Patents Assigned to Astellas Pharma Inc.
  • Patent number: 7985764
    Abstract: It was found that a compound according to the following formula: or a pharmaceutically acceptable salt thereof, has a strong antagonism for both the 5-HT2B and 5-HT7 receptors. In addition, the compound shows good pharmacological action as compared to antagonists selective for only one of these receptors. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).
    Type: Grant
    Filed: February 7, 2007
    Date of Patent: July 26, 2011
    Assignee: Astellas Pharma Inc.
    Inventors: Hidetaka Kaku, Hiroyoshi Yamada, Daisuke Kaga, Ryushi Seo, Shinobu Akuzawa
  • Patent number: 7982049
    Abstract: To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with ?-form crystal and ?-form crystal of (R)-2-(2-aminothiazol-4-yl)-4?-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide. The ?-form crystal does not exhibit hygroscopicity and has stability such that it can be used as a medicine, and is useful for mass synthesis in the industrial production. The ?-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the ?-form crystal.
    Type: Grant
    Filed: January 14, 2008
    Date of Patent: July 19, 2011
    Assignee: Astellas Pharma Inc.
    Inventors: Souichirou Kawazoe, Kenichirou Sakamoto, Yuji Awamura, Tatsuya Maruyama, Takayuki Suzuki, Kenichi Onda, Toshiyuki Takasu
  • Patent number: 7977466
    Abstract: The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
    Type: Grant
    Filed: July 15, 2008
    Date of Patent: July 12, 2011
    Assignees: Astellas Pharma Inc., Kotobuki Pharmaceutical Co., Ltd.
    Inventors: Masakazu Imamura, Takeshi Murakami, Ryota Shiraki, Kazuhiro Ikegai, Takashi Sugane, Fumiyoshi Iwasaki, Eiji Kurosaki, Hiroshi Tomiyama, Atsushi Noda, Kayoko Kitta, Yoshinori Kobayashi
  • Publication number: 20110166161
    Abstract: This invention relates to novel heterocyclic carboxamide derivatives and salts thereof. More particularly, it relates to novel heterocyclic carboxamide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
    Type: Application
    Filed: September 17, 2009
    Publication date: July 7, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Takeshi Terasawa, Shinji Shigenaga, Shinji Itoh, Jun Maeda, Hideyuki Watanabe, Satoshi Kubo, Noe Iahii
  • Publication number: 20110166348
    Abstract: Provided are an acid addition salt of (+)-2-[(inden-7-yloxy)methyl]morpholine (compound A) and a novel crystal thereof, which are for use as a medicament or a drug substance, and which has high storage stability, particularly high stability against humidity and light. An acid addition salt of the compound A with an acid selected from benzenesulfonic acid and hydrobromic acid is a compound which is isolated in the form of a crystal, is a solid at room temperature, exhibits no hygroscopicity at such a level that causes a problem for use as a medicament or a drug substance, has stability against humidity and light, and is therefore extremely useful as a medicament or a drug substance.
    Type: Application
    Filed: September 10, 2009
    Publication date: July 7, 2011
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Kazumi Kikuchi, Akio Kuroda, Ryo Mizoguchi, Kenichirou Sakamoto, Kazuhiro Takeguchi
  • Patent number: 7973078
    Abstract: A compound that can be used as an agent for treating a disease associated with an EP1 receptor, in particular a lower urinary tract symptom. It was confirmed that a sulfonamide compound having an amide structure and characterized by a chemical structure in which a carbon atom in the amide bonds to the N atom in sulfonamide through lower alkylene, or a salt thereof, has a potent EP1 receptor antagonistic activity, accomplishing the present invention. Since the sulfonamide compound of the present invention or a pharmaceutically acceptable salt thereof has a potent EP1 receptor antagonistic activity, it is useful as an agent for treating a disease associated with an EP1 receptor, in particular, a lower urinary tract symptom.
    Type: Grant
    Filed: August 9, 2007
    Date of Patent: July 5, 2011
    Assignee: Astellas Pharma Inc.
    Inventors: Hideki Kubota, Susumu Toda, Issei Tsukamoto, Yuta Fukuda, Ryutaro Wakayama, Kazuki Ono, Toru Watanabe, Hidenori Azami
  • Publication number: 20110158930
    Abstract: A method for treatment of a patient suffering from irritable bowel syndrome with diarrhea or mixed irritable bowel syndrome, which comprises administering to the patient a therapeutically effective amount of ramosetron or a pharmaceutically acceptable salt thereof in combination with a therapeutically effective amount of polycarbophil or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 27, 2009
    Publication date: June 30, 2011
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Takuya Hirata, Toshiyuki Funatsu, Yoshihiro Keto, Shinobu Akuzawa
  • Publication number: 20110160295
    Abstract: An antitumor agent containing, in combination, at least one kind of antitumor agent selected from the group consisting of an antitumor agent that forms a cross-link with DNA and shows an antitumor effect, an antimetabolite antitumor agent and a taxane antitumor agent, and a histone deacetylase inhibitor. According to the present invention, an antitumor agent causing reduced side effects and having a superior antitumor activity can be provided.
