Patents by Inventor Akio Kakefuda
Akio Kakefuda 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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Patent number: 11912679Abstract: [Problem] A compound which is useful as a STING inhibitor is provided. [Means for Solution] The present inventors have found aryl alkynamide derivatives having an inhibitory action on STING. The aryl alkynamide derivatives of the present invention have an inhibitory action on STING and can be used as an agent for treating an autoimmune disease, a neurodegenerative disease, a type I interferonopathy and/or other STING-mediated disease.Type: GrantFiled: September 26, 2023Date of Patent: February 27, 2024Assignees: Astellas Pharma, Inc., Mitobridge, Inc.Inventors: Junko Maeda, Ikumi Kuriwaki, Kai Kitamura, Yumi Yamashita, Kenichi Kakefuda, Akio Kamikawa, Kenji Negoro, Wataru Hamaguchi, Ryushi Seo, Jeffrey Ciavarri
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Publication number: 20140275105Abstract: [Problem] A crystal of (2R,5S)-4-(3-chloro-4-cyanophenyl)-N-(2-cyclopropylpyrimidin-5-yl)-2,5-dimethylpiperazine-1-carboxamide with excellent activity as an androgen receptor (AR) antagonistic compound, the salts thereof, or the solvate thereof, which is suitable for industrialization as a bulk drug of pharmaceutical products; a pharmaceutical composition comprising the crystal as an active ingredient; and the pharmaceutical composition which is the AR antagonistic drug are provided. [Solution] A01-type crystal of monohydrate, A01-type crystal of hydrochloride, A01-type crystal of hydrobromide, and A01-type crystal of methanesulfonate of (2R,5S)-4-(3-chloro-4-cyanophenyl)-N-(2-cyclopropylpyrimidin-5-yl)-2,5-dimethylpiperazine-1-carboxamide, which have certain crystal forms, are provided.Type: ApplicationFiled: October 19, 2012Publication date: September 18, 2014Applicant: ASTELLAS PHARMA INC.Inventors: Takashi Nakamura, Takumi Okamoto, Yutaka Hirakura, Kouji Yamazaki, Akio Kakefuda, Hiroyuki Yamashita
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Patent number: 8513422Abstract: As a result of studies on compounds having a selective inhibitory activity against 17?HSD type 5, the present inventors have confirmed that a {1-[(indol-2-yl)carbonyl]piperidyl}alkanol derivative has a potent selective inhibitory activity against 17?HSD type 5. The invention has been completed based on these findings. The compound of the present invention can be used as an agent for treating and/or an agent for preventing diseases associated with 17?HSD type 5, such as benign prostatic hyperplasia and prostate cancer, without accompanying adverse effects due to a decrease in testosterone.Type: GrantFiled: August 28, 2008Date of Patent: August 20, 2013Assignee: Astellas Pharma Inc.Inventors: Akio Kakefuda, Kazushi Watanabe, Akio Kamikawa, Kentaro Enjo, Takashi Furutani, Minoru Yasuda
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Publication number: 20130197009Abstract: [Problem] An object of the present invention is to provide a novel anticancer drug which is useful for treating prostate cancer accompanying androgen receptor mutation [Means for Solution] The present inventors conducted thorough research on mutant androgen-related diseases for which the traditional anti-androgen drugs become ineffective. As a result, they found that the compound, which is an active ingredient of the pharmaceutical composition of the present invention, exhibits an inhibitory action against transcriptional activation in a human mutant androgen receptor (AR), and has an excellent antitumor action in a human prostate cancer-bearing mouse, thereby completing the present invention. Accordingly, the compound, which is an active ingredient of the pharmaceutical composition of the present invention, is useful for a series of androgen receptor-related diseases including prostate cancer.Type: ApplicationFiled: October 21, 2011Publication date: August 1, 2013Applicant: ASTELLAS PHARMA INC.Inventors: Yukitaka Ideyama, Sadao Kuromitsu, Takashi Furutani, Masayoshi Takeda, Satoshi Konagai, Tomohiro Yamada, Nobuaki Taniguchi, Yutaka Kondoh, Masaaki Hirano, Kazushi Watanabe, Takashi Sugane, Akio Kakefuda
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Publication number: 20110172230Abstract: [Object] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly urinary frequency, urinary incontinence and/or overactive bladder. [Means for solution] It is confirmed that a urea compound chemical-structurally characterized by having a piperidine or piperazine ring or a salt thereof has an excellent FAAH-inhibitory activity, and thus the present invention is completed. The urea compound or its pharmaceutically acceptable salt of the present invention can increase the effective bladder capacity and ameliorate the state of urinary frequency, and is therefore useful as an agent for treating urinary frequency, urinary incontinence and/or overactive bladder.Type: ApplicationFiled: August 22, 2007Publication date: July 14, 2011Inventors: Takahiro Ishii, Takashi Sugane, Akio Kakefuda, Tatsuhisa Takahashi, Tokatoshi Kanayama, Kentaro Sato, Ikumi Kuriwaki, Chika Kitada, Jotaro Suzuki
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Patent number: 7919495Abstract: To provide a compound usable for treatment of diseases associated with fatty acid amide hydrolase (FAAH), especially for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. We have found that a novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative of the present invention has an excellent effect for increasing an effective bladder capacity, an excellent effect for relieving urinary frequency and an excellent anti-allodynia effect, and is therefore usable for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.Type: GrantFiled: February 16, 2006Date of Patent: April 5, 2011Assignee: Astellas Pharma, Inc.Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
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Patent number: 7919494Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.Type: GrantFiled: August 19, 2009Date of Patent: April 5, 2011Assignee: Astellas Pharma, Inc.Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
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Patent number: 7915261Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.Type: GrantFiled: August 19, 2009Date of Patent: March 29, 2011Assignee: Astellas Pharma, Inc.Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
