BR112021015737A2 - Formulações de 4-(7-hidróxi-2-isopropil-4-oxo-4h-quinazolin-3-il)-benzonitrila - Google Patents

Formulações de 4-(7-hidróxi-2-isopropil-4-oxo-4h-quinazolin-3-il)-benzonitrila Download PDF

Info

Publication number
BR112021015737A2
BR112021015737A2 BR112021015737-9A BR112021015737A BR112021015737A2 BR 112021015737 A2 BR112021015737 A2 BR 112021015737A2 BR 112021015737 A BR112021015737 A BR 112021015737A BR 112021015737 A2 BR112021015737 A2 BR 112021015737A2
Authority
BR
Brazil
Prior art keywords
compound
formulation
pain
salt
amount
Prior art date
Application number
BR112021015737-9A
Other languages
English (en)
Portuguese (pt)
Inventor
Joseph Paul Bullock
Chinmay MAHESHWARI
Quintus Medley
Muneto Mogi
Michela MONTECCHI-PALMER
Kalliopi STASI
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of BR112021015737A2 publication Critical patent/BR112021015737A2/pt

Links

Classifications

    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40Cyclodextrins; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/14Decongestants or antiallergics
    • 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]

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Dispersion Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
BR112021015737-9A 2019-02-15 2020-02-13 Formulações de 4-(7-hidróxi-2-isopropil-4-oxo-4h-quinazolin-3-il)-benzonitrila BR112021015737A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962806705P 2019-02-15 2019-02-15
US62/806,705 2019-02-15
PCT/IB2020/051211 WO2020165839A1 (en) 2019-02-15 2020-02-13 Formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile

Publications (1)

Publication Number Publication Date
BR112021015737A2 true BR112021015737A2 (pt) 2021-10-26

Family

ID=69740424

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021015737-9A BR112021015737A2 (pt) 2019-02-15 2020-02-13 Formulações de 4-(7-hidróxi-2-isopropil-4-oxo-4h-quinazolin-3-il)-benzonitrila

Country Status (23)

Country Link
US (4) US11478480B2 (https=)
EP (1) EP3923912A1 (https=)
JP (5) JP6994061B2 (https=)
KR (1) KR20210127197A (https=)
CN (2) CN111568906B (https=)
AU (2) AU2020220957B2 (https=)
BR (1) BR112021015737A2 (https=)
CA (1) CA3130237A1 (https=)
CL (1) CL2021002153A1 (https=)
CO (1) CO2021010689A2 (https=)
CR (1) CR20210428A (https=)
EC (1) ECSP21059628A (https=)
IL (1) IL284628A (https=)
JO (1) JOP20210224A1 (https=)
MX (2) MX2021009704A (https=)
MY (1) MY206327A (https=)
PE (1) PE20212106A1 (https=)
PH (1) PH12021551967A1 (https=)
SA (1) SA521430043B1 (https=)
SG (1) SG11202107259QA (https=)
TW (1) TWI827800B (https=)
WO (1) WO2020165839A1 (https=)
ZA (1) ZA202104594B (https=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20210129677A (ko) * 2019-02-15 2021-10-28 노파르티스 아게 안구 표면 통증의 치료 방법
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
WO2021191273A1 (en) * 2020-03-24 2021-09-30 Hovione Scientia Limited Compositions for use in treating meibomian gland dysfunction
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
WO2022074557A1 (en) * 2020-10-07 2022-04-14 Novartis Ag Drug containing dissolvable ocular inserts and method of using same
US20230159202A1 (en) * 2021-11-23 2023-05-25 Bausch + Lomb Ireland Limited Method for making a preservative-free packaged ophthalmic device product
US20240197691A1 (en) * 2022-12-15 2024-06-20 Cn2 Therapeutics, Inc. Tacrolimus compositions and methods of use
CN118340775A (zh) * 2023-01-09 2024-07-16 维眸生物科技(浙江)有限公司 一种含vvn539的眼用组合物及其用途
EP4454639A1 (en) * 2023-04-14 2024-10-30 Omnivision GmbH Ophthalmic composition comprising carbomer and taurine

