Patents by Inventor Hidetomo Imase
Hidetomo Imase has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Publication number: 20220363671Abstract: Described herein are glue degrader compounds, their various targets, their preparation, pharmaceutical compositions comprising them, and their use in the treatment or prevention of conditions, diseases, and disorders mediated by various target proteins.Type: ApplicationFiled: September 16, 2020Publication date: November 17, 2022Inventors: Jake AXFORD, Rohan Eric John BECKWITH, Simone BONAZZI, Nicole BUSCHMANN, Artiom CERNIJENKO, Janetta DEWHURST, Aleem FAZAL, Matthew James HESSE, Lauren HOLDER, Viktor HORNAK, Hidetomo IMASE, Rama JAIN, Xianming JIN, John Ryan KERRIGAN, Julie LACHAL, Fupeng MA, Hasnain Ahmed MALIK, James R. MANNING, Daniel MCKAY, Robert Joseph MOREAU, Pierre NIMSGERN, Gary O'BRIEN, Anna VULPETTI, Ken YAMADA, Junping ZHAO
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Patent number: 11311400Abstract: The invention provides methods to prepare protein conjugates from proteins having at least two cysteines. In one embodiment, a protein with a disulfide linkage is reduced to provide two free cysteines for reaction with a 1,3-dihaloacetone or similar reactant, linking the sulfur atoms of the two cysteines together. The ketone inserted between the sulfur atoms is then used to form a Schiff base to an aminated payload molecule, thus conjugating the protein to a payload. In another embodiment, two cysteine residues are tied together by reaction with a 1,3-dihaloacetone or similar reactant. The linkage between the sulfur atoms in each case holds the protein or peptide in a constrained conformation, while also providing a convenient place for attaching a payload with good specificity and efficiency.Type: GrantFiled: April 16, 2020Date of Patent: April 26, 2022Assignee: Novartis AGInventors: Qi-Ying Hu, Hidetomo Imase
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Publication number: 20200253768Abstract: The invention provides methods to prepare protein conjugates from proteins having at least two cysteines. In one embodiment, a protein with a disulfide linkage is reduced to provide two free cysteines for reaction with a 1,3-dihaloacetone or similar reactant, linking the sulfur atoms of the two cysteines together. The ketone inserted between the sulfur atoms is then used to form a Schiff base to an aminated payload molecule, thus conjugating the protein to a payload. In another embodiment, two cysteine residues are tied together by reaction with a 1,3-dihaloacetone or similar reactant. The linkage between the sulfur atoms in each case holds the protein or peptide in a constrained conformation, while also providing a convenient place for attaching a payload with good specificity and efficiency.Type: ApplicationFiled: April 16, 2020Publication date: August 13, 2020Inventors: Qi-Ying HU, Hidetomo IMASE
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Patent number: 10667935Abstract: The invention provides methods to prepare protein conjugates from proteins having at least two cysteines. In one embodiment, a protein with a disulfide linkage is reduced to provide two free cysteines for reaction with a 1,3-dihaloacetone or similar reactant, linking the sulfur atoms of the two cysteines together. The ketone inserted between the sulfur atoms is then used to form a Schiff base to an aminated payload molecule, thus conjugating the protein to a payload. In another embodiment, two cysteine residues are tied together by reaction with a 1,3-dihaloacetone or similar reactant. The linkage between the sulfur atoms in each case holds the protein or peptide in a constrained conformation, while also providing a convenient place for attaching a payload with good specificity and efficiency.Type: GrantFiled: July 13, 2018Date of Patent: June 2, 2020Assignee: Novartis AGInventors: Qi-Ying Hu, Hidetomo Imase
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Publication number: 20190194315Abstract: This application discloses anti-P-cadherin antibodies, antigen binding fragments thereof, and antibody drug conjugates of said antibodies or antigen binding fragments, particularly antibody drug conjugates comprising anti-P-cadherin antibodies conjugated to auristatin analogs. The invention also relates to methods of treating cancer using the antibody drug conjugates. Also disclosed herein are methods of making the antibodies, antigen binding fragments, and antibody drug conjugates, and methods of using the antibodies and antigen binding fragments as diagnostic reagents.Type: ApplicationFiled: June 17, 2016Publication date: June 27, 2019Applicant: Novartis AGInventors: Tinya ABRAMS, Steven Bruce COHEN, Joseph Anthony D'Alessio, Jason Damiano, Clemens Durr, Bernhard Hubert GEIERSTANGER, Qi-Ying HU, Thomas HUBER, Hidetomo IMASE, Yunho JIN, Daniel MENEZES, Kathy MILLER, Morvarid MOHSENI, Weijia OU, Katherine RENDAHL, Tetsuo UNO, Yongqin WAN, Xing WANG
