公开(公告)号：US20250145631A1

公开(公告)日：2025-05-08

申请号：US18684845

申请日：2023-07-20

Applicant: Astellas Pharma Inc.

Inventor： Tomohiro YOSHINARI ,  Hideyuki WATANABE ,  Hiroki ISHIOKA ,  Eiji KAWAMINAMI ,  Kenichi KAWAGUCHI ,  Fumie TAKAHASHI ,  Takashi KAMIKUBO ,  Tomoyoshi IMAIZUMI ,  Takahiro MORIKAWA ,  Hisao HAMAGUCHI ,  Kazuyuki KURAMOTO ,  Hiroshi INAMI ,  Takeyuki NAGASHIMA ,  Kohei INAMURA

IPC: C07D487/08 ,  C07D401/14

Abstract: [Problem] To provide a compound useful as an active ingredient of a pharmaceutical composition for treating pancreatic cancer.
[Means for resolution] The present inventors have studied about a compound that is useful as an active ingredient of a pharmaceutical composition for treating pancreatic cancer and have found that heterocyclic compounds represented by the formula (I) have an excellent degradation-inducing action on a G12D mutant KRAS protein and/or a G12D mutant KRAS inhibition activity and can be used as a therapeutic agent for pancreatic cancer, thus completing the present invention. The heterocyclic compound or a salt thereof of the present invention can be used as a therapeutic agent for pancreatic cancer.

公开(公告)号：US20250084062A1

公开(公告)日：2025-03-13

申请号：US18723117

申请日：2022-12-26

Applicant: ASTELLAS PHARMA INC.

Inventor： Ryuichi SEKIOKA ,  Eriko HONJO ,  Kei OHNUKI ,  Yohei KOGANEMARU ,  Takuya WASHIO ,  Ayaka MORIKAWA ,  Kenji NEGORO ,  Shota SATO ,  Sadanori MIYOSHI ,  Takao SUZUKI

IPC: C07D401/12 ,  A61K31/40 ,  A61K31/4375 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  A61P21/00 ,  C07D207/48 ,  C07D401/14 ,  C07D471/04 ,  C07D487/10

Abstract: The present inventors have studied and found that the substituted quinoline derivatives have acetylcholine receptor clustering-inducing action and can be useful as an active ingredient in the pharmaceutical compositions for preventing and/or treating neuromuscular diseases. The substituted quinoline derivative of the present invention may be used as an agent for preventing and/or treating neuromuscular diseases.

公开(公告)号：US20250064946A1

公开(公告)日：2025-02-27

申请号：US18723695

申请日：2022-12-23

Applicant: Astellas Pharma Inc.

Inventor： Takeyuki NAGASHIMA

IPC: A61K47/55 ,  A61P35/00

Abstract: The present invention has an object to provide a pharmaceutical composition for treating a cancer of colorectal cancer and/or lung cancer.
The present inventors have studied about a compound that is useful as an active ingredient of a pharmaceutical composition for treating a cancer, and have found that a quinazoline compound has an excellent degradation-inducing action on a G12D mutant KRAS protein and a G12D mutant KRAS inhibition activity and that a pharmaceutical composition containing the compound as an active ingredient can be used as a therapeutic agent for a cancer, completing the present invention. The pharmaceutical composition of the present invention which contains a quinazoline compound or a salt thereof as an active ingredient can be used as a therapeutic agent for a cancer of colorectal cancer and/or lung cancer.

公开(公告)号：US12227517B2

公开(公告)日：2025-02-18

申请号：US17427426

申请日：2020-12-24

Applicant: Astellas Pharma Inc. ,  Kotobuki Pharmaceutical Co., Ltd.

Inventor： Hideyuki Watanabe ,  Yohei Seki ,  Keiichiro Okuyama ,  Kazuo Kurosawa ,  Osamu Ikeda ,  Hiroshi Tomiyama ,  Yoshinori Iwai ,  Akihiko Nakamura ,  Kozo Miyasaka

IPC: C07D498/10 ,  A61P35/00 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04

Abstract: A compound useful as an active ingredient of a pharmaceutical composition for treatment of cancer related to activation of immune cells or cancer having resistance to anti-PD-1 antibody/anti-PD-L1 antibody therapy is provided.
The present inventors have conducted studies on a compound useful as an active ingredient of a pharmaceutical composition for treatment of cancer related to activation of immune cells or cancer having resistance to anti-PD-1 antibody/anti-PD-L1 antibody therapy, and found that a pyridazinyl-thiazolecarboxamide compound has DGK ξ (DGKzeta) inhibitory effect, leading to completion of the present invention. The pyridazinyl-thiazolecarboxamide compound of the present invention has DGK ξ inhibitory effect, and can be used as a therapeutic agent for treatment of cancer related to activation of immune cells or cancer having resistance to anti-PD-1 antibody/anti-PD-L1 antibody therapy.

公开(公告)号：US20250049721A1

公开(公告)日：2025-02-13

申请号：US18931464

申请日：2024-10-30

Applicant: Astellas Pharma Inc. ,  Medivation Prostate Therapeutics LLC

Inventor： Douglas Alan Lorenz ,  Sanjay Konagurthu ,  Randy J. Wald ,  Jason A. Everett ,  Sheila Matz ,  Yuuki Takaishi ,  Toshiro Sakai ,  Ryousuke Irie ,  Shinsuke Oba ,  Hiroyasu Toyota ,  Koji Nishimura ,  Atsushi Kanbayashi

IPC: A61K9/20 ,  A61K9/10 ,  A61K9/16 ,  A61K31/4164 ,  A61K31/4166 ,  A61K47/32 ,  A61K47/38 ,  C07D233/86

Abstract: This disclosure provides formulations of enzalutamide and their use for treating hyperproliferative disorders.

