Discovery and biological evaluation of 1-{2,7-diazaspiro[3.5]nonan-2-yl}prop-2-en-1-one derivatives as covalent inhibitors of KRAS G12C with favorable metabolic stability and anti-tumor activity
Imaizumi, Tomoyoshi, Akaiwa, Michinori, Abe, Tomoaki, Nigawara, Takahiro, Koike, Takanori, Satake, Yoshiki, Watanabe, Kazushi, Kaneko, Osamu, Amano, Yasushi, Mori, Kenichi, Yamanaka, Yosuke, Nagashima, Takeyuki, Shimazaki, Masashi, Kuramoto, Kazuyuki
Published in Bioorganic & medicinal chemistry (01.10.2022)
Published in Bioorganic & medicinal chemistry (01.10.2022)
Get full text
Journal Article
Discovery of ASP6918, a KRAS G12C inhibitor: Synthesis and structure-activity relationships of 1-{2,7-diazaspiro[3.5]non-2-yl} prop-2-en-1-one derivatives as covalent inhibitors with good potency and oral activity for the treatment of solid tumors
Imaizumi, Tomoyoshi, Shimada, Itsuro, Satake, Yoshiki, Yamaki, Susumu, Koike, Takanori, Nigawara, Takahiro, Kaneko, Osamu, Amano, Yasushi, Mori, Kenichi, Yamanaka, Yosuke, Nakayama, Ayako, Nishizono, Yoshihiro, Shimazaki, Masashi, Nagashima, Takeyuki, Kuramoto, Kazuyuki
Published in Bioorganic & medicinal chemistry (15.01.2024)
Published in Bioorganic & medicinal chemistry (15.01.2024)
Get full text
Journal Article
SUBSTITUTED PYRIDAZINE COMPOUND
NEGORO, Kenji, SABA, Kengo, IIDA, Maiko, KOIZUMI, Yuka, YAMAKI, Susumu, INAGAKI, Yusuke, KOIKE, Takanori, MAEDA, Junko, KAMIKUBO, Takashi, NIGAWARA, Takahiro, KURIWAKI, Ikumi, SHISHIKURA, Junichi
Year of Publication 22.05.2024
Get full text
Year of Publication 22.05.2024
Patent
SUBSTITUTED PYRIDAZINE COMPOUND
Yamaki, Susumu, Iida, Maiko, Kuriwaki, Ikumi, Kamikubo, Takashi, Koizumi, Yuka, Maeda, Junko, Saba, Kengo, Inagaki, Yusuke, Koike, Takanori, Negoro, Kenji, Nigawara, Takahiro, Shishikura, Junichi
Year of Publication 06.04.2023
Get full text
Year of Publication 06.04.2023
Patent
SUBSTITUTED PYRIDAZINE COMPOUND
NEGORO, Kenji, SABA, Kengo, IIDA, Maiko, KOIZUMI, Yuka, YAMAKI, Susumu, INAGAKI, Yusuke, KOIKE, Takanori, MAEDA, Junko, KAMIKUBO, Takashi, NIGAWARA, Takahiro, KURIWAKI, Ikumi, SHISHIKURA, Junichi
Year of Publication 08.02.2023
Get full text
Year of Publication 08.02.2023
Patent
QUINAZOLINE COMPOUND
WATANABE, KAZUSHI, NIGAWARA, TAKAHIRO, KUNIKAWA, SHIGEKI, ARAKAWA, KEISUKE, SHIMADA, ITSURO, IMAIZUMI, TOMOYOSHI, SATAKE, YOSHIKI, YAMAKI, SUSUMU, ARAKI, TAKANOBU, SHIMAZAKI, MASASHI, KOIKE, TAKANORI, KURAMOTO, KAZUYUKI, AKAIWA, MICHINORI, ABE, TOMOAKI
