A TRANS-N-(1H-PYRAZOLO(3,4-B)PYRIDINE-4-YL)-4-GUANIDINOMETHYL CYCLOHEXANE CARBOXAMIDE-1 METHANE SULFONIC ACID SALT-1 HYDRATE

Title:

A TRANS-N-(1H-PYRAZOLO(3,4-B)PYRIDINE-4-YL)-4-GUANIDINOMETHYL CYCLOHEXANE CARBOXAMIDE-1 METHANE SULFONIC ACID SALT-1 HYDRATE

Document Type and Number:

Japanese Patent JPH08198876

Kind Code:

A

Abstract:

PURPOSE: To obtain an 1 methane sulfonic acid salt.1 hydrate exhibiting high solubility to water without exhibiting hygroscopicity and having high stability in an aqueous solution useful as a remedy for hypertension, stenocardia or bronchial asthma, etc.

CONSTITUTION: This compound is expressed by the formula, e.g., trans-N-(1H- pyrazolo[3-4-b]pyridine-4-yl)-4-guanidinomethyl cyclohexane carboxamide.1 methane sulfonic acid salt.1 hydrate. The compound of the formula is obtained by dissolving trans-N-(1H-pyrazolo[3,4-b]pyridine-4-yl)-4-guanidinomethyl cyclohexane carboxamide into a solvent such as methanol, adding a solution containing 1-1.5eq. of methanesulfonic acid in water or methanol, etc., stirring or holding and recrystallizing from a mixed solvent such as water-methanol without contamination of an organic solvent in high purity. The compound is useful as an inhalant, an injection or ophthalmic solutions, etc., and a dose is preferably 0.1-100mg/1 day.

Inventors:

SAITO TADAMASA
HARADA KYO
KAWAHARA TOSHIO
SATO HIROYUKI
OBATA MINORU

Application Number:

JP1246395A

Publication Date:

August 06, 1996

Filing Date:

January 30, 1995

Export Citation:

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Assignee:

YOSHITOMI PHARMACEUTICAL

International Classes:

C07D471/04; A61K31/435; A61P9/00; A61P9/12; A61P11/00; A61P27/02; A61P27/06; (IPC1-7): C07D471/04

Attorney, Agent or Firm:

Takamiya Castle Masaru

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