Abstract: The present disclosure provides crystalline and amorphous forms of 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(2-propanyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(2-propenoyl)-1-piperazinyl)pyrido[2,3-d]pyrimidin-2(1H)-one, including several anhydrous, hydrate and solvate forms, and solid state forms thereof, pharmaceutical compositions, and methods of treating a disease mediated by KRAS G12C inhibition.
Type:
Application
Filed:
December 16, 2021
Publication date:
April 7, 2022
Applicant:
AMGEN INC.
Inventors:
Mary CHAVES, Patricia LOPEZ, Prashant AGARWAL, Albert AMEGADZIE, Stephanie AZALI, Roman SHIMANOVICH, Ron C. KELLY, Darren Leonard REID
Abstract: The invention provides a method for controlling contaminants in biopharmaceutical purification processes by using light scattering and UV absorbance to establish a determinant. The invention makes use of multi-angle light scattering (MALS) and UV as a continuous monitoring system to provide information about the elution peak fractions in real-time instead of conventional pooling methods that rely on a predetermined percent UV peak max value to initiate the pooling process; regardless of product quality.
Type:
Grant
Filed:
October 7, 2021
Date of Patent:
April 5, 2022
Assignee:
AMGEN INC.
Inventors:
Arthur C. Hewig, III, Duke H. Phan, Yinges Yigzaw, Robert Bailey
Abstract: The invention provides a method for culturing mammalian cells. The method provides greater control over cell growth to achieve high product titer cell cultures by changing the temperature of the cell culture and/or by starving the cells in their asparagine supply.
Type:
Grant
Filed:
June 29, 2012
Date of Patent:
April 5, 2022
Assignee:
AMGEN INC.
Inventors:
Brian D. Follstad, Rebecca E. McCoy, Arvia E. Morris
Abstract: Provided herein are KRAS G12C inhibitors, such as composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
Type:
Grant
Filed:
June 11, 2019
Date of Patent:
March 29, 2022
Assignee:
AMGEN INC.
Inventors:
John Gordon Allen, Brian Alan Lanman, Jian Chen, Anthony B. Reed, Victor J. Cee, Longbin Liu, Patricia Lopez, Ryan Paul Wurz, Thomas T. Nguyen, Shon Booker, Jennifer Rebecca Allen, Margaret Chu-Moyer, Albert Amegadzie, Ning Chen, Clifford Goodman, Jonathan D. Low, Vu Van Ma, Ana Elena Minatti, Nobuko Nishimura, Alexander J. Pickrell, Hui-Ling Wang, Youngsook Shin, Aaron C. Siegmund, Kevin C. Yang, Nuria A. Tamayo, Mary Walton, Qiufen Xue
Abstract: A drug delivery device includes a reservoir, a drug delivery member in fluid communication with the reservoir, and a plunger disposed in and moveable relative to the reservoir. A plunger rod has a mass MP and is movable from (i) a first position, where the distal end of the plunger rod is spaced apart from the plunger to (ii) a second position, where the distal end of the plunger rod contacts the plunger. A drive mechanism is coupled to the proximal end of the plunger rod and is configured to deliver a drive force FD to move the plunger rod from the first position to the second position. A ratio of the mass of the plunger rod to the drive force of the drive mechanism (MP/FD) is in a range of approximately a value greater than 0 kg/kgf to approximately 0.05 kg/kgf.
Abstract: Provided herein are methods of treating cancer with KRAS G12C inhibitors of Formula I and compositions of the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
Type:
Grant
Filed:
November 5, 2019
Date of Patent:
March 29, 2022
Assignee:
AMGEN INC.
Inventors:
Brian Alan Lanman, Victor J. Cee, Alexander J. Pickrell, Anthony B. Reed, Kevin C. Yang, David John Kopecky, Hui-Ling Wang, Patricia Lopez, Kate Ashton, Shon Booker, Christopher M. Tegley
Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stenoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
Type:
Grant
Filed:
August 27, 2018
Date of Patent:
March 22, 2022
Assignee:
AMGEN INC.
Inventors:
Sean P. Brown, Yunxiao Li, Paul E. Harrington, Brian Alan Lanman, Jonathan D. Low, Ana Elena Minatti, Vu Van Ma, Kexue Li
Abstract: The present invention relates to methods of upregulating the high mannose glycoform content of a recombinant protein during a mammalian cell culture by manipulating the mannose to total hexose ratio in the cell culture media formulation.
Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
Type:
Grant
Filed:
March 4, 2019
Date of Patent:
March 15, 2022
Assignee:
AMGEN INC.
Inventors:
Gwenaella Rescourio, Ana Gonzalez Buenrostro, Sean P. Brown, Mike Lizarzaburu, Julio Medina, Salman Yojiro Jabri, Daqing Sun, Scott Preston Simonovich, Xuelei Yan, Yihong Li, Yosup Rew
Abstract: An injector may include a container having a wall with an interior surface and a seal assembly with an interior surface, the interior surfaces of the wall and the seal assembly defining a closed sterile reservoir filled with a drug product. The injector may also include a fluid delivery system comprising a clean, unsheathed, rigid container needle having a point disposed only partially through the seal assembly in a storage state, and disposed through the interior surface of the seal assembly into the sterile reservoir in a delivery state. Further, the injection may include an actuator that is adapted to move the container needle from the storage state to the delivery state.