Year of Publication 17.01.2022
Get full text
Year of Publication 17.01.2022
Patent
QUINAZOLINE COMPOUND
ABE, Tomoaki, KURAMOTO, Kazuyuki, AKAIWA, Michinori, YAMAKI, Susumu, KOIKE, Takanori, SATAKE, Yoshiki, NIGAWARA, Takahiro, SHIMADA, Itsuro, IMAIZUMI, Tomoyoshi, ARAKI, Takanobu, ARAKAWA, Keisuke, WATANABE, Kazushi, SHIMAZAKI, Masashi, KUNIKAWA, Shigeki
Year of Publication 10.11.2021
Get full text
Year of Publication 10.11.2021
Patent
QUINAZOLINE COMPOUND
ABE, Tomoaki, KURAMOTO, Kazuyuki, AKAIWA, Michinori, YAMAKI, Susumu, KOIKE, Takanori, SATAKE, Yoshiki, NIGAWARA, Takahiro, SHIMADA, Itsuro, IMAIZUMI, Tomoyoshi, ARAKI, Takanobu, ARAKAWA, Keisuke, WATANABE, Kazushi, SHIMAZAKI, Masashi, KUNIKAWA, Shigeki
Year of Publication 21.10.2020
Get full text
Year of Publication 21.10.2020
Patent
Quinazoline compound
Kuramoto, Kazuyuki, Yamaki, Susumu, Arakawa, Keisuke, Araki, Takanobu, Satake, Yoshiki, Koike, Takanori, Nigawara, Takahiro, Kunikawa, Shigeki, Watanabe, Kazushi, Akaiwa, Michinori, Abe, Tomoaki, Imaizumi, Tomoyoshi, Shimada, Itsuro, Shimazaki, Masashi
Year of Publication 15.09.2020
Get full text
Year of Publication 15.09.2020
Patent
QUINAZONE COMPOUND
ABE, Tomoaki, KURAMOTO, Kazuyuki, AKAIWA, Michinori, YAMAKI, Susumu, KOIKE, Takanori, SATAKE, Yoshiki, NIGAWARA, Takahiro, SHIMADA, Itsuro, IMAIZUMI, Tomoyoshi, ARAKI, Takanobu, ARAKAWA, Keisuke, WATANABE, Kazushi, SHIMAZAKI, Masashi, KUNIKAWA, Shigeki
Year of Publication 01.06.2020
Get full text
Year of Publication 01.06.2020
Patent
QUINAZOLINE COMPOUND
Kuramoto, Kazuyuki, Yamaki, Susumu, Arakawa, Keisuke, Araki, Takanobu, Satake, Yoshiki, Koike, Takanori, Nigawara, Takahiro, Kunikawa, Shigeki, Watanabe, Kazushi, Akaiwa, Michinori, Abe, Tomoaki, Imaizumi, Tomoyoshi, Shimada, Itsuro, Shimazaki, Masashi
Year of Publication 07.05.2020
Get full text
Year of Publication 07.05.2020
Patent
Quinazoline compound
Kuramoto, Kazuyuki, Yamaki, Susumu, Arakawa, Keisuke, Araki, Takanobu, Satake, Yoshiki, Koike, Takanori, Nigawara, Takahiro, Kunikawa, Shigeki, Watanabe, Kazushi, Akaiwa, Michinori, Abe, Tomoaki, Imaizumi, Tomoyoshi, Shimada, Itsuro, Shimazaki, Masashi
Year of Publication 11.02.2020
Get full text
Year of Publication 11.02.2020
Patent
QUINAZOLINE COMPOUND
ABE, Tomoaki, KURAMOTO, Kazuyuki, AKAIWA, Michinori, YAMAKI, Susumu, KOIKE, Takanori, SATAKE, Yoshiki, NIGAWARA, Takahiro, SHIMADA, Itsuro, IMAIZUMI, Tomoyoshi, ARAKI, Takanobu, ARAKAWA, Keisuke, WATANABE, Kazushi, SHIMAZAKI, Masashi, KUNIKAWA, Shigeki
