CN116419918A - 4-(7-羟基-2-异丙基-4-氧代-4h-喹唑啉-3-基)-苄腈的结晶形式及其配制品 - Google Patents

4-(7-羟基-2-异丙基-4-氧代-4h-喹唑啉-3-基)-苄腈的结晶形式及其配制品 Download PDF

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Publication number
CN116419918A
CN116419918A CN202180066886.8A CN202180066886A CN116419918A CN 116419918 A CN116419918 A CN 116419918A CN 202180066886 A CN202180066886 A CN 202180066886A CN 116419918 A CN116419918 A CN 116419918A
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China
Prior art keywords
compound
crystalline form
formulation
pain
isopropyl
Prior art date
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Pending
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CN202180066886.8A
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English (en)
Chinese (zh)
Inventor
M·穆兹
F·王
M·夏
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bausch and Lomb Ireland Ltd
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Novartis AG
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Publication of CN116419918A publication Critical patent/CN116419918A/zh
Pending legal-status Critical Current

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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
    • 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

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  • 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)
CN202180066886.8A 2020-08-06 2021-08-04 4-(7-羟基-2-异丙基-4-氧代-4h-喹唑啉-3-基)-苄腈的结晶形式及其配制品 Pending CN116419918A (zh)

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

Publications (1)

Publication Number Publication Date
CN116419918A true CN116419918A (zh) 2023-07-11

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Family Applications (1)

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CN202180066886.8A Pending CN116419918A (zh) 2020-08-06 2021-08-04 4-(7-羟基-2-异丙基-4-氧代-4h-喹唑啉-3-基)-苄腈的结晶形式及其配制品

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 (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1956721A (zh) * 2004-06-08 2007-05-02 诺瓦提斯公司 用作辣椒素拮抗剂的喹唑啉酮衍生物
CN101356160A (zh) * 2005-12-08 2009-01-28 诺瓦提斯公司 作为辣椒素受体拮抗剂的三取代的喹唑啉酮衍生物
CN102281920A (zh) * 2009-01-13 2011-12-14 诺瓦提斯公司 用作辣椒素拮抗剂的喹唑啉酮衍生物
US20150352176A1 (en) * 2014-06-06 2015-12-10 Newport Research, Inc. Oil-free and fat-free aqueous suspensions of cyclosporin
WO2020165840A1 (en) * 2019-02-15 2020-08-20 Novartis Ag Crystalline forms of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile and formulations thereof
CN111568906A (zh) * 2019-02-15 2020-08-25 诺华股份有限公司 4-(7-羟基-2-异丙基-4-氧代-4h-喹唑啉-3-基)-苄腈的配制品
CN113453686A (zh) * 2019-02-15 2021-09-28 诺华股份有限公司 治疗眼表痛的方法

Family Cites Families (8)

* 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

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1956721A (zh) * 2004-06-08 2007-05-02 诺瓦提斯公司 用作辣椒素拮抗剂的喹唑啉酮衍生物
US20080194595A1 (en) * 2004-06-08 2008-08-14 Timothy John Ritchie Quinazolinone Derivatives Useful as Vanilloid Antagonists
CN101356160A (zh) * 2005-12-08 2009-01-28 诺瓦提斯公司 作为辣椒素受体拮抗剂的三取代的喹唑啉酮衍生物
CN102281920A (zh) * 2009-01-13 2011-12-14 诺瓦提斯公司 用作辣椒素拮抗剂的喹唑啉酮衍生物
US20150352176A1 (en) * 2014-06-06 2015-12-10 Newport Research, Inc. Oil-free and fat-free aqueous suspensions of cyclosporin
WO2020165840A1 (en) * 2019-02-15 2020-08-20 Novartis Ag Crystalline forms of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile and formulations thereof
CN111568906A (zh) * 2019-02-15 2020-08-25 诺华股份有限公司 4-(7-羟基-2-异丙基-4-氧代-4h-喹唑啉-3-基)-苄腈的配制品
CN113423696A (zh) * 2019-02-15 2021-09-21 诺华股份有限公司 4-(7-羟基-2-异丙基-4-氧代-4h-喹唑啉-3-基)-苄腈的结晶形式及其配制品
CN113453686A (zh) * 2019-02-15 2021-09-28 诺华股份有限公司 治疗眼表痛的方法

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
"saf312", pages 1 - 6, Retrieved from the Internet <URL:https://pubchem.ncbi.nlm.nih.gov/substance/341696399> *
NOVARTIS PHARMACEUTICALS: "Study of SAF312 as an Eye Drop for Treatment of Eye Pain Following Photorefractive Keratectomy (PRK) Surgery", pages 5, Retrieved from the Internet <URL:https://clinicaltrials.gov/study/NCT02961062cond=nct02961062&rank=1&tab=history&a=7> *

Also Published As

Publication number Publication date
US12459902B2 (en) 2025-11-04
JP2023536938A (ja) 2023-08-30
EP4192466A1 (en) 2023-06-14
US20230286924A1 (en) 2023-09-14
JP2026004313A (ja) 2026-01-14
WO2022029656A1 (en) 2022-02-10

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Effective date of registration: 20231127

Address after: Irish Dublin

Applicant after: Bausch & Lomb Ireland Ltd.

Address before: Basel, SUI

Applicant before: NOVARTIS AG