G.d. Searle & Company

International Plant Research Institute, Inc.

Other

Raphael Pappo

Paul Waddell Collins

Robert J Chorvat

Robert B Garland

Mildred S Bruhn

Leonard N Nysted

Christopher Jung

Arthur M Nonomura

Kenneth M Otteson

Martin A Apple

Paul B Sollman

Herschel S Zackheim

Rothwell Polk

The present invention relates to 5-fluoro-PGI.sub.2 derivatives of Formula I. These compounds are useful for the treatment of platelet dysfunction. Also disclosed is the process for preparing them and the appropriate intermediates.

5-fluoro-PGI.sub.2 compounds

5 Fluoro PGI compounds

A water extract of homogenized Cryptosiphonia woodii is useful for the treatment of herpes simplex viral infections. The active agent in the extract is a polysaccharide containing glucose and galactose. Herpes infections may be treated in subjects, e.g. human patients, by administering to the subject an effective amount of an aqueous extract of C. woodii, particularly a water extract. This treatment method is effective for treating subjects both prior to and subsequent to infection. It may involve topical application to alleviate symptoms associated with herpes infections or desirably may be systemic, e.g. by oral administration, to eradicate the virus and thereby prevent symptom recurrence.

Composition of matter from Cryptosiphonia woodii useful for the

A composition useful for relieving the symptoms of psoriasis in humans are disclosed. The composition is an N-trialkylsilyl-substituted 6-aminonicotinamide. The composition is applied in a suitable pharmaceutical base, such as a cream or ointment, to the affected area of skin.

Trialkylsilyl-6-aminonicotinamides

The use of a composition for relieving the symptoms of psoriasis in humans is disclosed. The composition is an N-trialkylsilyl-substituted 6-aminonicotinamide. The composition is applied in a suitable pharmaceutical base, such as a cream or ointment, to the affected area of skin.

Use of trialkylsilyl-6-aminonicotinamides for the treatment of psoriasis

11-Amino-11-deoxydaunorubicin and analogs represented by the formula: ##STR1## wherein: R is hydrogen, hydroxy or methoxy; R.sub.1 is hydrogen or hydroxy; and the pharmaceutically acceptable salts thereof. The compounds are useful in ameliorating tumor growth.

11-Amino-11-deoxydaunorubicin and analogs

A compound of the formula ##STR1## wherein R is hydrogen or lower alkyl having 1-7 carbon atoms; R', R', and R'' are each individually hydrogen or methyl; n is 0-3; and Ar is phenyl, halosubstituted phenyl, lower alkyl substituted phenyl wherein the lower alkyl contains 1-4 carbon atoms, lower alkoxy substituted phenyl wherein the lower alkoxy contains 1-4 carbon atoms, p-biphenyl, or trifluoromethyl substituted phenyl. Compounds of the present invention are useful as antifertility agents.

Prostaglandin derivatives having aryl, hydroxyl, and alkynyl functions

4,5-Unsaturated 16-hydroxy prostanoic acid derivatives displaying valuable pharmacological properties, e.g. gastric antisecretory, are described herein.

4,5-Unsaturated prostanoic acid derivatives

The present invention relates to bis(4-demethoxydaunorubicin)dihydrazone of the formula ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen or alkyl having from 1 to 4 carbon atoms and X represents

Bis(4-demethoxydaunorubicin)dihydrazone derivatives and

2,3,5-Trisubstituted cyclopentanealkenoic acids display anti-microbial activity, e.g. anti-bacterial and anti-fungal, and are, in addition, useful as intermediates in the manufacture of prostanoic acid derivatives.

2,3,5-Trisubstituted cyclopentanealkenoic acids, derivatives thereof and

The present invention encompasses novel intermediates having the following structural formulas: ##STR1## wherein X is hydrogen, methoxy, or hydroxy; ##STR2## wherein X is hydrogen, methoxy, or hydroxy; and ##STR3## wherein X is hydrogen, methoxy, or hydroxy. Compounds of the present invention are useful in synthesizing 4-demethoxydaunorubicin, daunorubicin, adriamycin, and carminomycin which are potent antitumor agents.

Intermediates for the synthesis of 4-demethoxydaunorubicin

Compounds of the formula ##STR1## wherein R is phenyl cyclohexyl or lower alkyl containing 1-6 carbon atoms; R' is hydrogen or methyl; R'' is alkenyl or alkynyl having 3-5 carbon atoms; R' is hydrogen, tetrahydrofuran-2-yl tetrahydropyran-2-yl or trialkylsilyl wherein the alkyl contains 1-4 carbon atoms. Compounds of the present invention are useful in synthesizing prostaglandin like molecules which are active anti-secretory agents.

Intermediates for prostaglandin synthesis

The present invention encompasses compounds of the formula: ##STR1## wherein n is 0 or 1; Y represents ethylene or vinylene; R represents hydrogen or lower alkyl having 1-7 carbon atoms; R', R', R'' each individually represent hydrogen or methyl; Ar represents phenyl, halosubstituted phenyl, alkyl substituted phenyl wherein the alkyl contains 1-4 carbon atoms, alkoxy substituted phenyl wherein the alkoxy contains 1-4 carbon atoms, trifluoromethylphenyl, or biphenyl; and the wavy line indicates R or S stereochemistry.

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Skokie, IL, United States of America

Raphael Pappo