WO2018001270A1 - Promédicaments de palbociclib et leur composition - Google Patents

Promédicaments de palbociclib et leur composition Download PDF

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Publication number
WO2018001270A1
WO2018001270A1 PCT/CN2017/090534 CN2017090534W WO2018001270A1 WO 2018001270 A1 WO2018001270 A1 WO 2018001270A1 CN 2017090534 W CN2017090534 W CN 2017090534W WO 2018001270 A1 WO2018001270 A1 WO 2018001270A1
Authority
WO
WIPO (PCT)
Prior art keywords
palbociclib
compound
present
formula
prodrugs
Prior art date
Application number
PCT/CN2017/090534
Other languages
English (en)
Inventor
Chih-Ming Chen
Original Assignee
Noratech Pharmaceuticals, 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 Noratech Pharmaceuticals, Inc. filed Critical Noratech Pharmaceuticals, Inc.
Publication of WO2018001270A1 publication Critical patent/WO2018001270A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Definitions

  • the present invention relates to Palbociclib prodrugs.
  • Palbociclib (trade name Ibrance) (IUPAC name: 6-Acetyl-8-cyclopentyl-5-methyl-2- ⁇ [5- (1-piperazinyl) -2-pyridinyl] amino ⁇ pyrido [2, 3-d] pyrimidin-7 (8H) -one) is a drug for treating ER-positive and HER2-negative breast cancer, which has the following formula:
  • Palbociclib is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6.
  • the present invention provides a compound having the formula:
  • the present invention provides a compound having the formula:
  • the compounds of Formulae (I) and (II) may be used as Palbociclib prodrugs in treating breast cancer.
  • the present invention provides a pharmaceutical composition, which comprises a compound of the present invention, and a pharmaceutically acceptable excipient.
  • Fig. 1 shows the concentration of Palbociclib in the blood samples from Group K (administered with Palbociclib) .
  • Fig. 2 shows the concentration of Palbociclib in the blood samples from Group L (administered with compound of Formula (I)) .
  • Fig. 3 shows the concentration of Palbociclib in the blood samples from Group M (administered with compound of Formula (II)) .
  • Fig. 4 shows the averaged concentrations of Palbociclib in the blood samples from Groups K, L, and M, respectively.
  • the present invention provides a compound having the formula:
  • the present invention provides a compound having the formula:
  • the compounds of Formulae (I) and (II) may be used as Palbociclib prodrugs in treating breast cancer.
  • the present invention provides a pharmaceutical composition, which comprises a compound of the present invention, and a pharmaceutically acceptable excipient.
  • the compound of Formula (I) may be prepared by the following process:
  • the compound of Formula (I) may be prepared by the following process:
  • the pharmaceutical composition of the present invention can be manufactured by conventionally known methods with one or more pharmaceutically acceptable excipients or carriers.
  • pharmaceutically acceptable excipient encompasses any of the standard pharmaceutical carriers. Excipients include, by way of illustration and not limitation, solvents, thickening agents, wetting agents, lubricants, penetration enhancers. Such excipients include but are not limited to: saline, buffered saline, dextrose, water, glycerol, ethanol, propylene glycol, cremophor, nanoparticles, liposome, polymer, and combinations thereof.

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

L'invention concerne des promédicaments de Palbociclib et des compositions pharmaceutiques comprenant lesdits Palbociclib promédicaments.
PCT/CN2017/090534 2016-06-30 2017-06-28 Promédicaments de palbociclib et leur composition WO2018001270A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662357130P 2016-06-30 2016-06-30
US62/357,130 2016-06-30

Publications (1)

Publication Number Publication Date
WO2018001270A1 true WO2018001270A1 (fr) 2018-01-04

Family

ID=60785092

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2017/090534 WO2018001270A1 (fr) 2016-06-30 2017-06-28 Promédicaments de palbociclib et leur composition

Country Status (2)

Country Link
TW (1) TW201803875A (fr)
WO (1) WO2018001270A1 (fr)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005005426A1 (fr) * 2003-07-11 2005-01-20 Warner-Lambert Company Llc Sel d'iséthionate d'un inhibiteur sélectif de la cdk4
WO2013142427A1 (fr) * 2012-03-19 2013-09-26 Plexxikon Inc. Composés et procédés pour une modulation de la kinase, et indications correspondantes
WO2015022609A1 (fr) * 2013-08-14 2015-02-19 Novartis Ag Polythérapie pour le traitement du cancer
WO2016015598A1 (fr) * 2014-07-26 2016-02-04 Sunshine Lake Pharma Co., Ltd. 2-amino-pyrido [2,3-d] pyrimidin -7 (8h)-one utilisés en tant qu'inhibiteurs de cdk et utilisations de ceux-ci
WO2016065980A1 (fr) * 2014-10-30 2016-05-06 康朴生物医药技术（上海）有限公司 Dérivé d'isoindoline, son intermédiaire, son procédé de préparation, sa composition pharmaceutique et son utilisation

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005005426A1 (fr) * 2003-07-11 2005-01-20 Warner-Lambert Company Llc Sel d'iséthionate d'un inhibiteur sélectif de la cdk4
WO2013142427A1 (fr) * 2012-03-19 2013-09-26 Plexxikon Inc. Composés et procédés pour une modulation de la kinase, et indications correspondantes
WO2015022609A1 (fr) * 2013-08-14 2015-02-19 Novartis Ag Polythérapie pour le traitement du cancer
WO2016015598A1 (fr) * 2014-07-26 2016-02-04 Sunshine Lake Pharma Co., Ltd. 2-amino-pyrido [2,3-d] pyrimidin -7 (8h)-one utilisés en tant qu'inhibiteurs de cdk et utilisations de ceux-ci
WO2016065980A1 (fr) * 2014-10-30 2016-05-06 康朴生物医药技术（上海）有限公司 Dérivé d'isoindoline, son intermédiaire, son procédé de préparation, sa composition pharmaceutique et son utilisation

Also Published As

Publication number Publication date
TW201803875A (zh) 2018-02-01

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