公开(公告)号：US20250009897A1

公开(公告)日：2025-01-09

申请号：US18764946

申请日：2024-07-05

Applicant: Astellas Pharma Inc.

Inventor： Jumpei Suemitsu ,  Megumi Ikeda ,  Moe Kohno

IPC: A61K47/68 ,  A61K47/10 ,  A61K47/26 ,  A61K51/04 ,  A61K51/10 ,  C07K16/30

Abstract: Provided is a stable pharmaceutical composition comprising a labeling moiety-anti-human antibody Fab fragment conjugate, and the like. In the pharmaceutical composition comprising a labeling moiety-anti-human antibody Fab fragment conjugate, citric acid, phosphoric acid, 2-[4-(2-hydroxyethyl)-1-piperazinyl]ethanesulfonic acid or trishydroxymethyl aminomethane is added as a buffering agent, sucrose or glycerin is added as a stabilizer, a nonionic surfactant is added, and the pH is adjusted to 6.5 to 7.5. This enables suppression of generation of multimers and insoluble subvisible particles during preservation of the labeling moiety-anti-human antibody Fab fragment conjugate.

公开(公告)号：US20240316115A1

公开(公告)日：2024-09-26

申请号：US18579093

申请日：2022-07-14

Applicant: Astellas Pharma Inc. ,  OSAKA UNIVERSITY

Inventor： Kenichiro SHIMATANI ,  Hiromu SATO ,  Masao SASAI ,  Yoshiki SAWA ,  Atsuhiro SAITO ,  Shigeru MIYAGAWA

IPC: A61K35/44 ,  C12N5/071

CPC classification number: A61K35/44 ,  C12N5/069 ,  C12N2500/32 ,  C12N2500/90 ,  C12N2501/115 ,  C12N2501/135 ,  C12N2506/02 ,  C12N2509/00 ,  C12N2513/00 ,  C12N2533/52 ,  C12N2533/54

Abstract: An object of the present invention is to provide a pericyte-like cell having high angiogenic potential with a higher cell proliferation ability than a primary pericyte available in the past and high VEGF expression, and a method for producing the same. Provided are a method for producing a VEGF-highly expressing pericyte-like cell, the method including selecting a CD56(−) pericyte-like cell from a population including a pericyte-like cell obtained by inducing differentiation of a pluripotent stem cell; and a VEGF-highly expressing pericyte-like cell produced by the production method.

公开(公告)号：US20240309108A1

公开(公告)日：2024-09-19

申请号：US18625004

申请日：2024-04-02

Applicant: Astellas Pharma Inc. ,  TRON-Translationale Onkologie an der Universitätsmedizin der Johannes Gutenberg-Universität Mainz

Inventor： Ugur Sahin ,  Ozlem Tureci ,  Rita Mitnacht-Kraus ,  Stefan Woll

IPC: C07K16/30 ,  C07K16/28 ,  G01N33/574

CPC classification number: C07K16/30 ,  C07K16/28 ,  C07K16/3023 ,  C07K16/303 ,  C07K16/3046 ,  G01N33/57492 ,  C07K2317/34 ,  G01N2800/52

Abstract: The invention relates to antibodies directed against an epitope located within the C-terminal portion of CLDN18.2 which are useful, for example, in diagnosing cancer and/or in determining whether cancer cells express CLDN18.2.

公开(公告)号：US12036315B2

公开(公告)日：2024-07-16

申请号：US16609062

申请日：2018-04-27

Applicant: Astellas Pharma Inc.

Inventor： Yoshiaki Umemoto ,  Takatsune Yoshida ,  Sachie Namiki ,  Akira Takagi ,  Ryo Kojima ,  Toshiro Sakai ,  Shinsuke Oba ,  Hajime Aoki

IPC: A61K9/20 ,  A61K9/00 ,  A61K9/16 ,  A61K31/4166

CPC classification number: A61K9/0053 ,  A61K9/2009 ,  A61K9/2027 ,  A61K9/2054 ,  A61K31/4166

Abstract: Provided is a pharmaceutical composition for oral administration in which the solubility and/or dissolution properties of enzalutamide are improved and supersaturation is maintained. Also provided is a pharmaceutical composition for oral administration in which the oral absorbability of enzalutamide is improved. The pharmaceutical composition for oral administration comprises enzalutamide and polyvinyl alcohol.

公开(公告)号：US20240209108A1

公开(公告)日：2024-06-27

申请号：US18556606

申请日：2022-04-21

Applicant: Astellas Pharma Inc. ,  National Cancer Center

Inventor： Yoshiyuki TENDA ,  Masatoshi YURI ,  Shigenori YAGI ,  Yoshiki SATAKE ,  Kazunori HIRAYAMA ,  Hiroki SHIRAI ,  Hiroki SASAKI ,  Fumiko CHIWAKI ,  Masayuki KOMATSU

IPC: C07K16/28 ,  A61K39/00 ,  A61P35/00

CPC classification number: C07K16/2878 ,  A61P35/00 ,  C07K16/28 ,  A61K2039/505 ,  C07K2317/31 ,  C07K2317/622

Abstract: An object of the present invention is to provide an anti-CLDN4/anti-CD137 bispecific antibody usable in treatment of cancer.
An anti-CLDN4/anti-CD137 bispecific antibody produced using an anti-CLDN4 antibody binding to CLDN4 and an anti-CD137 antibody binding to CD137 had agonistic activity for CD137, promoted production of interferon γ by a T cell, and exhibited cytotoxic activity against a cancer cell expressing CLDN4 on a cell surface thereof. Besides, it was shown that the anti-CLDN4/anti-CD137 bispecific antibody can be safely administered to monkeys. Therefore, the anti-CLDN4/anti-CD137 bispecific antibody is usable in treatment of human cancer.