Patents Assigned to Astellas Pharma Inc.
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Publication number: 20170190715Abstract: 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: ApplicationFiled: May 28, 2015Publication date: July 6, 2017Applicants: 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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Patent number: 9683051Abstract: Provided is an anti-human Tie2 antibody for preventing or treating diabetic macular edema, diabetic retinopathy, and critical limb ischemia by binding to a human Tie2 to activate the human Tie2. The present inventors have conducted investigations on an anti-human Tie2 antibody, and have thus provided an anti-human Tie2 antibody comprising four heavy chain variable regions and four light chain variable regions, in which the heavy chain variable region consists of the amino acid sequence of the amino acid numbers 1 to 122 of SEQ ID NO: 2, the light chain variable region consists of the amino acid sequence of the amino acid numbers 1 to 113 of SEQ ID NO: 4, the one heavy chain variable region and the one light chain variable region constitute one antigen-binding site, and the antibody comprises four antigen-binding sites.Type: GrantFiled: April 21, 2016Date of Patent: June 20, 2017Assignee: Astellas Pharma Inc.Inventors: Masazumi Kamohara, Shigenori Yagi, Yoshinori Ishii, Hiromi Nara
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Patent number: 9670219Abstract: [Problem] Provided is a compound having a positive allosteric modulating activity (PAM activity) on an ?7 nicotinic acetylcholine receptor (?7 nACh receptor). [Means for Solution] The present inventors have studied on a PAM activity on an ?7 nACh receptor, and they have found that a tetrahydrooxepinopyridine compound has a PAM activity on an ?7 nACh receptor, thereby completing the present invention. The tetrahydrooxepinopyridine compound of the present invention has a PAM activity on an ?7 nACh receptor and can be expected as an agent for preventing or treating dementia, cognitive impairment, schizophrenia, Alzheimer's disease, CIAS, negative symptoms of schizophrenia, inflammatory diseases, or pain.Type: GrantFiled: September 7, 2016Date of Patent: June 6, 2017Assignee: Astellas Pharma Inc.Inventors: Yohei Koganemaru, Satoshi Miyamoto, Shinya Nagashima, Akio Kamikawa, Koichi Yonezawa, Yuka Koizumi, Satoshi Aoki, Takashi Ogiyama, Shimpei Kawakami, Shigeki Kunikawa, Ryo Sato, Junichi Shishikura, Shuichirou Kakimoto, Hiroshi Yamada, Keisuke Tamaki
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Publication number: 20170152232Abstract: As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.Type: ApplicationFiled: September 27, 2016Publication date: June 1, 2017Applicants: Astellas Pharma Inc., Kotobuki Pharmaceutical Co., Ltd.Inventors: Minoru KAMEDA, Ikumi KURIWAKI, Kazuhiko IIKUBO, Hiroyuki HISAMICHI, Yuichiro KAWAMOTO, Hiroyuki MORITOMO, Tomoyuki SUZUKI, Takashi FUTAMI, Atsushi SUZUKI, Kazuhisa TSUNOYAMA, Makoto ASAUMI, Hiroshi TOMIYAMA, Atsushi NODA, Yoshinori IWAI, Kazuo TOKUZAKI, Haruki OKADA, Kozo MIYASAKA
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Publication number: 20170143678Abstract: Provided is a pharmaceutical composition for oral administration enabling improved solubility, improved dissolution properties, and improved oral absorbability of (2R)—N-({5-[3-(2,5-difluorophenyl)-2-(1,3-dihydro-2H-benzimidazole-2-ylidene)-3-oxopropanoyl]-2-fluorophenyl}sulfonyl)-2-hydroxypropane imide amide (hereinafter referred to as compound A) or a pharmaceutically acceptable salt thereof, as well as size reduction. The pharmaceutical composition for oral administration contains an amorphous form of compound A or its pharmaceutically acceptable salt, and a polymer.Type: ApplicationFiled: June 24, 2015Publication date: May 25, 2017Applicant: ASTELLAS PHARMA INC.Inventors: Hiroyuki KOJIMA, MASAKAZU MIYAZAKI, MARE NISHIURA, TAKASHI NISHIZATO
