Crystalline bortezomib process
First Claim
1. A process for preparing Bortezomib (Ia) crystalline Form-SB
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Abstract
The present invention provides process for preparation of crystalline Bortezomib (Ia) as its monohydrate which is designated as crystalline Form-SB
and characterized by having water content ranging between 3.5-6.0% w/w; X-ray powder diffraction pattern comprising characteristic 2θ° peaks selected from the XRPD peak set of 5.6, 7.5, 9.8, 10.2, 11.3, 15.1, 18.0, 20.5, 21.5 and 23.6±0.20 2θ°, wherein peaks at 9.8 and 11.39±0.20 2θ° are un-split and 100% intensity peak is present at 5.6±0.20 2θ°, DSC isotherm comprising the endothermic peaks ranging between 45 to 60° C. (Peak-1) and 175 to 185° C. (Peak-2) and IR absorption characteristic peaks approximately at 3387 cm−1, 3304 cm−1, 2953 cm−1, 2927 cm−1, 2868 cm−1, 1627 cm−1, 1455 cm−1, 1400 cm−1, 1201 cm−1, 1150 cm−1, 1020 cm−1, 747 cm−1 and 702 cm−1 and Raman absorption spectra having characteristic peaks approximately at 3066 cm−1, 1583 cm−1, 1528 cm−1, 1281 cm−1, 1213 cm−1, 1035 cm−1, 1022 cm−1 and 1004 cm−1. The invention also provides the use of said crystalline Form-SB as active pharmaceutical ingredient in pharmaceutical compositions for the treatment of cancer.
6 Citations
10 Claims
- 1. A process for preparing Bortezomib (Ia) crystalline Form-SB
-
4. Bortezomib (Ia) as monohydrate crystalline Form-SB characterized by having water content of 3.5-6% w/w;
- X-ray powder diffraction pattern comprising characteristic 2θ
°
peaks selected from the XRPD peak set of 5.6, 7.5, 9.8, 10.2, 11.3, 15.1, 18.0, 20.5, 21.5 and 23.6±
0.20 2θ
°
, wherein peaks at 9.8 and 11.39±
0.20 2θ
°
are un-split and 100% intensity peak is present at 5.6±
0.20 2θ
°
. - View Dependent Claims (5, 6, 7)
- X-ray powder diffraction pattern comprising characteristic 2θ
-
8. Bortezomib (Ia) crystalline Form-SB characterized by X-ray powder diffraction pattern comprising the characteristic 2θ
- °
peaks of 5.6, 7.5, 9.8, 10.2, 11.3, 15.1, 18.0, 20.5, 21.5 and 23.6±
0.20 2θ
°
, wherein peaks at 9.8 and 11.39±
0.20 2θ
°
are un-split and 100% intensity peak is present at 5.6±
0.20 2θ
°
, DSC isotherm comprising the endothermic peaks ranging between 45 to 60°
C. (Peak-1) and 175 to 185°
C. (Peak-2) and IR absorption characteristic peaks at approximately 3387 cm−
1, 3304 cm−
1, 2953 cm−
1, 2927 cm−
1, 2868 cm−
1, 1627 cm−
1, 1455 cm−
1, 1400 cm−
1, 1201 cm−
1, 1150 cm−
1, 1020 cm−
1, 747 cm−
1 and 702 cm−
1. - View Dependent Claims (9, 10)
- °
Specification
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- Resources
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Current AssigneeShilpa Medicare Limited
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Original AssigneeShilpa Medicare Limited
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InventorsShrawat, Vimal Kumar, Rafiuddin, Singh, Vinod Kumar, Chaturvedi, Akshay Kant
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Primary Examiner(s)Balasubramanian, Venkataraman
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Application NumberUS14/434,105Publication NumberTime in Patent Office770 DaysField of Search544/229US Class Current1/1CPC Class CodesA61P 35/00 Antineoplastic agentsC07B 2200/13 Crystalline forms, e.g. pol...C07D 241/12 with only hydrogen atoms, h...C07F 5/025 Boronic and borinic acid co...