Family Cites Families (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1280874B (de) 1963-10-09 1968-10-24 Boehringer Sohn Ingelheim 2-Methyl-3-(2-dimethylaminophenyl)-8-amino-3H-chinazolon-(4)
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
JP2003510263A (ja) * 1999-09-24 2003-03-18 アルコン,インコーポレイテッド シプロフロキサシンおよびデキサメタゾンを含有する局所用懸濁処方物
GB0412769D0 (en) 2004-06-08 2004-07-07 Novartis Ag Organic compounds
TWI358290B (en) * 2004-12-02 2012-02-21 Alcon Inc Topical nepafenac formulations
US7893260B2 (en) 2005-11-04 2011-02-22 Hydra Biosciences, Inc. Substituted quinazolin-4-one compounds for antagonizing TRPV3 function
GB0525069D0 (en) 2005-12-08 2006-01-18 Novartis Ag Organic compounds
GB0525068D0 (en) * 2005-12-08 2006-01-18 Novartis Ag Organic compounds
BRPI0620264A2 (pt) 2005-12-22 2011-11-08 Prolexys Pharmaceuticals Inc quinazolonas aril-substituìdas e sua utilização
TW200738232A (en) 2006-01-31 2007-10-16 Alcon Mfg Ltd Use of vanilloid receptor-1 antagonists for the prevention and treatment of glaucoma
EP1964548A1 (en) 2007-03-02 2008-09-03 Novartis AG Pharmaceutical compositions comprising a calcilytic agent
WO2008140750A1 (en) 2007-05-10 2008-11-20 Hydra Biosciences Inc. Compounds for modulating trpv3 function
KR20100039410A (ko) 2007-07-18 2010-04-15 노파르티스 아게 Vr-1 길항제 및 cox-2 억제제의 상승적 조합물
TW200927192A (en) * 2007-11-19 2009-07-01 Alcon Res Ltd Use of TRPV1 receptor antagonists for treating dry eye and ocular pain
WO2009081222A1 (en) 2007-12-21 2009-07-02 Glenmark Pharmaceuticals, S.A. Substituted tricyclic pyridine or pyrimidine vanilloid receptor ligands
US8163901B2 (en) 2008-01-09 2012-04-24 Evotec Ag Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
WO2009090548A2 (en) 2008-01-17 2009-07-23 Glenmark Pharmaceuticals, S.A. 3-azabicyclo [3.1.0] hexane derivatives as vanilloid receptor ligands
WO2009149239A1 (en) 2008-06-04 2009-12-10 Children's Medical Center Corporation Methods of modulating angiogenesis via trpv4
WO2010023512A1 (en) 2008-08-28 2010-03-04 Matrix Laboratories Ltd. Novel vanilloid receptor modulators, process for their preparation and pharmaceutical compositions containing them
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
EP2316420B1 (en) 2009-10-22 2014-02-26 Consorzio Universitario Unifarm Topical ophthalmic composition to reduce pain
EP2377850A1 (en) 2010-03-30 2011-10-19 Pharmeste S.r.l. TRPV1 vanilloid receptor antagonists with a bicyclic portion
EP2627178B1 (en) 2010-10-11 2018-05-02 Merck Sharp & Dohme Corp. Quinazolinone-type compounds as crth2 antagonists
CN102659629B (zh) * 2012-02-14 2014-03-19 杭州华东医药集团新药研究院有限公司 化合物及其在制备埃罗替尼中的用途
CN102875480A (zh) 2012-04-23 2013-01-16 中国药科大学 喹唑啉酮类血管抑制剂、其制备方法及其医药用途
GB201215857D0 (en) 2012-09-05 2012-10-24 Sylentis Sau siRNA and their use in methods and compositions for the treatment and/or prevention of eye conditions
CA2903114A1 (en) * 2013-03-15 2014-09-25 Inotek Pharmaceuticals Corporation Ophthalmic formulations
US20150352176A1 (en) * 2014-06-06 2015-12-10 Newport Research, Inc. Oil-free and fat-free aqueous suspensions of cyclosporin
EP3179982B1 (en) 2014-07-28 2023-07-19 Sun Pharma Advanced Research Company Ltd Method of increasing bioavailability and/or prolonging ophthalmic action of a drug
MY196072A (en) * 2014-09-15 2023-03-13 Verona Pharma Plc Liquid Inhalation Formulation Comprising RPL554
EP3470059B1 (en) * 2015-01-26 2020-04-01 Bausch & Lomb Incorporated Ophthalmic suspension composition
RU2019110821A (ru) 2016-09-20 2020-10-22 Глэксосмитклайн Интеллекчуал Проперти (Но.2) Лимитед Антагонисты trpv4
JP2019532054A (ja) 2016-09-20 2019-11-07 グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited Trpv4拮抗薬
TW201825458A (zh) 2016-09-20 2018-07-16 英商葛蘭素史克智慧財產(第二)有限公司 Trpv4拮抗劑
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
KR20210129677A (ko) * 2019-02-15 2021-10-28 노파르티스 아게 안구 표면 통증의 치료 방법

