Patents Examined by Kaipeen Yang
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Patent number: 10040751Abstract: The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R1, R2, R3, R4, R5, R6, n1, m, p Z1, Z2, and Z3 are as described in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.Type: GrantFiled: October 1, 2015Date of Patent: August 7, 2018Assignee: Ocera Therapeutics, Inc.Inventors: Eric Marsault, Kamel Benakli, Hamid Hoveyda, Mark L. Peterson, Sylvie Beaubien, Luc Ouellet, Carl St-Louis, Sophie Beauchemin
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Patent number: 10028995Abstract: The present invention relates, inter alia, to a method comprising administering to a subject having high output shock and undergoing treatment with a catecholamine at a dose equivalent to at least about 0.2 mcg/kg/min of norepinephrine a dose of angiotensin II which is effective to raise the blood pressure of the subject to a mean arterial pressure (MAP) of about 65 mm or above, and which is effective to reduce the dose of the catecholamine required to maintain a MAP of about 65 mm to the equivalent of about 0.05-0.2 mcg/kg/min norepinephrine or less, or to the equivalent of about 0.05 mcg/kg/min norepinephrine or less.Type: GrantFiled: November 13, 2015Date of Patent: July 24, 2018Assignee: The George Washington University a Congressionally Chartered Not-for-Profit CorporationInventor: Lakhmir Chawla
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Patent number: 10017540Abstract: Cyclic peptides represented by (Formula 1) selectively bind the oncoprotein K-Ras G12D in vitro and in cellulo, where Z1 and Z2 are each L-propargylglycine (Pra), azidoornithine (OrnN3), or L-azidolysine (Az4), and V1-V2-V3-V4-V5 is an amino acid variable region having a sequence selected from the group consisting of SEQ ID NOs: 1-20.Type: GrantFiled: March 11, 2016Date of Patent: July 10, 2018Assignee: California Institute of TechnologyInventors: Ryan K. Henning, Ashwin N. Ram, Samir Das, Arundhati Nag, James R. Heath
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Patent number: 10000542Abstract: The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue and a second K residue, at positions corresponding to position 26, and 37, respectively, of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of eight amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1: HOOC—(CH2)x—CO—*, and Chem. 2: HOOC—C6H4—O—(CH2)y—CO—*, in which x is an integer in the range of 8-16, and y is an integer in the range of 6-13; and the linker comprises Chem. 3: *—NH—(CH2)q—CH[(CH2)w—NR1R2]—CO—*, which is connected at its CO—* end to the epsilon amino group of the first or the second K residue of the GLP-1 analogue, and wherein q is an integer in the range of 0-5, R1 and R2 independently represent *—H or *—CH3, and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof.Type: GrantFiled: May 2, 2013Date of Patent: June 19, 2018Assignee: Novo Nordisk A/SInventors: Jacob Kofoed, Patrick W. Garibay, Jesper Lau
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Patent number: 9988420Abstract: Disclosed herein are novel cytotoxic peptides of formula (I) as described herein: and the use of such peptides in making immunoconjugates (i.e Antibody Drug Conjugates) Also described herein are immunoconjugates (i.e Antibody Drug Conjugates) comprising such novel cytotoxic peptide linked to an antigen binding moiety, such as an antibody; where such immunoconjugates are useful for treating cell proliferative disorders. The invention further provides pharmaceutical compositions comprising these immunoconjugates, compositions comprising the immunoconjugates with a therapeutic co-agent, and methods to use these immunoconjugates and compositions for treating cell proliferation disorders.Type: GrantFiled: December 17, 2014Date of Patent: June 5, 2018Assignee: Novartis AGInventors: Bernhard Hubert Geierstanger, Jan Grunewald, Weijia Ou, Tetsuo Uno, Yongqin Wan, Xing Wang, Yunho Jin
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Patent number: 9914755Abstract: The present invention relates to cyclosporin analogs that are potent inhibitors of cyclophilin D and have low immunosuppressive activity; processes for preparing them; pharmaceutical compositions containing them; and methods for using these analogs and compositions containing them for the treatment of medical conditions, including but not limited to ischemic conditions, such as ischemia-reperfusion (I/R) injury, including myocardial FR injury, cerebral I/R injury, and ocular or retinal I/R injury.Type: GrantFiled: January 8, 2016Date of Patent: March 13, 2018Assignee: Allergan, Inc.Inventors: Simon N. Pettit, Andrew D. Jones, Catherine Simone V. Frydrych, Alex J. Thomas, Michael E. Garst
