D. Western Therapeutics Institute, Inc.

Kengo Sumi

Hiroyoshi Hidaka

Yoshihiro Inoue

Kouichi Takahashi

Ryohei Nakamura

Takashi Izuhara

Osamu Kimata

Tomoyuki Koide

Kazunao Masubuchi

Yuji Takashima

A method may produce an isoquinoline-6-sulfonamide derivative useful as a medicinal drug; and an intermediate which is used for the method, and more specifically, a 1,4-diazocane compound of formula (8), wherein Ris an amino protecting group, or a salt thereof.

1,4-diazocane compound or salt thereof

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.

Isoquinoline sulfonyl chloride acid addition salts and method of manufacture thereof

A stable crystal of a salt of N&#x2014;[(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&#x2014;[(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 2&#x3b8; angles of 6.8&#xb1;0.1&#xb0;, 10.0&#xb1;0.1&#xb0;, 12.7&#xb1;0.1&#xb0;, 14.6&#xb1;0.1&#xb0;, 14.8&#xb1;0.1&#xb0;, 16.2&#xb1;0.1&#xb0;, 17.4&#xb1;0.1&#xb0;, 17.8&#xb1;0.1&#xb0;, 19.5&#xb1;0.1&#xb0;, 20.0&#xb1;0.1&#xb0;, 21.6&#xb1;0.1&#xb0;, 24.7&#xb1;0.1&#xb0;, 25.5&#xb1;0.1&#xb0;, 25.8&#xb1;0.1&#xb0;, 29.8&#xb1;0.1&#xb0;, 39.5&#xb1;0.1&#xb0;, and/or 44.9&#xb1;0.1&#xb0; in powder X-ray diffraction spectrum.

Form of isoquinoline sulfonamide

The present invention provides an isoquinoline-6-sulfonamide derivative that is useful as a novel pharmaceutical agent. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt: wherein X and Y each independently represent a direct bond, NH, CH&#x2550;CH, O, or S; Rand Reach independently represent a hydrogen atom, a halogen atom, a cyano group, an alkyl group, or the like; Rand Reach independently represent a hydrogen atom, an alkyl group, or the like, or Rand Rtogether form an alkylene group or an alkenylene group, which may be bridged between two carbon atoms to an arbitrary position; and l, m, and n represent an integer number of 1 to 4. 

Substituted isoquinoline derivative

The present invention provides a novel isoquinoline-6-sulfonamide derivative that is useful as a medicine. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt, wherein Rand Reach independently represent a hydrogen atom, or the like; Rand Reach independently represent a hydrogen atom, an alkyl group, or the like; Rrepresents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted cycloalkyl group, an optionally substituted alkanoyl group, or the like; and A represents a linear or branched alkylene group having 2 to 6 carbon atoms. 

Growing community of inventors

Nagoya, Japan

Kengo Sumi