xvi New Patents

A new pharmaceutical formulation as well as a process for its preparation are described, in which the active ingredient in one pharma- ceutical form is present in retarded release form in one part, and in another part is present in a form resistant to gastric juices.

4980171

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 F O R O R A L

A D M I N I S T R A T I O N , B A S E D O N A D I P H O S P H O N I C A C I D

D E R I V A T I V E

Jean-Pierre Fels, Jean-Claude Gromenil, Ber- nard Abramovici, Castelnau le lez, France as- signed to Societe Anonyme dite : SANOFI

Oshida, Koji Tomimori, Yasuhid Uejima, Hino, Japan assigned to Teijin Limited

A 4H-3,l-benzoxazin-4-one compound of the formula (I): See Patent for Chemical Structure (I) wherein R is a hydrogen atom or alkyl radical, A is an amino acid residue or a peptide having 2 to 3 amino acid residues, which amino acid residue may have a side chain thereof protected by a pro- tective radical, X is an alkyl, fluoroalkyl, OR1 or NHR1 radical wherein R1 is an alkyl radical, and Y is a protective radical for an amino radical, and salts thereof, exhibit an excellent in- hibitory activity against serine proteases, espe- cially against human leukocyte elastase, and thus are useful as an effective component of a medicine for inhibiting elastase.

4980349

The invention relates to oral pharmaceutical compositions comprising a diphosphonic acid derivative and sodium laurylsulfate in the amount of 1.5 to 6~o by weight, relative to the diphosphonic compound.

4980173

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 A N D M E T H O D

FOR T H E T R E A T M E N T OF C O L I T I S U L C E R O S A A N D

C R O H N ' S D I S E A S E B Y O R A L A D M I N I S T R A T I O N

Soren Halskov, Helsinge, Denmark assigned to Farmaceutisk Laboratorium Ferring A/S

A pharmaceutical composition containing as ac- tive ingredient 5-aminosalicylic acid or a pharmaceutically acceptable salt or ester thereof allow the treatment of colitis ulcerosa or Crohn's disease by oral administration. A particular slow-release tablet formation and its preparation is disclosed.

4980287

S U L P H O N A M I D E S DERIVED F R O M D I A R Y L M E T H A N E S , THE

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

T H E M

Pierre Roger, Jean-Paul Fournier, Alain Martin, Jean Choay, Montigny les Bretonneux, France assigned to SANOFI

The invention relates to new compounds cor- responding to formula I: See Patent for Chemical Structure (I) in which: W represents C = O, CH2 or CHOH, Z represents See Patent Jot Chemical Structure R 1 and R2 represent especially C1 or F, R, R' and R" represent especially H, X represents especially CH2, Y represents espe- cially COOH, u and v are two integers ranging from 0 to 10, p and q t a k e t h e value0 or 1, n and m are two integers ranging 0 to 10 and t is 0 or 1 the total number of carbon atoms in the chain See Patent Jot Chemical Structure ranging from 2 to 20, and to their physiologically acceptable salts obtained with organic or inorganic acids. These compounds are useful for preparing medicinal products which have, especially, anti- inflammatory properties.

4 H - 3 , 1 - B E N Z O X A Z I N - 4 - O N E C O M P O U N D S 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 S THEREOF FOR

THE INHIBITION OF SERINE P R O T E A S E S

Masayuk Kokubo, Katsuhik Fujii, Jun-ich

4980499

C Y C L O P E N T Y L E T H E R S A N D T H E I R P R E P A R A T I O N A N D

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

Eric W Collington, Welwyn, United Kingdom assigned to Glaxo Group Limited