Biogal Gyogyszergyar

Patentbureau Danubia

Gyogyszerkutato Intezet

Eva Toth-Sarudy

Gabor Ambrus

Imre Moravcsik

Gyorgy Cseh

Gyula Horvath

Attila Andor

Istvan Barta

Janos Borvendeg

Janos Erdei

Karoly Albrecht

Valeria Szell

Gyorgy Santha

Antonia Jekkel Nee Bokany

Bela Makadi

Kalman Konczol

Kalman Polya

Lajos Kiss

Karoly Nagy

Eva Tomori Nee Joszt

Bela Palotas

Karoly Buzasi

Etelka Deli Nee Konszky

Aniko Molnar Nee Antal

Vilma Szaszhegyesi

Istvan Mihaly

Agota Hulber Nee Dobos

Gabriella Mezei

The invention relates to a microbial process for the production of immunosuppressive cyclosporine antibiotic complex or of its components, cyclosporine A, cyclosporine B and cyclosporine C, by the aerobic fermentation of a filamentous fungus strain biosynthesizing the above antibiotic(s) in a nutrient medium containing utilizable carbon and nitrogen sources as well as mineral salts, and by isolating the products formed, which comprises culturing a strain of the novel Tolypocladium varium fungus species producing the cyclosporine antibiotic complex, preferably tolypocladium varium sp. nov. CY/93, deposited at the National Collection of Agricultural and Industrial Microorganisms, Budapest, Hungary under the number NCAIM(P)F 001005, on a nutrient medium containing carbon sources, organic and inorganic nitrogen sources as well as mineral salts, under aerobic conditions, at 25.degree. to 30.degree. C., and, if desired, isolating and purifying the cyclosporine antibiotic complex or its components produced.

Microbial process for the production of immunosuppressive antibiotics

The invention relates to new 16-amino-18,19,20-trinor-prostaglandin derivatives of general formula I, having at C-17 a substituted or unsubstituted phenyl group, wherein C-15 and C-16 may have either S or R configuration, Y stands for a hydrogen atom or a lower alkyl group, W stands for a hydrogen atom, halogen atom, hydroxy group, lower alkyl or alkoxy group, and their acid addition salts. These compounds can be prepared by removing the ester group and the p-nitrobenzyloxycarbonyl protective group of a 9.alpha.,11.alpha.,15-trihydroxy-16-p-nitrobenzyloxycarbonylamido-17-pheny l-5-cis,13-trans-18,19,20-trinor-prostadienoic acid derivative of general formula XII--wherein C-15 and C-16 may have either S or R configuration, W is as defined above, and Y stands for a lower alkyl group--in an optional sequence with the limitation that in those compounds of general formula I where W is as defined above and Y stands for a lower alkyl group, solely the p-nitrobenzyloxycarbonyl group is removed, and the resulting product of general formula I is optionally converted with an organic or inorganic acid into a salt. The new prostaglandin derivatives of the invention have valuable therapeutical properties, and can be applied in cattle raising for estrus and birth synchronization, furthermore in the veterinary praxis for the treatment of sterility, chronic endometritis and pyometry.

16-Amino-18,19,20-trinor-prostaglandin derivatives, and acid addition

The invention relates to new 16-amino-prostaglandin derivatives of general formula I, ##STR1## wherein C-15 and C-16 may have either S or R configuration, Z stands for a hydrogen atom or a lower alkyl group, and their acid addition salts. These compounds can be prepared by removing the ester group and the p-nitrocarbobenzyloxy protective group of a 9.alpha., 11.alpha., 15-trihydroxy-16-p-nitrobenzyloxycarbonylamido-5-cis,13-trans-prostadienoi c acid derivative of general formula XII--wherein C-15 and C-16 may have either S or R configuration and Z stands for a lower alkyl group--in an optional sequence with the limitation that in those compounds of general formula I where Z stands for a lower alkyl group solely the p-nitrocarbobenzyloxy group is removed, and the resulting product of general formula I is optionally converted with an organic or inorganic acid into a salt. The new prostaglandin derivatives of the invention have valuable therapeutical properties, and can be applied as abortive or oxytocic agents.

16-Amino-postaglandin derivatives, their acid addition salts, and a

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Budapest, Hungary

Eva Toth-Sarudy