Abbott Laboratories Corporation

David Lyon Garmaise

Raj Nandan Prasad

Daniel Tim-Wo Chu

Gerard Yvon Paris

Denis G Cimon

Gerald Y Paris

Triglycerides carrying an anti-bacterial drug moiety in the 2-position and a hydrocarbon acyl moiety in the 1- and 3-positions exhibit excellent anti-bacterial properties without causing the side effects often associated with oral antibiotics when used by themselves.

Glycerides with antibacterial properties

A specific anilino derivative of chelocardin having high antibiotic activity is described. This new derivative shows unusually low toxicity and consequently a very high therapeutic index as chemotherapeutic agent against gram-negative organisms.

3,4-Dimethyl-5-isoxazolylsulfamylaniline

Triglycerides carrying the anti-inflammatory drug moiety in the 2-position and hydrocarbon acyl moieties in the 1- and 3-position exhibit excellent anti-inflammatory properties without causing the side effects often associated with the anti-inflammatory drug itself.

Glycerides with anti-inflammatory properties

Esters of 1,N.sup.6 -etheno-5'-adenosine carboxylic acid represented by the formula ##SPC1## Wherein R.sub.1 is loweralkyl, loweralkenyl, loweralkynyl or cycloalkyl; and R.sub.2 and R.sub.3 each are hydrogen or acyl, or R.sub.2 and R.sub. 3 taken together form an isopropylidene or benzylidene moiety; and the pharmaceutically acceptable acid addition salts thereof. The compounds wherein R.sub.2 and R.sub.3 are hydrogen are useful in treating cardiovascular disorders and are particularly useful as anti-anginal and anti-hypertensive agents. Compounds wherein R.sub.2 and R.sub.3 are acyl or when taken together form an isopropylidene or benzylidene moiety are intermediates useful in the preparation of the final products. (R.sub.2 and R.sub.3 = hydrogen). The final products are also useful as intermediates for preparing pharmaceutically active compounds, and, more specifically, for preparing the corresponding 1,N.sup.6 -etheno-5'-adenosine carboxamides.

1,N.sup.6 -etheno-5'-adenosine carboxylates for increasing coronary

A number of specific anilino derivatives of chelocardin having high antibiotic activity are described. These new derivatives show unusually low toxicity and consequently a very high therapeutic index as chemotherapeutic agents against gram-negative organisms.

Anilino derivatives of chelocardin

Amides of 1,N.sup.6 -Etheno-5'-adensine carboxylic acid represented by the formula ##SPC1## Wherein R.sub.1 and R.sub.2 each are hydrogen, loweralkyl, loweralkenyl, loweralkynyl or cycloalkyl, and R.sub.3 and R.sub.4 each are hydrogen, acyl, or R.sub.3 and R.sub.4 taken together form an isopropylidene or benzylidene moiety; and the pharmaceutically acceptable acid addition salts thereof. The compounds wherein R.sub.3 and R.sub.4 are hydrogen are useful in treating cardiovascular disorders and are particularly useful as anti-anginal and anti-hypertensive agents. Compounds wherein R.sub.3 and R.sub.4 are acyl or when taken together form an isopropylidene or benzylidene moiety are intermediates useful in the preparation of the final products. (R.sub.3 and R.sub.4 = hydrogen).

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Montreal, Canada

David Lyon Garmaise