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iv New Patents 4552864 4552871 GONADOLIBERIN DERIVATIVES PROCESS FOR THE PREPARATION AND PHARMACEUTICAL COMPOSITIONS THEREOF Ferenc Antoni, Judit Erchegyi, Aniko Keri Gyorg Horvath, Imre Mezo, Karol Nikolics, Janos Seprodi, Andras Szell, Balazs Szoke, Ist- van Teplan, Budapest, Hungary assigned to Reanal Finomvegyszergyar STEROIDS OF THE 20- SPIROXANE SERIES, PROCESSES FOR THE MANUFACTURE THEREOF, PHARMACEUTICAL PREPARATIONS CONTAINING SUCH COMPOUNDS AND THE USE OF THE LATTER Jurgen Grob, Jaroslav Kalvoda, Giebenach, Switzerland assigned to Ciba Geigy Corporation The invention relates to new gonadoliberin derivatives of the formula (I) See Patent for Tabular Presentation PS wherein Y represents a glycine-amide group or an -NH-alkyl group having 1 to 4 carbon atoms in the alkyl moiety, X stands for a D-thyroxyl, D-thyronyl or D-4- chlorophenylalanyl group, and acid addition salts and metal complexes thereof. The new nona- and decapeptide derivatives have an excel- lent luteinizing and folliculus stimulating hor- mone releasing activity, and they can therefore be used as active ingredients in pharmaceutical compositions for human or veterinary applica- tion. X O ~ ' " H _ OII 12 ~ -'CH2--Ctt2--C--R 1, O" ~ : H (II) 4552867 ANTIBIOTIC LL-BO1208 ALPHA AND LL-BO1208 BETA, PROCESS OF PREPARATION, PHARMACEUTICAL COMPOSITION AND METHOD OF USE John H E J Martin, Jane P Kirby, Donald B Borders, Amedeo A Fantini, Raymond T Testa assigned to American Cyanamid Company This invention relates to two new antibacterial and anti-tumor agents designated LL-BO1208 alpha and LL-BO1208 beta produced during microbiological fermentation, under controlled conditions, using the novel microorganism Streptoverticillium stramineum and mutants thereof. (5 alpha)-20-spirox-l-en-3-ones (I) and 17- hydroxy-5 alpha,17 alpha-pregn-l-en-3-ones (II) of the formulae See Patent for Chemical Structure (I) and See Patent for Tabular Pre- sentation (II) in which X represents O or H2, R2 represents O and R I represents OH, OMe, OAlk, NH2, NHR3, NR3R4, or R2 represents H2 and RI represents OH, OAlk, OAr, OAralk or OAc, in which R3, R4 and Alk represent lower alkyl, Me represents a metal atom or metal equivalent or the cation of an organic base, Ar represents monocyclic aryl, Aralk represents monocyclic aryl-lower alkyl, and Ac represents lower alkanoyl, monocyclic aroyl, lower alkylsulphonyl or monocyclic arylsulphonyl, it being possible for R3 together with R4 also to represent a lower alkylene group optionally interrupted by a hetero atom, are manufactured by known analogy processes. They exhibit an aldosterone-antagonistic action and can there- fore be used, for example, as potassium- conserving diuretics, optionally together with another electrolyte-non-specific diuretic or saluretic.

Gonadoliberin derivatives process for the preparation and pharmaceutical compositions thereof

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iv New Patents

4552864 4552871

GONADOLIBERIN DERIVATIVES PROCESS FOR THE PREPARATION AND PHARMACEUTICAL

COMPOSITIONS THEREOF

Ferenc Antoni, Judit Erchegyi, Aniko Keri Gyorg Horvath, Imre Mezo, Karol Nikolics, Janos Seprodi, Andras Szell, Balazs Szoke, Ist- van Teplan, Budapest, Hungary assigned to Reanal Finomvegyszergyar

STEROIDS OF THE 20- SPIROXANE SERIES, PROCESSES

FOR THE MANUFACTURE THEREOF, PHARMACEUTICAL PREPARATIONS CONTAINING SUCH COMPOUNDS AND THE

USE OF THE LATTER

Jurgen Grob, Jaroslav Kalvoda, Giebenach, Switzerland assigned to Ciba Geigy Corporation

The invention relates to new gonadoliberin derivatives of the formula (I) See Patent for Tabular Presentation PS wherein Y represents a glycine-amide group or an -NH-alkyl group having 1 to 4 carbon atoms in the alkyl moiety, X stands for a D-thyroxyl, D-thyronyl or D-4- chlorophenylalanyl group, and acid addition salts and metal complexes thereof. The new nona- and decapeptide derivatives have an excel- lent luteinizing and folliculus stimulating hor- mone releasing activity, and they can therefore be used as active ingredients in pharmaceutical compositions for human or veterinary applica- tion.

X

O ~ ' " H

_ OII 12 ~ -'CH2--Ctt2--C--R 1,

O" ~ : H

(II)

4552867

ANTIBIOTIC LL-BO1208 ALPHA AND LL-BO1208 BETA, PROCESS

OF PREPARATION, PHARMACEUTICAL

COMPOSITION AND METHOD OF USE

John H E J Martin, Jane P Kirby, Donald B Borders, Amedeo A Fantini, Raymond T Testa assigned to American Cyanamid Company

This invention relates to two new antibacterial and anti-tumor agents designated LL-BO1208 alpha and LL-BO1208 beta produced during microbiological fermentation, under controlled conditions, using the novel microorganism Streptoverticillium stramineum and mutants thereof.

(5 alpha)-20-spirox-l-en-3-ones (I) and 17- hydroxy-5 alpha,17 alpha-pregn-l-en-3-ones (II) of the formulae See Patent for Chemical Structure (I) and See Patent for Tabular Pre- sentation (II) in which X represents O or H2, R2 represents O and R I represents OH, OMe, OAlk, NH2, NHR3, NR3R4, or R2 represents H2 and RI represents OH, OAlk, OAr, OAralk or OAc, in which R3, R4 and Alk represent lower alkyl, Me represents a metal atom or metal equivalent or the cation of an organic base, Ar represents monocyclic aryl, Aralk represents monocyclic aryl-lower alkyl, and Ac represents lower alkanoyl, monocyclic aroyl, lower alkylsulphonyl or monocyclic arylsulphonyl, it being possible for R3 together with R4 also to represent a lower alkylene group optionally interrupted by a hetero atom, are manufactured by known analogy processes. They exhibit an aldosterone-antagonistic action and can there- fore be used, for example, as potassium- conserving diuretics, optionally together with another electrolyte-non-specific diuretic or saluretic.