Year of Publication 11.12.2019
Get full text
Year of Publication 11.12.2019
Patent
COMPOSÉ DE QUINAZOLINE
ABE, Tomoaki, KURAMOTO, Kazuyuki, AKAIWA, Michinori, YAMAKI, Susumu, KOIKE, Takanori, SATAKE, Yoshiki, NIGAWARA, Takahiro, SHIMADA, Itsuro, IMAIZUMI, Tomoyoshi, ARAKAWA, Keisuke, ARAKI, Takanobu, WATANABE, Kazushi, SHIMAZAKI, Masashi, KUNIKAWA, Shigeki
Year of Publication 11.12.2019
Get full text
Year of Publication 11.12.2019
Patent
QUINAZOLINE COMPOUND
Kuramoto, Kazuyuki, Yamaki, Susumu, Arakawa, Keisuke, Araki, Takanobu, Satake, Yoshiki, Koike, Takanori, Nigawara, Takahiro, Kunikawa, Shigeki, Watanabe, Kazushi, Akaiwa, Michinori, Abe, Tomoaki, Imaizumi, Tomoyoshi, Shimada, Itsuro, Shimazaki, Masashi
Year of Publication 26.09.2019
Get full text
Year of Publication 26.09.2019
Patent
QUINAZOLINE COMPOUND
ABE, Tomoaki, KURAMOTO, Kazuyuki, AKAIWA, Michinori, YAMAKI, Susumu, KOIKE, Takanori, SATAKE, Yoshiki, NIGAWARA, Takahiro, SHIMADA, Itsuro, IMAIZUMI, Tomoyoshi, ARAKI, Takanobu, ARAKAWA, Keisuke, WATANABE, Kazushi, SHIMAZAKI, Masashi, KUNIKAWA, Shigeki
Year of Publication 27.08.2019
Get full text
Year of Publication 27.08.2019
Patent
Quinazoline compound
Kuramoto, Kazuyuki, Yamaki, Susumu, Arakawa, Keisuke, Araki, Takanobu, Satake, Yoshiki, Koike, Takanori, Nigawara, Takahiro, Kunikawa, Shigeki, Watanabe, Kazushi, Akaiwa, Michinori, Abe, Tomoaki, Imaizumi, Tomoyoshi, Shimada, Itsuro, Shimazaki, Masashi
Year of Publication 15.08.2019
Get full text
Year of Publication 15.08.2019
Patent
NITROGENATED BICYCLIC AROMATIC HETEROCYCLIC COMPOUND
TAKASUNA, YUJI, NIGAWARA, TAKAHIRO, SHIRAI, FUMIYUKI, SATO, JUNJI, NAKANISHI, KEITA, SHIRAKAMI, SHOHEI, NAKAJIMA, YUTAKA, IMADA, SUNAO, AOYAMA, NAOHIRO, KUBO, KAORI
Year of Publication 31.01.2018
Get full text
Year of Publication 31.01.2018
Patent
Compuesto heterocíclico aromático bicíclico nitrogenado
SHIRAKAMI, Shohei, SATO, Junji, NAKAJIMA, Yutaka, AOYAMA, Naohiro, IMADA, Sunao, KUBO, Kaori, NAKANISHI, Keita, TAKASUNA, Yuji, NIGAWARA, Takahiro, SHIRAI, Fumiyuki
Year of Publication 01.12.2017
Get full text
Year of Publication 01.12.2017
Patent
NITROGENATED BICYCLIC AROMATIC HETEROCYCLIC COMPOUND
NAOHIRO AOYAMA, JUNJI SATO, YUTAKA NAKAJIMA, KAORI KUBO, SUNAO IMADA, TAKAHIRO NIGAWARA, YUJI TAKASUNA, SHOHEI SHIRAKAMI, KEITA NAKANISHI, FUMIYUKI SHIRAI
Year of Publication 08.11.2017
Get full text
Year of Publication 08.11.2017
Patent