CA3102527A1 - Aqueous formulation comprising 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea - Google Patents

Aqueous formulation comprising 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea Download PDF

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Publication number
CA3102527A1
CA3102527A1 CA3102527A CA3102527A CA3102527A1 CA 3102527 A1 CA3102527 A1 CA 3102527A1 CA 3102527 A CA3102527 A CA 3102527A CA 3102527 A CA3102527 A CA 3102527A CA 3102527 A1 CA3102527 A1 CA 3102527A1
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CA
Canada
Prior art keywords
cyclodextrin
phenyl
triazin
urea
dimorpholin
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
CA3102527A
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English (en)
French (fr)
Inventor
James Joseph HUSSEY
Andrew Gilbert BRIGHT
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.)
Pfizer Inc
Original Assignee
Pfizer Inc
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 Pfizer Inc filed Critical Pfizer Inc
Publication of CA3102527A1 publication Critical patent/CA3102527A1/en
Pending legal-status Critical Current

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    • 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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40—Cyclodextrins; Derivatives thereof
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Dermatology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CA3102527A 2018-06-07 2019-06-04 Aqueous formulation comprising 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea Pending CA3102527A1 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201862681722P 2018-06-07 2018-06-07
US62/681,722 2018-06-07
US201862754651P 2018-11-02 2018-11-02
US62/754,651 2018-11-02
US201962796133P 2019-01-24 2019-01-24
US62/796,133 2019-01-24
US201962841882P 2019-05-02 2019-05-02
US62/841,882 2019-05-02
PCT/IB2019/054643 WO2019234632A1 (en) 2018-06-07 2019-06-04 Aqueous formulation comprising 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea

Publications (1)

Publication Number Publication Date
CA3102527A1 true CA3102527A1 (en) 2019-12-12

Family

ID=67402968

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3102527A Pending CA3102527A1 (en) 2018-06-07 2019-06-04 Aqueous formulation comprising 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea

Country Status (25)

Country Link
US (2) US12109308B2 (https=)
EP (3) EP4249069B1 (https=)
JP (2) JP7423200B2 (https=)
KR (2) KR20230142810A (https=)
CN (2) CN116270452A (https=)
AU (2) AU2019283550B2 (https=)
BR (1) BR112020023891A2 (https=)
CA (1) CA3102527A1 (https=)
DK (2) DK4249069T3 (https=)
ES (2) ES3057278T3 (https=)
FI (2) FI3810089T3 (https=)
HR (2) HRP20251602T1 (https=)
HU (1) HUE063493T2 (https=)
IL (1) IL279270A (https=)
LT (2) LT3810089T (https=)
MX (2) MX2020013238A (https=)
NZ (1) NZ805649A (https=)
PL (2) PL3810089T3 (https=)
PT (2) PT3810089T (https=)
RS (2) RS64692B1 (https=)
SG (1) SG11202011256RA (https=)
SI (2) SI4249069T1 (https=)
SM (2) SMT202300307T1 (https=)
TW (1) TWI696469B (https=)
WO (1) WO2019234632A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI3672571T1 (sl) 2017-08-25 2022-01-31 Pfizer Inc. Farmacevtska vodna raztopina, ki vsebuje 1-(4-((4-(dimetilamino) piperdin-1-il)karbonil)fenil)-3-(4-(4,6-dimorfolin-4-il-1,3, 5-triazin-2-il)fenil)sečnino
CA3227191A1 (en) 2021-07-26 2023-02-02 Celcuity Inc. 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea (gedatolisib) and its combinations for use in the treatment of cancer
WO2025128712A1 (en) 2023-12-12 2025-06-19 Celcuity Inc. Treatment of ocular diseases using 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl)phenyl)-3-[4-(4,6- dimorpholin-4- yl-1,3,5-triazin-2-yl)phenyl]urea
US20260053814A1 (en) 2024-08-21 2026-02-26 Celcuity Inc. Treatment regimens for gedatolisib in hormonally-driven disorders

