4868164 octahydro-pyridine diphosphonate compounds, pharmaceutical compositions, and methods for...

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New Patents xi 4868164 4868172 OCTAHYDRO-PYRIDINE DIPHOSPHONATE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHODS FOR TREATING ABNORMAL CALCIUM AND PHOSPHATE METABOLISM Frank H Ebetino, Kent W Buckingham, Jocelyn E McOsker assigned to Norwich Eaton Pharma- ceuticals Inc PHARMACEUTICAL COMPOSITION COMPRISING AN ORGANIC ZINC COMPLEX AND A PROCESS FOR PREPARING THE ACTIVE SUBSTANCE Gyula Sebestyen, Istvan Simonyi, Gizeli Miholics, Marta Kovacs, Frigye Gorgenyi, Mar- ton Fekete, VagoPal , lstva Seres, Jano Egri, Mafia Szeli, Budapest, Hungary assigned to BASF Aktiengesellschaft The present invention relates to novel com- pounds having nitrogen-containing, saturated bicyclic cyclopentane-fused rings which are geminally disubstituted with phosphonate groups. Most preferred compounds of the pre- sent invention have the general structure: See Patentfor Chemical Structure The present inven- tion further relates to pharmaceutical composi- tions containing these novel compounds. Finally, this invention relates to methods for treating or preventing diseases characterized by abnormal calcium and phosphate metabolism by utilizing a compound or pharmaceutical com- position of the present invention. The invention refers to a novel pharmaceutical composition having especially antimycotic ac- tivity and comprising the zinc complex of 5- chloro-7-iodo-8 hydroxyquinoline of formula (I) See Patent for Chemical Structure (I) and one or more pharmaceutically acceptable carriers. The pharmaceutical composition of the invention can be used for the effective treatment of mycotic infections on the skin surface, mucous mem- branes or nails. The complex of formula (I) is prepared by reacting a solution of an alkali metal salt of 5-chloro-7-iodo-8 hydroxyquinoline with a solution containing an excess of an inorganic or organic zinc salt or a zinc complex having a lower stability constant than that of the complex of formula (I) and separating the product pre- cipitated. 4868166 2,2:6,6 DIETHYLEN-3-OXO 17ALPHA PREGN-4-ENE-21 17ALPHA-CARBOLACTONES, PROCESS FOR THEIR PRODUCTION & PHARMACEUTICAL PREPARATIONS CONTAINING THEM Diete Bittler, Klau Nickisch, Henry Laurent, Rudolf Wiechert, Martin Haberey, Berlin, Federal Republic Of Germany assigned to Schering Aktiengesellschaft 2,2;6,6 diethylene-3-oxo 17alpha pregn-4-ene-21 17-carbolactones of general formula I, See Pa- tent for Chemical Structure (I) wherein R! represents a hydrogen atom or a methyl group, R2 represents a methyl or ethyl group and See Patent for Chemical Structure process for their production and their pharmaceutical use. 4868177 1,2,3,4-TETRAHYDRO-I 9- ACRIDINEDIAMINES, PHARMACEUTICAL COMPOSITIONS AND USE Gregory M Shutske, Kevin Kapples assigned to Hoechst-Roussel Pharmaceuticals Inc There are disclosed compounds having the for- mula See Patentfor Chemical Structure (I) where n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro or trifluoromethyi R I and R2 are each indepen- dently hydrogen, lower alkyl or arylloweralkyl, but both may not be arylloweralkyl simul- taneously; R3 and R4 are each independently hydrogen, lower alkyl, aryiloweralkyl, formyl or lower alkylcarbonyl, or alternatively the group - NR3R4 taken as a whole constitutes See Patent for Chemical Structure See Patent for Tabular Presentation See Patent for Tabular Presentation stereo isomers thereof and pharmaceutically ac- ceptable acid addition salts thereof, which are

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Page 1: 4868164 Octahydro-pyridine diphosphonate compounds, pharmaceutical compositions, and methods for treating abnormal calcium and phosphate metabolism

