New Patents iii

4695567

PYRROLOBENZIMIDAZOLES, PHARMACEUTICAL

COMPOSITIONS CONTAINING THEM AND METHOD OF USING

THEM TO TREAT CERTAIN HEART AND CIRCULATORY

DISEASES

Alfred Mertens, Jens-Peter Holck, Herbert Ber- ger, Bernd Muller-Beckmann, Klaus Strein, Egon Roesch, Schriesheim, Federal Republic Of Germany assigned to Boehringer Mannheim GmbH

treating heart or circulatory diseases, especially those which respond to a change of blood pre- ssure, an increase in cardiac output and/or a change in micro-circulation.

4696815

ANTI-DIABETIC PHARMACEUTICAL FORMS AND

THE PREPARATION THEREOF

Gottfried Schepky, Rolf Brickl, Eckhard Rup- precht, Andreas Greischel, Biberach 1, Federal Republic Of Germany

The present invention provided pyrroloben- zimidazoles or tautomer thereof, of the general formula: See Patent for Chemical Structure (I) wherein R1 is hydrogen, C1£14 C + H D 6 + L alkyl, C + H D 2 + L + 14 C + H D 6 + L alkenyl or C + H D 3 + L + 14 C + H D 7 + L cycloalkyl; + RE + P0 R + HD 2 + L is hydrogen, cyano, C + H D I + L + 1 4 C + H D 6 +LalkyI, C + H D 2 + L + 14 C + H D 6 + L alkenyl, or a carbonyl group substituted by hydroxyl, C + H D I + L +14 C + H D 6 + L alkyl, C + H D I + L +14 C + HD 6 + L alkyoxy, amino, C + HD 1 + L 1. 14 C ÷ H D 6 ÷ L alkylamino, C + H D 2 ÷ L + 14 C + HD 12 + L dialkylamino or hydrazino, or + R E ÷ P O R + H D 2 ÷ L a n d R ÷ H D 1 ÷ L together with the carbon to which they are at- tached form a C ÷ H D 3 ÷ L .1. 14 C ÷ H D 8 ÷ L spirocycloalkyl ring, or R + H D 1 ÷ L and R + HD 2 + L together form C + HD 3 + L .1. 14 C + H D 7 + L alkylidene or C ÷ H D 3 + L + 14 C + HD 7 + L cycloalkylkidene, .1. RE + P0 X is a valency bond, C ÷ H D I ÷ L -t-14 C ÷ H D 4 1. L alkylene or vinylene and .1. RE.1. P0 T is ox- ygen or sulphur; + RE.1. PS and Het is furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, ox- azolyl, thiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, pyrazinyl, pyrimidinyl or pyridazinyl wherein the heterocyclic +PG,2 five- and six-membered rings are unsubstituted or substituted by one or more C.1. HD 1.1. L + 14 C + H D 6 + L alkyl, C + H D 1 + L .1. 14 C ÷ H D 6 + L alkoxy, C + H D I ÷ L -t-14 C ÷ H D 6 + L alkylthio, hydroxyl, oxo, nitro, amino, halo, car- boxyl, C + HD 2 + L + 14 C + HD 7 + L alkoxy- carbonyl, aminocarbonyl or cyano groups; or a physiologically acceptable salt thereof with an inorganic or organic acid. These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation logically acceptable sa It thereof with an inorganic or or- ganic acid. These compounds are useful for

The invention is directed to novel galenic pre- paration forms for providing an oral anti- diabetic agent having an improved release of active substance and processes for producing these preparation forms. The novel pharma- ceutical compositions are characterized in that the onset of the activity and the duration of ac- tivity are adapted to the particular needs of diabetics with regard to proper control of the metabolism and the associated proper release of insulin, A basic or acidic excipient in a solvent is added to the anti-diabetic active substance in a quantity such that the active substance is made soluble, and then a solubilizing agent is added. Polyvinyl pyrrolidone is dissolved as carrier in this solution, but the carrier may simultaneously serve as the solubilizing adjuvant. This solution is further processed with other excipients to form corresponding preparation forms.

4696920

CERTAIN 2-SUBSTITUTED 1,3-

PROPYLIDENEDIPHOSPHONATE DERIVATIVES,

PHARMACEUTICAL COMPOSITIONS CONTAINING

THEM AND THEIR USE AS ANTIHYPERTENSIVE AGENTS

Craig L Bentzen, Yves Guyon-Gellin, Kyriaco Kalathakis, Hieu T Phan, Mong Lcir/a/ Nguyen, Eric Niesor, Jean-Robert Rossier, Chavannes de bogis, Switzerland assigned to Symphar S A

2-Substituted- 1,3-propylidenediphosphonates of formula (I), where A, R1 and R2 are defined in claim 1, are therapeutically active compounds, namely for the treatment of cardiovascular dis-