    Type: Application
    Filed: March 11, 2011
    Publication date: June 30, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Yoshinori Naoe, Takeshi Inoue, Yasuhiko Kano
  • Patent number: 7968552
    Abstract: A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like, is provided. It was found that an oxadiazolidinedione compound which is characterized by the possession of a benzyl or the like substituent binding to the cyclic group via a linker at the 2-position of the oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof, has excellent GPR40 agonist action. In addition, since the oxadiazolidinedione compound of the present invention showed excellent insulin secretion promoting action and blood glucose level-lowering action, it is useful as an insulin secretion promoter or an agent for preventing/treating diabetes.
    Type: Grant
    Filed: April 23, 2007
    Date of Patent: June 28, 2011
    Assignee: Astellas Pharma Inc.
    Inventors: Kenji Negoro, Fumiyoshi Iwasaki, Kei Ohnuki, Toshio Kurosaki, Yasuhiro Yonetoku, Norio Asai, Shigeru Yoshida, Takatoshi Soga
  • Publication number: 20110152268
    Abstract: The present invention relates to a pharmaceutical composition for treating nociceptive pain, containing a morpholine derivative or a pharmaceutically acceptable salt thereof, as an active ingredient. The present invention is useful in providing an excellent pharmaceutical composition for treating nociceptive pain. In addition, the present invention is particularly useful in providing a pharmaceutical composition for treating pain accompanying a disease selected from the group consisting of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, spondylosis deformans, gouty arthritis, juvenile arthritis, scapulohumeral periarthritis, and cervical syndrome, lumbago, lumbago accompanying spondylosis deformans, menalgia, pain and tumentia after inflammation, operation or injury, pain after odontectomy, and cancer pain. In addition, the present invention is particularly useful for alleviating pain in a damaged cartilage region, and is particularly useful for osteoarthritis in which NSAIDs are not effective.
    Type: Application
    Filed: September 10, 2009
    Publication date: June 23, 2011
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Nobuaki Takeshita, Fusako Nishigaki, Toshiaki Aoki, Seiji Tamura, Kazumi Kikuchi, Akio Kuroda
  • Patent number: 7964710
    Abstract: The present inventors found that a fusion gene present in some cancer patients is an oncogene. The present invention relates to a polypeptide as a novel fusion protein, a polynucleotide encoding the polypeptide, a vector comprising the polynucleotide, a transformed cell comprising the vector, a method for detecting the fusion protein or polynucleotide, a method for screening a therapeutic agent for cancer, and a method for treating cancer that is shown to be positive for the fusion gene. Further, the present invention relates kit, primer set, and probe useful in the detection of cancer that is shown to be positive for the fusion gene.
    Type: Grant
    Filed: May 15, 2009
    Date of Patent: June 21, 2011
    Assignees: Astellas Pharma Inc., CureGene K. K.
    Inventors: Hiroyuki Mano, Sadao Kuromitsu, Nobuaki Shindo, Takatoshi Soga, Takashi Furutani
  • Publication number: 20110142933
    Abstract: A controlled release dosage form of tacrolimus, comprising a solid dispersion of tacrolimus, wherein a controlled release base, which is selected from the group consisting of a water-soluble macromolecule, a gum base, and a membrane forming agent and does not form the solid dispersion of tacrolimus, is further contained, is disclosed. The controlled release dosage form of tacrolimus has an excellent controlled release and shows a stable blood concentration.
    Type: Application
    Filed: January 19, 2011
    Publication date: June 16, 2011
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Hiroyuki KOJIMA, Hiromu KONDO, Keiichi YOSHIHARA, Yuko TAKETANI, Takuya ISHII
  • Publication number: 20110144153
    Abstract: [Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided. [Solving Means] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic activity, and confirmed that the amide compound of the present invention has an EP4 receptor antagonistic activity, thereby completing the present invention. The amide compound of the present invention has an EP4 receptor antagonistic activity, and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating various EP4-related diseases, for example, chronic renal failure and/or diabetic nephropathy, and the like.
    Type: Application
    Filed: May 12, 2009
    Publication date: June 16, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo, Susumu Watanuki, Michihito Kageyama
  • Patent number: 7960562
    Abstract: It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.
    Type: Grant
    Filed: March 30, 2006
    Date of Patent: June 14, 2011
    Assignee: Astellas Pharma Inc.
