Abstract: The present invention provides novel co-crystal forms of dapagliflozin, namely a dapagliflozin lactose co-crystal and a dapagliflozin asparagine co-crystal, to pharmaceutical compositions comprising same, methods for their preparation and uses thereof for treating type 2 diabetes.
Abstract: The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.
Type:
Grant
Filed:
November 28, 2011
Date of Patent:
October 21, 2014
Assignee:
Mapi Pharma Ltd.
Inventors:
Ehud Marom, Michael Mizhiritskii, Shai Rubnov
Abstract: The present invention is based on the discovery of a process for preparing pyrimidin-dione compounds, especially alogliptin and its derivatives, which comprises the reaction of a urea derivative of formula (VIII) with a malonic acid or its derivatives to form intermediates of formulae (VII) or (VII-A), which are subsequently converted to a compound of formula (II) upon introduction of a leaving group X. Compound (II) then reacts with an amine to form compound (I), which is optionally converted to its salts of formula (IV).
Type:
Grant
Filed:
March 25, 2010
Date of Patent:
September 23, 2014
Assignee:
Mapi Pharma Ltd.
Inventors:
Ehud Marom, Michael Mizhiritskii, Shai Rubnov
Abstract: The present invention relates to a process for the preparation of darunavir, a nonpeptide protease inhibitor (PI), useful for the treatment of HIV/AIDS patients harboring multidrug-resistant HIV-1 variants that do not respond to previously existing HAART regimens. The present invention further relates to processes for the stereo-directed preparation of darunavir intermediates, in particular (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol and to certain novel intermediates obtained by such processes.
Abstract: The present invention relates to processes and intermediates for the preparation of derivatives of 2-arylthiazole such as Febuxostat and its analogs. Febuxostat which is an inhibitor of xanthine oxidase, is used for the treatment of chronic hyperuricaemia in conditions in which urate deposition has occurred, such as gouty arthritis.
Type:
Application
Filed:
January 23, 2012
Publication date:
August 14, 2014
Applicant:
MAPI PHARMA LTD.
Inventors:
Michael Mizhiritskii, Ehud Marom, Shai Rubnov
Abstract: Long acting parenteral pharmaceutical compositions comprising a therapeutically effective amount of glatiramer are provided. In particular, the long acting pharmaceutical composition comprises a therapeutically effective amount of glatiramer acetate in depot form suitable for administering at a medically acceptable location in a subject in need thereof. The depot form is suitable for subcutaneous or intramuscular implantation or injection.
Abstract: The present invention relates to processes for the preparation of deferasirox, an oral iron chelator developed to treat iron overload due to e.g. multiple blood transfusions. The present invention further provides novel deferasirox pseudopolymorphs and a novel amorphous form of deferasirox, processes for their preparation, as well as pharmaceutical compositions comprising same, and use thereof in treating iron overload.
Type:
Grant
Filed:
January 28, 2010
Date of Patent:
July 8, 2014
Assignee:
Mapi Pharma Ltd.
Inventors:
Michael Mizhiritskii, Ehud Marom, Shai Rubnov
Abstract: The present invention relates to a process for the preparation of Lurasidone or a pharmaceutically acceptable salt thereof, a compound useful for the treatment of schizophrenia and bipolar disorder. The present invention further relates to processes for the preparation of Lurasidone intermediates, and to certain novel intermediates obtained by such processes.
Type:
Application
Filed:
June 13, 2012
Publication date:
June 26, 2014
Applicant:
MAPI PHARMA LTD.
Inventors:
Ehud Marom, Michael Mizhiritskii, Susanna Tchilibon, Shai Rubnov
Abstract: The present invention relates to a process for the synthesis of (3beta)17-(3-pyridinyl)androsta-5,16-dien-3-yl acetate (Abiraterone acetate) represented by the structure of formula (1), and salts thereof, especially salts with pharmaceutically acceptable acids. The present invention further relates to certain intermediates in such processes.
Type:
Application
Filed:
February 10, 2014
Publication date:
June 5, 2014
Applicant:
MAPI PHARMA LTD.
Inventors:
Ehud MAROM, Shai RUBNOV, Michael MIZHIRITSKII
Abstract: The present invention relates to processes for the preparation of (2-Amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol hydrochloride (Fingolimod) and pharmaceutically acceptable salts thereof, and intermediates formed in such processes.
Type:
Grant
Filed:
October 27, 2011
Date of Patent:
May 27, 2014
Assignee:
Mapi Pharma Ltd.
Inventors:
Ehud Marom, Michael Mizhiritskii, Shai Rubnov
Abstract: The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.
Type:
Application
Filed:
November 28, 2011
Publication date:
September 19, 2013
Applicant:
MAPI PHARMA LTD.
Inventors:
Ehud Marom, Michael Mizhiritskii, Shai Rubnov
Abstract: The present invention relates to processes for the preparation of (2-Amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol hydrochloride (Fingolimod) and pharmaceutically acceptable salts thereof, and intermediates formed in such processes.
Type:
Application
Filed:
October 27, 2011
Publication date:
August 22, 2013
Applicant:
MAPI PHARMA LTD.
Inventors:
Ehud Marom, Michael Mizhiritskii, Shai Rubnov
Abstract: The present invention relates to a synthetic polypeptide which is a random linear pentapolymer comprising alanine, glutamic acid, lysine, tyrosine and phenylalanine and use thereof in treating autoimmune diseases, in particular multiple sclerosis.
Abstract: The present invention discloses processes for the preparation of 3-[(1R,2R)-3-(dimethyl-amino)-1-ethyl-2-methyl-propyl]phenol (Tapentadol), salts thereof and related compounds of formula (A), including stereoisomers and pharmaceutically acceptable salts thereof, and to certain intermediates used in such process.
Abstract: Long acting parenteral pharmaceutical compositions comprising a therapeutically effective amount of glatiramer are provided. In particular, the present invention provides a long acting pharmaceutical composition comprising a therapeutically effective amount of glatiramer acetate in depot form suitable for administering at a medically acceptable location in a subject in need thereof. The depot form is suitable for subcutaneous or intramuscular implantation or injection.
Abstract: The present invention provides long acting parenteral pharmaceutical compositions comprising a therapeutically effective amount of glatiramer. In particular, the present invention provides a long acting pharmaceutical composition comprising a therapeutically effective amount of glatiramer acetate in depot form suitable for administering at a medically acceptable location in a subject in need thereof. The depot form is suitable for subcutaneous or intramuscular implantation or injection.
Abstract: The present invention provides long acting parenteral pharmaceutical compositions comprising a therapeutically effective amount of glatiramer. In particular, the present invention provides a long acting pharmaceutical composition comprising a therapeutically effective amount of glatiramer acetate in depot form suitable for administering at a medically acceptable location in a subject in need thereof. The depot form is suitable for subcutaneous or intramuscular implantation or injection.