Patents Assigned to Astellas Pharma Inc.
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Publication number: 20190307906Abstract: The problem to be solved is to provide an anti-human MUC1 antibody Fab fragment that is expected to be useful in the diagnosis and/or treatment of a cancer, particularly, the diagnosis and/or treatment of breast cancer or bladder cancer, and a diagnosis approach and/or a treatment approach using a conjugate comprising the Fab fragment. The solution is an anti-human MUC1 antibody Fab fragment comprising a heavy chain fragment comprising a heavy chain variable region consisting of the amino acid sequence represented by SEQ ID NO: 8 or 10, and a light chain comprising a light chain variable region consisting of the amino acid sequence represented by SEQ ID NO: 12, and a conjugate comprising the Fab fragment.Type: ApplicationFiled: November 17, 2017Publication date: October 10, 2019Applicant: Astellas Pharma Inc.Inventors: Akifumi MORINAKA, Hiroki SHIRAI, Kazunori HIRAYAMA, Naomi HOSOGAI, Hitoshi DOIHARA
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Publication number: 20190309063Abstract: Described herein are novel anti-human Ig? antibodies, as well as methods for making the antibodies and using the antibodies to treat or prevent autoimmune disease.Type: ApplicationFiled: April 23, 2019Publication date: October 10, 2019Applicant: Astellas Pharma Inc.Inventors: Daisuke YAMAJUKU, Mutsumi SEKI, Takashi HONDA, Satoshi KUBO, Shinji SOGA, Akifumi MORINAKA
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Patent number: 10426784Abstract: Compounds of formula (I) defined herein are useful as a dopamine D1 receptor positive allosteric modulators (D1 PAM) and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating cognitive impairment, schizophrenia negative symptom, CIAS, Parkinson's disease, Alzheimer's disease, Huntington's disease, depression, ADHD, drug dependency, or the like.Type: GrantFiled: June 17, 2016Date of Patent: October 1, 2019Assignee: Astellas Pharma Inc.Inventors: Shimpei Kawakami, Tomoyoshi Imaizumi, Naoyuki Masuda, Shigeki Kunikawa, Masataka Morita, Junko Yarimizu
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Publication number: 20190292182Abstract: [Problem] Provided is a compound which is useful as an active ingredient of a pharmaceutical composition for treating lung cancer. [Means for Solution] The present inventors have studied a compound useful as an active ingredient of a pharmaceutical composition for treating lung cancer, and as a result, it was found that a quinazoline compound has an excellent G12C mutation KRAS inhibitory activity, and which can be used as a therapeutic agent for lung cancer, and thereby the present invention has been completed. The quinazoline compound of the present invention and a salt thereof may be used as the therapeutic agent for lung cancer.Type: ApplicationFiled: June 5, 2019Publication date: September 26, 2019Applicant: ASTELLAS PHARMA INC.Inventors: Kazuyuki Kuramoto, Michinori Akaiwa, Tomoaki Abe, Takanobu Araki, Susumu Yamaki, Shigeki Kunikawa, Tomoyoshi Imaizumi, Takahiro Nigawara, Keisuke Arakawa, Itsuro Shimada, Masashi Shimazaki, Yoshiki Satake, Kazushi Watanabe, Takanori Koike
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Patent number: 10421762Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production.Type: GrantFiled: July 20, 2018Date of Patent: September 24, 2019Assignees: Astellas Pharma Inc., KOTOBUKI PHARMACEUTICAL CO., LTD.Inventors: Kenichi Kawaguchi, Akihiro Ishihata, Yusuke Inagaki, Kazuyuki Tsuchiya, Tadaatsu Hanadate, Akira Kanai, Hiroyuki Kaizawa, Junichi Kazami, Hiroshi Morikawa, Masashi Hiramoto, Kentaro Enjo, Hajime Takamatsu
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Publication number: 20190282569Abstract: Provided is a pharmaceutical composition, which comprises 5-{[(3R)-1-acryloylpyrrolidin-3-yl]oxy}-6-ethyl-3-({4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-pyrazine-2-carboxamide or a pharmaceutically acceptable salt thereof, and is stabilized. The pharmaceutical composition comprises potassium chloride and/or sodium chloride, and inhibits the increase of related substances.Type: ApplicationFiled: October 25, 2017Publication date: September 19, 2019Applicant: ASTELLAS PHARMA INC.Inventors: Atsushi SAKURAI, Mitsuru YOSHIDA, Tetsuo TOMINAGA
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Publication number: 20190269804Abstract: The problem to be solved is to provide an anti-human MUC1 antibody Fab fragment that is expected to be useful in the diagnosis and/or treatment of a cancer, particularly, the diagnosis and/or treatment of breast cancer or bladder cancer, and a diagnosis approach and/or a treatment approach using a conjugate comprising the Fab fragment. The solution is an anti-human MUC1 antibody Fab fragment comprising a heavy chain fragment comprising a heavy chain variable region consisting of the amino acid sequence represented by SEQ ID NO: 8 or 10, and a light chain comprising a light chain variable region consisting of the amino acid sequence represented by SEQ ID NO: 12, and a conjugate comprising the Fab fragment.Type: ApplicationFiled: May 17, 2019Publication date: September 5, 2019Applicant: Astellas Pharma Inc.Inventors: Akifumi Morinaka, Hiroki Shirai, Kazunori Hirayama, Naomi Hosogai, Hitoshi Doihara
