公开(公告)号：US11535595B2

公开(公告)日：2022-12-27

申请号：US17296469

申请日：2019-12-16

申请人： D. WESTERN THERAPEUTICS INSTITUTE, INC.

发明人： Kengo Sumi ,  Ryohei Nakamura

IPC分类号： C07D217/22 ,  C07D217/02

摘要： A compound, such as isoquinoline-6-sulfonyl chloride acid and/or addition salts thereof, may be useful as a manufacturing intermediate for an isoquinoline-6-sulfonamide compound. A method for manufacturing such compounds and/or or acid addition salts thereof, may involve subjecting 6-(benzylthio)isoquinoline to an oxidative chlorination reaction and/or reacting 6-aminoisoquinoline with a nitrite or nitrous acid ester, then with thionyl chloride, and then with an acid.

公开(公告)号：US11427546B2

公开(公告)日：2022-08-30

申请号：US17296439

申请日：2019-12-16

申请人： D. WESTERN THERAPEUTICS INSTITUTE, INC.

发明人： Hiroyoshi Hidaka ,  Kengo Sumi ,  Takashi Izuhara

IPC分类号： C07D217/22

摘要： A stable crystal of a salt of N—[(R)-1-{(S)-2-hydroxy-2-phenylpropylamino}propan-2-yl]isoquinoline-6-sulfonamide may have desirable properties for a pharmaceutical drug substance, and more specifically N—[(R)-1-{(S)-2-hydroxy-2-phenylpropylamino}propan-2-yl]isoquinoline-6-sulfonamide dihydrochloride anhydride. A crystal of the anhydride may have characteristic peaks at 2θ angles of 6.8±0.1°, 10.0±0.1°, 12.7±0.1°, 14.6±0.1°, 14.8±0.1°, 16.2±0.1°, 17.4±0.1°, 17.8±0.1°, 19.5±0.1°, 20.0±0.1°, 21.6±0.1°, 24.7±0.1°, 25.5±0.1°, 25.8±0.1°, 29.8±0.1°, 39.5±0.1°, and/or 44.9±0.1° in powder X-ray diffraction spectrum.