公开(公告)号：US10689394B2

公开(公告)日：2020-06-23

申请号：US16306696

申请日：2017-06-14

Applicant: The University of Tokyo

Inventor： Hidenori Ichijo ,  Kengo Homma ,  Naomi Tsuburaya ,  Tetsuo Nagano ,  Takayoshi Okabe ,  Hirotatsu Kojima ,  Manabu Shimonishi ,  Takao Fujisawa ,  Norio Shiibata ,  Tsunehiko Higuchi ,  Seiichi Nakamura ,  Hidehiko Nakagawa ,  Shin-Ichi Ikeda

IPC: C07D495/04 ,  C07D401/04 ,  A61P21/02 ,  A61K31/4365 ,  A61P21/00

Abstract: A compound represented by the following formula (1) is provided: wherein X represents a sulfur atom or —CH═CH—; A1 to A4 each independently represent a carbon atom or a nitrogen atom, and at least one of A1 to A4 is a nitrogen atom; R1 represents any one of a 1,2,3,4-tetrahydroquinolyl group (or a 3,4-dihydro-1(2H)-quinolyl group), a 3,4-dihydro-4,4-dimethyl-1(2H)-quinolyl group, a 2,3,4,5-tetrahydro-1H-1-benzazepinyl group, or a substituent represented by the following formula (2): wherein R4 represents a 2,3,4-trifluorophenyl group, a 4-iodophenyl group, a 2,3-difluorophenyl group, a 3,5-difluorophenyl group, a 5-fluoro-2-methylphenyl group, a 3-pentafluorosulfanylphenyl group, a 2,6-dimethylphenyl group, a 4-benzyloxyphenyl group, a 3,5-bis(trifluoromethyl)biphenyl group, a 4-tert-butylphenyl group, a 3-methoxyphenyl group, an unsubstituted or substituted pyridyl group, or an unsubstituted or substituted naphthyl group; R5 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group optionally containing an oxygen atom and/or a double bond, or an unsubstituted or substituted aromatic lower alkyl group; R2 represents a hydrogen atom, a lower alkyl group, a lower acyl group, or an unsubstituted or substituted aromatic lower alkyl group; and R3 represents a hydrogen atom, or R2 and R3 may bind to each other to form a ring.

公开(公告)号：US20190177336A1

公开(公告)日：2019-06-13

申请号：US16306696

申请日：2017-06-14

Applicant: The University of Tokyo

Inventor： Hidenori Ichijo ,  Kengo Homma ,  Naomi Tsuburaya ,  Tetsuo Nagano ,  Takayoshi Okabe ,  Hirotatsu Kojima ,  Manabu Shimonishi ,  Takao Fujisawa ,  Norio Shiibata ,  Tsunehiko Higuchi ,  Seiichi Nakamura ,  Hidehiko Nakagawa ,  Shin-Ichi Ikeda

IPC: C07D495/04 ,  C07D401/04 ,  A61P21/00

Abstract: It is an object of the present invention to provide a compound inhibiting the binding between ALS-related mutant SOD1 and Derlin-1, a medicament comprising the compound, and a method for treating ALS by administering the medicament to a patient. More specifically, the aforementioned compound is represented by the following formula (1): wherein X represents a sulfur atom or —CH═CH—; A1 to A4 each independently represent a carbon atom or a nitrogen atom, and at least one of A1 to A4 is a nitrogen atom; R1 represents a 1,2,3,4-tetrahydroquinolyl group (or a 3,4-dihydro-1(2H)-quinolyl group), a 3,4-dihydro-4,4-dimethyl-1(2H)-quinolyl group, a 2,3,4,5-tetrahydro-1H-1-benzazepinyl group, or a substituent represented by the following formula (2): wherein R4 represents an unsubstituted or optionally substituted phenyl group, an unsubstituted or optionally substituted pyridyl group, or an unsubstituted or optionally substituted naphthyl group, and R5 represents any one of a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group (optionally containing an oxygen atom and/or a double bond), or an unsubstituted or optionally substituted aromatic lower alkyl group; R2 represents a hydrogen atom, a lower alkyl group, a lower acyl group, or an unsubstituted or optionally substituted aromatic lower alkyl group; and R3 represents a hydrogen atom, or R2 and R3 may bind to each other to form a ring.