Process of Preparation of Olanzapine Form I

• US 20080188465A1
• Filed: 10/30/2007
• Published: 08/07/2008
• Est. Priority Date: 05/31/2002
• Status: Abandoned Application

• Current Assignee: Sandoz Ag (Novartis Ag)
• Original Assignee: Sandoz Ag (Novartis Ag)
• Inventors: Patel, Mahendra R., Patel, Pramod B., Ray, Anup K., Patel, Hiren V.
• Application Number:
  US11/928,791
• Publication Number:
  US 20080188465A1
• Time in Patent Office: Days
• US Class Current: 514/220
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: C07D 495/04 Ortho-condensed systems

Abstract

A process for the preparation of polymorph Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2.3-b][1,5]benzodiazepine, or olanzapine.

Claims

1-17. -17. (canceled)

18. Olanzapine Form I having a polymorphic purity of at least 98%, having an X-ray diffraction pattern characterized by the following interplanar spacing values (d) and relative intensities (I/I₀)

19. Olanzapine Form I of claim 18 having a polymorphic purity of at least 99%.

20. Olanzapine Form I of claim 18 substantially free of olanzapine Form II.

21. A pharmaceutical composition comprising a compound of claim 18 and a pharmaceutically acceptable diluent or carrier therefor.

22. A method of treating a person suffering from or being, susceptible to psychosis, acute mania, or mild anxiety states which comprises administering to said person an effective amount of a compound of claim 18.