American Home Products Corporation

Biochem Pharma Inc.

Biochem Immunosystems Inc.

Iaf Biochem International, Inc.

Gervais Dionne

Leslie G Humber

Andre A Asselin

Nghe Nguyen-Ba

Martial Lacroix

William L Brown

Miguel Quimpere

Amedeo Failli

Clara Revesz

Laval Chan Kong

Maan Zrein

Francesco Bellini

Magid A Abou-Gharbia

Annmarie Louise Sabb

Laval Chan Chun Kong

There is provided cyclic peptides of the general formula

Synthetic peptides and mixtures thereof for detecting HIV antibodies

Nucleotide analogues having the general formula (I) and pharmaceutically acceptable derivatives:

Process for preparing antiviral 2-phosponate nucleotide analogs

Nucleotide analogues having the general formula (I) and pharmaceutically acceptable derivatives: ##STR1## wherein n is 0 or an integer; X is O or S, CH.sub.2, CH--halogen, CH--N.sub.3, or C.dbd.CH.sub.2 ;

Antiviral compounds

Nucleotide analogues having the general formula (I) and pharmaceutically acceptable derivatives: ##STR1## wherein n is 0 or an integer; X is O or S, CH.sub.2, CH-halogen, CH--N.sub.3, or C.dbd.CH.sub.2 ;

The invention relates to 1,3-oxathiolane nucleoside analogues and their use in the treatment of viral infections. More specifically, this invention relates to (-)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidi n-2-one and pharmaceutically acceptable derivatives and pharmaceutical formulations thereof.

1,3-oxathiolane nucleoside analogues and methods for using same

1,3-oxathiolane nucleoside compounds and compositions

Linear and cyclic peptides of the E1 and C protein of the rubella virus are disclosed. These peptides and analogues, are useful in detecting and quantifying antibodies raised against the rubella virus. They are also useful in raising antibodies to the rubella virus for use in the diagnosis of and protection against rubella viral infections.

Peptides and analogues and mixtures thereof for detecting and eliciting

Linear and cyclic peptides of the E1 and C protein of the rubella virus are disclosed. These peptides and analogues, mixtures and combinations of them are useful in detecting and quantifying antibodies raised against the rubella virus. They are also useful in raising antibodies to the rubella virus for use in the diagnosis of and protection against rubella viral infections.

The compound of the formula: ##STR1## in which R.sup.1 is hydrogen, alkoxy, cyano, halo, nitro, amino, or mono- or dialkylamino; R.sup.2 is hydrogen, alkyl, phenyl, benzyl, 2-thienyl, 3-thienyl or 2-,3- or 4-pyridinyl; R.sup.3 is hydrogen, alkyl or phenyl; R.sup.4 is N-methyl-pyrrolidin-2yl, 2-, 3- or 4-pyridinyl, 3-quinuclidinyl or ##STR2## where n is 1 to 5; m is 0 to 3; and R.sup.8 is hydrogen or alkyl of 1 to 6 carbon atoms; or R.sup.4 is ##STR3## wherein: (a) n is 2, R.sup.5 taken with R.sup.3 is ethylene and R.sup.6 is --CHO, alkyl, unsubstituted or substituted phenyl, pyrimidinyl, pyridinyl, or pyrazinyl, where the substituents are alkyl, alkoxyl, halo, cyano, nitro or trifluoromethyl; (b) n is 1 to 5, and R.sup.5 and R.sup.6 taken together are polymethylene which may be alkyl substituted or R.sup.5 nd R.sup.6 are morpholino, 3-azabicyclo[3.2.2]nonan-3-yl, pyrrol-1-yl, pyrrolidin-2-on-1-ytl, pyrrolidin-2-thion-1-yl, imidazol-1-yl, alkyl-piperidin-1-yl or a piperazin-1-yl moiety in the 4-position of which is hydrogen, --CHO, alkyl or unsubstituted or substituted phenyl, pyrimidinyl, pyridinyl, or pyrazinyl, alkoxy, halo, cyano, nitro or trifluoromethyl; or (c) n is 1 to 5, and R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, phenyl, 3-quinuclidinyl, 2-adamantyl, bicyclo[3.2.1]octan-1-yl, bicyclo[3.3.1]nonan-9-yl or 2-,3- or 4- pyridinyl; or a pharmaceutically acceptable salt thereof are M.sub.1 receptor agonists useful in treatment of dementias involving the cholinergic system. dd

Pyridazino(4,5-b)indolizines

Indole derivatives characterized by having a 1,2,3,4-tetrahydrocarbazole or 1,2,3,4-tetrahydrocyclopent[b]indole nucleus with a hydroxyalkanamine substituent are disclosed. The nucleus is optionally further substituted at various positions. The derivatives are useful diuretic agents, and methods for the preparation and use are also disclosed.

Hydroxyalkanamide tetrahydrocarbazoles

Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole or 1,3,4,9-tetrahydrothiopyrano[3,4-b]indole nucleus with a hydroxyalkanamine or lower alkoxyalkanamine substituent and a lower alkyl group at position 1 are disclosed. The nucelus is optionally further substituted at position 9 and on the aromatic ring. The derivatives are useful diuretic agents, and methods for their preparation and use are also disclosed.

Tricyclic indole derivatives

Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano-[3,4-b]indole or 1,3,4,9-tetrahydrothiopyrano[3,4-b]indole nucleus with a hydroxyalkanamine or lower alkoxyalkanamine substituent and a lower alkyl group at position 1 are disclosed. The nucleus is optionally further substituted at position 9 and on the aromatic ring. The derivatives are useful diuretic agents, and methods for their preparation and use are also disclosed.

1-Hydroxyalkanamine pyrano(3,4-b)indole compositions and use thereof

Indole derivatives characterized by having a 1,2,3,4-tetrahydrocarbazole or 1,2,3,4-tetrahydrocyclopent[b]indole nucleus with a hydroxyalkanamine substituent are disclosed. The nucleus is optionally further substituted at various positions. The derivatives are useful diuretic agents, and methods for their preparation and use are also disclosed.

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St-Laurent, Canada

Gervais Dionne