Isethionate salt of a selective CDK4 inhibitor
First Claim
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1. An 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 comprising a mono-isethionate salt of Form A, characterized by one or more of the following:
- a powder X-ray diffraction pattern having peaks at 2θ
values of about 8.7, 13.5, and 17.6, or a Raman spectrum having peaks at Raman Shift values of about 1600 cm−
1, 1290 cm−
1, 675 cm−
1, 470 cm−
1, 450 cm−
1, and 425 cm−
1, or a DSC thermogram having a sharp endotherm at about 273°
C.
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Abstract
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.
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Citations
4 Claims
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1. An 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 comprising a mono-isethionate salt of Form A, characterized by one or more of the following:
- a powder X-ray diffraction pattern having peaks at 2θ
values of about 8.7, 13.5, and 17.6, or a Raman spectrum having peaks at Raman Shift values of about 1600 cm−
1, 1290 cm−
1, 675 cm−
1, 470 cm−
1, 450 cm−
1, and 425 cm−
1, or a DSC thermogram having a sharp endotherm at about 273°
C. - View Dependent Claims (4)
- a powder X-ray diffraction pattern having peaks at 2θ
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2. An 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 comprising a mono-isethionate salt of Form B, characterized by one or more of the following:
- a powder X-ray diffraction pattern having peaks at 2θ
values of about 5.1, 11.8, 12.1, 12.8, 13.1, and 14.7, a Raman spectrum having peaks at Raman Shift values of about 1600 cm−
1, 1290 cm−
1, 470 cm−
1, 450 cm−
1, and 425 cm−
1, but no substantial peak at 675 cm−
1, or a DSC thermogram having a sharp endotherm at about 271°
C.
- a powder X-ray diffraction pattern having peaks at 2θ
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3. An 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 comprising a mono-isethionate salt of Form D, characterized by one or more of the following:
- a powder X-ray diffraction pattern having peaks at 2θ
values of about 8.4, 8.9, and 21.9, a Raman spectrum having a peak at a Raman Shift value of about 463 cm−
1, or a DSC thermogram having a sharp endotherm at about 277°
C.
- a powder X-ray diffraction pattern having peaks at 2θ
Specification