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Publication number: 20190038444Abstract: The invention provides methods to prepare protein conjugates from proteins having at least two cysteines. In one embodiment, a protein with a disulfide linkage is reduced to provide two free cysteines for reaction with a 1,3-dihaloacetone or similar reactant, linking the sulfur atoms of the two cysteines together. The ketone inserted between the sulfur atoms is then used to form a Schiff base to an aminated payload molecule, thus conjugating the protein to a payload. In another embodiment, two cysteine residues are tied together by reaction with a 1,3-dihaloacetone or similar reactant. The linkage between the sulfur atoms in each case holds the protein or peptide in a constrained conformation, while also providing a convenient place for attaching a payload with good specificity and efficiency.Type: ApplicationFiled: July 13, 2018Publication date: February 7, 2019Inventors: Qi-Ying HU, Hidetomo IMASE
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Patent number: 10172948Abstract: The invention provides improved methods to prepare protein conjugates from a ketone-modified protein. In one embodiment, the protein is prepared by linking two free cysteines by reaction with a 1,3-dihaloacetone or similar ketone-containing reactant, linking the sulfur atoms of the two cysteines together. The ketone inserted between the sulfur atoms is then used to form an oxime, thus conjugating the protein to a payload. In another embodiment, two cysteine residues are tied together by reaction with a 1,3-dihaloacetone or similar reactant, and the new ketone is used to form an oxime with a suitable payload molecule, thus conjugating the protein to a payload. The method provides improved reaction conditions for the oxime formation, whereby higher yields and improved product homogeneity are achieved.Type: GrantFiled: November 24, 2014Date of Patent: January 8, 2019Assignee: Novartis AGInventors: Qi-Ying Hu, Hidetomo Imase
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Patent number: 10022256Abstract: The invention provides methods to prepare protein conjugates from proteins having at least two cysteines. In one embodiment, a protein with a disulfide linkage is reduced to provide two free cysteines for reaction with a 1,3-dihaloacetone or similar reactant, linking the sulfur atoms of the two cysteines together. The ketone inserted between the sulfur atoms is then used to form a Schiff base to an aminated payload molecule, thus conjugating the protein to a payload. In another embodiment, two cysteine residues are tied together by reaction with a 1,3-dihaloacetone or similar reactant. The linkage between the sulfur atoms in each case holds the protein or peptide in a constrained conformation, while also providing a convenient place for attaching a payload with good specificity and efficiency.Type: GrantFiled: November 26, 2013Date of Patent: July 17, 2018Assignee: NOVARTIS AGInventors: Qi-Ying Hu, Hidetomo Imase
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Patent number: 9982017Abstract: The invention provides a synthetic polypeptide of Formula I?: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia.Type: GrantFiled: May 18, 2015Date of Patent: May 29, 2018Assignee: NOVARTIS AGInventors: Frederic Zecri, Andrei Golosov, Philipp Grosche, Hongjuan Zhao, Qi-Ying Hu, Hidetomo Imase
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Publication number: 20150252076Abstract: The invention provides a synthetic polypeptide of Formula I?: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia.Type: ApplicationFiled: May 18, 2015Publication date: September 10, 2015Applicant: NOVARTIS AGInventors: Frederic ZECRI, Andrei GOLOSOV, Philipp GROSCHE, Hongjuan ZHAO, Qi-Ying HU, Hidetomo IMASE
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Patent number: 9067971Abstract: The invention provides a synthetic polypeptide of Formula I?: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia.Type: GrantFiled: January 28, 2014Date of Patent: June 30, 2015Assignee: NOVARTIS AGInventors: Frederic Zecri, Andrei Golosov, Philippr Grosche, Hongjuan Zhao, Qi-Ying Hu, Hidetomo Imase
