1
ii New Patents cess for their manufacture and their use in the manufacture of antibiotically active pharma- ceuticals. New 2:1 complexes of N-methyl-I 1- aza- 10 deoxo- 10-dihydroerythromycin A or 1l- aza-10-deoxo-10 dihydroerythromycin A with bivalent metals chosen from the group com- prising Cu+2, Zn+2, Co+2, Ni+2 and Ca+2 are made by reacting N-methyl-ll-aza-10- deoxo- 10 dihydroerythromycin A or 11-aza- 10- deoxo-10 dihydroerythromycin A in its free base form or in its water-soluble salt form with salts of said bivalent metals. The compounds possess antibiotic activity. 4963530 RENIN INHIBITOR PEPTIDE COMPOUNDS, A PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME Keiji Hemmi, Masahiro Neya, Keisuke Imai, Natsuko Kayakiri, Masashi Hashimoto, Tsukuba, Japan assigned to Fujisawa Pharma- ceutical Company Ltd A compound of the formula: See Patent for Chemical Structure wherein R 1 is aryl optionally substituted with a substituent selected from the group consisting of halogen and halo(lower)alkyl; lower alkyl or cyclo- (lower)alkyl; and R2 is hydrogen or lower alkyl, or R1 and R2 are taken together with the at- tached nitrogen atom to form a heterocyclic group optionally substituted with a substituent selected from the group consisting of lower alkyl and esterified carboxy, R3 is hydrogen or lower alkyl, and R4 is lower alkyl, and its pharma- ceutically acceptable salt, a process for the pre- paration thereof and pharmaceutical composition comprising the same. 4963536 DIPHOSPHONIC ACID COMPOUNDS, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME USEFUL FOR TREATING BONE DISEASES Teruo Oku, Eishiro Todo, Chiyoshi Kasahara, Katsuya Nakamura, Hiroshi Kayakiri, Masashi Hashimoto, Sakuramura, Japan assigned to Fujisawa Pharmaceutical Company Ltd A compound of the formula: See Patent for Chemical Structure wherein R1-A- is a group of the formula: See Patent for Chemical Structure in which RI is aryl or a heterocyclic group, each of which may be substituted with substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halo(lower)alkyl, acyl, acylamino and halogen, or lower alkyl which may be substituted with a heterocyclic group optionally substituted with acyl, and X is O or S, and R2 is hydrogen or lower alkyl, pro- vided that when R1 is lower alkyl, then RI-A- is a group of the formula: See Patent for Chemical Structure in which R1 and X are each as defined above, processes for the preparation thereof and pharmaceutical composition comprising the same. 4963537 LABDANE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USE Raymond W Kosley, Robert J Cherill assigned to Hoechst-Roussel Pharmaceuticals Inc Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing com- pounds or compositions thereof are disclosed. 4963570 1-(ACETYLAMINOPHENYL) 2-AMINOPROPANONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF Louis Lafon, Paris, France assigned to Laboratoire L Lafon The present invention relates, by way of new industrial products, to l-(acetylaminophenyl) 2- amino-propanone derivatives selected from the group consisting of(a) the compounds of the for- mula See Patent for Tabular Presentation PS in which NR1R2 represents a piperidino group; and Ar represents an acetylaminophenyl group of the formula See Patent for Chemical Structure in which X is CH3CONH and Y and Z, which can be identical or different, each represent a hydrogen or halogen atom; and (b) their addi- tion salts. These new products are useful as anti-

4963530 Renin inhibitor peptide compounds, a process for the preparation thereof and pharmaceutical composition comprising the same

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ii New Pa ten t s

cess for their manufacture and their use in the manufacture of antibiotically active pharma- ceuticals. New 2:1 complexes of N-methyl-I 1- aza- 10 deoxo- 10-dihydroerythromycin A or 1 l- aza-10-deoxo-10 dihydroerythromycin A with bivalent metals chosen from the group com- prising Cu+2, Zn+2, Co+2, Ni+2 and Ca+2 are made by reacting N-methyl-ll-aza-10- deoxo- 10 dihydroerythromycin A or 11-aza- 10- deoxo-10 dihydroerythromycin A in its free base form or in its water-soluble salt form with salts of said bivalent metals. The compounds possess antibiotic activity.

4963530

RENIN INHIBITOR PEPTIDE COMPOUNDS, A PROCESS FOR T H E P R E P A R A T I O N T H E R E O F

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

Keiji Hemmi, Masahiro Neya, Keisuke Imai, Natsuko Kayakiri, Masashi Hashimoto, Tsukuba, Japan assigned to Fujisawa Pharma- ceutical Company Ltd

A compound of the formula: See Patent for Chemical Structure wherein R 1 is aryl optionally substituted with a substituent selected from the group consisting of halogen and halo(lower)alkyl; lower alkyl or cyclo- (lower)alkyl; and R2 is hydrogen or lower alkyl, or R1 and R2 are taken together with the at- tached nitrogen atom to form a heterocyclic group optionally substituted with a substituent selected from the group consisting of lower alkyl and esterified carboxy, R3 is hydrogen or lower alkyl, and R4 is lower alkyl, and its pharma- ceutically acceptable salt, a process for the pre- paration thereof and pharmaceutical composition comprising the same.

4963536

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

T R E A T I N G B O N E D I S E A S E S

Teruo Oku, Eishiro Todo, Chiyoshi Kasahara, Katsuya Nakamura, Hiroshi Kayakiri, Masashi Hashimoto, Sakuramura, Japan assigned to Fujisawa Pharmaceutical Company Ltd

A compound of the formula: See Patent for Chemical Structure wherein R1-A- is a group of the formula: See Patent for Chemical Structure in which RI is aryl or a heterocyclic group, each of which may be substituted with substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halo(lower)alkyl, acyl, acylamino and halogen, or lower alkyl which may be substituted with a heterocyclic group optionally substituted with acyl, and X is O or S, and R2 is hydrogen or lower alkyl, pro- vided that when R1 is lower alkyl, then RI-A- is a group of the formula: See Patent for Chemical Structure in which R1 and X are each as defined above, processes for the preparation thereof and pharmaceutical composition comprising the same.

4963537

L A B D A N E C O M P O U N D 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 U S E

Raymond W Kosley, Robert J Cherill assigned to Hoechst-Roussel Pharmaceuticals Inc

Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing com- pounds or compositions thereof are disclosed.

4963570

1-(ACETYLAMINOPHENYL) 2 - A M I N O P R O P A N O N E

D E R I V A T I V E 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 T H E R E O F

Louis Lafon, Paris, France assigned to Laboratoire L Lafon

The present invention relates, by way of new industrial products, to l-(acetylaminophenyl) 2- amino-propanone derivatives selected from the group consisting of(a) the compounds of the for- mula See Patent for Tabular Presentation PS in which NR1R2 represents a piperidino group; and Ar represents an acetylaminophenyl group of the formula See Patent for Chemical Structure in which X is CH3CONH and Y and Z, which can be identical or different, each represent a hydrogen or halogen atom; and (b) their addi- tion salts. These new products are useful as anti-