Ciba-geigy Corporation

John E Francis

Alan J Hutchison

Charles F Huebner

Karl O Gelotte

Wilhelm Kump

Benjamin B Mugrage

Siem J Veenstra

Jen Chen

Roger A Fujimoto

Christian Borel

The invention relates to novel acyl derivatives of rifamycins of the formula ##STR1## and the salts thereof, in which the structural elements --A.sub.1 --A.sub.2 --, --A.sub.3 --A.sub.4 -- and --A.sub.5 --A.sub.6 -- each denote ethylene or vinylene or the elements --A.sub.1 --A.sub.2 -- and --A.sub.3 --A.sub.4 -- each denote ethylene and --A.sub.5 --A.sub.6 -- denotes vinylene; X represents &gt;C(R.sub.6)-- or &gt;N-- and R.sub.6 denotes hydrogen or alkyl; alk denotes an aliphatic hydrocarbon radical; R.sub.1 denotes hydrogen or acyl; R.sub.2 denotes acyl, or alkyl which is optionally substituted by an aromatic radical, and R.sub.3 and R.sub.3 ' represent a common bond, or R.sub.3 denotes hydrogen or acyl, and R.sub.3 ' is hydrogen; R.sub.4 denotes hydrogen, cycloalkyl or aryl; R.sub.5 denotes hydrogen or acetyl; R.sub.7 denotes hydrogen or alkyl, which can be used as active compounds in medicaments, the preparation and use thereof, and pharmaceutical products and the preparation thereof.

Acyl derivatives of oxazolorifamycins

Disclosed are 2-substituted adenosine derivatives of the formula ##STR1## in which R represents a substituted amino grouping of the formula ##STR2## as defined herein; pharmaceutically acceptable ester derivatives thereof in which free hydroxy groups are esterified in the form of a pharmaceutically acceptable prodrug ester; and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for their preparation; and their use in mammals as therapeutically effective adenosine-2 (A-2) agonists.

2-(substituted amino) adenosines as antihypertensives

Disclosed are the compounds of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl or aryl-lower alkyl; R.sub.1 represents hydrogen, lower alkyl, C.sub.3 -C.sub.7 -alkenyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, or optionally lower alkyl substituted (C.sub.3 -C.sub.7 -cycloalkyl, bicycloheptyl, bicycloheptenyl, adamantyl, tetrahydropyranyl or tetrahydrothiopyranyl)-lower alkyl, or diaryl-lower alkyl; R.sub.2 represents hydrogen or lower alkyl; R.sub.3 represents hydroxymethyl or --CONHR.sub.4 in which R.sub.4 represents hydrogen, lower alkyl, aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl or hydroxy-lower alkyl; pharmaceutically acceptable ester derivatives thereof in which one or more of the hydroxy groups are esterified in form of a pharmaceutically acceptable ester; and pharmaceutically acceptable salts thereof; methods of preparation; pharmaceutical compositions; and their use as adenosine-2 agonists in mammals.

Imidazo[4,5-b]pyridine derivatives as cardiovascular agents

Compounds of the formula ##STR1## wherein each R is hydrogen or one R is hydrogen and the other is lower alkyl, R.sub.1 is hydrogen, lower alkyl, aryl, aralkyl or lower carboalkoxy, R.sub.2 is hydrogen or lower alkyl, and the ring A is unsubstituted or substituted by lower alkyl, lower alkoxy, halo or trifluoromethyl, and pharmaceutically acceptable salts thereof, their preparation, pharmaceutical compositions and the uses thereof, such as .alpha..sub.2 -adrenergic blocking agents, e.g. antidepressants, cognition enhancers and appetite supressants, and as intraocular pressure reducing agents are disclosed.

2,3-dihydro-2-(4,5-dihydroimidazol-2-yl)-indoles for reducing

Compounds of the formula ##STR1## wherein each R is hydrogen or one R is hydrogen and the other is lower alkyl, R.sub.1 is hydrogen, lower alkyl, aryl, aralkyl or lower carboalkoxy, R.sub.2 is hydrogen or lower alkyl, and the ring A is unsubstituted or substituted by lower alkyl, lower alkoxy, halo or trifluoromethyl, and pharmaceutically acceptable salts thereof, their preparation, pharmaceutical compositions and the uses thereof, such as .alpha..sub.2 -adrenergic blocking agents, e.g. antidepressants, cognition enhancers and appetite suppressants, and as intraocular pressure reducing agents are disclosed.

2,3-dihydro-2-(4,5-dihydroimidazol-2-yl)-indoles in composition form for

Compounds of the formula ##STR1## wherein R.sub.1 is optionally substituted phenyl, pyridyl, thienyl, furyl, pyrrolyl, thiazolyl, or ribofuranosyl; X is oxygen, NR, or sulfur; R is hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; and ring A is (a) an optionally substituted 5-8 membered monocycloalken-1,2-diyl; (b) an optionally substituted carbobicyclic ring of the formula ##STR2## wherein n and m are each independently one or two; or (c) an optionally substituted 5-6 membered heterocycle having one or two heteroatoms, the atoms of which are selected from carbon, oxygen, nitrogen, and sulfur. Also disclosed are tautomers of the above and pharmaceutically acceptable salts; compositions thereof; and methods of using the compounds, tautomer, or salts.

2-substituted-e-fused-[1,2,4]triazolo[1,5-c]pyrimidines, pharmaceutical

[1,2,4]triazolo[1,5-c]quinazoline compounds of the formula ##STR1## wherein R.sub.1 is optionally substituted phenyl, pyridyl, furyl thienyl, dihydro or tetrahydro furanyl or thienyl, pyranyl, or 0-ribofuranosyl; R.sub.2 is hydrogen or lower alkyl; X is oxygen or NR.sub.3, R.sub.3 is as defined in the claims, and ring A is unsubstituted or substituted as set forth in the claims. The compounds wherein X is N--R.sub.3 are especially useful as adenosine antagonists and for the treatment of asthma. The compounds wherein X is oxygen are useful as benzodiazepine antagonists and as intermediates in the synthesis of the compounds wherein X is N--R.sub.3.

Triazoloquinazoline compounds, and their methods of preparation,

1-(Aralkoxyphenyl)-2 or 3-(bis-arylalkylamino)-alkanes, e.g. those of the formula: ##STR1## or therapeutically acceptable salts thereof are hypotensive and cardioactive agents.

1-(Aralkoxyphenyl)-2-(bis-arylalkylamino)-alkanes

New 1-(azacyclic aralkoxyphenyl)-2 or 3-(diphenylalkylamino)-alkanes, e.g. those of the formula ##STR1## Py=pyridyl unsubst. or subst. by 1-2 alkyl, alkoxy, F or Cl; Ph=phenyl unsubst. or subst. as Py or by CF.sub.3

Bis-arylalkylamino-aralkanes

New 1-(azacyclic aralkoxyphenyl)-2- or 3-(diphenylalkylamino)-alkanes, e.g those of the formula: ##STR1## R = 5- or 6-membered, mono- or bicyclic, nitrogen-containing aromatic radical

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Basking Ridge, NJ, United States of America

John E Francis