4859701 Azulene derivatives and pharmaceutical compositions containing them

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Gen. Pharmac. Vol. 21, No. 3, pp. i-xii, 1990 Pergamon Press plc. Printed in Great Britain NEW PATENTS This Section contains abstracts and, where appropriate, illustrations of recently issued United States patents and published patent applications filed from over 30 countries under the Patent Cooperation Treaty. This information was obtained from recent additions to the Pergamon PATSEARCH ~ online database in accordance with interest profiles developed by the Editors. Further information about Pergamon PATSEARCH ~ can be obtained from Pergamon Orbit InfoLine Inc., 8000 Westpark Drive, McLean, Virginia 22102 U.S.A. Copies of complete patents announced in this Section are available from Pergamon Orbit InfoLine Inc. for $8 per copy. Payment with order is required. Orders outside North America add $2 for air postage. Order by patent number for Pergamon Orbit InfoLine only. 4859664 DERIVATIVES OF 2,3,4,5,6,7- HEXAHYDRO-2 7-METHANO-I 5-BENZOXAZONINES AND -1,4-BENZOXAZONINES, PROCESSES FOR THEIR PRODUCTION AND THEIR USE AS PHARMACEUTICALS Friedrich Eiden, Peter Gmeiner, Jurgen Schunemann, Gr Federal Republic Of Germana assigned to Madaus GmbH & Company New 2,3,4,5,6,7-hexahydro-2 7-methano-1 5- benzoxazonine and -1, 4-benzoxazonine com- pounds of the formula See Patent for Chemical Structure have useful pharmaceutical properites. They are prepared from ketones of the formula See Patent for Chemical Structure via a lactone intermediate. In the formula, the various R sub- stitutes are generally hydrogen or alkyl, with R4 also being halogen or alkoxy and R3R3' also being phenyl. R1 may be joined with R5/R5' in a 5- to 7-membered ring possibly interrupted by O, S, SO2 or amino. One of X and Y is CH2; the other is amino. The starting ketones also have pharmaceutical properties. The lactone inter- mediates are new compounds. 4859667 PHARMACEUTICAL COMPOSITIONS OF PHENOTHIAZONE DERIVATIVES AND ANALOGS Cheuk K Lau, Christiane Yoakim, Joshua Rokach, Rejean Fortin, Yvan Guindon, Pier- refonds, Canada assigned to Merck Frosst Canada Inc Phenothiazone derivatives and analogs thereof, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are use- ful therapeutic agents for treating allergic condi- tions, asthma, cardiovascular disorders and inflammation. 4859683 CERTAIN BENZOXEPINS AND THEIR PHARMACEUTICAL COMPOSITIONS AND METHODS Raymond Youssefyeh, Scott I Klein, Henry F Campbell, Donald Kuhla assigned to Rorer Pharmaceutical Corporation Certain specific substituted 9-N-(1-azabicyclo 3.3.1. nonan-4-yl)carboxamido-2,3,4, 5- tetrahydro-1-benzoxepins and their valuable use as 5-HT3 antagonists having CNS and gastric prokinetic activity and void of any significant D2 receptor binding properties are disclosed. Methods for their preparation also are described. 4859692 HETEROCYCLIC AMIDE DERIVATIVES AND PHARMACEUTICAL USE Peter Bernstein, Frederick Brown, Victor Matassa, Ying Kwong Yee assigned to ICI Americas Inc The invention concerns novel, pharmaceutically useful, amide derivatives of certain ben- zoheterocyclylalkanoic acids (and related tetra-

Transcript of 4859701 Azulene derivatives and pharmaceutical compositions containing them

Gen. Pharmac. Vol. 21, No. 3, pp. i-xii, 1990 Pergamon Press plc. Printed in Great Britain

NEW PATENTS

This Section contains abstracts and, where appropriate, illustrations of recently issued United States patents and published patent applications filed from over 30 countries under the Patent Cooperation Treaty. This information was obtained from recent additions to the Pergamon PATSEARCH ~ online database in accordance with interest profiles developed by the Editors. Further information about Pergamon PATSEARCH ~ can be obtained from Pergamon Orbit InfoLine Inc., 8000 Westpark Drive, McLean, Virginia 22102 U.S.A.

Copies of complete patents announced in this Section are available from Pergamon Orbit InfoLine Inc. for $8 per copy. Payment with order is required. Orders outside North America add $2 for air postage. Order by patent number for Pergamon Orbit InfoLine only.

4859664

DERIVATIVES OF 2,3,4,5,6,7- HEXAHYDRO-2 7-METHANO-I

5-BENZOXAZONINES AND -1,4-BENZOXAZONINES, PROCESSES FOR THEIR

PRODUCTION AND THEIR USE AS PHARMACEUTICALS

Friedrich Eiden, Peter Gmeiner, Jurgen Schunemann, Gr Federal Republic Of Germana assigned to Madaus GmbH & Company

New 2,3,4,5,6,7-hexahydro-2 7-methano-1 5- benzoxazonine and -1, 4-benzoxazonine com- pounds of the formula See Patent for Chemical Structure have useful pharmaceutical properites. They are prepared from ketones of the formula See Patent for Chemical Structure via a lactone intermediate. In the formula, the various R sub- stitutes are generally hydrogen or alkyl, with R4 also being halogen or alkoxy and R3R3' also being phenyl. R1 may be joined with R5/R5' in a 5- to 7-membered ring possibly interrupted by O, S, SO2 or amino. One of X and Y is CH2; the other is amino. The starting ketones also have pharmaceutical properties. The lactone inter- mediates are new compounds.

4859667

PHARMACEUTICAL COMPOSITIONS OF

PHENOTHIAZONE DERIVATIVES AND ANALOGS

Cheuk K Lau, Christiane Yoakim, Joshua Rokach, Rejean Fortin, Yvan Guindon, Pier- refonds, Canada assigned to Merck Frosst Canada Inc

Phenothiazone derivatives and analogs thereof, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are use- ful therapeutic agents for treating allergic condi- tions, asthma, cardiovascular disorders and inflammation.

4859683

CERTAIN BENZOXEPINS AND THEIR PHARMACEUTICAL

COMPOSITIONS AND METHODS

Raymond Youssefyeh, Scott I Klein, Henry F Campbell, Donald Kuhla assigned to Rorer Pharmaceutical Corporation

Certain specific substituted 9-N-(1-azabicyclo 3.3.1. nonan-4-yl)carboxamido-2,3,4, 5- tetrahydro-1-benzoxepins and their valuable use as 5-HT3 antagonists having CNS and gastric prokinetic activity and void of any significant D2 receptor binding properties are disclosed. Methods for their preparation also are described.

4859692

HETEROCYCLIC AMIDE DERIVATIVES AND

PHARMACEUTICAL USE

Peter Bernstein, Frederick Brown, Victor Matassa, Ying Kwong Yee assigned to ICI Americas Inc

The invention concerns novel, pharmaceutically useful, amide derivatives of certain ben- zoheterocyclylalkanoic acids (and related tetra-