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Patent number: 9913875Abstract: The present application provides stable peptide-based Botulinum neurotoxin (BoNT) serotype A capture agents and methods of use as detection and diagnosis agents and in the treatment of diseases and disorders. The application further provides methods of manufacturing BoNT serotype A capture agents using iterative on-bead in situ click chemistry.Type: GrantFiled: March 16, 2016Date of Patent: March 13, 2018Assignees: California Institute of Technology, Indi Molecular, Inc.Inventors: Blake Farrow, James R. Heath, Heather Dawn Agnew
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Patent number: 9908922Abstract: The present invention relates to peptides, proteins, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer. The present invention furthermore relates to tumor-associated T-cell peptide epitopes, alone or in combination with other tumor-associated peptides that can for example serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses, or to stimulate T cells ex vivo and transfer into patients. Peptides bound to molecules of the major histocompatibility complex (MHC), or peptides as such, can also be targets of antibodies, soluble T-cell receptors, and other binding molecules.Type: GrantFiled: June 30, 2016Date of Patent: March 6, 2018Assignee: IMMATICS BIOTECHNOLOGIES GMBHInventors: Andrea Mahr, Toni Weinschenk, Helen Hoerzer, Oliver Schoor, Jens Fritsche, Harpreet Singh
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Patent number: 9907862Abstract: The present invention is directed to an inventive polymeric carrier molecule according to generic formula (I) and variations thereof, which allows for efficient transfection of nucleic acids into cells in vivo and in vitro, a polymeric carrier cargo complex formed by a nucleic acid and the inventive polymeric carrier molecule, but also to methods of preparation of this inventive polymeric carrier molecule and of the inventive polymeric carrier cargo complex. The present invention also provides methods of application and use of this inventive polymeric carrier molecule and the inventive polymeric carrier cargo complex as a medicament, for the treatment of various diseases, and in the preparation of a pharmaceutical composition for the treatment of such diseases.Type: GrantFiled: March 9, 2016Date of Patent: March 6, 2018Assignee: CureVac AGInventors: Patrick Baumhof, Thomas Schlake
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Patent number: 9902724Abstract: Conjugates of an immune response modifier, a linker, and an antigen are disclosed. The linker is represented by formula: wherein A is CH or N, p is in a range from 1 to 50, R? is a bond or -alkylene-O—, R? is alkylene that is optionally interrupted or terminated with one or more amide or ether groups, and E is an amine- or thiol-reactive group. Pharmaceutical compositions containing the compound or the conjugate, methods of making a conjugate, and methods of use of the compounds or conjugates as immunomodulators for inducing cytokine biosynthesis in an animal and for vaccinating an animal are also disclosed. An antigen modified by the linker is also disclosed.Type: GrantFiled: October 24, 2016Date of Patent: February 27, 2018Assignee: 3M Innovative Properties CompanyInventor: Paul D. Wightman
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Patent number: 9895412Abstract: The present invention relates to novel cycloundecadepsipeptide compounds and their analogues which bind and inhibit cyclophilins, have reduced immunosuppressive activity and improved physicochemical properties including water solubility. The present invention further relates to pharmaceutical compositions containing said depsipeptide compounds and their analogues for use in the treatment or prevention of diseases and pathologies which may be ameliorated by the inhibition of cyclophilin activity.Type: GrantFiled: June 20, 2016Date of Patent: February 20, 2018Assignee: Cypralis LimitedInventors: Hans Georg Fliri, Rhonan Lee Ford, Antonio Kuok Keong Vong
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Patent number: 9879050Abstract: In one aspect, the invention relates to substituted urea depsipeptide analogs, derivatives thereof, and related compounds, which are useful as activators the ClpP endopeptidease; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating infectious disease using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: August 30, 2014Date of Patent: January 30, 2018Assignee: St. Jude Children's Research HospitalInventors: Richard E. Lee, Ying Zhao, Elizabeth Griffith, Zhong Zheng, Aman P. Singh
