4631278 Anti-protozoal alpha-aryl-4-(4,5-dihydro-3,5-dioxo-1,2,...

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New Patents vii 4631278 ANTI-PROTOZOAL ALPHA- ARYL-4-(4,5-DIHYDRO-3,5-DIOXO- 1,2, 4-TRIAZIN-2(3H)-YL)- BENZENEACETONITRILE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHOD OF USE THEREFOR Gustaaf M Boeckx, Alfons H M Raeymaekers, Victor Sipido, Oud Turnhout, Belgium assigned to Janssen Pharmaceutica N V The present invention is related with alpha-aryl- 4-(4,5-dihydro-3, 5-dioxo- 1,2,4-triazin-2(3H)- yl)benzeneacetonitriles which are effective in destructing or preventing the growth of Pro- tozoa in subjects suffering from such Protozoa. 4631293 (-) CAMPHOLENIC ACID ESTER OF SALICYLIC ACID AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF HAVING MUCOSECRETOLYTIC, ANTI-INFLAMMATORY, ANALGESIC, AND ANTIPYRETIC ACTIVITY Camillo C Mora, Piacenza, Italy assigned to Camillo Corvi S p A A novel salicylic acid ester is described, which may be combined with inorganic or organic bases to give pharmaceutically acceptable salts. Such an ester is obtained by reaction of (-) cam- pholenic acid chloride, as prepared by a well known technique, with salicylic acid. There are, further, described pharmaceutical compositions having mucosecretolytic, anti-inflammatory, analgesic, antipyretic activity, which contain the novel ester or the salts thereof. 8606586 A method of inducing a reservoir effect in skin and mucous membranes so as to enhance penetration and retention and reduce trans- dermal flux of topically applied therapeutic and cosmetic pharmacologically active agents. The invention also relates to topical treatment methods involving such reservoir effect en- hancers, and to pharmaceutical compositions containing them. 8606717 3-AMINOPROPYLOXYPHENYL DERIVATIVES THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM William John LOUIS, Richard BERTHOLD, Max-Peter SEILER, Andr@ STOLL, 5 Von Nida Crescent, Rosanna, VIC 3084, Australia Compounds of formula (I), characterised in that R signifies optionally substituted heteroaryl-, heteroarylalkyl or heteroarylalkenyl, R) 1 ( signifies hydrogen or a substituent, R)2( is hydroxy or a group -Z-(CH)2())n(-Y-R)3( wherein R)3( is hydrogen, alkyl, hydroxyalkyl, alkenyl, cycloalkyl, cycloalkylalkylene, hydroxy substituted cycloalkyl or cycloalkylalkylene, or optionally substituted aryl or aralkyl or aralkenyl moiety, and Y signifies oxygen or sul- fur, and either Z is an oxygen 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 imino, and X signifies a bond or imino, and their phys- iologically hydrolysable derivatives, in which at least one hydroxy group is in esterified form. The compounds exhibit beta adrenoceptor blocking activity. Process for the preparation of the com- pounds are also disclosed. 8606720 ASCORBIC ACID DERIVATIVES, PRODUCTION THEREOF, AND PHARMACEUTICAL PREPARATION THEREFROM PHARMACEUTICAL VEHICLES FOR RECUCING TRANSDERMAL FLUX Larry M ALLEN, Larry M ALLEN assigned to CHEMEX PHARMACEUTICALS INC; Shinji TERAO, Minoru HIRATA, 26-3, Shinsenri-minamimachi 2-chome, Toyonaka- shi, Osaka 565, Japan assigned to TAKEDA CHEMICAL INDUSTRIES LTD; A pharmaceutical preparation comprising an

Transcript of 4631278 Anti-protozoal alpha-aryl-4-(4,5-dihydro-3,5-dioxo-1,2,...

New Patents vii

4631278

ANTI-PROTOZOAL ALPHA- ARYL-4-(4,5-DIHYDRO-3,5-DIOXO-

1,2, 4-TRIAZIN-2(3H)-YL)- BENZENEACETONITRILE

DERIVATIVES, PHARMACEUTICAL

COMPOSITIONS, AND METHOD OF USE THEREFOR

Gustaaf M Boeckx, Alfons H M Raeymaekers, Victor Sipido, Oud Turnhout, Belgium assigned to Janssen Pharmaceutica N V

The present invention is related with alpha-aryl- 4-(4,5-dihydro-3, 5-dioxo- 1,2,4-triazin-2(3H)- yl)benzeneacetonitriles which are effective in destructing or preventing the growth of Pro- tozoa in subjects suffering from such Protozoa.

4631293

(-) CAMPHOLENIC ACID ESTER OF SALICYLIC ACID AND

PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF HAVING MUCOSECRETOLYTIC,

ANTI-INFLAMMATORY, ANALGESIC, AND ANTIPYRETIC

ACTIVITY

Camillo C Mora, Piacenza, Italy assigned to Camillo Corvi S p A

A novel salicylic acid ester is described, which may be combined with inorganic or organic bases to give pharmaceutically acceptable salts. Such an ester is obtained by reaction of (-) cam- pholenic acid chloride, as prepared by a well known technique, with salicylic acid. There are, further, described pharmaceutical compositions having mucosecretolytic, anti-inflammatory, analgesic, antipyretic activity, which contain the novel ester or the salts thereof.

8606586

A method of inducing a reservoir effect in skin and mucous membranes so as to enhance penetration and retention and reduce trans- dermal flux of topically applied therapeutic and cosmetic pharmacologically active agents. The invention also relates to topical treatment methods involving such reservoir effect en- hancers, and to pharmaceutical compositions containing them.

8606717

3-AMINOPROPYLOXYPHENYL DERIVATIVES THEIR PREPARATION AND PHARMACEUTICAL

COMPOSITIONS CONTAINING THEM

William John LOUIS, Richard BERTHOLD, Max-Peter SEILER, Andr@ STOLL, 5 Von Nida Crescent, Rosanna, VIC 3084, Australia

Compounds of formula (I), characterised in that R signifies optionally substituted heteroaryl-, heteroarylalkyl or heteroarylalkenyl, R) 1 ( signifies hydrogen or a substituent, R)2( is hydroxy or a group -Z-(CH)2())n(-Y-R)3( wherein R)3( is hydrogen, alkyl, hydroxyalkyl, alkenyl, cycloalkyl, cycloalkylalkylene, hydroxy substituted cycloalkyl or cycloalkylalkylene, or optionally substituted aryl or aralkyl or aralkenyl moiety, and Y signifies oxygen or sul- fur, and either Z is an oxygen 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 imino, and X signifies a bond or imino, and their phys- iologically hydrolysable derivatives, in which at least one hydroxy group is in esterified form. The compounds exhibit beta adrenoceptor blocking activity. Process for the preparation of the com- pounds are also disclosed.

8606720

ASCORBIC ACID DERIVATIVES, PRODUCTION THEREOF, AND

PHARMACEUTICAL PREPARATION THEREFROM

PHARMACEUTICAL VEHICLES FOR RECUCING TRANSDERMAL

FLUX

Larry M ALLEN, Larry M ALLEN assigned to CHEMEX PHARMACEUTICALS INC;

Shinji TERAO, Minoru HIRATA, 26-3, Shinsenri-minamimachi 2-chome, Toyonaka- shi, Osaka 565, Japan assigned to TAKEDA CHEMICAL INDUSTRIES LTD;

A pharmaceutical preparation comprising an