1
iv New Patents A compound of the general formula I; See Pa- tent for Chemical Structure (I) in which R is hydrogen or a halogen or an alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, carboxy, alkylsulphinyl, alkylsulphonyl, sulphamido, alkylsulphamido, dialkylsulphamido, car- bamoyl, alkylcarbamoyl, dialkylcarbamoyl, phenylcarbamoyl, diphenylcarbamoyl, pyridyl- carbamoyl, dipyridylcarbamoyl, benzyl, alkyl- carbonyl, benzoyl, alkyloxycarbonyl, phenoxycarbonyl, alkylcarbonyloxy, ben- zoyloxy, alkylcarbonylamino, benzamido, phenyl, phenoxy or phenylthio group, X is oxy- gen or sulphur or an imino, alkylimino, phenylimino, benzylimino, sulphinyl, sulphonyl, carbonyl, carbonylmethylene, methylenecar- bonyl, carbonylvinylene or vinylenecarbonyl group, or X represents a valency bond or a straight-chain alkylene group containing 1 to 4 carbon atoms and Ar is a phenyl, naphthyl, pyridyl, quinolinyl, isoquinolinyl, thienyl, ben- zothienyl, thieno(3,2-b)thien-2-yl or thieno(2,3- b)thien-2-yl group, it being possible for the group Ar to be unsubstituted or substituted with one or more halogen or alkyl, alkyloxy, alkyl- thio, trifluoromethyl, amino, alkylamino, dia- lkylamino, hydroxy, cyano, carboxy, alkylsulphinyl, alkylsulphonyl, sulphamido, alkylsulphamido, dialkylsulphamido, car- bamoyl, alkylcarbamoyl, dialkylcarbamoyl, phenylcarbamoyl, diphenylcarbamoyl, pyridyl- carbamoyl, dipyridylcarbamoyl, benzyl, alkyl- carbonyl, benzoyl, alkyloxycarbonyl, phenoxycarbonyl, alkylcarbonyloxy, ben- zoyloxy, alkylcarbonylamino or benzamido group; each alkyl moiety containing 1 to 4 straight- or branched-chain carbon atoms; the compound being in separate enantiomeric form or mixtures thereof or a pharmaceutically ac- ceptable salt thereof is useful in the treatment of all the pathological conditions in which PAF- acether may be directly or indirectly implicated. 4788179 A method of treating patients suffering from amyotrophic lateral sclerosis (ALS) by ad- ministering dipeptide derivatives of the formula See Patent for Chemical Structure wherein RI is hydrogen, a lower alkyl group, cyclohexyl or benzyl; Z is one of the groups See Patent for Chemical Structure wherein if Z is a group (a), R2 and R3 together represent an additional bond between the carbon atoms bearing R2 and R3, or ifZ is a group (b), R2 is hydrogen; R4 and R5 are hydrogen or lower alkyl, or R5 may also be phenyl; and R6 is hydrogen or methyl; hydrates or pharmaceutically acceptable acid additions salts thereof. Pharmaceutical com- positions containing effective ALS symptom counteracting amounts of such dipeptide derivatives may be administered by infusion, in- jection, orally, rectally or percutaneously. 4788180 PHARMACEUTICAL COMPOSITIONS Maurice Bloch, London, N3 1ES, United King- dom A pharmaceutical composition comprises magnesium oxide, hydroxide or a non-toxic salt of magnesium in a slow-release carrier; this material may be combined with or co-prescribed with a diuretic or cardiac glycoside or adrenergic receptor blocking agent or a calcium antagonist for the treatment of hypertension or angina pec- toris. 4788187 BENZOCYCLOBUTENE AMINOALKYLENE ETHERS AND THIOETHERS, PHARMACEUTICAL COMPOSITION AND USE METHOD OF TREATING AMYOTROPHIC LATERAL SCLEROSIS WITH DIPEPTIDE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS FOR USE THEREIN Leopold Flohe, Hans Barth, Roetgen, Federal Republic Of Germany assigned to Gruenenthal GmbH Donald E Kuhla, Henry F Campbell, William L Studt assigned to Rorer Pharmaceutical Cor- poration A class of benzocyclobutene aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti- secretory and anti-ulcerogenic activity, pharma- ceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.