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4727064A (en) * 1984-04-25 1988-02-23 The United States Of America As Represented By The Department Of Health And Human Services Pharmaceutical preparations containing cyclodextrin derivatives
US5002935A (en) * 1987-12-30 1991-03-26 University Of Florida Improvements in redox systems for brain-targeted drug delivery
US5298410A (en) * 1993-02-25 1994-03-29 Sterling Winthrop Inc. Lyophilized formulation of polyethylene oxide modified proteins with increased shelf-life
WO2003015828A1 (en) * 2001-08-20 2003-02-27 Boehringer Ingelheim Pharmaceuticals, Inc. Parenteral formulations of 1-(5-tert-butyl-2-p-tolyl-2h-pryrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea and a cyclodextrin
US20070111965A1 (en) * 2005-11-15 2007-05-17 Kipp James E Compositions comprising lipoxygenase inhibitors and cyclodextrin
LT2294072T (lt) 2008-05-23 2017-06-12 Wyeth Llc Triazino junginiai, kaip p13 kinazės ir mtor inhibitoriai
US10022381B2 (en) 2008-05-23 2018-07-17 Pfizer Inc. Triazine compounds as PI3 kinase and mTOR inhibitors
WO2010096619A1 (en) 2009-02-23 2010-08-26 Wyeth Llc Process, purification and crystallization of 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea
AR081364A1 (es) * 2010-05-05 2012-08-29 Glaxo Wellcome Mfg Pte Ltd Composiciones farmaceuticas de pazopanib y metodos para su elaboracion
WO2014121235A2 (en) * 2013-02-01 2014-08-07 Zoneone Pharma, Inc. Transformation of drug cyclodextrin complex compositions into compositions of mixtures of lipid vesicle encapsulated drug and cyclodextrin drug complexes
PE20170312A1 (es) * 2014-03-14 2017-03-30 Pfizer Nanoparticulas terapeuticas que comprenden un agente terapeutico, y metodos para su elaboracion y uso
ES2881214T3 (es) * 2014-12-17 2021-11-29 Pfizer Formulaciones de un inhibidor de PI3K/mTOR para la administración intravenosa
KR101829705B1 (ko) * 2016-09-21 2018-02-19 씨제이헬스케어 주식회사 안정성이 향상된 주사용 조성물
SI3672571T1 (sl) * 2017-08-25 2022-01-31 Pfizer Inc. Farmacevtska vodna raztopina, ki vsebuje 1-(4-((4-(dimetilamino) piperdin-1-il)karbonil)fenil)-3-(4-(4,6-dimorfolin-4-il-1,3, 5-triazin-2-il)fenil)sečnino

Also Published As

Publication number Publication date
CN112218618A (zh) 2021-01-12
AU2019283550A1 (en) 2020-12-10
WO2019234632A1 (en) 2019-12-12
FI3810089T3 (fi) 2023-09-22
US12109308B2 (en) 2024-10-08
LT3810089T (lt) 2023-11-10
SI3810089T1 (sl) 2023-11-30
US20210212944A1 (en) 2021-07-15
HRP20231337T1 (hr) 2024-02-16
MX2023012527A (es) 2023-10-31
EP3810089A1 (en) 2021-04-28
SI4249069T1 (sl) 2026-01-30
PL3810089T3 (pl) 2024-04-08
JP7423200B2 (ja) 2024-01-29
RS67535B1 (sr) 2026-01-30
AU2022211854A1 (en) 2022-08-25
EP4249069B1 (en) 2025-11-19
CN112218618B (zh) 2025-04-04
IL279270A (en) 2021-01-31
SMT202300307T1 (it) 2023-11-13
SG11202011256RA (en) 2020-12-30
FI4249069T3 (fi) 2025-12-29
EP4649940A3 (en) 2026-01-21
RS64692B1 (sr) 2023-11-30
AU2022211854B2 (en) 2024-01-04
EP4249069A2 (en) 2023-09-27
PT4249069T (pt) 2025-12-04
MX2020013238A (es) 2021-02-22
KR20210018341A (ko) 2021-02-17
HUE063493T2 (hu) 2024-01-28
JP2019218338A (ja) 2019-12-26
EP4249069A3 (en) 2023-11-29
PL4249069T3 (pl) 2026-02-23
HRP20251602T1 (hr) 2026-01-30
NZ805649A (en) 2024-11-29
NZ770000A (en) 2024-08-30
DK3810089T3 (en) 2023-09-25
KR102583563B1 (ko) 2023-10-05
TW202000234A (zh) 2020-01-01
PT3810089T (pt) 2023-08-23
DK4249069T3 (da) 2025-12-22
AU2019283550B2 (en) 2022-06-16
CN116270452A (zh) 2023-06-23
TWI696469B (zh) 2020-06-21
EP4649940A2 (en) 2025-11-19
JP7559162B2 (ja) 2024-10-01
KR20230142810A (ko) 2023-10-11
EP3810089B1 (en) 2023-08-02
JP2023138872A (ja) 2023-10-02
LT4249069T (lt) 2026-01-12
BR112020023891A2 (pt) 2021-02-09
US20250064732A1 (en) 2025-02-27
ES3057278T3 (en) 2026-02-27
SMT202500473T1 (it) 2026-01-12
ES2956225T3 (es) 2023-12-15

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