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Patent number: 9642852Abstract: A sulfur-containing bicyclic compound of the present invention has a PAM action of GABAB. A composition containing the sulfur-containing bicyclic compound. And, a method for preventing and/or treating schizophrenia, CIAS, cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, or Charcot-Marie-Tooth disease by administering the sulfur-containing bicyclic compound.Type: GrantFiled: April 17, 2015Date of Patent: May 9, 2017Assignee: Astellas Pharma Inc.Inventors: Nobuyuki Shiraishi, Hiroaki Hoshii, Wataru Hamaguchi, Eriko Honjo, Tomofumi Takuwa, Yuji Kondo, Takayuki Goto
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Patent number: 9629834Abstract: Provided is a pharmaceutical composition which enables the inhibition of formation and/or enlargement of cerebral aneurysm or the regression of cerebral aneurysm. The pharmaceutical composition for the inhibition of formation and/or enlargement of cerebral aneurysm or for the regression of cerebral aneurysm of the present invention, which includes a S1P1 receptor agonist as an active ingredient, enables the inhibition of formation and/or enlargement of cerebral aneurysm or the regression of cerebral aneurysm, and enables the prevention and/or treatment of a disease associated with cerebral aneurysm.Type: GrantFiled: April 22, 2014Date of Patent: April 25, 2017Assignees: KYOTO UNIVERSITY, ASTELLAS PHARMA INC.Inventors: Tomohiro Aoki, Ichiro Aramori, Jun Hirose, Rie Yamamoto
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Patent number: 9598434Abstract: Provided is a compound which is useful as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like. The present inventors have investigated compounds having a 5-HT2C receptor agonist activity and have found that the benzazepine compounds of the present invention have an excellent 5-HT2C receptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HT2C receptor agonist activity and can be used as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.Type: GrantFiled: July 13, 2015Date of Patent: March 21, 2017Assignee: ASTELLAS PHARMA INC.Inventors: Hiroyuki Koshio, Norio Asai, Taisuke Takahashi, Takafumi Shimizu, Yasuhito Nagai, Keiko Kawabata, Karl Bruce Thor
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Patent number: 9587015Abstract: Novel anti-human CTGF antibodies having excellent binding activity and/or neutralizing activity, as compared with conventional anti-human CTGF antibodies, are useful for treating various diseases in which human CTGF is involved in pathogenesis, including renal diseases such as chronic kidney disease and diabetic nephropathy.Type: GrantFiled: December 21, 2012Date of Patent: March 7, 2017Assignee: Astellas Pharma Inc.Inventors: Shoji Iwasaki, Ryuichi Moriya, Masayasu Yoshino, Koji Takakura
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Patent number: 9585889Abstract: On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. It was found that a nitrogen-containing bicyclic heterocyclic compound has an excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has an cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.Type: GrantFiled: February 8, 2016Date of Patent: March 7, 2017Assignee: Astellas Pharma Inc.Inventors: Yutaka Nakajima, Sunao Imada, Yuji Takasuna, Naohiro Aoyama, Takahiro Nigawara, Shohei Shirakami, Fumiyuki Shirai, Junji Sato, Keita Nakanishi, Kaori Kubo
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Publication number: 20170050973Abstract: [Problem] Provided is a compound having a positive allosteric modulating activity (PAM activity) on an ?7 nicotinic acetylcholine receptor (?7 nACh receptor). [Means for Solution] The present inventors have studied on a PAM activity on an ?7 nACh receptor, and they have found that a tetrahydrooxepinopyridine compound has a PAM activity on an ?7 nACh receptor, thereby completing the present invention. The tetrahydrooxepinopyridine compound of the present invention has a PAM activity on an ?7 nACh receptor and can be expected as an agent for preventing or treating dementia, cognitive impairment, schizophrenia, Alzheimer's disease, CIAS, negative symptoms of schizophrenia, inflammatory diseases, or pain.Type: ApplicationFiled: September 7, 2016Publication date: February 23, 2017Applicant: ASTELLAS PHARMA INC.Inventors: Yohei KOGANEMARU, Satoshi MIYAMOTO, Shinya NAGASHIMA, Akio KAMIKAWA, Koichi YONEZAWA, Yuka KOIZUMI, Satoshi AOKI, Takashi OGIYAMA, Shimpei KAWAKAMI, Shigeki KUNIKAWA, Ryo SATO, Junichi SHISHIKURA, Shuichirou KAKIMOTO, Hiroshi YAMADA, Keisuke TAMAKI
