Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Takenori Hitaka"'
Autor:
Hisashi Fujita, Masami Yamada, Atsushi Hasuoka, Takenori Hitaka, Masaharu Nakayama, Jason Yano, Takahito Hara, Moriteru Asano, Noriyuki Habuka, Keith Wilson, Takashi Santou, Masuo Yamaoka, Megumi Morimoto, Hiromi Shinohara, Takashi Imada, Yumi Imai
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(9)
We recently reported a class of novel tissue-selective androgen receptor modulators (SARMs), represented by a naphthalene derivative A. However, their pharmacokinetic (PK) profiles were poor due to low metabolic stability. To improve the PK profiles,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c672e0181d7569b25138c9706b59eef3
https://pubmed.ncbi.nlm.nih.gov/28363748
https://pubmed.ncbi.nlm.nih.gov/28363748
Autor:
Hideyuki Oki, Takahiko Taniguchi, Tomoaki Hasui, Makoto Fushimi, Masato Yoshikawa, Hironori Kokubo, Jun Kunitomo, Takenori Hitaka, Kosuke Nakashima
Publikováno v:
Bioorganicmedicinal chemistry. 24(16)
Utilizing structure-based drug design techniques, we designed and synthesized phosphodiesterase 10A (PDE10A) inhibitors based on pyridazin-4(1H)-one. These compounds can interact with Tyr683 in the PDE10A selectivity pocket. Pyridazin-4(1H)-one deriv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b445ab10c6d97d93e23106fd2cc873d4
https://pubmed.ncbi.nlm.nih.gov/27301679
https://pubmed.ncbi.nlm.nih.gov/27301679
Autor:
Masami Kusaka, Junzo Takahashi, Masuo Yamaoka, Satoru Asahi, Takahito Hara, Takenori Hitaka, Tomohiro Kaku, Toshiyuki Takeuchi, Hiroshi Miki, Akihiro Tasaka
Publikováno v:
The Journal of Steroid Biochemistry and Molecular Biology. 129:115-128
Surgical or pharmacologic methods to control gonadal androgen biosynthesis are effective approaches in the treatment of a variety of non-neoplastic and neoplastic diseases. For example, androgen ablation and its consequent reduction in circulating le
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e25cb51d6b392d67dbb96e8b943c392
https://doi.org/10.1016/j.jsbmb.2012.01.001
https://doi.org/10.1016/j.jsbmb.2012.01.001
Autor:
Nobuyuki Matsunaga, Akihiro Tasaka, Satoru Asahi, Mari Adachi, Takahito Hara, Toshimasa Tanaka, Teruaki Okuda, Akio Ojida, Takenori Hitaka, Shuichi Furuya, Tomohiro Kaku, Masami Kusaka, Masuo Yamaoka
Publikováno v:
Bioorganic & Medicinal Chemistry. 19:6383-6399
A novel naphthylmethylimidazole derivative 1 and its related compounds were identified as 17,20-lyase inhibitors. Based on the structure–activity relationship around the naphthalene scaffold and the results of a docking study of 1a in the homology
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0d9ae1020bfeecd91e9f7d00f654b7c3
https://doi.org/10.1016/j.bmc.2011.08.066
https://doi.org/10.1016/j.bmc.2011.08.066
Autor:
Daisuke Nakata, Satoshi Sasaki, Akira Tanaka, Mie Yoshimatsu, Kazumasa Hamamura, Shuichi Furuya, Kazuhiro Miwa, Tomoyuki Kitazaki, Takashi Imada, Takenori Hitaka, Satoshi Endo, Masami Kusaka
Publikováno v:
Journal of Medicinal Chemistry. 54:4998-5012
We previously discovered an orally active human gonadotropin-releasing hormone (GnRH) receptor antagonist, thieno[2,3-d]pyrimidine-2,4-dione derivative 1 (sufugolix). To reduce the cytochrome P450 (CYP) inhibitory activity and improve in vivo GnRH an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d51fe5b89594e0e28250d6034b09d875
https://doi.org/10.1021/jm200216q
https://doi.org/10.1021/jm200216q
Autor:
Takahito Hara, Mitsuru Shiraishi, Junichi Miyazaki, Akihiro Tasaka, Masuo Yamaoka, Takenori Hitaka, Toshio Miyawaki, Katsuji Aikawa, Naoyuki Kanzaki, Masami Kusaka, Satoshi Yamamoto, Yumi N. Imai
Publikováno v:
Bioorganicmedicinal chemistry. 23(10)
To develop effective drugs for hypogonadism, sarcopenia, and cachexia, we designed, synthesized, and evaluated selective androgen receptor modulators (SARMs) that exhibit not only anabolic effects on organs such as muscles and the central nervous sys
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59e2cc5819a7323d675f18b5607c7a37
https://pubmed.ncbi.nlm.nih.gov/25862209
https://pubmed.ncbi.nlm.nih.gov/25862209
Autor:
Tomohiro Kaku, Hitomi Yamasaki, Naohiro Kawaguchi, Masami Kusaka, Akihiro Tasaka, Masuo Yamaoka, Toshiyuki Takeuchi, Takenori Hitaka, Hiroshi Miki, Takahito Hara
Publikováno v:
Cancer Research. 70:DD01-03
Background: Recent studies suggest that residual adrenal androgen after castration could be responsible for the progression of castration-resistant prostate cancer (CRPC). To develop an effective therapy for CRPC that inhibits the production of adren
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::150f61e65f6504dfbf7f84361d9ec411
https://doi.org/10.1158/1538-7445.am10-dd01-03
https://doi.org/10.1158/1538-7445.am10-dd01-03
Publikováno v:
Chemical and Pharmaceutical Bulletin. 43:256-261
Novel pyrrolo[2, 3-d]pyrimidine antifolates (1a, b and 2a, b) with a nitrogen atom in the bridge chain between the 2, 4-diaminopyrrolo[2, 3-d]pyrimidine and phenylene rings were designed and efficiently synthesized. These compounds exhibited more pot
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2479efbc2a9ecb3555bdb3d7bcd9a76e
https://doi.org/10.1248/cpb.43.256
https://doi.org/10.1248/cpb.43.256
Autor:
Takahito Hara, Takenori Hitaka, Nobuyuki Matsunaga, Naoyuki Kanzaki, Masuo Yamaoka, Shuichi Furuya, Takashi Santou, Mitsuhiro Ito, Satoshi Yamamoto, Masami Kusaka, Junichi Miyazaki, Kazumasa Hamamura, Masami Yamada, Akihiro Tasaka
Publikováno v:
Bioorganicmedicinal chemistry. 20(1)
A series of 4-phenylpyrrole derivatives D were designed, synthesized, and evaluated for their potential as novel orally available androgen receptor antagonists therapeutically effective against castration-resistant prostate cancers. 4-Phenylpyrrole c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::274984d6cb2da2dcf7dd2adc6ff3fdb8
https://pubmed.ncbi.nlm.nih.gov/22094279
https://pubmed.ncbi.nlm.nih.gov/22094279
Publikováno v:
The Journal of Organic Chemistry. 58:1696-1701
A novel and efficient synthetic method for the synthesis of pyrrolo[2,3-d]pyrimidine antifolates is described. The key reaction of this method is the photo-initiated free radical addition of bromomalononitrile or ethyl bromocyanoacetate to an enol et
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8b663c90d45b38ae9ce28c722349f2a9
https://doi.org/10.1021/jo00059a016
https://doi.org/10.1021/jo00059a016