4788187 Benzocyclobutene aminoalkylene ethers and thioethers, pharmaceutical composition and use

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Page 1: 4788187 Benzocyclobutene aminoalkylene ethers and thioethers, pharmaceutical composition and use

iv New Patents

A compound of the general formula I; See Pa- tent for Chemical Structure (I) in which R is hydrogen or a halogen or an alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, carboxy, alkylsulphinyl, alkylsulphonyl, sulphamido, alkylsulphamido, dialkylsulphamido, car- bamoyl, alkylcarbamoyl, dialkylcarbamoyl, phenylcarbamoyl, diphenylcarbamoyl, pyridyl- carbamoyl, dipyridylcarbamoyl, benzyl, alkyl- carbonyl, benzoyl, alkyloxycarbonyl, phenoxycarbonyl, alkylcarbonyloxy, ben- zoyloxy, alkylcarbonylamino, benzamido, phenyl, phenoxy or phenylthio group, X is oxy- gen or sulphur or an imino, alkylimino, phenylimino, benzylimino, sulphinyl, sulphonyl, carbonyl, carbonylmethylene, methylenecar- bonyl, carbonylvinylene or vinylenecarbonyl group, or X represents a valency bond or a straight-chain alkylene group containing 1 to 4 carbon atoms and Ar is a phenyl, naphthyl, pyridyl, quinolinyl, isoquinolinyl, thienyl, ben- zothienyl, thieno(3,2-b)thien-2-yl or thieno(2,3- b)thien-2-yl group, it being possible for the group Ar to be unsubstituted or substituted with one or more halogen or alkyl, alkyloxy, alkyl- thio, trifluoromethyl, amino, alkylamino, dia- lkylamino, hydroxy, cyano, carboxy, alkylsulphinyl, alkylsulphonyl, sulphamido, alkylsulphamido, dialkylsulphamido, car- bamoyl, alkylcarbamoyl, dialkylcarbamoyl, phenylcarbamoyl, diphenylcarbamoyl, pyridyl- carbamoyl, dipyridylcarbamoyl, benzyl, alkyl- carbonyl, benzoyl, alkyloxycarbonyl, phenoxycarbonyl, alkylcarbonyloxy, ben- zoyloxy, alkylcarbonylamino or benzamido group; each alkyl moiety containing 1 to 4 straight- or branched-chain carbon atoms; the compound being in separate enantiomeric form or mixtures thereof or a pharmaceutically ac- ceptable salt thereof is useful in the treatment of all the pathological conditions in which PAF- acether may be directly or indirectly implicated.

4788179

A method of treating patients suffering from amyotrophic lateral sclerosis (ALS) by ad- ministering dipeptide derivatives of the formula See Patent for Chemical Structure wherein RI is hydrogen, a lower alkyl group, cyclohexyl or benzyl; Z is one of the groups See Patent for Chemical Structure wherein if Z is a group (a), R2 and R3 together represent an additional bond between the carbon atoms bearing R2 and R3, or ifZ is a group (b), R2 is hydrogen; R4 and R5 are hydrogen or lower alkyl, or R5 may also be phenyl; and R6 is hydrogen or methyl; hydrates or pharmaceutically acceptable acid additions salts thereof. Pharmaceutical com- positions containing effective ALS symptom counteracting amounts of such dipeptide derivatives may be administered by infusion, in- jection, orally, rectally or percutaneously.

4788180

P H A R M A C E U T I C A L C O M P O S I T I O N S

Maurice Bloch, London, N3 1ES, United King- dom

A pharmaceutical composition comprises magnesium oxide, hydroxide or a non-toxic salt of magnesium in a slow-release carrier; this material may be combined with or co-prescribed with a diuretic or cardiac glycoside or adrenergic receptor blocking agent or a calcium antagonist for the treatment of hypertension or angina pec- toris.

4788187

B E N Z O C Y C L O B U T E N E A M I N O A L K Y L E N E E T H E R S A N D

THIOETHERS, P H A R M A C E U T I C A L

COMPOSITION A N D U S E

METHOD OF TREATING AMYOTROPHIC LATERAL

SCLEROSIS WITH DIPEPTIDE DERIVATIVES AND PHARMACEUTICAL

COMPOSITIONS FOR USE THEREIN

Leopold Flohe, Hans Barth, Roetgen, Federal Republic Of Germany assigned to Gruenenthal GmbH

Donald E Kuhla, Henry F Campbell, William L Studt assigned to Rorer Pharmaceutical Cor- poration

A class of benzocyclobutene aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti- secretory and anti-ulcerogenic activity, pharma- ceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.