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4851423 Pharmaceutically active compounds
ii
New Patents
alkylaminocarbonyl or dialkylaminocarbonyl radical; R2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and sixmembered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R2 is See Patent for Chemical Structure (II) the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. Furthermore, the present invention provides intermediates of the general formula: See Patent for Chemical Structure (VI) in which R1, R2, A and X have the same meanings as above, and processes for the preparation of these intermediates.
4851409 2-SUBSTITUTED QUINOLINE DIOIC ACIDS AND PHARMACEUTICAL COMPOSITIONS Robert N Young, Robert Zamboni, Serge Leger, Senneville, Canada assigned to Merck Frosst Canada Inc Compounds having the formula: See Patent for Chemical Structure See Patent for Tabular Presentation are antagonists of leukotrienes and inhibitors of their biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, antiinflammatory, and cytoprotective agents.
4851420 2,6 D I A M I N O 3 HALOBENZYLPYRIDINES AND PROCESSES FOR T H E I R MANUFACTURE AS WELL AS THEIR USE IN PHARMACEUTICALS Peter Emig, Juergen Engel, Gerhar Scheffler, Carl H Weischer, Bern Nickel, Niederdorfelden, Federal Republic Of Germany assigned to ASTA Pharma Aktiengesellschaft
2,6 diamino 3 halobenzylpyridines of the formula I: See Patent for Chemical Structure wherein RI is fluorine and R2 is hydrogen or chlorine as well as their physiologically acceptable acid addition salts, processes for their manufacture and their use in pharmaceuticals.
4851423 PHARMACEUTICALLY COMPOUNDS
ACTIVE
Viyyoor Girijavallabhan, Ashit K Ganguly, Patrick A Pinto, Richard W Versace assigned to Schering Corporation The disclosed invention is compounds represented by the formula See Patent for Tabular Presentation PS See Patent for Tabular Presentation PS and pharmaceutically acceptable acid addition salts and quarternary amine salts thereof, wherein Z is phenyl, naphthyl or adamantyl; substituted phenyl wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile, nitro, phenylsulfonyl, methylsulfonyl, isoxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, loweralkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl; 5 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen and one carbon in the ring, wherein the substituents are one or more of carboxyl, hydroxymethyl, loweralkyl, loweralkylcarbonyl or aryl lower alkyl; or tertiary butyl; X and Y are each independently a bond, -O-, See Patentfor Chemical Structure See Patent for Tabular Presentation Q is a divalent substituted or unsubstituted straight or branched chain lower alkanediyl, -lower alkanedinyl- cycloalkanediyl- lower alkanediyl-, lower alkendiyl, lower alkynediyl, phenylene, tetrahydrofurandiyl or tetrahydropyrandiyl; W is a monovalent substituted or unsubstituted aromatic heterocyclic single or fused ring containing from 5 to 10 ring atoms, at least one hetero atom of which is a nitrogen atom, wherein the substituents are hydroxy, amino, carbamoyl, carboxyl, nitrile, nitro, oxo, lower alkoxy carbonyl, halogen, sulfamyl, lower alkyl, lower alkylthio, lower alkoxy, hydroxyloweralkyl, lower alkoxycarbonylloweralkyl, amino loweralkyl, carboxyloweralkyl, guanidino, thioureido, lower alkylsulfonylamino, aminocarbonylloweralkyl, allyloxycarbonylmethyl or carbamoyloxylowralkyl; and W' is divalent W. The compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.
New Patents
alkylaminocarbonyl or dialkylaminocarbonyl radical; R2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and sixmembered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R2 is See Patent for Chemical Structure (II) the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. Furthermore, the present invention provides intermediates of the general formula: See Patent for Chemical Structure (VI) in which R1, R2, A and X have the same meanings as above, and processes for the preparation of these intermediates.
4851409 2-SUBSTITUTED QUINOLINE DIOIC ACIDS AND PHARMACEUTICAL COMPOSITIONS Robert N Young, Robert Zamboni, Serge Leger, Senneville, Canada assigned to Merck Frosst Canada Inc Compounds having the formula: See Patent for Chemical Structure See Patent for Tabular Presentation are antagonists of leukotrienes and inhibitors of their biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, antiinflammatory, and cytoprotective agents.
4851420 2,6 D I A M I N O 3 HALOBENZYLPYRIDINES AND PROCESSES FOR T H E I R MANUFACTURE AS WELL AS THEIR USE IN PHARMACEUTICALS Peter Emig, Juergen Engel, Gerhar Scheffler, Carl H Weischer, Bern Nickel, Niederdorfelden, Federal Republic Of Germany assigned to ASTA Pharma Aktiengesellschaft
2,6 diamino 3 halobenzylpyridines of the formula I: See Patent for Chemical Structure wherein RI is fluorine and R2 is hydrogen or chlorine as well as their physiologically acceptable acid addition salts, processes for their manufacture and their use in pharmaceuticals.
4851423 PHARMACEUTICALLY COMPOUNDS
ACTIVE
Viyyoor Girijavallabhan, Ashit K Ganguly, Patrick A Pinto, Richard W Versace assigned to Schering Corporation The disclosed invention is compounds represented by the formula See Patent for Tabular Presentation PS See Patent for Tabular Presentation PS and pharmaceutically acceptable acid addition salts and quarternary amine salts thereof, wherein Z is phenyl, naphthyl or adamantyl; substituted phenyl wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile, nitro, phenylsulfonyl, methylsulfonyl, isoxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, loweralkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl; 5 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen and one carbon in the ring, wherein the substituents are one or more of carboxyl, hydroxymethyl, loweralkyl, loweralkylcarbonyl or aryl lower alkyl; or tertiary butyl; X and Y are each independently a bond, -O-, See Patentfor Chemical Structure See Patent for Tabular Presentation Q is a divalent substituted or unsubstituted straight or branched chain lower alkanediyl, -lower alkanedinyl- cycloalkanediyl- lower alkanediyl-, lower alkendiyl, lower alkynediyl, phenylene, tetrahydrofurandiyl or tetrahydropyrandiyl; W is a monovalent substituted or unsubstituted aromatic heterocyclic single or fused ring containing from 5 to 10 ring atoms, at least one hetero atom of which is a nitrogen atom, wherein the substituents are hydroxy, amino, carbamoyl, carboxyl, nitrile, nitro, oxo, lower alkoxy carbonyl, halogen, sulfamyl, lower alkyl, lower alkylthio, lower alkoxy, hydroxyloweralkyl, lower alkoxycarbonylloweralkyl, amino loweralkyl, carboxyloweralkyl, guanidino, thioureido, lower alkylsulfonylamino, aminocarbonylloweralkyl, allyloxycarbonylmethyl or carbamoyloxylowralkyl; and W' is divalent W. The compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.