    Inventors: Masaaki Hirano, Isao Kinoyama, Shunichiro Matsumoto, Eiji Kawaminami, Kei Ohnuki, Hirofumi Yamamoto, Kazuhiko Osoda, Tatsuhisa Takahashi, Takashi Shin, Takanori Koike, Itsuro Shimada, Hiroyuki Hisamichi, Toshiyuki Kusayama
  • Publication number: 20110128557
    Abstract: There is provided a tablet printing apparatus that can perform printing at a high speed on tablets arbitrarily supplied in volume at irregular intervals and has a high printing quality. A tablet printing apparatus 1 for multicolor printing on tablets T comprises a conveying belt 24 for conveying the tablets T in a moving direction A1-A2, an inkjet printer 42 disposed in the middle of the moving direction A1-A2 of the conveying belt 24 for performing non-contact printing onto surfaces of the tablets T conveyed by the conveying belt 24, an encoder 28 and a tablet sensor 29 for detecting moving positions of the tablets T conveyed by the conveying belt 24, and a unit control substrate 32 for controlling printing timing on the tablets T of the inject printer 42 or 46 based on the moving conditions or/and the moving positions of the tablets T detected by the encoder 28 and the tablet sensor 29.
    Type: Application
    Filed: August 22, 2008
    Publication date: June 2, 2011
    Applicants: ASTELLAS PHARMA INC., DAIICHI JITSUGYO CO., LTD., DAIICHI JITSUGYO VISWILL CO., LTD., MASTERMIND CO., LTD.
    Inventors: Noriyuki Kinoshita, Takao Mizumoto, Keizo Baba, Takashi Nishizato, Syuya Kawahama, Hideyuki Tomoda, Yoshihide Muramatsu, Shiro Hatano, Fumihiro Ogawa, Chizuo Ozawa
  • Patent number: 7951825
    Abstract: To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: May 31, 2011
    Assignee: Astellas Pharma Inc.
    Inventors: Hironori Harada, Kazuyuki Hattori, Kazuya Fujita, Masataka Morita, Sunao Imada, Yoshito Abe, Hiromichi Itani, Tatsuaki Morokata, Hideo Tsutsumi
  • Patent number: 7951780
    Abstract: An antitumor agent containing, in combination, at least one kind of antitumor agent selected from the group consisting of an antitumor agent that forms a cross-link with DNA and shows an antitumor effect, an antimetabolite antitumor agent and a taxane antitumor agent, and a histone deacetylase inhibitor. According to the present invention, an antitumor agent causing reduced side effects and having a superior antitumor activity can be provided.
    Type: Grant
    Filed: February 24, 2005
    Date of Patent: May 31, 2011
    Assignee: Astellas Pharma Inc.
    Inventors: Yoshinori Naoe, Takeshi Inoue, Yasuhiko Kano
  • Patent number: 7947690
    Abstract: The present invention provides a condensed pyrimidine compound represented by formula (I) or pharmaceutically acceptable salt thereof: where A represents a ring where at least one carbon atom within said ring is optionally substituted with one or more groups selected from the group consisting of lower alkyl, —O-(lower alkyl), halogen atom, carboxyl, —CO2-(lower alkyl), and carbamoyl, R1 represents: (1) phenyl substituted with at least three halogen atoms, which may have at least one additional substituent, or (2) cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl, each of which is optionally substituted; and R2 represents a group represented by formula (II) or an optionally substituted cyclic amino: wherein R21 and R22 may be identical or different and each represents —H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, phenyl, heteroaryl, non-aromatic heterocyclyl, or —O-(lower alkyl), each of which is optionally substituted.
    Type: Grant
    Filed: October 17, 2005
    Date of Patent: May 24, 2011
    Assignee: Astellas Pharma Inc.
    Inventors: Yasuhiro Yonetoku, Kenji Negoro, Kenichi Onda, Masahiko Hayakawa, Daisuke Sasuga, Takahiro Nigawara, Kazuhiko Iikubo, Hiroyuki Moritomo, Shigeru Yoshida, Takahide Ohishi
  • Publication number: 20110105460
    Abstract: [Problem] A compound, which can be used for preventing or treating diseases, in which 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11?-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.
    Type: Application
    Filed: July 2, 2009
    Publication date: May 5, 2011
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Seiji Yoshimura, Noriyuki Kawano, Tomoaki Kawano, Daisuke Sasuga, Takanori Koike, Hideyuki Watanabe, Hiroki Fukudome, Nobuyuki Shiraishi, Ryosuke Munakata, Hiroaki Hoshii, Kayoko Mihara
  • Publication number: 20110105420
    Abstract: [Object] Disclosed is a compound useful as an active ingredient for a pharmaceutical composition having an ?-amylase inhibitory activity, particularly a pharmaceutical composition for the treatment of diabetes. [Solution] An investigation has been made on a compound having an ?-amylase inhibitory activity among the compounds produced by Streptomyces sp. strain 6982, which is a actinomycetes belonging to the genus Streptomyces, and it was confirmed that an aminosugar compound has an ?-amylase inhibitory activity, thus completing the invention. The aminosugar compound of the present invention has an ?-amylase-inhibitory activity, and therefore can be used as a prophylactic or therapeutic agent for diabetes, obesity, NASH (non-alcoholic steatohepatitis), particularly as an ameliorating agent for postprandial blood glucose elevation.
    Type: Application
    Filed: April 9, 2009
    Publication date: May 5, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Satoshi Sasamura, Hiromi Sasamura, Shinya Nishiwaki