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New Patents vii 4581360 4581380 SPARSOMYCIN (SC-RS) DERIVATIVE; PHARMACEUTICAL COMPOSITION HAVING ANTI- TUMOR ACTIVITY Henricus C J Ottenheijm, Robertus M Liskamp, Milsbeek, NY, Netherlands assigned to Stichting Katholieke Universiteit The invention concerns novel sparsomycin (Sc- Rs) derivatives having superior cytostatic ac- tivity compared to sparsomycin itself. Said derivatives contain a lipophilic group R2, selec- ted from C2-C20-alkyl, aryl, aralkyl and alkaryl, which is preferably n-octyl or benzyl. 4581368 AZIRIDINO CONTAINING NITRO IMIDAZOLES AND PHARMACEUTICAL COMPOSITIONS Israr Ahmed, Gerald E Adams, Ian J Stratford, London, United Kingdom assigned to National Research Development Corporation 2,6-DISUBSTITUTED NAPHTHALENE DERIVATIVES, A PROCESS FOR PREPARING THE SAME AND PHARMACEUTICAL AND COSMETIC COMPOSITIONS CONTAINING THE SAME Braha Shroot, Jacques Eustache, Martine Bouclier, Antibes, France assigned to Groupe- ment Economique dire: Centre National de Recherches Dermatologiques C I R D New 2,6-disubstituted derivatives of naphtha- lene have the formula See Patent for Chemical Structure (I) wherein n is 1 or 2, R1 to R4 are hydrogen or CH3, R5 is See Patent for Chemical Structure (ii)CN, (iii)OCR8, or (iv) 2-oxazolinyl, wherein m is 0 or 1, R6 is hydrogen, alkyl, OR9 wherein R9 is H, alkyl or See Patent for Chemical Structure wherein R10 is alkyl or aryl, or R6 is See Patent for Chemical Structure when m = 1, r' and r" representing H, alkyl, mono- or poly- hydroxyalkyl, aryl or a heterocycle when taken together, R7 is H or alkyl, R8 is H, alkyl and the acetal of said compounds, and the salts of the compounds of formula I. These compounds are usefully employed in the pharmaceutical and cosmetic fields. A compound of formula I See Patent for Chem- ical Structure I in which formula: R1 represents hydrogen or an alkyl group; R2-R5 represent hydrogen, alkyl aryl, aralkyl or alkaryl group; and n is 1. 4581371 PHARMACEUTICAL COMPOSITION HAVING IMMUNOMODULATING ACTIVITY Massimo Baldacci, Pisa, Italy assigned to Laboratori Baldacci S p A The administration by oral route of a composi- tion comprising arginine pyrrolidone carboxy- late and lysine pyrrolidone carboxylate at a dose of 150 to 200 mg/kg of body weight has immuno- modulating activity capable of restoring depres- sed immunodefenses. 4582717 PROCESS FOR PRODUCTION OF VAGINAL TAMPONS CONTAINING PHARMACEUTICAL ACTIVE COMPOUND Miklos von Bittera, Karl Buchel, Manfre Plem- pel, Erik Regel, Leverkusen, Federal Republic Of Germany assigned to Bayer Aktiengesel- lschaft The invention relates to a process for production of tampons containing novel formulations of antimycotic azole derivatives which provide a higher release of active compounds and make short-term therapy possible. The tampon for- mulations of the invention contain active anti- mycotic azole derivatives in impregnated form, only melting at body temperature, or dissolved form, such as, for example, in suppository bases or their combinations with emulsifiers and/or spreading agents and/or solubilisers.

4581380 2,6-disubstituted naphthalene derivatives, a process for preparing the same and pharmaceutical and cosmetic compositions containing the same

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Page 1: 4581380 2,6-disubstituted naphthalene derivatives, a process for preparing the same and pharmaceutical and cosmetic compositions containing the same

New Patents vii

4581360 4581380

SPARSOMYCIN (SC-RS) DERIVATIVE;

PHARMACEUTICAL COMPOSITION HAVING ANTI-

TUMOR ACTIVITY

Henricus C J Ottenheijm, Robertus M Liskamp, Milsbeek, NY, Netherlands assigned to Stichting Katholieke Universiteit

The invention concerns novel sparsomycin (Sc- Rs) derivatives having superior cytostatic ac- tivity compared to sparsomycin itself. Said derivatives contain a lipophilic group R2, selec- ted from C2-C20-alkyl, aryl, aralkyl and alkaryl, which is preferably n-octyl or benzyl.

4581368

AZIRIDINO CONTAINING NITRO IMIDAZOLES AND

PHARMACEUTICAL COMPOSITIONS

Israr Ahmed, Gerald E Adams, Ian J Stratford, London, United Kingdom assigned to National Research Development Corporation

2,6-DISUBSTITUTED NAPHTHALENE DERIVATIVES, A PROCESS FOR PREPARING THE SAME AND PHARMACEUTICAL

AND COSMETIC COMPOSITIONS CONTAINING THE SAME

Braha Shroot, Jacques Eustache, Martine Bouclier, Antibes, France assigned to Groupe- ment Economique dire: Centre National de Recherches Dermatologiques C I R D

New 2,6-disubstituted derivatives of naphtha- lene have the formula See Patent for Chemical Structure (I) wherein n is 1 or 2, R1 to R4 are hydrogen or CH3, R5 is See Patent for Chemical Structure (ii)CN, (iii)OCR8, or (iv) 2-oxazolinyl, wherein m is 0 or 1, R6 is hydrogen, alkyl, OR9 wherein R9 is H, alkyl or See Patent for Chemical Structure wherein R10 is alkyl or aryl, or R6 is See Patent for Chemical Structure when m = 1, r' and r" representing H, alkyl, mono- or poly- hydroxyalkyl, aryl or a heterocycle when taken together, R7 is H or alkyl, R8 is H, alkyl and the acetal of said compounds, and the salts of the compounds of formula I. These compounds are usefully employed in the pharmaceutical and cosmetic fields.

A compound of formula I See Patent for Chem- ical Structure I in which formula: R1 represents hydrogen or an alkyl group; R2-R5 represent hydrogen, alkyl aryl, aralkyl or alkaryl group; and n is 1.

4581371

PHARMACEUTICAL COMPOSITION HAVING IMMUNOMODULATING

ACTIVITY

Massimo Baldacci, Pisa, Italy assigned to Laboratori Baldacci S p A

The administration by oral route of a composi- tion comprising arginine pyrrolidone carboxy- late and lysine pyrrolidone carboxylate at a dose of 150 to 200 mg/kg of body weight has immuno- modulating activity capable of restoring depres- sed immunodefenses.

4582717

PROCESS FOR PRODUCTION OF VAGINAL TAMPONS

CONTAINING PHARMACEUTICAL ACTIVE

COMPOUND

Miklos von Bittera, Karl Buchel, Manfre Plem- pel, Erik Regel, Leverkusen, Federal Republic Of Germany assigned to Bayer Aktiengesel- lschaft

The invention relates to a process for production of tampons containing novel formulations of antimycotic azole derivatives which provide a higher release of active compounds and make short-term therapy possible. The tampon for- mulations of the invention contain active anti- mycotic azole derivatives in impregnated form, only melting at body temperature, or dissolved form, such as, for example, in suppository bases or their combinations with emulsifiers and/or spreading agents and/or solubilisers.