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Patent number: 9562044Abstract: Thiazole derivatives having pyrazine-2-carbonylamino substituted at the 2-position of the following formula (I): are excellent muscarinic M3 receptor positive allosteric modulators, and are useful for treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor. The 2-acylaminothiazole derivatives and salts thereof can be used for treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor, for example, voiding dysfunctions such as underactive bladder.Type: GrantFiled: February 27, 2014Date of Patent: February 7, 2017Assignee: Astellas Pharma Inc.Inventors: Taisuke Takahashi, Jun Maeda, Yusuke Inagaki, Kenji Negoro, Hiroaki Tanaka, Kazuhiro Yokoyama, Hajime Takamatsu, Takanori Koike, Issei Tsukamoto
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Patent number: 9556276Abstract: The invention provides an anti-human IL-23R antibody having excellent activity and/or cross-reactivity compared to conventional IL-23R antibodies and methods of using the same for treating or preventing various diseases in which human IL-23R is involved in the pathogenesis of the diseases.Type: GrantFiled: March 30, 2012Date of Patent: January 31, 2017Assignee: Astellas Pharma Inc.Inventors: Makoto Ohori, Takanori Sasaki, Hiromu Sato, Katsunari Taguchi
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Patent number: 9556160Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.Type: GrantFiled: March 27, 2015Date of Patent: January 31, 2017Assignee: Astellas Pharma Inc.Inventors: Kousei Yoshihara, Daisuke Suzuki, Susumu Yamaki, Hiroyoshi Yamada, Hisashi Mihara, Norio Seki
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Publication number: 20170014632Abstract: Methods of treating premature ejaculation include arranging one or more electrodes to face dorsal penile nerves (DPNs) of a patient with premature ejaculation, and applying an electro stimulation having a frequency and a current by which seminal fluid expulsion is not induced in the patient by the one or more electrodes during a time period from before the start of sexual intercourse to ejaculation. The electro stimulation reversibly extends an intravaginal ejaculatory latency time (IELT) of the patient. Methods of controlling a premature ejaculation treatment device are also provided.Type: ApplicationFiled: July 13, 2015Publication date: January 19, 2017Applicant: ASTELLAS PHARMA INC.Inventor: Yasuharu KIMURA
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Publication number: 20160375023Abstract: The present invention aims to elucidate a polynucleotide as a novel responsible gene for cancer and aims to thus provide a method for detecting the polynucleotide and a polypeptide encoded by the polynucleotide and a detection kit, a probe set, and a primer set for the detection. The present invention also aims to provide a pharmaceutical composition for treating cancer. The method detects a fusion gene composed of a portion of an FGFR3 gene and a portion of a TACC3 gene or a fusion protein encoded by the fusion gene. The primer set, the probe set, or the detection kit comprises a sense primer and a probe set designed from the portion encoding FGFR3 and an antisense primer and a probe set designed from the portion encoding TACC3. Since an inhibitor of the polypeptide exhibits antitumor effect, a pharmaceutical composition for treating cancer which is positive for either the fusion gene or the polypeptide is provided.Type: ApplicationFiled: September 14, 2016Publication date: December 29, 2016Applicant: Astellas Pharma Inc.Inventors: Atsushi Suzuki, Makoto Asaumi, Kazuhisa Tsunoyama, Kouichi Nishimura, Akifumi Norinaka, Tomohiro Yamauchi, Masayasu Yoshino, Hiroaki Yoshizaki
