New Patents xiii

4977151

ETHANONE OXIMES AND PHARMACEUTICAL

COMPOSITIONS THEREOF

Shinichiro Fujimori, Satoshi Yamazaki, Mamoru Sugano, Makoto Kawamura, Kunihiro Ninomiya, Akihiro Tobe, Issei Nitta, Yokohama, Japan assigned to Mitsubishi Kasei Corporation

Ethanone oximes represented by the following general formula: See Patent for Chemical Struc- ture (I) wherein R1 represents a cycloalkyl group, aryl group, aralkyl group, aryloxy group, aralkyloxy group, arylthio group or aryl sulfonyl group, those groups being optionally substituted with a substituent selected from an alkyl group having 1 to 3 carbon atoms, an alkoxy group having 1 to 3 carbon atoms and a halogen atom, piperidino group, piperazino group, 4-alkyl sub- stituted piperazino group, imidazolyl group 4- alkyl substituted imidazolyl group or substituted amino group, R2 represents a hydrogen atom or an alkoxy group having 1 to 3 carbon atoms, and R3 represents a piperidino group, piperazino group or 4-alkyl substituted piperazino group, or R1 and R2 together with a phenyl group to which they are attached may form a phenothiazin-2-yl group, N-acetyl- phenothiazin-2-yl group, thianthren-2-yl group, dibenzothiophen-3-yl group, dibenzofuran-3-yl group or a group of the formula: See Patent for Chemical Structure wherein R4 represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, or a pharmaceutically acceptable acid addition salts thereof are disclosed. They are a potent antiulcer agent.

4977153

3-AMINOPROPYLOXYPHENYL DERIVATIVES,

PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND METHOD FOR THE

THERAPY OF DISEASES

William J Louis, Richard Berthold, Max-Peter Seiler, Andre Stoll, Rosanna, Victoria, 3084, Australia assigned to Louis William J

Compounds of formula (I), See Patent for Chemical Structure (I) characterized in that R signifies optionally substituted heteroaryl-, heteroarylakyl or heteroarylalkenyl, R I signifies

hydrogen or a substituent, R2 is hydroxy or a group -z-(CH2)n-Y-R3 wherein R3 is hydrogen, alkyl, hydroxyalkyl, alkenyl, cycloalkyl, cyclo- alkylalkylene, hydroxy substituted cycloalkyl or cycloalkylalkylene, or optionally substituted aryl or aralkyl or aralkenyl moiety, and Y signifies oxygen or sulfur, and either Z is an oxy- gen atom and n is 2 or 3, or Z is a bond and n is 1, 2 or 3, A signifies alkylene or branched alkylene of 2 to 5 carbon atoms, W signifies a bond or im- ino, and X signifies a bond or imino, and their physiologically hydrolyzable derivatives, in which at least one hydroxy group is in esterified form. The compounds exhibit beta adrenoceptor blocking activity. Processes for the preparation of the compounds are also disclosed.

4977163

AMINOCYCLOPENTANOL ACIDS AND ESTERS AND THEIR

PREPARATION AND PHARMACEUTICAL

FORMULATION

Eric Collington, Peter Hallett, Christopher Wal- lis, Alan Wadsworth, Norman F Hayes, Welwyn, United Kingdom assigned to Glaxo Group Limited

Compounds are described of the formula See Patent for Chemical Structure in which Rl is H, C1-6 alkyl or C7-10 aralkyl; W is C1-7 alkylene; X is cis or trans -CH double bondCH- or - CH2CH2-; n is 1 or 2; Y is a saturated hetero- cyclic amino group having 5-8 ring members; R2 is (i) substituted or unsubstituted phenylalkyl, thienylalkyl or naphthylalkyl or (ii) substituted or unsubstituted cinnamyl; and their salts and solvates. These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and antiasthmatic agents.

4977166

BENZOPYRAN DERIVATIVES AND PHARMACEUTICAL

COMPOSITIONS CONTAINING THEM

Jean-Claud Hardy, Christia Renault, Cergy, France assigned to Rhone-Poulenc Sante

New benzopyran derivatives of formula: See Pa- tent for Chemical Structure (I) in which RI is