Crystal of substituted piperidine compound, salts of substituted piperidine compound, and crystals thereof
AssigneeEisai R&D Management Co., Ltd.
InventorsIkuo Kushida, Yoko Ito, So Yasui, Takashi Fukuyama, Nobuaki Sato, Taro Asaba
Life of this patent
Estimating the term…
Abstract
Crystals of compounds represented by formula (I) having potential as drug substances for pharmaceuticals, as well as salts of compounds represented by formula (I) and their crystals.
Claims33
(canceled)
A crystal of (2R)-2-cyclopropyl-2-{(1R,3S,5S)-3-[(3S,4R)-1-(5-fluoropyrimidin-2-yl)-3-methoxypiperidin-4-yl]-8-azabicyclo[3.2.1]octan-8-yl}acetamide mono D-tartrate represented by formula (II):
- or
- a crystal of (2R)-2-cyclopropyl-2-{(1R,3S,5S)-3-[(3S,4R)-1-(5-fluoropyrimidin-2-yl)-3-methoxypiperidin-4-yl]-8-azabicyclo[3.2.1]octan-8-yl}acetamide hemioxalate represented by formula (III):
A Form α crystal of (2R)-2-cyclopropyl-2-{(1R,3S,5S)-3-[(3S,4R)-1-(5-fluoropyrimidin-2-yl)-3-methoxypiperidin-4-yl]-8-azabicyclo[3.2.1]octan-8-yl}acetamide represented by formula (I):
- having one or more diffraction peaks selected from the group consisting of diffraction angles (2θ±0.2°) of 12.2°, 12.8°, 15.5°, 21.2° and 24.6° in a powder X-ray diffraction.
-7. (canceled)
A Form α crystal of (2R)-2-cyclopropyl-2-{(1R,3S,5S)-3-[(3S,4R)-1-(5-fluoropyrimidin-2-yl)-3-methoxypiperidin-4-yl]-8-azabicyclo[3.2.1]octan-8-yl}acetamide represented by formula (I):
- having peaks at chemical shifts (δ±0.5 ppm) of 49.2 ppm, 67.6 ppm and 72.5 ppm in a solid state 13C NMR spectrum.
-10. (canceled)
A Form α crystal of (2R)-2-cyclopropyl-2-{(1R,3S,5S)-3-[(3S,4R)-1-(5-fluoropyrimidin-2-yl)-3-methoxypiperidin-4-yl]-8-azabicyclo[3.2.1]octan-8-yl}acetamide represented by formula (I):
- having Raman shift peaks (±2 cm−1) at 842.1 cm−1, 895.0 cm−1 and 1199.4 cm−1 in Raman spectrophotometry.
(canceled)
A Form β crystal of (2R)-2-cyclopropyl-2-{(1R,3S,5S)-3-[(3S,4R)-1-(5-fluoropyrimidin-2-yl)-3-methoxypiperidin-4-yl]-8-azabicyclo[3.2.1]octan-8-yl}acetamide represented by formula (I):
- having one or more diffraction peaks selected from the group consisting of diffraction angles (2θ±0.2°) of 4.9°, 9.8°, 11.8°, 14.6° and 16.1° in a powder X-ray diffraction.
-17. (canceled)
A Form β crystal of (2R)-2-cyclopropyl-2-{(1R,3S,5S)-3-[(3S,4R)-1-(5-fluoropyrimidin-2-yl)-3-methoxypiperidin-4-yl]-8-azabicyclo[3.2.1]octan-8-yl}acetamide represented by formula (I):
- having peaks at chemical shifts (δ±0.5 ppm) of 74.1 ppm, 159.2 ppm and 177.7 ppm in a solid state 13C NMR spectrum.
-20. (canceled)
A Form β crystal of (2R)-2-cyclopropyl-2-{(1R,3S,5S)-3-[(3S,4R)-1-(5-fluoropyrimidin-2-yl)-3-methoxypiperidin-4-yl]-8-azabicyclo[3.2.1]octan-8-yl}acetamide represented by formula (I):
- having Raman shift peaks (±2 cm−1) at 889.9 cm−1, 1089.4 cm−1 and 1194.6 cm−1 in Raman spectrophotometry.
(canceled)
-27. (canceled)
(canceled)
-34. (canceled)
-37. (canceled)
Dependencies are inferred from the claim text.