Abstract: The invention relates to pharmaceutical compositions comprising anhydrous(2R,3S)4-acetoxy-2-a-benzoyloxy-5?-20-epoxy-1,7-?-10-?-tri-hydroxy-9-oxo-tax-11-en-13?-il 3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate (I)(docetaxel) and 4-acetoxy-2-?-benzoyloxy-5-?-20-epoxy-1,7?-10-?-tri-hydroxy-9-oxo-tax-11-en-13?-il (2R,3S)3-benzoylamino-2-hydroxy-3-phenylpropionate (II) (paclitaxel), methods for treating neoplastic tumors using anhydrous docetaxel and paclitaxel, and a process for the preparation of the anhydrous docetaxel and paclitaxel.
Type:
Grant
Filed:
August 7, 2008
Date of Patent:
November 6, 2012
Assignees:
Quiral Quimica Do Brasil S.A., Biorganica Ltda.
Inventors:
Marco Antônio Santini, Antônio Machado, Aurélio Maranduba, Eneida Guimarães, Marcio Santiago Junior, Maria Silva
Abstract: This invention describes a process for the production of ANHYDROUS active pharmaceutical ingredients (APIs); a process for the preparation of HYDRATED active pharmaceutical ingredients, a process for the preparation of sterile and stable injectable solutions, and their use, more specifically, APIs which are taxane derivatives, especially (2R,3S) 4-acetoxy-2-?-benzoyloxy-5?-20-epoxy-1,7-?-10-?-tri-hydroxy-9-oxo-tax-11-en-13?-il 3-tert-butoxy carbonylamino-2-hydroxy-3-phenylpropionate (I); 4-acetoxy-2-?-benzoyloxy-5-?-20-epoxy-1,7?-10-?-tri-hidroxy-9-oxo-tax-11-en-13?-il (2R,3S) 3-benzoylamino-2-hydroxy-3-phenylpropionate (II), and particularly 4-acetoxy-2-?-benzoyloxy-5?-20-epoxy-1, 7-?-10-?-tri-hidroxy-9-oxo-tax-11-en-13?-il (2R,3S) 3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate tri-hydrate (III).
Type:
Grant
Filed:
December 10, 2004
Date of Patent:
November 23, 2010
Assignees:
Quiral Quimica do Basil S.A., Biorganica LTDA.
Inventors:
Marco Antônio Santini, Antônio Machado, Aurélio Maranduba, Eneida Guimarães, Marcio Santiago Junior, Maria Silva
Abstract: Pharmaceutical compositions containing polysorbate 80, anhydrous docetaxel (I) or its trihydrate and an organic acid with a pKa between 2.5-4.5 employed as a degradation inhibitor.
Type:
Application
Filed:
February 9, 2006
Publication date:
September 3, 2009
Applicants:
Quiral Quimica DO Brasil S.A., Biorganica Ltda.
Inventors:
Antonio Machado, Aurelio Maranduba, Eneida Guimaraes, Livia Machado, Marcio Santiago, JR., Maria Silva
Abstract: The invention relates to pharmaceutical compositions comprising anhydrous(2R,3S)4-acetoxy-2-a-benzoyloxy-5?-20-epoxy-1,7-?-10-?-tri-hydroxy-9-oxo-tax-11-en-13?-il 3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate (I)(docetaxel) and 4-acetoxy-2-?-benzoyloxy-5-?-20-epoxy-1,7?-10-?-tri-hydroxy-9-oxo-tax-11-en-13?-il (2R, 3S)3-benzoylamino-2-hydroxy-3-phenylpropionate (II) (paclitaxel), methods for treating neoplastic tumors using anhydrous docetaxel and paclitaxel, and a process for the preparation of the anhydrous docetaxel and paclitaxel.
Type:
Application
Filed:
August 7, 2008
Publication date:
March 12, 2009
Applicants:
QUIRAL QUIMICA DO BRASIL, BIORGANICA LTDA.
Inventors:
Marco Antonio SANTINI, Antonio Machado, Aurelio Maranduba, Eneida Guimaraes, Marcio Santiago Junior, Maria Silva
Abstract: This invention describes a process for the production of ANHYDROUS active pharmaceutical ingredients (APIs); a process for the preparation of HYDRATED active pharmaceutical ingredients, a process for the preparation of sterile and stable injectable solutions, and their use, more specifically, APIs which are taxane derivatives, especially (2R,3S) 4-acetoxy-2-?-benzoyloxy-5?-20-epoxy-1,7-?-10-?-tri-hydroxy-9-oxo-tax-11-en-13?-il 3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate (I); 4-acetoxy-2-?-benzoyloxy-5-?-20-epoxy-1, 7?-10-?-tri-hidroxy-9-oxo-tax-11-en-13?-il (2R,3S) 3-benzoylamino-2-hydroxy-3-phenylpropionate (II), and particularly 4-acetoxy-2-?-benzoyloxy-5?-20-epoxy-1,7-?-10-?-tri-hidroxy-9-oxo-tax-11-en-13?-il (2R,3S) 3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate tri-hydrate (III).
Type:
Application
Filed:
December 10, 2004
Publication date:
February 28, 2008
Applicant:
BIORGANICA LTDA.
Inventors:
Marco Antonio Santini, Antonio Machado, Aurelio Maranduba, Eneida Guimaraes, Marcio Santiago, Maria Silva