Abstract: The present invention relates to extended-release pharmaceutical compositions comprising pregabalin or a salt thereof, which are adapted to release the pregabalin active ingredient according to a dual release profile. The formulations comprise two components, the first (fast ER) providing extended-release of the active ingredient in a short controlled manner lasting from about 4 to about 6 hours, and the second (slow ER or maintenance) providing extended release of the active ingredient over a period of 24 hours. The proportion of each component in the formulation may be adjusted to achieve the desired AUC and therapeutic effect following oral administration to a subject. The invention further relates to methods of using the pharmaceutical compositions for treating conditions and disorders which are responsive to pregabalin treatment, such as neuropathic pain associated with diabetic peripheral neuropathy (DPN), post herpetic neuralgia (PHN), epilepsy, seizures and fibromyalgia.
Abstract: The present invention describes a process for the synthesis of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-di-hydro-pyridin-2-one (Perampanel) represented by the structure of formula (1), and salts thereof, especially salts with pharmaceutically acceptable acids. The present invention further relates to certain intermediates formed and/or used in such process.
Abstract: The present invention provides a new amorphous form of apremilast, pharmaceutical compositions comprising same, methods for preparation and use thereof in treating conditions mediated by inhibition of TNF-? production or inhibition of phosphodiesterase 4 (PDE4), e.g., psoriatic arthritis and other chronic inflammatory diseases.
Abstract: The present invention describes a process for the synthesis of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-di-hydro-pyridin-2-one (Perampanel) represented by the structure of formula (1), and salts thereof, especially salts with pharmaceutically acceptable acids. The present invention further relates to certain intermediates formed and/or used in such process.
Abstract: The present invention provides a new amorphous form of apremilast, pharmaceutical compositions comprising same, methods for preparation and use thereof in treating conditions mediated by inhibition of TNF-? production or inhibition of phosphodiesterase 4 (PDE4), e.g., psoriatic arthritis and other chronic inflammatory diseases.
Abstract: The present invention relates to a process for the preparation of (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylene-1-piperidinyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol (Efinaconazole) and intermediates used in such process.
Type:
Grant
Filed:
March 2, 2015
Date of Patent:
April 11, 2017
Assignee:
MAPI PHARMA LTD.
Inventors:
Anna Gopin, Shai Rubnov, Galina Zats, Ehud Marom
Abstract: The present invention relates to a process for the preparation of (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylene-1-piperidinyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol (Efinaconazole) and intermediates used in such process.
Type:
Application
Filed:
March 2, 2015
Publication date:
December 8, 2016
Applicant:
MAPI PHARMA LTD.
Inventors:
Anna GOPIN, Shai RUBNOV, Galina ZATS, Ehud MAROM
Abstract: The present invention provides new pseudopolymorphic forms of darunavir as well as a novel amorphous form of darunavir, pharmaceutical compositions comprising these compounds, methods for their preparation and use thereof in treating retroviral infections, in particular, HIV infection.
Abstract: An amorphous form of dolutegravir sodium, pharmaceutical compositions comprising same, methods for its preparation and use thereof as an antiretroviral agent.
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 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:
August 28, 2014
Date of Patent:
August 11, 2015
Assignee:
MAPI PHARMA LTD.
Inventors:
Ehud Marom, Michael Mizhiritskii, Shai Rubnov
Abstract: The present invention provides novel crystalline forms of perampanel, pharmaceutical compositions comprising same, methods for their preparation and uses thereof for treating seizures and epilepsy.
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 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:
Grant
Filed:
June 13, 2012
Date of Patent:
March 17, 2015
Assignee:
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:
Grant
Filed:
February 10, 2014
Date of Patent:
March 10, 2015
Assignee:
Mapi Pharma Ltd.
Inventors:
Ehud Marom, Shai Rubnov, Michael Mizhiritskii
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:
August 28, 2014
Publication date:
February 19, 2015
Applicant:
MAPI PHARMA LTD.
Inventors:
Ehud MAROM, Michael MIZHIRITSKII, Shai RUBNOV
Abstract: The present invention provides new pseudopolymorphic forms of darunavir as well as a novel amorphous form of darunavir, pharmaceutical compositions comprising these compounds, methods for their preparation and use thereof in treating retroviral infections, in particular, HIV infection.
Abstract: The present invention provides novel crystalline forms of perampanel, pharmaceutical compositions comprising same, methods for their preparation and uses thereof for treating seizures and epilepsy.
Abstract: The present invention provides an amorphous form of dolutegravir sodium, pharmaceutical compositions comprising same, methods for its preparation and use thereof as an antiretroviral agent.