JP2023536938A - 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

Info

Publication number
JP2023536938A
JP2023536938A JP2023507688A JP2023507688A JP2023536938A JP 2023536938 A JP2023536938 A JP 2023536938A JP 2023507688 A JP2023507688 A JP 2023507688A JP 2023507688 A JP2023507688 A JP 2023507688A JP 2023536938 A JP2023536938 A JP 2023536938A
Authority
JP
Japan
Prior art keywords
compound
crystalline form
formulation
isopropyl
benzonitrile
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
JP2023507688A
Other languages
English (en)
Japanese (ja)
Other versions
JP2023536938A5 (https=
Inventor
マッツ，ミハエル
ワン，ファン
シャア，メイ
Original Assignee
ノバルティス アーゲー
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by ノバルティス アーゲー filed Critical ノバルティス アーゲー
Publication of JP2023536938A publication Critical patent/JP2023536938A/ja
Publication of JP2023536938A5 publication Critical patent/JP2023536938A5/ja
Priority to JP2025147197A priority Critical patent/JP2026004313A/ja
Pending legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
JP2023507688A 2020-08-06 2021-08-04 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 JP2023536938A (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2025147197A JP2026004313A (ja) 2020-08-06 2025-09-04 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
CN2020107444 2020-08-06
CNPCT/CN2020/107444 2020-08-06
PCT/IB2021/057165 WO2022029656A1 (en) 2020-08-06 2021-08-04 Crystalline forms of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile and formulations thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2025147197A Division JP2026004313A (ja) 2020-08-06 2025-09-04 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)

Publication Number Publication Date
JP2023536938A true JP2023536938A (ja) 2023-08-30
JP2023536938A5 JP2023536938A5 (https=) 2024-08-13

Family

ID=77358315

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2023507688A Pending JP2023536938A (ja) 2020-08-06 2021-08-04 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
JP2025147197A Pending JP2026004313A (ja) 2020-08-06 2025-09-04 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

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2025147197A Pending JP2026004313A (ja) 2020-08-06 2025-09-04 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) US12459902B2 (https=)
EP (1) EP4192466A1 (https=)
JP (2) JP2023536938A (https=)
CN (1) CN116419918A (https=)
WO (1) WO2022029656A1 (https=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4431497A1 (en) * 2019-02-15 2024-09-18 Bausch + Lomb Ireland Limited Crystalline forms of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile and formulations thereof

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007065662A2 (en) * 2005-12-08 2007-06-14 Novartis Ag Trisubstituted quinazolinone derivatives as vanilloid antagonists
JP2008501763A (ja) * 2004-06-08 2008-01-24 ノバルティス アクチエンゲゼルシャフト 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
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
JP2022520410A (ja) * 2019-02-15 2022-03-30 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
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

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US4525346A (en) 1981-09-28 1985-06-25 Alcon Laboratories, Inc. Aqueous antimicrobial ophthalmic solutions
US4407791A (en) 1981-09-28 1983-10-04 Alcon Laboratories, Inc. 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
US20150352176A1 (en) * 2014-06-06 2015-12-10 Newport Research, Inc. Oil-free and fat-free aqueous suspensions of cyclosporin
JP6994061B2 (ja) * 2019-02-15 2022-01-14 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）－ベンゾニトリルの製剤

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008501763A (ja) * 2004-06-08 2008-01-24 ノバルティス アクチエンゲゼルシャフト 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
WO2007065662A2 (en) * 2005-12-08 2007-06-14 Novartis Ag Trisubstituted quinazolinone derivatives as vanilloid antagonists
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
JP2022520410A (ja) * 2019-02-15 2022-03-30 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
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

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
厚生省医薬安全局審査管理課長: "医薬品の残留溶媒ガイドラインについて", 医薬審, JPN6014031669, 1998, ISSN: 0005738086 *
川口洋子ら, 生活工学研究, vol. 4, no. 2, JPN6015027394, 2002, pages 310 - 317, ISSN: 0005738084 *
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: 0005738083 *
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: 0005738085 *

Also Published As

Publication number Publication date
US12459902B2 (en) 2025-11-04
CN116419918A (zh) 2023-07-11
EP4192466A1 (en) 2023-06-14
US20230286924A1 (en) 2023-09-14
JP2026004313A (ja) 2026-01-14
WO2022029656A1 (en) 2022-02-10

Similar Documents

Publication Publication Date Title
JP7465453B2 (ja) 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）－ベンゾニトリルの製剤
JP2026004320A (ja) 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
JP2025004186A (ja) 眼表面疼痛を治療する方法
JP2026004313A (ja) 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
RU2853589C2 (ru) Составы на основе 4-(7-гидрокси-2-изопропил-4-оксо-4h-хиназолин-3-ил)-бензонитрила
WO2024062389A1 (en) Crystalline polymorph forms of a trpv1 antagonist and formulations thereof
KR20260057219A (ko) 4-(7-히드록시-2-이소프로필-4-옥소-4h-퀴나졸린-3-일)-벤조니트릴의제형

Legal Events

Date Code Title Description
A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20240305

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20240801

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20240801

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20250304

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20250603

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20250731

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20250904

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20251125