190786-13-1Relevant academic research and scientific papers
RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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, (2020/07/06)
Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.
Synthesis of 2-phenylbenzofuran derivatives as testosterone 5α- reductase inhibitor
Ishibashi, Koki,Nakajima, Katsuyoshi,Sugioka, Yuki,Sugiyama, Mitsuo,Hamada, Takakazu,Horikoshi, Hiroyoshi,Nishi, Takahide
, p. 226 - 240 (2007/10/03)
A series of 2-phenylbenzofuran derivatives with a carbamoyl, alkylamino, or alkyloxy group at the 5 or 6 position of the benzofuran ring were synthesized and evaluated for rat and human testosterone 5α-reductase inhibitory activities in vitro. Against rat enzyme, the carbamoyl derivatives had more potent inhibitory activities than the alkylamino or alkyloxy derivatives, and the 6-carbamoyl derivatives tended to be more potent than the 5-carbamoyl derivatives. Against human enzyme, the 6-substituted derivatives had more potent inhibitory activities than the 5-substituted derivatives. The 6-carbamoyl and 6-alkylamino derivatives tended to show stronger inhibitory activities against human type 1 enzyme than against type 2 enzyme, but they were not largely selective.
Synthesis and 5α-reductase inhibitory activities of benzofuran derivatives with a carbamoyl group
Ishibashi, Koki,Nakajima, Katsuyoshi,Sugioka, Yuki,Sugiyama, Mitsuo,Hamada, Takakazu,Horikoshi, Hiroyoshi,Nishi, Takahide
, p. 561 - 566 (2007/10/03)
A series of 2-phenylbenzofuran derivatives with a diphenylmethylcarbamoyl group at the 5 or 6 position of the benzofuran ring were synthesized and evaluated for rat and human testosterone 5α-reductase inhibitory activities in vitro. They had inhibitory activities against both enzymes and the 6-carbamoyl derivatives tended to be more potent than the 5-carbamoyl compounds.
