Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.
Type:
Grant
Filed:
February 4, 2014
Date of Patent:
August 11, 2015
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Laura Cook Blumberg, Julius F. Remenar, Orn Almarsson, Tarek A. Zeidan
Abstract: The present invention provides compounds of formula (I), wherein: R1 is unsubstituted C1-C6 alkyl; La is substituted or unsubstituted C1-C6 alkyl linker, substituted or unsubstituted C3-C10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R2 and R3 are each, independently, H, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C6-C10 aryl; or alternatively, R2 and R3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.
Type:
Grant
Filed:
February 14, 2014
Date of Patent:
July 28, 2015
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.
Type:
Grant
Filed:
September 24, 2013
Date of Patent:
July 7, 2015
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Laura Cook Blumberg, Julius F. Remenar, Orn Almarsson, Tarek A. Zeidan
Abstract: The present invention is directed to nanoparticulate compositions comprising megestrol. The megestrol particles of the composition have an effective average particle size of less than about 2000 nm.
Abstract: The present invention relates to compounds of Formula I or II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which relates to mophinan compounds useful as ?, ? and/or ? receptor opioid compounds and pharmaceuticals containing same that may be useful for mediating analgesia, combating drug addiction, alcohol addiction, drug overdose, mental illness, bladder dysfunctions, neurogenic bladder, interstitial cystitis, urinary incontinence, premature ejaculation, inflammatory pain, peripherally mediated and neuropathic pain, cough, lung edema, diarrhea, cardiac disorders, cardioprotection, depression, and cognitive, respiratory, diarrhea, irritable bowel syndrome and gastro-intestinal disorders, immunomodulation, and anti-tumor agents.
Type:
Grant
Filed:
December 4, 2012
Date of Patent:
May 26, 2015
Assignee:
Alkermes, Inc.
Inventors:
Derrick Arnelle, Daniel Deaver, Reginald L. Dean, III, Mark Todtenkopf
Abstract: Described are compositions of stable nanoparticulate cinacalcet or a salt thereof, and methods of making and using them. The compositions exhibit an improved dissolution rate, improved bioavailability, and reduced difference in absorption when administered orally under fed as compared to fasting conditions.
Type:
Grant
Filed:
May 18, 2011
Date of Patent:
April 21, 2015
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Deborah Neville, Scott Jenkins, David Manser
Abstract: The invention relates to a controlled release composition comprising a combination of isosorbide dinitrate and hydralazine, such as hydralazine hydrochloride, that in operation delivers the drug in a pulsed or multi-modal manner for the treatment of angina, ischaemic heart disease, arterial hypertension and related disease conditions. Preferably, the isosorbide dinitrate and hydralazine hydrochloride can be released from the dosage form in an erodable, diffusion and/or osmotic-controlled release profile.
Type:
Grant
Filed:
September 7, 2012
Date of Patent:
March 31, 2015
Assignee:
Alkermes Science One Limited
Inventors:
Gurvinder Singh Rekhi, Richard Sidwell, Sharon Hamm
Abstract: The present invention is directed to nanoparticulate compositions comprising megestrol. The megestrol particles of the composition have an effective average particle size of less than about 2000 nm.
Abstract: The present application relates methods for treating a depressive symptom comprising administering an effective amount of a ? opioid receptor agonist or a pharmaceutically acceptable salt thereof to a subject in need thereof. Non-limiting examples of such agonist include the compounds of Formulas I, II, III, and IV, as well as the compounds of Table A.
Type:
Application
Filed:
May 23, 2014
Publication date:
March 12, 2015
Applicant:
Alkermes Pharma Ireland Limited
Inventors:
Laura Cook Blumberg, Dan Deaver, David Eyerman, Thomas Wynn
Abstract: This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof. These novel forms of naltrexone impart advantages in pharmaceutical formulations incorporating them, including sustained release, or long acting, formulations.
Type:
Grant
Filed:
April 10, 2014
Date of Patent:
March 10, 2015
Assignee:
Alkermes, Inc.
Inventors:
Harry G. Brittain, David A. Dickason, Joyce M. Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
Abstract: The present invention is directed to nanoparticulate compositions comprising megestrol. The megestrol particles of the composition have an effective average particle size of less than about 2000 nm.
Abstract: The present invention is directed to nanoparticulate compositions comprising megestrol. The megestrol particles of the composition have an effective average particle size of less than about 2000 nm.
Abstract: This invention relates to compositions for the sustained release of biologically active polypeptides, and methods of forming and using said compositions, for the sustained release of biologically active polypeptides. The sustained release compositions of this invention comprise a biocompatible polymer having dispersed therein, a biologically active polypeptide and a sugar.
Type:
Grant
Filed:
November 22, 2013
Date of Patent:
November 4, 2014
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Steven G. Wright, Troy Christensen, Thean Yeoh, Michael E. Rickey, Joyce M. Hotz, Rajesh Kumar, Henry R. Costantino
Abstract: This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof. These novel forms of naltrexone impart advantages in pharmaceutical formulations incorporating them, including sustained release, or long acting, formulations.
Type:
Application
Filed:
April 10, 2014
Publication date:
October 9, 2014
Applicant:
Alkermes, Inc.
Inventors:
Harry G. Brittain, David A. Dickason, Joyce M. Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
Abstract: The present invention relates, in part, to the discovery that a pharmaceutical composition comprising aripiprazole and a carrier administered in a bolus injection resulted in an extended release profile similar to that obtained by the injection of a poly lactide-co-glycolide microsphere formulation containing the active agent. This surprising result suggests that pharmacologically beneficial extended release formulations without the complexities and expense associated with the manufacture microspheres.