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Publication number: 20190248738Abstract: Phenyldifluoromethyl-substituted prolinamide compounds that have a cathepsin S inhibitory effect, and are usable as active ingredients of pharmaceutical compositions for preventing and/or treating autoimmune diseases including systemic lupus erythematosus (SLE) and lupus nephritis, allergies, or graft rejection of an organ, bone marrow or tissue.Type: ApplicationFiled: April 25, 2019Publication date: August 15, 2019Applicant: Astellas Pharma Inc.Inventors: Yutaka Nakajima, Sunao Imada, Eriko Yamamoto, Kazuyuki Tsuchiya, Yu Harayama, Shunichiro Matsumoto
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Publication number: 20190248904Abstract: [Problem] Provided is an anti-human BDCA-2 antibody for preventing or treating an autoimmune disease by binding to a human BDCA-2 to control the function of a plasmacytoid dendritic cell through human BDCA-2.Type: ApplicationFiled: April 15, 2019Publication date: August 15, 2019Applicant: Astellas Pharma Inc.Inventors: Shinsuke NAKAO, Masayuki ITO, Yoshiyuki TENDA
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Publication number: 20190217531Abstract: Provided is a fast-eluting three-dimensionally molded object, which is formed by fused deposition modeling type three-dimensional molding and quickly elutes an active component. The fast-eluting three-dimensionally molded object is formed by the fused deposition modeling type three-dimensional molding and includes an active component, a water-soluble thermoplastic polymer, a water-soluble sugar and/or a water-soluble sugar alcohol, and a plasticizer component. The fast-eluting three-dimensionally molded object has an elution rate of the active component of 80% or higher within 85 minutes by a dissolution test method in the Japanese Pharmacopoeia, Sixteenth Edition.Type: ApplicationFiled: April 5, 2017Publication date: July 18, 2019Applicant: ASTELLAS PHARMA INC.Inventors: SORATO IKEDA, Shota HATTORI, Masanori KOBAYASHI
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Publication number: 20190218620Abstract: The purpose is to reveal a polynucleotide that is a novel causal gene of pancreatic cancer and thereby provide a method for detecting the polynucleotide or a polypeptide encoded thereby to select a subject positive for the polynucleotide or polypeptide and a method expected to be useful for to identify patients suitable for therapies and a primer set therefor and a kit for detection. In the method, a polynucleotide comprising a fusion point of a part of a CLDN18 gene and an ARHGAP6 gene or a polynucleotide comprising a fusion point of a part of a CLDN18 gene and an ARHGAP26 gene, or a fusion protein encoded thereby is detected. The primer set comprises a sense primer designed for a part encoding CLDN18 and an antisense primer designed for a part encoding ARHGAP6 or a part encoding ARHGAP26.Type: ApplicationFiled: August 9, 2017Publication date: July 18, 2019Applicants: Astellas Pharma Inc., National Cancer CenterInventor: Hiroki SASAKI
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Publication number: 20190202815Abstract: [Problem] To provide a compound useful as an MC4 receptor agonist. [Means for Solution] The present inventors studied MC4 receptor agonists, and have found that a piperazine derivative has an MC4 receptor agonistic action, thereby completing the present invention. The piperazine derivative of the present invention has an MC4 receptor agonistic action, and can be used as an agent for preventing or treating bladder and/or urinary tract diseases, in particular, underactive bladder, hypotonic bladder, acontractile bladder, detrusor underactivity, neurogenic bladder, urethral relaxation failure, detrusor-external urethral sphincter dyssynergia, and voiding dysfunctions in benign prostatic hyperplasia.Type: ApplicationFiled: July 18, 2017Publication date: July 4, 2019Applicant: Astellas Pharma Inc.Inventors: Takashi SUGANE, Norio ASAI, Hiroyuki MORITOMO, Daisuke YAMASHITA, Naomi HOSOGAI
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Publication number: 20190194220Abstract: Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.Type: ApplicationFiled: March 4, 2019Publication date: June 27, 2019Applicants: Astellas Pharma Inc., Cytokinetics, IncorporatedInventors: Ippei Sato, Takashi Kamikubo, Masanori Miura, Yuji Matsushima, Hiroaki Tanaka, Yasuhiro Shiina, Susumu Yamaki, Tomoyuki Saito, Hiroshi Kiyohara, Munemichi Ohe, Kayoko Mihara, Bradley Paul Morgan, Fady Malik, Scott Emile Collibee, Luke Ashcraft, Pu-Ping Lu, Jeffrey Michael Warrington, Marc Garard