Type:
Grant
Filed:
June 17, 2021
Date of Patent:
March 15, 2022
Assignee:
AMGEN INC.
Inventors:
Francisca Tan-Malecki, Ronald Forster, Scott M. Nunn, Mark D. Holt, Son C. Tran, Sheldon Moberg
Abstract: The invention relates to a method of determining glycan moiety on a recombinant glycoprotein using condensation nucleation light scattering detection.
Abstract: Compounds of formula (I): (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.
Type:
Application
Filed:
December 20, 2019
Publication date:
March 10, 2022
Applicant:
AMGEN INC.
Inventors:
NURIA A TAMAYO, ABHISEK BANERJEE, JAMES ALEXANDER BROWN, MICHAEL J FROHN, JIAN JEFFREY CHEN, KEXUE LI, QINGYIAN LIU, JONATHAN DANTE LOW, VU MA, LIPING H PETTUS, MARY CATHERINE WALTON, ANA ELENA MINATTI, MATTHEW PAUL BOURBEAU, LEI JIA, THOMAS T NGUYEN, NOBUKO NISHIMURA, QIUFEN MAY XUE, JOHN GORDON ALLEN
Abstract: Disclosed is a process for preparing a pharmacologically active compound, in which at least one internal conjugation site of an Fc domain sequence is selected that is amenable to conjugation of an additional functional moiety by a defined conjugation chemistry through the side chain of an amino acid residue at the conjugation site. An appropriate amino acid residue for conjugation may be present in a native Fc domain at the conjugation site or may be added by insertion (i.e., between amino acids in the native Fc domain) or by replacement (i.e., removing amino acids and substituting different amino acids). In the latter case, the number of amino acids added need not correspond to the number of amino acids removed from the previously existing Fc domain. This technology may be used to produce useful compositions of matter and pharmaceutical compositions containing them.
Type:
Grant
Filed:
November 30, 2018
Date of Patent:
March 8, 2022
Assignee:
AMGEN INC.
Inventors:
Colin V. Gegg, Kenneth W. Walker, Leslie P. Miranda, Fei Xiong
Abstract: The present invention relates to binding proteins that bind to HER-3 and polynucleotides encoding the same. Expression vectors and host cells comprising the same for the production of the binding protein of the invention are also provided. In addition, the invention provides compositions and methods for diagnosing and treating diseases associated with HER-3 mediated signal transduction and/or its ligand heregulin.
Type:
Grant
Filed:
October 9, 2018
Date of Patent:
March 8, 2022
Assignees:
Daiichi Sankyo Europe GmbH, Amgen Inc.
Inventors:
Mike Rothe, Martin Treder, Eric Borges, Larry L. Green, Susanne Hartmann
Abstract: Disclosed herein is a wearable drug delivery device including a container filled at least partially with a drug including at least one of a PCSK9 (Proprotein Convertase Subtilisin/Kexin Type 9) specific antibody, a granulocyte colony-stimulating factor (G-CSF), a sclerostin antibody, or a calcitonin gene-related peptide (CGRP) antibody. The wearable drug delivery device may include a needle and an insertion mechanism configured to insert the needle into a patient. A fluid pathway connector may define a sterile fluid flowpath between the container and the insertion mechanism. Optionally, a cannula initially disposed about the needle may be included. The cannula may be retained in the patient at an injection site created by the needle after the needle is withdrawn from the patient. Methods of assembly and operation are also provided.
Type:
Grant
Filed:
February 13, 2017
Date of Patent:
March 8, 2022
Assignee:
AMGEN INC.
Inventors:
Scott R. Gibson, Sheldon B. Moberg, Basel Hasan Taha, Margaux Frances Boyaval, Mark A. Destefano, John C. Love, Ian B. Hanson, Paul F. Bente, IV, Matthew J. Clemente, Rajan Ramaswamy, Daniel S. Codd, Scott Beaver, Kevin L. Bokelman, Sean M. O'connor, Robert Decker, Gautam N. Shetty, Ryan M. Agard, Nicholas J. Ciccarelli, Daniel Davenport
Abstract: PiggyBac transposases engineered to increase stability in a cell. The engineered piggyBac transposases are useful for stably transforming cells, cell line development, genome modification, and improving titer of recombinant proteins, among other uses.
Type:
Application
Filed:
December 9, 2019
Publication date:
March 3, 2022
Applicant:
AMGEN INC.
Inventors:
Neeraj J. AGRAWAL, Kristine M. DARIS, Jennitte L. STEVENS, Huong Thi Ngoc LE, Noelia Blanco TALAVAN
Abstract: Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
Type:
Grant
Filed:
August 26, 2020
Date of Patent:
March 1, 2022
Assignee:
AMGEN INC.
Inventors:
George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
Abstract: The present invention relates to chemical compounds having a general formula (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.
Type:
Application
Filed:
December 20, 2019
Publication date:
February 24, 2022
Applicant:
AMGEN INC.
Inventors:
NURIA A TAMAYO, ABHISEK BANERJEE, JIAN JEFFREY CHEN, KEXUE LI, LIPING H. PETTUS, MATTHEW PAUL BOURBEAU, LEI JIA
Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.
Type:
Grant
Filed:
March 27, 2020
Date of Patent:
February 22, 2022
Assignees:
Amgen Inc., Cytokinetics, Inc.
Inventors:
Mikkel V. Debenedetto, Justin Malinowski, Joshua Payette, Antonio Romero, David St. Jean, Jr.