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Publication number: 20110071146Abstract: To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17?HSD type 5. It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17?HSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone, and the present invention has thus been completed.Type: ApplicationFiled: November 10, 2010Publication date: March 24, 2011Inventors: Tatsuya Niimi, Akio Kamikawa, Yasushi Amano, Tomohiko Yamaguchi, Kenichi Suzumura, Kentaro Enjo, Takashi Furutani, Akio Kakefuda, Yutaka Kondoh, Masaaki Hirano
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Patent number: 7855225Abstract: To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17?HSD type 5. It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17?HSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone, and the present invention has thus been completed.Type: GrantFiled: March 1, 2007Date of Patent: December 21, 2010Assignee: Astellas Pharma Inc.Inventors: Tatsuya Niimi, Akio Kamikawa, Yasushi Amano, Tomohiko Yamaguchi, Kenichi Suzumura, Kentaro Enjo, Takashi Furutani, Akio Kakefuda, Yutaka Kondoh, Masaaki Hirano
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Publication number: 20100256189Abstract: As a result of studies on compounds having a selective inhibitory activity against 17?HSD type 5, the present inventors have confirmed that a {1-[(indol-2-yl)carbonyl]piperidyl}alkanol derivative has a potent selective inhibitory activity against 17?HSD type 5. The invention has been completed based on these findings. The compound of the present invention can be used as an agent for treating and/or an agent for preventing diseases associated with 17?HSD type 5, such as benign prostatic hyperplasia and prostate cancer, without accompanying adverse effects due to a decrease in testosterone.Type: ApplicationFiled: August 28, 2008Publication date: October 7, 2010Inventor: Akio KAKEFUDA
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Patent number: 7807664Abstract: A novel 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or a pharmaceutically acceptable salt thereof, which is useful as an agent for treating or preventing nocturia and/or diabetes insipidus, is provided.Type: GrantFiled: November 14, 2006Date of Patent: October 5, 2010Assignee: Astella Pharma Inc.Inventors: Hiroyuki Koshio, Issei Tsukamoto, Akio Kakefuda, Seijiro Akamatsu, Chikashi Saitoh
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Publication number: 20100190826Abstract: Provided is a novel and excellent method for treating and/or preventing benign prostatic hyperplasia, prostate cancer, and the like based on selective inhibitory activity against 17?HSD type 5. It was found that an indole or benzimidazole derivative, where a nitrogen atom of the indole ring or benzimidazole ring is substituted with a phenyl group substituted with COOH, has a potent selective inhibitory activity against 17?HSD type 5 and may become an agent for treating and/or an agent for preventing a disease associated with 17?HSD type 5, such as benign prostatic hyperplasia, prostate cancer and the like, without accompanying adverse effects due to a decrease in testosterone; and the present invention has thus been completed.Type: ApplicationFiled: July 23, 2008Publication date: July 29, 2010Inventors: Akio Kakefuda, Yutaka Kondoh, Masaaki Hirano, Akio Kamikawa, Kentaro Enjo, Takashi Furutani
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Publication number: 20100009972Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.Type: ApplicationFiled: August 19, 2009Publication date: January 14, 2010Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
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Publication number: 20100009971Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.Type: ApplicationFiled: August 19, 2009Publication date: January 14, 2010Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
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Publication number: 20090181960Abstract: To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17?HSD type 5. It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17?HSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone, and the present invention has thus been completed.Type: ApplicationFiled: March 1, 2007Publication date: July 16, 2009Inventors: Tatsuya Niimi, Akio Kamikawa, Yasushi Amano, Tomohiko Yamaguchi, Kenichi Suzumura, Kentaro Enjo, Takashi Furutani, Akio Kakefuda, Yutaka Kondoh, Masaaki Hirano
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Publication number: 20080306046Abstract: [Problem] To provide a compound usable for treatment of diseases associated with fatty acid amide hydrolase (FAAH), especially for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. [Means for Solution] We have found that a novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative of the present invention has an excellent effect for increasing an effective bladder capacity, an excellent effect for relieving urinary frequency and an excellent anti-allodynia effect, and is therefore usable for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.Type: ApplicationFiled: February 16, 2006Publication date: December 11, 2008Applicant: FMC CORPORATIONInventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
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Publication number: 20070167429Abstract: A novel 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or a pharmaceutically acceptable salt thereof, which is useful as an agent for treating or preventing nocturia and/or diabetes insipidus, is provided.Type: ApplicationFiled: November 14, 2006Publication date: July 19, 2007Inventors: Hiroyuki Koshio, Issei Tsukamoto, Akio Kakefuda, Seijiro Akamatsu, Chikashi Saitoh
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Patent number: 7183271Abstract: A novel 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or a pharmaceutically acceptable salt thereof, which is useful as an agent for treating or preventing nocturia and/or diabetes insipidus, is provided.Type: GrantFiled: April 26, 2004Date of Patent: February 27, 2007Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Koshio, Issei Tsukamoto, Akio Kakefuda, Seijiro Akamatsu, Chikashi Saitoh
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Publication number: 20060142268Abstract: To provide a compound having a superior arginine vasopressin antagonism. A novel 1,4,5,6-tetrahydroimidazo[4,5-d]benzazepine derivative or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 15, 2006Publication date: June 29, 2006Inventors: Hiroyuki Koshio, Akio Kakefuda, Ippei Sato, Ryutaro Wakayama, Masanao Sanagi