- PROCESS FOR PREPARATION OF PALBOCICLIB
-
The present application relates to a process for the preparation of crystalline form A of palbociclib having specific surface area more than 2m2/g comprising one-pot process for the preparation of compound of formula (IV). The present application further relates to the preparation of acid-addition salts of palbociclib and their use for the synthesis of crystalline form A of palbociclib having specific surface area more than 2 m2/g.
- -
-
-
- PREPARATION METHODS FOR PALBOCICLIB FREE BASE CRYSTAL FORM A AND CRYSTAL FORM B
-
Disclosed is a preparation method for a Palbociclib free base crystal form A as shown in Formula I, comprising the following steps: treating a Palbociclib free base and/or a Palbociclib salt compound by using an inorganic base in a water solvent at the temperature of 35 to 100° C. to obtain a Palbociclib free base crystal form A, the water solvent being water or mixed solvent obtained by water and an organic solvent capable of being mixed and disclosed in the water. Also disclosed is a preparation method for a Palbociclib free base crystal form B, comprising the following steps: treating a Palbociclib salt compound by using an inorganic base in a water solvent at the temperature of 0 to 20° C. to obtain a Palbociclib free crystal form B, the water solvent being water or a mixed solvent obtained by water and an organic solvent capable of being mixed and dissolved in the water. The method is safe and convenient in operation and low in pollution, and facilitates industrial production.
- -
-
Paragraph 0040
(2018/11/26)
-
- Now crystal form of antitumor drug, preparation method and uses thereof
-
The present invention discloses the crystal form C of a compound represented by a formula I, a preparation method and uses thereof, wherein the X-ray powder diffraction (XRPD) of the crystal form C has the following 2[theta] angle characteristic peaks: 5.56+/-0.2 DEG, 7.68+/-0.2 DEG and 8.67+/-0.2 DEG. The formula I is defined in the specification.
- -
-
Paragraph 0097; 0098; 0099; 0100
(2017/08/27)
-
- Preparation method of palbociclib crystal form A
-
The invention provides a preparation method of a palbociclib crystal form A. The preparation method is simple and easy to perform. The used reagents are all common reagents. The preparation method is suitable for industrial massive production. The product purity is high and meets requirements of pharmaceutical crystal form.
- -
-
Paragraph 0055; 0056
(2017/08/27)
-
- SALTS AND CRYSTALLINE FORMS OF 6-ACETYL-8-CYCLOPENTYL-5-METHYL-2((5-(PIPERAZIN-1-YL)PYRIDIN-2-YL)AMINO)PYRIDO[2,3-D] PYRIMIDIN-7(8H)-ONE (PALBOCICLIB)
-
New salts and crystalline Forms of palbociclib, processes for their preparation, pharmaceutical compositions comprising the new salts or crystalline Forms, and use of the new salts and crystalline Forms of palbociclib for treating or delaying diseases or
- -
-
Page/Page column 38-40
(2016/06/28)
-
- Preparation method of Palbociclib isethionate
-
The invention belongs to the field of chemical medicine synthesis technology, and more specifically relates to a preparation method of Palbociclib isethionate. The method comprises four steps and is used for preparing Palbociclib, that is 2-(pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-one isethionate. The method has the advantages of mild process conditions, simple post-treatment, high purity, low reaction cost, and easy industrial production.
- -
-
-
- SYNTHESIS OF 2-(PYRIDIN-2-YLAMINO)-PYRIDO[2,3-D]PYRIMIDIN-7-ONES
-
The present invention provides methods of preparing substituted 2-(pyridin-2-ylamino)-pirido[2,3- d]pyrimidin-7-ones (formula 1 ), useful in treating cell proliferative disorders, or a pharmaceutically acceptable salt thereof.
- -
-
Page/Page column 28
(2008/06/13)
-
- ISETHIONATE SALT OF A SELECTIVE CDK4 INHIBITOR
-
Disclosed are polymorphs of the isethionate salt of 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one, which is a selective cyclin-dependent kinase 4 (CDK4) inhibitor useful for treating inflammation and cell proliferative diseases such as cancer and restenosis.
- -
-
Page/Page column 25; 26
(2008/06/13)
-
- Combinations of signal transduction inhibitors
-
The present invention relates to methods for treating cancer comprising utilizing a combination of signal transduction inhibitors. More specifically, the present invention relates to combinations of so called cell cycle inhibitors with mitogen stimulated kinase signal transduction inhibitors, more specifically combinations of CDK inhibitors with mitogen stimulated kinase signal transduction inhibitors, more preferably MEK inhibitors. Other embodiments of the invention relate to additional combinations of the aforesaid combinations with standard anti-cancer agents such as cytotoxic agents, palliatives and antiangiogenics. Most specifically this invention relates to combinations of 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one including salt forms, which is a selective cyclin-dependent kinase 4 (CDK4) inhibitor, in combination with one or more MEK inhibitors, most preferably N-[(R)-2,3-dihydroxy-propoxy]-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide. The aforementioned combinations are useful for treating inflammation and cell proliferative diseases such as cancer and restenosis.
- -
-
Page/Page column 28
(2010/02/14)
-