Also Published As

Publication number Publication date
US20230139170A1 (en) 2023-05-04
JP6994061B2 (ja) 2022-01-14
JOP20210224A1 (ar) 2023-01-30
AU2023203933B2 (en) 2025-06-12
US20200261457A1 (en) 2020-08-20
US20200390767A1 (en) 2020-12-17
CN111568906B (zh) 2023-09-01
IL284628A (en) 2021-08-31
CO2021010689A2 (es) 2021-08-30
JP7465453B2 (ja) 2024-04-11
JP2022520795A (ja) 2022-04-01
CL2021002153A1 (es) 2022-04-18
WO2020165839A1 (en) 2020-08-20
CR20210428A (es) 2021-09-22
AU2020220957B2 (en) 2023-04-06
SG11202107259QA (en) 2021-08-30
MX2024002989A (es) 2024-03-27
ZA202104594B (en) 2024-10-30
JP2020132634A (ja) 2020-08-31
CN117752662A (zh) 2024-03-26
ECSP21059628A (es) 2021-09-30
US12290517B2 (en) 2025-05-06
MX2021009704A (es) 2021-09-14
PH12021551967A1 (en) 2022-05-23
KR20210127197A (ko) 2021-10-21
US20260034132A1 (en) 2026-02-05
CA3130237A1 (en) 2020-08-20
AU2023203933A1 (en) 2023-07-13
TWI827800B (zh) 2024-01-01
WO2020165839A9 (en) 2021-03-18
SA521430043B1 (ar) 2022-11-20
US11478480B2 (en) 2022-10-25
JP2022017260A (ja) 2022-01-25
JP2024037806A (ja) 2024-03-19
JP2024095674A (ja) 2024-07-10
MY206327A (en) 2024-12-11
PE20212106A1 (es) 2021-11-04
AU2020220957A1 (en) 2021-08-05
TW202045178A (zh) 2020-12-16
CN111568906A (zh) 2020-08-25
EP3923912A1 (en) 2021-12-22

Similar Documents

Publication Publication Date Title
US12290517B2 (en) Formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile
US20240342174A1 (en) Methods for treating ocular surface pain
RU2853589C2 (ru) Составы на основе 4-(7-гидрокси-2-изопропил-4-оксо-4h-хиназолин-3-ил)-бензонитрила
RU2850452C2 (ru) Способы лечения боли на поверхности глаза
KR20260057219A (ko) 4-(7-히드록시-2-이소프로필-4-옥소-4h-퀴나졸린-3-일)-벤조니트릴의제형

Legal Events

Date Code Title Description
B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B25A Requested transfer of rights approved

Owner name: BAUSCH + LOMB IRELAND LIMITED (IE)