WO2018001270A1 - Promédicaments de palbociclib et leur composition - Google Patents
Promédicaments de palbociclib et leur composition Download PDFInfo
- 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
- 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.)
- Ceased
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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.
Landscapes
- 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.
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 Ceased 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)
| 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 |
-
2017
- 2017-06-28 WO PCT/CN2017/090534 patent/WO2018001270A1/fr not_active Ceased
- 2017-06-29 TW TW106121845A patent/TW201803875A/zh unknown
Patent Citations (5)
| 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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