026-04-14
JP2024161426A (ja) 2024-11-19
WO2020165840A1 (en) 2020-08-20
CN113423696A (zh) 2021-09-21
EP4431497A1 (en) 2024-09-18
US20220162170A1 (en) 2022-05-26

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