New Patents xi

4868164 4868172

OCTAHYDRO-PYRIDINE DIPHOSPHONATE COMPOUNDS,

PHARMACEUTICAL COMPOSITIONS, AND METHODS

FOR TREATING ABNORMAL CALCIUM AND PHOSPHATE

METABOLISM

Frank H Ebetino, Kent W Buckingham, Jocelyn E McOsker assigned to Norwich Eaton Pharma- ceuticals Inc

PHARMACEUTICAL COMPOSITION COMPRISING AN ORGANIC ZINC COMPLEX AND

A PROCESS FOR PREPARING THE ACTIVE SUBSTANCE

Gyula Sebestyen, Istvan Simonyi, Gizeli Miholics, Marta Kovacs, Frigye Gorgenyi, Mar- ton Fekete, VagoPal , lstva Seres, Jano Egri, Mafia Szeli, Budapest, Hungary assigned to BASF Aktiengesellschaft

The present invention relates to novel com- pounds having nitrogen-containing, saturated bicyclic cyclopentane-fused rings which are geminally disubstituted with phosphonate groups. Most preferred compounds of the pre- sent invention have the general structure: See Patent for Chemical Structure The present inven- tion further relates to pharmaceutical composi- tions containing these novel compounds. Finally, this invention relates to methods for treating or preventing diseases characterized by abnormal calcium and phosphate metabolism by utilizing a compound or pharmaceutical com- position of the present invention.

The invention refers to a novel pharmaceutical composition having especially antimycotic ac- tivity and comprising the zinc complex of 5- chloro-7-iodo-8 hydroxyquinoline of formula (I) See Patent for Chemical Structure (I) and one or more pharmaceutically acceptable carriers. The pharmaceutical composition of the invention can be used for the effective treatment of mycotic infections on the skin surface, mucous mem- branes or nails. The complex of formula (I) is prepared by reacting a solution of an alkali metal salt of 5-chloro-7-iodo-8 hydroxyquinoline with a solution containing an excess of an inorganic or organic zinc salt or a zinc complex having a lower stability constant than that of the complex of formula (I) and separating the product pre- cipitated.

4868166

2,2:6,6 DIETHYLEN-3-OXO 17ALPHA PREGN-4-ENE-21

17ALPHA-CARBOLACTONES, PROCESS FOR THEIR

PRODUCTION & PHARMACEUTICAL

PREPARATIONS CONTAINING THEM

Diete Bittler, Klau Nickisch, Henry Laurent, Rudolf Wiechert, Martin Haberey, Berlin, Federal Republic Of Germany assigned to Schering Aktiengesellschaft

2,2;6,6 diethylene-3-oxo 17alpha pregn-4-ene-21 17-carbolactones of general formula I, See Pa- tent for Chemical Structure (I) wherein R! represents a hydrogen atom or a methyl group, R2 represents a methyl or ethyl group and See Patent for Chemical Structure process for their production and their pharmaceutical use.

4868177

1,2,3,4-TETRAHYDRO-I 9- ACRIDINEDIAMINES, PHARMACEUTICAL

COMPOSITIONS AND USE

Gregory M Shutske, Kevin Kapples assigned to Hoechst-Roussel Pharmaceuticals Inc

There are disclosed compounds having the for- mula See Patent for Chemical Structure (I) where n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro or trifluoromethyi R I and R2 are each indepen- dently hydrogen, lower alkyl or arylloweralkyl, but both may not be arylloweralkyl simul- taneously; R3 and R4 are each independently hydrogen, lower alkyl, aryiloweralkyl, formyl or lower alkylcarbonyl, or alternatively the group - NR3R4 taken as a whole constitutes See Patent for Chemical Structure See Patent for Tabular Presentation See Patent for Tabular Presentation stereo isomers thereof and pharmaceutically ac- ceptable acid addition salts thereof, which are