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Publication number: 20150150998Abstract: The invention provides improved methods to prepare protein conjugates from a ketone-modified protein. In one embodiment, the protein is prepared by linking two free cysteines by reaction with a 1,3-dihaloacetone or similar ketone-containing reactant, linking the sulfur atoms of the two cysteines together. The ketone inserted between the sulfur atoms is then used to form an oxime, thus conjugating the protein to a payload. In another embodiment, two cysteine residues are tied together by reaction with a 1,3-dihaloacetone or similar reactant, and the new ketone is used to form an oxime with a suitable payload molecule, thus conjugating the protein to a payload. The method provides improved reaction conditions for the oxime formation, whereby higher yields and improved product homogeneity are achieved.Type: ApplicationFiled: November 24, 2014Publication date: June 4, 2015Applicant: NOVARTIS AGInventors: Qi-Ying Hu, Hidetomo Imase
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Patent number: 8759365Abstract: The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.Type: GrantFiled: December 1, 2008Date of Patent: June 24, 2014Assignee: Novartis AGInventors: Muneto Mogi, Toshio Kawanami, Ken Yamada, Kayo Yasoshima, Hidetomo Imase, Takahiro Miyake, Osamu Ohmori
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Publication number: 20140142022Abstract: The invention provides a synthetic polypeptide of Formula I?: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia.Type: ApplicationFiled: January 28, 2014Publication date: May 22, 2014Inventors: Frederic ZECRI, Andrei GOLOSOV, Philipp GROSCHE, Kayo YASOSHIMA, Hongjuan ZHAO, Qi-Ying HU, Hidetomo IMASE, David Thomas PARKER
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Patent number: 8673848Abstract: The invention provides a synthetic polypeptide of Formula I?: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia.Type: GrantFiled: January 23, 2013Date of Patent: March 18, 2014Assignee: Novartis AGInventors: Frédéric Zecri, Andrei Golosov, Philipp Grosche, Kayo Yasoshima, Hongjuan Zhao, Qi-Ying Hu, Hidetomo Imase, David Thomas Parker
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Patent number: 8519134Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: November 16, 2010Date of Patent: August 27, 2013Assignee: Novartis AGInventors: Martin Allan, Sylvie Chamoin, Qi-Ying Hu, Hidetomo Imase, Julien Papillon
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Publication number: 20130196899Abstract: The invention provides a synthetic polypeptide of Formula I?: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia.Type: ApplicationFiled: January 23, 2013Publication date: August 1, 2013Applicant: NOVARTIS AGInventors: Frédéric ZECRI, Andrei GOLOSOV, Philipp GROSCHE, Kayo YASOSHIMA, Hongjuan ZHAO, Qi-Ying HU, Hidetomo IMASE, David Thomas PARKER
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Patent number: 8440682Abstract: The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R5, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.Type: GrantFiled: June 7, 2012Date of Patent: May 14, 2013Assignee: Novartis AGInventors: Muneto Mogi, Ken Yamada, Kayo Yasoshima, Toshio Kawanami, Ichiro Umemura, Yuki Iwaki, Hongbo Qin, Hidetomo Imase
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Patent number: 8420641Abstract: The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R5, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.Type: GrantFiled: April 18, 2012Date of Patent: April 16, 2013Assignee: Novartis AGInventors: Muneto Mogi, Ken Yamada, Kayo Yasoshima, Toshio Kawanami, Ichiro Umemura, Yuki Iwaki, Hongbo Qin, Hidetomo Imase
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Patent number: 8410275Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutical composition thereof, with all the variables being defined in the text. The present invention further relates to the use of the compounds herein for treatment of or delay progression to overt to diseases in which CETP is involved.Type: GrantFiled: May 17, 2012Date of Patent: April 2, 2013Assignee: Novartis AGInventors: Masashi Kishida, Naoko Matsuura, Hidetomo Imase, Yuki Iwaki, Ichiro Umemura, Osamu Ohmori, Eiji Kawahara