CN116270452A - 水性制剂 - Google Patents

水性制剂 Download PDF

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Publication number
CN116270452A
CN116270452A CN202310372451.7A CN202310372451A CN116270452A CN 116270452 A CN116270452 A CN 116270452A CN 202310372451 A CN202310372451 A CN 202310372451A CN 116270452 A CN116270452 A CN 116270452A
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CN
China
Prior art keywords
cyclodextrin
phenyl
urea
triazin
piperidin
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
CN202310372451.7A
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English (en)
Chinese (zh)
Inventor
J·J·赫西
A·G·布赖特
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 CN116270452A publication Critical patent/CN116270452A/zh
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
    • 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
    • A61K9/08—Solutions
    • 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)
CN202310372451.7A 2018-06-07 2019-06-04 水性制剂 Pending CN116270452A (zh)

Applications Claiming Priority (10)

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
CN201980037499.4A CN112218618B (zh) 2018-06-07 2019-06-04 包含1-(4-{[4-(二甲基氨基)哌啶-1-基]羰基}苯基)-3-[4-(4,6-二吗啉-4-基-1,3,5-三嗪-2-基)苯基]脲的水性制剂
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

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201980037499.4A Division CN112218618B (zh) 2018-06-07 2019-06-04 包含1-(4-{[4-(二甲基氨基)哌啶-1-基]羰基}苯基)-3-[4-(4,6-二吗啉-4-基-1,3,5-三嗪-2-基)苯基]脲的水性制剂

Publications (1)

Publication Number Publication Date
CN116270452A true CN116270452A (zh) 2023-06-23

Family

ID=67402968

Family Applications (2)

Application Number Title Priority Date Filing Date
CN202310372451.7A Pending CN116270452A (zh) 2018-06-07 2019-06-04 水性制剂
CN201980037499.4A Active CN112218618B (zh) 2018-06-07 2019-06-04 包含1-(4-{[4-(二甲基氨基)哌啶-1-基]羰基}苯基)-3-[4-(4,6-二吗啉-4-基-1,3,5-三嗪-2-基)苯基]脲的水性制剂

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201980037499.4A Active CN112218618B (zh) 2018-06-07 2019-06-04 包含1-(4-{[4-(二甲基氨基)哌啶-1-基]羰基}苯基)-3-[4-(4,6-二吗啉-4-基-1,3,5-三嗪-2-基)苯基]脲的水性制剂

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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030068340A1 (en) * 2001-08-20 2003-04-10 Boehringer Ingelheim Pharmaceuticals, Inc. Parenteral formulations of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea
CN102036995A (zh) * 2008-05-23 2011-04-27 惠氏有限责任公司 作为PI3激酶和mTOR抑制剂的三嗪化合物
CN106163503A (zh) * 2014-03-14 2016-11-23 辉瑞大药厂 包含治疗剂的治疗性纳米颗粒及其制造及使用方法
CN107205923A (zh) * 2014-12-17 2017-09-26 辉瑞大药厂 用于静脉内给药的pi3k/mtor‑抑制剂的制剂

Family Cites Families (10)

* Cited by examiner, † Cited by third party
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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
US20070111965A1 (en) * 2005-11-15 2007-05-17 Kipp James E Compositions comprising lipoxygenase inhibitors and cyclodextrin
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
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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030068340A1 (en) * 2001-08-20 2003-04-10 Boehringer Ingelheim Pharmaceuticals, Inc. Parenteral formulations of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea
CN102036995A (zh) * 2008-05-23 2011-04-27 惠氏有限责任公司 作为PI3激酶和mTOR抑制剂的三嗪化合物
CN106163503A (zh) * 2014-03-14 2016-11-23 辉瑞大药厂 包含治疗剂的治疗性纳米颗粒及其制造及使用方法
CN107205923A (zh) * 2014-12-17 2017-09-26 辉瑞大药厂 用于静脉内给药的pi3k/mtor‑抑制剂的制剂

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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
CA3102527A1 (en) 2019-12-12
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
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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