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US 10,329,281 B2Granted
Polymorphs and process for the preparation of quinazolinyl derivatives
AssigneeHetero Labs Limited
InventorsBandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Bandi Vamsi Krishna, Nimmala Srinivas Rao
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Abstract
The present invention relates to Quinazolinyl derivatives polymorph, process and composition thereof. (I)
Claims14
An Afatinib solid Form selected from the group consisting of:
- Afatinib dimaleate crystalline Form H1 characterized by Powder X-Ray Diffraction, having the ° 2θ characteristic peaks at 5.0, 20.2, 25.6, 28.1±0.2 degrees;
- Afatinib dimaleate crystalline Form H2 characterized by Powder X-Ray Diffraction, having the ° 2θ characteristic peaks at 5.0, 5.4, 20.1, 25.8±0.2 degrees;
- Afatinib dimaleate crystalline Form H3 characterized by Powder X-Ray Diffraction, having the ° 2θ characteristic peaks at 5.3, 18.1, 24.7±0.2 degrees;
- Afatinib free base crystalline form Form H4 which is characterized by Powder X-Ray Diffraction, having the ° 2θ characteristic peaks at 5.3, 6.2, 12.3, 18.4±0.2 degrees;
- and
- Afatinib free base crystalline form Form H5, which is characterized by Powder X-Ray Diffraction, having the ° 2θ characteristic peaks at 6.1, 18.8, 23.6±0.2 degrees.
3 more elements
A process for the preparation of Afatinib dimaleate, which comprises:
- a. treating Afatinib base with a solvent;
- b. adding maleic acid solution;
- and
- b. isolating Afatinib dimaleate;
- wherein the solvent treated with an anti-oxidant, wherein the anti-oxidant is selected from the group consisting of butylated hydroxy toluene, butylated hydroxy anisole, further wherein the anti-oxidant is used in an amount of 0.1 to 5% w/w wrt Afatinib.
2 more elements
A process for the preparation of Afatinib free base crystalline form, which comprises:
- a. treating Afatinib base with an organic solvent or mixtures thereof;
- b. optionally adding water;
- and
- c. isolating Afatinib free base crystalline form;
- wherein organic solvent treated with an anti-oxidant, wherein the anti-oxidant is selected from the group consisting of butylated hydroxy toluene, butylated hydroxy anisole, further wherein the anti-oxidant is used in an amount of 0.1 to 5% w/w wrt Afatinib.
2 more elements
Dependencies are inferred from the claim text.