Treatment of ulcerative colitis and Crohn's disease - by admin. of 9-amino-pyridazino:pyrrolo:isoquinoline derivs. which act as vaso-spasmolytic endothelin antagonists

• Main Authors: ROOS, OTTO. DR., 6501 SCHWABENHEIM, DE, ARNDTS, DIETRICH., 6531 APPENHEIM, DE, LOESEL, WALTER. DR., 6535 GAU-ALGESHEIM, DE
• Format: Patent
• Language: English; German
• Published: 23.12.1993
• Edition: 5
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

Treating ulcerative colitis and Crohn's disease comprises admin. of a 9-amino-pyridazino(4',5':3,4)pyrrolo(2,1-a) isoquinoline deriv. (I) or an addn., base or complex salt. R1 is H, 3-7C cycloalkyl, 2-5C alkenyl; PH1; propargyl; or 1-5C alkyl opt. subtd. by OH, 1-4C alkoxy, halo, NH2, mono- or di- 1-2C alkylamino, 2-4C acylamino, 3-7C cycloalkyl, Ph2, furyl, thienyl or a N-contg. 5- or 6-membered ring opt. contg. an O or S atom and opt. subtd. by 1-4C alkyl; R2 is R1 or, where R1 is H, R2 is NH2; di(1-2C alkylamino; acetonylamno; 2-3C acylamino, 1-3C alkylsulphonyl; 1-3C alkoxy-carbonyl; isopropylideneamino or a 5- or 6-membered N-contg. ring opt. contg. a further N atom or an O or S atom; or NR1R2 forms a 3-7 membered ring opt. contg. an O or S atom and opt. substd. by Ph1-1-4C alkyl; Ph1 is phenyl opt. mono- or di-substd. by halo or OMe; Ph2 is phenyl opt. substd. with 1 or more halo, 1-2C alkyl, 1-2C alkoxy, mono- or di- 1-2C alkylamino, NH2, 2-3C acyalmino or alkylsulphonylamino; R3-R5 are H or 1-4C alkyl; R6, R9 are H; OH; 1-4C alkoxy; 1-4C alkylthio; or -NR10R11; R7, R8 are OH; 1-4C alkoxy; or 1-4C alkylthio; R10 is H or 1-4C alkyl; R11 is H or 1-4C alkyl opt. subtd. by OH, OMe or furfuryl. Cpds. (I) are known from DE 3500941 and DE 3525048. They are also described in EP -252299. USE - Cpds. (I) act as vasospasmolyitc endothielin antagonists which block non-selective cation channels. Admin. of cpds. (I) is in conventional formulations at doses of 0.1-500 mg p.o. and 0.05-150 mg i.v.