Abstract: This invention is directed to reduction of flake-like aggregation in nanoparticulate compositions. Also encompassed by the invention are compositions comprising a nanoparticulate active agent, at least one surface stabilizer and a flake-like aggregation reducing agent, such as a buffer and a sugar. The nanoparticulate active agent compositions comprise particles of the active agent having an effective average particle size of less than about 2000 nm.
Type:
Grant
Filed:
May 4, 2018
Date of Patent:
February 22, 2022
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Niels P. Ryde, Peter Snyder, Wei Liu, David M. Slifer
Abstract: The invention provides compositions, methods and treatment regimens for treating cancer comprising periodic subcutaneous administration of the fusion protein of SEQ ID NO:1 to a cancer patient resulting in enhanced activation of CD8+ T-cells with minimal effects on regulatory T cell (Treg) expansion and providing enhanced anti-tumor efficacy while also mitigating T cell inactivation/exhaustion.
Type:
Grant
Filed:
June 10, 2020
Date of Patent:
February 15, 2022
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Heather C. Losey, Jared Lopes, Lei Sun, Raymond J. Winquist
Abstract: The invention provides compositions and methods of treating cancer in a patient with a combination therapy comprising a fusion protein of SEQ ID NO: 1 in combination with an immune checkpoint inhibitor. Preferably the patient has failed to achieve complete or partial response with prior or ongoing treatment with an immune checkpoint inhibitor.
Type:
Grant
Filed:
October 16, 2020
Date of Patent:
February 15, 2022
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Heather C. Losey, Jared Lopes, Raymond J. Winquist
Abstract: The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.
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:
August 7, 2020
Date of Patent:
January 25, 2022
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
Abstract: Provided herein are compounds and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of conditions associated with inhibition of HDAC (e.g., HDAC2).
Type:
Grant
Filed:
August 7, 2018
Date of Patent:
January 18, 2022
Assignee:
Alkermes, Inc.
Inventors:
Nathan Oliver Fuller, John A. Lowe, III
Abstract: Provided herein are compounds and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of conditions associated with inhibition of HDAC (e.g., HDAC2).
Type:
Grant
Filed:
August 31, 2020
Date of Patent:
January 18, 2022
Assignee:
Alkermes, Inc.
Inventors:
Nathan Oliver Fuller, John A. Lowe, III
Abstract: The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.
Abstract: The present invention provides compounds useful for the treatment of opioid dependence, alcohol dependence, alcohol use disorder, or the prevention of relapse to opioid dependence in a subject in need thereof. Related pharmaceutical compositions and methods are also provided herein.
Type:
Grant
Filed:
November 5, 2019
Date of Patent:
April 13, 2021
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Brian M. Aquila, Hoan Huynh, Lewis D. Pennington, Ingo Mugge, Baudouin Gerard, Markus Haeberlein, Roman A. Valiulin, Julius F. Remenar, Demetri Theodore Moustakas, Thomas Andrew Wynn, Todd Bosanac
Abstract: This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula I, II or any of Compounds 100-128 or any of those in Tables 2 or 3) accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or impairment.
Type:
Grant
Filed:
December 26, 2019
Date of Patent:
February 16, 2021
Assignee:
Alkermes, Inc.
Inventors:
Martin R. Jefson, John A. Lowe, III, Fabian Dey, Andreas Bergmann, Andreas Schoop, Nathan Oliver Fuller
Abstract: The present invention provides novel, single chain Fc fusion proteins having improved properties. The invention provides single chain fusions of soluble proteins fused to the Fc region of an immunoglobulin via a novel linker comprising a constant region of an immunoglobulin light chain linked to a CH1 constant region of an immunoglobulin heavy chain. This novel linker confers favorable properties on the Fc fusion proteins of the invention such as improved bioactivity and increased half-life as compared to non-Fc fusion counterparts or as compared to prior art Fc fusion proteins. The novel Fc fusion protein scaffold as described herein may be designed to include soluble proteins of interest capable of binding or interacting with any target of interest. Preferably, the Fc fusion protein of the invention is a dimer. The dimer preferably forms via a disulfide bond between free cysteine residues in the hinge region of two monomeric Fc fusion proteins of the invention.
Type:
Grant
Filed:
April 10, 2018
Date of Patent:
January 5, 2021
Assignee:
Alkermes, Inc.
Inventors:
Juan Alvarez, Demetri T. Moustakas, Heather R. Brodkin, Leslie A. McSweeney
Abstract: The present invention provides compounds useful for the treatment of opioid dependence, alcohol dependence, alcohol use disorder, or the prevention of relapse to opioid dependence in a subject in need thereof. Related pharmaceutical compositions and methods are also provided herein.
Type:
Grant
Filed:
July 11, 2019
Date of Patent:
October 20, 2020
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Brian M. Aquila, Hoan Huynh, Lewis D. Pennington, Ingo Mugge, Baudouin Gerard, Markus Haeberlein, Roman A. Valiulin, Julius F. Remenar, Demetri T. Moustakas, Thomas Andrew Wynn, Todd Bosanac
Abstract: The invention relates to a composition comprising buprenorphine and a ? opioid receptor antagonist, wherein the composition is characterized by an Agonist Antagonist Activity Index (AAnAI) of between about 0.7 and about 2.2; wherein; AAnAI = [ C max ? ( BUP ) / EC 50 ] [ C max ? ( ANTAGONIST ) / IC 50 ] .
Abstract: The present invention provides compounds useful for the treatment of opioid dependence, alcohol dependence, alcohol use disorder, or the prevention of relapse to opioid dependence in a subject in need thereof. Related pharmaceutical compositions and methods are also provided herein.
Type:
Grant
Filed:
July 11, 2019
Date of Patent:
October 13, 2020
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Brian M. Aquila, Hoan Huynh, Lewis D. Pennington, Ingo Mugge, Baudouin Gerard, Markus Haeberlein, Roman A. Valiulin, Julius F. Remenar, Demetri T. Moustakas, Thomas Andrew Wynn, Todd Bosanac
Abstract: The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.