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Patent number: 10322997Abstract: Phenyldifluoromethyl-substituted prolinamide compounds that have a cathepsin S inhibitory effect, and are usable as active ingredients of pharmaceutical compositions for preventing and/or treating autoimmune diseases including systemic lupus erythematosus (SLE) and lupus nephritis, allergies, or graft rejection of an organ, bone marrow or tissue.Type: GrantFiled: November 5, 2018Date of Patent: June 18, 2019Assignee: ASTELLAS PHARMA INC.Inventors: Yutaka Nakajima, Sunao Imada, Eriko Yamamoto, Kazuyuki Tsuchiya, Yu Harayama, Shunichiro Matsumoto
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Patent number: 10314890Abstract: The present invention provides a combination therapy for effectively treating and/or preventing diseases associated with cells expressing CLDN18.2, including cancer diseases such as pancreatic cancer and metastases thereof.Type: GrantFiled: August 23, 2017Date of Patent: June 11, 2019Assignees: ASTELLAS PHARMA INC., TRON—TRANSLATIONALE ONKOLOGIE AN DER UNIVERSITATSMEDIZIN DER JOHANNES GUTENBERG-UNIVERSITAT MAINZ GEMEINNUTZIGE GMBHInventors: Ugur Sahin, Ozlem Tureci, Rita Mitnacht-Kraus, Stefan Woll, Stefan Jacobs, Cornelia Heinz
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Patent number: 10316086Abstract: [Problem] Provided is an anti-human Ig? antibody which crosslinks BCR and Fc?RIIb and has an immunosuppressive function more enhanced than that of an antibody in the prior art. [Means for Solution] An anti-human Ig? antibody comprising a heavy chain variable region comprising CDR1 consisting of the amino acid sequence of amino acid numbers 31 to 35 of SEQ ID NO: 2, CDR2 consisting of the amino acid sequence of amino acid numbers 50 to 65 of SEQ ID NO: 2, and CDR3 consisting of the amino acid sequence of amino acid numbers 98 to 108 of SEQ ID NO: 2, a light chain variable region comprising CDR1 consisting of the amino acid sequence of amino acid numbers 24 to 38 of SEQ ID NO: 4, CDR2 consisting of the amino acid sequence of amino acid numbers 54 to 60 of SEQ ID NO: 4, and CDR3 consisting of the amino acid sequence of amino acid numbers 93 to 101 of SEQ ID NO: 4, and a heavy chain constant region which is a human Ig?1 constant region having amino acid mutations of S239D, H268D, and L328W.Type: GrantFiled: August 5, 2015Date of Patent: June 11, 2019Assignee: ASTELLAS PHARMA INC.Inventors: Daisuke Yamajuku, Mutsumi Seki, Takashi Honda, Satoshi Kubo, Shinji Soga, Akifumi Morinaka
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Patent number: 10301286Abstract: To provide a compound which can be used as an MC4 receptor agonist. The present inventors have investigated MC4 receptor agonists, and have found that a piperazine derivative has an action related to the agonists, thereby completing the present invention. That is, the piperazine derivative of the present invention has an MC4 receptor agonistic action, and can be used as an agent for preventing or treating bladder and/or urinary tract diseases, in particular, underactive bladder, hypotonic bladder, acontractile bladder, detrusor underactivity, neurogenic bladder, urethral relaxation failure, detrusor-external urethral sphincter dyssynergia, and voiding dysfunctions in benign prostatic hyperplasia.Type: GrantFiled: August 2, 2016Date of Patent: May 28, 2019Assignee: Astellas Pharma Inc.Inventors: Takashi Sugane, Takuya Makino, Daisuke Yamashita, Yasuhiro Yonetoku, Daisuke Tanabe, Hisashi Mihara, Norio Asai, Kazuhiko Osoda, Takafumi Shimizu, Hiroyuki Moritomo, Keizo Sugasawa, Kyoichi Maeno, Naomi Hosogai
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Patent number: 10294301Abstract: [Problem] Provided is an anti-human BDCA-2 antibody for preventing or treating an autoimmune disease by binding to a human BDCA-2 to control the function of a plasmacytoid dendritic cell through human BDCA-2.Type: GrantFiled: December 22, 2014Date of Patent: May 21, 2019Assignee: ASTELLAS PHARMA INC.Inventors: Shinsuke Nakao, Masayuki Ito, Yoshiyuki Tenda
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Publication number: 20190117649Abstract: Provided are methods, uses, and compositions for treating acute myeloid leukemia which includes therapeutically effective combinations of 6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide, or a salt thereof, and 4-amino-1-?-D-ribofuranosyl-1,3,5-triazin-2(1H)-one, or a salt thereof.Type: ApplicationFiled: March 27, 2017Publication date: April 25, 2019Applicant: ASTELLAS PHARMA INC.Inventors: Erkut BAHCECI, Yoko YAMAKI
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Publication number: 20190111129Abstract: Provided is a stable pharmaceutical composition comprising an anti-human TSLP receptor antibody, capable of inhibiting the generation of chemically modified substances, such as deamidated forms and oxidized forms, or degradants, or multimers. The pharmaceutical composition comprises an anti-human TSLP receptor antibody, a pharmaceutically acceptable buffer, arginine or a pharmaceutically acceptable salt thereof, and a surfactant.Type: ApplicationFiled: December 16, 2016Publication date: April 18, 2019Applicant: ASTELLAS PHARMA INC.Inventors: Megumi IKEDA, Akinori CHIKUSHI