IL252158B - Formulations of a pi3k/mtor-inhibitor for intravenous administration - Google Patents

Formulations of a pi3k/mtor-inhibitor for intravenous administration

Info

Publication number
IL252158B
IL252158B IL252158A IL25215817A IL252158B IL 252158 B IL252158 B IL 252158B IL 252158 A IL252158 A IL 252158A IL 25215817 A IL25215817 A IL 25215817A IL 252158 B IL252158 B IL 252158B
Authority
IL
Israel
Prior art keywords
pi3k
intravenous administration
mtor inhibitor
inhibitor formulations
formulations
Prior art date
Application number
IL252158A
Other languages
English (en)
Hebrew (he)
Other versions
IL252158A0 (en
Original Assignee
Pfizer
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 filed Critical Pfizer
Publication of IL252158A0 publication Critical patent/IL252158A0/en
Publication of IL252158B publication Critical patent/IL252158B/en

Links

Classifications

    • 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
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/17Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic rings
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K47/12Carboxylic acids; Salts or anhydrides 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
    • A61K47/06Organic 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
    • 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
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Dermatology (AREA)
  • Inorganic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
IL252158A 2014-12-17 2017-05-08 Formulations of a pi3k/mtor-inhibitor for intravenous administration IL252158B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462093060P 2014-12-17 2014-12-17
US201562250633P 2015-11-04 2015-11-04
PCT/IB2015/059515 WO2016097949A1 (en) 2014-12-17 2015-12-10 Formulations of a pi3k/mtor-inhibitor for intravenous administration

Publications (2)

Publication Number Publication Date
IL252158A0 IL252158A0 (en) 2017-07-31
IL252158B true IL252158B (en) 2021-01-31

Family

ID=54937330

Family Applications (1)

Application Number Title Priority Date Filing Date
IL252158A IL252158B (en) 2014-12-17 2017-05-08 Formulations of a pi3k/mtor-inhibitor for intravenous administration

Country Status (25)

Country Link
US (2) US10172942B2 (https=)
EP (1) EP3233054B1 (https=)
JP (1) JP6420753B2 (https=)
KR (1) KR102016822B1 (https=)
CN (1) CN107205923B (https=)
AU (1) AU2015365497B2 (https=)
CA (1) CA2915199C (https=)
CY (1) CY1124527T1 (https=)
DK (1) DK3233054T3 (https=)
ES (1) ES2881214T3 (https=)
HR (1) HRP20211446T1 (https=)
HU (1) HUE055928T2 (https=)
IL (1) IL252158B (https=)
LT (1) LT3233054T (https=)
MX (1) MX380172B (https=)
NZ (1) NZ731518A (https=)
PL (1) PL3233054T3 (https=)
PT (1) PT3233054T (https=)
RS (1) RS62337B1 (https=)
RU (1) RU2672875C1 (https=)
SG (1) SG11201703826TA (https=)
SI (1) SI3233054T1 (https=)
TW (1) TWI660729B (https=)
WO (1) WO2016097949A1 (https=)
ZA (1) ZA201703764B (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS62663B1 (sr) 2017-08-25 2021-12-31 Pfizer Farmaceutska vodena formulacija koja sadrži 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]ureu
MX2020013238A (es) * 2018-06-07 2021-02-22 Pfizer Formulacion acuosa que comprende 1-(4-{[4-(dimetilamino)piperidin- 1-il]carbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il )fenil]urea.
WO2023009438A1 (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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009143313A1 (en) * 2008-05-23 2009-11-26 Wyeth Triazine compounds as p13 kinase and mtor inhibitors

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0852951A1 (de) * 1996-11-19 1998-07-15 Roche Diagnostics GmbH Stabile lyophilisierte pharmazeutische Zubereitungen von mono- oder polyklonalen Antikörpern
KR20080018908A (ko) * 2005-05-27 2008-02-28 바이엘 헬스케어 아게 암 치료용 디아릴 우레아 화합물 및 pi3, akt 키나제또는 mtor 억제제 (라파마이신)를 포함하는 병용요법
US20080234262A1 (en) * 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
DE202008001253U1 (de) * 2008-01-28 2008-04-10 Mirror Image Ag Bildanzeigegerät
JP2011521968A (ja) * 2008-05-30 2011-07-28 ジェネンテック, インコーポレイテッド プリンpi3k阻害剤化合物および使用方法
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
WO2014078522A1 (en) * 2012-11-14 2014-05-22 Ohio State Innovation Foundation Materials and methods useful for treating glioblastoma
EP2968191B1 (en) * 2013-03-14 2021-06-16 Abraxis BioScience, LLC Methods of treating bladder cancer
MA39734B1 (fr) * 2014-03-14 2019-07-31 Pfizer Nanoparticules thérapeutiques comportant un agent thérapeutique, et leurs procédés de fabrication et d'utilisation

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009143313A1 (en) * 2008-05-23 2009-11-26 Wyeth Triazine compounds as p13 kinase and mtor inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
VENKATESAN AM ET AL., BIS(MORPHOLINO-1,3,5-TRIAZINE) DERIVATIVES: POTENT ADENOSINE 5'-TRIPHOSPHATE COMPETITIVE PHOSPHATIDYLINOSITOL-3-KINASE/MAMMALIAN TARGET OF RAPAMYCIN INHIBITORS: DISCOVERY OF COMPOUND 26 (PKI-587), A HIGHLY EFFICACIOUS DUAL INHIBITOR, 1 March 2010 (2010-03-01) *

Also Published As

Publication number Publication date
HRP20211446T1 (hr) 2021-12-24
EP3233054A1 (en) 2017-10-25
BR112017010841A2 (pt) 2017-12-26
ES2881214T3 (es) 2021-11-29
EP3233054B1 (en) 2021-06-30
SI3233054T1 (sl) 2021-11-30
AU2015365497A1 (en) 2017-06-01
TWI660729B (zh) 2019-06-01
TW201632188A (zh) 2016-09-16
RS62337B1 (sr) 2021-10-29
MX380172B (es) 2025-03-12
LT3233054T (lt) 2021-07-26
CN107205923B (zh) 2021-03-05
AU2015365497B2 (en) 2020-07-02
US20190105390A1 (en) 2019-04-11
CN107205923A (zh) 2017-09-26
SG11201703826TA (en) 2017-07-28
JP6420753B2 (ja) 2018-11-07
WO2016097949A1 (en) 2016-06-23
JP2016113461A (ja) 2016-06-23
US10660959B2 (en) 2020-05-26
IL252158A0 (en) 2017-07-31
RU2672875C1 (ru) 2018-11-20
CA2915199C (en) 2018-11-06
CY1124527T1 (el) 2022-07-22
NZ731518A (en) 2019-03-29
MX2017008072A (es) 2017-09-28
PT3233054T (pt) 2021-08-02
PL3233054T3 (pl) 2021-12-20
KR102016822B1 (ko) 2019-08-30
DK3233054T3 (da) 2021-08-02
CA2915199A1 (en) 2016-06-17
KR20170082638A (ko) 2017-07-14
US20170360935A1 (en) 2017-12-21
HUE055928T2 (hu) 2022-01-28
US10172942B2 (en) 2019-01-08
ZA201703764B (en) 2020-11-25

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