New Patents i x

4394382

DIHYDROBENZOPYRAN COM- POUNDS A N D 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 C O M P R I S I N G S A I D

C O M P O U N D S

Masam Shiratsuchi, Noboru Shimizu, Hir- omichi Shigyo, Yoshinori Kyotani, Hisashi Kunieda, Kiyoshi Kawamura, Seiichi Sato, Toshihiro Akashi, Masahiko Nagakura, Na- otoshi Sawada, Yasumi Uchida, Musash- imurayama, Japan assigned to Kowa Company Ltd

RI OR3 N I

NCH2CHA A O

H / i ~ RZ

(B--ONO2)n

A benzopyran compound represented by the fol- lowing See Patent jbr Chemical Structure (I) wherein A represents a direct bond or the bond -CH2-O-, R1 represents a member selected from the group consisting of a C3-C5 alkyl group, a hydroxy-(C3-C5 alkyl) group, a lower alkylamino-lower alkyl group, a nitrato-(C3-C5 alkyl) group and a phenyl-(C1-C5) alkyl group, provided that the phenyl may be substituted by a lower alkoxy group, R2 represents a member selected from the group consisting of hydrogen, halogen, OH, NO2, a carbamoyl group, a lower alkyl group, a lower alkoxy group, a lower alkyleneoxy group and acetyl group, R3 repr- esents hydrogen or NO2, B represents a direct bond, a C1-C7 alkylene group, a -O-lower alky- lene group or a -CONH-lower alkylene group, and n represents 1 or 2; and an acid addition salt thereof and a pharmaceutical composition com- prising aforesaid compound.

4393079

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

William Cole, Alexander Goudie, Carl J Rose, Twickenham, United Kingdom assigned to Beecham Group Limited

R3~Y

CH--X--CH3

Anti-inflammatory compositions are prepared which comprise a therapeutically effective amount of a compound of the formula See Patent for Chemical Structure (I) wherein X is CO or CHOH; Y is CO; the dotted line represents a double bond which is present or a- bsent; R1 is hydrogen or methyl; R2 is hydrogen, fluorine, chlorine, bromine, methyl, triftuor- omethyl, methoxyl, hydroxyl, acetoxyl, nitro or amino; R3 is alkyl of 3 to 8 carbon atoms, cyclo- alkyl of 3 to 8 carbon atoms, alkenyl of 3 to 8 car- bon atoms, cycloalkenyl of 5 to 8 carbon atoms or phenyl unsubstituted or substituted by 1 or 2 substituents selected from the group consisting of fluorine, chlorine, bromine, methyl, ethyl, methoxyl, ethoxyl, benzyloyl, hydroxyl, ace- toxyl, trifluoromethyl, nitro, amino, acetyl, methylthiol, methylsulphonyl, methylamino and dimethylamino. Compounds of formula I above are also novel.

4393070

D I H Y D R O P Y R I D I N E D E R I V A - T I V E , A N D 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 C O M P R I S I N G

T H E S A M E

Yoshinari Sato, Tsutomu Teraji, Takaishi, Japan assigned to Fujisawa Pharmaceutical Co Ltd

R2OOC COOR 3

w'---~.. ..A--R~ N H

1,4-dihydropyridine derivatives of the general formula: See Patent Jor Chemical Structure having vasodilating and anti-hypertensive act- ivity, processes for preparing same, and pharma- ceutical compositions thereof for treating cardiovascular diseases.

4393062

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 A N D M E T H O D F O R T H E

P R O D U C T I O N O F AN A N T I - I N F L A M M A T O R Y E F F E C T

David R Brittain, Robin Wood, Macclesfield, United Kingdom assigned to Imperial Chemical Industries PLC

This invention relates to enzyme inhibitory, novel phthalazin-4-ylacetic acid derivatives of

x New Patents

the general formula I: See Patent Jor Chemical Structure I and pharmaceutically acceptable salts as appropriate, to pharmaceutical composi- tions thereof, and to analogy processes for their manufacture. The compounds of formula I are inhibitors of the enzyme aldose reductase in vivo and as such may be useful in the reduction or pre- vention of the development of the peripheral ef- fects such as macular oedema, cataract, retinopathy or impaired neural conduction. A preferred compound is 2-(2-ftuoro-4 -bromobenzyl)- 1, 2-dihydro- 1-oxop- hthalazin-4-ylacetic acid.

4391817

PYRROLO-DIAZEPINE D E R I V A T I V E S A N D T H E I R

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

O

(CH2)3--N N N--R

/ F O

X Novel (1-(3-(6-fluoro-1, 2-benzisox- azol-3-yl)propyl) -4-(2-oxo- 1 -ben- zimidazolinyl))piperidines, process for the preparation thereof, and methods of treating psychoses and alleviating pain employing com- pounds and compositions thereof are disclosed.

4390540

I M I D A Z O Q U I N A Z O L I N E S H A V I N G P H A R M A C E U T I C A L

A C T I V I T Y

Luigi Mariani, Giorgio Tarzia, Milan, Italy as- signed to Gruppo Lepetit S p A

R,, o / / R _ ~ R ~ N~C~

CH2

CH3- ~C=N I

A new class of pyrrolo-diazepines with anti- convulsant and anti-anxiety activity of the ge- neral formula See Patent for Chemical Structure I wherein R is (C1-C4)alkyl, R1 is chloro, bromo or nitro, R2 is hydrogen or (C 1-C4)alkyl and R3 is hydrogen, chloro, bromo, fluoro, trifiuor- omethyl or methoxy. The new compounds are prepared starting from the corresponding com- pounds wherein Rl is hydrogen through hal- ogenation or nitration. Pharmaceutical preparations containing the new compounds of formula I are also described.

Madhukar S Chodnekar, Ado Kaiser, Frank Kienzle, Seltisberg, Switzerland assigned to Hof- fmann-La Roche Inc

R 5 O

R 2 _ ~ N . ~ NH

R3 ~ N

Imidazoquinazolines of the formula See Patent for Chemical Structure I wherein R1, R2 and R3 are hydrogen, halogen, C1-4-alkyl, C1-4-alkoxy or C2-5-alkoxyalkyl; or two of R1, R2 and R3 on adjacent carbon atoms taken together are meth- ylenedioxy or ethylenedioxy; and R4 and R5 are hydrogen or C I-4-alkyl, and their tautomers, as well as their physiologically compatible acid addition salts, are described. The compounds of formula I inhibit the aggregation of the blood platelets, as well as gastric acid secretion, and have activity on the circulatory system.

4390526

4390544

( 1 - ( 3 - ( 6 - F L U O R O - 1 , 2 - B E N Z I S O X A Z O L - 3 - Y L ) P R O P Y L )

-4-(2-OXO-1-BEN- ZIMIDAZOLINYL) P I P E R I D I N E S , 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 A N D M E T H O D S O F U S E

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

S I C K L E C E L L D I S E A S E

Marian Gorecki, Clemenceau T A Acquaye, Meir Wilchek, Alexander Rich, Rehovot, Israel assigned to Yeda Research & Development Co Ltd

Larry Davis, Joseph Klein assigned to Hoechst -Roussel Pharmaceuticals Inc

The present invention relates to novel com- pounds selected from RI-COO(CH2)n-R2 and