Azachroman derivatives with effects on the cardiovascular system

US4931454A · kind A · utility

Assignee

• Merck Patent GmbH · DE

Inventors

• Manfred Baumgarth
• Rolf Gericke · Seeheim-Jugenheim, DE
• Ingeborg Lues · Darmstadt, DE
• Jacques De Peyer · Darmstadt, DE
• Rolf Bergmann

Key dates

• Filing date: Sep 23, 1988
• Grant date: Jun 5, 1990
• Expiry date: Sep 23, 2008

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P25/02
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

An azachroman derivative of the formula ##STR1## wherein Z is PA1 (a) --N.dbd.CH--CH.dbd.CH--, PA1 (b) --CH.dbd.N--CH.dbd.CH--, PA1 (c) --CH.dbd.CH--N.dbd.CH-- or PA1 (d) --CH.dbd.CH--CH.dbd.N--; PA0 R.sup.1 is A, PA0 R.sup.2 is H or A, or PA0 R.sup.1 and R.sup.2 together are alkylene with 3-6 C atoms; PA0 R.sup.3 is OH or OAc, PA0 R.sup.4 is H, or PA0 R.sup.3 and R.sup.4 together are a bond; PA0 R.sup.5 is 1H-2-pyridon-1-yl, 1H-6-pyridazinon-1-yl, 1H-2-pyrimidinon-1-yl, 1H-6-pyrimidinon-1-yl, 1H-2-pyrazinon-1-yl or 1H-2-thiopyridon-1-yl, or 1H-2-pyridon-1-yl, 1H-6-pyridazinon-1-yl, 1H-2-pyrimidinon-1-yl, 1H-6-pyrimidinon-1-yl, 1H-2-pyrazinon-1-yl or 1H-2-thiopyridon-1-yl mono- or disubstituted by A, F, Cl, Br, I, OH, OA, OAc, NO.sub.2, NH.sub.2, AcNH, HOOC or AOOC; PA0 A is C.sub.1-6 -alkyl and PA0 Ac is C.sub.1-18 -alkanoyl or C.sub.7-11 -aroyl; or a pharmaceutically acceptable salt thereof is claimed. This compound exhibits vasodilatory and anti-hypertensive effects and is suitable for the treatment of alopecia.