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Patent number: 9527818Abstract: Provided are a method for producing a sulfonyl amidine compound, which has an excellent gonadotropin releasing hormone receptor antagonism and is useful as a therapeutic agent for gonadotropin-dependent diseases (for example, prostate cancer, breast cancer, endometriosis, uterine fibroid, prostatic hyperplasia, or the like) or a salt thereof, and a synthesis intermediate useful in the production method. The production method of the present invention controls formation of a by-product which is hardly removed unless column purification is conducted and racemization of a target compound, thereby obtaining the target compound with a high purity, and therefore, the production method is suitable for industrial production.Type: GrantFiled: September 6, 2013Date of Patent: December 27, 2016Assignee: Astellas Pharma Inc.Inventors: Takashi Kikuchi, Shinya Yoshida, Atsushi Nakamura, Takahiro Akiba, Toshitaka Yoshino, Shuichi Nakagawa, Kiichi Sato
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Publication number: 20160369008Abstract: [Problem] To provide an anti-human PAI-1 antibody for preventing or treating pulmonary fibrosis by binding to active human PAI-1 and inhibiting effects mediated by the active human PAI-1. [Means for Solution] The present inventors have investigated anti-PAI-1 antibodies and consequently have provided an anti-human PAI-1 antibody comprising a heavy chain variable region consisting of the amino acid sequence of amino acid numbers 1 to 118 of SEQ ID NO: 2 and a light chain variable region consisting of the amino acid sequence of amino acid numbers 1 to 108 of SEQ ID NO: 4.Type: ApplicationFiled: February 20, 2015Publication date: December 22, 2016Applicant: Astellas Pharma Inc.Inventors: Hirotsugu TANAKA, Masayasu YOSHINO
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Publication number: 20160355602Abstract: [Problem] To provide a bispecific antibody for preventing or treating an immune inflammatory disease by acting on both human TLR2 and human TLR4 to inhibit human TLR2- and human TLR4-mediated immune inflammatory effects. [Means for Solution] Provided is a bispecific antibody for human TLR2 and human TLR4, including a heavy chain variable region of an anti-human TLR2 antibody consisting of the amino acid sequence of amino acid numbers 1 to 120 of SEQ ID NO: 4; a light chain variable region of an anti-human TLR2 antibody consisting of the amino acid sequence of amino acid numbers 1 to 113 of SEQ ID NO: 6; a heavy chain variable region of an anti-human TLR4 antibody consisting of the amino acid sequence of amino acid numbers 491 to 609 of SEQ ID NO: 4; and a light chain variable region of an anti-human TLR4 antibody consisting of the amino acid sequence of amino acid numbers 625 to 732 of SEQ ID NO: 4.Type: ApplicationFiled: February 27, 2015Publication date: December 8, 2016Applicant: ASTELLAS PHARMA INC.Inventors: Satoshi TAKEUCHI, Masahito SATO, Jotarou SUZUKI, Shinji SOGA, Jun TAKASAKI, Koji AOYAMA, Chie OKUYAMA
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PHARMACEUTICAL COMPOSITION COMPRISING DIAMINO HETEROCYCLIC CARBOXAMIDE COMPOUND AS ACTIVE INGREDIENT
Publication number: 20160339020Abstract: A pharmaceutical composition is suitable for treating AXL-related cancer. The cancer can be cancer with high expression of AXL. The cancer can also be cancer which has acquired resistance by the activation of AXL against therapy with an anticancer agent. Specific diamino heterocyclic carboxamide compounds have an AXL inhibitory action, and pharmaceutical compositions comprising these compounds as an active ingredient have a therapeutic effect on AXL-related cancer. This AXL-related cancer can be cancer with high expression of AXL and/or cancer which has acquired resistance by the activation of AXL against therapy with an anticancer agent.Type: ApplicationFiled: February 3, 2015Publication date: November 24, 2016Applicant: ASTELLAS PHARMA INC.Inventors: Tomohiro EGUCHI, Masamichi MORI, Yoko YAMAKI