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Patent number: 9877965Abstract: Described herein are compositions, methods, compounds, conjugates, and kits for use in targeted drug delivery using drug delivery conjugates containing hydrophilic spacer linkers for use in treating disease states caused by pathogenic cell populations, such as inflammatory cells.Type: GrantFiled: March 27, 2015Date of Patent: January 30, 2018Assignee: Endocyte, Inc.Inventors: Christopher Paul Leamon, Iontcho Radoslavov Vlahov, Yingjuan June Lu, Kevin Yu Wang, Fei Yu, Paul Joseph Kleindl, Hari Krishna R. Santhapuram
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Patent number: 9878047Abstract: This disclosure features compounds that are useful as pro-drugs of epoxy ketone protease inhibitors.Type: GrantFiled: March 9, 2016Date of Patent: January 30, 2018Assignee: Onyx Therapeutics, Inc.Inventors: Pasit Phiasivongsa, Gary W. Luehr, Ge Peng, Kolbot By, Shabbir T. Anik
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Patent number: 9873716Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.Type: GrantFiled: June 16, 2015Date of Patent: January 23, 2018Assignees: Gilead Sciences, Inc., Cypralis LimitedInventors: Caroline Aciro, David Kenneth Dean, Neil Andrew Dunbar, Adrian John Highton, Petr Jansa, Kapil Kumar Karki, Andrew J. Keats, Linos Lazarides, Richard L. Mackman, Simon N. Pettit, Karine G. Poullennec, Adam James Schrier, Dustin Siegel, Victoria Alexandra Steadman
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Patent number: 9873720Abstract: The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. Peptide complexes also are provided. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, treat a blood coagulation disorder in a subject, purify TFPI, and identify a TFPI-binding compound.Type: GrantFiled: December 29, 2014Date of Patent: January 23, 2018Assignees: Baxalta GmbH, Baxalta IncorporatedInventors: Michael Dockal, Rudolf Hartmann, Friedrich Scheiflinger, Frank Osterkamp, Thomas Polakowski, Ulrich Reineke
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Patent number: 9867805Abstract: The invention provides compounds, compositions, and methods for the treatment of diseases, disorders, or conditions that are modulated by matrix metalloproteinases (MMPs). The disease, disorder, or condition can include, for example, stroke, neurological disorders, or ophthalmological disorders. The treatment can include administering a compound or composition described herein, thereby providing a prodrug compound that metabolizes to an active MMP inhibitor in vivo. The MMP inhibition can be selective inhibition, for example, selective inhibition of MMP-2, MMP-9, and/or MMP-14. Thus, the invention provides non-mutagenic prodrug compounds of the formulas described herein that result in the inhibition of MMPs upon in vivo administration.Type: GrantFiled: April 26, 2016Date of Patent: January 16, 2018Assignee: University of Notre Dame du LacInventors: Mayland Chang, Shahriar Mobashery, Mijoon Lee
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Patent number: 9868743Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, are set forth, in addition to compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: February 4, 2014Date of Patent: January 16, 2018Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, Zhongxing Zhang, Eric Gillis, Paul Michael Scola
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Patent number: 9867862Abstract: The present invention provides compounds and methods for the treatment of an individual having or at risk of having a condition associated with alpha-1-antitrypsin by using a pharmacological chaperone. In particular, such methods are useful for the treatment and/or prevention of lung disorders associated with alpha-1-antitrypsin deficiency as well as liver disorders associated with an excess of alpha-1-antitrypsin. Suitable pharmacological chaperones include peptides and low-molecular weight compounds. The present invention also provides an assay for determining whether a test compound modulates alpha-1-antitrypsin activity.Type: GrantFiled: February 23, 2015Date of Patent: January 16, 2018Assignee: Amicus Therapeutics, Inc.Inventors: Eric Richard Sjoberg, Gary Lee
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Patent number: 9867868Abstract: The present invention relates to a composition for the treatment or prevention of a corneal injury, which comprises thymosin ?4, and citric acid or its salt as active ingredients. The composition may further comprise at least one organic acid selected from acetic acid, ascorbic acid or salts thereof. The composition can maintain or increase the activity of thymosin ?4 conventionally used to effectively treat wounds on the cornea, and thus, is useful as an ophthalmic formulation for treating the corneal injury.Type: GrantFiled: September 3, 2015Date of Patent: January 16, 2018Assignee: G-TREEBNT CO., LTD.Inventors: Sin Wook Kang, Kyoungsun Kim, Ji Hye Sung